WorldWideScience

Sample records for hydrochloride aminolevulinic acid

  1. Aminolevulinic Acid Topical

    Science.gov (United States)

    ... on or under the skin that result from exposure to sunlight and can develop into skin cancer) of the ... acid will make your skin very sensitive to sunlight (likely to get sunburn). Avoid exposure of treated skin to direct sunlight or bright ...

  2. Accumulation of porphyrins in Propionibacterium acnes by 5-aminolevulinic acid and its esters.

    Science.gov (United States)

    Ogata, Arisa; Hasunuma, Yuya; Kikuchi, Emii; Ishii, Takuya; Ishizuka, Masahiro; Tokuoka, Yoshikazu

    2017-09-01

    We have investigated the accumulation of porphyrins in Propionibacterium acnes (P.acnes) by 5-aminolevulinic acid hydrochloride (ALA) and its esters, ALA methyl ester hydrochloride (mALA), ALA octyl ester hydrochloride (oALA), and ALA benzyl ester hydrochloride (bALA). From the fluorescence spectra of porphyrins accumulated in P.acnes, the order of porphyrin accumulation is as follows: ALA≫mALA≈bALA>oALA (≈0). Moreover, the PDT efficacy is reduced in the order of ALA>mALA≈bALA>oALA (≈without additives). These results confirm that ALA is superior to ALA esters in accumulating porphyrins in P.acnes. Copyright © 2017 Elsevier B.V. All rights reserved.

  3. 5-Aminolevulinic acid-mediated photodynamic therapy for bladder cancer.

    Science.gov (United States)

    Inoue, Keiji

    2017-02-01

    Photodynamic therapy using 5-aminolevulinic acid is a treatment method in which the fluorescent substance of protoporphyrin IX excessively accumulated specifically in cancer cells is excited by visible red or green light irradiation, and reactive oxygen is produced and injures cancer cells. Photodynamic therapy using 5-aminolevulinic acid less markedly influences the surrounding normal cells and tissue as a result of no accumulation of protoporphyrin IX, being a low-invasive, less harmful treatment localized to cancer. Furthermore, photodynamic therapy using 5-aminolevulinic acid is painless, requiring no anesthesia because localized lesions are treated at a low-energy level, and repeatedly applicable, unlike radiotherapy, and so is expected to be a new low-invasive treatment based on a concept completely different from existing treatments. In fact, photodynamic therapy using 5-aminolevulinic acid for bladder cancer was clinically demonstrated mainly for treatment-resistant bladder carcinoma in situ, and favorable outcomes have been obtained. Photodynamic therapy using 5-aminolevulinic acid are photodynamic technologies based on the common biological characteristic of cancers, and are expected as novel therapeutic strategies for many types of cancer. © 2017 The Japanese Urological Association.

  4. Effect of aminolevulinic acid hydrochloride on the acne model of rabbits' ears%盐酸氨基乙酰丙酸搽剂对实验性兔耳痤疮的疗效观察

    Institute of Scientific and Technical Information of China (English)

    张成梅; 武传涛; 尹志圣; 李春令; 于学慧; 王立; 刘兆平

    2011-01-01

    Objective To investigate the therapeutic effect of aminolevulinic acid (ALA) linimentum on exprimental acne of New Zealand rabbits' ears. Methods Thirty-two healthy adult New Zealand rabbits were used in this experiment. Propionibacterium acnes and oleic acid were administrated to the right inner ears (2 cm× 2 cm range) of the rabbits to establish acne models. Then all the animals were randomly divided into 5 groups, ① the model control group:photodynamics therapy(PDT) was given after solvent was applied in the disease region, once per week for 3 weeks, ②the clindamycin metronidazole acne positive control group: clindamycin metronidazole was smeared in the disease region, 3 times/d for 2 weeks, ③ the retinoid positive control group: retinoid was applied in the disease region, 3 times/d for 2 weeks, ④ the ALA single treatment group: ALA was applied in the disease region, once in the first week, ⑤the ALA repeated treatment group: ALA was applied in the disease region, once per week for 3 weeks, and ⑥the normal control group. The animals in the ALA treatment groups and model control group were protected from light for 3 hours after administration, and then ALA photodynamic therapy(ALA-PDT) was given for 15 min/time. After treatment biopsy, and HE staining, microscopic and histological examination were carried out. Results Statistical resuits and biopsy showed that there was a good therapeutic effect on the rabbits' acne models caused by propionibacterium acnes / oleic acid in the ALA-PDT treatment group ( P <0.01 or P <0.05). The effect in the other two positive treatment groups was also obvious ( P < 0.05 ), and the therapeutic effect in the ALA-PDT repeated treatment group was stronger than in the ALA-PDT single treatment group and the two positive drug groups. Conclusion Repeated ALAPDT treatment has good therapeutic effect on rabbits' acne models caused by pwpionibacterium acnes/oleic acid.%目的 研究盐酸氨基乙酰丙酸(ALA)搽剂对新

  5. Efficacy of 5-Aminolevulinic Acid Photodynamic Therapy in treatment of nasal inverted papilloma.

    Science.gov (United States)

    Zhang, Yunjie; Yang, Yuguang; Zou, Xianbiao

    2013-12-01

    Evaluate the efficacy of 5-Aminolevulinic Acid Photodynamic Therapy (PDT) in medical treatment of nasal inverted papilloma (NIP). Three patients with nasal inverted papilloma were treated with 5-Aminolevulinic Acid Photodynamic Therapy at our department from April to September 2012. The efficacy and adverse effects of 5-Aminolevulinic Acid Photodynamic Therapy were evaluated during 6-8 months of follow-up medical examination. After treated with 5-Aminolevulinic Acid Photodynamic Therapy, the nasal inverted papillomas were removed. No recurrence was found during the 6-8 months of follow-up medical examination. The major adverse effects were mild erosion, pain, and exudation. 5-Aminolevulinic Acid Photodynamic Therapy appears to be an effective treatment of nasal inverted papilloma. It can clear the papilloma lesions and is well tolerated by the patients. Copyright © 2013 Elsevier B.V. All rights reserved.

  6. Photodynamic Detection of Peritoneal Metastases Using 5-Aminolevulinic Acid (ALA

    Directory of Open Access Journals (Sweden)

    Yutaka Yonemura

    2017-03-01

    Full Text Available In the past, peritoneal metastasis (PM was considered as a terminal stage of cancer. From the early 1990s, however, a new comprehensive treatment consisting of cytoreductive surgery and perioperative chemotherapy has been established to improve long-term survival for selected patients with PM. Among prognostic indicators after the treatment, completeness of cytoreduction is the most independent predictors of survival. However, peritoneal recurrence is a main cause of recurrence, even after complete cytoreduction. As a cause of peritoneal recurrence, small PM may be overlooked at the time of cytoreductive surgery (CRS, therefore, development of a new method to detect small PM is desired. Recently, photodynamic diagnosis (PDD was developed for detection of PM. The objectives of this review were to evaluate whether PDD using 5-aminolevulinic acid (ALA could improve detection of small PM.

  7. Degradation mechanism and stability of 5-aminolevulinic acid.

    Science.gov (United States)

    Bunke, A; Zerbe, O; Schmid, H; Burmeister, G; Merkle, H P; Gander, B

    2000-10-01

    The physiological substance and precursor of the heme synthesis 5-aminolevulinic acid (ALA) is a promising prodrug for photodiagnosis and photodynamic therapy of epithelial tumors, particularly in urological and gynecological tissues. For the clinical use of this substance, a chemically stable and sterile drug formulation is required. In the present study, degradation mechanism of ALA in aqueous solution and possibilities to improve its stability were examined. A capillary electrophoretic method was developed that was suitable for the quantification of ALA and of two degradation products. The intermediate degradation product was 2, 5-dicarboxyethyl-3,6-dihydropyrazine, which was further oxidized to 2,5-dicarboxyethylpyrazine. The structures of the degradation products were proven by (1)H and (13)C nuclear magnetic resonance spectroscopy. ALA degradation was very efficiently inhibited by adjusting the pH of the aqueous solution to a value market introduction.

  8. Photodynamic therapy with 5-aminolevulinic acid: basic principles and applications

    Science.gov (United States)

    Pottier, Roy H.; Kennedy, James C.

    1996-01-01

    Numerous photosensitizing pigments that absorb visible light and are selectively retained in neoplastic tissue are being investigated as potential photochemotherapeutic agents. While much emphasis is being placed on the synthesis of new, far-red absorbing photosensitizers, an alternative approach has been to stimulate the human body to produce its own natural photosensitizer, namely protoporphyrin IX (PpIX). Exogenous 5-aminolevulinic acid (ALA) is rapidly bioconverted into PP by mitochondria, the process being particularly efficient in tumor cells. Since PpIX has a natural and rapid clearing mechanism (via the capture of iron in the process of being converted into heme), ALA-PDT does not suffer from lingering skin phototoxicity. ALA may be introduced orally, intravenously, or topically, and ALA-PDT has been shown to be effective in the treatment of both malignant and non-malignant lesions.

  9. Delta-aminolevulinic acid dehydratase (ALAD) polymorphism in lead exposed Bangladeshi children and its effect on urinary aminolevulinic acid (ALA)

    Energy Technology Data Exchange (ETDEWEB)

    Tasmin, Saira, E-mail: rimzim1612@yahoo.com [Department of Human Ecology, School of International Health, Graduate School of Medicine, University of Tokyo, 7-3-1 Hongo, Bunkyo-ku, Tokyo 113-0033 (Japan); Furusawa, Hana [Department of Human Ecology, School of International Health, Graduate School of Medicine, University of Tokyo, 7-3-1 Hongo, Bunkyo-ku, Tokyo 113-0033 (Japan); Ahmad, Sk. Akhtar [Department of Occupational and Environmental Health, Bangladesh Institute of Health Sciences, 125/1, Darus Salam, Mirpur, Dhaka 1216 (Bangladesh); Faruquee, M.H. [Department of Public Health, State University of Bangladesh, 77 Satmasjid Road, Dhanmondi, Dhaka 1205 (Bangladesh); Watanabe, Chiho [Department of Human Ecology, School of International Health, Graduate School of Medicine, University of Tokyo, 7-3-1 Hongo, Bunkyo-ku, Tokyo 113-0033 (Japan)

    2015-01-15

    Background and objective: Lead has long been recognized as a harmful environmental pollutant. People in developing countries like Bangladesh still have a higher risk of lead exposure. Previous research has suggested that the delta-aminolevulinic acid dehydratase (ALAD) genotype can modify lead toxicity and individual susceptibility. As children are more susceptible to lead-induced toxicity, this study investigated whether the ALAD genotype influenced urinary excretion of delta-aminolevulinic acid (U-ALA) among children exposed to environmental lead in Bangladesh. Methods: Subjects were elementary schoolchildren from a semi-urban industrialized area in Bangladesh. A total of 222 children were studied. Blood and urine were collected to determine ALAD genotypes, blood lead levels and urinary aminolevulinic acid (U-ALA). Results: The mean BPb level was 9.7 µg/dl for the study children. BPb was significantly positively correlated with hemoglobin (p<0.01). In total, allele frequency for ALAD 1 and 2 was 0.83 and 0.17 respectively. The mean U-ALA concentration was lower in ALAD1-2/2-2 carriers than ALAD1-1 carriers for boys (p=0.001). But for girls, U-ALA did not differ significantly by genotype (p=0.26). When U-ALA was compared by genotype at the same exposure level in a multiple linear regression analysis, boys who were ALAD1-2/2-2 carriers still had a lower level of U-ALA compared to ALAD1-1carriers. Conclusion: This study provides information about the influence of ALAD polymorphism and its association with U-ALA in Bangladeshi children. Our results indicate that the ALAD1-2/2-2 genotype may have a protective effect in terms of U-ALA for environmentally lead exposed boys. - Highlights: • High blood lead level for the environmentally exposed schoolchildren. • BPb was significantly correlated with U-ALA and Hb. • Effect of ALAD genotype on U-ALA is differed by sex. • Lower U-ALA in ALAD2 than ALAD1 carriers only for boys at same exposure.

  10. Biological formation of 5-aminolevulinic acid by photosynthetic bacteria

    Institute of Scientific and Technical Information of China (English)

    LIU Xiu-yan; XU Xiang-yang; MA Qing-lan; WU Wei-hong

    2005-01-01

    In this study, 7 stains of Rhodopseudomonas sp. were selected from 36 photosynthetic bacteria stains storied in our laboratory.Rhodopseudomonas sp. strain 99-28 has the highest 5-aminolevulinic acid(ALA) production ability in these 7 strains. Rhodopseudomonas sp. 99-28 strain was mutated using ultraviolet radiation and a mutant strain L-1, which ALA production is higher than wild strain 99-28 about one times, was obtained. The elements affecting ALA formation of strain 99-28 and L-1 were studied. Under the optimal condition(pH 7.5,supplement of ALA dehydratase(ALAD) inhibitor, levulinic acid(LA) and precursors of ALA synthesis, glycine and succinat, 3000 Ix of light density), ALA formation of mutant L-1 was up to 22.15 mg/L. Strain L-1 was used to treat wastewater to remove CODCr and produce ALA. ALA production was 2.819 my/L, 1.531 rog/L, 2.166 mg/L, and 2.424 mg/L in monosodium glutamate wastewater(MGW),succotash wastewater(SW), brewage wastewater(BW), and citric acid wastewater(CAW) respectively. More than 90% of CODCr was removed in four kinds of wastewater. When LA, glycin and succinate were supplied, ALA production was dramatically increased,however, CODCr could hardly be removed.

  11. Comparative Study of Photodynamic Therapy with Topical Methyl Aminolevulinate versus 5-Aminolevulinic Acid for Facial Actinic Keratosis with Long-Term Follow-Up

    OpenAIRE

    Ko, Dong-Yeob; Kim, Ki-Ho; Song, Ki-Hoon

    2014-01-01

    Background Few studies have compared the efficacy, cosmetic outcomes, and adverse events between 5-aminolevulinic acid photodynamic therapy (ALA-PDT) and methyl aminolevulinate-PDT (MAL-PDT) for actinic keratoses (AKs) in Asian ethnic populations with dark-skin. Objective We retrospectively compared the long-term efficacy, recurrence rates, cosmetic outcomes, and safety of ALA-PDT versus MAL-PDT for facial AKs in Koreans. Methods A total of 222 facial AKs in 58 patients were included in this ...

  12. 21 CFR 182.1047 - Glutamic acid hydrochloride.

    Science.gov (United States)

    2010-04-01

    ... 21 Food and Drugs 3 2010-04-01 2009-04-01 true Glutamic acid hydrochloride. 182.1047 Section 182.1047 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED... Food Substances § 182.1047 Glutamic acid hydrochloride. (a) Product. Glutamic acid hydrochloride....

  13. Pleiotropic effects of 5-aminolevulinic acid in mouse brain.

    Science.gov (United States)

    Lavandera, Jimena; Rodríguez, Jorge; Ruspini, Silvina; Meiss, Roberto; Zuccoli, Johanna Romina; Martínez, María Del Carmen; Gerez, Esther; Batlle, Alcira; Buzaleh, Ana María

    2016-08-01

    5-Aminolevulinic acid (ALA) seems to be responsible for the neuropsychiatric manifestations of acute intermittent porphyria (AIP). Our aim was to study the effect of ALA on the different metabolic pathways in the mouse brain to enhance our knowledge about the action of this heme precursor on the central nervous system. Heme metabolism, the cholinergic system, the defense enzyme system, and nitric oxide metabolism were evaluated in the encephalon of CF-1 mice receiving a single (40 mg/kg body mass) or multiple doses of ALA (40 mg/kg, every 48 h for 14 days). We subsequently found ALA accumulation in the encephalon of the mice. ALA also altered the brain cholinergic system. After one dose of ALA, a decrease in superoxide dismutase activity and a reduction in glutathione levels were detected, whereas malondialdehyde levels and catalase activity were increased. Heme oxygenase was also increased as an antioxidant response to protect the encephalon against injury. All nitric oxide synthase isoforms were induced by ALA, these changes were more significant for the inducible isoform in glial cells. In conclusion, ALA affected several metabolic pathways in mouse encephalon. Data indicate that a rapid response to oxidative stress was developed; however, with long-term intoxication, the redox balance was probably restored, thereby minimizing oxidative damage.

  14. 5-aminolevulinic acid in photodynamic diagnosis and therapy of urological malignancies

    Science.gov (United States)

    Nelius, Thomas; de Riese, Werner T. W.

    2003-06-01

    Completeness and certainty of tumor detection are very important issues in clinical oncology. Recent technological developments in ultrasound, radiologic and magnetic resonance imaging diagnostics are very promising, but could not improve the detection rate of early stage malignancies. One of the most promising new approaches is the use of 5-aminolevulinic acid, a potent photosensitizer, in photodynamic diagnosis and therapy. 5-aminolevulinic acid is meanwhile a well-established tool in the photodynamic diagnosis of bladder cancer. It has been shown to improve the sensitivity of detection of superficial tumors and carcinoma in situ, which enables to reduce the risk of tumor recurrence related to undetected lesions or incomplete transurethral resection of the primary lesions. The use of 5-aminolevulinic acid is steadily expanding in diagnostics of urological malignancies. First clinical results are now reported in detection of urethral and ureteral lesions as well as in urine fluorescence cytology. Furthermore, due to the selective accumulation in transitional cell carcinoma of the bladder, 5-aminolevulinic acid may be an ideal candidate for photodynamic therapy in superficial bladder cancer. Summarizing the data of multiple clinical trials, 5-aminolevulinic acid is a promising agent in photodynamic diagnostics and treatment of superficial bladder cancer.

  15. Photodynamic inactivation of Klebsiella pneumoniae biofilms and planktonic cells by 5-aminolevulinic acid and 5-aminolevulinic acid methyl ester.

    Science.gov (United States)

    Liu, Chengcheng; Zhou, Yingli; Wang, Li; Han, Lei; Lei, Jin'e; Ishaq, Hafiz Muhammad; Nair, Sean P; Xu, Jiru

    2016-04-01

    The treatment of Klebsiella pneumoniae, particularly extended-spectrum β-lactamase (ESBL)-producing K. pneumoniae, is currently a great challenge. Photodynamic antimicrobial chemotherapy is a promising approach for killing antibiotic-resistant bacteria. The aim of this study was to evaluate the capacity of 5-aminolevulinic acid (5-ALA) and its derivative 5-ALA methyl ester (MAL) in the presence of white light to cause photodynamic inactivation (PDI) of K. pneumoniae planktonic and biofilm cells. In the presence of white light, 5-ALA and MAL inactivated planktonic cells in a concentration-dependent manner. Biofilms were also sensitive to 5-ALA and MAL-mediated PDI. The mechanisms by which 5-ALA and MAL caused PDI of ESBL-producing K. pneumonia were also investigated. Exposure of K. pneumonia to light in the presence of either 5-ALA or MAL induced cleavage of genomic DNA and the rapid release of intracellular biopolymers. Intensely denatured cytoplasmic contents and aggregated ribosomes were also detected by transmission electron microscopy. Scanning electron microscopy showed that PDI of biofilms caused aggregated bacteria to detach and that the bacterial cell envelope was damaged. This study provides insights into 5-ALA and MAL-mediated PDI of ESBL-producing K. pneumoniae.

  16. 21 CFR 862.1060 - Delta-aminolevulinic acid test system.

    Science.gov (United States)

    2010-04-01

    ... 21 Food and Drugs 8 2010-04-01 2010-04-01 false Delta-aminolevulinic acid test system. 862.1060 Section 862.1060 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) MEDICAL DEVICES CLINICAL CHEMISTRY AND CLINICAL TOXICOLOGY DEVICES Clinical Chemistry Test...

  17. Photofrin and 5-aminolevulinic acid permeation through oral mucosa in vitro

    Science.gov (United States)

    Flock, Stephen T.; Alleman, Anthony; Lehman, Paul; Blevins, Steve; Stone, Angie; Fink, Louis; Dinehart, Scott; Stern, Scott J.

    1994-07-01

    Photofrin and 5-aminolevulinic acid are photosensitizers that show promise in the photodynamic treatment of cancer, port-wine stains, atherosclerosis and viral lesions. Photofrin is a mixture of porphyrins which, upon the absorption of light, become temporarily cytotoxic. One side-effect associated with the use of Photofrin is long-term cutaneous photosensitivity. It is possible that topical application of this photosensitizing dye will ameliorate such a side-effect. Another way to avoid the cutaneous photosensitivity in photodynamic therapy is to use 5- aminolevulinic acid, which is a porphyrin precursor that causes an increase in the synthesis and concentration of the photosensitizer protoporphyrin IX. 5-aminolevulinic acid is usually applied topically, and so minimizes cutaneous photosensitivity while maximizing the local protoporphyrin concentration. There are a host of disorders in oral mucosa that are potentially treatable by photodynamic therapy. However, since stratum corneum presents an impermeable barrier to many pharmaceuticals, it is not clear that topical application of the photosensitizer will result in a clinically relevant tissue concentration. We have therefore studied the permeation behavior of Photofrin and 5-aminolevulinic acid by applying them to the surface of ex vivo oral mucosa tissue positioned by a Franz diffusion cell. In order to increase the permeability of the photosensitizer across the stratum corneum, we studied the effects of four different drug carriers: phosphate buffered saline, dimethylsulfoxide, ethanol and Azone with isopropyl alcohol.

  18. Reactive oxygen species involved cancer cellular specific 5-aminolevulinic acid uptake in gastric epithelial cells.

    Science.gov (United States)

    Ito, Hiromu; Tamura, Masato; Matsui, Hirofumi; Majima, Hideyuki J; Indo, Hiroko P; Hyodo, Ichinosuke

    2014-03-01

    Photodynamic therapy and photodynamic diagnosis using 5-aminolevulinic acid (ALA) are clinically useful for cancer treatments. Cancer cells have been reported that 5-aminolevulinic acid is incorporated via peptide transporter 1, which is one of the membrane transport proteins, and has been reported to be significantly expressed in various gastrointestinal cancer cells such as Caco-2. However, the mechanism of this protein expression has not been elucidated. Concentration of reactive oxygen species (ROS) is higher in cancer cells in comparison with that of normal cells. We have previously reported that ROS derived from mitochondria is likely related to invasions and proliferations of cancer cells. Since 5-aminolevulinic acid is the most important precursor of heme which is necessary protein for cellular proliferations, mitochondrial ROS (mitROS) may be also related to peptide transporter 1 expressions. In this study, we used a rat gastric mucosal cell line RGM1 and its cancer-like mutated cell line RGK1, and we clarified the ALA uptake mechanism and its relations between mitROS and peptide transporter 1 expression in RGK1. We also used our self-established stable clone of cell which over-expresses manganese superoxide dismutase, a mitROS scavenger. We studied differences of the photodynamic therapy effects in these cells after ALA administrations to clear the influence of mitROS.

  19. Comparative study of trichloroacetic acid vs. photodynamic therapy with topical 5-aminolevulinic acid for actinic keratosis of the scalp.

    Science.gov (United States)

    Di Nuzzo, Sergio; Cortelazzi, Chiara; Boccaletti, Valeria; Zucchi, Alfredo; Conti, Maria Luisa; Montanari, Paola; Feliciani, Claudio; Fabrizi, Giuseppe; Pagliarello, Calogero

    2015-09-01

    Photodynamic therapy with 5-methyl-aminolevulinate and photodynamic therapy with trichloroacetic acid 50% are the two techniques utilized in the management of actinic keratosis. This study was planned to compare the efficacy, adverse effects, recurrence and cosmetic outcome of these option therapies in patients with multiple actinic keratosis of the scalp. Thirteen patients with multiple actinic keratosis were treated with one of the two treatments on half of the scalp at baseline, while the other treatment was performed on the other half 15 days apart, randomly. Efficacy, adverse effects, cosmetic outcome and recurrence were recorded at follow-up visit at 1, 3, 6 and 12 months. Photodynamic therapy with 5 methyl-aminolevulinate was more effective than trichloroacetic acid although less tolerated by patients as it was more painful. Early adverse effects were almost the same even if trichloroacetic acid leads also to crust formation and to a worse cosmetic outcome characterized by hypopigmentation. Recurrence was lower in the area treated with photodynamic therapy. Trichloroacetic acid 50% is less effective than photodynamic therapy with 5 methyl-aminolevulinate in the treatment of multiple actinic keratosis of the scalp although better tolerated by patients. As this technique is less painful and less expensive than photodynamic therapy, we hypothesize and suggest that more sequential treatments could lead to better results. © 2015 John Wiley & Sons A/S. Published by John Wiley & Sons Ltd.

  20. Homology modeling of human γ-butyric acid transporters and the binding of pro-drugs 5-aminolevulinic acid and methyl aminolevulinic acid used in photodynamic therapy.

    Directory of Open Access Journals (Sweden)

    Yan Baglo

    Full Text Available Photodynamic therapy (PDT is a safe and effective method currently used in the treatment of skin cancer. In ALA-based PDT, 5-aminolevulinic acid (ALA, or ALA esters, are used as pro-drugs to induce the formation of the potent photosensitizer protoporphyrin IX (PpIX. Activation of PpIX by light causes the formation of reactive oxygen species (ROS and toxic responses. Studies have indicated that ALA and its methyl ester (MAL are taken up into the cells via γ-butyric acid (GABA transporters (GATs. Uptake via GATs into peripheral sensory nerve endings may also account for one of the few adverse side effects of ALA-based PDT, namely pain. In the present study, homology models of the four human GAT subtypes were constructed using three x-ray crystal structures of the homologous leucine transporter (LeuT as templates. Binding of the native substrate GABA and the possible substrates ALA and MAL was investigated by molecular docking of the ligands into the central putative substrate binding sites in the outward-occluded GAT models. Electrostatic potentials (ESPs of the putative substrate translocation pathway of each subtype were calculated using the outward-open and inward-open homology models. Our results suggested that ALA is a substrate of all four GATs and that MAL is a substrate of GAT-2, GAT-3 and BGT-1. The ESP calculations indicated that differences likely exist in the entry pathway of the transporters (i.e. in outward-open conformations. Such differences may be exploited for development of inhibitors that selectively target specific GAT subtypes and the homology models may hence provide tools for design of therapeutic inhibitors that can be used to reduce ALA-induced pain.

  1. Evidence that isolated developing chloroplasts are capable of synthesizing chlorophyll b from 5-aminolevulinic acid

    Energy Technology Data Exchange (ETDEWEB)

    Huang, Laiqiang; Hoffman, N.E. (Carnegie Institution of Washington, Stanford, CA (USA))

    1990-09-01

    Developing chloroplasts isolated from cucumber (Cucumis sativus L. var Beit Alpha) cotyledons are capable of incorporating ({sup 14}C)5-aminolevulinic acid into chlorophyll (Chl) b and Chl a when incubated under photosynthetic illumination. Thin layer chromatography and high pressure liquid chromatography were employed to analyze the pigments. The specific radioactivity in Chl a was over three times higher than that found in Chl b. Both Chl a and b synthesizing activities in organello decayed rapidly at approximately the same rate. We conclude that concomitant synthesis of Chl a/b-binding apoprotein is not required for Chl b synthesis.

  2. Recent advances in photodynamic diagnosis of gastric cancer using 5-aminolevulinic acid.

    Science.gov (United States)

    Koizumi, Noriaki; Harada, Yoshinori; Minamikawa, Takeo; Tanaka, Hideo; Otsuji, Eigo; Takamatsu, Tetsuro

    2016-01-21

    Photodynamic diagnosis based on 5-aminolevulinic acid-induced protoporphyrin IX has been clinically applied in many fields based upon its evidenced efficacy and adequate safety. In order to establish a personalized medicine approach for treating gastric cancer patients, rapid intraoperative detection of malignant lesions has become important. Feasibility of photodynamic diagnosis using 5-aminolevulinic acid for gastric cancer patients has been investigated, especially for the detection of peritoneal dissemination and lymph node metastasis. This method enables intraoperative real-time fluorescence detection of peritoneal dissemination, exhibiting higher sensitivity than white light observation without histopathological examination. The method also enables detection of metastatic foci within excised lymph nodes, exhibiting a diagnostic accuracy comparable to that of a current molecular diagnostics technique. Although several complicating issues still need to be resolved, such as the effect of tissue autofluorescence and the insufficient depth penetration of excitation light, this simple and rapid method has the potential to become a useful diagnostic tool for gastric cancer, as well as urinary bladder cancer and glioma.

  3. Enhanced 5-aminolevulinic acid-gold nanoparticle conjugate-based photodynamic therapy using pulse laser

    Science.gov (United States)

    Xu, Hao; Yao, Cuiping; Wang, Jing; Chang, Zhennan; Zhang, Zhenxi

    2016-02-01

    The low bioavailability is a crucial limitation for the application of 5-aminolevulinic acid (ALA) in theranostics. In this research, 5-aminolevulinic acid and gold nanoparticle conjugates (ALA-GNPs) were synthesized to improve the bioavailability of ALA and to investigate the impact of ALA photodynamic therapy (ALA-PDT) in Hela cells. A 532 nm pulse laser and light-emitting diode (central wavelengths 502 nm) were jointly used as light sources in PDT research. The results show a 532 nm pulse laser can control ALA release from ALA-GNPs by adjusting the pulse laser dose. This laser control release may be attributed to the heat generation from GNPs under pulse laser irradiation, which indicates accurately adjusting the pulse laser dose to control the drug release in the cell interior can be considered as a new cellular surgery modality. Furthermore, the PDT results in Hela cells indicate the enhancement of ALA release by pulse laser before PDT can promote the efficacy of cell eradication in the light-emitting diode PDT (LED-PDT). This laser mediated drug release system can provide a new online therapy approach in PDT and it can be utilized in the optical monitor technologies based individual theranostics.

  4. The possibility of using 5-aminolevulinic acid in lead phytoextraction process

    Directory of Open Access Journals (Sweden)

    Zbigniew Jarosz

    2013-04-01

    Full Text Available Studies conducted in the greenhouse involving a sunflower (Helianthus annuus L. grown in medium containing 200 mg Pb ∙ dm -3 which were designed to evaluate the impact of foliar nutrition with 5-aminolevulinic acid (5-ALA on the chemical composition of sunflower in reference to possible use of this plant in the process of induced phytoextraction. The study revealed from 4.8% to 34.1% increase in aboveground matter of sunflower which was sprayed by 5-ALA solution at concentrations of 0.01-0.1 ppm in comparison with plants grown in a medium containing 200 mg Pb ∙ dm -3 with no 5-ALA spraying. The sunflower leaves sprayed by 5-ALA solution contained from 3.78% to 27.1% more lead in comparison to plants not sprayed by this agent. As well as remarkable decrease in lead content from 17.4 to 33.4% was recorded in the roots of sunflower sprayed by 5-ALA solution. The lead content in plant shoots was independent from foliar application of 5-aminolevulinic acid

  5. Clinical utility of 5-aminolevulinic acid HCl to better visualize and more completely remove gliomas

    Directory of Open Access Journals (Sweden)

    Halani SH

    2016-09-01

    Full Text Available Sameer H Halani,1 D Cory Adamson1,2 1Department of Neurosurgery, Emory University School of Medicine, Atlanta, GA, USA; 2Neurosurgery Section, Atlanta VA Medical Center, Decatur, GA, USA Abstract: Surgical resection is typically the first line of treatment for gliomas. However, the neurosurgeon faces a major challenge in achieving maximal resection in high-grade gliomas as these infiltrative tumors make it difficult to discern tumor margins from normal brain with conventional white-light microscopy alone. To aid in resection of these infiltrative tumors, fluorescence-guided surgery has gained much popularity in intraoperative visualization of malignant gliomas, with 5-aminolevulinic acid (5-ALA leading the way. First introduced in an article in Neurosurgery, 5-ALA has since become a safe, effective, and inexpensive method to visualize and improve resection of gliomas. This has undoubtedly led to improvements in the clinical course of patients as demonstrated by the increased overall and progression-free survival in patients with such devastating disease. This literature review aims to discuss the major studies and trials demonstrating the clinical utility of 5-ALA and its ability to aid in complete resection of malignant gliomas. Keywords: aminolevulinic acid, 5-ALA, fluorescence, glioblastoma multiforme, high-grade glioma, resection

  6. Comparison of aminolevulinic acid and hexylester aminolevulinate induced protoporphyrin IX fluorescence for the detection of ovarian carcinoma metastases: an experimental study

    Science.gov (United States)

    Ascencio, Manuel; Regis, Claudia; Mordon, Serge; Collinet, Pierre

    2009-06-01

    The present study aimed at comparing the photo detection of peritoneal micrometastases in an ovarian cancer model following administration of two precursors of protoporphyrin IX (PpIX): aminolevulinic acid (ALA) and hexylester aminolevulinate (He-ALA). ALA or He-ALA (100mg/kg) was injected in the peritoneum cavity of 16 rats with induced peritoneal metastases of ovarian cancer. Two hours later, the tumours were visualized laparoscopically using both white light for standard exploration and blue light for fluorescence (D-light, Karl Storz, Tuttlingen, Germany). Peritoneal micrometastases were counted. The distribution of PpIX through the peritoneum was studied on frozen biopsies using fluorescence microscopy and correlated with pathological findings. The number of micrometastases detected by the fluorescence blue mode was significantly higher (pcancer cells. Macroscopically fluorescing nodules were histopathology confirmed as malignant. In conclusion, He-ALA is an excellent precursor for PpIX synthesis giving the highest PpIX fluorescence contrast between normal and tumoral peritoneum. Imaging with He-ALA improves the detection of peritoneal metastases comparing to ALA.

  7. Optical spectroscopy by 5-aminolevulinic acid hexylester induced photodynamic treatment in rat bladder cancer

    Science.gov (United States)

    Larsen, Eivind L. P.; Randeberg, Lise L.; Gederaas, Odrun A.; Arum, Carl-Jørgen; Krokan, Hans E.; Hjelme, Dag R.; Svaasand, Lars O.

    2006-02-01

    Photodynamic therapy (PDT) is a treatment modality which has been shown to be effective for both malignant and non-malignant diseases. New photosensitizers such as 5-aminolevulinic acid hexylester (hALA) may increase the efficiency of PDT. Monitoring of the tissue response provides important information for optimizing factors such as drug and light dose for this treatment modality. Optical spectroscopy may be suited for this task. To test the efficacy of hALA induced PDT, a study on rats with a superficial bladder cancer model, in which a bladder cancer cell line (AY-27) is instilled, will be performed. Preliminary studies have included a PDT feasibility study on rats, fluorescence spectroscopy on AY-27 cell suspensions, and optical reflection and fluorescence spectroscopy in rat bladders in vivo. The results from the preliminary studies are promising, and the study on hALA induced PDT treatment of bladder cancer will be continued.

  8. Utilization of 5-aminolevulinic acid in the photodynamic therapy of tumors: biochemical and photobiological aspects

    Science.gov (United States)

    Pottier, Roy H.; Kennedy, James C.

    1994-03-01

    Inherent in both plants and animals is the natural porphyrin, Protoporphyrin IX (Pp). Although Pp does not appear to have any intrinsic biological activity, it is a potent natural photosensitizer. When activated with ultraviolet or visible light, this photosensitizer can induce significant photodynamic effects on tissues, cells, subcellular elements, and macromolecules via the production of singlet oxygen. The biosynthesis of endogenous Pp is under strict enzymatic control. It is possible to bypass a rate controlling step and induce large, transient concentrations of Pp by the addition of exogenous 5-aminolevulinic acid (ALA). ALA may be administered systemically or topically. Much larger amounts of Pp are produced in certain types of tumor tissue than in adjacent normal tissue. Topically applied ALA can be used to treat a variety of skin lesions, including actinic keratosis, basal cell carcinomas and psoriasis.

  9. Photodynamic diagnosis following intravesical instillation of aminolevulinic acid (ALA): first clinical experiences in urology

    Science.gov (United States)

    Baumgartner, Reinhold; Kriegmair, M.; Stepp, Herbert G.; Lumper, W.; Heil, Peter; Riesenberg, Rainer; Stocker, Susanne; Hofstetter, Alfons G.

    1993-06-01

    Delta Aminolevulinic acid (ALA), a precursor of Protoporphyrin IX (PP IX) in hem biosynthesis has been topically applied in urinary bladders in order to study its potential as fluorescent tumor marker. Preclinical experiments have been performed on chemically induced tumors in rats, revealing a ratio of PP IX-fluorescence intensity up to 20:1 in tumors as compared to healthy urothelium. Synthesis of PP IX has been stimulated in 56 patients by intravesical instillation of a pH-neutral ALA-solution. After an incubation time of two to four hours strong red fluorescence was endoscopically observed even in tiny superficial tumors. Brightness and contrast allows visualization of early stage urothelial diseases with naked eyes and without the necessity suppressing background fluorescence or violet excitation light.

  10. Treatment of actinic cheilitis by photodynamic therapy with 5-aminolevulinic acid and blue light activation.

    Science.gov (United States)

    Zaiac, Martin; Clement, Annabelle

    2011-11-01

    Actinic cheilitis (AC), a common disorder of the lower lip, should be treated early to prevent progression to invasive squamous cell carcinoma. This study evaluated the safety and efficacy of photodynamic therapy (PDT) with 5-aminolevulinic acid (ALA) activated by blue light for the treatment of AC. Fifteen patients with clinically evident or biopsy-proven AC received two treatments with ALA PDT with blue light activation. Treatments were spaced three to five weeks apart. Most patients achieved 65% to 75% clearance three to five weeks after the first treatment and all achieved more than 75% clearance one month after the second treatment. Three patients achieved complete clearance. Pain and burning during irradiation were absent or mild. All patients said they would repeat the procedure. ALA PDT with 417 nm blue light is a promising option for the treatment of AC of the lower lip.

  11. OPTIMIZATIONS FOR 5-AMINOLEVULINIC ACID BASED PHOTODYNAMIC THERAPY IN PURGING LEUKEMIA CELL HL60

    Institute of Scientific and Technical Information of China (English)

    2005-01-01

    Objective To optimize experimental parameters for the photosensitization of 5-aminolevulinic acid (ALA) in promyelocytic leukemia cell HL60 and compare them with normal human peripheral blood mononuclear cell (PBMC). Methods ALA incubation time, wavelength applied to irradiate, concentration of ALA incubated, irradiation fluence may modulate the effect of 5-aminolevulinic acid based Photodynamic Therapy (ALA-PDT).The high-pressure mercury lamps of 400W served as light source, the interference filter of 410nm, 432nm, 545nm, 577nm were used to select the specific wavelength. Fluorescence microscope was used to detect the fluorescence intensity and location of protoporphyrin IX (PpIX) endogenously produced by ALA. MTT assay was used to measure the survival of cell. Flow cytometry with ANNEXIN V FITC kit (contains annexin V FITC, binding buffer and PI) was used to detect the mode of cell death. Results ① 1mmol/L ALA incubated 1×105/mL HL60 cell line for 4 hours, the maximum fluorescence of ALA induced PpIX was detected in cytomembrane. ② Irradiated with 410nm for 14.4J/cm2 can result in the minimum survivability of HL60 cell. ③ The main mode of HL60 cell death caused by ALA-PDT is necrosis. Conclusion ALA for 1mmol/L, 4 hours for dark incubation time, 410nm for irradiation wavelength, 14.4J/cm2 for irradiation fluence were the optimal parameters to selectively eliminate promyelocytic leukemia cell HL60 by ALA based PDT. The photosensitization of ALA based PDT caused the necrosis of HL60 cell, so it could be used for inactivation of certain leukemia cells.

  12. Lead in Missouri Streams: Monitoring Pollution from Mining with an Assay for Erythrocyte [delta]-Aminolevulinic Acid Dehydratase (ALA-D) in Fish Blood

    Data.gov (United States)

    US Fish and Wildlife Service, Department of the Interior — The activity of the erythrocyte enzyme d-aminolevulinic acid dehydratase (ALA-D) has long been used as a biomarker of lead exposure in humans and waterfowl and, more...

  13. Synthesis of imidazol-1-yl-acetic acid hydrochloride: A key intermediate for zoledronic acid

    OpenAIRE

    Singh, Santosh Kumar; Manne, Narendra; Ray, Purna Chandra; Pal, Manojit

    2008-01-01

    A convenient and practical synthesis of imidazol-1-yl-acetic acid hydrochloride was achieved via N-alkylation of imidazole using tert-butyl chloroacetate followed by a non-aqueous ester cleavage of the resulting imidazol-1-yl-acetic acid tert-butyl ester in the presence of titanium tetrachloride. The synthesized imidazol-1-yl-acetic acid hydrochloride was then utilized to prepare zoledronic acid.

  14. Synthesis of imidazol-1-yl-acetic acid hydrochloride: A key intermediate for zoledronic acid

    Science.gov (United States)

    Manne, Narendra; Ray, Purna Chandra

    2008-01-01

    Summary A convenient and practical synthesis of imidazol-1-yl-acetic acid hydrochloride was achieved via N-alkylation of imidazole using tert-butyl chloroacetate followed by a non-aqueous ester cleavage of the resulting imidazol-1-yl-acetic acid tert-butyl ester in the presence of titanium tetrachloride. The synthesized imidazol-1-yl-acetic acid hydrochloride was then utilized to prepare zoledronic acid. PMID:19104672

  15. [Production of 5-aminolevulinic acid from organic industrial wastewater by photosynthetic bacteria].

    Science.gov (United States)

    Xiuyan, Liu; Xiangyang, Xu; Min, Ye; Shuo, Xiang

    2008-09-01

    We used Rhodopseudomonas strains with high-yield of 5-aminolevulinic acid (ALA) to produce ALA from wastewater of producing monosodium glutamate, citric acid, beer, and soybean product. Cultivation was carried out under anaerobic light condition (3000 Lux) at 30 degrees C. For comparison, we tested the addition of levulinic acid (LA), glycin and succinate to the substrate to increase the production of ALA, effect of sterilization of the wastewater for both strains. Cell mass concentration (OD660) and the content of ALA were determined with spectrophotometer. Without adding levulinic acid (LA), glycin and succinate, the growth of strain 99-28 reached plateau after 72-96 h. The maxiam ALA production was obtained at 96 h. Both the yield of ALA and the Chemical Oxygen Demand (CODcr) removal rate of monosodium glutamate waster water were the highest in all tested wasterwaters. When LA, glycin and succinate were added, ALA production of strain 99-28 was significantly increased whereas the CODcr removal was adversely affected. Non-sterial wasterwater slightly reduced the growth and CODcr removal rate of strain 99-28, however the ALA production could be strongly reduced with the addition of LA, glycin and succinate. The growth and CODcr removal of mutant strain L-1 was similar with strain 99-28, but its ALA production was much higher than that of strain 99-28. The Rhodopseudomonas strains screened in our laboratory can use organic wasterwater as substrates to produce ALA and remove CODcr.

  16. In vitro evaluation of 5-aminolevulinic acid (ALA loaded PLGA nanoparticles

    Directory of Open Access Journals (Sweden)

    Shi L

    2013-07-01

    Full Text Available Lei Shi,1 Xiuli Wang,1 Feng Zhao,2 Hansen Luan,2 Qingfeng Tu,1 Zheng Huang,3 Hao Wang,2 Hongwei Wang1,41Shanghai Skin Disease Hospital, Shanghai, People's Republic of China; 2National Pharmaceutical Engineering Research Center, China State Institute of Pharmaceutical Industry, Shanghai, People's Republic of China; 3Ministry of Education (MOE Key Laboratory of OptoElectronic Science and Technology for Medicine, Fujian Normal University, Fuzhou, People's Republic of China; 4Huadong Hospital, Fudan University, Shanghai, People's Republic of ChinaBackground: 5-Aminolevulinic acid (ALA is a prodrug for topical photodynamic therapy. The effectiveness of topical ALA can be limited by its bioavailability. The aim of this study was to develop a novel ALA delivery approach using poly(lactic-co-glycolic acid (PLGA nanoparticles (NPs.Methods: A modified double emulsion solvent evaporation method was used to prepare ALA loaded PLGA NPs (ALA PLGA NPs. The characteristics, uptake, protoporphyrin IX fluorescence kinetics, and cytotoxicity of ALA PLGA NPs toward a human skin squamous cell carcinoma cell line were examined.Results: The mean particle size of spherical ALA PLGA NPs was 65.6 nm ± 26 nm with a polydispersity index of 0.62. The encapsulation efficiency was 65.8% ± 7.2% and ALA loading capacity was 0.62% ± 0.27%. When ALA was dispersed in PLGA NPs, it turned into an amorphous phase. ALA PLGA NPs could be taken up by squamous cell carcinoma cells and localized in the cytoplasm. The protoporphyrin IX fluorescence kinetics and 3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyltetrazolium bromide assay showed that ALA PLGA NPs were more effective than free ALA of the same concentration.Conclusion: PLGA NPs provide a promising ALA delivery strategy for topical ALA-photodynamic therapy of skin squamous cell carcinoma.Keywords: 5-Aminolevulinic acid (ALA, nanoparticles, poly(lactic-co-glycolic acid (PLGA, skin squamous cell carcinoma, photodynamic therapy (PDT

  17. Herbicide clomazone effects on δ-aminolevulinic acid activity and metabolic parameters in Cyprinus carpio.

    Science.gov (United States)

    Menezes, Charlene; Leitemperger, Jossiele; Murussi, Camila; Toni, Cândida; Araújo, Maria do Carmo Santos; Farias, Iria Luiza; Perazzo, Giselle Xavier; Barbosa, Nilda Vargas; Loro, Vania Lucia

    2014-04-01

    The objective of this study was to investigate δ-aminolevulinic acid (δ-ALA-D) activity and metabolic parameters of Cyprinus carpio exposed to clomazone herbicide. Fish were exposed 2.5, 5, 10 and 20 mg L(-1) of clomazone for 192 h. Results indicated that δ-ALA-D activity was decreased in the gills at concentrations of 5 and 10 mg L(-1). Liver glycogen increased, while muscle and gill glycogen levels decreased at 5, 10 and 20 mg L(-1). Glucose was increased in the gills and plasma. Lactate decreased in the gills and liver and increased in the muscle. Protein and amino acids levels increased in the liver and gills and decreased in the muscle. At a clomazone concentration of 20 mg L(-1), ammonia increased in the gills and muscle and decreased in the liver. The results indicated that the metabolic parameters of glycogen, lactate, protein and amino acids in liver, muscle and gills, blood glucose levels, and the enzyme δ-ALA-D in gills may be useful indicators of clomazone toxicity in carp.

  18. Clinical applications of 5-aminolevulinic acid-mediated fluorescence for gastric cancer.

    Science.gov (United States)

    Namikawa, Tsutomu; Yatabe, Tomoaki; Inoue, Keiji; Shuin, Taro; Hanazaki, Kazuhiro

    2015-08-07

    5-aminolevulinic acid (ALA) is a naturally occurring amino acid that is a protoporphyrin IX (PpIX) precursor and a next-generation photosensitive substance. After exogenous administration of ALA, PpIX specifically accumulates in cancer cells owing to the impaired metabolism of ALA to PpIX in mitochondria, which results in a red fluorescence following irradiation with blue light and the formation of singlet oxygen. Fluorescence navigation by photodynamic diagnosis (PDD) using ALA provides good visualization and detection of gastric cancer lesions and is a potentially valuable diagnostic tool for gastric cancer for evaluating both the surgical resection margins and extension of the lesion. Furthermore, PDD using ALA might be used to detect peritoneal metastases during preoperative staging laparoscopy, where it could provide useful information for the selection of a therapeutic approach. Another promising application for this modality is in the evaluation of lymph node metastases. Photodynamic therapy (PDT) using ALA to cause selective damage based on the accumulation of a photosensitizer in malignant tissue is expected to be a non-invasive endoscopic treatment for superficial early gastric cancer. ALA has the potential to be used not only as a diagnostic agent but also as a therapeutic drug, resulting in a new strategy for cancer diagnosis and therapy. Here, we review the current use of PDD and PDT in gastric cancer and evaluate its future potential beyond conventional modalities combined with a light energy upconverter, a light-emitting diode and near-infrared rays as light sources.

  19. 5-Aminolevulinic Acid-Based Sonodynamic Therapy Induces the Apoptosis of Osteosarcoma in Mice.

    Science.gov (United States)

    Li, Yongning; Zhou, Qi; Hu, Zheng; Yang, Bin; Li, Qingsong; Wang, Jianhua; Zheng, Jinhua; Cao, Wenwu

    2015-01-01

    Sonodynamic therapy (SDT) is promising for treatment of cancer, but its effect on osteosarcoma is unclear. This study examined the effect of 5-Aminolevulinic Acid (5-ALA)-based SDT on the growth of implanted osteosarcoma and their potential mechanisms in vivo and in vitro. The dose and metabolism of 5-ALA and ultrasound periods were optimized in a mouse model of induced osteosarcoma and in UMR-106 cells. The effects of ALA-SDT on the proliferation and apoptosis of UMR-106 cells and the growth of implanted osteosarcoma were examined. The levels of mitochondrial membrane potential (ΔψM), ROS production, BcL-2, Bax, p53 and caspase 3 expression in UMR-106 cells were determined. Treatment with 5-ALA for eight hours was optimal for ALA-SDT in the mouse tumor model and treatment with 2 mM 5-ALA for 6 hours and ultrasound (1.0 MHz 2.0 W/cm2) for 7 min were optimal for UMR-106 cells. SDT, but not 5-ALA, alone inhibited the growth of implanted osteosarcoma in mice (Ptreatment with 5-ALA significantly enhanced the SDT-mediated apoptosis (posteosarcoma cells and BcL-2 expression, but increased levels of Bax, p53 and caspase 3 expression in the implanted osteosarcoma tissues (posteosarcoma growth in vivo and reduced UMR-106 cell survival by inducing osteosarcoma cell apoptosis through the ROS-related mitochondrial pathway.

  20. Regulation of ion homeostasis by aminolevulinic acid in salt-stressed wheat seedlings

    Energy Technology Data Exchange (ETDEWEB)

    Türk, Hülya, E-mail: hulyaa.turk@hotmail.com [Biology Department, Science Faculty, Ataturk University, Erzurum (Turkey); East Anatolian High Technology Research and Application Center, Ataturk University, Erzurum (Turkey); Genişel, Mucip, E-mail: m.genisel@hotmail.com [Department of Crop and Animal Production, Vocational High School, Agri (Turkey); Erdal, Serkan, E-mail: serkanerdal25@hotmail.com [Biology Department, Science Faculty, Ataturk University, Erzurum (Turkey)

    2016-04-18

    Salinity is regarded as a worldwide agricultural threat, as it seriously limits plant development and productivity. Salt stress reduces water uptake in plants by disrupting the osmotic balance of soil solution. In addition, it creates a damaged metabolic process by causing ion imbalance in cells. In this study, we aim to examine the negative effects of 5-aminolevulinic acid (ALA) (20 mg/l) on the ion balance in wheat seedling leaves exposed to salt stress (150 mM). Sodium is known to be highly toxic for plant cells at high concentrations, and is significantly increased by salt stress. However, it can be reduced by combined application of ALA and salt, compared to salt application alone. On the other hand, while the K{sup +}/Na{sup +} ratio was reduced by salt stress, ALA application changed this ratio in favor of K{sup +}. Manganese, iron, and copper were also able to reduce stress. However, ALA pre-treatment resulted in mineral level increments. Conversely, the stress-induced rise in magnesium, potassium, calcium, phosphorus, zinc, and molybdenum were further improved by ALA application. These data clearly show that ALA has an important regulatory effect of ion balance in wheat leaves.

  1. 5-Aminolevulinic Acid Fluorescence in High Grade Glioma Surgery: Surgical Outcome, Intraoperative Findings, and Fluorescence Patterns

    Directory of Open Access Journals (Sweden)

    Alessandro Della Puppa

    2014-01-01

    Full Text Available Background. 5-Aminolevulinic acid (5-ALA fluorescence is a validated technique for resection of high grade gliomas (HGG; the aim of this study was to evaluate the surgical outcome and the intraoperative findings in a consecutive series of patients. Methods. Clinical and surgical data from patients affected by HGG who underwent surgery guided by 5-ALA fluorescence at our Department between June 2011 and February 2014 were retrospectively evaluated. Surgical outcome was evaluated by assessing the resection rate as gross total resection (GTR>98% and GTR>90%. We finally stratified data for recurrent surgery, tumor location, tumor size, and tumor grade (IV versus III grade sec. WHO. Results. 94 patients were finally enrolled. Overall GTR>98% and GTR>90% was achieved in 93% and 100% of patients. Extent of resection (GTR>98% was dependent on tumor location, tumor grade (P<0.05, and tumor size (P<0.05. In 43% of patients the boundaries of fluorescent tissue exceeded those of tumoral tissue detected by neuronavigation, more frequently in larger (57% (P<0.01 and recurrent (60% tumors. Conclusions. 5-ALA fluorescence in HGG surgery enables a GTR in 100% of cases even if selection of patients remains a main bias. Recurrent surgery, and location, size, and tumor grade can predict both the surgical outcome and the intraoperative findings.

  2. The effect of iron ion on the specificity of photodynamic therapy with 5-aminolevulinic acid.

    Directory of Open Access Journals (Sweden)

    Maiko Hayashi

    Full Text Available Recently, photodynamic therapy using 5-aminolevulinic acid (ALA-PDT has been widely used in cancer therapy. ALA administration results in tumor-selective accumulation of the photosensitizer protoporphyrin IX (PpIX via the heme biosynthetic pathway. Although ALA-PDT has selectivity for tumor cells, PpIX is accumulated into cultured normal cells to a small extent, causing side effects. The mechanism of tumor-selective PpIX accumulation is not well understood. The purpose of the present study was to identify the mechanism of tumor-selective PpIX accumulation after ALA administration. We focused on mitochondrial labile iron ion, which is the substrate for metabolism of PpIX to heme. We investigated differences in iron metabolism between tumor cells and normal cells and found that the amount of mitochondrial labile iron ion in cancer was lower than that in normal cells. This finding could be because of the lower expression of mitoferrins, which are the mitochondrial iron transporters. Accordingly, we added sodium ferrous citrate (SFC with ALA as a source of iron. As a result, we observed the accumulation of PpIX only in tumor cells, and only these cells showed sensitivity to ALA-PDT. Taken together, these results suggest that the uptake abilities of iron ion into mitochondria play a key role in tumor-selective PpIX accumulation. Using SFC as a source of iron might thus increase the specificity of ALA-PDT effects.

  3. The effect of iron ion on the specificity of photodynamic therapy with 5-aminolevulinic acid.

    Science.gov (United States)

    Hayashi, Maiko; Fukuhara, Hideo; Inoue, Keiji; Shuin, Taro; Hagiya, Yuichiro; Nakajima, Motowo; Tanaka, Tohru; Ogura, Shun-ichiro

    2015-01-01

    Recently, photodynamic therapy using 5-aminolevulinic acid (ALA-PDT) has been widely used in cancer therapy. ALA administration results in tumor-selective accumulation of the photosensitizer protoporphyrin IX (PpIX) via the heme biosynthetic pathway. Although ALA-PDT has selectivity for tumor cells, PpIX is accumulated into cultured normal cells to a small extent, causing side effects. The mechanism of tumor-selective PpIX accumulation is not well understood. The purpose of the present study was to identify the mechanism of tumor-selective PpIX accumulation after ALA administration. We focused on mitochondrial labile iron ion, which is the substrate for metabolism of PpIX to heme. We investigated differences in iron metabolism between tumor cells and normal cells and found that the amount of mitochondrial labile iron ion in cancer was lower than that in normal cells. This finding could be because of the lower expression of mitoferrins, which are the mitochondrial iron transporters. Accordingly, we added sodium ferrous citrate (SFC) with ALA as a source of iron. As a result, we observed the accumulation of PpIX only in tumor cells, and only these cells showed sensitivity to ALA-PDT. Taken together, these results suggest that the uptake abilities of iron ion into mitochondria play a key role in tumor-selective PpIX accumulation. Using SFC as a source of iron might thus increase the specificity of ALA-PDT effects.

  4. Light-induced cytotoxicity after aminolevulinic acid treatment is mediated by heme and not by iron.

    Science.gov (United States)

    Breusing, Nicolle; Grimm, Stefanie; Mvondo, Dagmar; Flaccus, Andrea; Biesalski, Hans Konrad; Grune, Tilman

    2010-04-02

    Photodynamic therapy (PDT) is a promising antitumor treatment strategy. However, effectiveness of PDT is limited due to an initiation of rescue responses in tumor cells, including the induction of heme oxygenase-1 (HO-1). Furthermore, the main sources of free radical production in PDT-induced oxidative stress are not clear. Here, human melanoma cells were loaded with the photosensitizer 5-aminolevulinic acid and exposed to non-thermal light of 420-800 nm at different doses. It was shown that inhibition of HO-1 activity by zinc protoporphyrin IX increased PDT-induced cytotoxicity in a dose-dependent manner. Interestingly, the cytotoxic effects were not diminished by the simultaneous application of the iron chelator desferrioxamine. Importantly, PDT together with non-toxic doses of hemin increased the number of dead cells. From these results can be concluded that heme but not iron act as the main source of free radicals in PDT treatment. This is supported by the fact that during PDT ferritin is readily up-regulated, able to bind excess iron formed by the HO-1 action. The combined treatment of photosensitizers with HO-1 inhibitors might increase the effectiveness of PDT in tumor treatment.

  5. Association between Blood Lead Levels and Delta-Aminolevulinic Acid Dehydratase in Pregnant Women.

    Science.gov (United States)

    La-Llave-León, Osmel; Méndez-Hernández, Edna M; Castellanos-Juárez, Francisco X; Esquivel-Rodríguez, Eloísa; Vázquez-Alaniz, Fernando; Sandoval-Carrillo, Ada; García-Vargas, Gonzalo; Duarte-Sustaita, Jaime; Candelas-Rangel, Jorge L; Salas-Pacheco, José M

    2017-04-18

    Blood lead levels (BLLs) and delta-aminolevulinic acid dehydratase (ALAD) activity are considered biomarkers of lead exposure and lead toxicity, respectively. The present study was designed to investigate the association between BLLs and ALAD activity in pregnant women from Durango, Mexico. A total of 633 pregnant women aged 13-43 years participated in this study. Blood lead was measured by a graphite furnace atomic absorption spectrometer. ALAD activity was measured spectrophotometrically. Mean blood lead was 2.09 ± 2.34 µg/dL; and 26 women (4.1%) crossed the Centers for Disease Control (CDC) recommended level of 5 µg/dL. ALAD activity was significantly lower in women with levels of lead ≥5 µg/dL compared to those with BLLs lead and ALAD activity was observed in the fourth quartile of BLLs (r = -0.113; p lead concentrations ≥2.2 µg/dL ALAD activity was negatively correlated with BLLs (r = -0.413; p lead in blood above 2.2 µg/dL.

  6. Association between Blood Lead Levels and Delta-Aminolevulinic Acid Dehydratase in Pregnant Women

    Directory of Open Access Journals (Sweden)

    Osmel La-Llave-León

    2017-04-01

    Full Text Available Blood lead levels (BLLs and delta-aminolevulinic acid dehydratase (ALAD activity are considered biomarkers of lead exposure and lead toxicity, respectively. The present study was designed to investigate the association between BLLs and ALAD activity in pregnant women from Durango, Mexico. A total of 633 pregnant women aged 13–43 years participated in this study. Blood lead was measured by a graphite furnace atomic absorption spectrometer. ALAD activity was measured spectrophotometrically. Mean blood lead was 2.09 ± 2.34 µg/dL; and 26 women (4.1% crossed the Centers for Disease Control (CDC recommended level of 5 µg/dL. ALAD activity was significantly lower in women with levels of lead ≥5 µg/dL compared to those with BLLs < 5 µg/dL (p = 0.002. To reduce the influence of extreme values on the statistical analysis, BLLs were analyzed by quartiles. A significant negative correlation between blood lead and ALAD activity was observed in the fourth quartile of BLLs (r = −0.113; p < 0.01. Among women with blood lead concentrations ≥2.2 µg/dL ALAD activity was negatively correlated with BLLs (r = −0.413; p < 0.01. Multiple linear regression demonstrated that inhibition of ALAD in pregnant women may occur at levels of lead in blood above 2.2 µg/dL.

  7. δ-Aminolevulinic acid cytotoxic effects on human hepatocarcinoma cell lines

    Directory of Open Access Journals (Sweden)

    del Batlle Alcira M

    2002-03-01

    Full Text Available Abstract Background Acute Intermittent Porphyria is a genetic disorder of heme metabolism, characterized by increased levels of porphyrin precursors, δ-aminolevulinic acid (ALA and porphobilinogen (PBG. ALA has been reported to generate reactive oxygen species and to cause oxidative damage to proteins, subcellular structures and DNA. It is known that oxidative stress can induce apoptosis. The aim of this work was to study the cytotoxic effect of ALA on two hepatocarcinoma cell lines. Results We have determined the impact of ALA on HEP G2 and HEP 3B hepatocarcinoma cell lines survival as measured by the MTT assay. ALA proved to be cytotoxic in both cell lines however; HEP G2 was more sensitive to ALA than HEP 3B. Addition of hemin or glucose diminished ALA cytotoxicity in HEP G2 cells; instead it was enhanced in HEP 3B cells. Because apoptosis is usually associated with DNA fragmentation, the DNA of ALA treated and untreated cells were analyzed. The characteristic pattern of DNA fragmentation ladders was observed in ALA treated cells. To elucidate the mechanisms of ALA induced apoptosis, we examined its effect on p53 expression. No changes in p53 mRNA levels were observed after exposure of both cell lines to ALA for 24 h. CDK2 and CDK4 protein levels were reduced after ALA treatment at physiological concentrations.

  8. Enhanced transdermal delivery of 5-aminolevulinic acid and a dipeptide by iontophoresis.

    Science.gov (United States)

    Krishnan, Gayathri; Roberts, Michael S; Grice, Jeffrey; Anissimov, Yuri G; Benson, Heather A E

    2011-01-01

    Poor skin permeability limits the application of peptides to the skin. Enhanced skin permeation could facilitate the development of new therapies for dermatologic and cosmeceutical applications. The aim of this study was to investigate the application of iontophoresis to the delivery of small peptide model compounds (5-aminolevulinic acid and L-alanine-L-tryptophan) across human skin. Under the conditions tested, iontophoresis increased the in vitro permeability coefficient of ALA.HCl across human epidermis from 7 X 10(-5) cm/h with passive diffusion to 110 x 10(-5) cm/h with iontophoresis. D-Glucose permeation elucidated the iontophoretic electrotransport of ALA.HCl to have contributions of both electrorepulsion and electroosmosis. The L-alanine-L-tryptophan permeability coefficient was increased from 1.5 x 10(-5) cm/h to 35 x 10(-5) cm/h with iontophoretic application. Iontophoretic delivery of the dipeptide increased markedly at lower pH because of an increase in electrorepulsive transport. The study demonstrates that iontophoresis can enhance epidermal permeation of a small peptide and peptide-like drug by up to 15- and 22-fold under the conditions tested.

  9. FERTILIZATION OF VINE BY A 5-AMINOLEVULINIC ACID-BASED FERTILIZER AND ITS PROFITABILITY

    Directory of Open Access Journals (Sweden)

    VLADIMR IMANSK

    2013-03-01

    Full Text Available In this work we investigated the effect of different doses of NPKS fertilizer added into the soil for nutrient contents in the soil, as well as the quantity and quality of grapes. During the vegetation of the vine, we tested the 5-aminolevulinic acid-based fertilizer (ALA. We summarize that higher doses of fertilizer added into soil caused higher amounts of available nutrients. During the vegetation of the vine an increase of ALA had a positive effect on the optimal balance of nutrients. Fertilization also increased the grape-vine yield, with the strongest effect (by 68% observed due to the application of ALA during the vegetation period of the vine. Added fertilizers had a statistically significant influence on decreased sugar concentration in the grape-vine however the addition of fertilizer into the soil, mainly the application of ALA during vegetation of the vine (by 57% had a positive effect on increase of the total content of sugar in the grape-vine, produced on 1 hectare. The year had a significant influence on the economical evaluation.

  10. 5-Aminolevulinic acid-mediated sonosensitization of rat RG2 glioma cells in vitro

    Directory of Open Access Journals (Sweden)

    Krzysztof Bilmin

    2016-10-01

    Full Text Available Sonodynamic therapy (SDT is a promising technique based on the ability of certain substances, called sonosensitizers, to sensitize cancer cells to non-thermal effects of low-energy ultrasound waves, allowing their destruction. Sonosensitization is thought to induce cell death by direct physical effects such as cavitation and acoustical streaming as well as by complementary chemical reactions generating oxygen free radicals. One of the promising sonosensitizers is 5-aminolevulinic acid (ALA which upon selective uptake by cancer cells is metabolized and accumulated as protoporphyrin IX. The objective of the study was to describe ALA-mediated sonodynamic effects in vitro on a rat RG2 glioma cell line. Glioma cells, seeded at the bottom of 96-well plates and incubated with ALA (10 µg/ml for 6 h, were exposed to the sinusoidal US pulses with a resonance frequency of 1 MHz, 1000 µs duration, 0.4 duty-cycle, and average acoustic power varying from 2 W to 6 W. Ultrasound waves were generated by a flat circular piezoelectric transducer with a diameter of 25 mm. Cell viability was determined by MTT assay. Structural cellular changes were visualized with a fluorescence microscope. Signs of cytotoxicity such as a decrease in cell viability, chromatin condensation and apoptosis were found. ALA-mediated SDT evokes cytotoxic effects of low intensity US on rat RG2 glioma cells in vitro . This cell line is indicated for further preclinical assessment of SDT in in vivo conditions.

  11. 5-Aminolevulinic acid-mediated sonosensitization of rat RG2 glioma cells in vitro.

    Science.gov (United States)

    Bilmin, K; Kujawska, T; Secomski, W; Nowicki, A; Grieb, P

    2016-01-01

    Sonodynamic therapy (SDT) is a promising technique based on the ability of certain substances, called sonosensitizers, to sensitize cancer cells to non-thermal effects of low-energy ultrasound waves, allowing their destruction. Sonosensitization is thought to induce cell death by direct physical effects such as cavitation and acoustical streaming as well as by complementary chemical reactions generating oxygen free radicals. One of the promising sonosensitizers is 5-aminolevulinic acid (ALA) which upon selective uptake by cancer cells is metabolized and accumulated as protoporphyrin IX. The objective of the study was to describe ALA-mediated sonodynamic effects in vitro on a rat RG2 glioma cell line. Glioma cells, seeded at the bottom of 96-well plates and incubated with ALA (10 µg/ml) for 6 h, were exposed to the sinusoidal US pulses with a resonance frequency of 1 MHz, 1000 µs duration, 0.4 duty-cycle, and average acoustic power varying from 2 W to 6 W. Ultrasound waves were generated by a flat circular piezoelectric transducer with a diameter of 25 mm. Cell viability was determined by MTT assay. Structural cellular changes were visualized with a fluorescence microscope. Signs of cytotoxicity such as a decrease in cell viability, chromatin condensation and apoptosis were found. ALA-mediated SDT evokes cytotoxic effects of low intensity US on rat RG2 glioma cells in vitro. This cell line is indicated for further preclinical assessment of SDT in in vivo conditions.

  12. Regulation of ion homeostasis by aminolevulinic acid in salt-stressed wheat seedlings

    Science.gov (United States)

    Türk, Hülya; Genişel, Mucip; Erdal, Serkan

    2016-04-01

    Salinity is regarded as a worldwide agricultural threat, as it seriously limits plant development and productivity. Salt stress reduces water uptake in plants by disrupting the osmotic balance of soil solution. In addition, it creates a damaged metabolic process by causing ion imbalance in cells. In this study, we aim to examine the negative effects of 5-aminolevulinic acid (ALA) (20 mg/l) on the ion balance in wheat seedling leaves exposed to salt stress (150 mM). Sodium is known to be highly toxic for plant cells at high concentrations, and is significantly increased by salt stress. However, it can be reduced by combined application of ALA and salt, compared to salt application alone. On the other hand, while the K+/Na+ ratio was reduced by salt stress, ALA application changed this ratio in favor of K+. Manganese, iron, and copper were also able to reduce stress. However, ALA pre-treatment resulted in mineral level increments. Conversely, the stress-induced rise in magnesium, potassium, calcium, phosphorus, zinc, and molybdenum were further improved by ALA application. These data clearly show that ALA has an important regulatory effect of ion balance in wheat leaves.

  13. Dietary supplementation with 5-aminolevulinic acid modulates growth performance and inflammatory responses in broiler chickens.

    Science.gov (United States)

    Sato, K; Matsushita, K; Takahashi, K; Aoki, M; Fuziwara, J; Miyanari, S; Kamada, T

    2012-07-01

    The objective of this study was to investigate the effect of dietary supplementation with 5-aminolevulinic acid (5-ALA) on the immune system, inflammatory response, and growth performance of broiler chickens. The levels of cluster of differentiation 3 (CD3) mRNA in the spleens of chickens gradually increased with dietary 5-ALA concentration, while the expression levels of interleukin (IL)-2 decreased. Mitogen-induced proliferation of splenic mononuclear cells and blood mononuclear cell phagocytosis in chickens fed 0.001 and 0.01% 5-ALA-supplemented diets were significantly greater than in chickens fed a basal diet (control). Plasma thiobarbituric acid reactive substance (TBARS) concentration gradually increased along with 5-ALA supplement concentration. These results provide the first evidence that the use of dietary 0.001 and 0.01% 5-ALA supplementation induces the T-cell immune system via mild oxidative stress in chickens. Three hours after Escherichia coli lipopolysaccharide-induced immune stimulation, the levels of mRNA encoding pro-inflammatory cytokines, such as IL-6 and tumor necrosis factor-like ligand 1A (TL1A), in chickens fed a 0.001% 5-ALA-supplemented diet were significantly lower than those in chickens exposed to other treatments. The plasma caeruloplasmin concentration in chickens fed a 0.001% 5-ALA-supplemented diet was significantly lower than in controls or in chickens fed diets supplemented with other concentrations of 5-ALA 24 h after injection of LPS. In addition, BW at 21 and 50 d of age was significantly higher in chickens fed a 0.001% 5-ALA-supplemented diet than in control chickens. The findings suggest that supplementation of diets with 0.001% 5-ALA could prevent the catabolic changes induced by immunological stimulation. These results show that 5-ALA might be useful as an immunomodulator to stimulate T-cells via mild oxidative stress in growing broiler chickens, thereby improving the growth performance.

  14. Photodynamic therapy using systemic administration of 5-aminolevulinic acid and a 410-nm wavelength light-emitting diode for methicillin-resistant Staphylococcus aureus-infected ulcers in mice.

    Science.gov (United States)

    Morimoto, Kuniyuki; Ozawa, Toshiyuki; Awazu, Kunio; Ito, Nobuhisa; Honda, Norihiro; Matsumoto, Sohkichi; Tsuruta, Daisuke

    2014-01-01

    Bacterial resistance to antibiotics has become a worldwide problem. One potential alternative for bacterial control is photodynamic therapy. 5-aminolevulinic acid is a natural precursor of the photosensitizer protoporphyrin IX. Relatively little is known about the antibacterial efficacy of photodynamic therapy using the systemic administration of 5-aminolevulinic acid; a few reports have shown that 5-aminolevulinic acid exerts photodynamic effects on methicillin-resistant Staphylococcus aureus (MRSA) in vitro. In this study, we evaluated the effectiveness of photodynamic therapy using 5-aminolevulinic acid and a 410-nm wavelength light-emitting diode in vitro and in vivo for the treatment of MRSA. We found that 5-aminolevulinic acid photodynamic therapy with the light-emitting diode had an in-vitro bactericidal effect on MRSA. In vivo, protoporphyrin IX successfully accumulated in MRSA on ulcer surfaces after intraperitoneal administration of 5-aminolevulinic acid to mice. Furthermore, 5-aminolevulinic acid photodynamic therapy accelerated wound healing and decreased bacterial counts on ulcer surfaces; in contrast, vancomycin treatment did not accelerate wound healing. Our findings indicate that 5-aminolevulinic acid photodynamic therapy may be a new treatment option for MRSA-infected wounds.

  15. Effects of 5-aminolevulinic acid-mediated sonodynamic therapy on macrophages

    Directory of Open Access Journals (Sweden)

    Cheng J

    2013-02-01

    Full Text Available Jiali Cheng,1,* Xin Sun,1,2,* Shuyuan Guo,1,* Wei Cao,1 Haibo Chen,1 Yinghua Jin,1 Bo Li,1 Qiannan Li,1 Huan Wang,1 Zhu Wang,3 Qi Zhou,3 Peng Wang,3 Zhiguo Zhang,3 Wenwu Cao,3,4 Ye Tian1,21Division of Cardiology, the First Affiliated Hospital, Cardiovascular Institute, Harbin Medical University, Harbin, People’s Republic of China; 2Division of Pathophysiology, the State-Province Key Laboratories of Biomedicine-Pharmaceutics of China, Key Laboratory of Cardiovascular Research, Ministry of Education, Harbin, People’s Republic of China; 3Laboratory of Photo- and Sono-theranostic Technologies and Condensed Matter Science and Technology Institute, Harbin Institute of Technology, Harbin, People’s Republic of China; 4Materials Research Institute, The Pennsylvania State University, University Park, PA, USA*These authors contributed equally to this workBackground: Inflammatory cells exhibit an elevated level of protoporphyrin IX (PpIX after the administration of 5-aminolevulinic acid (ALA. Here, we investigate the sonodynamic effects of ALA-derived PpIX (ALA-PpIX on macrophages, which are the pivotal inflammatory cells in atherosclerosis.Methods and results: Cultured THP-1 macrophages were incubated with ALA. Fluorescence microscope and fluorescence spectrometer detection showed that intracellular PpIX increased with the concentration of ALA in the incubation solution in a time dependent manner; the highest level of intracellular PpIX was observed after 3-hour incubation. 3-[4,5-dimethylthiazol-2-yl]-2,5-diphenyltetrazolium bromide assays demonstrated that lower concentrations (less than 2 mM of ALA have no influence on cell viability (more than 90% of cells survived, but sonodynamic therapy (SDT with a low concentration of ALA significantly decreased the survival rate of cells, and the effect was increased with both ALA concentration and ultrasound exposure time. Cell apoptosis and necrosis induced by ALA-mediated SDT (ALA-SDT were measured using

  16. Alleviation of salt-induced oxidative damage by 5-aminolevulinic acid in wheat seedlings

    Science.gov (United States)

    Genişel, Mucip; Erdal, Serkan

    2016-04-01

    The aim of this study was to elucidate how 5-aminolevulinic acid (ALA), the precursor of chlorophyll compounds, affects the defence mechanisms of wheat seedlings induced by salt stress. To determine the possible stimulative effects of ALA against salinity, 11-day old wheat seedlings were sprayed with ALA at two different concentrations (10 and 20 mg.l-1) and then stressed by exposure to salt (150 mM NaCl). The salt stress led to significant changes in the antioxidant activity. While guaiacol peroxidase activity decreased, the activities of superoxide dismutase, catalase, and ascorbate peroxidase markedly increased under salt stress. Compared to the salt stress alone, the application of ALA beforehand further increased the activity of these enzymes. This study is the first time the effects of ALA have been monitored with regard to protein content and the isoenzyme profiles of the antioxidant enzymes. Although the salt stress reduced both the soluble protein content and protein band intensities, pre-treating with ALA significantly mitigated these stress-induced reductions. The data for the isoenzyme profiles of the antioxidant enzymes paralleled that of the ALA-induced increases in antioxidant activity. As a consequence of the high antioxidant activity in the seedlings pre-treated with ALA, the stress-induced elevations in the reactive oxygen species, superoxide anion, and hydrogen peroxide contents and lipid peroxidation levels were markedly diminished. Taken together, this data demonstrated that pre-treating with ALA confers resistance to salt stress by modulating the protein synthesis and antioxidant activity in wheat seedlings.

  17. Aminolevulinic Acid-Mediated Photodynamic Therapy Causes Cell Death in MG-63 Human Osteosarcoma Cells.

    Science.gov (United States)

    White, Bradley; Rossi, Vince; Baugher, Paige J

    2016-09-01

    The aim of this study was to test the efficacy of aminolevulinic acid-mediated photodynamic therapy (PDT) against the human osteosarcoma cell line MG-63. Osteosarcoma is the most common type of primary malignant bone tumor diagnosed in the United States among adolescents and children. Treatments for osteosarcoma often result in diminished limb use or amputation. Because ALA-mediated PDT exhibits dual specificity in the context of tumor killing, this therapy could represent a less invasive, but effective, treatment for this disease. To assess ALA dark toxicity in MG-63 cells, cells were incubated with varying concentrations of ALA, and cell viability was determined by crystal violet assay. Protoporphyrin IX (PpIX) accumulation was assessed subsequent to ALA incubation at various concentrations using spectrofluorometry. Cell death subsequent to ALA-PDT was determined by illuminating cells at a wavelength of 635 nm at various light intensities subsequent to ALA incubation. Cell viability was assessed using the MTT assay. ALA dark toxicity was observed only at the highest concentrations of 2, 5, and 10 mM. Maximal PpIX concentration was observed at 0.5 and 1 mM ALA, subsequent to a 24-h incubation. Maximal cell death with minimal light toxicity was observed at 0.5 and 1 mM ALA after illumination with 0.6 and 3 J/cm(2) light. Collectively, our data indicate that ALA-PDT can result in the death of MG-64 human osteosarcoma cells in vitro.

  18. Interference with the Jaffé Method for Creatinine Following 5-Aminolevulinic Acid Administration

    Science.gov (United States)

    Quon, Harry; Grossman, Craig E.; King, Rebecca L.; Putt, Mary; Donaldson, Keri; Kricka, Larry; Finlay, Jarod; Malloy, Kelly; Cengel, Keith A.; Busch, Theresa M.

    2013-01-01

    Background The photosensitizer pro-drug 5-aminolevulinic acid (5-ALA) has been administered systemically for photodynamic therapy. Although several toxicities have been reported, nephrotoxicity has never been observed. Materials and Methods Patients with head and neck mucosal dysplasia have been treated on a phase 1 study of escalating light doses in combination with 60 mg/kg of oral 5-ALA. Serum creatinine was measured with the modified Jaffe method or an enzymatic method in the first 24 hours after 5-ALA. Interference by 5-ALA, as well as by its photosensitizing product protoporphyrin IX, was assessed. Results Among 11 subjects enrolled to date, 9 of 11 had blood chemistries collected within the first 5 hours with 7 demonstrating significant grade 3 creatinine elevations (p=0.030). There was no additional evidence of compromised renal function or increased PDT-induced mucositis. Creatinine levels measured by the Jaffe assay increased linearly as a function of the ex-vivo addition of ALA (p<.0001). The exogenous addition of PpIX did not alter creatinine levels. ALA did not interfere with creatinine levels as measured by an enzymatic assay. A total of 4 of the 11 subjects had creatinine levels prospectively measured by both the Jaffe and the enzymatic assays. Only the Jaffe method demonstrated significant elevations as a function of time after ALA administration. Conclusions The transient increase in creatinine after systematic ALA can be attributed, in part, if not entirely, to interference of ALA in the Jaffe reaction. Alternative assays should be employed in situations calling for monitoring of kidney function after systemic ALA. PMID:21112550

  19. 5-Aminolevulinic acid induced photodynamic inactivation on Staphylococcus aureus and Pseudomonas aeruginosa

    Directory of Open Access Journals (Sweden)

    Chien-Ming Hsieh

    2014-09-01

    Full Text Available The aim of the present study was to develop a simple and fast screening technique to directly evaluate the bactericidal effects of 5-aminolevulinic acid (ALA-mediated photodynamic inactivation (PDI and to determine the optimal antibacterial conditions of ALA concentrations and the total dosage of light in vitro. The effects of PDI on Staphylococcus aureus and Pseudomonas aeruginosa in the presence of various concentrations of ALA (1.0 mM, 2.5 mM, 5.0 mM, 10.0 mM were examined. All bacterial strains were exponentially grown in the culture medium at room temperature in the dark for 60 minutes and subsequently irradiated with 630 ± 5 nm using a light-emitting diode (LED red light device for accumulating the light doses up to 216 J/cm2. Both bacterial species were susceptible to the ALA-induced PDI. Photosensitization using 1.0 mM ALA with 162 J/cm2 light dose was able to completely reduce the viable counts of S. aureus. A significant decrease in the bacterial viabilities was observed for P. aeruginosa, where 5.0 mM ALA was photosensitized by accumulating the light dose of 162 J/cm2. We demonstrated that the use of microplate-based assays—by measuring the apparent optical density of bacterial colonies at 595 nm—was able to provide a simple and reliable approach for quickly choosing the parameters of ALA-mediated PDI in the cell suspensions.

  20. Stability of ranitidine hydrochloride and amino acids in parenteral nutrient solutions.

    Science.gov (United States)

    Bullock, L; Parks, R B; Lampasona, V; Mullins, R E

    1985-12-01

    The stability of ranitidine hydrochloride in parenteral nutrient (PN) solutions and the effect of ranitidine hydrochloride on the amino acids in the PN solutions were studied. Six PN solutions (three each with amino acid contents of 2.125 and 4.25%) were prepared. Each PN solution also contained dextrose 25%, electrolytes, trace elements, vitamins, and heparin sodium. Ranitidine hydrochloride injection was added to four of the PN samples. Of the final samples, two contained no ranitidine, two contained ranitidine hydrochloride 50 micrograms/mL, and two contained ranitidine hydrochloride 100 micrograms/mL. Admixtures of ranitidine hydrochloride at the two concentrations in 0.9% sodium chloride injection were also prepared. Samples were observed for color change and tested for pH during storage at room temperature. Concentrations of amino acids were measured after 24 hours in samples without ranitidine and in samples containing ranitidine hydrochloride 100 micrograms/mL. Ranitidine hydrochloride content was determined by high-performance liquid chromatography at 12, 24, and 48 hours. No visual changes or pH changes occurred by 24 hours. All PN solutions became darker by 48 hours. The presence of ranitidine hydrochloride did not substantially affect amino acid concentrations. At 24 hours, at least 90% of the initial ranitidine concentrations remained in all samples. In three of the four PN samples at 48 hours, less than 90% of initial ranitidine concentrations remained. Ranitidine hydrochloride in concentrations of 50 and 100 micrograms/mL in parenteral nutrient solutions containing 4.25 and 2.125% crystalline amino acids is stable for 24 hours at room temperature. Under these conditions, concentrations of the amino acids contained in the PN solutions were not affected by the addition of ranitidine hydrochloride.

  1. 5-Aminolevulinic Acid-Based Sonodynamic Therapy Induces the Apoptosis of Osteosarcoma in Mice.

    Directory of Open Access Journals (Sweden)

    Yongning Li

    Full Text Available Sonodynamic therapy (SDT is promising for treatment of cancer, but its effect on osteosarcoma is unclear. This study examined the effect of 5-Aminolevulinic Acid (5-ALA-based SDT on the growth of implanted osteosarcoma and their potential mechanisms in vivo and in vitro.The dose and metabolism of 5-ALA and ultrasound periods were optimized in a mouse model of induced osteosarcoma and in UMR-106 cells. The effects of ALA-SDT on the proliferation and apoptosis of UMR-106 cells and the growth of implanted osteosarcoma were examined. The levels of mitochondrial membrane potential (ΔψM, ROS production, BcL-2, Bax, p53 and caspase 3 expression in UMR-106 cells were determined.Treatment with 5-ALA for eight hours was optimal for ALA-SDT in the mouse tumor model and treatment with 2 mM 5-ALA for 6 hours and ultrasound (1.0 MHz 2.0 W/cm2 for 7 min were optimal for UMR-106 cells. SDT, but not 5-ALA, alone inhibited the growth of implanted osteosarcoma in mice (P<0.01 and reduced the viability of UMR-106 cells (p<0.05. ALA-SDT further reduced the tumor volumes and viability of UMR-106 cells (p<0.01 for both. Pre-treatment with 5-ALA significantly enhanced the SDT-mediated apoptosis (p<0.01 and morphological changes. Furthermore, ALA-SDT significantly reduced the levels of ΔψM, but increased levels of ROS in UMR-106 cells (p<0.05 or p<0.01 vs. the Control or the Ultrasound. Moreover, ALA-SDT inhibited the proliferation of osteosarcoma cells and BcL-2 expression, but increased levels of Bax, p53 and caspase 3 expression in the implanted osteosarcoma tissues (p<0.05 or p<0.01 vs. the Control or the Ultrasound.The ALA-SDT significantly inhibited osteosarcoma growth in vivo and reduced UMR-106 cell survival by inducing osteosarcoma cell apoptosis through the ROS-related mitochondrial pathway.

  2. 5-Aminolevulinic acid-mediated photodynamic therapy for oral cancers and precancers

    Directory of Open Access Journals (Sweden)

    Hsin-Ming Chen

    2012-12-01

    Full Text Available Previous studies have used both systemic and topical 5-aminolevulinic acid (ALA-mediated photodynamic therapy (PDT to treat oral precancers including oral leukoplakia (OL, oral erythroleukoplakia (OEL, and oral verrucous hyperplasia (OVH as well as oral cancers including oral verrucous carcinoma (OVC and oral squamous cell carcinoma (OSCC. Systemic ALA-PDT has been used to treat oral dysplastic lesions and oral cancers with promising clinical outcomes. The efficacy of a regular topical ALA-PDT (fluence rate, 100 mW/cm2; light dose, 100 J/cm2 was tested on an extensive buccal OVC and an enhanced topical ALA-PDT (fluence rate, 200 mW/cm2; light dose, 200 J/cm2 on an early-invasive OSCC; complete regression of the carcinomas was demonstrated after 28 and 18 PDT treatments, respectively. Several previous studies showed relatively good outcomes for OL lesions treated with topical ALA-PDT. However, it was found that the regular topical ALA-PDT is very effective for OVH and OEL lesions but less so for OL lesions. Better PDT outcomes are significantly associated with OVH and OEL lesions with smaller size, pink to red color, epithelial dysplasia, or thinner surface keratin layer. Moreover, the thicker surface keratin layer on the OL lesions is responsible for the relatively poorer PDT outcomes for OL lesions. In addition, both light emitting diode light- and laser light-mediated topical ALA-PDTs are comparative treatment modalities for OVH and OEL lesions. Methotrexate- or vitamin D3-preconditioned prostate or skin carcinoma cells can accumulate more intracellular protoporphyrin IX, resulting in an increased killing of these preconditioned cells by subsequent ALA-PDT. Because chemotherapy can help destroy carcinoma cells and tumor-associated vasculatures and cryotherapy pretreatment may help the diffusion of ALA into lesional epithelial cells, the chemotherapy or cryotherapy-combined topical ALA-PDT may be a new effective PDT alternative for

  3. Evaluation of the risk of liver damage from the use of 5-aminolevulinic acid for intra-operative identification and resection in patients with malignant gliomas

    DEFF Research Database (Denmark)

    Offersen, Cecilie Mørck; Skjoeth-Rasmussen, Jane

    2017-01-01

    BACKGROUND: The clinical efficacy of 5-aminolevulinic acid (5-ALA) for fluorescence-guided surgery of malignant gliomas is evident from several studies; however, as post-operative elevations of liver enzymes have been seen, there is a potential risk of liver damage upon administration. The aim of...

  4. Applications of 5-aminolevulinic acid on the physiological and biochemical characteristics of strawberry fruit during postharvest cold storage

    Directory of Open Access Journals (Sweden)

    Yi Li

    Full Text Available ABSTRACT: The compound 5-aminolevulinic acid (ALA is a key precursor in the biosynthesis of porphyrins, such as chlorophyll, heme and phytochromobilin, and has multiple physiological effects on plants. Varying concentrations of ALA (50mg L-1, 100mg L-1, and 150mg L-1 and water (control were applied to white stage 'Sweet Charlie' strawberry fruit. All ALA treatments delayed senescence and improved the qualities of strawberries fruit during storage. Among the treatments, 150mg L-1 ALA was the most effective dosage concentration. Exogenously applied ALA significantly reduced the decay index, respiration rate, O2 - production rate (O2 -, H2O2 and malondialdehyde (MDA content, increased superoxide dismutase (SOD, ascorbate peroxidase activities (APX, total soluble solids (TSS content, titratable acidity (TA and anthocyanin content during the initial stage of storage. These results supported the pre harvest application of ALA as a beneficial strategy for the prevention of postharvest decay of strawberry fruit.

  5. Biosynthesis of 1-aminocyclopropane-1-carboxylic acid and ethylene from delta-aminolevulinic acid in ripening tomato fruits

    Energy Technology Data Exchange (ETDEWEB)

    El-Rayes, D.E.D.A.

    1987-01-01

    A new pathway for ethylene (C/sub 2/H/sub 4/) biosynthesis, which utilizes delta-aminolevulinic acid (ALA) as a precursor of 1-aminocyclopropane-1-carboxylic acid (ACC), the immediate precursor of C/sub 2/H/sub 4/, is presented. ALA enhanced ACC accumulation to 410% and C/sub 2/H/sub 4/ production to 232% of the control. The C/sub 2/H/sub 4/ production rate varied with the ALA concentration and the stage of tomato fruit development. As the ALA concentration increased from zero to 40 mM, the C/sub 2/H/sub 4/ production rate increased. Both treated and untreated pericarp discs from fruits at the pink stage of development yielded the largest C/sub 2/H/sub 4/ production rate. Radioactivity from (2,3-/sup 3/H)ALA was detected in both ACC and C/sub 2/H/sub 4/, and radioactivity from (4-/sup 14/C)ALA was detected in ACC and CO/sub 2/ but not in C/sub 2/H/sub 4/. However, radioactivity from (5-/sup 14/C)ALA was detected in CO/sub 2/, and its amount was greater than that obtained from (4-/sup 14/C)ALA. Neither ACC nor C/sub 2/H/sub 4/ showed any radioactivity when (5-/sup 14/C)ALA was supplied to the fruit discs. In addition, when (2,3-/sup 3/H)ALA or (4-/sup 14/C)ALA was supplied to the fruit discs, radioactivity was detected in other metabolites such as fumarate, succinate, malate, glutamate, glutamine, ..cap alpha..-ketoglutarate, and methionine, but the amount of radioactivity was insignificant as compared with the amount of radioactivity found in C/sub 2/H/sub 4/ and ACC.

  6. New proposal for the treatment of viral warts with intralesional injection of 5-aminolevulinic acid photodynamic therapy.

    Science.gov (United States)

    Kim, Jung Eun; Kim, Sun Ji; Hwang, Jong Ik; Lee, Kyung Jin; Park, Hyun Jeong; Cho, Baik Kee

    2012-06-01

    Although photodynamic therapy (PDT) using intralesional injection (ILI) can theoretically enhance the efficacy of the PDT, the effect of ILI-PDT on warts has not been reported in the literature so far. Eight patients with multiple viral warts were enrolled in the study. PDT was performed after the incubation for 1 h, followed by the ILI of aminolevulinic acid (ALA) into the warts. The treatment was repeated at 2-3 week intervals. Fifty percent of patients showed good to cure response. Complete remission was observed in two patients. There was no apparent correlation between the initial severity of warts and the likelihood of response. No one reported severe adverse reaction. The present study suggests that intralesional administration of ALA might be a safe and effective treatment option of thick treatment-resistant warts and can be performed with a shorter incubation period.

  7. Comparison of blood lead and blood and plasma δ-aminolevulinic acid concentrations as biomarkers for lead poisoning in cattle.

    Science.gov (United States)

    Kang, Hwan Goo; Bischoff, Karyn; Ebel, Joseph G; Cha, Sang Ho; McCardle, James; Choi, Cheong Up

    2010-11-01

    Lead (Pb) concentrations in whole blood and δ-aminolevulinic acid (ALA) concentrations in plasma and whole blood from 37 cattle with suspected Pb exposure were determined in order to investigate the usefulness of ALA as a biological indicator for Pb poisoning in cattle. Cows were divided into 4 groups based on blood Pb, as follows: ppb (group 1), 30-100 ppb (group 2), 100-300 ppb (group 3), and >300 ppb (group 4). The derivatization reaction for ALA was improved by a greater than 2-fold measure in whole blood and by a 10-fold measure in plasma by adding 75 and 50 µl of 0.1 N HCl, respectively. Blood Pb concentrations ranged from ppb to 1,006 ppb (185.5 ± 254.9 ppb), with 17 samples containing >50 ppb Pb. Delta-aminolevulinic acid concentrations in whole blood and plasma ranged from ppb to 96.9 ppb (77.4 ± 8.4 ppb) and from ppb to 24.0 ppb (4.6 ± 3.8 ppb), respectively. Whole blood ALA did not correlate with blood lead concentrations in any group. Increase in plasma ALA concentration was dependent on blood Pb concentration. There was no correlation between blood Pb concentration and plasma ALA concentration in group 2 (n  =  4), but correlation coefficients were 0.736 in group 3 and 0.807 in group 4, respectively. The correlation coefficient was increased to 0.851 when groups 3 and 4 were combined. Based on these observations, in cattle, plasma ALA is a more reliable biological biomarker for Pb exposure than is blood ALA.

  8. 5-aminolevulinic acid-incorporated poly(vinyl alcohol nanofiber-coated metal stent for application in photodynamic therapy

    Directory of Open Access Journals (Sweden)

    Kang DH

    2012-05-01

    Full Text Available Jin Ju Yoo*, Chan Kim*, Chung-Wook Chung, Young-Il Jeong, Dae Hwan KangNational Research and Development Center for Hepatibiliary Disease, Pusan National University Yangsan Hospital, Gyeongnam 626-770, Korea *These authors contributed equally to this work.Background: The study investigated the use of combined photodynamic therapy (PDT and stent placement for the treatment of cholangiocarcinoma (CC. For this purpose, 5-aminolevulinic acid (ALA was incorporated into poly(vinyl alcohol (PVA nanofiber, and coated onto metal stents. Their efficacy was assessed in PDT towards HuCC-T1 CC cells.Methods: Fabrication of ALA-PVA nanofiber, and simultaneous coating onto metal stents, was performed through electrospinning. The dark-toxicity, generation of protoporphyrin IX (PpIX, and PDT effect of ALA and ALA-PVA nanofiber were studied in vitro, using HuCC-T1 CC cells.Results: The ALA-PVA nanofibers were coated onto metal stents less than 1000 nm in diameter. ALA-only displayed marginal cytotoxicity; ALA-PVA nanofiber showed less cytotoxicity. PpIX generation was not sigficantly different between ALA and ALA-PVA nanofiber treatments. PVA itself did not generate PpIX in tumor cells. ALA and ALA-PVA nanofiber displayed a similar PDT effect on tumor cells. Cell viability was decreased, dose-dependently, until ALA concentration reached 100 µg/mL. Necrosis and apoptosis of tumor cells occurred similarly for ALA and ALA- PVA nanofiber treatments.Conclusion: The ALA-PVA nanofiber-coated stent is a promising candidate for therapeutic use with cholangiocarcinoma.Keywords: nanofiber, photodynamic therapy, 5-aminolevulinic acid, poly(vinyl alcohol

  9. Effect of 5-aminolevulinic acid on erythropoiesis: A preclinical in vitro characterization for the treatment of congenital sideroblastic anemia

    Energy Technology Data Exchange (ETDEWEB)

    Fujiwara, Tohru [Department of Hematology and Rheumatology, Tohoku University Graduate School, Sendai (Japan); Department of Molecular Hematology/Oncology, Tohoku University Graduate School, Sendai (Japan); Okamoto, Koji; Niikuni, Ryoyu [Department of Hematology and Rheumatology, Tohoku University Graduate School, Sendai (Japan); Takahashi, Kiwamu [SBI Pharmaceuticals Co., Ltd., Tokyo (Japan); Okitsu, Yoko; Fukuhara, Noriko; Onishi, Yasushi [Department of Hematology and Rheumatology, Tohoku University Graduate School, Sendai (Japan); Ishizawa, Kenichi [Department of Hematology and Rheumatology, Tohoku University Graduate School, Sendai (Japan); Clinical Research, Innovation and Education Center, Tohoku University Hospital, Sendai (Japan); Ichinohasama, Ryo [Department of Hematopathology, Tohoku University Graduate School, Sendai (Japan); Nakamura, Yukio [Cell Engineering Division, RIKEN BioResource Center, Tsukuba, Ibaraki (Japan); Nakajima, Motowo; Tanaka, Tohru [SBI Pharmaceuticals Co., Ltd., Tokyo (Japan); Harigae, Hideo, E-mail: harigae@med.tohoku.ac.jp [Department of Hematology and Rheumatology, Tohoku University Graduate School, Sendai (Japan); Department of Molecular Hematology/Oncology, Tohoku University Graduate School, Sendai (Japan)

    2014-11-07

    Highlights: • Treatment with ALA induces erythroid differentiation of K562 cells. • Transportation of ALA into erythroid cells occurs predominantly via SLC36A1. • ALA restores defects in ALAS2 in human iPS cell-derived erythroblasts. • ALA may represent a novel therapeutic option for CSA caused by ALAS2 mutations. - Abstract: Congenital sideroblastic anemia (CSA) is a hereditary disorder characterized by microcytic anemia and bone marrow sideroblasts. The most common form of CSA is attributed to mutations in the X-linked gene 5-aminolevulinic acid synthase 2 (ALAS2). ALAS2 is a mitochondrial enzyme, which utilizes glycine and succinyl-CoA to form 5-aminolevulinic acid (ALA), a crucial precursor in heme synthesis. Therefore, ALA supplementation could be an effective therapeutic strategy to restore heme synthesis in CSA caused by ALAS2 defects. In a preclinical study, we examined the effects of ALA in human erythroid cells, including K562 cells and human induced pluripotent stem cell-derived erythroid progenitor (HiDEP) cells. ALA treatment resulted in significant dose-dependent accumulation of heme in the K562 cell line. Concomitantly, the treatment substantially induced erythroid differentiation as assessed using benzidine staining. Quantitative reverse transcription polymerase chain reaction (RT-PCR) analysis confirmed significant upregulation of heme-regulated genes, such as the globin genes [hemoglobin alpha (HBA) and hemoglobin gamma (HBG)] and the heme oxygenase 1 (HMOX1) gene, in K562 cells. Next, to investigate the mechanism by which ALA is transported into erythroid cells, quantitative RT-PCR analysis was performed on previously identified ALA transporters, including solute carrier family 15 (oligopeptide transporter), member (SLC15A) 1, SLC15A2, solute carrier family 36 (proton/amino acid symporter), member (SLC36A1), and solute carrier family 6 (neurotransmitter transporter), member 13 (SLC6A13). Our analysis revealed that SLC36A1 was abundantly

  10. Effect of 5-aminolevulinic acid on erythropoiesis: a preclinical in vitro characterization for the treatment of congenital sideroblastic anemia.

    Science.gov (United States)

    Fujiwara, Tohru; Okamoto, Koji; Niikuni, Ryoyu; Takahashi, Kiwamu; Okitsu, Yoko; Fukuhara, Noriko; Onishi, Yasushi; Ishizawa, Kenichi; Ichinohasama, Ryo; Nakamura, Yukio; Nakajima, Motowo; Tanaka, Tohru; Harigae, Hideo

    2014-11-07

    Congenital sideroblastic anemia (CSA) is a hereditary disorder characterized by microcytic anemia and bone marrow sideroblasts. The most common form of CSA is attributed to mutations in the X-linked gene 5-aminolevulinic acid synthase 2 (ALAS2). ALAS2 is a mitochondrial enzyme, which utilizes glycine and succinyl-CoA to form 5-aminolevulinic acid (ALA), a crucial precursor in heme synthesis. Therefore, ALA supplementation could be an effective therapeutic strategy to restore heme synthesis in CSA caused by ALAS2 defects. In a preclinical study, we examined the effects of ALA in human erythroid cells, including K562 cells and human induced pluripotent stem cell-derived erythroid progenitor (HiDEP) cells. ALA treatment resulted in significant dose-dependent accumulation of heme in the K562 cell line. Concomitantly, the treatment substantially induced erythroid differentiation as assessed using benzidine staining. Quantitative reverse transcription polymerase chain reaction (RT-PCR) analysis confirmed significant upregulation of heme-regulated genes, such as the globin genes [hemoglobin alpha (HBA) and hemoglobin gamma (HBG)] and the heme oxygenase 1 (HMOX1) gene, in K562 cells. Next, to investigate the mechanism by which ALA is transported into erythroid cells, quantitative RT-PCR analysis was performed on previously identified ALA transporters, including solute carrier family 15 (oligopeptide transporter), member (SLC15A) 1, SLC15A2, solute carrier family 36 (proton/amino acid symporter), member (SLC36A1), and solute carrier family 6 (neurotransmitter transporter), member 13 (SLC6A13). Our analysis revealed that SLC36A1 was abundantly expressed in erythroid cells. Thus, gamma-aminobutyric acid (GABA) was added to K562 cells to competitively inhibit SLC36A1-mediated transport. GABA treatment significantly impeded the ALA-mediated increase in the number of hemoglobinized cells as well as the induction of HBG, HBA, and HMOX1. Finally, small-interfering RNA

  11. Dependence between the level of delta-aminolevulinic acid in urine and some parameters with workers of the Zletovo battery factory in Probistip

    OpenAIRE

    Stavreva Veselinovska, Snezana; Zivanovic, Jordan

    1998-01-01

    Lead has the key part in relation to intoxication by heavy metals. The aim of this determination of correlation between the level of delta-aminolevulinic acid in urine and some other parameters with workers professionally expose to the influence of lead in different parts of the factory producing batteries "Zletovo" in Probistip. The material being used for analysis was the urine 256 persons of both sexses, age level 20-50 years.

  12. Cystic acne improved by photodynamic therapy with short-contact 5-aminolevulinic acid and sequential combination of intense pulsed light and blue light activation.

    Science.gov (United States)

    Melnick, Stuart

    2005-01-01

    Photodynamic therapy with short-contact 5-aminolevulinic acid (Levulan Kerastick, Dusa Pharmaceuticals, Inc.) and activation by intense pulsed light in an initial treatment and blue light in 3 subsequent treatments has resulted in significant improvement in severity of acne, reduction in the number of lesions, improvement in skin texture, and smoothing of scar edges in an Asian patient with severe (class 4) facial cystic acne and scarring.

  13. A gas chromatography-mass spectrometry method for the determination of delta-aminolevulinic acid in plant leaves.

    Science.gov (United States)

    Hijaz, Faraj; Killiny, Nabil

    2016-05-20

    Delta-aminolevulinic (δ-ALA) acid is an important intermediate for tetrapyrroles biosynthesis and it has recently received great attention in plant physiology and human toxicology. However, the colorimetric method which is the most common method for determination of δ-ALA is time consuming and is not specific. In this study, a method for determination of δ-ALA in plant tissues was developed based on the trimethylsilyl (TMS) derivative of the pyrrole formed from the reaction of δ-ALA with ethyl acetoacetate via Knorr condensation. The δ-ALA in the HCl extract was reacted with ethyl acetoacetate to form a pyrrole. Then, the pyrrole compound was extracted using ethyl acetate and the solvent was evaporated to dryness. The dried sample was derivatized to its TMS ester and analyzed using GC-MS. The concentration of δ-ALA in citrus leaves incubated with levulinic acid was also determined by the conventional colorimetric method. The linear range was 10-200ppm in the full scan mode and 0.1-20ppm in the selected ion monitoring (SIM). The limit of detection was 6ppm in the full scan and 0.05ppm in SIM mode, representing a four-fold increase in sensitivity compared to the colorimetric method. The GC-MS method developed in this study is simple, accurate, sensitive, and could also be used to measure δ-ALA in other biological samples.

  14. Optimization of Biomass and 5-Aminolevulinic Acid Production by Rhodobacter sphaeroides ATCC17023 via Response Surface Methodology.

    Science.gov (United States)

    Liu, Shuli; Zhang, Guangming; Li, Jianzheng; Li, Xiangkun; Zhang, Jie

    2016-06-01

    Microbial 5-aminolevulinic acid (ALA) produced from wastewater is considered as potential renewable energy. However, many hurdles are needed to be overcome such as the regulation of key influencing factors on ALA yield. Biomass and ALA production by Rhodobacter sphaeroides was optimized using response surface methodology. The culturing medium was artificial volatile fatty acids wastewater. Three additives were optimized, namely succinate and glycine that are precursors of ALA biosynthesis, and D-glucose that is an inhibitor of ALA dehydratase. The optimal conditions were achieved by analyzing the response surface plots. Statistical analysis showed that succinate at 8.56 mmol/L, glycine at 5.06 mmol/L, and D-glucose at 7.82 mmol/L were the best conditions. Under these optimal conditions, the highest biomass production and ALA yield of 3.55 g/L and 5.49 mg/g-biomass were achieved. Subsequent verification experiments at optimal values had the maximum biomass production of 3.41 ± 0.002 g/L and ALA yield of 5.78 ± 0.08 mg/g-biomass.

  15. SIMULTANEOUS ESTIMATION OF MEFENAMIC ACID AND DICYCLOMINE HYDROCHLORIDE BY SPECTROSCOPIC METHODS

    Directory of Open Access Journals (Sweden)

    D.N. Prajapati et al

    2012-10-01

    Full Text Available A novel, simple, accurate, sensitive, reproducible, economical spectroscopic method was developed and validated for the determination of Mefenamic acid and Dicyclomine hydrochloride in combined dosage form. Three different analytical methods, Absorption correction method, Differential derivative method, Simultaneous equation method were developed for estimation of Dicyclomine hydrochloride(10mg and Mefenamic acid (250mg in tablet dosage form. wavelength for estimation was 223nm for Dicyclomine hydrochloride and 308.60nm for Mefenamic acid in absorption correction method. 211.60nm was Zero crossing point of Mefenamic acid and 308.80nm was Zero crossing point of Dicyclomine hydrochloride which can estimate in differential derivative method. Simultaneous equation method was developed in NaOH which was linear in the range of 1-6µg/ml for Dicyclomine hydrochloride and 25-150µg/ml for Mefenamic acid, the correlation coefficient obtained was nearer to one. The method was validated for linearity, accuracy and precision as per ICH guidelines. The developed and validated method was successfully used for the quantitative analysis of commercially available dosage form.

  16. The influence of photodynamic therapy (PDT) with δ-aminolevulinic acid (ALA) on J-774A.1 macrophage cell line

    Science.gov (United States)

    Kawczyk-Krupka, Aleksandra; Czuba, Zenon; Ledwon, Aleksandra; Latos, Wojciech; Sliszka, Ewelina; Mianowska, Marta; Krol, Wojciech; Sieron, Aleksander

    2008-02-01

    Introduction. The whole mechanism of the cellular level of tumor destruction by photodynamic therapy (PDT) is still unknown. Despite necrotic and apoptotic ways of cell death, there is a variety of events leading to and magnifying the inactivation of tumor cells. Material and methods. J-774A.1 were incubated with δ-aminolevulinic acid (ALA) at different concentrations (125, 250, 500, 1000 μM) and then irradiated with VIS (400 - 750 nm) at the dose of 5,10 and 30 J/cm2 delivered from the incoherent light source. The effects of the application of ALA-PDT were evaluated on the basis of cell viability, nitric oxide (NO), tumor necrosis factor α- (TNF-α) and interleukin-1β (IL-1β) produced by the J-774A.1 cells. Results. The cell viability (assessed using MTT test) was comparable with control group at 5,10 and 30 J/cm2. At these doses of energy using different concentrations of ALA we have observed that at the higher energy doses, the greater increase of TNF-α release, lowering of the level of IL-1β production and decrease of NO release were observed. There was also observed the dependence of the secretional activity of the cells on the ALA concentrations. Conclusion. The cell viability and production of cytokines depended on ALA concentrations and energy doses of the light. The higher some cytokines' release after PDT could be an additional factor for the complete eradication of tumor.

  17. Effects of 5-aminolevulinic acid photodynamic therapy on TLRs in acne lesions and keratinocytes co-cultured with P. acnes.

    Science.gov (United States)

    Ma, Ying; Chen, Qinyi; Liu, Ye; Wang, Qianqian; Huang, Zheng; Xiang, Leihong

    2016-09-01

    To investigate the effect of 5-aminolevulinic acid photodynamic therapy (ALA-PDT) on the expression of Toll like receptors (TLRs) in human keratinocytes and its role in acne treatment. TLR2 and TLR4 expression in acne lesions before and after ALA-PDT were examined by immunohistochemical assay. Primary keratinocytes were obtained from acne lesions, co-cultured with P. acnes and then treated with ALA-PDT using red or blue LED. Cytokines production were examined by ELISA, TLR2 and TLR4 gene expression by real-time PCR, and TLR2 and TLR4 protein expression by Western-blot assay. The overexpression of TLR2 and TLR4 in acne lesion were detected, which became negative or weaker after ALA-PDT. The infection of P. acnes in keratinocytes could significantly increase the levels of early inflammatory cytokines (e.g. IL-1α, TNF-α and IL-8) (Pkeratinocytes (Pkeratinocytes treated with P. acnes via TLRs pathways. Copyright © 2016. Published by Elsevier B.V.

  18. Enhancement of 5-aminolevulinic acid-based fluorescence detection of side population-defined glioma stem cells by iron chelation

    Science.gov (United States)

    Wang, Wenqian; Tabu, Kouichi; Hagiya, Yuichiro; Sugiyama, Yuta; Kokubu, Yasuhiro; Murota, Yoshitaka; Ogura, Shun-ichiro; Taga, Tetsuya

    2017-01-01

    Cancer stem cells (CSCs) are dominantly responsible for tumor progression and chemo/radio-resistance, resulting in tumor recurrence. 5-aminolevulinic acid (ALA) is metabolized to fluorescent protoporphyrin IX (PpIX) specifically in tumor cells, and therefore clinically used as a reagent for photodynamic diagnosis (PDD) and therapy (PDT) of cancers including gliomas. However, it remains to be clarified whether this method could be effective for CSC detection. Here, using flow cytometry-based analysis, we show that side population (SP)-defined C6 glioma CSCs (GSCs) displayed much less 5-ALA-derived PpIX fluorescence than non-GSCs. Among the C6 GSCs, cells with ultralow PpIX fluorescence exhibited dramatically higher tumorigenicity when transplanted into the immune-deficient mouse brain. We further demonstrated that the low PpIX accumulation in the C6 GSCs was enhanced by deferoxamine (DFO)-mediated iron chelation, not by reserpine-mediated inhibition of PpIX-effluxing ABCG2. Finally, we found that the expression level of the gene for heme oxygenase-1 (HO-1), a heme degradation enzyme, was high in C6 GSCs, which was further up-regulated when treated with 5-ALA. Our results provide important new insights into 5-ALA-based PDD of gliomas, particularly photodetection of SP-defined GSCs by iron chelation based on their ALA-PpIX-Heme metabolism. PMID:28169355

  19. Characterization of Three Homoeologous cDNAs Encoding Chloroplast-targeted Aminolevulinic Acid Dehydratase in Common Wheat

    Institute of Scientific and Technical Information of China (English)

    Yu Takenouchi; Haruka Nakajima; Kengo Kanamaru; Shigeo Takumi

    2011-01-01

    In the tetrapyrrole biosynthetic pathway of higher plants,5-aminolevulinic acid (ALA) is metabolized by ALA dehydratase (ALAD).Here,we isolated ALAD1 cDNA from common wheat (Triticum aestivum L.) and its diploid progenitors,and produced transgenic tobacco plants expressing the wheat ALAD1 gene.The ALAD1 genes were highly conserved among wheat relatives,and three homoeologous loci of wheat ALAD1 (TaALAD1) were equally transcribed in common wheat.A transient expression assay of a TaALAD1-GFP (green fluorescent protein) fusion protein suggested that TaALAD1 is localized in chloroplasts.Overexpression of TaALAD1 in transgenic tobacco resulted in a significant increase in ALAD activity in leaves.Moreover,the transgenic tobacco showed vigorous growth and increased survival rate on medium containing ALA at herbicidal concentrations.These results indicate that wheat ALAD1 has catalytic activity in metabolizing ALA in plastids,and that ectopic expression of TaALAD1 in transgenic plants increases their tolerance to ALA application at high concentrations.

  20. Comparative analysis of the effects of CO2 fractional laser and sonophoresis on human skin penetration with 5-aminolevulinic acid.

    Science.gov (United States)

    Choi, J H; Shin, E J; Jeong, K H; Shin, M K

    2017-08-19

    Successful delivery of a photosensitizer into the skin is an important factor for effective photodynamic therapy (PDT). The effective method to increase drug penetration within short incubation time overcoming skin barrier have been investigated. This study was performed to analyze and compare the effectiveness of ablative fractional laser (FXL) pretreatment and/or sonophoresis for enhancing the penetration of 5-aminolevulinic acid (ALA) into human skin in vivo. Twenty-four identical 1 × 1 cm(2) treatment areas were mapped on the backs of ten healthy male subjects. Each area received FXL pretreatment and/or sonophoresis with different energy settings and ALA incubation times. After treatments, porphyrin fluorescence reflecting the ALA penetration were measured. Application of ablative CO2 FXL pretreatment resulted to higher fluorescence intensities than the non-treatment group. Incubation times were positively correlated with the increments of ALA penetration. However, increasing pulse energy or combining with sonophoresis did not show additional positive effects on ALA penetration. Ablative CO2 FXL pretreatment effectively facilitated ALA penetration in human skin in vivo. Ablative CO2 FXL alone without sonophoresis setting pulse energy of 10 and 20 mJ with more than 60 min of ALA incubation time could be an ideal setting for ALA penetration.

  1. Evaluation of Hydrogel Suppositories for Delivery of 5-Aminolevulinic Acid and Hematoporphyrin Monomethyl Ether to Rectal Tumors.

    Science.gov (United States)

    Ye, Xuying; Yin, Huijuan; Lu, Yu; Zhang, Haixia; Wang, Han

    2016-10-12

    We evaluated the potential utility of hydrogels for delivery of the photosensitizing agents 5-aminolevulinic acid (ALA) and hematoporphyrin monomethyl ether (HMME) to rectal tumors. Hydrogel suppositories containing ALA or HMME were administered to the rectal cavity of BALB/c mice bearing subcutaneous tumors of SW837 rectal carcinoma cells. For comparison, ALA and HMME were also administered by three common photosensitizer delivery routes; local administration to the skin and intratumoral or intravenous injection. The concentration of ALA-induced protoporphyrin IX or HMME in the rectal wall, skin, and subcutaneous tumor was measured by fluorescence spectrophotometry, and their distribution in vertical sections of the tumor was measured using a fluorescence spectroscopy system. The concentration of ALA-induced protoporphyrin IX in the rectal wall after local administration of suppositories to the rectal cavity was 9.76-fold (1 h) and 5.8-fold (3 h) higher than in the skin after cutaneous administration. The maximal depth of ALA penetration in the tumor was ~3-6 mm at 2 h after cutaneous administration. Much lower levels of HMME were observed in the rectal wall after administration as a hydrogel suppository, and the maximal depth of tumor penetration was suppository is thus a potential delivery route for photodynamic therapy of rectal cancer.

  2. Evaluation of Hydrogel Suppositories for Delivery of 5-Aminolevulinic Acid and Hematoporphyrin Monomethyl Ether to Rectal Tumors

    Directory of Open Access Journals (Sweden)

    Xuying Ye

    2016-10-01

    Full Text Available We evaluated the potential utility of hydrogels for delivery of the photosensitizing agents 5-aminolevulinic acid (ALA and hematoporphyrin monomethyl ether (HMME to rectal tumors. Hydrogel suppositories containing ALA or HMME were administered to the rectal cavity of BALB/c mice bearing subcutaneous tumors of SW837 rectal carcinoma cells. For comparison, ALA and HMME were also administered by three common photosensitizer delivery routes; local administration to the skin and intratumoral or intravenous injection. The concentration of ALA-induced protoporphyrin IX or HMME in the rectal wall, skin, and subcutaneous tumor was measured by fluorescence spectrophotometry, and their distribution in vertical sections of the tumor was measured using a fluorescence spectroscopy system. The concentration of ALA-induced protoporphyrin IX in the rectal wall after local administration of suppositories to the rectal cavity was 9.76-fold (1 h and 5.8-fold (3 h higher than in the skin after cutaneous administration. The maximal depth of ALA penetration in the tumor was ~3–6 mm at 2 h after cutaneous administration. Much lower levels of HMME were observed in the rectal wall after administration as a hydrogel suppository, and the maximal depth of tumor penetration was <2 mm after cutaneous administration. These data show that ALA more readily penetrates the mucosal barrier than the skin. Administration of ALA as an intrarectal hydrogel suppository is thus a potential delivery route for photodynamic therapy of rectal cancer.

  3. Effects of Delta-Aminolevulinic Acid Dehydratase Polymorphisms on Susceptibility to Lead in Han Subjects from Southwestern China

    Directory of Open Access Journals (Sweden)

    Pin Sun

    2012-07-01

    Full Text Available This study is to determine the distribution of the delta-aminolevulinic acid dehydratase (ALAD polymorphism among Han subjects of the Chinese population and to study whether the polymorphism in the ALAD gene modifies the toxicity of lead in lead-exposed workers. For this purpose we conducted a cross-sectional study on 156 Chinese workers who were exposed to lead in lead-acid battery and electric-flex manufacturing plants. The authors found that the allele frequencies of ALAD1 and ALAD2 were 0.9679 and 0.0321, respectively. Workers with the ALAD 1-1 genotype were associated with higher blood lead levels than those with the ALAD 1-2 genotype. Blood and urine lead levels were much higher in storage battery workers than in cable workers. The self-conscious symptom survey showed that the incidences of debilitation, amnesia and dreaminess were much higher in those had more than five years of tenure or contact with lead on the job within the ALAD 1-1 genotype subgroup. Laboratory examinations showed that serum iron and zinc levels in workers’ with the ALAD 1-2 genotype were higher than those with the ALAD 1-1 genotype, especially in storage-battery workers. Correlation analysis indicated that the blood lead level negatively correlated with serum calcium, iron and zinc level. The data of this study suggest that the ALAD gene polymorphism and serum ion levels may modify the kinetics of lead in blood. Therefore, the authors recommend that an adequate intake of dietary calcium, iron, and zinc or the calcium, iron, and zinc supplementation should be prescribed to Chinese lead exposed workers.

  4. In Vivo Curative and Protective Potential of Orally Administered 5-Aminolevulinic Acid plus Ferrous Ion against Malaria

    Science.gov (United States)

    Suzuki, Shigeo; Hikosaka, Kenji; Balogun, Emmanuel O.; Komatsuya, Keisuke; Niikura, Mamoru; Kobayashi, Fumie; Takahashi, Kiwamu; Tanaka, Tohru; Nakajima, Motowo

    2015-01-01

    5-Aminolevulinic acid (ALA) is a naturally occurring amino acid present in diverse organisms and a precursor of heme biosynthesis. ALA is commercially available as a component of cosmetics, dietary supplements, and pharmaceuticals for cancer diagnosis and therapy. Recent reports demonstrated that the combination of ALA and ferrous ion (Fe2+) inhibits the in vitro growth of the human malaria parasite Plasmodium falciparum. To further explore the potential application of ALA and ferrous ion as a combined antimalarial drug for treatment of human malaria, we conducted an in vivo efficacy evaluation. Female C57BL/6J mice were infected with the lethal strain of rodent malaria parasite Plasmodium yoelii 17XL and orally administered ALA plus sodium ferrous citrate (ALA/SFC) as a once-daily treatment. Parasitemia was monitored in the infected mice, and elimination of the parasites was confirmed using diagnostic PCR. Treatment of P. yoelii 17XL-infected mice with ALA/SFC provided curative efficacy in 60% of the mice treated with ALA/SFC at 600/300 mg/kg of body weight; no mice survived when treated with vehicle alone. Interestingly, the cured mice were protected from homologous rechallenge, even when reinfection was attempted more than 230 days after the initial recovery, indicating long-lasting resistance to reinfection with the same parasite. Moreover, parasite-specific antibodies against reported vaccine candidate antigens were found and persisted in the sera of the cured mice. These findings provide clear evidence that ALA/SFC is effective in an experimental animal model of malaria and may facilitate the development of a new class of antimalarial drug. PMID:26324278

  5. Coupling of Carbon Dioxide with Epoxides Catalyzed by Amino Acid Hydrochloride Salts

    Institute of Scientific and Technical Information of China (English)

    2008-01-01

    Using amino acid hydrochloride salt as a catalyst, the coupling reaction of CO2 with epoxides could proceed smoothly to give cyclic carbonates in very good yields and high selectivity. The reaction conditions such as the pressure of carbon dioxide, reaction temperature, time and catalyst loading were carefully investigated.

  6. Esterification of pseudoephedrine hydrochloride by citric acid in a solid dose pharmaceutical preparation.

    Science.gov (United States)

    Goel, Alok; Zhao, Zhicheng; Sørensen, Dan; Zhou, Jay; Zhang, Fa

    2016-09-10

    Esterification of pseudoephedrine hydrochloride (PSE) by citric acid was observed in a solid dose pharmaceutical preparation at room temperature and accelerated stability condition (40°C/75% relative humidity). The esterification of PSE with citric acid was confirmed by a solid-state binary reaction in the presence of minor level of water at elevated temperature to generate three isomeric esters. The structures of the pseudoephedrine citric acid esters were elucidated using high-resolution mass spectrometry and nuclear magnetic resonance spectroscopy (NMR). Occurrence of esterification in solid state, instead of amidation which is generally more favorable than esterification, is likely due to remaining HCl salt form of solid pseudoephedrine hydrochloride to protect its amino group from amidation with citric acid. In contrast, the esterification was not observed from solution reaction between PSE and citric acid.

  7. Low-Dose Topical 5-Aminolevulinic Acid Photodynamic Therapy in the Treatment of Different Severity of Acne Vulgaris.

    Science.gov (United States)

    Tao, Shi-Qin; Li, Fei; Cao, Lei; Xia, Ru-Shan; Fan, Hua; Fan, Ying; Sun, Hui; Jing, Cheng; Yang, Li-Jia

    2015-12-01

    The objective of this article is to investigate the effectiveness and safety of photodynamic therapy (PDT) with 3.6 % topical aminolevulinic acid (ALA) and a short incubation time with red light in moderate to severe acne. One hundred and thirty-six patients with moderate to severe acne were treated with 3.6 % topical ALA-PDT for three sessions with an interval of 2 weeks. Patients were evaluated for efficacy and safety on week 2, 4, 6, 8, and 12 after the initial treatment. Most patients showed apparent clearance of acne lesions at the treated site after three sessions. The effective treatment rates were increased after the multiple therapies. The clinical outcomes are the best at 4 weeks after the final treatment. The total effectiveness rate and cure rate of the low-dose ALA-PDT procedure is 92.65 and 47.06 %, respectively. Thirty-one patients and nineteen patients showed apparent exacerbation of acne lesions before the 2nd and 3rd treatment, respectively, but all of them showed good or excellent improvement after a three-course treatment. A few patients showed mild relapse including papules and comedos at 8 weeks after the final treatment. No significant differences are found in the effects of different acne severity and different genders. Adverse reactions are mild and transient. A 3.6 % topical ALA-PDT with a short time incubation with red light is a simple and an effective treatment option for moderate to severe acne with mild side effects in Chinese people.

  8. Diagnostic approach for cancer cells in urine sediments by 5-aminolevulinic acid-based photodynamic detection in bladder cancer.

    Science.gov (United States)

    Miyake, Makito; Nakai, Yasushi; Anai, Satoshi; Tatsumi, Yoshihiro; Kuwada, Masaomi; Onishi, Sayuri; Chihara, Yoshitomo; Tanaka, Nobumichi; Hirao, Yoshihiko; Fujimoto, Kiyohide

    2014-05-01

    Bladder urothelial carcinoma is diagnosed and followed up after transurethral resection using a combination of cystoscopy, urine cytology and urine biomarkers at regular intervals. However, cystoscopy can overlook flat lesions like carcinoma in situ, and the sensitivity of urinary tests is poor in low-grade tumors. There is an emergent need for an objective and easy urinary diagnostic test for the management of bladder cancer. In this study, three different modalities for 5-aminolevulinic acid (ALA)-based photodynamic diagnostic tests were used. We developed a compact-size, desktop-type device quantifying red fluorescence in cell suspensions, named "Cellular Fluorescence Analysis Unit" (CFAU). Urine samples from 58 patients with bladder cancer were centrifuged, and urine sediments were then treated with ALA. ALA-treated sediments were subjected to three fluorescence detection assays, including the CFAU assay. The overall sensitivities of conventional cytology, BTA, NMP22, fluorescence cytology, fluorescent spectrophotometric assay and CFAU assay were 48%, 33%, 40%, 86%, 86% and 87%, respectively. Three different ALA-based assays showed high sensitivity and specificity. The ALA-based assay detected low-grade and low-stage bladder urothelial cells at shigher rate (68-80% sensitivity) than conventional urine cytology, BTA and NMP22 (8-20% sensitivity). Our findings demonstrate that the ALA-based fluorescence detection assay is promising tool for the management of bladder cancer. Development of a rapid and automated device for ALA-based photodynamic assay is necessary to avoid the variability induced by troublesome steps and low stability of specimens.

  9. Clearance of protoporphyrin IX induced by 5-aminolevulinic acid from WiDr human colon carcinoma cells

    Science.gov (United States)

    Juzeniene, Asta; Kaliszewski, Miron; Bugaj, Andrzej; Moan, Johan

    2009-06-01

    5-aminolevulinic acid-mediated photodynamic therapy (ALA-PDT) is the most widely practiced form of PDT in dermatology. One of the advantages of ALA-PDT is that undesirable photosensitization lasts only for 24-48 h. In order to optimize ALA-PDT it is necessary to understand the mechanisms controlling intracellular PpIX clearance (efflux and transformation into heme) in order to decrease protoporphyrin IX (PpIX) clearance rates in the early stages of its production. The aim of this study was to investigate the factors controlling the clearance of intracellular PpIX. Fluorescence spectroscopy was used to study PpIX kinetics in WiDr cells initially treated with ALA. The clearance rate of PpIX in WiDr cells was faster after application of a low concentration of ALA (0.1 mM) than after application of high concentration of ALA (1 mM). PpIX was cleared faster from cells which initially were seeded at low densities than cells seeded at higher densities. The presence of the iron chelator deferoxamine reduced the clearance rate of PpIX, while the presence of ferrous sulfate acted oppositely. The decay rate of PpIX in WiDr cells was faster at higher temperature than at lower. The ferrochelatase activity at pH 7.2 was significantly greater than that at pH 6.7. ALA concentration, application time, cell density, temperature, pH, intracellular iron content, intracellular amount and localization of PpIX are factors controlling PpIX clearance.

  10. Comprehensive analysis of 5-aminolevulinic acid dehydrogenase (ALAD variants and renal cell carcinoma risk among individuals exposed to lead.

    Directory of Open Access Journals (Sweden)

    Dana M van Bemmel

    Full Text Available BACKGROUND: Epidemiologic studies are reporting associations between lead exposure and human cancers. A polymorphism in the 5-aminolevulinic acid dehydratase (ALAD gene affects lead toxicokinetics and may modify the adverse effects of lead. METHODS: The objective of this study was to evaluate single-nucleotide polymorphisms (SNPs tagging the ALAD region among renal cancer cases and controls to determine whether genetic variation alters the relationship between lead and renal cancer. Occupational exposure to lead and risk of cancer was examined in a case-control study of renal cell carcinoma (RCC. Comprehensive analysis of variation across the ALAD gene was assessed using a tagging SNP approach among 987 cases and 1298 controls. Occupational lead exposure was estimated using questionnaire-based exposure assessment and expert review. Odds ratios (OR and 95% confidence intervals (CI were calculated using logistic regression. RESULTS: The adjusted risk associated with the ALAD variant rs8177796(CT/TT was increased (OR = 1.35, 95%CI = 1.05-1.73, p-value = 0.02 when compared to the major allele, regardless of lead exposure. Joint effects of lead and ALAD rs2761016 suggest an increased RCC risk for the homozygous wild-type and heterozygous alleles ((GGOR = 2.68, 95%CI = 1.17-6.12, p = 0.01; (GAOR = 1.79, 95%CI = 1.06-3.04 with an interaction approaching significance (p(int = 0.06. No significant modification in RCC risk was observed for the functional variant rs1800435(K68N. Haplotype analysis identified a region associated with risk supporting tagging SNP results. CONCLUSION: A common genetic variation in ALAD may alter the risk of RCC overall, and among individuals occupationally exposed to lead. Further work in larger exposed populations is warranted to determine if ALAD modifies RCC risk associated with lead exposure.

  11. Separation and partial characterization of enzymes catalyzing delta-aminolevulinic acid formation in Synechocystis sp. PCC 6803.

    Science.gov (United States)

    Rieble, S; Beale, S I

    1991-09-01

    Formation of the universal tetrapyrrole precursor, delta-aminolevulinic acid (ALA), from glutamate via the five-carbon pathway requires three enzymes: glutamyl-tRNA synthetase, glutamyl-tRNA reductase, and glutamate-1-semialdehyde (GSA) aminotransferase. All three enzymes were separated from extracts of the unicellular cyanobacterium Synechocystis sp. PCC 6803, and two of them, glutamyl-tRNA synthetase and GSA aminotransferase, were partially characterized. After an initial high speed centrifugation and differentiatial ammonium sulfate fractionation of cell extract, the enzymes were separated by successive affinity chromatography on Reactive Blue 2-Sepharose and 2',5'-ADP-agarose. All three enzyme fractions were required to reconstitute ALA formation from glutamate. The apparent native molecular masses of glutamyl-tRNA synthetase and GSA aminotransferase were determined by gel filtration chromatography to be 63 and 98 kDa, respectively. Neither glutamyl-tRNA synthetase nor GSA aminotransferase activity was affected by hemin concentrations up to 10 and 30 microM, respectively, and neither activity was affected by protochlorophyllide concentrations up to 2 microM. GSA aminotransferase was inhibited 50% by 0.5 microM gabaculine. The gabaculine inhibition was reversible for up to 1 h after its addition, if the gabaculine was removed by gel filtration before the enzyme was incubated with substrate. However, irreversible inactivation was obtained by preincubating the enzyme at 30 degrees C either for several hours with gabaculine alone or for a few minutes with both gabaculine and GSA. Neither pyridoxal phosphate nor pyridoxamine phosphate significantly affected the activity of GSA aminotransferase at physiologically relevant concentrations, and neither of these compounds reactivated the gabaculine-inactivated enzyme. It was noted that the presence of pyridoxamine phosphate in the ALA assay mixture produced a false positive color reaction even in the absence of enzyme.

  12. Topical 5-aminolevulinic acid photodynamic therapy improved refractory acne conglobata and perifolliculitis capitis abscedens et suffodiens rather than hidradenitis suppurativa

    Directory of Open Access Journals (Sweden)

    Linglin Zhang

    2016-01-01

    Full Text Available Acne conglobata (AC, perifolliculitis capitis abscedens et suffodiens (PCAS and hidradenitis suppurativa (HS are uncommon refractory chronic, inflammatory, scarring diseases but cause serious damage to the quality of life. These three diseases are associated with follicular occlusion. Several studies indicated topical 5-aminolevulinic acid photodynamic therapy (ALA-PDT improved follicular occlusion besides acne treatment. So we attempted to apply ALA-PDT to medicine resistant AC, PCAS and HS. Topical ALA-PDT was applied to 10 patients with AC, seven patients with PCAS and three patients with HS for more than three sessions. All the patients completed the dermatology life quality index (DLQI questionnaire and were assessed for the efficacy at the baseline and on two weeks after each treatment. Adverse effects were recorded at each visit. The results showed 25.5% (5/20, two cases of AC and three cases of PCAS of patients achieved excellent improvement after three sessions of PDT and another 60.0% (12/20, eight cases of AC and four cases of PCAS of patients achieved good improvement. 15.0% (3/20, three cases of HS got poor response (< 20% lesions clearance. Another five cases (three cases of AC and two cases of PCAS also achieved excellent response after 5–7 sessions of PDT. We also found that papular/nodular, cyst/abscess showed higher clearance rate than sinus/fistula (88.5%, 86.1% versus 11.1%. DLQI was reduced after three sessions of PDT in AC and PCAS patients rather than HS patients. 5-ALA-PDT could improve refractory AC and PCAS but could not lead to improvement in late stage of HS. The efficacy increased with more treatment sessions.

  13. Blood Lead Level and Δ-Aminolevulinic Acid Dehydratase Activity in Pre-Menopausal and Postmenopausal Women

    Directory of Open Access Journals (Sweden)

    I.R Elezaj

    2012-07-01

    Full Text Available To describe the relationship of blood lead levels (BLL and blood, δ-aminolevulinic acid dehydratase(ALAD activity and haematocrit value(Hct to menopause , were examined 17 pre-or perimenopausal (PreM and 17 postmenopausal women (PosMfrom Prishtina City, the capital ofRepublic Kosovo. The mean age of the PreM women was 28.8 years (21-46, with a mean blood lead level of 1.2 μg/dL (SD=0.583 μg/dL , the mean blood ALAD activity53.2 U/LE (SD= 2.8 U/LE and haematocrit value42.1 % (SD= 4.3 %. The mean age of the PosM women was 53.6 years (43-67, with a mean blood lead level1.9 μg/dL (SD=0.94 μg/dL, the mean blood ALAD activity 44.4 U/LE(SD=7.2 U/LE and haematocrit value 42.1 % ( SD= 4.3 % and 42.2 % (SD=4.4 %. The BPb level of PosM women was significantly higher (P<0.001 in comparison with the BPb level in PreM women. The blood ALAD activity of PosM was significantly inhibited (P<0.002 in comparison with blood ALAD activity in PreM women. The haematocrit values were relatively unchanged. There was established significantly negative correlation between BPb and blood ALAD activity (r=- 0.605; P<0.01 in the PreM women.These results support the hypothesis that release of bone lead stores increases during menopause and constitutes an internal source of exposure possibly associated with adverse health effects on women in menopause transition.

  14. Study on Insecticidal Activities and Effect on Three Kinds of Enzymes by 5- Aminolevulinic Acid on Oxya chinensis

    Institute of Scientific and Technical Information of China (English)

    YIN Kun; MA En-bo; XUE Chun-rong; WU Hai-hua; GUO Ya-ping; ZHANG Jian-zhen

    2008-01-01

    Insecticidal activities and effects on three enzymic activities caused by 5-aminolevulinic acid (ALA) on Oxya chinensis were studied. Fourth-instar nymphs of O. chinensis were treated with different doses of ALA (A 1,250 mM; A2, 450 mM; A3,750 mM; A4, 1 000 mM). Mortality and the activities of acetylcholinesterase (ACHE), glutathione S-transferase (GSTs), and glutathione peroxidase (GPx) were determinated. The mortality of O. chinensis rose with an increasing dose of ALA. The mortality of high-dose treatments A3 and A4 reached 66.19 and 80.21%, respectively. The value of LD50 was 3.61 (3.29-3.93) mg g-1 body weight (95% confidence interval). Biochemical studies showed that the activities of AChE and GPx in the A4 treatment declined by 51.53 and 42.82% in the female, and 42.65 and 43.85% in the male compared to the control, respectively, and the degree of decline reached a significant level at P < 0.05. Meanwhile, the GSTs activities of O. chinensis enhanced with increasing dose of ALA. The GSTs activities of female and male O. chinensis in the A4 treatment remarkably increased by 171.05 and 97.42% compared to the control (P < 0.05). ALA had an obviously toxic effect on O. chinensis. Moreover, ALA caused the photoinactivation of AChE and GPx, which induced nerve transmission blocking and the capability to defend oxidation damage declining. Meanwhile, a high dose of ALA could activate GSTs, which caused a feedback inhibition of the insect to the phototoxic substance.

  15. Inhibition of erythrocytes δ-aminolevulinic acid dehydratase (ALAD) activity in fish from waters affected by lead smelters

    Science.gov (United States)

    Schmitt, Christopher J.; Caldwell, Colleen A.; Olsen, Bill; Serdar, Dave; Coffey, Mike

    2002-01-01

    We assessed the effects on fish of lead (Pb) released to streamsby smelters located in Trail, BC (Canada), E. Helena, MT, Herculaneum, MO, and Glover, MO. Fish were collected by electrofishing from sites located downstream of smelters and from reference sites. Blood from each fish was analyzed for δ-aminolevulinic acid dehydratase (ALAD) activity and hemoglobin (Hb), and samples of blood, liver, or carcass were analyzed for Pb, zinc (Zn), or both. Fish collected downstreamof all four smelters sites had elevated Pb concentrations, decreased ALAD activity, or both relative to their respectivereference sites. At E. Helena, fish from the downstream site also had lower Hb concentrations than fish from upstream. Differences among taxa were also apparent. Consistent with previous studies, ALAD activity in catostomids (Pisces: Catostomidae-northern hog sucker,Hypentelium nigricans;river carpsucker, Carpiodes carpio; largescale sucker, Catostomus macrocheilus; and mountain sucker, C. platyrhynchus) seemed more sensitive to Pb-induced ALADinhibition than the salmonids (Pisces: Salmonidae-rainbow trout,Oncorhynchus mykiss; brook trout,Salvelinus fontinalis) or common carp (Cyprinus carpio). Some of these differences may have resulted from differential accumulation of Zn, which was not measured at all sites. We detected noALAD activity in channel catfish (Ictaluruspunctatus) from either site on the Mississippi River at Herculaneum, MO. Our findings confirmed that Pb is releasedto aquatic ecosystems by smelters and accumulated by fish, andwe documented potentially adverse effects of Pb in fish. We recommend that Zn be measured along with Pb when ALAD activityis used as a biomarker and the collection of at least 10 fish ofa species at each site to facilitate statistical analysis.

  16. A first-principles study of functionalized clusters and carbon nanotubes or fullerenes with 5-Aminolevulinic acid as vehicles for drug delivery

    Science.gov (United States)

    Kia, Majid; Golzar, Maryam; Mahjoub, Kosar; Soltani, Alireza

    2013-10-01

    At present work, we explore the adsorption properties of the 5-Aminolevulinic acid (5ALA) interacting with SWCNTs, C60, and C24 by density functional ab initio (DFT) calculations. It was found that the electronic structure of C60 is more sensitive to the presence of 5ALA in comparison with C24, (5, 5), and (9, 0) SWCNT. Our results demonstrate that the interactions between 5ALA and the nanostructures are chemisorption. The natural bond orbital (NBO) and density of states (DOSs) analyses represent that the nature of 5ALA adsorption on the applied nanostructures is permanently electrostatic rather than covalent.

  17. Improved 5-Aminolevulinic Acid Production with Recombinant Escherichia coli by a Short-term Dissolved Oxygen Shock in Fed-batch Fermentation

    Institute of Scientific and Technical Information of China (English)

    杨俊; 朱力; 傅维琦; 林逸君; 林建平; 岑沛霖

    2013-01-01

    5-Aminolevulinic acid (ALA) is a common precursor for tetrapyrrole compounds in all kinds of organ-isms and has wide applications in agriculture and medicines. In this study, a new strategy, i.e. short-term dissolved oxygen (DO) shock during aerobic fermentation, was introduced to produce 5-aminolevulinic acid with a recombi-nant E. coli. Effects of duration time of DO shock operation on plasmid concentration, intracellular ALA synthase (ALAS) activity and ALA production were investigated in Erlenmeyer shake flasks. The results indicated that both ALAS activity and ALA yield were enhanced in an anaerobic operation of 45 min in the early exponential phase during fermentation, while they decreased when the anaerobic operation time was further increased to 60 min. The DO shock protocol was confirmed with the fed-batch fermentation in a 15 L fermenter and the ALA production achieved 9.4 g·L-1 (72 mmol·L-1), which is the highest yield in the fermentation broth reported up to now.

  18. Aminolevulinic Acid-Mediated Photodynamic Therapy of Human Meningioma: An in Vitro Study on Primary Cell Lines

    Directory of Open Access Journals (Sweden)

    Mustafa El-Khatib

    2015-04-01

    Full Text Available Objective: Five-aminolevulinic acid (5-ALA-induced porphyrins in malignant gliomas are potent photosensitizers. Promising results of ALA-PDT (photodynamic therapy in recurrent glioblastomas have been published. Recently, 5-ALA-induced fluorescence was studied in meningioma surgery. Here, we present an experimental study of ALA-PDT in an in vitro model of primary meningioma cell lines. Methods: We processed native tumor material obtained intra-operatively within 24 h for cell culture. Epithelial membrane antigen (EMA immunohistochemistry was performed after the first passage to confirm that cells were meningioma cells. For 5-ALA-PDT treatment, about 5000 cells per well were seeded in 20 wells of a blank 96-well plate. Each block of 4 wells was inoculated with 150 µL of 0, 25, 50 and 100 µg/mL 5-ALA solutions; one block was used as negative control without 5-ALA and without PDT. Following incubation for 3 h PDT was performed using a laser (635 nm, 18.75 J/cm2. The therapeutic response was analyzed by the water soluble tetrazolium salt (WST-1 cell viability assay 90 min after PDT. Results: 5-ALA-PDT was performed in 14 primary meningioma cell lines. EMA expression was verified in 10 primary cell cultures. The remaining 4 were EMA negative and PDT was without any effect in these cultures. All 10 EMA-positive cell lines showed a significant and dose-dependent decrease in viability rate (p < 0.001. Cell survival at 5-ALA concentrations of 12.5, 25, 50 and 100 μg/mL was 96.5% ± 7.6%, 67.9% ± 29.9%, 24.0% ± 16.7% and 13.8% ± 7.5%, respectively. For the negative controls (no 5-ALA/PDT and ALA/no PDT, the viability rates were 101.72% ± 3.5% and 100.17% ± 3.6%, respectively. The LD50 for 5-ALA was estimated between 25 and 50 µg/mL. Conclusion: This study reveals dose-dependent cytotoxic effects of 5-ALA-PDT on primary cell lines of meningiomas. Either 5-ALA or PDT alone did not affect cell survival. Further efforts are necessary to study the

  19. Safety and Efficacy of 5-Aminolevulinic Acid for High Grade Glioma in Usual Clinical Practice: A Prospective Cohort Study.

    Directory of Open Access Journals (Sweden)

    Pilar Teixidor

    Full Text Available During the last decade, the use of 5-aminolevulinic acid (5-ALA has been steadily increasing in neurosurgery. The study's main objectives were to prospectively evaluate the effectiveness and safety of 5-ALA when used in clinical practice setting on high-grade gliomas' patients.National, multicenter and prospective observational study.authorized conditions of use of 5-ALA.contraindication to 5-ALA, inoperable or partial resected tumors, pregnancy and children. Epidemiological, clinical, laboratory, radiological, and safety data were collected. Effectiveness was assessed using complete resection of the tumor, and progression-free and overall survival probabilities.Between May 2010 and September 2014, 85 patients treated with 5-ALA were included, and 77 were suitable for the effectiveness analysis. Complete resection was achieved in 41 patients (54%. Surgeons considered suboptimal the fluorescence of 5-ALA in 40% of the patients assessed. The median duration of follow-up was 12.3 months. The progression-free survival probability at 6 months was 58%. The median duration overall survival was 14.2 months. Progression tumor risk factors were grade of glioma, age and resection degree; and death risk factors were grade of glioma and gender. No severe adverse effects were reported. At one month after surgery, new or increased neurological morbidity was 6.5%. Hepatic enzymes were frequently increased within the first month after surgery; however, they subsequently normalized, and this was found to have no clinical significance.In clinical practice, the 5-ALA showed a good safety profile, but the benefits related to 5-ALA have not been yet clearly shown. The improved differentiation expected by fluorescence between normal and tumor cerebral tissue was suboptimal in a relevant number of patients; in addition, the expected higher degree of resection was lower than in clinical trials as well as incomplete resection was not identified as a prognostic factor

  20. [delta-Aminolevulinate dehydratase deficiency].

    Science.gov (United States)

    Fujita, H; Ishida, N; Akagi, R

    1995-06-01

    delta-Aminolevulinate dehydratase (ALAD: E. C. 4.2.1.24), the second enzyme in the heme biosynthetic pathway, condenses two moles of delta-aminolevulinic acid to form porphobilinogen. ALAD deficiency is well known to develop signs and symptoms of typical hepatic porphyria, and classified into three categories as follows: (i) ALAD porphyria, a genetic defect of the enzyme, (ii) tyrosinemia type I, a genetic defect of fumarylacetoacetase in the tyrosine catabolic pathway, producing succinylacetone (a potent inhibitor of ALAD), and (iii) ALAD inhibition by environmental hazards, such as lead, trichloroethylene, and styrene. In the present article, we will describe molecular and biochemical mechanisms to cause the enzyme defect to discuss the significance of ALAD defect on human health.

  1. In vitro skin permeation and retention of 5-aminolevulinic acid ester derivatives for photodynamic therapy.

    Science.gov (United States)

    De Rosa, Fernanda Scarmato; Tedesco, Antônio Cláudio; Lopez, Renata Fonseca Vianna; Pierre, Maria Bernadete Riemma; Lange, Norbert; Marchetti, Juliana Maldonado; Rotta, Jeane Cristina Gomes; Bentley, Maria Vitória Lopes Badra

    2003-04-29

    In photodynamic therapy (PDT), 5-aminiolevulinic acid (5-ALA) applied topically is converted, via the heme cycle, into protoporphyrin IX (PpIX), a photosensitizing agent, which upon excitation with light can induce tumor destruction. Due to its hydrophilic and zwitterionic characteristics, 5-ALA has limited penetration into the skin. More lipophilic 5-ALA ester derivatives are expected to cross stratum corneum more easily than 5-ALA. According to the determination of the partition coefficients of 5-ALA methyl, n-butyl, n-hexyl and n-octyl esters, these compounds showed an increased affinity to the SC, with 5-ALA hexyl ester and 5-ALA-octyl ester having the highest partition coefficients. Our in vitro skin permeation studies demonstrated an increased permeated amount for hexyl-ALA after 6 h of incubation, compared to other esters and 5-ALA. After 6 h, more 5-ALA-hexyl ester and -octyl ester were retained at viable epidermis and dermis than 5-ALA. According to these results, and considering that the conversion of 5-ALA into PpIX occurs preferentially in epidermis, it can be supposed that topical use of ester derivatives with longer chains (C(6) or C(8)) is an interesting proposal to optimize topical 5-ALA-PDT

  2. Analysis of the role of the Aspergillus niger aminolevulinic acid synthase (hemA) gene illustrates the difference between regulation of yeast and fungal haem- and sirohaem-dependent pathways

    NARCIS (Netherlands)

    Franken, A.C.; Christien Lokman, B.; Ram, A.F.; Hondel, C.A. van den; Weert, S. de; Punt, P.J.

    2012-01-01

    To increase knowledge on haem biosynthesis in filamentous fungi like Aspergillus niger, pathway-specific gene expression in response to haem and haem intermediates was analysed. This analysis showed that iron, 5′-aminolevulinic acid (ALA) and possibly haem control haem biosynthesis mostly via modula

  3. Bi-functional prodrugs of 5-aminolevulinic acid and butyric acid increase erythropoiesis in anemic mice in an erythropoietin-independent manner.

    Science.gov (United States)

    Rephaeli, Ada; Tarasenko, Nataly; Fibach, Eitan; Rozic, Gabriela; Lubin, Ido; Lipovetsky, Julia; Furman, Svetlana; Malik, Zvi; Nudelman, Abraham

    2016-08-25

    Anemia is a major cause of morbidity and mortality worldwide resulting from a wide variety of pathological conditions. In severe cases it is treated by blood transfusions or injection of erythroid stimulating agents, e.g., erythropoietin (Epo), which can be associated with serious adverse effects. Therefore, there is a need to develop new treatment modalities. We recently reported that treatment of erythroleukemic cells with the novel the bi-functional prodrugs of 5-aminolevulinic acid (ALA) and butyric acid (BA), AN233 and AN908, enhanced hemoglobin (Hb) synthesis to a substantially higher level than did ALA and BA individually or their mixture. Herein, we describe that these prodrugs when given orally to mice induced histone deacetylase inhibition in the kidneys, bone marrow and spleen, thus, indicating good penetrability to the tissues. In mice where anemia was chemically induced, treatment with the prodrugs increased the Hb, the number of red blood cells (RBCs) and the percentage of reticulocytes to normal levels. The prodrugs had no adverse effects even after repeated treatment at 100-200mg/kg for 50days. The lack of increased levels of Epo in the blood of mice that were treated with the prodrugs suggests that AN233 and AN908 affected the Hb and RBC levels in an Epo-independent manner. Taken together with our previous studies, we propose that the prodrugs increase globin expression by BA inhibition of histone deacetylase and elevation heme synthesis by ALA. These results support an Epo-independent approach for treating anemia with these prodrugs. Copyright © 2016 Elsevier B.V. All rights reserved.

  4. Constitutive expression of RyhB regulates the heme biosynthesis pathway and increases the 5-aminolevulinic acid accumulation in Escherichia coli.

    Science.gov (United States)

    Li, Fangfang; Wang, Yang; Gong, Kai; Wang, Qian; Liang, Quanfeng; Qi, Qingsheng

    2014-01-01

    In the current study, the small RNA ryhB, which regulates the metabolism of iron in Escherichia coli, was constitutively expressed in engineered E. coli DALA. The resulting strain E. coli DALRA produced 16% more 5-aminolevulinic acid (ALA) than the parent strain E. coli DALA in batch fermentation. Meanwhile, we found that addition of iron in the medium increased heme formation and reduced ALA yield, whereas the presence of iron chelator in the medium decreased heme concentration and increased the ALA production efficiency (ALA yield per OD600). The qRT-PCR analysis showed that the mRNA levels of hemB and hemH were also decreased as well as the known RyhB target genes of acnAB, sdhAB, fumA, and cydAB in E. coli DALRA. These results indicated that small RNA can be used as a tool for regulating ALA accumulation in E. coli.

  5. Improvement of manganese peroxidase production by the hyper lignin-degrading fungus Phanerochaete sordida YK-624 by recombinant expression of the 5-aminolevulinic acid synthase gene.

    Science.gov (United States)

    Hirai, Hirofumi; Misumi, Kenta; Suzuki, Tomohiro; Kawagishi, Hirokazu

    2013-12-01

    The manganese peroxidase (MnP) gene (mnp4) promoter of Phanerochaete sordida YK-624 was used to drive expression of 5-aminolevulinic acid synthase (als), which is a key heme biosynthesis enzyme. The expression plasmid pMnP4pro-als was transformed into P. sordida YK-624 uracil auxotrophic mutant UV-64, and 14 recombinant als expressing-transformants were generated. Average cumulative MnP activities in the transformants were 1.18-fold higher than that of control transformants. In particular, transformants A-14 and A-61 showed significantly higher MnP activity (approximately 2.8-fold) than wild type. RT-PCR analysis indicated that the increased MnP activity was caused by elevated recombinant als expression. These results suggest that the production of MnP is improved by high expression of als.

  6. Comparison of neurotropic effects of L-glutamic acid and its new derivative β-phenylglutamic acid hydrochloride (RGPU-135, glutarone).

    Science.gov (United States)

    Tyurenkov, I N; Bagmetova, V V; Chernysheva, Yu V; Merkushenkova, O V

    2014-04-01

    In contrast to L-glutamic acid (200 mg/kg), β-phenylglutamic acid hydrochloride (26 mg/kg) produces no anticonvulsant effects during generalized convulsions induced by "maximum electric shock". However, β-phenylglutamic acid hydrochloride was more potent than L-glutamic acid in increasing survival rate, promoting recovery of spontaneous motor activity, and maintainance locomotor and exploratory activity in the open field test and cognitive functions in conditioned passive avoidance test, i.e. exhibited neuroprotective activity. This substance did not change the threshold of pain induced by electric stimulation of paws (up to vocalization) and thermal tail stimulation (tail-flick), whereas L-glutamic acid decreased this parameter. β-Phenylglutamic acid suppressed aggression in the test for provoked unmotivated aggression, while L-glutamic acid enhanced it. Due to these neurotropic effects, β-phenylglutamic acid hydrochloride can be used as the basis for the development of drugs with antidepressant, anxiolytic, and neuroprotective actions.

  7. Hydroxylamine hydrochloride-acetic acid-soluble and -insoluble fractions of pelagic sediment: Readsorption revisited

    Science.gov (United States)

    Piper, D.Z.; Wandless, G.A.

    1992-01-01

    The extraction of the rare earth elements (REE) from deep-ocean pelagic sediment, using hydroxylamine hydrochloride-acetic acid, leads to the separation of approximately 70% of the bulk REE content into the soluble fraction and 30% into the insoluble fraction. The REE pattern of the soluble fraction, i.e., the content of REE normalized to average shale on an element-by-element basis and plotted against atomic number, resembles the pattern for seawater, whereas the pattern, as well as the absolute concentrations, in the insoluble fraction resembles the North American shale composite. These results preclude significant readsorption of the REE by the insoluble phases during the leaching procedure.

  8. Spectrophotometric determination of procaine hydrochloride in pharmaceutical products using 1,2-naphthoquinone-4-sulfonic acid as the chromogenic reagent

    Science.gov (United States)

    Xu, Li Xiao; Shen, Yun Xiu; Wang, Huai You; Jiang, Ji Gang; Xiao, Yan

    2003-11-01

    Spectrophotometric determination of procaine hydrochloride is described. The procaine hydrochloride reacts with 1,2-naphthoquinone-4-sulfonic acid in pH 3.60 buffer solution to form a salmon pink compound, and its maximum absorption wavelength is at 484 nm, ɛ 484=5.22×10 3.The absorbance for procaine hydrochloride from 0.30 to 100 μg ml -1 obeys Beer's law. The linear regression equation of the calibration graph is C=19.23A-0.03, with a linear regression correlative coefficient is 0.9996, the detection limit is 0.28 μg ml -1; recovery is from 98.0 to 105.2%. Effects of pH, surfactant, organic solvent, foreign ions, and standing time on the determination of procaine hydrochloride have been examined. This method is rapid and simple, and can be used for the determination of procaine hydrochloride in injection solution of procaine hydrochloride. The results obtained by this method agreed with those by the official method (dead-stop titration).

  9. Oxidation of Tetracaine Hydrochloride by Chloramine-B in Acid Medium: Kinetic Modeling

    Directory of Open Access Journals (Sweden)

    Jayachamarajapura Pranesh Shubha

    2014-01-01

    Full Text Available Tetracaine hydrochloride (TCH is one of the potent local anaesthetics. A kinetic study of oxidation of tetracaine hydrochloride by sodium N-chlorobenzenesulfonamide (chloramine-B or CAB has been carried in HClO4 medium at 303 K. The rate shows first-order dependence on [CAB]o, shows fractional–order dependence on [substrate]o, and is self-governing on acid concentration. Decrease of dielectric constant of the medium, by adding methanol, increased the rate. Variation of ionic strength and addition of benzenesulfonamide or NaCl have no significant effect on the rate. The reaction was studied at different temperatures and the activation parameters have been evaluated. The stoichiometry of the reaction was found to be 1 : 5 and the oxidation products were identified by spectral analysis. The conjugate free acid C6H5SO2NHCl of CAB is postulated as the reactive oxidizing species. The observed results have been explained by plausible mechanism and the related rate law has been deduced.

  10. Simultaneous derivative spectrophotometric analysis of doxylamine succinate, pyridoxine hydrochloride and folic Acid in combined dosage forms.

    Science.gov (United States)

    Pathak, A; Rajput, S J

    2008-01-01

    Two UV spectrophotometric methods have been developed, based on first derivative spectrophotometry for simultaneous estimation of doxylamine succinate, pyridoxine hydrochloride, and folic acid in tablet formulations. In method I, the concentrations of these drugs were determined by using linear regression equation. Method II is also based on first derivative spectrophotometry however simultaneous equations (Vierdot's method) were derived on derivative spectra. The first derivative amplitudes at 270.0, 332.8 and 309.2 nm were utilized for simultaneous estimation of these drugs respectively by both methods. In both the methods, linearity was obtained in the concentration range 2.5-50 mug/ml, 1-40 mug/ml and 1-30 mug/ml for doxylamine succinate, pyridoxine hydrochloride, and folic acid respectively. The developed methods show best results in terms of linearity, accuracy, precision, LOD, LOQ and ruggedness for standard laboratory mixtures of pure drugs and marketed formulations. The common excipients and additives did not interfere in their determinations.

  11. Simultaneous derivative spectrophotometric analysis of doxylamine succinate, pyridoxine hydrochloride and folic acid in combined dosage forms

    Directory of Open Access Journals (Sweden)

    Pathak A

    2008-01-01

    Full Text Available Two UV spectrophotometric methods have been developed, based on first derivative spectrophotometry for simultaneous estimation of doxylamine succinate, pyridoxine hydrochloride, and folic acid in tablet formulations. In method I, the concentrations of these drugs were determined by using linear regression equation. Method II is also based on first derivative spectrophotometry however simultaneous equations (Vierdot′s method were derived on derivative spectra. The first derivative amplitudes at 270.0, 332.8 and 309.2 nm were utilized for simultaneous estimation of these drugs respectively by both methods. In both the methods, linearity was obtained in the concentration range 2.5-50 µg/ml, 1-40 µg/ml and 1-30 µg/ml for doxylamine succinate, pyridoxine hydrochloride, and folic acid respectively. The developed methods show best results in terms of linearity, accuracy, precision, LOD, LOQ and ruggedness for standard laboratory mixtures of pure drugs and marketed formulations. The common excipients and additives did not interfere in their determinations.

  12. Ivabradine Hydrochloride (S-Mandelic Acid Co-Crystal: In Situ Preparation during Formulation

    Directory of Open Access Journals (Sweden)

    Veronika Sládková

    2017-01-01

    Full Text Available The pharmaceutical salt ivabradine hydrochloride is indicated for the symptomatic treatment of chronic stable angina pectoris and chronic heart failure. It exhibits extensive polymorphism and co-crystallization, which could be a way to provide an alternative solid form. We conducted a co-crystal screen, from which two hits were identified: with (S-mandelic and (R-mandelic acid. Both structures were determined from single-crystal X-ray diffraction data as co-crystals. The co-crystals were further characterized by common solid-state techniques, such as X-ray powder diffraction (XRPD, differential scanning calorimetry (DSC, solid-state NMR, IR and Raman spectroscopy, and dynamic vapor sorption (DVS. The co-crystal with (S-mandelic acid was selected for further development; its physical and chemical stability was compared with two different polymorphs of the hydrochloride salt. The co-crystal exhibited a similar stability with the polymorph used in the original drug product and was, therefore, selected for formulation into the drug product. During the pre-formulation experiments, the in situ formation of the co-crystal was achieved during the wet granulation process. The following formulation experiments showed no influence of in situ prepared co-crystal on the overall stability of the bulk, when compared with pre-prepared co-crystal formulation.

  13. Promotion by 5-Aminolevulinic Acid of Germination of Pakchoi (Brassica campestris ssp. chinensis var. communis Tsen et Lee) Seeds Under Salt Stress

    Institute of Scientific and Technical Information of China (English)

    Liang-Ju WANG; Wei-Bing JIANG; Hui LIU; Wei-Qin LIU; Lang KANG; Xi-Lin HOU

    2005-01-01

    The seed germination and seedling growth of pakchoi (Brassica campestris ssp. chinensis var.communis Tsen et Lee cv. Hanxiao) were not significantly inhibited until the concentration of NaCl was increased to150 mmol/L. Treatment of pakchoi seeds with exogenous 5-aminolevulinic acid (ALA), at concentrations ranging from 0.01 to 10.00 mg/L, promoted seed germination when seeds were stressed by salinity, whereas levulinic acid (LA), an inhibitor of ALA dehydrase, significantly inhibited seed germination and seedling growth, suggesting that metabolism of ALA into porphyrin compounds was necessary for seed germination and seedling growth. Determination of respiratory rate during seed germination showed that ALA increased seed respiration under both normal conditions and salt stress. Furthermore, salt stress decreased levels of endogenous ALA, as well as heme, in etiolated seedlings. More salt-tolerant cultivars of pakchoi contained higher relative levels of endogenous ALA and heme under conditions of salt stress.These results indicate that salt stress may inhibit the biosynthesis of endogenous ALA and then heme,which is necessary for seed germination, and treatment of seeds with exogenous ALA prior to germination may be associated with the biosynthesis of heme.

  14. Stratum corneum lipids liposomes for the topical delivery of 5-aminolevulinic acid in photodynamic therapy of skin cancer: preparation and in vitro permeation study

    Directory of Open Access Journals (Sweden)

    Bentley M Vitória LB

    2001-08-01

    Full Text Available Abstract Background Photodynamic therapy (PDT using 5-aminolevulinic acid (5-ALA is a skin cancer therapy that still has limitations due to the low penetration of this drug into the skin. We have proposed in this work a delivery system for 5-ALA based on liposomes having lipid composition similar to the mammalian stratum corneum (SCLLs in order to optimize its skin delivery in Photodynamic Therapy (PDT of skin cancers. Methods SCLLs were obtained by reverse phase evaporation technique and size distribution of the vesicles was determinated by photon correlation spectroscopy. In vitro permeation profile was characterized using hairless mouse skin mounted in modified Franz diffusion cell. Results Size exclusion chromatography on gel filtration confirmed vesicle formation. SCLLs obtained by presented a degree of encapsulation of 5-ALA around 5.7%. A distribution of vesicle size centering at around 500 nm and 400 nm respectively for SCLLs and SCLLs containing 5-ALA was found. In vitro 5-ALA permeation study showed that SCLLs preparations presented higher skin retention significantly (p Conclusions The in vitro delivery performance provided by SCLLs lead to consider this systems adequate for the 5-ALA-PDT of skin cancer, since SCLLs have delivered 5-ALA to the target skin layers (viable epidermis + dermis to be treated by topical PDT of skin cancer.

  15. Promotive role of 5-aminolevulinic acid on chromium-induced morphological, photosynthetic, and oxidative changes in cauliflower (Brassica oleracea botrytis L.).

    Science.gov (United States)

    Ahmad, Rehan; Ali, Shafaqat; Hannan, Fakhir; Rizwan, Muhammad; Iqbal, Muhammad; Hassan, Zaidul; Akram, Nudrat Aisha; Maqbool, Saliha; Abbas, Farhat

    2017-03-01

    Chromium (Cr) is among the most toxic pollutants in the environment that adversely affect the living organisms and physiological processes in different plants. The present study investigated the effect of 15 mg L(-1) of 5-aminolevulinic acid (ALA) on morpho-physiological attributes of cauliflower (Brassica oleracea botrytis L.) under different Cr concentrations (0, 10, 100, and 200 μM) in the growth medium. The results showed that Cr stress decreased the growth, biomass, photosynthetic, and gas exchange parameters. Chromium stress enhanced the activities of enzymatic antioxidants, catalase (CAT), superoxide dismutase (SOD), and peroxidase (POD) in response to oxidative stress caused by the elevated levels of malondialdehyde (MDA), hydrogen peroxide (H2O2), and electrolyte leakage (EL) in both roots and leaves of cauliflower. Chromium concentrations and total Cr uptake were increased in leaves, stems, and roots with increasing Cr levels in the culture medium. Foliar application of ALA increased the plant growth parameters, biomass, gas exchange parameters, and photosynthetic pigments under Cr stress compared to the treatments without ALA. Foliar application ALA decreased the levels of MDA, EL, and H2O2 while further improved the performance of antioxidant in both leaves and roots compared to only Cr-stressed plant. Chromium concentrations and total Cr uptake were decreased by the ALA application compared to treatments without ALA application. The results of the present study indicated that foliar application of ALA might be beneficial in minimizing Cr uptake and its toxic effects in cauliflower.

  16. Transporter-Mediated Drug Interaction Strategy for 5-Aminolevulinic Acid (ALA-Based Photodynamic Diagnosis of Malignant Brain Tumor: Molecular Design of ABCG2 Inhibitors

    Directory of Open Access Journals (Sweden)

    Toshihisa Ishikawa

    2011-09-01

    Full Text Available Photodynamic diagnosis (PDD is a practical tool currently used in surgical operation of aggressive brain tumors, such as glioblastoma. PDD is achieved by a photon-induced physicochemical reaction which is induced by excitation of protoporphyrin IX (PpIX exposed to light. Fluorescence-guided gross-total resection has recently been developed in PDD, where 5-aminolevulinic acid (ALA or its ester is administered as the precursor of PpIX. ALA induces the accumulation of PpIX, a natural photo-sensitizer, in cancer cells. Recent studies provide evidence that adenosine triphosphate (ATP-binding cassette (ABC transporter ABCG2 plays a pivotal role in regulating the cellular accumulation of porphyrins in cancer cells and thereby affects the efficacy of PDD. Protein kinase inhibitors are suggested to potentially enhance the PDD efficacy by blocking ABCG2-mediated porphyrin efflux from cancer cells. It is of great interest to develop potent ABCG2-inhibitors that can be applied to PDD for brain tumor therapy. This review article addresses a pivotal role of human ABC transporter ABCG2 in PDD as well as a new approach of quantitative structure-activity relationship (QSAR analysis to design potent ABCG2-inhibitors.

  17. The Safety and Tolerability of 5-Aminolevulinic Acid Phosphate with Sodium Ferrous Citrate in Patients with Type 2 Diabetes Mellitus in Bahrain

    Directory of Open Access Journals (Sweden)

    Feryal Al-Saber

    2016-01-01

    Full Text Available Type 2 diabetes mellitus is prevalent especially in Gulf countries and poses serious long-term risks to patients. A multifaceted treatment approach can include nutritional supplements with antioxidant properties such as 5-aminolevulinic acid (5-ALA with sodium ferrous citrate (SFC. This prospective, randomized, single-blind, placebo-controlled, dose escalating pilot clinical trial assessed the safety of 5-ALA with SFC at doses up to 200 mg 5-ALA/229.42 mg SFC per day in patients living in Bahrain with type 2 diabetes mellitus that was uncontrolled despite the use of one or more antidiabetic drugs. Fifty-three patients (n=53 from 3 sites at one center were enrolled by Dr. Feryal (Site #01, Dr. Hesham (Site #02, and Dr. Waleed (Site #03 (n=35, 5-ALA-SFC; n=18, placebo. There was no significant difference in incidence of adverse events reported, and the most frequent events reported were gastrointestinal in nature, consistent with the known safety profile of 5-ALA in patients with diabetes. No significant changes in laboratory values and no difference in hypoglycemia between patients receiving 5-ALA and placebo were noted. Overall, the current results support that use of 5-ALA-SFC up to 200 mg per day taken as 2 divided doses is safe in patients taking concomitant oral antidiabetic medications and may offer benefits in the diabetic population. This trial is registered with ClinicalTrials.gov NCT02481141.

  18. Fractionated illumination after topical application of 5-aminolevulinic acid on normal skin of hairless mice: the influence of the dark interval.

    Science.gov (United States)

    de Bruijn, H S; van der Ploeg-van den Heuvel, A; Sterenborg, H J C M; Robinson, D J

    2006-12-01

    We have previously shown that light fractionation during topical aminolevulinic acid based photodynamic therapy (ALA-PDT) with a dark interval of 2h leads to a significant increase in efficacy in both pre-clinical and clinical PDT. However this fractionated illumination scheme required an extended overall treatment time. Therefore we investigated the relationship between the dark interval and PDT response with the aim of reducing the overall treatment time without reducing the efficacy. Five groups of mice were treated with ALA-PDT using a single light fraction or the two-fold illumination scheme with a dark interval of 30 min, 1, 1.5 and 2h. Protoporphyrin IX fluorescence kinetics were monitored during illumination. Visual skin response was monitored in the first seven days after PDT and assessed as PDT response. The PDT response decreases with decreasing length of the dark interval. Only the dark interval of 2h showed significantly more damage compared to all the other dark intervals investigated (Pdark interval used. We conclude that in the skin of the hairless mouse the dark interval cannot be reduced below 2h without a significant reduction in PDT efficacy.

  19. Alleviation of Lead Toxicity by 5-Aminolevulinic Acid Is Related to Elevated Growth, Photosynthesis, and Suppressed Ultrastructural Damages in Oilseed Rape

    Directory of Open Access Journals (Sweden)

    Tian Tian

    2014-01-01

    Full Text Available Lead (Pb is a widely spread pollutant and leads to diverse morphological and structural changes in the plants. In this study, alleviating role of 5-aminolevulinic acid (ALA in oilseed rape (Brassica napus L. was investigated with or without foliar application of ALA (25 mg L−1 in hydroponic environment under different Pb levels (0, 100, and 400 µM. Outcomes stated that plant morphology and photosynthetic attributes were reduced under the application of Pb alone. However, ALA application significantly increased the plant growth and photosynthetic parameters under Pb toxicity. Moreover, ALA also lowered the Pb concentration in shoots and roots under Pb toxicity. The microscopic studies depicted that exogenously applied ALA ameliorated the Pb stress and significantly improved the cell ultrastructures. After application of ALA under Pb stress, mesophyll cell had well-developed nucleus and chloroplast having a number of starch granules. Moreover, micrographs illustrated that root tip cell contained well-developed nucleus, a number of mitochondria, and golgi bodies. These results proposed that under 15-day Pb-induced stress, ALA improved the plant growth, chlorophyll content, photosynthetic parameters, and ultrastructural modifications in leaf mesophyll and root tip cells of the B. napus plants.

  20. No-Needle Jet Intradermal Aminolevulinic Acid Photodynamic Therapy for Recurrent Nodular Basal Cell Carcinoma of the Nose: A Case Report

    Directory of Open Access Journals (Sweden)

    Daniel Barolet

    2011-01-01

    Full Text Available Photodynamic therapy (PDT with aminolevulinic acid (ALA to treat nodular basal cell carcinoma (BCC has been shown to be beneficial. The success rate of ALA-PDT in the treatment of nodular BCC is dependent on optimal penetration of the photosensitizing agent and subsequent PpIX production. To enhance topical delivery of drugs intradermally, a needleless jet injection (NLJI, which employs a high-speed jet to puncture the skin without the side effects of needles, was used in one patient with recurrent BCC of the nose. Photoactivation was then performed using red light emitting diode [CW @ λ 630 nm, irradiance 50 mW/cm2, total fluence 51 J/cm2] for 17 minutes. Excellent cosmesis was obtained. Aside from mild crusting present for six days, no other adverse signs were noted. Clinically, there was no recurrent lesion up two years postintervention. Additional studies in larger samples of subjects are needed to further evaluate this promising technique.

  1. The Safety and Tolerability of 5-Aminolevulinic Acid Phosphate with Sodium Ferrous Citrate in Patients with Type 2 Diabetes Mellitus in Bahrain

    Science.gov (United States)

    Al-Saber, Feryal; Aldosari, Waleed; Alselaiti, Mariam; Khalfan, Hesham; Kaladari, Ahmed; Khan, Ghulam; Harb, George; Rehani, Riyadh; Kudo, Sizuka; Koda, Aya; Tanaka, Tohru

    2016-01-01

    Type 2 diabetes mellitus is prevalent especially in Gulf countries and poses serious long-term risks to patients. A multifaceted treatment approach can include nutritional supplements with antioxidant properties such as 5-aminolevulinic acid (5-ALA) with sodium ferrous citrate (SFC). This prospective, randomized, single-blind, placebo-controlled, dose escalating pilot clinical trial assessed the safety of 5-ALA with SFC at doses up to 200 mg 5-ALA/229.42 mg SFC per day in patients living in Bahrain with type 2 diabetes mellitus that was uncontrolled despite the use of one or more antidiabetic drugs. Fifty-three patients (n = 53) from 3 sites at one center were enrolled by Dr. Feryal (Site #01), Dr. Hesham (Site #02), and Dr. Waleed (Site #03) (n = 35, 5-ALA-SFC; n = 18, placebo). There was no significant difference in incidence of adverse events reported, and the most frequent events reported were gastrointestinal in nature, consistent with the known safety profile of 5-ALA in patients with diabetes. No significant changes in laboratory values and no difference in hypoglycemia between patients receiving 5-ALA and placebo were noted. Overall, the current results support that use of 5-ALA-SFC up to 200 mg per day taken as 2 divided doses is safe in patients taking concomitant oral antidiabetic medications and may offer benefits in the diabetic population. This trial is registered with ClinicalTrials.gov NCT02481141.

  2. 提高氨基酮戊酸透皮能力的方法%Methods to improve transdermal delivery of aminolevulinic acid

    Institute of Scientific and Technical Information of China (English)

    石磊; 王秀丽; 王宏伟

    2012-01-01

    氨基酮戊酸光动力治疗在皮肤科领域应用广泛,由于氨基酮戊酸透皮能力低,限制氨基酮戊酸光动力治疗的疗效.氨基酮戊酸衍生物,微针、激光、离子导入和运输载体技术相继被应用于提高氨基酮戊酸的透皮能力,并且取得了一定的效果.它们可通过不同的机制提高氨基酮戊酸透皮的深度和透皮的量,使氨基酮戊酸光动力治疗能更有效地应用于皮肤科领域.%Aminolevulinic acid-based photodynamic therapy (ALA-PDT) has been extensively applied in dermatology.However,the low permeability of ALA across intact skin has limited the efficacy of ALA-PDT.To enhace the percutaneous penetration of ALA,esterified derivatives,microneedles,laser,iontophoresis,delivery vehicles have been used in succession,and some achievements have been made.These methods can increase the transdermal delivery of ALA in terms of depth and quantity by different mechanisms,and indirectly promote the efficacy of ALA-PDT in dermatoses.

  3. Production of uroporphyrinogen III, which is the common precursor of all tetrapyrrole cofactors, from 5-aminolevulinic acid by Escherichia coli expressing thermostable enzymes.

    Science.gov (United States)

    Hibino, Aiko; Petri, René; Büchs, Jochen; Ohtake, Hisao

    2013-08-01

    Uroporphyrinogen III (urogen III) was produced from 5-aminolevulinic acid (ALA), which is a common precursor of all metabolic tetrapyrroles, using thermostable ALA dehydratase (ALAD), porphobilinogen deaminase (PBGD), and urogen III synthase (UROS) of Thermus thermophilus HB8. The UROS-coding gene (hemD₂) of T. thermophilus HB8 was identified by examining the gene product for its ability to produce urogen III in a coupled reaction with ALAD and PBGD. The genes encoding ALAD, PBGD, and UROS were separately expressed in Escherichia coli BL21 (DE3). To inactivate indigenous mesophilic enzymes, the E. coli transformants were heated at 70 °C for 10 min. The bioconversion of ALA to urogen III was performed using a mixture of heat-treated E. coli transformants expressing ALAD, PBGD, and UROS at a cell ratio of 1:1:1. When the total cell concentration was 7.5 g/l, the mixture of heat-treated E. coli transformants could convert about 88 % 10 mM ALA to urogen III at 60 °C after 4 h. Since eight ALA molecules are required for the synthesis of one porphyrin molecule, approximately 1.1 mM (990 mg/l) urogen III was produced from 10 mM ALA. The present technology has great potential to supply urogen III for the biocatalytic production of vitamin B₁₂.

  4. Bucher's indirect comparison of daylight photodynamic therapy with methyl aminolevulinate cream versus diclofenac plus hyaluronic acid gel for the treatment of multiple actinic keratosis.

    Science.gov (United States)

    Calzavara-Pinton, Piergiacomo; Zane, Cristina; Pacou, Maud; Szeimies, Rolf-Markus

    2016-10-01

    Actinic keratosis (AK) is a pre-cancerous condition characterised by patches of thick, scaly skin developing on sun-exposed areas of the body. When multiple AKs develop on severely photodamaged skin, commonly used treatments include photodynamic therapy and diclofenac plus hyaluronic acid gel (DHA). Methyl aminolevulinate daylight photodynamic therapy (MAL DL-PDT) is an alternative to conventional photodynamic therapy (MAL c-PDT). Trials have indicated that MAL DL-PDT is as effective as MAL c-PDT but reduces treatment-related pain and dermatological side effects. To indirectly compare between MAL DL-PDT and DHA in patients with AK. A total of three randomised trials were collected using a systematic literature review. An adjusted indirect comparison was conducted on complete lesion response rate at 12 weeks. The data indicated that mild lesions, moderate lesions, and mild and moderate lesions treated with MAL DL-PDT were more than four times more likely to undergo a complete response than lesions treated with DHA at 12 weeks, with ORs ranging from 4.23 to 4.81. Results were all statistically significant. This is the first indirect comparison demonstrating the effectiveness of MAL-PDT over DHA for the treatment of AK, and further research is needed to assess the long-term efficacy of these interventions (i.e. six months and beyond), as well as safety and patient-reported outcomes.

  5. Topical glycerol monooleate/propylene glycol formulations enhance 5-aminolevulinic acid in vitro skin delivery and in vivo protophorphyrin IX accumulation in hairless mouse skin.

    Science.gov (United States)

    Steluti, Regilene; De Rosa, Fernanda Scarmato; Collett, John; Tedesco, Antônio Cláudio; Bentley, Maria Vitória Lopes Badra

    2005-08-01

    Photodynamic therapy (PDT), a potential therapy for cancer treatment, utilizes exogenously applied or endogenously formed photosensitizers, further activated by light in an appropriate wavelength and dose to induce cell death through free radical formation. 5-Aminolevulinic acid (5-ALA) is a pro-drug which can be converted to the effective photosensitizer, protoporphyrin IX (PpIX). However, the use of 5-ALA in PDT is limited by the low penetration capacity of this highly hydrophilic molecule into appropriate skin layers. In the present study, we propose to increase 5-ALA penetration by using formulations containing glycerol monooleate (GMO), an interesting and useful component of pharmaceutical formulations. Propylene glycol solutions containing different concentrations of GMO significantly increased the in vitro skin permeation/retention of 5-ALA in comparison to control solutions. In vivo studies also showed increased PpIX accumulation in mouse hairless skin, after the use of topical 5-ALA formulations containing GMO in a concentration-dependent manner. The results show that skin 5-ALA penetration and PpIX accumulation, important factors for the success of topical 5-ALA-PDT in skin cancer, are optimized by GMO/propylene glycol formulations.

  6. ABSORPTION RATIO METHOD FOR ESTIMATION OF DROTAVERINE HYDROCHLORIDE AND MEFENAMIC ACID IN THEIR COMBINED TABLET DOSAGE FORM

    OpenAIRE

    Sakhare Ram Suresh; Jamkhande Prasad Govindrao

    2012-01-01

    A new, simple, accurate and sensitive UV-spectrophotometric absorption Ratio method has been developed for simultaneous determination of Drotaverine Hydrochloride and Mefenamic Acid in their combined Tablet dosage form. The method is based upon determination of Drotaverine HCl and Mefenamic Acid at 239 nm, and 280nm in Methanol. Drotaverine HCl and Mefenamic Acid at isoabsorptive λmax 239 nm and at 280 nm λmax Mefenamic acid shows linearity in the concentration range of 3-30 μg/ml and 3 -30...

  7. ABSORPTION RATIO METHOD FOR ESTIMATION OF DROTAVERINE HYDROCHLORIDE AND MEFENAMIC ACID IN THEIR COMBINED TABLET DOSAGE FORM

    Directory of Open Access Journals (Sweden)

    Sakhare Ram Suresh

    2012-10-01

    Full Text Available A new, simple, accurate and sensitive UV-spectrophotometric absorption Ratio method has been developed for simultaneous determination of Drotaverine Hydrochloride and Mefenamic Acid in their combined Tablet dosage form. The method is based upon determination of Drotaverine HCl and Mefenamic Acid at 239 nm, and 280nm in Methanol. Drotaverine HCl and Mefenamic Acid at isoabsorptive λmax 239 nm and at 280 nm λmax Mefenamic acid shows linearity in the concentration range of 3-30 μg/ml and 3 -30 μg/ml respectively. The method was validated statistically.

  8. Development and validation of a liquid chromatographic method for estimation of dicyclomine hydrochloride, mefenamic Acid and paracetamol in tablets.

    Science.gov (United States)

    Shah, D A; Rana, Jainika P; Chhalotiya, Usmangani K; Baldania, S L; Bhatt, K K

    2014-01-01

    Liquid chromatographic method was developed for simultaneous quantitative determination of dicyclomine hydrochloride, mefenamic acid and paracetamol in their combined dosage form. The separation was achieved using a C18 column (250×4.6 mm id, 5 μm) using acetonitrile:20 mM potassium dihydrogen phosphate 70:30 (v/v) adjusted to pH 4 using orthophosphoric acid as mobile phase at a flow rate of 1 ml/min and detection at 220 nm. Separation was completed within 12 min. The retention times of dicyclomine hydrochloride, mefenamic acid and paracetamol were 3.8, 9.3 and 2.5 minutes respectively. The proposed method was found to have linearity in concentration range of 10-100 μg/ml for dicyclomine hydrochloride, 0.05-10 μg/ml for mefenamic acid and 0.1-20 μg/ml for paracetamol. The developed method has been statistically validated and was found to be simple, precise, reproducible and accurate. The developed and validated method was successfully used for the quantitative analysis of commercially available dosage form.

  9. Spectrophotometric Determination of Gemifloxacin Mesylate, Moxifloxacin Hydrochloride, and Enrofloxacin in Pharmaceutical Formulations Using Acid Dyes

    Directory of Open Access Journals (Sweden)

    Ayman A. Gouda

    2014-01-01

    Full Text Available Simple, rapid, and extractive spectrophotometric methods were developed for the determination of some fluoroquinolones antibiotics: gemifloxacin mesylate (GMF, moxifloxacin hydrochloride (MXF, and enrofloxacin (ENF in pure forms and pharmaceutical formulations. These methods are based on the formation of ion-pair complexes between the basic drugs and acid dyes, namely, bromocresol green (BCG, bromocresol purple (BCP, bromophenol blue (BPB, bromothymol blue (BTB, and methyl orange (MO in acidic buffer solutions. The formed complexes were extracted with chloroform and measured at 420, 408, 416, 415, and 422 nm for BCG, BCP, BPB, BTB, and MO, respectively, for GMF; at 410, 415, 416, and 420 nm for BCP, BTB, BPB, and MO, respectively, for MXF; and at 419 and 414 nm for BCG and BTB, respectively, in case of ENF. The analytical parameters and their effects are investigated. Beer’s law was obeyed in the ranges 1.0–30, 1.0–20, and 2.0–24 μg mL−1 for GMF, MXF, and ENF, respectively. The proposed methods have been applied successfully for the analysis of the studied drugs in pure forms and pharmaceutical formulations. Statistical comparison of the results with the reference methods showed excellent agreement and indicated no significant difference in accuracy and precision.

  10. [Inhibition rate of gamma-aminolevulinic acid dehydratase activity in erythrocytes as a reliable index for individual workers of low lead exposure].

    Science.gov (United States)

    Hirano, H; Omichi, M; Ohishi, H; Ishikawa, K; Hirashima, N

    1983-09-01

    As the delta-aminolevulinic acid dehydratase (ALAD) activity in erythrocytes is decreased by lead exposure, we considered that a net reduction of ALAD activity by lead in blood should be the difference between the activity fully activated with zinc (Zn2+) and dithiothreitol (DTT) and that without activation. The optimal condition of activation of ALAD was found by addition of 0.25 mM of Zn2+ and 10 mM of DTT in the reaction mixture. Judging from our previous results that the amount of inhibition of ALAD activity can be represented as the rate of inhibition and is closely correlated with the dose of lead administered to rabbits, the inhibition rate of ALAD activity and lead content in blood (Pb-B) of lead workers were measured. The scatter diagram obtained from the inhibition rate and lead content in blood has two groups being divided at 50 micrograms/ml of Pb-B. In one group less than 50 micrograms/100 ml of Pb-B, the inhibition rate has been closely related to Pb-B., the regression equation being Y = 1.82 X + 11.7, and the correlation coefficient + 0.926. In another group more than 50 micrograms/100 ml of Pb-B the inhibition rate remained constant at the 90% level. Measurement of the inhibition rate suggests to have practical validity for monitoring lead exposure in workers, and by means of a nomograph lead content in blood can be estimated from the inhibition rate.

  11. Nuclear receptor 5A (NR5A) family regulates 5-aminolevulinic acid synthase 1 (ALAS1) gene expression in steroidogenic cells.

    Science.gov (United States)

    Ju, Yunfeng; Mizutani, Tetsuya; Imamichi, Yoshitaka; Yazawa, Takashi; Matsumura, Takehiro; Kawabe, Shinya; Kanno, Masafumi; Umezawa, Akihiro; Kangawa, Kenji; Miyamoto, Kaoru

    2012-11-01

    5-Aminolevulinic acid synthase 1 (ALAS1) is a rate-limiting enzyme for heme biosynthesis in mammals. Heme is essential for the catalytic activities of P450 enzymes including steroid metabolic enzymes. Nuclear receptor 5A (NR5A) family proteins, steroidogenic factor-1 (SF-1), and liver receptor homolog-1 (LRH-1) play pivotal roles in regulation of steroidogenic enzymes. Recently, we showed that expression of SF-1/LRH-1 induces differentiation of mesenchymal stem cells into steroidogenic cells. In this study, genome-wide analysis revealed that ALAS1 was a novel SF-1-target gene in differentiated mesenchymal stem cells. Chromatin immunoprecipitation and reporter assays revealed that SF-1/LRH-1 up-regulated ALAS1 gene transcription in steroidogenic cells via binding to a 3.5-kb upstream region of ALAS1. The ALAS1 gene was up-regulated by overexpression of SF-1/LRH-1 in steroidogenic cells and down-regulated by knockdown of SF-1 in these cells. Peroxisome proliferator-activated receptor-γ coactivator-1α, a coactivator of nuclear receptors, also strongly coactivated expression of NR5A-target genes. Reporter analysis revealed that peroxisome proliferator-activated receptor-γ coactivator-1α strongly augmented ALAS1 gene transcription caused by SF-1 binding to the 3.5-kb upstream region. Finally knockdown of ALAS1 resulted in reduced progesterone production by steroidogenic cells. These results indicate that ALAS1 is a novel NR5A-target gene and participates in steroid hormone production.

  12. 5-Aminolevulinic acid protects against cisplatin-induced nephrotoxicity without compromising the anticancer efficiency of cisplatin in rats in vitro and in vivo.

    Directory of Open Access Journals (Sweden)

    Yoshio Terada

    Full Text Available BACKGROUND/AIMS: Nephrotoxicity is a frequent and major limitation in cisplatin (CDDP-based chemotherapy. 5-Aminolevulinic acid (ALA is widely distributed in animal cells, and it is a precursor of tetrapyrole compounds such as heme that is fundamentally important in aerobic energy metabolism. The aim of this study is to evaluate the protective role of ALA in CDDP-induced acute kidney injury (AKI. METHOD: We used CDDP-induced AKI rat model and cultured renal tubular cells (NRK-52E. We divided four groups of rats: control, CDDP only, CDDP + ALA(post;(ALA 10 mg/kg + Fe in drinking water after CDDP, CDDP + ALA(pre & post. RESULT: CDDP increased Cr up to 6.5 mg/dl, BUN up to 230 mg/dl, and ALA significantly reduced these changes. ALA ameliorates CDDP-induced morphological renal damages, and reduced tubular apoptosis evaluated by TUNEL staining and cleaved caspase 3. Protein and mRNA levels of ATP5α, complex(COX IV, UCP2, PGC-1α in renal tissue were significantly decreased by CDDP, and ALA ameliorates reduction of these enzymes. In contrast, Heme Oxigenase (HO-1 level is induced by CDDP treatment, and ALA treatment further up-regulates HO-1 levels. In NRK-52E cells, the CDDP-induced reduction of protein and mRNA levels of mitochondrial enzymes was significantly recovered by ALA + Fe. CDDP-induced apoptosis were ameliorated by ALA + Fe treatment. Furthermore, we evaluated the size of transplantated bladder carcinoma to the rat skin, and ALA did not change the anti cancer effects of CDDP. CONCLUSION: These data suggested that the protective role of ALA in cisplatin-induced AKI is via protection of mitochondrial viability and prevents tubular apoptosis. Also there are no significant effects of ALA on anticancer efficiency of CDDP in rats. Thus, ALA has the potential to prevent CDDP nephrotoxicity without compromising its anticancer efficacy.

  13. 5-Aminolevulinic acid protects against cisplatin-induced nephrotoxicity without compromising the anticancer efficiency of cisplatin in rats in vitro and in vivo.

    Science.gov (United States)

    Terada, Yoshio; Inoue, Keiji; Matsumoto, Tatsuki; Ishihara, Masayuki; Hamada, Kazu; Shimamura, Yoshiko; Ogata, Koji; Inoue, Kosuke; Taniguchi, Yoshinori; Horino, Taro; Karashima, Takashi; Tamura, Kenji; Fukuhara, Hideo; Fujimoto, Shimpei; Tsuda, Masayuki; Shuin, Taro

    2013-01-01

    Nephrotoxicity is a frequent and major limitation in cisplatin (CDDP)-based chemotherapy. 5-Aminolevulinic acid (ALA) is widely distributed in animal cells, and it is a precursor of tetrapyrole compounds such as heme that is fundamentally important in aerobic energy metabolism. The aim of this study is to evaluate the protective role of ALA in CDDP-induced acute kidney injury (AKI). We used CDDP-induced AKI rat model and cultured renal tubular cells (NRK-52E). We divided four groups of rats: control, CDDP only, CDDP + ALA(post);(ALA 10 mg/kg + Fe in drinking water) after CDDP, CDDP + ALA(pre & post). CDDP increased Cr up to 6.5 mg/dl, BUN up to 230 mg/dl, and ALA significantly reduced these changes. ALA ameliorates CDDP-induced morphological renal damages, and reduced tubular apoptosis evaluated by TUNEL staining and cleaved caspase 3. Protein and mRNA levels of ATP5α, complex(COX) IV, UCP2, PGC-1α in renal tissue were significantly decreased by CDDP, and ALA ameliorates reduction of these enzymes. In contrast, Heme Oxigenase (HO)-1 level is induced by CDDP treatment, and ALA treatment further up-regulates HO-1 levels. In NRK-52E cells, the CDDP-induced reduction of protein and mRNA levels of mitochondrial enzymes was significantly recovered by ALA + Fe. CDDP-induced apoptosis were ameliorated by ALA + Fe treatment. Furthermore, we evaluated the size of transplantated bladder carcinoma to the rat skin, and ALA did not change the anti cancer effects of CDDP. These data suggested that the protective role of ALA in cisplatin-induced AKI is via protection of mitochondrial viability and prevents tubular apoptosis. Also there are no significant effects of ALA on anticancer efficiency of CDDP in rats. Thus, ALA has the potential to prevent CDDP nephrotoxicity without compromising its anticancer efficacy.

  14. Differential antioxidant defense and detoxification mechanisms in photodynamically stressed rice plants treated with the deregulators of porphyrin biosynthesis, 5-aminolevulinic acid and oxyfluorfen

    Energy Technology Data Exchange (ETDEWEB)

    Phung, Thu-Ha; Jung, Sunyo, E-mail: sjung@knu.ac.kr

    2015-04-03

    This study focuses on differential molecular mechanisms of antioxidant and detoxification systems in rice plants under two different types of photodynamic stress imposed by porphyrin deregulators, 5-aminolevulinic acid (ALA) and oxyfluorfen (OF). The ALA-treated plants with white necrosis exhibited a greater decrease in photochemical quantum efficiency, F{sub v}/F{sub m}, as well as a greater increase in activity of superoxide dismutase, compared to the OF-treated plants. By contrast, the brown necrosis in OF-treated plants resulted in not only more widely dispersed H{sub 2}O{sub 2} production and greater increases in H{sub 2}O{sub 2}-decomposing enzymes, catalase and peroxidase, but also lower ascorbate redox state. In addition, ALA- and OF-treated plants markedly up-regulated transcript levels of genes involved in detoxification processes including transport and movement, cellular homeostasis, and xenobiotic conjugation, with prominent up-regulation of serine/threonine kinase and chaperone only in ALA-treated plants. Our results demonstrate that different photodynamic stress imposed by ALA and OF developed differential actions of antioxidant enzymes and detoxification. Particularly, detoxification system may play potential roles in plant protection against photodynamic stress imposed by porphyrin deregulators, thereby contributing to alleviation of photodynamic damage. - Highlights: • We employ two different types of photodynamic stress, white and brown necrosis. • We examine molecular mechanisms of antioxidative and detoxification systems. • ALA and OF develop differential actions of antioxidant and detoxification systems. • Coordinated mechanism of antioxidants and detoxification works against toxic ROS. • Detoxification system plays critical roles in protection against photodynamic stress.

  15. Effects of exogenous 5-aminolevulinic acid on PIP1 and NIP aquaporin gene expression in seedlings of cucumber cultivars subjected to salinity stress.

    Science.gov (United States)

    Yan, F; Qu, D; Zhao, Y Y; Hu, X H; Zhao, Z Y; Zhang, Y; Zou, Z R

    2014-01-22

    Aquaporins play a direct role in plant water relation under salt stress, but the effects of 5-aminolevulinic acid (ALA) on aquaporin gene expression in salt-treated plants remain unknown. This study investigated the potential effects of exogenous ALA (50 mg/dm3) on aquaporin expression levels under salt stress (75 mM NaCl) in the salt-sensitive (Jinchun No.4) and the relatively salt-tolerant cucumber (Jinyou No.1) seedlings. The expressions of cucumber PIP aquaporin gene (CsPIP1:1) and cucumber NIP aquaporin gene (CsNIP) were analyzed in 20-day-old seedling leaves at 2, 4, 8, 16, and 24 h after ALA treatment. After treatment with saline alone and ALA alone, CsPIP1:1 and CsNIP gene expression levels in the 2 cucumber cultivars increased to maximum at 2 h. The aquaporin gene expression in salt-treated cucumber seedling leaves was considerably higher than that in leaves subjected to exogenous ALA. Further, the aquaporin expression levels in Jinchun No.4 were higher than those in Jinyou No.1, reaching 5.20- and 2-fold induction levels, respectively. After treatment with both ALA and NaCl, the CsNIP gene expression was downregulated in both the cucumber cultivars, while that of CsPIP1:1 decreased at 2 h and then increased to 3.8-fold in Jinchun No.4. In Jinyou No.1, CsPIP1:1 gene expression gradually increased to 2.3-fold at 4 h, followed by a decline in expression. The results indicated that ALA might delay and counteract the upregulated expression of CsPIP1:1 and CsNIP genes in cucumber seedlings under NaCl stress. Thus, salt tolerance of cucumber seedlings might be enhanced by ALA application.

  16. Effects of exogenous 5-aminolevulinic acid on photosynthesis, stomatal conductance, transpiration rate, and PIP gene expression of tomato seedlings subject to salinity stress.

    Science.gov (United States)

    Zhao, Y Y; Yan, F; Hu, L P; Zhou, X T; Zou, Z R; Cui, L R

    2015-06-11

    The effects of exogenous 5-aminolevulinic acid (ALA) on photosynthesis, plant growth, and the expression of two aquaporin genes in tomato seedlings under control and salinity conditions were investigated. Exogenous ALA application significantly improved net photosynthetic rate (Pn), total chlorophyll content, and plant biomass accumulation of tomato seedlings under salinity stress. As revealed by real-time PCR analyses, after treatment with ALA alone, expression of both LePIP1 and LePIP2 in the two tomato cultivars was up-regulated at 2 h and subsequently decreased to normal levels. Under salinity stress, transcript levels of LePIP1 in both leaves and roots of salt-sensitive cultivars (cv. Zhongza No.9) increased significantly and were considerably higher than in cultivars exposed to ALA alone. In contrast, the expression levels of LePIP1 and LePIP2 in cvs. Jinpeng No.1 cultivars were slightly lower under salinity stress than under ALA treatment. In addition, transcript levels of both LePIP1 and LePIP2 in the roots of Jinpeng No. 1 cultivars were considerably lower than those in the roots of Zhongza No. 9 cultivars under salinity stress, regardless of ALA supplementation, implying that Jinpeng No. 1 cultivars had a better capacity to maintain membrane intrinsic protein stability. Further, ALA application distinctly counteracted the up- or down-regulation of LePIP1 and LePIP2 in both cultivars under salinity stress, in accordance with the improvements instomatal conductance, transpiration rate, and Pn of tomato leaves. The results presented here indicate that ALA controls aquaporin expression, thus, presumably ALA regulates water homeostasis and enhances salt tolerance of tomato seedlings.

  17. The role of 5-aminolevulinic acid in enhancing surgery for high-grade glioma, its current boundaries, and future perspectives: A systematic review.

    Science.gov (United States)

    Mansouri, Alireza; Mansouri, Sheila; Hachem, Laureen D; Klironomos, George; Vogelbaum, Michael A; Bernstein, Mark; Zadeh, Gelareh

    2016-08-15

    5-Aminolevulinic acid (5-ALA) has been approved as an intraoperative adjunct in glioma surgery in Europe, but not North America. A systematic review was conducted to assess the evidence regarding 5-ALA as a surgical adjunct. The MEDLINE, EMBASE, and CENTRAL databases were searched, using terms relevant to "5-ALA" and "high-grade gliomas." Included studies were based on adults aged ≥18 years who underwent surgical resection/biopsy. No language or date limitations were used. Forty-three studies (1830 patients) were identified. Thirty-six were coordinated by European countries, 2 were in the United States, and none were in Canada. One was randomized, 28 were prospective, and 14 were retrospective. Twenty-six studies assessed the utility of 5-ALA as a diagnostic tool, 24 assessed its influence on the extent of resection (EOR), 9 assessed survival, and 22 reported adverse events. 5-ALA had high sensitivity and positive predictive value, whereas its specificity increased with additional adjuncts. The EOR increased with 5-ALA, but only progression-free survival was significantly influenced. Reporting of adverse events was not systematic. The use of 5-ALA improved tumor visualization and thus enabled a greater EOR and perhaps increased survival. However, additional adjuncts may be necessary for maximizing the specificity of resection and patient safety. Additional parameters, such as patient quality of life and health economic analyses, would be informative. Thus, additional systematic collection of prospective evidence may be necessary for the global incorporation of this potentially valuable surgical adjunct into routine practice. Cancer 2016;122:2469-78. © 2016 American Cancer Society. © 2016 American Cancer Society.

  18. Topical delivery of 5-aminolevulinic acid-encapsulated ethosomes in a hyperproliferative skin animal model using the CLSM technique to evaluate the penetration behavior.

    Science.gov (United States)

    Fang, Yi-Ping; Huang, Yaw-Bin; Wu, Pao-Chu; Tsai, Yi-Hung

    2009-11-01

    Psoriasis, an inflammatory skin disease, exhibits recurring itching, soreness, and cracked and bleeding skin. Currently, the topical delivery of 5-aminolevulinic acid-photodynamic therapy (ALA-PDT) is an optional treatment for psoriasis which provides long-term therapeutic effects, is non-toxic and enjoys better compliance with patients. However, the precursor of ALA is hydrophilic, and thus its ability to penetrate the skin is limited. Also, little research has provided a platform to investigate the penetration behavior in disordered skin. We employed a highly potent ethosomal carrier (phosphatidylethanolamine; PE) to investigate the penetration behavior of ALA and the recovery of skin in a hyperproliferative murine model. We found that the application of ethosomes produced a significant increase in cumulative amounts of 5-26-fold in normal and hyperproliferative murine skin samples when compared to an ALA aqueous solution; and the ALA aqueous solution appeared less precise in terms of the penetration mode in hyperproliferative murine skin. After the ethosomes had been applied, the protoporphyrin IX (PpIX) intensity increased about 3.64-fold compared with that of the ALA aqueous solution, and the penetration depth reached 30-80 microm. The results demonstrated that the ethosomal carrier significantly improved the delivery of ALA and the formation of PpIX in both normal and hyperproliferative murine skin samples, and the expression level of tumor necrosis factor (TNF)-alpha was reduced after the ALA-ethosomes were applied to treat hyperproliferative murine skin. Furthermore, the results of present study encourage more investigations on the mechanism of the interaction with ethosomes and hyperproliferative murine skin.

  19. Growth and properties of semi-organic nonlinear optical crystal: L-Glutamic acid hydrochloride

    Directory of Open Access Journals (Sweden)

    J. Uma

    2016-02-01

    Full Text Available Semiorganic nonlinear optical crystal of L-Glutamic acid hydrochloride (LGHC was grown from aqueous solution by slow evaporation technique. Single crystal X-ray Diffraction analysis confirms that LGHC crystallizes in orthorhombic system with noncentrosymmetric space group P212121. The powder X-ray diffraction study confirms the crystallinity of the grown crystal. The fundamental functional groups of the grown crystals were analyzed by Fourier Transform Infrared spectroscopic analysis in the range of 450–4000 cm−1. The range of optical transmission was ascertained using UV–vis–NIR studies. The Refractive Index of the LGHC crystal was found to be 1.4. The second harmonic generation efficiency of the LGHC was determined using Kurtz and Perry powder technique and it was 0.5 times greater than that of the KDP crystal. Thermo Gravimetric Analysis (TGA and Differential Thermal Analysis (DTA were used to study thermal behavior of the sample. The dielectric behavior and ac conductivity of the sample were studied as a function of frequency for different temperatures. The mechanical strength of the crystal was determined by Vicker׳s Hardness test. The elastic stiffness constant and yield strength of the sample was calculated.

  20. Growth and properties of semi-organic nonlinear optical crystal:L-Glutamic acid hydrochloride

    Institute of Scientific and Technical Information of China (English)

    J.Uma; V.Rajendran

    2016-01-01

    Semiorganic nonlinear optical crystal of L-Glutamic acid hydrochloride (LGHC) was grown from aqueous solution by slow evaporation technique. Single crystal X-ray Diffraction analysis confirms that LGHC crystallizes in orthorhombic system with noncentrosymmetric space group P212121. The powder X-ray diffraction study confirms the crystallinity of the grown crystal. The fundamental functional groups of the grown crystals were analyzed by Fourier Transform Infrared spectroscopic analysis in the range of 450–4000 cm¯1. The range of optical transmission was ascertained using UV–vis–NIR studies. The Refractive Index of the LGHC crystal was found to be 1.4. The second harmonic generation efficiency of the LGHC was determined using Kurtz and Perry powder technique and it was 0.5 times greater than that of the KDP crystal. Thermo Gravimetric Analysis (TGA) and Differential Thermal Analysis (DTA) were used to study thermal behavior of the sample. The dielectric behavior and ac conductivity of the sample were studied as a function of frequency for different temperatures. The mechanical strength of the crystal was determined by Vicker's Hardness test. The elastic stiffness constant and yield strength of the sample was calculated.

  1. New copper(II) complexes with dopamine hydrochloride and vanillymandelic acid: Spectroscopic and thermal characterization

    Science.gov (United States)

    Mohamed, Gehad G.; Nour El-Dien, F. A.; El-Nahas, R. G.

    2011-10-01

    The dopamine derivatives participate in the regulation of wide variety of physiological functions in the human body and in medication life. Increase and/or decrease in the concentration of dopamine in human body reflect an indication for diseases such as Schizophrenia and/or Parkinson diseases. The Cu(II) chelates with coupled products of dopamine hydrochloride (DO.HCl) and vanillymandelic acid (VMA) with 4-aminoantipyrine (4-AAP) are prepared and characterized. Different physico-chemical techniques namely IR, magnetic and UV-vis spectra are used to investigate the structure of these chelates. Cu(II) forms 1:1 (Cu:DO) and 1:2 (Cu:VMA) chelates. DO behave as a uninegative tridentate ligand in binding to the Cu(II) ion while VMA behaves as a uninegative bidentate ligand. IR spectra show that the DO is coordinated to the Cu(II) ion in a tridentate manner with ONO donor sites of the phenolic- OH, -NH and carbonyl- O, while VMA is coordinated with OO donor sites of the phenolic- OH and -NH. Magnetic moment measurements reveal the presence of Cu(II) chelates in octahedral and square planar geometries with DO and VMA, respectively. The thermal decomposition of Cu(II) complexes is studied using thermogravimetric (TG) and differential thermal analysis (DTA) techniques. The activation thermodynamic parameters, such as, energy of activation, enthalpy, entropy and free energy change of the complexes are evaluated and the relative thermal stability of the complexes are discussed.

  2. Inhibition of VDAC1 prevents Ca²⁺-mediated oxidative stress and apoptosis induced by 5-aminolevulinic acid mediated sonodynamic therapy in THP-1 macrophages.

    Science.gov (United States)

    Chen, Haibo; Gao, Weiwei; Yang, Yang; Guo, Shuyuan; Wang, Huan; Wang, Wei; Zhang, Shuisheng; Zhou, Qi; Xu, Haobo; Yao, Jianting; Tian, Zhen; Li, Bicheng; Cao, Wenwu; Zhang, Zhiguo; Tian, Ye

    2014-12-01

    Ultrasound combined with endogenous protoporphyrin IX derived from 5-aminolevulinic acid (ALA-SDT) is known to induce apoptosis in multiple cancer cells and macrophages. Persistent retention of macrophages in the plaque has been implicated in the pathophysiology and progression of atherosclerosis. Here we investigated the effects of inhibition of voltage-dependent anion channel 1 (VDAC1) on ALA-SDT-induced THP-1 macrophages apoptosis. Cells were pre-treated with VDAC1 inhibitor 4,4'-diisothiocyanostilbene-2,2'-disulfonic acid (DIDS) disodium salt for 1 h or downregulated VDAC1 expression by small interfering RNA and exposed to ultrasound. Cell viability was assessed by MTT assay, and cell apoptosis along with necrosis was evaluated by Hoechst 33342/propidium iodide staining and flow cytometry. Levels of cytochrome c release was assessed by confocal microscope and Western blot. The levels of full length caspases, caspase activation, and VDAC isoforms were analyzed by Western blot. Intracellular reactive oxygen species generation, mitochondrial membrane permeability, and intracellular Ca(2+) [Ca(2+)]i levels were measured with fluorescent probes. We confirmed that the pharmacological inhibition of VDAC1 by DIDS notably prevented ALA-SDT-induced cell apoptosis in THP-1 macrophages. Additionally, DIDS significantly inhibited intracellular ROS generation and apoptotic biochemical changes such as inner mitochondrial membrane permeabilization, loss of mitochondrial membrane potential, cytochrome c release and activation of caspase-3 and caspase-9. Moreover, ALA-SDT elevated the [Ca(2+)]i levels and it was also notably reduced by DIDS. Furthermore, both of intracellular ROS generation and cell apoptosis were predominately inhibited by Ca(2+) chelating reagent BAPTA-AM. Intriguingly, ALA-treatment markedly augmented VDAC1 protein levels exclusively, and the downregulation of VDAC1 expression by specific siRNA also significantly abolished cell apoptosis. Altogether, these

  3. Arsenic Induced Inhibition of δ-aminolevulinate Dehydratase Activity in Rat Blood and its Response To Meso 2,3-dimercaptosuccinic Acid and Monoisoamyl DMSA

    Institute of Scientific and Technical Information of China (English)

    SMRATI BHADAURIA; SWARAN J.S.FLORA

    2004-01-01

    Objective The objective of this study was to investigate arsenic induced changes in blood δ-aminolevulinic acid dehydratase (ALAD) after in vitro and in vivo exposure to this element and its response to co-administration of meso 2,3-dimercaptosuccinic acid (DMSA) and monoisoamyl DMSA (MiADMSA) either individually or in combination. Methods Rat whole blood was exposed to varying concentrations (0.1, 0.2 and 0.5 mmol/L) of arsenic (Ⅲ) or arsenic (V), to assess their effects on blood ALAD activity. Varying concentrations of MiADMSA and DMSA (0.1, 0.5 and 1.0 mmol/L) were also tried in combination to determine its ability to mask the effect of arsenic induced (0.5 mmol/L) inhibition of blood ALAD in vitro. In vitro and in vivo experiments were also conducted to determine the effects of DMSA and MiADMSA either individually or in combination with arsenic, on blood ALAD activity and blood arsenic concentration. Results In vitro experiments showed significant inhibition of the enzyme activity when 0.1-0.5 mmol/L of arsenic (Ⅲ and V) was used. Treatment with MiADMSA increased ALAD activity when blood was incubated at the concentration of 0.1 mmol/L arsenic (Ⅲ) and 0.1 mmol/L MiADMSA. No effect of 0.1 mmol/L MiADMSA on ALAD activity was noticed when the arsenic concentration was increased to 0.2 and 0.5 mmol/L. Similarly, MiADMSA at a lower concentration (0.1 mmol/L) was partially effective in the turnover of ALAD activity against 0.5 mmol/L arsenic (Ⅲ), but at two higher concentrations (0.5and 1.0 mmol/L) a complete restoration of ALAD activity was observed. DMSA at all the three concentrations (0.1, 0.5 and 1.0 mmol/L) was effective in restoring ALAD activity to the normal value.Conclusions The results thus suggest that arsenic has a distinct effect on ALAD activity. Another important toxicological finding of the present study, based on in vivo experiments further suggests that combined administration of DMSA and MiADMSA could be more beneficial for reducing blood

  4. Effect of cell cycle phase on the sensitivity of SAS cells to sonodynamic therapy using low-intensity ultrasound combined with 5-aminolevulinic acid in vitro.

    Science.gov (United States)

    Li, Nan; Sun, Miao; Wang, Yao; Lv, Yanhong; Hu, Zheng; Cao, Wenwu; Zheng, Jinhua; Jiao, Xiaohui

    2015-08-01

    Sonodynamic therapy (SDT) with 5-aminolevulinic acid (5-ALA) can effectively inhibit various types of tumor in vitro and in vivo. However, the association between the efficacy of SDT and the phase of the cell cycle remains to be elucidated. 5-ALA may generate different quantities of sonosensitizer, protoporphyrin IX (PpIX), in different phases of the cell cycle, which may result in differences in sensitivity to 5-ALA-induced SDT. The present study aimed to investigate the effect of the cell cycle on the susceptibility of SAS cells to SDT following synchronization to different cell cycle phases. These results indicates that the rates of cell death and apoptosis of the SAS cells in the S and G2/M phases were significantly higher following SDT, compared with those in the G1-phase cells and unsynchronized cells, with a corresponding increase in PpIX in the S and G2/M cells. In addition, the expression of caspase-3 increased, while that of B-cell lymphoma (Bcl)-2 decreased markedly in theS and G2/M cells following SDT. Cyclin A was also expressed at higher levels in the S and G2/M cells, compared with the G1-phase cells. SDT also caused a significant upregulation of cyclin A in all phases of the cell cycle, however this was most marked in the S and G2/M cells. It was hypothesized that high expression levels of cyclin A in the S and G2/M cells may promote the induction of caspase-3 and reduce the induction of Bcl-2 by SDT and, therefore, enhance apoptosis. Taken together, these data demonstrated that cells in The S and G2/M phases generate more intracellular PpIX, have higher levels of cyclin A and are, therefore, more sensitive to SDT-induced cytotoxicity. These findings indicate the potential novel approach to preventing the onset of cancer by combining cell-cycle regulators with SDT. This sequential combination therapy may be a simple and cost-effective way of enhancing the effects of SDT in clinical settings.

  5. Comparison of colorimetric and HPLC methods for determination of delta-aminolevulinic acid in urine with reference to dose-response relationship in occupational exposure to lead.

    Science.gov (United States)

    Fukui, Yoshinari; Miki, Mieko; Ukai, Hirohiko; Okamoto, Satoru; Takada, Shiro; Ikeda, Masayuki

    2005-10-01

    Both traditional colorimetry and recently developed HPLC-fluorometry have been in use for determination of delta-aminolevulinic acid in urine (ALA-U), an effect marker of occupational exposure to lead (Pb). The present study was initiated to compare the values by the two methods on an epidemiology basis among workers occupationally exposed to lead (Pb), to estimate quantitatively the colorimetry-associated increment over the values by the HPLC method, to evaluate ALA-U determination in occupational health service for Pb-exposed workers, and to identify a critical Pb-B to induce an elevation in ALA-U. For this purpose, blood and urine samples were collected from three groups of Pb-exposed workers (both men and women in combination, including smokers) and analyzed for Pb in blood (Pb-B; measured in all subjects) and ALA-U (by colorimetry or HPLC), i.e., Group 1 (164 subjects with urinalysis by the two methods), Group 2 (2,923 subjects by colorimetry), and Group 3 (2,540 subjects by HPLC). ALA-U when measured by colorimetry was higher than the values by HPLC, and that the mean difference on a group basis was 1.4 mg/l (in a range of 1.1 to 1.8 mg/l), irrespective of Pb-B levels. It was also found that the increase in ALA-U was small when Pb-B was relatively low (e.g., < or = 40 microg/100 ml), and that the increase on a group basis in response to an increase in Pb-B from 5 to 40 microg/100 ml was as small as < or = 0.6 mg/l. Thus, ALA-U appeared to be not a sensitive marker of Pb effects at low Pb-B levels. ALA-U however increased substantially with a point of inflection at the Pb-B level of about 17-34 microg/100 ml. Thus it was concluded that ALA-U as measured by colorimetry is greater than ALA-U by HPLC by 1.4 mg/l on average irrespective of intensity of Pb-exposure, which may induce bias in evaluation of health effect, and that ALA-U levels will increase when Pb-B is in excess of 17-34 microg/100 ml.

  6. Safety test of a supplement, 5-aminolevulinic acid phosphate with sodium ferrous citrate, in diabetic patients treated with oral hypoglycemic agents

    Directory of Open Access Journals (Sweden)

    Naohide Yamashita

    2014-09-01

    Full Text Available Objective: This study aimed to examine the safety of 5-aminolevulinic acid phosphate (5-ALA with sodium ferrous citrate (SFC in diabetic patients treated with one or more oral hypoglycemic agents (OHAs. Background: Recent intervention studies performed in the USA and Japan have shown that a nutritional supplement of 5-ALA with SFC efficiently reduced blood glucose levels in pre-diabetic population without any adverse events. Thus, it was anticipated that 5-ALA with SFC may potentially be taken as a beneficial supplement by diabetic patients who were being treated with OHA therapy. Nevertheless, it is important to examine its safety and efficacy in diabetic population. Methods: This study was a prospective single-blinded, randomized, placebo-controlled and parallel-group comparison study. Medically treated diabetic patients between the ages of 30 and 75 were recruited from the Tokyo metropolitan area of Japan and 45 subjects were selected after screening. These subjects were randomly assigned to three groups: daily intake of 15mg 5-ALA, 50mg 5-ALA, and a placebo (n=15, respectively. The supplement or placebo was administered for 12 weeks followed by a four week washout period. The primary endpoint was safety and occurrence of hypoglycemic attack, while the secondary endpoint was changes of fasting blood glucose (FBG and hemoglobin A1c (HbA1c. Results: Adverse events related to 5-ALA with SFC were not observed in all the groups. Abnormalities in blood and urine tests were not observed either. Significant decrease in FBG was not detected in all the groups. However, there was a small but significant decrease in HbA1c at 4 and 8 week in the 15 mg 5-ALA group. Significant decrease in HbA1c was not observed in the 50 mg 5-ALA group, although a tendency to decrease after 4 weeks was apparent. Conclusion: 5-ALA with SFC is a safe and potentially beneficial supplement if taken by diabetic patients treated with OHAs.

  7. Glucosamine hydrochloride

    Science.gov (United States)

    ... combination of glucosamine hydrochloride, chondroitin sulfate, and manganese ascorbate. Some evidence suggests that this combination can improve ... combination of glucosamine hydrochloride, chondroitin sulfate, and calcium ascorbate twice daily reduces joint swelling and pain, as ...

  8. Protoporphyrin IX distribution after intra-articular and systemic application of 5-aminolevulinic acid in healthy and arthritic joints

    Science.gov (United States)

    Huettmann, Gereon; Hendrich, Christian; Birngruber, Reginald; Lehnert, Christiane; Seara, Jose; Siebert, Werner E.; Diddens, Heyke C.

    1996-04-01

    Arthroscopic synovectomy, which is limited today to the large joints, is an important early treatment of rheumatoid arthritis (RA). Photodynamic therapy (PDT) is potentially to be a less invasive method of removing the synovial membrane. Therefore, in a rabbit model of RA, the accumulation of the photosensitizer Protoporphyrin IX (PPIX) after intra-articular and systemic application of ALA into arthritic rabbit knee joints was studied in skin, patella, synovial tissue, and meniscus by fluorescence microscopy. PPIX fluorescence was measured in biopsies taken at different times after application of neutral and acid ALA solutions. Significant PPIX fluorescence was observed in the synovial membrane and skin 2 and 4 hours after application. Using intra-articular application, ALA solutions prepared with pH 5.5 were at least as efficient as neutral solutions in sensitizing the synovial membrane. Skin also showed PPIX within 4 hours after application. After 24 hours, a marginal PPIX fluorescence was detected in these tissues. On the other hand, in cartilage and meniscus significant PPIX accumulation was still observed 24 hours after ALA injection. Systemic application of ALA also showed a good accumulation of PPIX. Further experiments are needed to show whether accumulation of the photosensitizer and tissue selectivity are sufficient for a successful treatment of rheumatoid synovitis.

  9. In vitro study of cell death with 5-aminolevulinic acid based photodynamic therapy to improve the efficiency of cancer treatment

    Science.gov (United States)

    Firdous, S.; Nawaz, M.; Ikram, M.; Ahmed, M.

    2012-03-01

    Photodynamic therapy (PDT) is a kind of photochemo therapeutic treatment that exerts its effect mainly through the induction of cell death. Distinct types of cell death may be elicited by different PDT regimes. In this study, efforts are underway to optimize PDT protocols for improved efficacy and combination of all three PDT mechanisms involved in the different human carcinomas cell narcosis. Our in vitro cell culture experiments with 5-aminolevulanic acid (ALA) a clinically approved photiosensitizer (PS) and 635 nm laser light have yielded promising results, as follow: (1) (human cervical cancer (HeLa) cell line incubated, for 18 h, with 30 μg/ml of 5-ALA, treated with laser light dose of 50 J/cm2 can produce 85% of cell killing (2) human larynx carcinoma (Hep2c) cell line incubated, for 7 h, with 55 μg/ml of 5-ALA, treated with laser light dose of 85 J/cm2 can produce 75% of cell killing (3) human liver cancer (HepG2) cell line incubated, for 22-48 h, with 262 μg/ml of 5-ALA, treated with laser light dose of 120 J/cm2 can produce 95% of cell killing (4) human muscle cancer (RD) cell line incubated, for 47 h, with 250 μg/ml of 5-ALA, treated with laser light dose of 80 J/cm2 can produce 76% of cell killing (5) Human embryonic kidney (HEK293T) cell line incu-bated, for 18 h, with 400 μg/ml of 5-ALA, treated with laser light dose of 40 J/cm2 can produce 82% of cell killing confirming the efficacy of photodynamic therapy.

  10. Clinical Effect of 5-aminolevulinic Acid Photodynamic Treating 10 Cases Bowen' s Disease%5-氨基酮戊酸光动力疗法治疗鲍温病10例疗效观察

    Institute of Scientific and Technical Information of China (English)

    熊林; 陆延娜; 万静; 魏亚东; 赵延东

    2012-01-01

    目的 观察5-氨基酮戊酸光动力疗法治疗鲍温病的临床疗效.方法 将20例鲍温病患者分为两组,各10例.治疗组予5-氨基酮戊酸外涂于皮损处,3h后予红光照射20min,能量密度100~120 J/cm2,1次/周,共4周.对照组外涂5-氟尿嘧啶软膏皮损处,2次/d,共4周.结果 治疗组完全缓解率为90.00%,对照组为30.00%,两组间完全缓解率比较,差异有统计学意义(P<0.05).且治疗组均未见严重不良反应,对照组有溃疡及瘢痕等不良反应.结论 5-氨基酮戊酸光动力疗法治疗鲍温病临床疗效较好,且无严重不良反应,值得临床推广应用.%Objective To observe the clinical effect of 5-aminolevulinic acid photodynamic therapy ( ALA-PDT) treating Bowen' s disease. Methods Twonty cases of Bowen' s disease were randomly divided into treatment group and control. Each group has 10 cases. Treatment group: applied 5-aminolevulinic acid (ALA) to the skin lesions, 3 hours later red light irradiated 20min, energy density was 100 ~ 120 J/cm2, one time a week for 4 weeks. Control group: smearing 5-fluorouracil cream(5-Fu ointment) on skin lesions,, twice daily for 4 weeks. Results Completely remission rate was 90. 00% in treatment group and 30. 00% in control. The difference between them had statistical significance(P <0.05). There were no serious side effects in the treatment group, but the control group appeared ulcer, scar and other side effects. Conclusion 5-aminolevulinic acid photodynamic is a good therapeutic method for Bowen' s disease.

  11. Source and impact of lead contamination on {delta}-aminolevulinic acid dehydratase activity in several marine bivalve species along the Gulf of Cadiz

    Energy Technology Data Exchange (ETDEWEB)

    Company, R.; Serafim, A.; Lopes, B.; Cravo, A. [CIMA, University of Algarve, Campus de Gambelas, 8005-139 Faro (Portugal); Kalman, J.; Riba, I.; DelValls, T.A. [Catedra UNESCO/UNITWIN/WiCop, Department of Physical-Chemistry, Faculty Marine and Environmental Sciences, University of Cadiz, 11510 Puerto Real, Cadiz (Spain); Blasco, J. [Instituto Ciencias Marinas Andalucia (CSIC), Campus Rio San Pedro, 11510 Puerto Real, Cadiz (Spain); Delgado, J. [Department of Geology, University of Huelva, Avda Fuerzas Armadas s/n, 21071 Huelva (Spain); Sarmiento, A.M. [Catedra UNESCO/UNITWIN/WiCop, Department of Physical-Chemistry, Faculty Marine and Environmental Sciences, University of Cadiz, 11510 Puerto Real, Cadiz (Spain); Department of Geology, University of Huelva, Avda Fuerzas Armadas s/n, 21071 Huelva (Spain); Nieto, J.M. [Department of Geology, University of Huelva, Avda Fuerzas Armadas s/n, 21071 Huelva (Spain); Shepherd, T.J.; Nowell, G. [Department of Earth Sciences, University of Durham, Science Laboratories, Durham DH1 3LE (United Kingdom); Bebianno, M.J., E-mail: mbebian@ualg.pt [CIMA, University of Algarve, Campus de Gambelas, 8005-139 Faro (Portugal)

    2011-01-17

    Coastal areas and estuaries are particularly sensitive to metal contamination from anthropogenic sources and in the last few decades the study of space-time distribution and variation of metals has been extensively researched. The Gulf of Cadiz is no exception, with several rivers draining one of the largest concentrations of sulphide deposits in the world, the Iberian Pyrite Belt (IPB). Of these rivers, the Guadiana, one of the most important in the Iberian Peninsula, together with smaller rivers like the Tinto and Odiel, delivers a very high metal load to the adjacent coastal areas. The purpose of this work was to study the source and impact of lead (Pb) drained from historical or active mining areas in the IPB on the activity of a Pb inhibited enzyme ({delta}-aminolevulinic acid dehydratase, ALAD) in several bivalve species along the Gulf of Cadiz. Seven marine species (Chamelea gallina, Mactra corallina, Donax trunculus, Cerastoderma edule, Mytilus galloprovincialis, Scrobicularia plana and Crassostrea angulata) were collected at 12 sites from Mazagon, near the mouth of the rivers Tinto and Odiel (Spain), to Cacela Velha (Ria Formosa lagoon system, Portugal). Lead concentrations, ALAD activity and lead isotope ratios ({sup 206}Pb/{sup 204}Pb, {sup 207}Pb/{sup 204}Pb and {sup 208}Pb/{sup 204}Pb) were determined in the whole soft tissues. The highest Pb concentrations were determined in S. plana (3.50 {+-} 1.09 {mu}g g{sup -1} Pb d.w.) and D. trunculus (1.95 {+-} 0.10 {mu}g g{sup -1} Pb d.w.), while M. galloprovincialis and C. angulata showed the lowest Pb levels (<0.38 {mu}g g{sup -1} Pb d.w.). In general, ALAD activity is negatively correlated with total Pb concentration. However this relationship is species dependent (e.g. linear for C. gallina ALAD = -0.36[Pb] + 0.79; r = 0.837; or exponential for M. galloprovincialis ALAD = 2.48e{sup -8.3[Pb]}; r = 0.911). This indicates that ALAD activity has considerable potential as a biomarker of Pb and moreover, in

  12. Light fractionation does not enhance the efficacy of methyl 5-aminolevulinate mediated photodynamic therapy in normal mouse skin.

    NARCIS (Netherlands)

    Bruijn, H.S. de; Haas, E.R. de; Hebeda, K.M.; Ploeg-van den Heuvel, A. van der; Sterenborg, H.J.C.M.; Neumann, H.A.; Robinson, D.J.

    2007-01-01

    Previous work demonstrated that fractionated illumination using two fractions separated by a dark interval of 2 h, significantly enhanced the clinical efficacy of photodynamic therapy (PDT) with 5-aminolevulinic acid (ALA). Considering the increasing clinical use of methyl 5-aminolevulinate (MAL) an

  13. Comparative study of two routes of administration of 5-aminolevulinic acid (oral and intratumoral via) and their effect on the accumulation of PpIX in tissues in murine model of breast cancer

    Science.gov (United States)

    González-Agüero, G.; Ramón-Gallegos, E.

    2012-10-01

    Protoporphyrin IX (PpIX) is a photosensitizer synthesized from 5-aminolevulinic acid (ALA) that has been used in photodynamic therapy (PDT) as a promising treatment for many types of cancer. In this work it was quantified the accumulation of PpIX in tumors and in different tissues of female mice (nu/nu) inoculated with breast cancer cells. Two routes of administration of ALA: gastric probe and intratumoral injection were used to find optimum time of accumulation and the via that induce the higher quantity of PpIX to improve the efficiency of PDT. The results show that the accumulation of PpIX using the intratumoral via is two times bigger than the oral via in tumors at 8 h of treatment. The concentrations obtained in the different tissues are not physiologically significant.

  14. A contribution to the determination of aflatoxin B1, quinine hydrochloride and L(+)-ascorbic acid in foodstuffs by quantitative in situ thin-layer chromatographic analysis

    NARCIS (Netherlands)

    Beljaars, P.R.

    1974-01-01

    The application of quantitative thin-layer chromatography (TLC) involving in situ spectrodensitometric measurements with a flying-spot densitometer is described in this study for the analysis of aflatoxin B 1 , quinine hydrochloride and L(+)-ascorbic acid (vitamin C

  15. Infrared and Raman spectroscopy and DFT calculations of DL amino acids: Valine and lysine hydrochloride

    Science.gov (United States)

    Paiva, F. M.; Batista, J. C.; Rêgo, F. S. C.; Lima, J. A.; Freire, P. T. C.; Melo, F. E. A.; Mendes Filho, J.; de Menezes, A. S.; Nogueira, C. E. S.

    2017-01-01

    Single crystals of DL-valine and DL-lysine hydrochloride were grown by slow evaporation method and the crystallographic structure were confirmed by X-ray diffraction experiment and Rietveld method. These two crystals have been studied by Raman spectroscopy in the 25-3600 cm-1 spectral range and by infrared spectroscopy through the interval 375-4000 cm-1 at room temperature. Experimental and theoretical vibrational spectra were compared and a complete analysis of the modes was done in terms of the Potential Energy Distribution (PED).

  16. Quantitative determination of amorphous nicardipine hydrochloride in long acting formula (NIC-LA) using light anhydrous silicic acid.

    Science.gov (United States)

    Kohinata, Takeru; Fujii, Mitsuo; Nakamura, Souichiro; Hamada, Noritaka; Yonemochi, Etsuo; Terada, Katsuhide

    2004-12-01

    We investigated a method to quantitatively determine amorphous nicardipine hydrochloride (NIC) in the NIC-long acting formula (LA) model formulas prepared using NIC, light anhydrous silicic acid (LASA) and carboxymethylethylcellulose (CMEC). Consequently, since the quantity of total NIC in the formula can be determined by means of HPLC and crystal NIC can be determined by the differential scanning calorimetry (DSC) method because the heat of fusion (85.08 J/g) of NIC is constant and unaffected by excipients, we developed the HPLC-DSC method by which the quantity of amorphous NIC is calculated as the difference between the quantity of total NIC determined by HPLC and the quantity of crystal NIC determined by DSC. This practical HPLC-DSC method was confirmed to have good accuracy and reproducibility.

  17. 5-Aminolevulinic acid and the hepatic oxidative stress in the early phase of experimental hexachlorobenzene intoxication Ácido delta-aminolevulinico e estresse oxidativo hepático na fase inicial da intoxicação experimental por hexaclorobenzeno

    OpenAIRE

    Tânia Cristina Higashi Sawada; Vanessa Vitoriano da Silva; Sonia Barros; Cristina Dislich Röpke; Silvia Berlanga de Moraes Barros

    2004-01-01

    This work evaluated the levels of 5-aminolevulinic acid (ALA) in the liver of rats exposed to different doses of HCB (25,50, and 100 mg/kg b.w. for 4 weeks) and correlated them with lipid peroxidation parameters. Levels of ALA were determined by high-pressure liquid chromatography after derivatization with acetylacetone and formaldehyde, followed by fluorescence detection. The methodology was carefully validated, nonetheless hepatic levels of ALA in all animals treated or not were below the d...

  18. Comparison of hot hydroxylamine hydrochloride and oxalic acid leaching of stream sediment and coated rock samples as anomaly enhancement techniques

    Science.gov (United States)

    Filipek, L.H.; Chao, T.T.; Theobald, P.K.

    1982-01-01

    A hot hydroxylamine hydrochloride (H-Hxl) extraction in 25% acetic acid is compared with the commonly used oxalic acid extraction as a method of anomaly enhancement for Cu and Zn in samples from two very different metal deposits and climatic environments. Results obtained on minus-80-mesh stream sediments from an area near the Magruder massive sulfide deposit in Lincoln County, Georgia, where the climate is humid subtropical, indicate that H-Hxl enhances the anomaly for Cu by a factor of 2 and for Zn by a factor of 1.5, compared to the oxalic method. Analyses of Fe oxide-coated rock samples from outcrops overlying the North Silver Bell porphyry copper deposit near Tucson, Arizona, where the climate is semi-arid to arid, indicate that both techniques effectively outline the zones of hydrothermal alteration. The H-Hxl extraction can also perform well in high-carbonate or high-clay environments, where other workers have suggested that oxalic acid is not very effective. Therefore, the H-Hxl method is recommended for general exploration use. ?? 1982.

  19. Selective and Efficient Oxidation of Aldehydes to Their Corresponding Carboxylic Acids Using H2O2/HC1 in the Presence of Hydroxylamine Hydrochloride

    Institute of Scientific and Technical Information of China (English)

    BAHRAMI,Kiumars; KHODAEI,Mohammad Mehdi; KAMALI,Shahab

    2008-01-01

    A wide variety of aldehydes were efficiently converted to their corresponding carboxylic acids in high yields using H2O2/HC1 in the presence of hydroxylamine hydrochloride.In addition,selective oxidation of aldehydes in the presence of other functional groups such as hydroxyl group,carbon-carbon double bond and other heteroatoms can be considered a noteworthy advantage of this method.

  20. Comparison of efficacy of the phosphate binders nicotinic acid and sevelamer hydrochloride in hemodialysis patients

    National Research Council Canada - National Science Library

    Ahmadi, Farrokhlagha; Shamekhi, Fatemeh; Lessan-Pezeshki, Mahbob; Khatami, Mohammad Reza

    2012-01-01

    ...), and must be controlled with the use of phosphate binders. Studies comparing the effects of sevelamer and nicotinic acid, both similar non-calcium and non-aluminum phosphate binders, are not available...

  1. pH-independent release of propranolol hydrochloride from HPMC-based matrices using organic acids

    Directory of Open Access Journals (Sweden)

    2008-08-01

    Full Text Available Background and purpose of the study: Propranolol HCl, a widely used drug in the treatment of cardiac arrhythmias and hypertension, is a weak basic drug with pH-dependent solubility that may show release problems from sustained release dosage forms at higher pH of small intestine. This might decrease drug bioavailability and cause variable oral absorption. Preparation of a sustained release matrix system with a pH-independent release profile was the aim of the present study. Methods: Three types of organic acids namely tartaric, citric and fumaric acid in the concentrations of 5, 10 and 15 % were added to the matrices prepared by hydroxypropyl methylcellulose (HPMC and dicalcium phosphate. The drug release studies were carried out at pH 1.2 and pH 6.8 separately and mean dissolution time (MDT as well as similarity factor (¦2 were calculated for all formulations. Results and discussion: It was found that incorporation of 5 and 10 % tartaric acid in tablet formulations with 30 % HPMC resulted in a suitable pH-independent release profiles with significant higher ¦2 values (89.9 and 87.6 respectively compared to acid free tablet (58.03. The other two acids did not show the desirable effects. It seems that lower pKa of tartaric acid accompanied by its higher solubility were the main factors in the achievement of pH-independent release profiles.

  2. Determination of ranitidine hydrochloride in pharmaceutical preparations by titrimetry and visible spectrophotometry using bromate and acid dyes.

    Science.gov (United States)

    Basavaiah, K; Nagegowda, P

    2004-02-01

    Four new methods using titrimetry and spectrophotometry are described for the determination of ranitidine hydrochloride (RNH) with potassium bromate as the oxidimetric reagent and acid dyes, methyl orange, indigo carmine and metanil yellow. In direct titrimetry (method A), the drug is titrated directly with bromate in acid medium and in the presence of excess of bromide using methyl orange indicator. In back titrimetry (method B), the drug is treated with a measured excess of bromate in the presence of bromide and acid, and the unreacted bromine is determined iodometrically. Both spectrophotometric methods are based on the oxidation of RNH by a known excess of bromate in acid medium and in the presence of excess of bromide followed by estimation of surplus oxidant by reacting with either indigo carmine (method C) or metanil yellow (method D), and measuring the absorbance at 610 or 530 nm. In methods B, C and D, reacted oxidant corresponds to the drug content. The experimental conditions are optimized. Titrimetric procedures are applicable over the ranges 1-10 mg (A) and 1-17 mg (B), and the reaction stoichiometry is found to be 1:1 (BrO(-)(3): RNH). In spectrophotometric methods, the absorbance is found to increase linearly with increasing concentration of RNH, which is corroborated by the calculated correlation coefficient (r) of 0.9984 (C) and 0.9976 (D). The systems obey Beer's law for 2-12 and 1-7 microg ml(-1), for methods C and D, respectively. Method D with a molar absorptivity of 9.82 x 10(4) l mol(-l) cm(-1) is found to be more sensitive than method C ( epsilon = 2.06 x l0(4) l mol(-1) cm(-1)). The limits of detection and quantification are reported for both the spectrophotometric methods. The proposed methods were applied successfully to the determination of RNH in tablets and injections. The reliability of the assay was established by parallel determination by the official method and by recovery studies.

  3. Comparison of efficacy of the phosphate binders nicotinic acid and sevelamer hydrochloride in hemodialysis patients

    Directory of Open Access Journals (Sweden)

    Farrokhlagha Ahmadi

    2012-01-01

    Full Text Available Hyperphosphatemia is a significant risk factor for the development of ectopic calcification and coronary artery diseases in patients on hemodialysis (HD, and must be controlled with the use of phosphate binders. Studies comparing the effects of sevelamer and nicotinic acid, both similar non-calcium and non-aluminum phosphate binders, are not available. In this study, 40 patients on HD with a serum phosphorus level of more than 6 mg/dL were enrolled. After a two week washout period without phosphate binders, the patients were randomly divided into two equal groups (n = 20 and were started on nicotinic acid or sevelamer for a period of four weeks. The dose of nicotinic acid used was 500 mg and that of sevelamer was 1600 mg daily. Blood samples were drawn for the measurement of the total calcium (Ca, phosphorus (P, alkaline phosphatase (ALP, triglyceride (TG, total cholesterol (Chol, high-density lipoprotein (HDL, low-density lipoprotein (LDL, uric acid and parathyroid hormone (PTH. Patients receiving sevelamer showed a significant reduction in serum P level (2.2 ± 0.69 mg/dL; P <0.0001 in comparison with the nicotinic acid group (1.7 ± 1.06 mg/dL; P = 0.004. Reduction in the Ca-P product was significantly different in the two groups; in the sevelamer group, it was 21 ± 7; (P <0.0001 while in the nicotinic acid group, it was 16 ± 11 (P = 0.007. Also, patients on sevelamer showed greater reduction in the mean TG level (38.9 ± 92 mg/dL; P = 0.005. No significant changes were observed in the mean serum Ca, total Chol, HDL, LDL, ALP and iPTH levels in the two study groups. Our short-term study suggests that although nicotinic acid reduced hyperphosphatemia, sevelamer showed higher efficacy in controlling hyperphosphatemia as well as the Ca-P product.

  4. β-氨基酸乙酯盐酸盐的合成与表征%Synthesis and Characterization of β-Amino Acid Ethyl Ester Hydrochlorides

    Institute of Scientific and Technical Information of China (English)

    韩秋敏; 李登超

    2011-01-01

    β-Phenylalanine ethyl ester hydrochloride,2-F-β-phenylalanine ethyl ester hydrochloride and 3-F-β-phenylalanine ethyl ester hydrochloride were synthesized by reacting amino acids with ethanol in the presence of thionyl chloride,respectively.The structures of these compounds were characterized by melting point,1H-NMR,13C-NMR and mass spectrometry.This synthetic method was simple,with mild reaction conditions and the yields above 85%.%以三种β-苯丙氨酸、二氯亚砜、乙醇为原料分别合成了β-苯丙氨酸乙酯盐酸盐、2F-β-苯丙氨酸乙酯盐酸盐和3F-β-苯丙氨酸乙酯盐酸盐三种稳定的β-氨基酸乙酯盐酸盐,并通过熔点、核磁和质谱对化合物的结构进行了表征。该合成方法操作简单、反应条件温和,收率均在85%以上。

  5. Erlotinib hydrochloride.

    Science.gov (United States)

    Minna, John D; Dowell, Jonathan

    2005-05-01

    Erlotinib hydrochloride (Tarceva; OSI Pharmaceuticals/Genentech/Roche), a member of a class of targeted anticancer drugs that inhibit the activity of the epidermal growth factor receptor, was approved by the US FDA in November 2004 for the treatment of advanced non-small-cell lung cancer after failure of at least one prior chemotherapy regimen. It is the first such drug to demonstrate an increase in survival in Phase III trials in patients with advanced non-small-cell lung cancer.

  6. Comparison of the efficacy of ethylenediaminetetraacetic acid and tetracycline hydrochloride as root conditioning agents: An in vitro study

    Directory of Open Access Journals (Sweden)

    Tarun Nanda

    2012-01-01

    Full Text Available Objective: Root surfaces of periodontitis-affected teeth are hypermineralized and contaminated with cytotoxic and other biologically active substances. Various root conditioning agents have been recommended as an adjunct to mechanical root surface debridement to expose dentin collagen and cementum bound proteins. The aim of the present in vitro study was to compare the efficacy of ethylenediaminetetraacetic acid (EDTA and tetracycline hydrochloride (HCl as root conditioning agents on planed root surfaces. Materials and Methods: A total of 20 human maxillary anterior teeth indicated for extraction due to chronic periodontitis were collected and root planed. The teeth were sectioned and specimens were divided into two groups - Group I and II. Group I dentin specimens were treated with EDTA and Group II specimens were treated with tetracycline HCl solution at a concentration of 10% by active burnishing technique for 3 min. The root surface samples were then examined by scanning electron microscope. Results: The results of this study showed that EDTA and tetracycline HCl were equally effective in removing the smear layer. It was observed that the total and patent dentinal tubules were more in number in teeth treated with tetracycline when compared to EDTA group. However, EDTA was found to be much more effective as root conditioning agent because it enlarged the diameter of dentinal tubules more than that of tetracycline HCl. Conclusion: The results of in vitro study showed that both the agents are good root conditioning agents if applied in addition to periodontal therapy. However, further studies are required to establish the in vivo importance of EDTA and tetracycline HCL as root conditioners.

  7. Metal Accumulation, Blood δ-Aminolevulinic Acid Dehydratase Activity and Micronucleated Erythrocytes of Feral pigeons (Columba Livia Living Near Former Lead-Zinc Smelter “ Trepça” – Kosovo

    Directory of Open Access Journals (Sweden)

    Elezaj I. R.

    2013-04-01

    Full Text Available The concentration of lead in blood and tibia (Pb, zinc (Zn and cupper (Cu in tibia, blood δ- aminolevulinic acid dehydratase (ALA-D; EC: 4.2.1.24 activity, hematocrit value (Hct and micronuclei frequency (MN of peripheral erythrocytes have been determinated in three different populations of feral pigeons (Columba livia; forma urbana and forma domestica, collected in Mitrovica town (situated close to smelter “Trepça”, down closed in 2000 year and in rural area (Koshare willage . The blood lead level in feral pigeons from Mitrovica (forma urbana was 3 times higher (149.6; 50.5 μg% in comparison with that in feral pigeons from Mitrovica (forma domestica and 27.7 times higher (5.4 μg% in comparison with pigeons from rural area. The Pb concentration of tibia of feral pigeons (froma urbana and forma domestica, from Mitrovica town was significantly higher (P<0.001 in comparison with control. The concentration of Zn in tibia of feral pigeons from Mitrovica town (forma urbana, was significantly higher (P<0.006 in comparison with control. The blood ALA-D activity of feral pigeons from Mitrovica town (forma urbana and froma domestica, was significantly inhibited in comparison with control. The blood ALA-D activity of feral pigeons –forma urbana from Mitrovica town was significantly inhibited (P<0.001 in comparison with the blood ALA-D activity of feral pigeons-forma domestica from Mitrovica town. The erythrocyte MN frequency of feral pigeons from Mitrovica was significantly higher (P <0.001 in comparison with controls. The smelter “Trepça” ten year after closed down pose a threat to the local environment, biota and people’s health.

  8. 5-氨基酮戊酸光动力学疗法在皮肤科的应用进展%Applied advances of 5-aminolevulinic acid photodynamic therapy in dermatology

    Institute of Scientific and Technical Information of China (English)

    张立坤; 竺炯; 张萍

    2012-01-01

    To explore the mechanism and application of photodynamic therapy using aminolevulinic acid (5-ALA) in skin diseases, and provide reference for the rational use in clinic. Summarize the reported articles of mechanism and clinical application of photodynamic therapy in recent ten years, analysis the mechanism in the photodynamic therapy treatment for various skin disease, sort the types of skin disease cured by photodynamic therapy and the side effect related with photodynamic therapy. Photodynamic therapy have good clinical curative effect in skin cancer, erythema scaly skin neoplasms, psoriasis, viral warts, acne, nevus flammeus, etc. and have fewer adverse reactions. Photodynamic therapy is a safe, efficient treatment of psoriasis, and have great application prospects in skin diseases.%探讨5-氨基酮戊酸(ALA)光动力学疗法(PDT)治疗皮肤病的作用原理及应用范围,为临床合理使用ALA-PDT提供参考依据.对近10余年来文献报道的有关PDT研究进展及其临床应用的文献进行总结和分析,综述ALA-PDT治疗各类皮肤病的作用原理和机制,以及ALA-PDT治疗皮肤病的范围,所引起的不良反应.PDT对皮肤肿瘤、红斑鳞屑性皮肤病、人乳头瘤病毒(HPV)感染性皮肤病、痤疮、鲜红斑痣等均有良好的临床效果,不良反应相对较小,在皮肤科有很大的应用前景.

  9. Removal of Chloroform from Hydrochloride Acid Solution Using Fine Powder of Polymer as Adsorbent

    Institute of Scientific and Technical Information of China (English)

    LU,Yingzhou; QUE,Yong; LI,Chunxi; MENG,Hong; WANG,Zihao

    2009-01-01

    In order to choose a suitable adsorbent for the removal of chloroform from its hydrochloric acid solution,the adsorptive ability of some polymer adsorbents was investigated in terms of their adsorption curves in water and 20% hydrochloric acid solutions at 298.15 K,and compared with that of active carbon (AC) and solid paraffin (SP).The adsorbents studied include the fine powders of chlorinated rubber (CR),polypropylene (PP),chlorinated polypropylene (CPP) and polyvinylchloride (PVC).The results showed that the adsorption behavior followed the Langmuir equation and the adsorption ability of these adsorbents followed the order AC > PVC > CR > PP > CPP> SP.This order is basically in line with the decrease of chloro-content of the adsorbents from PVC to SP.The adsorptivity of PVC and CR was nearly equivalent to that of AC with their saturated adsorption being about 1.4 g-CHCl3 (g-absorbent) -1.For all adsorbents studied,the adsorption capacity always decreases with the increase of hydrochloric acid concentration.It is showed that the commercial polymer powder of PVC or CR can be used as an efficient absorbent for the removal of chloroform from its aqueous solution for its low cost,good adsorption ability and ease of thermal desorption for recycling.

  10. 外源5-氨基乙酰丙酸对红香芋试管苗耐冷性的影响%Effect of Exogenous 5 -aminolevulinic Acid on Cold Tolerance of Taro Plantlets in vitro

    Institute of Scientific and Technical Information of China (English)

    何继红; 蒋芳玲; 李洁英; 吴震

    2012-01-01

    The effects of different concentrations of exogenous 5 - aminolevulinic acid ( ALA) on the cold tolerance and related physiological indexes of taro [ Colocasia esculenta ( L. ) Schott ] plantlets in vitro were studied under the low temperature stress simulated artificially. The results showed that: under short -term (16 h) low temperature stress, the 2 ~20 mg/L exogenous ALA treatment could reduce the damaged degree of taro plantlets in vitro, promote the activities of superoxide dismutase ( SOD) , peroxidase ( POD) , catalase ( CAT) and ascorbic acid peroxidase ( APX) , decrease the production speed of superoxide anion ( · O2 -) and the content of hydrogen peroxide ( H2 O2 ) , suppress the increase in malonaldehyde ( MDA) content and plasma membrane permeability, and strengthen the ability of cell osmoregulation. The above results indicated that the ALA with suitable concentration could enhance the cold tolerance of taro plantlets in vitro, and relieve the injury of low temperature stress to taro test -tube plantlets. The application of 10 mg/L ALA could obtain the best effect.%为探讨外源5 -氨基乙酰丙酸对芋试管苗耐冷性的影响,以红香芋为试材,通过人工模拟低温逆境,研究了不同浓度外源ALA处理下芋试管苗耐冷性相关生理指标的变化.结果表明:短期(16 h)低温胁迫下,添加2~20 mg/L外源ALA可减轻芋试管苗冷害程度,提高超氧化物歧化酶(SOD)、过氧化物酶(POD)、过氧化氢酶(CAT)和抗坏血酸过氧化物酶(APX)活性,降低超氧阴离子(·O2-)产生速率和过氧化氢( H2O2)含量,抑制丙二醛(MDA)含量和质膜透性的上升,同时增强细胞渗透调节能力.以上结果说明,适宜浓度的ALA处理可缓解低温胁迫对芋试管苗的伤害,提高其耐冷性;ALA处理浓度以10 mg/L效果最好.

  11. Cold-knife conization versus photodynamic therapy with topical 5-aminolevulinic acid (5-ALA) in cervical intraepithelial neoplasia (CIN) II with associated human papillomavirus infection: a comparison of preliminary results.

    Science.gov (United States)

    Bodner, Klaus; Bodner-Adler, Barbara; Wierrani, Franz; Kubin, Andreas; Szölts-Szölts, Josef; Spängler, Babette; Grünberger, Werner

    2003-01-01

    The optimal treatment of preinvasive cervical lesions is still not clear as all surgical techniques cause substantial cervical stroma destruction with the risk of a possible incompetent cervix. Photodynamic therapy can preserve fertility due to selective tissue destruction. The aim of the present study was to compare the efficacy of cold-knife conization versus photodynamic therapy with topical 5-aminolevulinic acid in eradicating cervical intraepithelial neoplasia (CIN) II and associated HPV infection. Eleven HPV-positive non-pregnant women were selected for photodynamic therapy (PDT). To be eligible for this procedure superficial cervical PAP smears as well as colposcopic biopsies performed before therapy had to show CIN II with the lesion involving at least 15% of the cervix and being colposcopically visible. The deep endocervical PAP smear had to show normal endocervical epithelium. The next (following each PDT) 11 HPV-positive women with CIN II treated with cold-knife conization were used as a control group. The cervical sampling for HPV DNA was performed 3 months after conization and PDT. Patients were followed-up for 1 year with cytological smears and colposcopy at the outpatient department of the hospital. Follow-up at three months revealed that HPV was eradicated by both techniques in 73%. After 12 months follow-up, 100 vs. 91% (conization vs. PDT) of the patients were disease-free. No systemic side-effects and no local necrosis, sloughing or scarring occurred due to PDT. One patient treated with PDT presented with a relapsing suspicious PAP smear and an abnormal white colposcopic lesion after application of acetic acid 6 months post-PDT. A subsequent conization was performed and revealed a CIN I lesion. No statistically significant differences concerning HPV eradication (p > 0.05) and recurrence (p > 0.05) could be observed between the two methods. The results presented in this study indicate that topical PDT with 5-ALA is in most cases a successful

  12. Inhibitory effect of 5-aminolevulinic acid photodynamic therapy on Candida albicans%5-氨基酮戊酸光动力疗法对白念珠菌抑制效应的实验研究

    Institute of Scientific and Technical Information of China (English)

    梁义; 卢丽明; 陈勇; 尹琦

    2013-01-01

    Objective To evaluate the inhibitory effect of 5-aminolevulinic acid Photodynamic therapy on Candida albicans in vitro. Methods 96-well cell culture plates were used for experimental carriers, and Candida albicans suspension was added to these wells, which were divided into experimental group and four control groups. With He-Ne laser as the excitation source, ALA as photosensitizer, DMSO as penetration enhancer and a solvent, ALA-PDT was performed. Results The growth of Candida albicans was inhibited in experimental group, with MIC of 500 mg/ml (50%). At concentration of 200 mg/ml (20%), ALA began to inhibit the growth of Candida albicans in experimental group, and ALA inhibited the growth of Candida albicans in a concentration-dependent way. The growth of Candida albicans was not inhibited in four control groups, and the CFU of Candida albicans showed no statistically significant difference between the groups. Conclusion ALA-PDT can effectively inhibit the growth of Candida albicans.%目的 评估5-氨基酮戊酸光动力疗法(5-ALA-PDT)在体外对白念珠菌的抑制效应.方法 以96孔细胞培养板为实验载体,加入白念珠菌悬液,分为治疗组和4个对照组,以氦氖激光为激发光源,ALA为光敏剂,使用DMSO作为ALA的溶剂兼穿透增强剂,进行ALA-PDT.结果 治疗组白念珠菌的生长受到抑制,其MIC值为500mg/ml(50%),ALA浓度在200mg/ml(20%)时,开始使治疗组白念珠菌的生长受到抑制,且抑制作用对ALA的浓度呈剂量依赖关系.而对照组中白念珠菌的生长未受到抑制,四组的白念珠菌的CFU数量变化无明显差异.结论 按本实验所使用的方法进行的ALA-PDT能有效地抑制白念珠菌.

  13. Danos ao DNA promovidos por ácido 5-aminolevulínico: possível associação com o desenvolvimento de carcinoma hepatocelular em portadores de porfiria aguda intermitente DNA damage induced by 5-aminolevulinic acid: a possible association with the development of hepatocellular carcinoma in acute intermittent porphyria patients

    Directory of Open Access Journals (Sweden)

    Janice Onuki

    2002-07-01

    Full Text Available 5-Aminolevulinic acid (ALA is a heme precursor accumulated in acute intermittent porphyria (AIP, which might be associated with hepatocellular carcinoma (HCC in symptomatic patients. Under metal catalyzed oxidation, ALA and its cyclic dimerization product, 3,6-dihydropyrazine-2,5-dipropanoic acid, produce reactive oxygen species that damage plasmid and calf thymus DNA bases, increase the steady state level of 8-oxo-7,8-dihydro-2´-deoxyguanosine in liver DNA and promote mitochondrial DNA damage. The final product of ALA, 4,5-dioxovaleric acid (DOVA, is able to alkylate guanine moieties, producing adducts. ALA and DOVA are mutagenic in bacteria. This review shows an up-to-date literature data that reinforce the hypothesis that the DNA damage induced by ALA may be associated with the development of HCC in AIP patients.

  14. In vitro study of 5-aminolevulinic acid-based photodynamic therapy for apoptosis in human cervical HeLa cell line

    Science.gov (United States)

    Atif, M.; Firdous, S.; Khurshid, A.; Noreen, L.; Zaidi, S. S. Z.; Ikram, M.

    2009-12-01

    5-aminolevulanic acid (ALA), belonging among the promising second generation of sensitizers, was evaluated as an inducer of photodamage on HeLa (human cervical adenocarcinoma) cell line. A diode laser (635 nm) was used as a source for initiation of the photodynamic effect. We studied the influence of different incubation times, various concentrations of sensitizer, different irradiation doses and various combinations of sensitizer and light doses on the photodamage of HeLa cells. Viability of cells was determined by means of neutral red assay. The quantitative cellular uptake of ALA sensitizer was done by spectrophotometric measurements. No prominent cytotoxic or phototoxic effects on HeLa were observed due to sensitizer or light doses when studied independently of each other. However phototoxicity evoked by laser irradiated sensitizer was detected in HeLa cell line.

  15. Fluorescence cytology with 5-aminolevulinic acid in EUS-guided FNA as a method for differentiating between malignant and benign lesions (with video).

    Science.gov (United States)

    Ikeura, Tsukasa; Takaoka, Makoto; Uchida, Kazushige; Shimatani, Masaaki; Miyoshi, Hideaki; Kato, Kota; Ohe, Chisato; Uemura, Yoshiko; Kaibori, Masaki; Kwon, A-Hon; Okazaki, Kazuichi

    2015-01-01

    EUS-guided FNA (EUS-FNA) has been increasingly performed to obtain specimens for the pathological evaluation of patients with GI and pancreaticobiliary masses as well as lymphadenopathies of unknown origin. Photodynamic diagnosis by using 5-aminolebulinic acid (ALA) has been reported to be useful for enabling the visual differentiation between malignant and normal tissue in various cancers. To evaluate the diagnostic accuracy of fluorescence cytology with ALA in EUS-FNA. A prospective study. A single center. A total of 28 consecutive patients who underwent EUS-FNA for the pathological diagnosis of a pancreaticobiliary mass lesion or intra-abdominal lymphadenopathy of unknown origin. Patients were orally administered ALA 3 to 6 hours before EUS-FNA. The sample was obtained via EUS-FNA for fluorescence cytology and conventional cytology. A single gastroenterologist performed the fluorescence cytology by using fluorescence microscopy after the procedure, independently of the conventional cytology by pathologists. The accuracy of fluorescence cytology with ALA in the differentiation between benign and malignant lesions by comparing the results of fluorescence cytology with the final diagnosis. Of the 28 patients included in the study, 22 were considered as having malignant lesions and 6 patients as having benign lesions. Fluorescence cytology could correctly discriminate between benign and malignant lesions in all patients. Therefore, both the sensitivity and specificity of fluorescence cytology were 100% in our study. Fluorescence cytology was performed by only 1 gastroenterologist with a small number of patients. Fluorescence cytology with ALA in EUS-FNA may be an effective and simple method for differentiating between benign and malignant lesions. Copyright © 2015 American Society for Gastrointestinal Endoscopy. Published by Elsevier Inc. All rights reserved.

  16. Glucose and δ-Aminolevulinic Acid Stimulate the Dark Chlorophyll Synthesis of Rice Seedlings%葡萄糖和δ-氨基酮戊酸促进水稻在黑暗中合成叶绿素

    Institute of Scientific and Technical Information of China (English)

    杨棋明; 蔡慧美; 杨佳豪

    2003-01-01

    This research was to examine if rice (Oryza sativa L.), a monocotyledon of angiosperm, was able to synthesize chlorophyll (Chl) in complete darkness. Five-cm-tall etiolated seedlings of rice were used as starting materials and treated with or without various concentrations of glucose and/or δ-aminolevulinic acid (ALA) in the dark. Leaves harvested at the indicated time were determined for their contents of Chl, protoporphyrin Ⅸ (Proto), Mg-protoporphyrin Ⅸ (Mg-Proto) and protochlorophyllide (Pchlide). The mole percentage of porphyrin was calculated. The Chl content in the etiolated rice seedlings slightly increased from about 2.5 μg/g to 7.5 μg/g within 12 d in the dark, but the total Chl of dark-grown rice increased from 0.36 μg/g to 3.6 μg/g. While the mole percentages of Proto, Mg-Proto and Pchlide in the dark-grown seedlings without any treatment were about 65%, 27.5% and 7.5% at the beginning, respectively, those in the light-grown seedlings were about 42.5%, 35% and 22.5%, respectively. The mole percentage of porphyrin of etiolated seedlings resumed its normal ratio within 2 d after treatment with glucose. While the Chl content of etiolated seedlings grown in culture solution with 3% and 6% glucose increased 2.5 and 4.0 folds, respectively, those with 3% and 6% glucose and 1 mmol/L ALA increased 22 and 24 folds, respectively. It is concluded that angiosperm might be able to synthesize a small amount of Chl in complete darkness, that either glucose or ALA could stimulate dark Chl synthesis in angiosperm, and that a combination of glucose and ALA exhibited an additional effect. It is still unknown and remains to be further explored what is the mechanism of the effect of glucose and ALA on the Chl synthesis of rice in the dark.%本研究检测单子叶被子植物水稻(Oryza sativa L.)在完全黑暗中是否能合成叶绿素.以5 cm高的水稻黄化幼苗为研究材料,在黑暗中用不同浓度的葡萄糖和δ-氨基酮戊酸(δ-aminolevulinic

  17. 氨基酮戊酸光动力疗法对铜绿假单胞菌的杀灭作用的体外研究%Photodynamic inactivation of pseudomonas aeruginosa by 5-aminolevulinic acid in vitro

    Institute of Scientific and Technical Information of China (English)

    成琼辉; 陈年; 欧东; 刘渤; 伍津津; 雷霞

    2014-01-01

    目的:研究氨基酮戊酸(5-aminolevulinic acid,5-ALA)光动力疗法(photodynamic therapy)(ALA-PDT)对铜绿假单胞菌的杀灭作用。方法:以铜绿假单胞菌标准菌株ATCC27853为研究对象,采用ALA为光敏剂,用630nm的红光为光源,按不同的浓度剂量组合分为6组,用细菌涂板法观察细菌浓度,同时利用氯仿萃取法测定照射后48小时的绿脓毒素;结果:仅有光敏剂实验组与对照组(无ALA,无红光)细菌量相比,对铜绿假单胞菌无杀灭作用,仅有红光照射(90J/cm2×40分钟)组有轻度杀菌作用,抑制率为18.9%,而ALA与红光组合的三个ALA-PDT实验组对铜绿假单胞菌均有不同程度的杀菌作用(10nM ALA+90J/cm2红光×20分钟组的抑制率为82.0%,20nM ALA+90J/cm2红光×20分钟组的抑制率为96.4%,而20nM ALA+90J/cm2红光×40分钟组抑制率为100%),ALA-PDT对铜绿假单胞菌的杀灭作用随ALA浓度增高和红光能量增高作用加强;绿脓毒素的量在光动力治疗组也有明显下降,随剂量增加明显下降。结论:ALA-PDT对体外培养的铜绿假单胞菌ATCC27853具有明确的杀灭作用,能减少绿脓毒素分泌,且与剂量相关。%Objective To investigate the effect of 5-aminolevulinic acid-based photodynamic therapy (ALA-PDT) on pseudomonas aeruginosa planktonic cells in vitro. Medhods: Pseudomonas aeruginosa standard strain ATCC27853 was used in this study. Pseudomonas aeruginosa was divided into 6 groups according to different dose of ALA and 630nm red light. Spread plate method was used to count the bacteria. The chloroform extraction method was used to detect the exotoxin of Pseudomonas aeruginosa. Results:Compared with blank group, the experimental group with only ALA had no effect to Pseudomonas aeruginosa. But, the experimental group with only red light has mild inhibition (18.9%) to Pseudomonas aeruginosa. Pseudomonas aeruginosa was inhibited in three

  18. pH-sensing properties of cascaded long- and short-period fiber grating with poly acrylic acid/poly allylamine hydrochloride thin-film overlays

    Science.gov (United States)

    Yang, Ying

    2014-11-01

    Based on coupled-mode theory and transfer matrix method, the mode coupling mechanism and the reflection spectral properties of coated cascaded long- and short-period gratings (CLBG) are discussed. The effects of the thin-film parameters (film refractive index and film thickness) on the reflection spectra of the coated CLBG are simulated. By using electrostatic self-assembly method, poly acrylic acid (PAA) and poly allylamine hydrochloride (PAH) multilayer molecular pH-sensitive thin-films are assembled on the surface of the partial corroded CLBG. When the CLBG coated with PAA/PAH films are used to sense pH values, the resonant wavelengths of the CLBG have almost no shift, whereas the resonance peak reflectivities change with pH values. In addition, the sensitivities of the resonance peak reflectivities responding to pH values are improved by an order of magnitude.

  19. Cartap Hydrochloride Poisoning.

    Science.gov (United States)

    Kalyaniwala, Kimmin; Abhilash, Kpp; Victor, Peter John

    2016-08-01

    Cartap hydrochloride is a moderately hazardous nereistoxin insecticide that is increasingly used for deliberate self-harm in India. It can cause neuromuscular weakness resulting in respiratory failure. We report a patient with 4% Cartap hydrochloride poisoning who required mechanical ventilation for 36-hours. He recovered without any neurological deficits. We also review literature on Cartap hydrochloride poisoning.

  20. Dynamic Changes of Ephedrine Hydrochloride, Pseudoephedrine Hydrochloride, Amygdalin and Glycyrrhizic Acid in Different Compatibility of San-Ao Decoction%三拗汤不同配伍煎液中盐酸麻黄碱、盐酸伪麻黄碱、苦杏仁苷和甘草酸动态规律变化

    Institute of Scientific and Technical Information of China (English)

    张金花; 刘陶世; 程建明; 陈冬冬; 钱海峰

    2015-01-01

    目的:研究三拗汤在不同配伍煎液中盐酸麻黄碱、盐酸伪麻黄碱、苦杏仁苷和甘草酸的动态规律变化.方法:采用高效液相色谱法(HPLC)同时测定三拗汤煎液中盐酸麻黄碱、盐酸伪麻黄碱、苦杏仁苷和甘草酸的转移率,选用Kromasil C18(4.6 mm×250 mm,5μm)色谱柱,以流动相甲醇-0.1%磷酸进行梯度洗脱,流速为1 mL·min-1,柱温30℃,进样量10μL.其中盐酸麻黄碱、盐酸伪麻黄碱和苦杏仁苷在208 nm波长下检测,甘草酸铵在250 nm波长下检测.结果:麻黄碱转移率在合煎液中大于分煎液,伪麻黄碱转移率在麻黄与苦杏仁配伍中最高,苦杏仁苷转移率在麻黄与苦杏仁配伍中最高,甘草酸转移率在合煎液中大于分煎液.结论:中药复方在煎煮过程中存在动态规律变化,应根据其变化有针对性提高药物的有效性和稳定性.%This paper was aimed to study the dynamic changes of San-Ao(SA) decoction in different compatibility of ephedrine hydrochloride,pseudoephedrine hydrochloride,amygdalin and glycyrrhizic acid.HPLC was used to simultaneously determinate the transfer rate of SA decoction of ephedrine hydrochloride,pseudoephedrine hydrochloride,amygdalin and glycyrrhizic acid.Kromasil C18 (4.6 mm×250 mm,5μm) column was selected with methanol and 0.1% phosphoric acid as a mobile phase to gradient.The flow rate was 1 mL·min-1.The column temperature was 30℃.The injection volume was 10μL.Ephedrine hydrochloride,pseudoephedrine hydrochloride and amygdalin were detected at the wavelength of 208 nm.The glycyrrhizic acid was detected at the wavelength of 250 nm.The results showed that the transfer rate of ephedrine hydrochloride in decoction was more than that of the single preparation.The transfer rate of pseudoephedrine hydrochloride was the highest in the combination of ephedra and bitter almond.The transfer rate of amygdalin was the highest in the combination of ephedra and bitter almond.The transfer rate of

  1. A volumetric and viscometric study of 4-aminobutyric acid in aqueous solutions of metformin hydrochloride at 308.15, 313.15 and 318.15 K

    Directory of Open Access Journals (Sweden)

    KRISHA RAJAGOPAL

    2011-01-01

    Full Text Available Density (r and viscosity (h measurements were performed for4-aminobutyric acid in 0.05, 0.10 and 0.15 M aqueous metformin hydrochloride at 308.15, 313.15 and 318.15 K. The measured values of density and viscosity were used to estimate some important parameters, such as the partial molal volume, Vf, the standard partial molal volume, Vf, the standard partial molal volume of transfer, DVf, the hydration number, nH, the second derivative of the infinite dilution of the standard partial molal volume with temperature ¶2Vf/¶T2, the viscosity B-coefficients, variation of B with temperature, dB/dT, the free energy of activation per mole of solvent Dm1* and solute Dm2* of the amino acid in a ternary system. These parameters were interpreted in terms of solute–solute and solute–solvent interactions and structure making/breaking ability of solutes in the given solution.

  2. Terapêutica fotodinâmica com ácido delta-aminolevulínico em neoplasias queratinocíticas superficiais Photodynamic therapy with delta-aminolevulinic acid for superficial keratinocytic neoplasms

    Directory of Open Access Journals (Sweden)

    Renato Marchiori Bakos

    2003-04-01

    %, dor em cinco (6,7% e prurido em um caso (1,3%. A maioria dos casos (60% apresentou boa tolerância ao tratamento, não havendo efeitos paralelos dignos de nota. CONCLUSÕES: Os resultados obtidos no trabalho assemelham-se, em parte, aos relatados na literatura com aplicação única da terapêutica fotodinâmica com ácido delta-aminolevulínico em neoplasias queratinocíticas superficiais, principalmente nas ceratoses actínicas e na doença de Bowen.BACKGROUND: Photodynamic therapy (PDT is a treatment technique in which photosensitizing substances are applied in tissues and excited with specific wavelengths of light energy to obtain cell destruction through photoactive cytotoxic substances. This method has been used in several skin neoplasms, with quite successful results. OBJECTIVES: To study the effects of one single session of topical delta-aminolevulinic acid (ALA irradiated with incoherent light, in actinic keratosis (AK, superficial basal cell carcinoma (BCC and Bowen's disease (BD. PATIENT AND METHODS: Eighty skin lesions, in 52 patients, were treated with an incoherent light source prototype built by the Service of Biomedical Engineering of Hospital de Clínicas de Porto Alegre (HCPA, after the application of 20% ALA under occlusion. Thirty two (40% were superficial BCC, 37 (46.3% AK, and 11 (13.7% BD. Diagnosis was confirmed by biopsy and histology in 23 cases (28.7%. RESULTS: Follow up was not available in five lesions. From the remaining 75, 41 (54.6% were completely resolved, 22 (29.4% showed partial remission, and 12 (16.0% were considered as treatment failures. Considering the 35 treated AK, 23 (65.7% presented complete response, 7 (20% improved, and 5 (14.3% showed no benefit after treatment. Thirty BCC were treated, 10 (33.3% completely resolved, 13 (43.4% improved, and 7 (23.3% remained unaffected. From 10 treated BD, 8 (80% resolved and 2 (20% improved. Observed side effects were burning sensation in 24 lesions (32%, pain in 5 (6.7%, and itch in

  3. 5-氨基乙酰丙酸介导的光动力学治疗胃癌的实验研究%Effect of photodynamic therapy with 5-aminolevulinic acid on human gastric cancer cells in vitro

    Institute of Scientific and Technical Information of China (English)

    黄宗海; 周广军; 俞金龙; 厉周; 丁涟沭; 徐如祥; 姜晓丹

    2006-01-01

    目的探讨5-氨基乙酰丙酸(5-ALA)介导的光动力学对人胃癌细胞MGC-803的治疗作用.方法将不同浓度的5-ALA加入细胞培养基中,随之给予相同剂量的激光辐射;之后用固定浓度的5-ALA处理细胞,并给予不同剂量的激光辐射.MTT法测定细胞生存率.结果在相同的辐射剂量下,经0.25、0.5、1.0、2.0、4.0 mmol/L的5-ALA处理的细胞生存率分别为(70.07±5.37)%、(50.04±4.99)%、(34.53±5.30)%、(26.89±4.44)%和23.90%±2.80%,除2.0和4.0 mmol/L5-ALA两组间外,其余各组间具有显著性差异(F=266.39,P<0.001).在相同的5-ALA的浓度下,辐射剂量为6.25、12.5、25.0、50.0、100 J/cm2的细胞生存率分别为(83.50±10.43)%、(67.96±9.23)%、(33.80±8.26)%、(23.31±5.98)%和(14.96±3.50)%,各组之间有显著性差异(F=226.31,P<0.0001).而单用5-ALA处理细胞,对应于其浓度为0.25、0.5、1.0、2.0,和4.0 mmol/L时的细胞生存率分别为(96.46±6.72)%、(97.48±5.27)%、(98.33±6.67)%、(99.47±6.97)%和(95.66±7.72)%,各浓度之间无显著性差异(F=0.79,P=0.5383).单纯激光辐射,其剂量为6.25、12.5、25.0、50.0、100.0 J/cm2时的细胞生存率也无显著性差异(F=0.61,P=0.6551).结论在较低的浓度范围内,5-ALA介导的光动力学治疗对人胃癌MGC-803细胞的杀伤作用随着5-ALA浓度的增加而增加,在较高浓度时则存在饱和现象,杀伤力与光剂量成正比.单纯激光不能产生光动力效应,5-ALA本身对细胞无毒性作用.5-ALA介导的光动力学治疗是很有希望的胃癌治疗方法.%Objective To investigate the effect of 5-aminolevulinic acid (5-ALA)-mediated photodynamic therapy (PDT) on MGC-803 human gastric cancer cells in vitro. Methods MGC-803 human gastric cancer cells were treated with 5-ALA at various concentrations followed by laser irradiation. The cells were also treated with 5-ALA at the same concentration before laser exposure at various doses. PDT-induced phototoxicity of the cells was

  4. Synthesis, growth, morphology of the semiorganic nonlinear optical crystal L-glutamic acid hydrochloride and its structural, thermal and SHG characterizations

    Energy Technology Data Exchange (ETDEWEB)

    Dhanasekaran, P.; Srinivasan, K. [Crystal Growth Laboratory, Department of Physics, School of Physical Sciences, Bharathiar University, Coimbatore-641 046, Tamil Nadu (India)

    2012-12-15

    One of the halide derivatives of L-glutamic acid which was identified as a semiorganic nonlinear optical material, L-glutamic acid hydrochloride [HOOC(CH{sub 2}){sub 2}CH(NH{sub 2})COOH.HCl], was grown as bulk single crystal and its significant properties were characterized. The stoichiometric title compound was synthesized and the solubility of its recrystallized form in DD water was determined in the temperature range 30-80 C by gravimetric method. Structural confirmation was carried out by powder X-ray diffraction study through lattice parameter verification. Optical quality smaller dimension single crystals were grown from aqueous solution by self nucleation through slow evaporation of solvent method and a large dimension single crystal was grown by slow cooling method with reversible seed rotation technique. Morphological importances of different growth facets of the as grown crystals were studied through optical goniometry. Unit cell structure of the grown crystal was refined by single crystal X-ray diffraction analysis, functional groups present in the crystal responsible for various modes of vibrations were confirmed by FTIR spectroscopy analysis, thermal stability of the grown crystal was analysed by TG/DTA and DSC and second harmonic generation (SHG) of a fundamental Nd:YAG laser beam by Kurtz technique. Results indicate that the grown crystal is in stoichiometric composition and has significant improvement in its thermal and SHG properties when compared to pure L-glutamic acid polymorphs. (Copyright copyright 2012 WILEY-VCH Verlag GmbH and Co. KGaA, Weinheim)

  5. Differences Between the Concentrations in Rabbit Body Fluid of Berberine Hydrochloride,Chlorogenic Acid,Baicalin,and Their Minimal Inhibitory Concentrations

    Institute of Scientific and Technical Information of China (English)

    ZHANG Tao; HUANG Hui-ling; ZHANG Shuang; LU Ping; HU Ge; SUO Zhan-wei; JIANG Dai-xun; MU Xiang

    2009-01-01

    To explore the relationship between the heat-clearing and detoxicating functions and the bacteriostatic actions of berberine hydrochloride (Ber.H),chlorogenic acid (Chlo.A),and baicalin (Bai),their concentrations in rabbit body fluid were compared with their minimal inhibitory concentrations (MICs).Their concentrations in rabbit blood and tissue fluid were determined by reversed-phase high performance liquid chromatography,and their MICs to Escherichia coli were determined by tube dilution method.The results showed that the peak concentrations of Ber.H,Chlo.A,and Bai in rabbit blood were 3.2,5.03,and 7.63 μg mL-1,and in rabbit tissue fluid were 0.12,0.11,and 0.12 μg mL-1,respectively.Their MICs to E.coli were,respectively,1.0×103,3.75×103,and 6.75×103 μg mL-1,which were far higher than the concentrations in rabbit body fluids.This study indicates that Ber.H,Chlo.A,and Bai have weak bacteriostatic actions and do not reach their effective inhibitory concentrations in rabbit body fluids,and their heat-clearing and detoxicating functions are independent on the bacteriostatic actions.

  6. Cell adhesion properties of patterned poly(acrylic acid)/poly(allylamine hydrochloride) multilayer films created by room-temperature imprinting technique.

    Science.gov (United States)

    Lu, Yingxi; Sun, Junqi; Shen, Jiacong

    2008-08-05

    Patterned poly(acrylic acid) (PAA)/poly(allylamine hydrochloride) (PAH) multilayer films with line structures of different lateral size and vertical height were fabricated by a room-temperature imprinting technique, and their cell adhesion properties were investigated. The nonimprinted PAA/PAH multilayer films are cytophilic toward NIH/3T3 fibroblasts and HeLa cells whether PAA or PAH is the outer most layer. In contrast, the PAA/PAH multilayer films with a 6.5-microm-line/3.5-microm-space pattern structure are cytophobic toward NIH/3T3 fibroblasts and HeLa cells when the height of the lines is 1.29 microm. By either increasing the lateral size of the patters to 69-microm-line/43-mum-space or decreasing the height of the imprinted lines to approximately 107 nm, imprinted PAA/PAH multilayer films become cytophilic. This kind of transition of cell adhesion behavior derives from the change of the physical pattern size of the PAA/PAH multilayer films and is independent of the chemical composition of the films. The easy patterning of layer-by-layer assembled polymeric multilayer films with the room-temperature imprinting technique provides a facile way to tailor the cellular behavior of the layered polymeric films by simply changing the pattern dimensions.

  7. Clinical Effect of 5-aminolevulinic Acid Photodynamic Therapy Combined with Carbon Dioxide Laser on Condyloma Acuminatum in Senile Patients%5-氨基酮戊酸光动力联合CO2激光治疗老年尖锐湿疣临床疗效观察

    Institute of Scientific and Technical Information of China (English)

    李灿; 兰长贵; 梅晓锋; 陈伟; 赵静

    2015-01-01

    目的:探讨5-氨基酮戊酸光动力疗法(5-aminolevulinic acid photodynamic therapy ,ALA-PDT)联合CO2激光治疗老年尖锐湿疣的临床疗效。方法选择我院就诊的60例老年尖锐湿疣患者,随机分为治疗组和对照组各30人,对照组仅采用CO2激光去除疣体;治疗组用CO2激光去除疣体,用20%ALA溶液沿疣体周围2cm外敷创面,薄膜封包3小时后用光动力治疗仪距离患处15cm照射20分钟,每周1次,连续3周。治疗结束后两组患者均随访6个月。结果治疗组完成随访27例,对照组完成随访29例。治疗组治愈率为70.37%,对照组治愈率为37.93%,两组治愈率差异具有统计学意义(P<0.05)。结论5-氨基酮戊酸光动力联合CO2激光治疗老年尖锐湿疣治愈率高,复发率低。%Objective To discuss the clinical effect of 5-aminolevulinic acid photodynamic therapy (ALA-PDT) combined with car-bon dioxide laser on condyloma acuminatum in senile patients. Methods 60 senile out-patients with condyloma acuminatum were select-ed and divided randomly into 2 groups:treatment group and control group, 30 in each;carbon dioxide laser was applied in removing the warts of the patients in both groups while ALA-PDT was added to patients in treatment group:external application of 20%ALA liquid was made on the lesions and the round area within 2cm and the lesions were covered with occlusive film for 3 hours, and then were irra-diated by Photodynamic Therapeutic Apparatus with a distance of 15cm from the lesions for 20 minutes, once a week, 3 times in total;follow-up lasted from 6 months in both group. Results 27 patients in treatment group received follow-up while 29 in control group;the cure rate in treatment group was 70.37%while 37.93%in control group, the difference was of statistical significance (P<0.05). Conclu-sions 5-aminolevulinic acid photodynamic therapy (ALA-PDT) combined with carbon dioxide laser is of high cure rate and low reoccur

  8. Trifluridine and Tipiracil Hydrochloride

    Science.gov (United States)

    This page contains brief information about trifluridine and tipiracil hydrochloride and a collection of links to more information about the use of this combination drug, research results, and ongoing clinical trials.

  9. Stereospecific ligands and their complexes. VI. The crystal structure of (S,S-ethylenediamine-N,N’-di-2-propanoic acid hydrochloride, (S,S-H2eddp•HCl

    Directory of Open Access Journals (Sweden)

    VERICA V. GLODJOVIĆ

    2011-07-01

    Full Text Available (S,S-Ethylenediamine-N,N’-di-2-propanoic acid hydrochloride, (S,S-H2eddp·HCl, was prepared and its crystal structure determined. The compound was characterized by infrared and 1H- and 13C-NMR spectroscopy. It forms P1 in the space group of a triclinic crystal system with a = 5.3902(2 Å, b = 5.8967(2 Å, c = 10.3319(2 Å, a = 99.625(2°, b = 91.645(2°, g = 109.995(2° and Z = 1.

  10. A contribution to the determination of aflatoxin B1, quinine hydrochloride and L(+)-ascorbic acid in foodstuffs by quantitative in situ thin-layer chromatographic analysis

    NARCIS (Netherlands)

    Beljaars, P.R.

    1974-01-01

    The application of quantitative thin-layer chromatography (TLC) involving in situ spectrodensitometric measurements with a flying-spot densitometer is described in this study for the analysis of aflatoxin B 1 , quinine hydrochloride

  11. Neuroprotective effect of penehyclidine hydrochloride on focal cerebral ischemiareperfusion injury

    Institute of Scientific and Technical Information of China (English)

    Cuicui Yu; Junke Wang

    2013-01-01

    Penehyclidine hydrochloride can promote microcirculation and reduce vascular permeability. However, the role of penehyclidine hydrochloride in cerebral ischemia-reperfusion injury remains unclear. In this study, in vivo middle cerebral artery occlusion models were established in experimental rats, and penehyclidine hydrochloride pretreatment was given via intravenous injection prior to model establishment. Tetrazolium chloride, terminal deoxynucleotidyl transferase-mediated deoxyuridine triphosphate-biotin nick end labeling and immunohistochemical staining showed that, penehyclidine hydrochloride pretreatment markedly attenuated neuronal histopathological changes in the cortex, hippocampus and striatum, reduced infarction size, increased the expression level of Bcl-2, decreased the expression level of caspase-3, and inhibited neuronal apoptosis in rats with cerebral ischemia-reperfusion injury. Xanthine oxidase and thiobarbituric acid chromogenic results showed that penehyclidine hydrochloride upregulated the activity of superoxide dismutase and downregulated the concentration of malondialdehyde in the ischemic cerebral cortex and hippocampus, as well as reduced the concentration of extracellular excitatory amino acids in rats with cerebral ischemia-reperfusion injury. In addition, penehyclidine hydrochloride inhibited the expression level of the NR1 subunit in hippocampal nerve cells in vitro following oxygen-glucose deprivation, as detected by PCR. Experimental findings indicate that penehyclidine hydrochloride attenuates neuronal apoptosis and oxidative stress injury after focal cerebral ischemia-reperfusion, thus exerting a neuroprotective effect.

  12. 5-氨基酮戊酸光动力疗法治疗中、重度痤疮的疗效观察%The Study of Clinical Efficacy on 5-Aminolevulinic acid-photodynamic Therapy in Treatment of Moderate and Severe Acne

    Institute of Scientific and Technical Information of China (English)

    黄咏梅

    2013-01-01

    目的 观察5%5-氨基酮戊酸光动力疗法治疗中、重度痤疮的临床疗效和安全性.方法 将60例中、重度痤疮患者随机分为治疗组和对照组.治疗组根据患者皮损面积配制易透皮吸收的5%5-氨基酮戊酸凝胶外敷于皮损处,避光1h后,戴护目镜,红光照射20min,每周治疗1次,共4次.对照组仅采用红光照射,隔日治疗1次,共14次.每次治疗前进行疗效观察及不良反应记录,两组患者均在治疗4周后,进行疗效判定,随访6个月.结果 治疗组5%5-氨基酮戊酸光动力疗法(ALA-PDT)治疗4次后有效率为93.33%,对照组为73.33%,两组差异有统计学意义(P<0.05).结论 5%5-氨基酮戊酸光动力疗法治疗中重度痤疮安全、有效,疗效优于单用红光.%Objective To evaluate the efficacy and safety of 5-aminolevulinic acid-photodynamic(ALA-PDT)on patients with moderate and severe acne.Methods Sixty patients were randomly divided into treatment group and control group.5%5-aminolevulinic acid-mediated photodynamic gel,which was prepared to be easily absorbed according to the extent of skin lesions,was external application to the patients in treatment group.After 1 hour away from light,those patients received a treatment for 20 minutes' red laser irradiation wearing goggles once a week,which lasted 4 weeks in all.In control group,only a treatment of red laser irradiation on every other day was applied,which were a total of 14 times treatment.The efficacy was evaluated 4weeks later.All patients were observed and recorded the therapeutic and side effects before every treatment,and were followed up for 6 months.Results The total effective rate of two groups was 93.33%and 73.33%respectively after 4-week treatment.There were obvious statistics differences of efficacy between ALA-PDT and red laser only(P<0.05).Conclusion ALA-PDT which is effective and safe in treatment of moderate and severe acne surpassed the red laser irradiation only.

  13. 5-aminolevulinic acid-mediated photodynamic therapy combined with CO2 laser therapy in treatment of condyloma acuminatum%5-氨基酮戊酸光动力疗法联合二氧化碳激光治疗尖锐湿疣的疗效观察

    Institute of Scientific and Technical Information of China (English)

    顾俊瑛; 史玉玲; 李秀丽; 李晓建; 刘至昱; 高飞

    2011-01-01

    目的 比较5-氨基酮戊酸光动力疗法(5-aminolevulinic acid-mediated photodynamic therapy,ALA-PDT)和二氧化碳( CO2)激光治疗尖锐湿疣(CA)的临床疗效.方法 将同济大学附属第十人民医院皮肤科2010年4月至2010年12月就治的111例尖锐湿疣患者分为3组,第一组为特殊部位(尿道口、系带或宫颈部位)的疣体患者,共17例,单用ALA-PDT治疗;余94例患者随机分为两组,每组47例,分别采用ALA-PDT联合CO2激光治疗和单一CO2激光治疗.ALA-PDT每周治疗1次,3次为1个疗程.CO2激光治疗根据疣体大小一次或分次清除疣体.3组患者治疗结束后每1、2、3个月分别电话随访一次.结果 单用ALA-PDT组一个疗程结束后的清除率为93.4%(16/17),3个月后总复发率为11.8%(2/17).联合治疗组和CO2激光单一治疗组3个月后的总复发率分别为14.9%(7/47)和55.3%(26/47),差异有统计学意义(x2=16.857,P<0.001).结论 ALA-PDT联合CO2激光治疗CA疗效确切,复发率低;ALA-PDT可有效治疗特殊部位的疣体,临床适用范围广.%Objective To evaluate the efficacy of 5-aminolevulinic acid-mediated photodynamic therapy (ALA-PDT) combined with CO2 laser therapy in treatment of condyloma acuminatum. Methods One hundred and eleven patients with condyloma acuminatum admitted from April to December 2010 were enrolled in the study. Seventeen cases whose condylomas are at urethral orifice, vinculum or cervix uteri were treated with ALA-PDT alone. Other 94 cases were randomly assigned into two groups with 47 in each, who were treated by ALA-PDT combined with CO2 laser therapy or CO2 laser alone, respectively. Results The clearance rate was 93. 4% (16/17) and the relapse rate was 11.8% (2/17) in patients treated with ALA-PDT alone. The relapse rates of ALA-PDT combined with CO2 laser and CO2 laser alone were 14. 9% (7/47 ) and 55. 3% (26/47 ) , respectively (x2 = 16. 857, P < 0. 001). Conclusion ALA-PDT is effective in treatment of condyloma

  14. Effect of 5-aminolevulinic acid-mediated photodynamic therapy on human gastric cancer xenografts in nude mice in vivo%5-氨基乙酰丙酸介导的光动力学对裸鼠人胃癌移植瘤的治疗作用

    Institute of Scientific and Technical Information of China (English)

    周广军; 黄宗海; 俞金龙; 厉周; 丁涟沭

    2008-01-01

    Objective To investigate the effect of 5-aminolevulinic acid (ALA)-mediated photodynamic therapy (PDT) on human gastric cancer xenografts in vivo and to explore its potential tumoreidal mechanism. Methods Cultured MGC-803 human gastric cancer cells were injected below the skins of the nude mice to develop the tumor model. The tumor-bearing nude mice were examined under the Leica LT-9MACIMSYSPULS to detect the fluorescence. The tumor volume of day 1, 3, 7, 14, 21 after treatment were measured, and its histological changes were also studied. The tissues of the tumors in nude mice of the control group, light group, 5-ALA group and PDT group were examined with the electron microscope and apoptosis was detected by TUNEL assay. Results The tumor model was successfully developed. The tumor in the nude mice emited the red fluorescence under the Leica LT-9MACIMSYSPULS. The tumor volumes were (0.189±0.010)cm3, (0.183±0.011)cm3, (0.185±0.019) cm3, (0.182±0.015)cm3 for the control group, light group, 5-ALA group, PDT group, respectively at day 1 after treatment, while at day 3, (0.294±0.010)cm3, (0.280±0.013)cm3, (0.278±0.016)cm3, (0.183±0.014)cm3;at day 7, (0.409±0.016)cm3, (0.411±0.009)cm3, (0.407±0.015)cm3, (0.221±0.008)cm3;at day 14, (0.970±0.055)cm3 (0.976±0.054)cm3, (0.981±0.032)cm3, (0.318±0.005)cm3;at day 21, (1.495±0.059)cm3, (1.513±0.057)cm3, ( 1.524±0.063)cm3, (0.446±0.042)cm3(F=1003.086, P=0.000). The histology demonstrated that most tumor blood vessels were congested and necrosis developed after PDT while not in the control group, light group and 5-ALA group. Necrosis and apoptosis were observed in the cells of the tumors of the PDT group examined by TUNEL and electron microscope while not in the cells of the tumors of the other groups. Conclusions 5-aminolevulinic acid-mediated photodynamic therapy (PDT) can induce injury to human gastric cancer xenografts and inhibit the tumor growth while light only and 5-ALA only can not. 5-aminolevulinic

  15. Absorption Spectra of the 4f Electron Transitions of the Nd, Ho and and Er Complexes with 1-Cyclopyropyl-6-fluoro-1,4-dihydro-7-(4-ethyl-1-piperazin yl)-4-oxo-3-quinoline Carboxylic Acid Hydrochloride in the Presence of TX-100

    Institute of Scientific and Technical Information of China (English)

    2002-01-01

    The absorption spectra of the neodymium, holmium and erbium complexes with l-cyclopropyl-6-fluoro-l,4-dihydro-7-(4-ethyl-l-piperazinyl)-4-oxo-3-quinoline carboxylic acid hydrochloride in the presence of TX-100 have been shown. The characteristic absorption bands of the 4f electron transitions of the complexes are enhanced markedly.

  16. Kinetic and analytical study on precipitation reactions with /sup 110/AgNO/sub 3/ of some di(. beta. -chloroethyl)amine derivatives and hydrochlorides with esters of N-(p-aminobenzoyl)-L-aspartic acid as carriers from dimethylformamide - water solution

    Energy Technology Data Exchange (ETDEWEB)

    Cecal, Al.; Sunel, V.; Ghimiciu, L. (Institutul Politehnic, Iasi (Romania))

    1983-01-01

    The kinetics of precipitation reactions with /sup 110/AgNO/sub 3/ of some di(..beta..-chloroethyl) amine derivates and hydrochlorides with esters of N-(p-aminobenzoyl)-L-aspartic acid as carriers in dimethylformamide-water mixture, were studied. The rate constants of these reactions were of the order of 10/sup -4/ lxmol/sup -1/xmin/sup -1/. The concentrations of the corresponding hydrochloride solutions were measured by radiometric titration with /sup 110/AgNO/sub 3/ solution of given concentration.

  17. Effect of matrine hydrochloride on liver injury

    Institute of Scientific and Technical Information of China (English)

    CHEN Li-bo; XU Feng; MA Wen-hui

    2008-01-01

    Objective Searching the function that the Injection of the matrine hydrochloride prevents and cures acute chemical liver injury of mice、 immunity liver injury of mice and chronic liver injury of rats. Methods Acute hepatic injury models of mice induced by Chemical poison carbon tetrachloride (CCl4), thioacetamide(TAA), D-galactosamine(D-GalN), immunity hepatic injury model of mice induced by BCG and fat polysaccharide (LPS), chronic liver injury model of rats induced by CCI, were introduced in the experiment. The serum ALT and AST were measured in acute hepatic injury experiments. Serum ALT, AST, AKP, ALB, TP, BiL-T, ereatinine, triglyceride, sialie acid, larninin, hyaluronic acid, type Ⅲ proeollagen and type Ⅳ collagen, hepatic hydroxyproline (HyP) of rats in chronic liver injury animals were determined after Injection of the matrine hydrochloride. Results The Injection of the matrine hydrochloride reduced serum ALT and AST level of acute chemical liver injury of mice induced by CCl4, TAA and D-GaIN. The index of the liver and the spleen of immunity liver injury of mice induced by BCG and LPS were decreased after the injection of matrine hydrochloride treatment. Compared with the model group, the injection may obviously inhibited serum ALT, AST, TP, AKP, TRI, BiL-T, creatinine, triglyceride, sialic acid, laminin , hyaluronic acid , type Ⅲ procollagen and type Ⅳ collagen activity of chronic liver injury of rats induced by CCl4, elevated ALB、A/G, reduced the liver HyP, decreased the index of the liver and the spleen. The liver visual observation, the pathology inspection and the HAI grading result showed the injection may reduce the inflammatory activity in liver tissue, restrain the liver cell damage, reduce the pseudolobuli formation. Conclusions The Injection of matrine hydrochloride had the protective function to acute chemical hepatic injury of mice induced by CCl4、TAA、D-GalN、immunity hepatic injury of mice induced by the BCG and LPS and

  18. Efficacies of cryotherapy plus 5-aminolevulinic acid-photodynamic therapy in patients with condyloma acuminatum and nursing experiences%冷冻联合5-氨基酮戊酸光动力治疗尖锐湿疣的临床疗效观察和护理体会

    Institute of Scientific and Technical Information of China (English)

    段颖; 黄英

    2015-01-01

    用冷冻联合5-氨基酮戊酸光动力(ALA-PDT)和单独光动力两种方法治疗65例尖锐湿疣患者.冷冻时动作轻柔,深度适中,光动力治疗时敷药、照光护理细致、全面,出现不良反应者给予康复新液湿敷和抗生素软膏.联合组先冷冻2次,再经ALA-PDT治疗1~3次,单独治疗组经ALA-PDT治疗1~4次,所有患者均给予1次ALA-PDT巩固治疗.联合组治愈率83% (29/35),复发率17%(6/35);光动力组治愈率70%(21/30),复发率30%(9/30).冷冻联合光动力疗法是一种实用、疗效更好、复发率更低的治疗方法,治疗时全面、细致、舒适的护理能保证临床疗效,减少复发和治疗的不适感.%A total of 65 patients of condyloma acuminatum (CA) received cryotherapy plus 5-aminolevulinic acid-photodynamic therapy (ALA-PDT) or ALA-PDT alone.During cryotherapy,handling was gentle with a moderate depth.The nursing of PDT was both meticulous and comprehensive.Patients with adverse reactions received Kangfuxin liquid for wet packing and topical antibiotic ointment.The combination group received cryotherapy for 2 sessions and then PDT for 1-3 sessions while PDT was administered for 1-4 sessions in single PDT group.Then all patients received PDT once for consolidation therapy.For groups 1 and 2,the effective rates were 83% and 70% and the recurrent rates 17% and 30% respectively.Cryotherapy plus ALA-PDT is feasible for CA and it offers better efficacies and lower recurrent rates.And comprehensive,meticulous and comfortable nursing may achieve clinical efficacies,reduce the recurrent rate and minimize discomforts during treatment.

  19. Simultaneous Estimation of Gemcitabine Hydrochloride and Capecitabine Hydrochloride in Combined Tablet Dosage Form by RP-HPLC Method

    Directory of Open Access Journals (Sweden)

    V. Rajesh

    2011-01-01

    Full Text Available A new reverse phase high performance liquid chromatography (RP-HPLC method has been developed for the simultaneous estimation of gemcitabine hydrochloride and capecitabine hydrochloride in combined tablet dosage form. An inertsil ODS-3 C-18 column having dimensions of 250×4.6 mm and particle size of 5 µm, with mobile phase containing a mixture of acetonitrile : water : triethyelamine in the ratio of (70 : 28 : 2v/v was used. The pH of mobile phase was adjusted to 4.0 with ortho-phosphoric acid. The flow rate was 1 mL/min and the column effluents were monitored at 260 nm. The retention time for gemcitabine hydrochloride and capecitabine hydrochloride was found to be 2.76 and 2.3 min respectively. The proposed method was validated in terms of linearity, accuracy, precision, limit of detection, limit of quantitation and robustness. The method was found to be linear in the range of 10-50 µg/mL and 4-24 µg/mL for gemcitabine hydrochloride and capecitabine hydrochloride, with regression coefficient r = 0.999 and r = 0.999, respectively.

  20. Advances in the treatment of skin diseases with δ-aminolevulinic acid-based photodynamic therapy%δ-氨基酮戊酸光动力学疗法治疗皮肤病的研究进展

    Institute of Scientific and Technical Information of China (English)

    夏育民; 徐世正

    2008-01-01

    δ-氨基酮戊酸光动力学疗法是一种非创伤性局部治疗技术,可特异性杀死病变细胞.近年研究表明,该疗法对靶细胞某些生物学特征的影响是重要作用机制之一.除非色素细胞性皮肤恶性肿瘤外,δ-氨基酮戊酸光动力学疗法的适应症逐渐扩展至癌前病变、病毒疣、痤疮、结缔组织病、光化性疾病等范围.升高温度、促溶剂、金属离子螫合物、电离子导入、脂质体载体等因素可促进其疗效.%δ-aminolevulinic acid(ALA)-based photodynamic therapy(PDT)is a noninvasive topical treatment choice that can selectively kill target cells.One important mechanism for its therapeutic effect is to intluence some biological characteristics of target cells.Besides nonpigment cell malignant tumors of skin,ALA-PDT could be used in the treatment of premalignant lesions,viral warts,acne,connective tissue diseases,actinic skin diseases,and SO on.Appropriate higher temperature,cosolvents,metal chelating agents.iontoplaoretic delivery and liposome vector may enhance the therapeutic efrect of ALA-PDT.

  1. Determination of berberine hydrochloride and gallic acid in Suxiao Zhixie capsules by HPLC%HPLC-PDA法测定速效止泻胶囊中盐酸小檗碱的含量

    Institute of Scientific and Technical Information of China (English)

    何琳; 孙银华

    2011-01-01

    Aim To establish a method for the determination of berberine hydrochloride and gallic acid in Suxiao Zhixie capsules.Methods The separation was performed on SunfireTM C18column(5 μm,4. 6 mm × 150 mm) . The column temperature was 35 ℃ . The mobile phase was methonal-acetonitrile-0. 1%phasphoric acid( 3∶ 2 ∶ 95 ) and eluted with a gradient. The flow rate was 1. 0 ml · min -1·The injection volume was 20 μl, The detection wavelength was at 270 nm. Results The linear of berberine hydrochloride was in the range of 20. 931 - 209. 31 mg · L -1 ( r = 1. 000 0) . The average recovery was 100. 02% and RSD was 1. 5% ( n = 6) . The linear of gallic acid was in the range of 13. 075 - 130. 754μg · L-1 ( r = 1. 000 0). Conclusions The method is convenient , rapid, economical and accurate. It can be used for quality control of Suxiao Zhixie capsules.%目的 建立以高效液相色谱法测定速效止泻胶囊中盐酸小檗碱和没食子酸含量的方法.方法 采用SunfireTM C18(5 μm,4.6 mm×150 mm)色谱柱,柱温:35℃.流动相为甲醇-乙腈-0.1%磷酸(3:2:95),采用梯度洗脱程序,流速1.0 ml·min-1,进样量为20 μl,检测波长:270 nm.结果 盐酸小檗碱在20.931~209.31 mg·L-1范围内呈良好的线性关系,r=1.0000,平均回收率为100.02%,RSD=1.5%(n=6).没食子酸在13.075~130.754 mg·L-1范围内呈良好的线性关系,r=1.0000.结论 该方法简单、快速、准确、重现性好,能够较好地控制该产品的质量.

  2. Allergic contact dermatitis to methyl aminolevulinate after photodynamic therapy in 9 patients.

    Science.gov (United States)

    Hohwy, Thomas; Andersen, Klaus Ejner; Sølvsten, Henrik; Sommerlund, Mette

    2007-11-01

    This report describes 9 patients who developed allergic contact dermatitis to methyl aminolevulinate used for photodynamic therapy (PDT). The risk of developing contact allergy to methyl aminolevulinate in PDT treated patients was calculated to 1% after an average of 7 treatments (range 2-21).

  3. Allergic contact dermatitis to methyl aminolevulinate after photodynamic therapy in 9 patients

    DEFF Research Database (Denmark)

    Hohwy, Thomas; Andersen, Klaus Ejner; Sølvsten, Henrik;

    2007-01-01

    This report describes 9 patients who developed allergic contact dermatitis to methyl aminolevulinate used for photodynamic therapy (PDT). The risk of developing contact allergy to methyl aminolevulinate in PDT treated patients was calculated to 1% after an average of 7 treatments (range 2...

  4. 5-Aminolevulinic acid fluorescence-guided surgery for spinal meningioma.

    Science.gov (United States)

    Muroi, Carl; Fandino, Javier; Coluccia, Daniel; Berkmann, Sven; Fathi, Ali-Reza; Landolt, Hans

    2013-01-01

    Fluorescence-guided surgery for cranial meningioma has been reported to be useful. There are no reports about spinal cases using this technique. We report on a meningioma of the cervical spine for which fluorescence-guided surgery was used. A 78-year-old female patient with a meningioma located in the cervical spine underwent surgery using fluorescence guidance. After complete removal of the meningioma and removal and coagulation of the dural attachment (equal to Simpson grade II resection), a fluorescence-positive remnant could be identified and successfully removed. The remnant was found to harbor meningioma tissue on histological examination. Fluorescence-guided microsurgery is helpful in achieving a total resection of spinal meningiomas, and might therefore reduce the risk of recurrence. Copyright © 2013 Elsevier Inc. All rights reserved.

  5. Interaction between lidocaine hydrochloride (with and without adrenaline) and various irrigants: A nuclear magnetic resonance analysis

    Science.gov (United States)

    Vidhya, Nirmal; Karthikeyan, Balasubramanian Saravana; Velmurugan, Natanasabapathy; Abarajithan, Mohan; Nithyanandan, Sivasankaran

    2014-01-01

    Background: Interaction between local anesthetic solution, lidocaine hydrochloride (with and without adrenaline), and root canal irrigants such as sodium hypochlorite (NaOCl), ethylene diamine tetra-acetic acid (EDTA), and chlorhexidine (CHX) has not been studied earlier. Hence, the purpose of this in vitro study was to evaluate the chemical interaction between 2% lidocaine hydrochloride (with and without adrenaline) and commonly used root canal irrigants, NaOCl, EDTA, and CHX. Materials and Methods: Samples were divided into eight experimental groups: Group I-Lidocaine hydrochloride (with adrenaline)/3% NaOCl, Group II-Lidocaine hydrochloride (with adrenaline)/17% EDTA, Group III- Lidocaine hydrochloride (with adrenaline)/2% CHX, Group IV-Lidocaine hydrochloride (without adrenaline)/3% NaOCl, Group V-Lidocaine hydrochloride (without adrenaline)/17% EDTA, Group VI-Lidocaine hydrochloride (without adrenaline)/2% CHX, and two control groups: Group VII-Lidocaine hydrochloride (with adrenaline)/deionized water and Group VIII-Lidocaine hydrochloride (without adrenaline)/deionized water. The respective solutions of various groups were mixed in equal proportions (1 ml each) and observed for precipitate formation. Chemical composition of the formed precipitate was then analysed by nuclear magnetic resonance spectroscopy (NMR) and confirmed with diazotation test. Results: In groups I and IV, a white precipitate was observed in all the samples on mixing the respective solutions, which showed a color change to reddish brown after 15 minutes. This precipitate was then analysed by NMR spectroscopy and was observed to be 2,6-xylidine, a reported toxic compound. The experimental groups II, III, V, and VI and control groups VII and VIII showed no precipitate formation in any of the respective samples, until 2 hours. Conclusion: Interaction between lidocaine hydrochloride (with and without adrenaline) and NaOCl showed precipitate formation containing 2,6-xylidine, a toxic compound

  6. Interaction of articaine hydrochloride with prokaryotic membrane lipids.

    Science.gov (United States)

    Lygre, Henning; Moe, Grete; Nerdal, Willy; Holmsen, Holm

    2009-01-01

    Local anesthetics are the most commonly used drugs in dentistry, with a wide range of effects, including antimicrobial activity. High antimicrobial effects have recently been reported on oral microbes from articaine hydrochloride, revealed by the minimum inhibitory concentration and minimal bactericidal concentration. Additionally, articaine has recently been used as an alkaline component in endodontic materials with a proposed antibacterial activity. However, the detailed mechanisms of action have not been discussed. We determined the Langmuir surface pressure/molecular area isotherms of prokaryotic lipid monolayers, as well as the phospholipid phase transitions, by employing differential scanning calorimetry on unilamellar prokaryotic liposomes (bilayers). Articaine hydrochloride was found to interact with the prokaryotic membrane lipids in both monolayers and bilayers. An increase of the phospholipid molecular area of acidic glycerophospholipids as well as a decrease in phase transition temperature and enthalpy were found with increasing articaine hydrochloride concentration. The thermodynamic changes by adding articaine hydrochloride to prokaryotic membrane lipids are potentially related to the effects observed from antimicrobial peptides resulting from membrane insertion, aggregate composition, pore formation, and lysis. Interaction of articaine hydrochloride with prokaryotic membrane lipids is indicated. Hence, further research is necessary to gain insight into where these compounds exert their effects at the molecular level.

  7. Spectrophotometric estimation of pioglitazone hydrochloride in tablet dosage form

    Directory of Open Access Journals (Sweden)

    Basniwal Pawan

    2008-01-01

    Full Text Available Two simple, rapid, and precise methods - linear regression equation (LRE and standard absorptivity - were developed and validated for the estimation of pioglitazone hydrochloride in tablet dosage form. The maximum absorbance (lmax of pioglitazone hydrochloride was found to be 269.8 nm in methanol:water:hydrochloric acid (250:250:1. Beer-Lambert law was obeyed in the concentration range of 10-50 µg/ml, and the standard absorptivity was found to be 253.97 dl/g/cm. Both the methods were validated for linearity, accuracy, precision (days, analysts, and instrument variation, and robustness (solvent composition. The numerical values for all parameters lie within the acceptable limits. Pioglitazone hydrochloride was estimated in the range of 99.58-99.97% by LRE method and 100.25-100.75% by standard absorptivity method. At 99% confidence limit, the F-test value for the methods was found to be 1.8767.

  8. Effects of exogenous 5-aminolevulinic acid on chlorophyll fluorescence characteristics and energy dissipation of Sarcandra glabra under drought stress%外源5-氨基乙酰丙酸对干旱胁迫下草珊瑚叶绿素荧光特性及能量分配的影响

    Institute of Scientific and Technical Information of China (English)

    张春平; 何平; 袁凤刚; 喻泽莉; 杜丹丹; 韦品祥; 胡世俊

    2012-01-01

    Objective To study the effects of drought stress on chlorophyll fluorescence characteristics and energy dissipation of Sarcandra glabra and get the method of alleviating drought stress, so as to provide theoretical basis against drought in planting. Methods Several physiological indexes of S. Glabra treated by 5-aminolevulinic acid (ALA) under drought stress (PEG-6000 at the concentration of 15%) were measured, such as the contents of photosynthetic pigment, chlorophyll fluorescence parameters, and energy parameters. Results Exogenous ALA obviously increased the content of chlorophyll and carotenoids, enhanced the maximum fluorescence (Fm), photochemical efficiency of photosystem II (PSII, Fv/Fm), potential photochemical efficiency (Fv/Fo), photochemical efficiency (Fv'/Fmr), PSII actual photochemical efficiency (OPSII), photochemical quenching coefficient (qP), electronic transfer rate (ETR), and photochemistry rate (PCR), as well as significnatly decreased the level of minimum fluorescence (Fo), non-photochemical quenching (NPQ) coefficient, and heat dissipation rate (HDR). The proportion of ALA absorbed light in photochemistry (P) was increased, the fraction of antenna pigment heat dissipation (D) and excess energy (£) for NPQ was decreased. The fraction of P was the main pathway for excessive energy dissipation. ALA could promote the redistribution of energy reasonablely. Conclusion Exogenous ALA (100 mg/L) could significantly reduce the dissipation of excess excitation energy, improve the photochemical electron transport efficiency,and efficiently protect leaf blade of S. Glabra from PSII damage under drought stress. ALA could obviously promote the droughtresistance of S. Glabra plantlet.%目的 探讨干旱胁迫对草珊瑚叶绿素荧光特性及能量分配的影响,找到延缓干旱胁迫的方法,为抗旱栽培提供理论依据.方法 考察15% PEG-6000模拟干旱胁迫条件下,经过不同浓度5-氨基乙酰丙酸(ALA)和不同时间处理后

  9. A study on clinical efifcacy of two kinds of concentration of 5-Aminolevulinic acid photodynamic therapy in treatment of moderate to severe acne%两种浓度5-氨基酮戊酸光动力疗法治疗中重度痤疮疗效观察

    Institute of Scientific and Technical Information of China (English)

    刘海波; 王雪松

    2016-01-01

    目的:探讨两种浓度5-氨基酮戊酸光动力疗法(ALA-PDT)治疗中重度痤疮的有效性及安全性。方法:将68例中重度痤疮患者随机分为两组:低浓度组:31例,给予5%ALA-PDT治疗;高浓度组:37例,给予10%ALA-PDT治疗,两组均每2周治疗1次,共治疗3次。在治疗后第2、4、6周对两组患者进行疗效判断和比较,同时记录治疗过程中出现的不良反应。结果:31例接受5%ALA-PDT治疗的患者经3次治疗后,总有效率87.10%;37例接受10%ALA-PDT治疗的患者经3次治疗后,总有效率为94.59%,两组疗效相比无统计学意义(P>0.05)。结论:5%ALA封包组与10%ALA封包组疗效相比无统计学意义,但低浓度组红斑、水肿、色素沉着等不良反应小。%Objective To study the safety and efifcacy of two kinds of concentrations of 5-aminolevulinic acid photodynamic therapy (5-ALA-PDT) in the treatment of moderate to severe acne. Methods 68 patients with moderate to severe acne were randomly divided into two groups:31 cases in low concentration group were treated with 5%5-ALA followed by red laser irradiation with a photodynamic therapy device;37 patients in high concentration group were treated with 10%5-ALA followed by red laser irradiation with a photodynamic therapy device. Patients in both groups were treated once every two weeks, 3 times totally. The patients were followed up 2, 4, and 6 weeks after the treatment, the therapeutic effects in two groups were compared and the adverse reactions were recorded. Results After 3 times treatments, the total effective rates of low and high concentration groups were respectively 87.1%and 94.59%. There was no signiifcant difference between the two groups (P>0.05). Conclusion The clinical efifcacy has no signiifcant difference between 5%5-ALA group and 10%5-ALA group, but the cases with adverse reactions in 5%5-ALA group, such as erythema, oedema, hyperpigmentation, were less.

  10. Effects of Foliar Spraying 5 - Aminolevulinic Acid on Growth, Photosynthesis and Yield of Tomato under Shade Conditions%叶面喷施5-氨基乙酰丙酸对遮阴条件下番茄生长、光合特性和产量的影响

    Institute of Scientific and Technical Information of China (English)

    郭晓青; 李超汉; 李青竹; 李霞; 李衍素; 于贤昌

    2011-01-01

    为明确喷施外源5-氨基乙酰丙酸(ALA)对弱光条件下番茄生长发育的影响,以“金丰盛冠”番茄为材料,研究了叶面喷施ALA(0.06 g/m2)对遮阴条件下番茄植株形态、叶绿素含量、光合特性及产量的影响.结果表明,遮阴处理使番茄植株高度增加,茎粗减小,叶片净光合速率(Pn)、气孔导度(Gs)、羧化效率(CE)、表观量子效率(AQY)、光补偿点(LCP)和产量降低,胞间二氧化碳浓度(Ci)、CO2补偿点(CCP)和叶绿索含量升高.遮阴环境下,叶面喷施ALA使番茄叶片Pn、Gs、CE、AQY、LCP和产量的降低幅度及Ci、CCP的升高幅度减小,并提高了叶绿素的含量,但对植株形态的影响不显著.叶面喷施ALA对80%遮阴下番茄生长、光合特性和产量的影响较小.表明在遮阴导致的弱光环境下,叶面喷施ALA能在一定程度上提高番茄叶片的光合能力,提高产量,并在一定范围内缓解遮阴对番茄生长造成的不利影响.%To make clear the influence of 5 - aminolevulinic acid ( ALA ) on the growth and development of tomato under weak light, the plant height, stem diameter, photosynthesis characteristics, chlorophyll content and yield of tomato were investigated after sprayed 0.06 g/m2 ALA. The results showed that the stem diameter, net photosynthetic rate (Pn), stomatal conductance (Gs), carboxylation efficiency (CE) , apparent quantum yield ( AQY) , the light compensation point ( LCP) and yield of tomato were decreased by shadingtreatment. On the contrary, the intercellular CO2 concentration ( Ci) and CO2 compensation point ( CCP) , chlorophyll content and plant height of tomato increased. Compared with spraying water, the decrease range of Pn, Gs, CE, AQY, LCP and yield and the increase range of Ci and CCP were relatively smaller after sprayed ALA under shade conditions, while the chlorophyll content increased. The foliar application of ALA had little influence on the tomato growth, photosynthesis

  11. 三氯异氰尿酸与盐酸环丙沙星对蛋白核小球藻的毒性效应%Toxic effects of trichloroisocyanuric acid and ciprofloxacin hydrochloride on a freshwater alga, chlorella pyrenoidosa

    Institute of Scientific and Technical Information of China (English)

    聂湘平; 王翔; 陈菊芳; 鹿金雁; 李潇; 杨永涛

    2007-01-01

    测试了典型渔药三氯异氰尿酸(Trichloroisocyanuric acid,TCCA)、盐酸环丙沙星(Ciprofloxacin hydrochloride,CPFX)对蛋白核小球藻(Chlorella pyrenoidosa)的急性毒性及其Ⅰ相、Ⅱ相代谢酶活性的影响.结果表明,TCCA和CPFX作用小球藻96h后EC50分别为0.31 mg·L-1和20.61mg·L-1.TCCA在低浓度下对小球藻Ⅰ、Ⅱ相代谢酶GSH、GST、CAT和EROD都存在诱导作用,当TCCA浓度大于0.13 mg·L-1时,对GSH、GST和EROD的诱导减弱.GSH、GST、EROD三种酶对CPFX作用的响应较弱,当CPFX大于70.20mg·L-1时,GST受到显著抑制,而EROD则明显升高,与对照组差异显著,GSH没有明显变化.CAT对CPFX作用的响应较敏感,表现为典型适应性诱导现象"钟形曲线",适合作为CPFX暴露的生物标记物.

  12. Evolution of cyclizing 5-aminolevulinate synthases in the biosynthesis of actinomycete secondary metabolites: outcomes for genetic screening techniques.

    Science.gov (United States)

    Petříčková, Kateřina; Chroňáková, Alica; Zelenka, Tomáš; Chrudimský, Tomáš; Pospíšil, Stanislav; Petříček, Miroslav; Krištůfek, Václav

    2015-01-01

    A combined approach, comprising PCR screening and genome mining, was used to unravel the diversity and phylogeny of genes encoding 5-aminolevulinic acid synthases (ALASs, hemA gene products) in streptomycetes-related strains. In actinomycetes, these genes were believed to be directly connected with the production of secondary metabolites carrying the C5N unit, 2-amino-3-hydroxycyclopent-2-enone, with biological activities making them attractive for future use in medicine and agriculture. Unlike "classical" primary metabolism ALAS, the C5N unit-forming cyclizing ALAS (cALAS) catalyses intramolecular cyclization of nascent 5-aminolevulinate. Specific amino acid sequence changes can be traced by comparison of "classical" ALASs against cALASs. PCR screening revealed 226 hemA gene-carrying strains from 1,500 tested, with 87% putatively encoding cALAS. Phylogenetic analysis of the hemA homologs revealed strain clustering according to putative type of metabolic product, which could be used to select producers of specific C5N compound classes. Supporting information was acquired through analysis of actinomycete genomic sequence data available in GenBank and further genetic or metabolic characterization of selected strains. Comparison of 16S rRNA taxonomic identification and BOX-PCR profiles provided evidence for numerous horizontal gene transfers of biosynthetic genes or gene clusters within actinomycete populations and even from non-actinomycete organisms. Our results underline the importance of environmental and evolutionary data in the design of efficient techniques for identification of novel producers.

  13. Fractional laser-assisted delivery of methyl aminolevulinate

    DEFF Research Database (Denmark)

    Haak, Christina S; Farinelli, William A; Tam, Joshua

    2012-01-01

    Pretreatment of skin with ablative fractional lasers (AFXL) enhances the uptake of topical photosensitizers used in photodynamic therapy (PDT). Distribution of photosensitizer into skin layers may depend on depth of laser channels and incubation time. This study evaluates whether depth of intrade...... of intradermal laser channels and incubation time may affect AFXL-assisted delivery of methyl aminolevulinate (MAL).......Pretreatment of skin with ablative fractional lasers (AFXL) enhances the uptake of topical photosensitizers used in photodynamic therapy (PDT). Distribution of photosensitizer into skin layers may depend on depth of laser channels and incubation time. This study evaluates whether depth...

  14. pH- and sugar-sensitive multilayer films composed of phenylboronic acid (PBA)-modified poly(allylamine hydrochloride) (PBA-PAH) and poly(vinyl alcohol) (PVA): A significant effect of PBA content on the film stability.

    Science.gov (United States)

    Seno, Masaru; Yoshida, Kentaro; Sato, Katsuhiko; Anzai, Jun-ichi

    2016-05-01

    Multilayer thin films composed of phenylboronic acid (PBA)-modified poly(allylamine hydrochloride) (PAH), PBA-PAH, with different PBA contents were prepared to study the effect of PBA content on the stability of the films. An alternate deposition of PBA-PAH and poly(vinyl alcohol) (PVA) on the surface of a quartz slide afforded multilayer films through forming boronate ester bonds between PBA-PAH and PVA. The 10-layered (PBA-PAH/PVA)10 films constructed using PBA-PAHs containing 16% and 26% PBA residues were stable in aqueous solutions over the range of pH 4.0-10.0, whereas the multilayer films composed of PBA-PAHs with 5.9% and 8.3% PBA decomposed at pH 8.0 or lower. The pH-sensitive decomposition of the films was rationalized based on the destabilization of the boronate ester bonds in neutral and acidic solutions. In addition, the (PBA-PAH/PVA)10 films decomposed in glucose and fructose solutions as a result of competitive binding of sugars to PBA-PAH in the films. The sugar response of the films depended on the PBA content in PBA-PAH. The (PBA-PAH/PVA)10 films consisting of 16% and 26% PBA-substituted PBA-PAHs are sensitive to physiological relevant level of glucose at pH7.4 while stable in glucose-free solution, suggesting a potential use of the films in constructing glucose-induced delivery systems.

  15. Effect of ethylene glycol dimethacrylate on swelling and on metformin hydrochloride release behavior of chemically crosslinked pH-sensitive acrylic acid-polyvinyl alcohol hydrogel

    National Research Council Canada - National Science Library

    Akhtar, Muhammad Faheem; Ranjha, Nazar Muhammad; Hanif, Muhammad

    2015-01-01

    The present work objective was to prepare and to observe the effect of ethylene glycol dimethacrylate on swelling and on drug release behavior of pH-sensitive acrylic acid-polyvinyl alcohol hydrogel...

  16. 21 CFR 582.5676 - Pyridoxine hydrochloride.

    Science.gov (United States)

    2010-04-01

    ... 21 Food and Drugs 6 2010-04-01 2010-04-01 false Pyridoxine hydrochloride. 582.5676 Section 582.5676 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED... Dietary Supplements 1 § 582.5676 Pyridoxine hydrochloride. (a) Product. Pyridoxine hydrochloride....

  17. Simultaneous determination of a ternary mixture of doxylamine succinate, pyridoxine hydrochloride, and folic acid by the ratio spectra-zero-crossing, double divisor-ratio spectra derivative, and column high-performance liquid chromatographic methods.

    Science.gov (United States)

    Pathak, Ashutosh; Rajput, Sadhana J

    2008-01-01

    Three simple, rapid, and accurate methods, i.e., the derivative ratio spectra-zero-crossing method (method I), double divisor-ratio spectra derivative method (method II), and column reversed-phase high-performance liquid chromatographic (RP-HPLC) method (method III) were developed for the simultaneous determination of doxylamine succinate (DOX), pyridoxine hydrochloride (PYR), and folic acid (FA) in their ternary mixtures and in tablets. In methods I and II, the calibration graphs were linear in the range of 2.5-80, 1.0-40, and 1.0-30 microg/mL for DOX, PYR, and FA, respectively. In the HPLC method, the separation of these compounds was performed using mobile phase consisting of 0.05 M phosphate buffer (pH 6.3)-methanol-acetonitrile (50 + 20 + 30, v/v/v), and UV detection was performed at 263 nm. Linearity was observed between the concentrations of the analytes and peak areas [correlation coefficient (r) > or =0.9998] in the concentration range of 1.0-200, 4.0-600, and 4.0-600 microg/mL for DOX, PYR, and FA, respectively. The standard deviation of retention time in method III was 0.011, 0.015, and 0.016 for DOX, PYR, and FA, respectively. The precision studies for all of the methods gave relative standard deviation values of <2%. The results obtained from the methods were statistically compared by means of Student's t-test and the variance ratio F-test. It was concluded that all of the developed methods were equally accurate, sensitive, and precise. These methods could be applied to determine DOX, PYR, and FA in their combined dosage forms.

  18. Identification of atherosclerosis using aminolevulinic gold nanoparticle assay in fecal specimens

    Science.gov (United States)

    Gonçalves, Karina de O.; da Silva, Mônica N.; Courrol, Lilia C.

    2015-06-01

    The atheromatous plaques exhibit an accumulation of protoporphyrin IX, or PpIX, which is transferred to the feces. In this work it was associated a precursor of the PpIX, the 5-aminolevulinic acid, ALA, with gold nanoparticles (ALA:AuNps). The objective was verify the possibility to use ALA:AuNPs as a diagnosis agent for atherosclerosis. ALA:AuNps were synthesized mixing ALA with Tetrachloroauric(III) acid in miliQ water solution followed by photoreduction with light from a Xenon lamp. A total of 22 Male New Zealand rabbits were divided into 3 groups: control group (CG) where animals received normal diet, control group with ALA (CGALA ) and Experimental Group with ALA:AuNPs ( EGALAAu ) in which the animals received a diet with 1% cholesterol. Measurements of the emission intensity of extracted porphyrins from the feces in the region between 575 and 725 nm were done. An increase in the feces porphyrin emission after ALA and ALA:AuNPs administration was observed.

  19. Delta-aminolevulinate dehydratase activity and oxidative stress markers in preeclampsia.

    Science.gov (United States)

    de Lucca, Leidiane; Rodrigues, Fabiane; Jantsch, Letícia B; Kober, Helena; Neme, Walter S; Gallarreta, Francisco M P; Gonçalves, Thissiane L

    2016-12-01

    Preeclampsia is an important pregnancy-specific multisystem disorder characterized by the onset of hypertension and proteinuria. It is of unknown etiology and involves serious risks for the pregnant women and fetus. One of the main factors involved in the pathophysiology of preeclampsia is oxidative stress, where excess free radicals produce harmful effects, including damage to macromolecules such as lipids, proteins and DNA. In addition, the sulfhydryl delta-aminolevulinate dehydratase enzyme (δ-ALA-D) that is part of the heme biosynthetic pathway in pro-oxidant conditions can be inhibited, which may result in the accumulation of 5-aminolevulinic acid (ALA), associated with the overproduction of free radicals, suggesting it to be an indirect marker of oxidative stress. As hypertensive pregnancy complications are a major cause of morbidity and mortality maternal and fetal where oxidative stress appears to be an important factor involved in preeclampsia, the aim of this study was to evaluate the activity of δ-ALA-D and classic oxidative stress markers in the blood of pregnant women with mild and severe preeclampsia. The analysis and quantification of the following oxidative stress markers were performed: thiobarbituric acid-reactive species (TBARS); presence of protein and non-protein thiol group; quantification of vitamin C; Catalase and δ-ALA--D activities in samples of blood of pregnant women with mild preeclampsia (n=25), with severe preeclampsia (n=30) and in a control group of healthy pregnant women (n=30). TBARS was significantly higher in women with preeclampsia, while the presence of thiol groups, levels of vitamin C, catalase and δ-ALA-D activity were significantly lower in groups of pregnant women with preeclampsia compared with healthy women. In addition, the results showed no significant difference between groups of pregnant women with mild and severe preeclampsia. The data suggest a state of increased oxidative stress in pregnant women with

  20. Study on the syhthesis process of tetracaine hydrochloride

    Science.gov (United States)

    Li, Wenli; Zhao, Jie; Cui, Yujie

    2017-05-01

    Tetrachloride hydrochloride is a local anesthetic with long-acting ester, and it is usually present in the form of a hydrochloride salt. Firsleb first synthesized the tetracaine by experiment in 1928, which is one of the recognized clinical potent anesthetics. This medicine has the advantages of stable physical and chemical properties, the rapid role and long maintenance. Tetracaine is also used for ophthalmic surface anesthesia as one of the main local anesthetic just like conduction block anesthesia, mucosal surface anesthesia and epidural anesthesia. So far, the research mainly engaged in its clinical application research, and the research strength is relatively small in the field of synthetic technology. The general cost of the existing production process is high, and the yield is low. In addition, the reaction time is long and the reaction conditions are harsh. In this paper, a new synthetic method was proposed for the synthesis of tetracaine hydrochloride. The reaction route has the advantages of few steps, high yield, short reaction time and mild reaction conditions. The cheap p-nitrobenzoic acid was selected as raw material. By esterification with ethanol and reaction with n-butyraldehyde (the reaction process includes nitro reduction, aldol condensation and hydrogenation reduction), the intermediate was transesterified with dimethylaminoethanol under basic conditions. Finally, the PH value was adjusted in the ethanol solvent. After experiencing 4 steps reaction, the crude tetracaine hydrochloride was obtained.

  1. Effects of pantothenic acid on growth performance and carcass characteristics of growing-finishing pigs fed diets with or without ractopamine hydrochloride.

    Science.gov (United States)

    Groesbeck, C N; Goodband, R D; Tokach, M D; Dritz, S S; Nelssen, J L; DeRouchey, J M

    2007-10-01

    Two experiments evaluated effects of added pantothenic acid on performance of growing-finishing pigs. In Exp. 1, 156 pigs (PIC, initial BW = 25.7 kg) were used in a 3 x 2 x 2 factorial to evaluate the effects of added pantothenic acid (PA; 0, 22.5, or 45 ppm), ractopamine.HCl (RAC; 0 or 10 mg/kg), and sex on growth performance and carcass traits. Pigs were fed increasing PA from 25.7 to 123.6 kg (d 0 to 98) and RAC for the last 28 d before slaughter. Increasing the amount of added PA had no effect (P > 0.40) on ADG, ADFI, or G:F from d 0 to 70. A PA x sex interaction (P 0.38) on carcass traits. Added RAC increased (P PIC, initial BW = 40.4 kg, final BW = 123.6 kg) were used to determine the effects of increasing PA on growth performance and carcass characteristics of growing-finishing pigs reared in a commercial finishing facility. Pigs were fed 0, 22.5, 45.0, or 90 mg/kg of added PA. Increasing the amount of added PA had no effect (P > 0.45) on ADG, ADFI, or G:F, and no differences were observed (P > 0.07) for carcass traits. In summary, adding dietary PA to diets during the growing-finishing phase did not provide any advantages in growth performance or carcass composition of growing-finishing pigs. Furthermore, it appears that the pantothenic acid in corn and soybean meal may be sufficient to meet the requirements of 25- to 120-kg pigs.

  2. δ氨基酮戊酸光动力疗法对体外培养三株嗜角质真菌杀伤效应的实验研究%Antifungal Effect of Delta-Aminolevulinic Acid Mediated Photodynamic Therapy on Three Strains of Kratinophilic Fungi in Vitro

    Institute of Scientific and Technical Information of China (English)

    黄望强; 史赢; 雷铁池

    2012-01-01

    Objective: To evaluate the killing effect of S-Aminolevulinic acid (ALA) -mediated photody-namic therapy on three strains of keratinophilic fungi in vitro and to investigate its mechanism. Methods: Trichophyton rubrum , Trichophyton mentagrophytes, and Candida albicans were inoculated in Sabouraud glucose peptone, for preparing fungi suspensions. The fungi suspensions were treated with different concentrations of ALA (3, 10, 30, 100, and 300 mmol/L) cultures in DMEM containing 2. 5% fetal calf serum. Confocal fluorescence microscope was used to examine proto-porphyrin IX (PpIX) formation. MTT assay was used to determine the inhibitory rates by different concentrations of ALA-PDT. The ult restructure changes of fungi were observed by transmission electron microscopy after the treatment of 100 mmol/L ALA-PDT. Results: After incubated with 100 mmol/L ALA, PpK was shown as brick-red fluorescent signal in the three stains of fungal inside by confocal laser scanning microscope. There is a positive correlation be-tween the concentration of ALA and the inhibition ratio of three strains of fungi (P<0. 05), but when the concentration of ALA increased to 300 mmol/L, the inhibition rate did not increase significantly. Simple laser and simple ALA treatment had no significant inhibition on fungal growth. The structures of cell wall, cell membrane, and organelles in all the three strains of fungi were destroyed at some extent after 100 mmol/L ALA-PDT treatment. Conclusion: 8-Aminolevulini-cacid-mediated photodynamic treatment have a definite killing effect in these, three strains fungi in vitro, which provides a theoretical basis for treatment of onychomycosis.%目的:探讨δ氨基酮戊酸(ALA)光动力学疗法(PDT)对体外培养的三株嗜角质真菌杀伤效应及作用机制.方法:将红色毛癣菌、须癣毛癣菌、白念珠菌三株标准菌株在沙氏葡萄糖琼脂培养基(SDA)活化培养后制备菌悬液,菌悬液与不同浓度ALA(3,10,30,100,300mmol

  3. 5-氨基乙酰丙酸介导的光动力学作用对胃癌细胞MKN-45增殖与凋亡作用的研究%Effect of 5-aminolevulinic acid mediated photodynamic therapy on proliferation and apoptosis of gastric cancer cell line MKN-45

    Institute of Scientific and Technical Information of China (English)

    王晓龙; 魏军; 程立文; 张骞; 闫鹏; 王贵玉

    2016-01-01

    Objective To explore the 5-aminolevulinic acid (5-ALA) mediated photodynamic therapy (PDT) for proliferation and apoptosis of gastric cancer cell line MKN-45.Methods The human gastric cancer cell line MKN-45 was cultured in vitro.The MTT method was used to detect fixed lighting processing (laser radiation dose fixed for 25.00 J/cm2,5-ALA photosensitizer concentrations were 0 mmol/L,0.25 mmol/L,0.50 mmol/L,1.00 mmol/L,2.00 mmol/L),fixed photosensitizer concentration treatment (5-ALA photosensitizer concentrations fixed to 1.00 mmol/L,laser radiation dose were 0 J/cm2,6.25 J/cm2,12.50 J/cm2,25.00 J/cm2,50.00 J/cm2,100.00 J/cm2) of the cell apoptosis rate,and then fixed 5-ALA photosensitizer 1 mmol/L and selected the control group,5-ALA group,pure illumination group and PDT group.The promoting effect on cell apoptosis was determined by MTT,electron microscope and flow cytometry.The activity of human gastric cancer cells MKN-45 apoptosis related proteins p65 and the downstream gene regulatory protein bcl-2,bax,caspase-3 and caspase-9 were detected by using Western blot method.Results When laser radiation dose was fixed,5-ALA photosensitizer concentrations in promoting gastric cancer cell apoptosis was positively related to the dominant (P < 0.01).When 5-ALA photosensitizer concentration was fixed,laser radiation dose effect had no longer dominant after 25.00 J/cm2 positive correlation (P =0.613).When 5-ALA photosensitizer concentration was fixed in 1 mmol/L,compared to control group,5-ALA group and pure illumination group,the inhibition of the MKN-45 cell proliferation in PDT group was more apparently,apoptosis rate increased obviously,signal pathways in cell apoptosis protein involved in the NF-kappa B p65 expression was reduced,the downstream gene regulation of target protein bcl-2,caspase-3 and caspase-9 expression were reduced,and bax protein expression was increased.Conclusions 5-ALA mediated photodynamic has a strong inhibitory effect on the growth of gastric

  4. Stability of cefozopran hydrochloride in aqueous solutions.

    Science.gov (United States)

    Zalewski, Przemysław; Skibiński, Robert; Paczkowska, Magdalena; Garbacki, Piotr; Talaczyńska, Alicja; Cielecka-Piontek, Judyta; Jelińska, Anna

    2016-01-01

    The influence of pH on the stability of cefozopran hydrochloride (CZH) was investigated in the pH range of 0.44-13.00. Six degradation products were identified with a hybrid ESI-Q-TOF mass spectrometer. The degradation of CZH as a result of hydrolysis was a pseudo-first-order reaction. As general acid-base hydrolysis of CZH was not occurred in the solutions of hydrochloric acid, sodium hydroxide, acetate, borate and phosphate buffers, kobs = kpH because specific acid-base catalysis was observed. Specific acid-base catalysis of CZH consisted of the following reactions: hydrolysis of CZH catalyzed by hydrogen ions (kH+), hydrolysis of dications (k1H2O), monocations (k2H2O) and zwitter ions (k3H2O) and hydrolysis of zwitter ions (k1OH-) and monoanions (k2OH-) of CZH catalyzed by hydroxide ions. The total rate of the reaction was equal to the sum of partial reactions: [Formula: see text]. CZH similarly like other fourth generation cephalosporin was most stable at slightly acidic and neutral pH and less stable in alkaline pH. The cleavage of the β-lactam ring resulting from a nucleophilic attack on the carbonyl carbon in the β-lactam moiety is the preferred degradation pathway of β-lactam antibiotics in aqueous solutions.

  5. "Sustained release formulation of Metoclopramide Hydrochloride "

    Directory of Open Access Journals (Sweden)

    Dabbagh MA

    2000-08-01

    Full Text Available In this research, several formulations containing, an anti emetic agent (Metoclopramide hydrochloride, a hydrophilic polymer (hydroxypropylmethylcellulose and a hydrophobic polymer (ethylcellulose 10 cP were prepared by direct compression. Different factors such as: the effect of different ratios of the polymers, particle size, pressure force and differences of release in acidic and distilled water as media were investigated. After developing the ideal formulation, the effect of changing the ratio of drug in core: coating on the formulation was investigated. Coating of tablets with ethylcellulose, changed the release mechanism of drug and shifted it to near zero order release. The results showed that except when matrices were coated with ethylcellulose, drug release was proportioned to the square root of time, which might be due to the change of release pattern from matrix to reservoir system.

  6. Synthesis of /sup 14/C-Bucromarone succinate and hydrochloride

    Energy Technology Data Exchange (ETDEWEB)

    Nicolas, C.; Verny, M.; Maurizis, J.-C.; Payard, M.; Faurie, M.

    1986-08-01

    /sup 14/C-Bucromarone, 2-(4-(3-N,N dibutylamino propoxy) 3,5-dimethyl benzoyl) chromone, was synthesized from (U-/sup 14/C) oxalic acid. The labelling takes place at the first step of the synthesis, giving /sup 14/C-Bucromarone succinate (specific activity 7.45 mCi/mmol) and /sup 14/C-Bucromarone hydrochloride (specific activity 7.5 mCi/mmol).

  7. Enantiospecific synthesis of (1- sup 3 H)-(+)-pseudoephedrine hydrochloride

    Energy Technology Data Exchange (ETDEWEB)

    Hill, J.A.; Scharver, J.D. (Burroughs Wellcome Co., Research Triangle Park, North Carolina (USA). Chemical Development Labs.)

    1990-06-01

    The naturally occurring dextrorotary enantiomer (+)-pseudoephedrine was synthesized in the ({sup 3}H)-labelled form with specific activity 17.5 Ci/mmol suitable for development of a radioimmunoassay procedure. The chirally specific route from L-alanine to (1-{sup 3}H)-d-pseudoephedrine hydrochloride was based on the use of {alpha}-amino acids as chiral educts for asymmetric products. (author).

  8. Formulation, Development and Evaluation of delayed release capsules of Duloxetine Hydrochloride made of different Enteric Polymers

    Directory of Open Access Journals (Sweden)

    Pallavi Yerramsetty

    2012-03-01

    Full Text Available Delayed release systems have acquired a centre stage in the arena of pharmaceutical research and development. The present study involves formulation and evaluation of Duloxetine Hydrochloride delayed release capsules. Duloxetine Hydrochloride is an acid labile drug. It degrades in the acidic environment of the stomach thus leading to therapeutic inefficacy. Therefore it is necessary to bypass the acidic pH of the stomach which can be achieved by formulating delayed release dosage form by using different enteric polymers. Protection of drug from acidic environment is done by coating the drug with enteric polymers by using suspension layering technique in Fluidized bed processor (FBP with different enteric polymers like HPMCAS (Hydroxy Propyl Methyl Cellulose Acetate Succinate, Acryl EZE and HPMCP (Hydroxy propyl methyl cellulose phthalate.The formulation (E12 of delayed release capsules of Duloxetine Hydrochloride containing HPMCP (HP-55: HP- 50 as enteric polymer can be taken as optimized

  9. Stability-indicating HPLC method for simultaneous determination of montelukast and fexofenadine hydrochloride

    Directory of Open Access Journals (Sweden)

    Mona Pankhaniya

    2013-01-01

    Full Text Available A simple, specific, accurate, and stability-indicating reversed-phase high-performance liquid chromatographic method was developed for the simultaneous determination of montelukast and fexofenadine hydrochloride, using a Lichrospher ® 100, RP-18e column and a mobile phase composed of methanol:0.1% o-phosphoric acid (90:10 v/v, pH 6.8. The retention times of montelukast and fexofenadine hydrochloride were found to be 10.16 and 12.03 min, respectively. Linearity was established for montelukast and fexofenadine hydrochloride in the range of 2-10 μg/ml and 24-120 μg/ml, respectively. The percentage recoveries of montelukast and fexofenadine hydrochloride were found to be in the range of 99.09 and 99.81%, respectively. Both the drugs were subjected to acid and base hydrolysis, oxidation, photolytic, and thermal degradation conditions. The degradation products of montelukast and fexofenadine hydrochloride were well resolved from the pure drug with significant differences in their retention time values. This method can be successfully employed for simultaneous quantitative analysis of montelukast and fexofenadine hydrochloride in bulk drugs and formulations.

  10. Oxidative Profile and δ-Aminolevulinate Dehydratase Activity in Healthy Pregnant Women with Iron Supplementation.

    Science.gov (United States)

    De Lucca, Leidiane; Rodrigues, Fabiane; Jantsch, Letícia B; Neme, Walter S; Gallarreta, Francisco M P; Gonçalves, Thissiane L

    2016-05-03

    An oxidative burst occurs during pregnancy due to the large consumption of oxygen in the tissues and an increase in metabolic demands in response to maternal physiological changes and fetal growth. This study aimed to determine the oxidative profile and activity of δ-aminolevulinate dehydratase (δ-ALA-D) in pregnant women who received iron supplementation. Oxidative stress parameters were evaluated in 25 pregnant women with iron supplementation, 25 pregnant women without supplementation and 25 non-pregnant women. The following oxidative stress parameters were evaluated: thiobarbituric acid reactive substances (TBARS), protein thiol groups (P-SH), non-protein thiol levels (NP-SH), vitamin C levels, catalase and δ-ALA-D activity. Markers of oxidative stress and cell damage, such as TBARS in plasma were significantly higher in pregnant women without supplementation. Levels of P-SH, NP-SH and δ-ALA-D activity were significantly lower in pregnant women without supplementation compared to non-pregnant and pregnant women with supplementation, while vitamin C levels were significantly lower in pregnant women without supplementation when compared to non-pregnant women. The increase in the generation of oxidative species and decrease of antioxidants suggest the loss of physiological oxidative balance during normal pregnancy, which was not observed in pregnant women with iron supplementation, suggesting a protective effect of iron against oxidative damage.

  11. Cartap hydrochloride poisoning: A clinical experience

    OpenAIRE

    Hari K Boorugu; Anugrah Chrispal

    2012-01-01

    Cartap hydrochloride, a nereistoxin analog, is a commonly used low toxicity insecticide. We describe a patient who presented to the emergency department with alleged history of ingestion of Cartap hydrochloride as an act of deliberate self-harm. The patient was managed conservatively. To our knowledge this is the first case report of Cartap hydrochloride suicidal poisoning. Cartap toxicity has been considered to be minimal, but a number of animal models have shown significant neuromuscular to...

  12. 21 CFR 522.1222b - Ketamine hydrochloride with promazine hydrochloride and aminopentamide hydrogen sulfate injection.

    Science.gov (United States)

    2010-04-01

    ... 21 Food and Drugs 6 2010-04-01 2010-04-01 false Ketamine hydrochloride with promazine... RELATED PRODUCTS IMPLANTATION OR INJECTABLE DOSAGE FORM NEW ANIMAL DRUGS § 522.1222b Ketamine.... Ketamine hydrochloride, (±),-2-(o-chlorophenyl)-2-(methylamino) cyclohexanone hydrochloride, with promazine...

  13. Evolution of cyclizing 5-aminolevulinate synthases in the biosynthesis of actinomycete secondary metabolites: Outcomes for genetic screening techniques

    Directory of Open Access Journals (Sweden)

    Katerina ePetrickova

    2015-08-01

    Full Text Available A combined approach, comprising PCR screening and genome mining, was used to unravel the diversity and phylogeny of genes encoding 5-aminolevulinic acid synthases (ALASs, hemA gene products in streptomycetes-related strains. In actinomycetes, these genes were believed to be directly connected with the production of secondary metabolites carrying the C5N unit, 2-amino-3-hydroxycyclopent-2-enone, with biological activities making them attractive for future use in medicine and agriculture. Unlike classical primary metabolism ALAS, the C5N unit-forming cALAS (cyclizing ALAS catalyses intramolecular cyclization of nascent 5-aminolevulinate. Specific amino acid sequence changes can be traced by comparison of classical ALASs against cALASs. PCR screening revealed 226 hemA gene-carrying strains from 1,500 tested, with 87 % putatively encoding cALAS. Phylogenetic analysis of the hemA homologues revealed strain clustering according to putative type of metabolic product, which could be used to select producers of specific C5N compound classes. Supporting information was acquired through analysis of actinomycete genomic sequence data available in GeneBank and further genetic or metabolic characterization of selected strains. Comparison of 16S rRNA taxonomic identification and BOX-PCR profiles provided evidence for numerous horizontal gene transfers of biosynthetic genes or gene clusters within actinomycete populations and even from non-actinomycete organisms. Our results underline the importance of environmental and evolutionary data in the design of efficient techniques for identification of novel producers.

  14. Thermoanalytical Investigation of Terazosin Hydrochloride

    OpenAIRE

    Mona Mohamed Abdel-Moety; Ali Kamal Attia

    2013-01-01

    Purpose: Thermal analysis (TGA, DTG and DTA) and differential scanning calorimetry (DSC) have been used to study the thermal behavior of terazosin hydrochloride (TER). Methods: Thermogravimetric analysis (TGA/DTG), differential thermal analysis (DTA) and differential scanning calorimetry (DSC) were used to determine the thermal behavior and purity of the used drug. Thermodynamic parameters such as activation energy (E*), enthalpy (∆H*), entropy (∆S*) and Gibbs free energy change of the decomp...

  15. Electrochemical Behavior and Determination of Pyridoxine Hydrochloride at the Poly Nicotinic Acid Modified Electrode%盐酸吡哆辛在聚烟酸修饰电极上的电化学行为及测定

    Institute of Scientific and Technical Information of China (English)

    顾小燕; 唐鹏鹏; 李宁波; 刘欢; 俞静; 何凤云

    2014-01-01

    采用电聚合方法制备了聚烟酸修饰玻碳电极(PNA/GCE),并利用循环伏安法(CV)和差分脉冲伏安法(DPV)考察了盐酸吡哆辛(VB6)在该修饰电极上的电化学行为。结果表明,VB6在 PNA/GCE 上的氧化峰电流显著提高,电极反应为扩散控制的一电子两质子反应。利用差分脉冲伏安法对 VB6进行测定,线性范围为0.08~400μmol/L,VB6的检出限为0.02μmol/L,测定结果的相对标准偏差为3.1%(n=8),加标回收率为95.8%~103.7%。该方法可用于 VB6片中 VB6含量的测定。%Poly(nicotinic acid) modified electrode (PNA/GCE) was prepared and the electrochemical behavior of pyridoxine hydrochloride(VB6) was investigated at the modified electrode by cyclic voltammetry(CV) and differential pulse voltammetry(DPV). Results showed that the oxidation current of VB6 at the PNA/GCE was obviously larger than that at GCE. The oxidation process of VB6 was an irreversible diffusion–controlled process involving one electron and two protons. The liner range between the peak current of DPV and the concentration of VB6 was 0.08–400 μmol/L, and the detection limit was 0.02 μmol/L. The modified electrode showed a good reproducibility with a relative standard deviation of 3.1%(n=8). The recoveries were between 95.8% and 103.7%. The method can be applied to the analysis of vitamin B6 content in vitamin B6 tablets.

  16. 氨基酮戊酸光动力疗法对鲜红斑痣动物模型鸡冠的影响%Effects of aminolevulinic acid-based photodynamic therapy on chicken combs, an animal model for port wine stains

    Institute of Scientific and Technical Information of China (English)

    王娇; 黄熙

    2015-01-01

    目的:探讨外用氨基酮戊酸光动力疗法(ALA-PDT)对鲜红斑痣(PWS)动物模型鸡冠的作用和治疗鲜红斑痣的可行性。方法80只莱亨鸡随机分为10组:空白对照组、单纯 ALA 组、单纯激光75 J/cm2组、100 J/cm2组、150 J/cm2、200 J/cm2组,ALA-PDT 75 J/cm2组、100 J/cm2组、150 J/cm2组、200 J/cm2组。单纯激光组仅给予630 nm 红光照射,ALA-PDT 组外用 ALA 后给予红光照射。干预14 d、28 d 分别取材,观察鸡冠形态学、组织学变化,计算毛细血管减少率和血管内皮细胞凋亡情况。结果外用 ALA-PDT 75 J/cm2、100 J/cm2、150 J/cm2和200 J/cm2组鸡冠实验区域颜色变淡,光镜下真皮毛细血管数目减少、管径变小,部分血管内皮细胞凋亡;毛细血管减少率分别为33.53%±4.89%、52.02%±2.77%、67.48%±5.58%、88.96%±2.47%;凋亡指数分别为:63.44±1.09、88.50±6.11、94.32±3.67、113.76±10.57,与其余各组分别比较,均 P <0.01;血管内皮细胞凋亡深度分别为:201.19μm ±0.33μm、266.15μm ±1.02μm、546.09μm ±2.45μm、766.37μm ±1.08μm,各组间两两比较,均 P <0.01。结论外用 ALA-PDT 对鸡冠毛细血管有明显损伤,损伤程度和深度与红光能量密度相关;诱导血管内皮细胞凋亡可能是其治疗机制之一。%Objective To investigate the effects of aminolevulinic acid-based photodynamic therapy(ALA-PDT) on chicken combs, an animal model for port wine stains (PWS), and to explore the feasibility of PWS treatment with ALA-PDT. Methods A total of 80 leghorns were randomly and equally divided into 10 groups: blank control group receiving no treatment, ALA group treated with ALA alone, four single laser groups irradiated with 630-nm red laser at 75, 100, 150 and 200 J/cm2 respectively, four ALA-PDT groups pretreated with ALA followed by 630-nm red laser radiation at 75, 100, 150 and 200 J/cm2 respectively. An area sized 1 cm × 1 cm were marked at one side

  17. [Clinical evaluation of roxatidine acetate hydrochloride injection as preanesthetic medication].

    Science.gov (United States)

    Kawanishi, M; Enomoto, A; Shimada, Y; Kurokawa, Y

    1991-09-01

    The effects of single intravenous administration of roxatidine acetate hydrochloride 75 mg on the volume and pH of gastric juice were investigated in 43 patients undergoing elective surgery under general anesthesia. The drug was given 1 hour before anesthesia. The percentages of patients with gastric pH above 2.5 and gastric juice volume under 25 ml were 95.3% and 97.7% at the time of induction of anesthesia and at the time of extubation, respectively. As for overall assessment on gastric secretion, 93.0% was judged as very effective. In 2 cases, pricking sensations were observed at the time of injection, but these symptoms disappeared without any treatment within a few minutes. No other adverse reactions nor abnormal laboratory test findings were observed. In conclusion, roxatidine acetate hydrochloride administered intravenously 1 hour prior to anesthesia is thought to be useful to prevent acid aspiration pneumonitis.

  18. Thermal Analysis Applied to Verapamil Hydrochloride Characterization in Pharmaceutical Formulations

    Directory of Open Access Journals (Sweden)

    Maria Irene Yoshida

    2010-04-01

    Full Text Available Thermogravimetry (TG and differential scanning calorimetry (DSC are useful techniques that have been successfully applied in the pharmaceutical industry to reveal important information regarding the physicochemical properties of drug and excipient molecules such as polymorphism, stability, purity, formulation compatibility among others. Verapamil hydrochloride shows thermal stability up to 180 °C and melts at 146 °C, followed by total degradation. The drug is compatible with all the excipients evaluated. The drug showed degradation when subjected to oxidizing conditions, suggesting that the degradation product is 3,4-dimethoxybenzoic acid derived from alkyl side chain oxidation. Verapamil hydrochloride does not present the phenomenon of polymorphism under the conditions evaluated. Assessing the drug degradation kinetics, the drug had a shelf life (t90 of 56.7 years and a pharmaceutical formulation showed t90 of 6.8 years showing their high stability.

  19. SYNTHESIS OF 2, 6-DIAMINO-3-PHENYLAZOPYRIDINE-1-OXIDE AND ITS HYDRO-CHLORIDE

    Directory of Open Access Journals (Sweden)

    Ganesh Babu Talagadadeevi, Ramakrishna Muvva, Bangar Reddy Vancha and Madhusudana Rao Jampani*

    2013-11-01

    Full Text Available The compound 2, 6-diamino-3-phenylazopyridine hydrochloride salt is a genito-urinary antiseptic drug under the trade name Pyridinium. This study is directed towards the occurrence of an oxidation reaction to convert the tertiary amine present in 2, 6-diamino-3-phenylazopyridine hydrochloride to form an N-oxide derivative as an impurity in the process for its preparation. This was done by the independent synthesis of 2, 6-diamino-3-phenylazopyridine-1-oxide hydrochloride salt by two independent routes. The presence of three amine functions in the molecule required first to protect the primary amine groups by derivatisation so that oxidation occurs exclusively at the tertiary amino group of the pyridine ring. 2, 6-diamino-3-phenylazopyridine was acetylated to get 2, 6-diacetamido-3-phenylazopyridine whose structure was confirmed from 1H NMR and mass spectral data. The oxidation of diacetyl derivative with peracetic acid resulted not only in the N-oxide formation but also in the cleavage of one of the acetamido group to give 2(6-acetamido-6(2amino-3-phenylazopyridine-1-oxide. The alkaline hydrolysis of the N-oxide form gave 2, 6-diamino-3-phenylazopyridine-1-oxide which on treatment with hydrochloric acid gave 2, 6-diamino-3-phenylazopyridine-1-oxide hydrochloride. In yet another route the N-oxide was prepared by the coupling reaction between benzene diazonium chloride and 2, 6-diaminopyridine-1-oxide in aqueous hydrochloric acid medium. This reaction resulted in the formation of 2, 6-diamino-3- phenylazopyridine-1-oxide hydrochloride as an insoluble salt. The structure of the N-oxide was confirmed from 1H NMR and mass spectral data. A co-injection HPLC analysis showed the complete absence of 2, 6-diamino-3-phenylazopyridine-1-oxide hydrochloride in 2, 6-diamino-3-phenylazopyridine hydrochloride in its manufacturing process.

  20. HPLC Simultaneous Determination of Glucosamine Hydrochloride and Glucosaminic Acid in Catalytic Reaction Solution%高效液相色谱法同时测定催化反应液中氨基葡萄糖盐酸盐和氨基葡萄糖酸

    Institute of Scientific and Technical Information of China (English)

    肖静静; 吴婷婷; 顾文秀; 杨盼; 李炜

    2013-01-01

    向制备氨基葡萄糖酸的催化反应液中加入亚硝酸盐试剂,在25℃下衍生反应5 min,所得含有氨基葡萄糖盐酸盐和氨基葡萄糖酸衍生物的溶液用作高效液相色谱分析.选用AminexHPX-87H离子排斥色谱柱为固定相,以5 mmol·L1硫酸溶液为流动相进行淋洗,用示差折光检测器进行检测,提出了同时测定氨基葡萄糖盐酸盐和氨基葡萄糖酸的高效液相色谱法.2种化合物的色谱峰面积与其浓度均在50 mmol·L-1以内呈线性关系,检出限(3S/N)依次为0.014,0.034 mmol·L-1.方法用于5批催化反应液中氨基葡萄糖盐酸盐和氨基葡萄糖酸的测定,加标回收率依次在99.3%~100%,99.2%~102%之间;测定值的相对标准偏差均小于2.5%.%The catalytic reaction solution used for preparation of glucosaminic acid was mixed with NaNCi as derivatizing reagent, and derivatized for 5 min at 25 ℃ The solution containing derivatives of glucosamine hydrochloride and glucosaminic acid was used for HPLC analysis, using Aminex HPX-87H ion replusive column as stationary phase and 5 mmol · L-1 H2SO4 solution as mobile phase in isocratic elution. Differential refractive index detector was adopted in the determination. Linear relationships between values of peak area and concentration of the 2 compounds were obtained in the same range within 50 mmol · L-1 , with detection limits (3S/N) 0. 014 mmol · L-1(for glucosamine hydrochloride) and 0. 034 mmol· L-1 (for glucosaminic acid). The proposed method was applied to the determination of glucosamine hydrochloride and glucosaminic acid in catalytic reaction solution, giving values of recovery in the ranges of 99. 3% —100% and 99. 2% —102% with RSD's less than 2. 5%.

  1. Thermoanalytical Investigation of Terazosin Hydrochloride

    Directory of Open Access Journals (Sweden)

    Mona Mohamed Abdel-Moety

    2013-02-01

    Full Text Available Purpose: Thermal analysis (TGA, DTG and DTA and differential scanning calorimetry (DSC have been used to study the thermal behavior of terazosin hydrochloride (TER. Methods: Thermogravimetric analysis (TGA/DTG, differential thermal analysis (DTA and differential scanning calorimetry (DSC were used to determine the thermal behavior and purity of the used drug. Thermodynamic parameters such as activation energy (E*, enthalpy (H*, entropy (S* and Gibbs free energy change of the decomposition (G* were calculated using different kinetic models. Results: The purity of the used drug was determined by differential scanning calorimetry (99.97% and specialized official method (99.85% indicating to satisfactory values of the degree of purity. Thermal analysis technique gave satisfactory results to obtain quality control parameters such as melting point (273 ºC, water content (7.49% and ash content (zero in comparison to what were obtained using official method: (272 ºC, (8.0% and (0.02% for melting point, water content and ash content, respectively. Conclusion: Thermal analysis justifies its application in quality control of pharmaceutical compounds due to its simplicity, sensitivity and low operational costs. DSC data indicated that the degree of purity of terazosin hydrochloride is similar to that found by official method.

  2. Acute Psychotic Symptoms due to Benzydamine Hydrochloride Abuse with Alcohol

    Directory of Open Access Journals (Sweden)

    Yahya Ayhan Acar

    2014-01-01

    Full Text Available Benzydamine hydrochloride is a locally acting nonsteroidal anti-inflammatory drug. Benzydamine hydrochloride overdose can cause stimulation of central nervous system, hallucinations, and psychosis. We presented a young man with psychotic symptoms due to benzydamine hydrochloride abuse. He received a total dose of 1000 mg benzydamine hydrochloride with alcohol for its hallucinative effects. Misuse of benzydamine hydrochloride must be considered in differential diagnosis of first-episode psychosis and physicians should consider possibility of abuse in prescribing.

  3. Vitamin D as a potential enhancer of aminolevulinate-based photodynamic therapy for nonmelanoma skin cancer

    Science.gov (United States)

    Maytin, Edward V.; Anand, Sanjay; Atanaskova, Natasha; Wilson, Clara

    2010-02-01

    Vitamin D3 (Vit D3) is a hormone essential for normal bone and cardiovascular health, and may participate in preventing nonmelanoma skin cancers (NMSC). Calcitriol (1,25 dihydroxyD3) is the active form of the hormone. We showed previously that calcitriol is a potent inducer of protoporphyrin IX (PpIX) in skin keratinocytes grown in organotypic cultures. Here, we investigated the ability of Vit D3 to enhance PpIX levels within skin tumors in vivo. Squamous tumors, generated by chemical carcinogenesis in mice, were pretreated for 3 days with topical calcitriol. Then 5-aminolevulinic acid (5-ALA) was applied topically, and PpIX levels were measured by noninvasive fluorimetry and in biopsied tissue. Calcitriol pretreatment resulted in a 3 to 4-fold elevation of PpIX in tumors, relative to no pretreatmen, providing significantly more photosensitizer available for tumor destruction. For deep tumors, topical calcitriol may not penetrate sufficiently. Therefore we explored whether systemic Vit D3, given short-term (3 days), might elevate PpIX within NMSC in a deep tumor model (subcutaneously-implanted A431 human squamous carcinoma cells). Defined amounts of calcitriol were injected into the mice for 3 d, followed by systemic 5-ALA, tissue biopsy, and confocal microscopic measurement of PpIX in frozen tissues. PpIX was clearly elevated after systemically delivered calcitriol. More work is needed, but if the amount of calcitriol required to elevate PpIX levels proves to be small, then the approach may ultimately prove attractive. Since most Americans are currently Vitamin D deficient, a small increase in calcitriol might be possible without risk of hypercalcemia.

  4. Spectrophotometric simultaneous estimation of ranitidine hydrochloride and ondansetron hydrochloride from tablet formulation

    Directory of Open Access Journals (Sweden)

    Pillai S

    2007-01-01

    Full Text Available Three simple, accurate, economical and reproducible UV spectrophotometric methods for simultaneous estimation of two component drug mixture of ranitidine hydrochloride and ondansetron hydrochloride from combined tablet dosage form have been developed. First developed method involves formation and solving of simultaneous equations at 267.2 nm and 314.4 nm. Second method was developed making use of first order derivative spectroscopy using 340.8 nm and 276.0 nm as zero crossing points for estimation of ranitidine hydrochloride and ondansetron hydrochloride respectively. Third method is based on two wavelength calculation, wavelengths selected for estimation of ranitidine hydrochloride were 266.1 nm and 301.8 nm and for ondansetron hydrochloride 305.7 nm and 319.2 nm. The results of analysis have been validated statistically and by recovery studies.

  5. Spectrophotometric determination of diphenhydramine hydrochloride using dipicrylamine.

    Science.gov (United States)

    Shamsa, F A; Maghssoudi, R H

    1976-05-01

    A spectrophotometric procedure for the determination of diphenhydramine hydrochloride based on the reaction with dipicrylamine was developed. A yellow complex forms and is easily extractable by chloroform at pH 5. The mole ratio of diphenydramine hydrochloride to dipicrylamine in the complex is 1:3. The absorbance of the complex obeys Beer's law over the concentration range of 3-10 mug of diphenhydramine hydrochloride per ml of chloroform. This procedure can be carried out in the presence of other compounds without interference.

  6. Delta aminolevulinate dehydratase (ALA-D) activity in human and experimental diabetes mellitus.

    Science.gov (United States)

    Fernández-Cuartero, B; Rebollar, J L; Batlle, A; Enriquez de Salamanca, R

    1999-01-01

    The haem pathway is impaired in porphyrias and a frequent coexistence of diabetes mellitus and porphyria disease has been reported. We have therefore decided to investigate delta-aminolevulinate dehydratase, one of the more sensitive enzymes in the haem pathway, in both human diabetic patients and diabetic rats. We have studied 131 diabetes mellitus patients, 32 insulin dependent and 99 non-insulin dependent. The latter group was further subdivided according to treatment: diet alone (n = 24), diet plus oral hypoglycemic agents (n = 28) and diet plus insulin (n = 47). We have also performed similar studies in the rat model of diabetes mellitus, induced in 11 Wistar rats by streptozotocin. Control groups of both humans and animals were used. Erythrocytic aminolevulinate dehydratase activity was reduced in both insulin dependent and non-insulin dependent diabetic patients as compared to their controls (p glycosilated hemoglobin concentration (p < 0.05) and in non-insulin dependent diabetes mellitus to the glycemia (p < 0.01). In the diabetic rat, aminolevulinate dehydratase activity was diminished on both erythrocytes (p < 0.01) and hepatic tissue (p < 0.01) when compared to the control group. The decrease in activity of erythrocyte aminolevulinate dehydratase observed in diabetic patients, may represent an additional and useful parameter for the assessment of the severity of carbohydrate metabolism impairment.

  7. Allergic contact dermatitis to methyl aminolevulinate (Metvix) cream used in photodynamic therapy.

    Science.gov (United States)

    Harries, Matthew J; Street, Gill; Gilmour, Elizabeth; Rhodes, Lesley E; Beck, Michael H

    2007-02-01

    Topical photodynamic therapy (PDT) is increasingly used in the treatment of superficial skin malignancies including actinic keratosis, Bowen's disease and superficial basal cell carcinoma. Contact allergy to the prodrug is rarely reported. We report a case of allergic contact dermatitis to methyl aminolevulinate cream used in PDT.

  8. 口服盐酸氨基葡萄糖和注射透明质酸钠以及两者联合治疗膝关节骨性关节炎的临床研究%A Randomized Controlled Clinical Trial of Glucosamine Hydrochloride, Hyaluronic Acid and Combined Use in the Treatment of Knee Osteoarthritis

    Institute of Scientific and Technical Information of China (English)

    姜丹生

    2012-01-01

    目的 评价口服盐酸氨基葡萄糖和注射透明质酸钠以及两者联合治疗膝关节骨性关节炎的疗效.方法 采用随机对照临床研究方法,将162例诊断为膝骨性关节炎的患者随机分为3组,口服组、注射组、联合用药组各54例,分别给予口服盐酸氨基葡萄糖480毫克/次,每天口服3次,关节内注射2毫升/次,每周1次.共治疗5周.停药后观察2周.收集3组患者治疗期间Lequesne指数评分和VAS评分,来评估治疗前后膝关节症状变化程度.结果 治疗5周后,口服组、注射组、联合用药组Lequesne总指数比治疗前均有明显下降,分别为3.3±1.6、3.1±1.3、2.8±1.3.联合用药组和其他两组差异具有统计学意义(P<0.05).VAS评分治疗5周后口服组、注射组、联合用药组分别下降为1.77±0.91、1.66±1.21、1.53±1.13.与治疗前相比均具有统计学差异(P<0.05).结论 口服盐酸氨基葡萄糖和关节内注射透明质酸钠均对膝骨性关节炎具有良好的疗效,两者联合治疗方式效果优于单独用药治疗方式.%Objective To evaluate the efficacy of glucosamine hydrochloride,hyaluronic acid and combined use of the two drugs in the treatment of patients with knee osteoarthritis. Methods Totally 162 patients suffering from knee osteoarthritis were random divided into 3 groups, and were treated with glucosamine hydrochloride, hyaluronic acid and combined of above two therapies. Patients reveived medicine 3 times daily with total 480mg/d for glucosamine hydrochloride group, intra - articular injection of hyaluronic acid one time a week with 2ml per time and two treatments combined for combined group. Lequesne index and VAS score were recorded at 1,2,3,4,5 weeks during therapy and 1,2 weeks after therapy. Results Lequesne index were obviously decreased at 5 weeks for 3 groups. It was 3.3 ±1.6、3.1 ±1.3、2.8 ±1.3 , respectively. VAS scores were 1.77 ±0.91、1.66 ±1.21、1. 53 ± 1.13 at 5 weeks for 3 groups

  9. Stability Indicating HPLC Method for Simultaneous Quantification of Trihexyphenidyl Hydrochloride, Trifluoperazine Hydrochloride and Chlorpromazine Hydrochloride from Tablet Formulation

    Directory of Open Access Journals (Sweden)

    P. Shetti

    2010-01-01

    Full Text Available A new, simple, precise, rapid, selective and stability indicating reversed-phase high performance liquid chromatographic (HPLC method has been developed and validated for simultaneous quantification of trihexyphenidyl hydrochloride, trifluoperazine hydrochloride and chlorpromazine hydrochloride from combined tablet formulation. The method is based on reverse-phase using C-18 (250×4.6 mm, 5 μm particle size column. The separation is achieved using isocratic elution by methanol and ammonium acetate buffer (1% w/v, pH 6.5 in the ratio of 85:15 v/v, pumped at flow rate 1.0 mL/min and UV detection at 215 nm. The column is maintained at 30 °C through out the analysis. This method gives baseline resolution. The total run time is 15 min. Stability indicating capability is established buy forced degradation experiment. The method is validated for specificity, accuracy, precision and linearity as per International conference of harmonisation (ICH. The method is accurate and linear for quantification of trihexyphenidyl hydrochloride, trifluoperazine hydrochloride and Chlorpromazine hydrochloride between 5 - 15 μg/mL, 12.5- 37.5 μg/mL and 62.5 - 187.5 μg/mL respectively.

  10. High performance thin layer chromatographic method for simultaneous estimation of ibuprofen and pseudoephedrine hydrochloride

    Directory of Open Access Journals (Sweden)

    Chitlange S

    2008-01-01

    Full Text Available High performance thin layer chromatographic method is developed for simultaneous estimation of ibuprofen and pseudoephedrine hydrochloride in tablets. Silica gel 60F 254 plates were used as stationary phase and t.butanol: ethyl acetate: glacial acetic acid: water (7:4:2:2 v/v as mobile phase. Wavelength selected for analysis was 254 nm. Percent estimation of ibuprofen and pseudoephedrine hydrochloride was found to be 99.56% and 98.77%, respectively. Percent recovery for both the drugs was found in the range of 98.27% to 100.91%, respectively.

  11. A Novel Synthesis of Difloxacin Hydrochloride

    Institute of Scientific and Technical Information of China (English)

    2001-01-01

    Difloxacin hydrochloride, one of aryl-fluoro quinolone antibiotic, has been synthesized in seven steps from 2, 4-dichloro-5-fluoroacetophenone via oxalylation, ethoxymethylenation,amination, cyclization, hydrolysis, decarbonylation and N-methylpiperazination. Additional four new intermediates are produced.

  12. A novel asymmetric synthesis of cinacalcet hydrochloride

    OpenAIRE

    Arava, Veera R; Laxminarasimhulu Gorentla; Pramod K. Dubey

    2012-01-01

    A novel route to asymmetric synthesis of cinacalcet hydrochloride by the application of (R)-tert-butanesulfinamide and regioselective N-alkylation of the naphthyl ethyl sulfinamide intermediate is described.

  13. A novel asymmetric synthesis of cinacalcet hydrochloride

    Directory of Open Access Journals (Sweden)

    Veera R. Arava

    2012-08-01

    Full Text Available A novel route to asymmetric synthesis of cinacalcet hydrochloride by the application of (R-tert-butanesulfinamide and regioselective N-alkylation of the naphthyl ethyl sulfinamide intermediate is described.

  14. A novel asymmetric synthesis of cinacalcet hydrochloride

    Science.gov (United States)

    Gorentla, Laxminarasimhulu; Dubey, Pramod K

    2012-01-01

    Summary A novel route to asymmetric synthesis of cinacalcet hydrochloride by the application of (R)-tert-butanesulfinamide and regioselective N-alkylation of the naphthyl ethyl sulfinamide intermediate is described. PMID:23019473

  15. Identification of impurities and statistical classification of methamphetamine hydrochloride drugs seized in the China

    Science.gov (United States)

    Zhang, Jian Xin; Zhang, Da Ming; Han, Xu Guang

    2008-01-01

    A total of 48 methamphetamine hydrochloride samples from eight seizures were analyzed using gas chromatography–mass spectrometry (GC–MS) and a flame ionization detector (GC–FID). Major impurities detected include 1,2-dimethyl-3-phenylaziridine, Ephedrine/pseudoephedrine, 1,3-dimethyl-2-phenylnaphthalene, 1-benzyl-3-methylnaphthalene. These data are suggestive of ephedrine/pseudoephedrine as the main precursor of the methamphetamine hydrochloride samples seized during 2006–2007. Additionally the presence of 1,3-dimethyl-2-phenylnaphthalene, 1-benzyl-3-methylnaphthalene is indicative that six seizures were synthesized via the more specific ephedrine/hydriodic acid/red phosphorus method. In addition, five impurities were found for the first time in methamphetamine hydrochloride samples. Seventeen impurity peaks were selected from the GC–FID chromatograms. The peak areas of the selected peaks were then grouped for cluster analysis. PMID:19008060

  16. Multi-walled carbon nanotubes based catalyst plasmon resonance light scattering analysis of tetracycline hydrochloride

    Institute of Scientific and Technical Information of China (English)

    2008-01-01

    It was found that multi-walled carbon nanotubes (MWNTs) could catalyze the redox reaction between chlorauric acid (HAuCl4) and reductive drugs such as tetracycline hydrochloride (TC), producing gold nanoparticles (Au NPs). By measuring the plasmon resonance light scattering (PRLS) signals of the resulting Au NPs, tetracycline hydrochloride can be detected simply and rapidly with a linear range of 4―26 μmol/L, a correlated coefficient (r ) of 0.9955, and a limit of detection (3σ) of 6.0 nmol/L. This method has been successfully applied to the detection of tetracycline hydrochloride tablets in clinic with the recovery of 101.9% and that of fresh urine samples with the recovery of 98.3%―102.0%.

  17. HPLC Method for the Determination of Tamsulosin Hydrochloride in Sustained Release Tablets

    Institute of Scientific and Technical Information of China (English)

    齐美玲; 王鹏; 耿颖姝; 顾峻岭

    2003-01-01

    The development and validation of an isocratic high performance liquid chromatographic method is described for the determination of tamsulosin hydrochloride in sustained release tablets. The determination was performed on a Diamonsil BDS C18 column with a mobile phase consisting of a mixture of acetonitrile, methanol and 0.5% phosphoric acid solution (20∶30∶50,V/V/V) at a flow rate of 1.0 mL/min. UV detection was made at 274 nm. The linear range for tamsulosin hydrochloride was 0.81-8.10 μg/mL. The mean recovery was 99.8% (SR=0.7%, n=9), and the precision was found to be 0.45% (n=9). The proposed method can be used for routine analysis of tamsulosin hydrochloride in sustained release tablets.

  18. Second generation lipid nanoparticles (NLC) as an oral drug carrier for delivery of lercanidipine hydrochloride.

    Science.gov (United States)

    Ranpise, Nisharani S; Korabu, Swati S; Ghodake, Vinod N

    2014-04-01

    Lercanidipine hydrochloride is a calcium channel blocker used in the treatment of hypertension. It is a poor water soluble drug with absolute bioavailability of 10%. The aim of this study was to design lercanidipine hydrochloride-loaded nanostructured lipid carriers to investigate whether the bioavailability of the same can be improved by oral delivery. Lercanidipine hydrochloride nanostructured lipid carriers were prepared by the method of solvent evaporation at a high temperature and solidification by freeze drying. The nanostructured lipid carriers were evaluated for particle size analysis, zeta potential, entrapment efficiency, in vitro drug diffusion, ex vivo permeation studies and pharmacodynamic study. The resultant nanostructured lipid carriers had a mean size of 214.97 nm and a zeta potential of -31.6 ± 1.5 mV. More than 70% lercanidipine hydrochloride was entrapped in the NLCs. The SEM studies indicated the formation of type 2 nanostructured lipid carriers. The in vitro release studies demonstrated 19.36% release in acidic buffer pH 1.2 indicating that the drug entrapped in the nanostructured lipid carriers remains entrapped at acidic pH. The ex vivo studies indicated that the drug release was enhanced from 10% to 60.54% at blood pH in 24h. The in vivo pharmacodynamic study showed that NLCs released lercanidipine hydrochloride in a controlled manner for a prolonged period of time as compared to plain drug. These results clearly indicate that nanostructured lipid carriers are a potential controlled release formulation for lercanidipine hydrochloride and may be a promising drug delivery system for the treatment of hypertension. Copyright © 2013 Elsevier B.V. All rights reserved.

  19. 78 FR 34108 - Determination That SUBOXONE (Buprenorphine Hydrochloride and Naloxone Hydrochloride) Sublingual...

    Science.gov (United States)

    2013-06-06

    ... HUMAN SERVICES Food and Drug Administration Determination That SUBOXONE (Buprenorphine Hydrochloride and... (buprenorphine hydrochloride (HCl) and naloxone HCl) sublingual tablets, 2 milligrams (mg)/0.5 mg and 8 mg/2 mg... to approve abbreviated new drug applications (ANDAs) for buprenorphine HCl and naloxone...

  20. 盐酸表柔比星-聚乳酸-羟基乙酸共聚物纳米粒的制备%Study on Preparation of Epirubicin Hydrochloride Loaded Poly (L-Lactic-co-Glycolic Acid) Nanoparticles and the Effects in Vitro

    Institute of Scientific and Technical Information of China (English)

    宋晶晶; 李慧; 傅红兴; 纪建松

    2012-01-01

    目的 制备盐酸表柔比星-聚乳酸-羟基乙酸(PLGA)共聚物纳米粒,对其进行质量评价.方法 采用乳化-溶剂挥发法制备盐酸表柔比星纳米粒;对主要处方因素如PLGA用量、外水相中聚山梨酯-80用量、泊洛沙姆188和聚山梨酯-80比例进行正交设计,以药物的包封率、载药量和药物利用率等为考察指标.结果 采用优化后处方制得的纳米粒药物包封率为(32.6±1.2)%,载药量为(7.2±0.5)%,药物利用率为(51.6±3.4)%,纳米粒平均粒径166.6nm,药物可持续160h释放.结论 该方法制备盐酸表柔比星纳米粒工艺简单,无需使用聚乙烯醇,药物释放缓慢.%Objective To prepare epirubicin hydrochloride-loaded poly L-lactic-eo-glycolic acid (PLGA) nanoparticles and investigate the characteristics. Methods The epirubicin hydrochloride-loaded PLGA nanoparticles were prepared by double emulsion-solvent evaporation method. The main effective factors such as the amount of PLGA, Tween-80 in external water phase, and Ine ratio of poloxamer 188 to Tween-80 were orthogonally designed. Drag entrapment efficiency, drug loading rate and drug utilization were determined. Results By using the optimal formulation, the drug encapsulation efficiency of the nanoparticles was (32.6±1.2)% ; the drug loading was (7.2±0.5)% ; the drug utilization was (51.6±3.4)% ; the mean size of the nanoparticles was 166.6 ran; the drug release continued 160 hours. Conclusion Epirubicin hydrochloride-loaded PLGA nanoparticles are prepared successfully and simpiy without use of polyviol and display sustained drug release properties.

  1. [Clinical evaluation of roxatidine acetate hydrochlorides as a preanesthetic medication].

    Science.gov (United States)

    Namba, M; Chihara, E; Ibuki, T; Ashida, H; Fukushima, H; Tanaka, Y

    2001-02-01

    Roxatidine acetate hydrochloride capsule is slowly absorbed from the gastrointestinal tract, and its acid suppressive effect on the stomach is long-lasting compared with other H2-blockers. The reduction of gastric juice in perioperative period is considered advantageous for patients not only because it decreases the risk for aspiration pneumonia but also because it reduces the risk of bronchial spasm induced by gastroesophageal reflux of acidic gastric content. The effects of single oral administration of roxatidine acetate hydrochloride 150 mg at night before the operation on the volume and pH of gastric juice were investigated during anesthesia using two types of anesthetic agents (isoflurane and propofol) in 93 patients of three age groups (group Y: age 20-40, group M: age 41-64, group O: age 65 roxatidine on reduction of gastric juice was found at the time of anesthetic induction and 2 hours after the induction in any age group with either anesthetic agent. The serum concentration of roxatidine at the time of induction was much higher in group O. The value of residual concentration of roxatidine 20 hours after oral intake was estimated from the intraoperative measurements of serum concentration. The results suggest that single administration at night before the operation is sufficient for the oldest group, but an additive dose is recommended for the younger groups.

  2. Octenidine hydrochloride in hydatid disease.

    Science.gov (United States)

    Altindis, Mustafa; Arikan, Yuksel; Cetinkaya, Zafer; Polat, Coskun; Yilmaz, Sezgin; Akbulut, Gökhan; Dilek, Osman Nuri; Gokce, Ozcan

    2004-01-01

    Hydatid disease is still endemic in many devoloping countries and continues to be an important cause of morbidity. The objective of this study was to determine the in vitro scolicidal effects of octenidine hydrochloride in different concentrations using different exposure times. After hydatid cyst liquid was left to precipitate for 1 h to obtain cystic sand, various concentrations of octenidine (undiluted, 1% and 0.1% diluted) were added to concentrated hydatid cyst sediments for 5, 10, 15, 20, 25, 30, 45, and 60 min, and scolicidal effects of octenidine were compared with 20% saline and control group for the same times. It was found that undiluted octenidine had a strong scolicidal effect at 15 min compared to saline at 20%. One percent octenidine had a scolicidal effect at 30 min. However, 0.1% octenidine did not have enough scolicidal effect in 1 h. It was concluded that undiluted and 1% diluted octenidine might be used for scolicidal purpose in the treatment of hydatid disease.

  3. Compound list: fluoxetine hydrochloride [Open TG-GATEs

    Lifescience Database Archive (English)

    Full Text Available fluoxetine hydrochloride FLX 00158 ftp://ftp.biosciencedbc.jp/archive/open-tggates/...LATEST/Human/in_vitro/fluoxetine_hydrochloride.Human.in_vitro.Liver.zip ftp://ftp.biosciencedbc.jp/archive/o...pen-tggates/LATEST/Rat/in_vivo/Liver/Single/fluoxetine_hydrochloride.Rat.in_vivo.Liver.Single.zip ftp://ftp....biosciencedbc.jp/archive/open-tggates/LATEST/Rat/in_vivo/Liver/Repeat/fluoxetine_hydrochloride.Rat.in_vivo.Liver.Repeat.zip ...

  4. Effects of aluminum sulfate on delta-aminolevulinate dehydratase from kidney, brain, and liver of adult mice

    Directory of Open Access Journals (Sweden)

    Schetinger M.R.C.

    1999-01-01

    Full Text Available The purpose of the present study was to investigate the in vitro and in vivo effects of aluminum sulfate on delta-aminolevulinic acid dehydratase (ALA-D activity from the brain, liver and kidney of adult mice (Swiss albine. In vitro experiments showed that the aluminum sulfate concentration needed to inhibit the enzyme activity was 1.0-5.0 mM (N = 3 in brain, 4.0-5.0 mM (N = 3 in liver and 0.0-5.0 mM (N = 3 in kidney. The in vivo experiments were performed on three groups for one month: 1 control animals (N = 8; 2 animals treated with 1 g% (34 mM sodium citrate (N = 8 and 3 animals treated with 1 g% (34 mM sodium citrate plus 3.3 g% (49.5 mM aluminum sulfate (N = 8. Exposure to aluminum sulfate in drinking water inhibited ALA-D activity in kidney (23.3 ± 3.7%, mean ± SEM, P<0.05 compared to control, but enhanced it in liver (31.2 ± 15.0%, mean ± SEM, P<0.05. The concentrations of aluminum in the brain, liver and kidney of adult mice were determined by graphite furnace atomic absorption spectrometry. The aluminum concentrations increased significantly in the liver (527 ± 3.9%, mean ± SEM, P<0.05 and kidney (283 ± 1.7%, mean ± SEM, P<0.05 but did not change in the brain of aluminum-exposed mice. One of the most important and striking observations was the increase in hepatic aluminum concentration in the mice treated only with 1 g% sodium citrate (34 mM (217 ± 1.5%, mean ± SEM, P<0.05 compared to control. These results show that aluminum interferes with delta-aminolevulinate dehydratase activity in vitro and in vivo. The accumulation of this element was in the order: liver > kidney > brain. Furthermore, aluminum had only inhibitory properties in vitro, while in vivo it inhibited or stimulated the enzyme depending on the organ studied.

  5. Porphyrin biodistribution in UV-exposed murine skin after methyl- and hexyl-aminolevulinate incubation

    DEFF Research Database (Denmark)

    Togsverd-Bo, Katrine; Lerche, Catharina M; Philipsen, Peter A

    2012-01-01

    Topical photodynamic therapy (PDT) with methyl-aminolevulinate (MAL) is a well-established treatment for precancerous skin lesions and non-melanoma skin cancer. Treatment outcomes are less effective for thick than for superficial lesions, which are presumed to be due to insufficient Pp......IX biodistribution in tumour tissue. Hexyl-aminolevulinate (HAL) is a more lipophilic photosensitizer precursor than MAL and may penetrate the skin to a greater depth and more homogeneously. We compared HAL- and MAL-induced PpIX accumulation in specific skin compartments using concentrations of 2%, 6% and 20% HAL...... and MAL on long-term UV-irradiated mouse skin. Furthermore, 20% HAL and 20% MAL were applied to non-irradiated skin. Porphyrin fluorescence was measured by fluorescence microscopy in selected skin regions: the epidermis, superficial dermis, deep dermis and sebaceous gland epithelium down to a depth of 1...

  6. Urticaria after methyl aminolevulinate photodynamic therapy in a patient with nevoid basal cell carcinoma syndrome.

    Science.gov (United States)

    Wolfe, Christopher M; Green, W Harris; Hatfield, H Keith; Cognetta, Armand B

    2012-11-01

    Methyl aminolevulinate photodynamic therapy (MAL-PDT) is utilized in several countries for the treatment of basal cell carcinoma, but allergic sensitization has been reported by the manufacturer. To the best of our knowledge, we report the first case of urticaria following MAL-PDT in a patient with nevoid basal cell carcinoma syndrome. Prophylactic use of antihistamines may allow continued use of MAL-PDT in this setting.

  7. A 10-Year Retrospective Analysis of Methyl Aminolevulinate Photodynamic Therapy Consultation at the Hospital de Braga

    OpenAIRE

    Brito, C; Resende, C.; Oliveira, P.

    2016-01-01

    Introduction Photodynamic therapy (PDT) is a well-established treatment for actinic keratosis (AK), basal cell carcinoma (BCC), and Bowen’s disease (BD). The object of this study was to describe the results of a retrospective analysis of patients treated with methyl aminolevulinate PDT (MAL-PDT) with red light, over the past decade at the Hospital de Braga (Braga, Portugal). Methods This study is based on the retrospective analysis of the clinical records of patients treated with MAL-PDT from...

  8. Oxidative Profile and δ-Aminolevulinate Dehydratase Activity in Healthy Pregnant Women with Iron Supplementation

    OpenAIRE

    Leidiane De Lucca; Fabiane Rodrigues; Letícia B. Jantsch; Neme, Walter S.; Gallarreta, Francisco M. P.; Gonçalves, Thissiane L.

    2016-01-01

    An oxidative burst occurs during pregnancy due to the large consumption of oxygen in the tissues and an increase in metabolic demands in response to maternal physiological changes and fetal growth. This study aimed to determine the oxidative profile and activity of δ-aminolevulinate dehydratase (δ-ALA-D) in pregnant women who received iron supplementation. Oxidative stress parameters were evaluated in 25 pregnant women with iron supplementation, 25 pregnant women without supplementation and 2...

  9. Reduced aminolevulinate dehydrase activity in rats with functional renal failure induced by cyclosporin A.

    Science.gov (United States)

    Fontanellas, A; Herrero, J A; Enríquez de Salamanca, R

    1997-01-01

    Patients with chronic failure evidence various abnormalities in heme metabolism, primarily erythrocyte aminolevulinate dehydrase hypoactivity and increased plasma and erythrocyte porphyrin levels. Such abnormalities have also been observed in animals with both acute and chronic experimental renal failure. The aim of this work was to study these parameters of porphyrin metabolism in an experimental model of functional renal failure. A group of 11 male Wistar rats received 13 doses (25 mg/kg body weight/day) of cyclosporin A. Serum creatinine did not vary, but the blood urea nitrogen levels increased and a significant decrease in the creatinine clearance was observed. The drug also caused a marked decrease in the erythrocyte aminolevulinate dehydrase activity, a slight reduction of the hematocrit value, and increased levels of blood porphyrins. The plasma of treated rats showed capacity to inhibit aminolevulinate dehydrase activity when incubated in vitro with erythrocytes from control rats. Porphyrin metabolism remained unchanged in the liver. The daily diuresis was significantly decreased in the cyclosporin as compared to the control group; however, the porphyrinuria showed no changes. The derangements in the erythrocyte heme biosynthesis pathway observed in patients with chronic renal failure are reproducible in an experimental model of cyclosporin A-induced functional renal failure.

  10. Reaction of diphenyl diselenide with hydrogen peroxide and inhibition of delta-aminolevulinate dehydratase from rat liver and cucumber leaves

    Directory of Open Access Journals (Sweden)

    M. Farina

    2002-06-01

    Full Text Available The interaction of the product of H2O2 and (PhSe2 with delta-aminolevulinate dehydratase (delta-ALA-D from mammals and plants was investigated. (PhSe2 inhibited rat hepatic delta-ALA-D with an IC50 of 10 µM but not the enzyme from cucumber leaves. The reaction of (PhSe2 with H2O2 for 1 h increased the inhibitory potency of the original compound and the IC50 for animal delta-ALA-D inhibition was decreased from 10 to 2 µM. delta-ALA-D from cucumber leaves was also inhibited by the products of reaction of (PhSe2 with H2O2 with an IC50 of 4 µM. The major product of reaction of (PhSe2 with H2O2 was identified as seleninic acid and produced an intermediate with a lambdamax at 265 nm after reaction with t-BuSH. These results suggest that the interaction of (PhSe2 with mammal delta-ALA-D requires the presence of cysteinyl residues in close proximity. Two cysteine residues in spatial proximity have been recently described for the mammalian enzyme. Analysis of the primary structure of plant delta-ALA-D did not reveal an analogous site. In contrast to (PhSe2, seleninic acid, as a result of the higher electrophilic nature of its selenium atom, may react with additional cysteinyl residue(s in mammalian delta-ALA-D and also with cysteinyl residues from cucumber leaves located at a site distinct from that found at the B and A sites in mammals. Although the interaction of organochalcogens with H2O2 may have some antioxidant properties, the formation of seleninic acid as a product of this reaction may increase the toxicity of organic chalcogens such as (PhSe2.

  11. Synthesis and Molecular Recognition of Novel Cyclic Pseudopeptides Containing L-Glutamic Acid or L-Aspartic Acid Backbones

    Institute of Scientific and Technical Information of China (English)

    WANG Tao王涛; HUANG Xiao-Yi黄小毅; XIA Chuan-Qin夏传琴; YU Xiao-Qi余孝其; XIE Ru-Gang谢如刚

    2004-01-01

    Novel cyclic pseudopeptides containing L-glutamic acid or L-aspartic acid backbone structures were efficiently synthesized and characterized. Their chiral recognition properties for L- and D-amino acid methyl ester hydrochloride were discussed also.

  12. Extractive determination of ephedrine hydrochloride and bromhexine hydrochloride in pure solutions, pharmaceutical dosage form and urine samples.

    Science.gov (United States)

    Abdel-Ghani, N T; Rizk, M S; Mostafa, M

    2013-07-01

    Simple, rapid, sensitive, precise and accurate spectrophotometeric methods for the determination of ephedrine hydrochloride (E-HCl) and bromhexine hydrochloride (Br-HCl) in bulk samples, dosage form and in spiked urine samples were investigated. The methods are based on the formation of a yellow colored ion-associates due to the interaction between the examined drugs with picric acid (PA), chlorophyllin coppered trisodium salt (CLPH), alizarin red (AR) and ammonium reineckate (Rk) reagents. A buffer solution had been used and the extraction was carried out using organic solvent, the ion associates exhibit absorption maxima at 410, 410, 430 and 530 nm of (Br-HCl)with PA, CLPH, AR and Rk respectively; 410, 410, 435 and 530 of (E-HCl) with PA, CLPH, AR and Rk respectively. (E-HCl) and (Br-HCl) could be determined up to 13, 121, 120 and 160; 25, 200, 92 and 206 μg mL(-1), using PA, CLPH, AR and Rk respectively. The optimum reaction conditions for quantitative analysis were investigated. In addition, the molar absorptivity, Sandell sensitivity were determined for the investigated drug. The correlation coefficient was ≥0.995 (n=6) with a relative standard deviation (RSD) ≤1.15 for five selected concentrations of the reagents. Therefore the concentration of Br-HCl and E-HCl drugs in their pharmaceutical formulations and spiked urine samples had been determined successfully.

  13. Extractive determination of ephedrine hydrochloride and bromhexine hydrochloride in pure solutions, pharmaceutical dosage form and urine samples

    Science.gov (United States)

    Abdel-Ghani, N. T.; Rizk, M. S.; Mostafa, M.

    2013-07-01

    Simple, rapid, sensitive, precise and accurate spectrophotometeric methods for the determination of ephedrine hydrochloride (E-HCl) and bromhexine hydrochloride (Br-HCl) in bulk samples, dosage form and in spiked urine samples were investigated. The methods are based on the formation of a yellow colored ion-associates due to the interaction between the examined drugs with picric acid (PA), chlorophyllin coppered trisodium salt (CLPH), alizarin red (AR) and ammonium reineckate (Rk) reagents. A buffer solution had been used and the extraction was carried out using organic solvent, the ion associates exhibit absorption maxima at 410, 410, 430 and 530 nm of (Br-HCl)with PA, CLPH, AR and Rk respectively; 410, 410, 435 and 530 of (E-HCl) with PA, CLPH, AR and Rk respectively. (E-HCl) and (Br-HCl) could be determined up to 13, 121, 120 and 160; 25, 200, 92 and 206 μg mL-1, using PA, CLPH, AR and Rk respectively. The optimum reaction conditions for quantitative analysis were investigated. In addition, the molar absorptivity, Sandell sensitivity were determined for the investigated drug. The correlation coefficient was ⩾0.995 (n = 6) with a relative standard deviation (RSD) ⩽1.15 for five selected concentrations of the reagents. Therefore the concentration of Br-HCl and E-HCl drugs in their pharmaceutical formulations and spiked urine samples had been determined successfully.

  14. [Simultaneous determination of five cold medicine ingredients in paracetamol triprolidine hydrochloride and pseudoephedrine hydrochloride tablets by pH/organic solvent double-gradient high performance liquid chromatography].

    Science.gov (United States)

    Xuan, Xueyi; Huang, Lina; Pan, Xiaoling; Li, Ning

    2013-02-01

    A pH/organic solvent double-gradient mode in reversed-phase high performance liquid chromatography (HPLC) has been established as a new approach to the simultaneous determination of acetaminophen, caffeine, salicylamide, pseudoephedrine hydrochloride and triprolidine hydrochloride in paracetamol triprolidine hydrochloride and pseudoephedrine hydrochloride tablets. Through the optimization of the organic solvent gradient mode and pH/organic solvent double-gradient mode, the optimum double-gradient HPLC system of the five cold medicine ingredients has been built. The determination was carried out on a Diamonsiol C18 column (250 mm x 4.6 mm, 5 microm). The mobile phase consisted of methanol, 0.05 mol/L ammonium acetate solution and 0.08 mol/L acetic acid solution. The column temperature was set at 30 degrees C. The flow rate was 1.0 mL/min. The sample was measured at multiple wavelengths: 0-6 min, 280 nm; 6-7 min, 257 nm; 7-14 min, 280 nm; 14 min, 233 nm. The separation of the five cold medicine ingredients in the tablets was achieved in 25.5 min. The linear ranges of acetaminophen, pseudoephedrine hydrochloride, caffeine, salicylamide and triprolidine hydrochloride were 0.055 -0.998 g/L, 0.053-0.946 g/L, 0.007-0.129 g/L, 0.035-0.622 g/L and 0.002-0.039 g/L, respectively, with their correlation coefficients greater than 0.999 0. The detection limits (S/N = 3) were 0.09, 6, 0.02, 0.128 and 0.02 mg/L, respectively. Their mean recoveries were 97.9%-102.8%. The advantage of the method is the simultaneous determination of acidic, neutral and basic compounds. It also can improve the column efficiency of the analyte, compress the half-peak width and reduce the trailing. The optimized and validated method can be used for the simultaneous determination of the five cold medicine ingredients in the tablets.

  15. Cartap hydrochloride poisoning: A clinical experience

    Directory of Open Access Journals (Sweden)

    Hari K Boorugu

    2012-01-01

    Full Text Available Cartap hydrochloride, a nereistoxin analog, is a commonly used low toxicity insecticide. We describe a patient who presented to the emergency department with alleged history of ingestion of Cartap hydrochloride as an act of deliberate self-harm. The patient was managed conservatively. To our knowledge this is the first case report of Cartap hydrochloride suicidal poisoning. Cartap toxicity has been considered to be minimal, but a number of animal models have shown significant neuromuscular toxicity resulting in respiratory failure. It is hypothesized that the primary effect of Cartap hydrochloride is through inhibition of the [ 3 H]-ryanodine binding to the Ca 2+ release channel in the sarcoplasmic reticulum in a dose-dependent manner and promotion of extracellular Ca 2+ influx and induction of internal Ca 2+ release. This results in tonic diaphragmatic contraction rather than paralysis. This is the basis of the clinical presentation of acute Cartap poisoning as well as the treatment with chelators namely British Anti Lewisite and sodium dimercaptopropane sulfonate.

  16. 21 CFR 556.350 - Levamisole hydrochloride.

    Science.gov (United States)

    2010-04-01

    ... 21 Food and Drugs 6 2010-04-01 2010-04-01 false Levamisole hydrochloride. 556.350 Section 556.350 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL DRUGS, FEEDS, AND RELATED PRODUCTS TOLERANCES FOR RESIDUES OF NEW ANIMAL DRUGS IN FOOD Specific Tolerances for Residues of New Animal Drugs...

  17. Cartap hydrochloride poisoning: A clinical experience.

    Science.gov (United States)

    Boorugu, Hari K; Chrispal, Anugrah

    2012-01-01

    Cartap hydrochloride, a nereistoxin analog, is a commonly used low toxicity insecticide. We describe a patient who presented to the emergency department with alleged history of ingestion of Cartap hydrochloride as an act of deliberate self-harm. The patient was managed conservatively. To our knowledge this is the first case report of Cartap hydrochloride suicidal poisoning. Cartap toxicity has been considered to be minimal, but a number of animal models have shown significant neuromuscular toxicity resulting in respiratory failure. It is hypothesized that the primary effect of Cartap hydrochloride is through inhibition of the [(3)H]-ryanodine binding to the Ca(2+) release channel in the sarcoplasmic reticulum in a dose-dependent manner and promotion of extracellular Ca(2+) influx and induction of internal Ca(2+) release. This results in tonic diaphragmatic contraction rather than paralysis. This is the basis of the clinical presentation of acute Cartap poisoning as well as the treatment with chelators namely British Anti Lewisite and sodium dimercaptopropane sulfonate.

  18. 21 CFR 184.1676 - Pyridoxine hydrochloride.

    Science.gov (United States)

    2010-04-01

    ... hydrochloride that is prepared by chemical synthesis. (b) The ingredient meets the specifications of the Food... chapter; meat products as defined in § 170.3(n)(29) of this chapter; milk products as defined in § 170.3(n)(31) of this chapter; plant protein products as defined in § 170.3(n)(33) of this chapter; and...

  19. Spectrophotometric and HPLC methods for simultaneous estimation of pseudoephedrine hydrochloride and loratadine from tablets

    Directory of Open Access Journals (Sweden)

    Singhvi I

    2006-01-01

    Full Text Available Two simple, accurate, economical and reproducible UV spectrophotometric and one HPLC method for simultaneous estimation of two-component drug mixture of pseudoephedrine hydrochloride and loratadine in combined tablet dosage form have been developed. The first developed method employs multiwavelength spectroscopy using seven mixed standards and 257.0 nm and 283.0 nm as two wavelengths for estimation. The second method involves first derivative spectroscopy using 308.6 nm and 263.0 nm as zero crossing points for pseudoephedrine hydrochloride and loratadine respectively. For both spectrophotometric methods, 0.2 M hydrochloric acid was used as solvent. Linearity was observed in concentration range of 0-40 mg/ml of loratadine and 0-800 mg/ml of pseudoephedrine hydrochloride. Developed HPLC method is reverse-phase chromatographic method using Inertsil C 18 column and methanol:ammonium acetate buffer in ratio of 80:20 pH 7.5 as mobile phase. Nimesulide was used as internal standard for HPLC method. For HPLC method, linearity was observed in concentration range of 0-200 mg/ml of loratadine and 100-2000 mg/ml of pseudoephedrine hydrochloride. Results of analysis were validated statistically and by recovery studies.

  20. HPLC Determination of Propranolol Hydrochloride,Verapamil Hydrochloride and Propafenone Hydrochloride Ilegally Mixed into Wenxin Granules%高效液相色谱法测定稳心颗粒中非法添加药物的含量

    Institute of Scientific and Technical Information of China (English)

    张士勇; 程军; 叶云

    2012-01-01

    Objective To set up a method for the determination of propranolole hydrochloride, verapamil hydrochloride and propafenone hydrochloride illegally mixed into Wenxin Granules by HPLC. Methods The HPLC method was used. The Inertsil ODS - SP C18 column (250 mm × 4. 6 mm, 5 μm) was used with the mobile phase of phosphate buffer (adding water to dissolve potassium dihydrogen phosphate 6. 8 g and sodium 1 - octanesulfonate 1. 3 g, and diluting to 1 000 mL, adjusting pH value to 3.0 with phosphoric acid ) -methanol(40: 60). The flow rate was 0.8 mL/min, the detection wavelength was set at 223 nm and the column temperature was 25 ℃. Results The calibration curve showed the good linearity for propranolole hydrochloride, verapamil hydrochloride and propafenone hydrochloride in the range of 00. 019 76-2.47 μg( r = 1) ,0. 01-2. 5 μg(r = l) and 0.009 948-2.487 μg( r = 1) respectively;the average recovery rates (n = 6) were 97. 11% , 97. 63% and 98. 88% , respectively; RSD were 1. 85% , 1. 92% and 1. 46% , respectively. Conclusion This method is accurate and reproducible, which can be used for the determination of propranolole hydrochloride, verapamil hydrochloride and propafenone hydrochloride illegally mixed into Wenxin Granules.%目的 建立检测稳心颗粒中非法添加的盐酸普萘洛尔、盐酸维拉帕米和盐酸普罗帕酮含量的高效液相色谱法.方法 采用lnertsil ODS-SP C18色谱柱(250 mm×4.6 mm,5μm),流动相为磷酸盐缓冲液(取磷酸二氢钾6.8 g,辛烷磺酸钠1.3 g,加水溶解并稀释至1 000 mL,用磷酸调节pH至3.0)-甲醇(40:60),流速为0.8 mL/min,检测波长为223 nm,柱温为25℃.结果 盐酸普萘洛尔、盐酸维拉帕米和盐酸普罗帕酮进样量的线性范围分别为0.019 76~2.47 μg(r=1),0.01~2.5μg(r=1)和0.009 948~2.487μg(r=1);平均回收率分别为97.11%,97.63%和98.88%,RSD分别为1.85%,1.92%和1.46%(n=6).结论 该方法准确、重现性好,可作为稳心颗粒中非法添加盐酸普萘洛尔、

  1. Clinical studies of combined photodynamic therapy using 5-fluorouracil and methyl-aminolevulinate in patients at high risk for squamous cell carcinoma

    Science.gov (United States)

    Maytin, Edward V.; Lohser, Sara; Tellez, Alejandra; Wene, Lauren; Ishak, Rim; Anand, Sanjay

    2013-03-01

    Photodynamic therapy (PDT) using aminolevulinic acid or its methyl ester, methyl-aminolevulinate (MAL), is an increasingly recognized approach for treating squamous neoplasia of the skin. Advantages of MAL-PDT include its ability to cover broad diseased areas (field treatment), and to do multiple sessions with little-to-no risk of scarring or mutagenesis. MAL-PDT is especially valuable in certain populations at high risk for skin cancer, including Caucasian patients with extensive solar damage, and organ transplant recipients (OTR) who take immunosuppressive drugs to prevent graft rejection. The latter group has a 65-200 fold increased risk of developing squamous cell carcinoma (SCC), a major cause of mortality. Therapeutic options for those patients, other than frequent surgeries, are very limited. Topical 5-Fluorouracil (5-FU), frequently prescribed in normal patients for pre-SCC of the skin, is only minimally effective in the OTR group. MAL-PDT, however, has ~40% efficacy for pre-SCC in OTR patients. Based upon our preclinical studies in mouse tumor models, which showed that preconditioning with 5-FU can drive higher accumulation of target protoporphyins (PpIX), we proposed a rational combination regimen of 5-FU and MAL-PDT in humans. A clinical trial was designed to test the hypothesis that a combination of 5-FU followed by MAL-PDT will elevate PpIX levels and achieve better clinical outcomes in high-risk OTR patients. Primary endpoints include PpIX levels and biochemical markers (p53) measured noninvasively and in skin biopsies. Lesion clearance and recurrence (via photographs and clinical exam) are secondary endpoints. Ongoing results of this clinical trial are presented.

  2. Molecular dynamics analysis of the structural and dynamic properties of the functionally enhanced hepta-variant of mouse 5-aminolevulinate synthase.

    Science.gov (United States)

    Na, Insung; DeForte, Shelly; Stojanovski, Bosko M; Ferreira, Gloria C; Uversky, Vladimir N

    2017-01-09

    Heme biosynthesis, a complex, multistage, and tightly controlled process, starts with 5-aminolevulinate (ALA) production, which, in metazoa and certain bacteria, is a reaction catalyzed by 5-aminolevulinate synthase (ALAS), a pyridoxal 5'-phosphate (PLP)-dependent enzyme. Functional aberrations in ALAS are associated with several human diseases. ALAS can adopt open and closed conformations, with segmental rearrangements of a C-terminal, 16-amino acid loop and an α-helix regulating accessibility to the ALAS active site. Of the murine erythroid ALAS (mALAS2) forms previously engineered to assess the role of the flexible C-terminal loop versus mALAS2 function one stood out due to its impressive gain in catalytic power. To elucidate how the simultaneously introduced seven mutations of this activity-enhanced variant affected structural and dynamic properties of mALAS2, we conducted extensive molecular dynamics simulation analysis of the dimeric forms of wild-type mALAS2, hepta-variant and Rhodobacter capsulatus ALAS (aka R. capsulatus HemA). This analysis revealed that the seven simultaneous mutations in the C-terminal loop, which extends over the active site of the enzyme, caused the bacterial and murine proteins to adopt different conformations. Specifically, a new β-strand in the mutated 'loop' led to interaction with two preexisting β-strands and formation of an anti-parallel three-stranded β-sheet, which likely endowed the murine hepta-variant a more 'stable' open conformation than that of wild-type mALAS2, consistent with a kinetic mechanism involving a faster closed-to-open conformation transition and product release for the mutated than wild-type enzyme. Further, the dynamic behavior of the mALAS2 protomers was strikingly different in the two dimeric forms.

  3. Neurotrophic Effect of Asiatic acid, a Triterpene of Centella asiatica Against Chronic 1-Methyl 4-Phenyl 1, 2, 3, 6-Tetrahydropyridine Hydrochloride/Probenecid Mouse Model of Parkinson's disease: The Role of MAPK, PI3K-Akt-GSK3β and mTOR Signalling Pathways.

    Science.gov (United States)

    Nataraj, Jagatheesan; Manivasagam, Thamilarasan; Justin Thenmozhi, Arokiasamy; Essa, Musthafa Mohamed

    2017-02-08

    Regulation of various signalling (Ras-MAPK, PI3K and AKT) pathways by augmented activity of neurotrophic factors (NTFs) could prevent or halt the progress of dopaminergic loss in Parkinson's disease (PD). Various in vitro and in vivo experimental studies indicated anti-parkinsonic potential of asiatic acid (AA), a pentacyclic triterpene obtained from Centella asiatica. So the present study is designed to determine the neurotrophic effect of AA against 1-methyl 4-phenyl 1, 2, 3, 6-tetrahydropyridine hydrochloride/probenecid (MPTP/p) neurotoxicity in mice model of PD. AA treatment for 5 weeks significantly attenuated MPTP/p induced motor abnormalities, dopamine depletion and diminished expressions NTFs and tyrosine kinase receptors (TrKB). We further, revealed that AA treatment significantly inhibited the MPTP/p-induced phosphorylation of MAPK/P38 related proteins such as JNK and ERK. Moreover, AA treatment increased the phosphorylation of PI3K, Akt, GSK-3β and mTOR, suggesting that AA activated PI3K/Akt/mTOR signalling pathway, which might be the cause of neuroprotection offered by AA. The present findings provided more elaborate in vivo evidences to support the neuroprotective effect of AA on dopaminergic neurons of chronic Parkinson's disease mouse model and the potential of AA to be developed as a possible new therapeutic target to treat PD.

  4. Investigation of olopatadine hydrochloride under stress conditions by hydrophilic interaction liquid chromatography

    Directory of Open Access Journals (Sweden)

    Maksić Jelena Đ.

    2016-01-01

    Full Text Available The purpose of the present research was to conduct stress degradation studies on the olopatadine hydrochloride, an antiallergic drug, using the hydrophilic interaction liquid chromatography (HILIC. HILIC requires the utilization of polar and moderately polar stationary phases and aqueous-organic mobile phase usually containing more than 70% of organic solvent. In this study, olopatadine hydrochloride was subjected to acid and base hydrolysis, oxidation and termolytic degradation in order to estimate its stability under different stress conditions recommended by ICHQ1A (R2 guideline. Degree of degradation was followed by HILIC method. The chromatographic conditions were: column Betasil Cyano (100 mm × 4.6 mm, 5 mm particle size, mobile phase consisted of acetonitrile and ammonium acetate 5 mM (pH adjusted to 4.50 in ratio 85:15 V/V, flow rate was 1 mL min-1, column temperature was set at 30°C and detection was performed at 257 nm. Results obtained for stress studies indicated that olopatadine hydrochloride underwent transformation under acidic and oxidative (30% w/v hydrogen peroxyde conditions showing high degree of degradation. Furthermore, it was found that olopatadine hydrochloride is relatively stable when exposed to thermal (60°C and basic (1 M NaOH conditions. Therewith, kinetics of degradation reaction was determined with an aim to define the corresponding reaction rate constants and half-lives. Firstly, the order of the reaction was evaluated experimentally using the integral method. Based on the calculated values of the correlation coefficients, it was shown that the acidic, basic and oxidative degradation are the second-order reaction. High stability under basic conditions was achieved on the basis of the great degradation half-life values. Also, it has been verified that acidic degradation is the fastest reaction. [Projekat Ministarstva nauke Republike Srbije, br. 172052

  5. 氨基酮戊酸光动力疗法抑制成纤维细胞生长因子10诱导的HaCaT细胞过度角化及增殖的机制研究%Mechanisms underlying the inhibitory effects of aminolevulinic acid-based photodynamic therapy on fibroblast growth factor 10-induced excessive cornification and proliferation of HaCaT cells

    Institute of Scientific and Technical Information of China (English)

    易飞; Maya Valeska Gozali; 张家安; 周炳荣; 骆丹; 张丽超; 王申; 刘娟; 吴红巾

    2015-01-01

    目的 探讨氨基酮戊酸光动力疗法(ALA-PDT)对成纤维细胞生长因子10(FGF-10)诱导的HaCaT细胞过度角化及增殖的作用及其机制.方法 将培养的HaCaT细胞分为4组:空白对照组(无任何处理),FGF-10组(加入FGF-10孵育24 h),ALA-PDT组(ALA孵育24 h后红光照射),FGF-10+ ALA-PDT组(FGF-10孵育24 h后,再加ALA孵育24 h,红光照射).用CCK-8法检测各组细胞增殖活性,Western印迹法检测K1、K6、K16及角质形成细胞生长因子受体(KGFR)的含量,ELISA法检测各组细胞上清液中白细胞介素1α(IL-1α)蛋白表达,免疫荧光检测各组细胞KGFR和K6蛋白表达水平.统计学分析采用析因设计的方差分析和单因素方差分析.结果 析因分析显示,ALA-PDT和FGF-10对HaCaT细胞增殖无交互作用(F交互=1.369,P=0.276),FGF-10对HaCaT细胞增殖有促进作用(FFGF-10=20.853,P<0.05),而ALA-PDT有抑制作用(FALA-PDT=24.822,P< 0.05).与空白对照组细胞增殖活性(A值为0.924±0.024)比较,FGF-10组(1.233±0.099)显著升高(P<0.05),而ALA-PDT组(0.718±0.107)显著降低(P<0.05),FGF-10+ ALA-PDT组(0.901±0.014)较FGF-10组显著降低(P<0.05).Western印迹法显示,FGF-10可促进K1、K6、K16蛋白和KGFR的表达(均P<0.05),而ALA-PDT抑制这些蛋白的表达(均P< 0.05),FGF-10+ ALA-PDT组K1、K6、K16和KGFR的相对表达量与FGF-10组比较均显著降低(均P< 0.05).ELISA法显示,FGF-10会增加HaCaT细胞IL-1α蛋白分泌(P<0.05),但ALA-PDT对其没有影响(P=0.467).此外,免疫荧光检测显示,FGF-10增加HaCaT细胞K6和KGFR免疫荧光强度(P<0.05),而ALA-PDT降低K6和KGFR免疫荧光强度(P<0.05),FGF-10+ ALA-PDT组K6和KGFR免疫荧光强度显著低于FGF-10组(P<0.05).结论 ALA-PDT能抑制FGF-10诱导的HaCaT细胞过度角化及增殖,其机制与下调K1、K6、K16、KGFR及IL-1α有关.%Objective To evaluate the inhibitory effects of aminolevulinic acid-based photodynamic therapy (ALA-PDT) on fibroblast growth factor

  6. Pharmacokinetic study of benfotiamine and the bioavailability assessment compared to thiamine hydrochloride.

    Science.gov (United States)

    Xie, Feifan; Cheng, Zeneng; Li, Sanwang; Liu, Xingling; Guo, Xin; Yu, Peng; Gu, Zhenkun

    2014-06-01

    Benfotiamine is a lipid-soluble thiamine precursor which can transform to thiamine in vivo and subsequently be metabolized to thiamine monophosphate (TMP) and thiamine diphosphate (TDP). This study investigated the pharmacokinetic profiles of thiamine and its phosphorylated metabolites after single- and multiple-dose administration of benfotiamine in healthy Chinese volunteers, and assessed the bioavailability of orally benfotiamine administration compared to thiamine hydrochloride. In addition, concentration of hippuric acid in urine which is produced in the transformation process of benfotiamine was determined. The results showed that thiamine and its phosphorylated metabolites exhibited different pharmacokinetic characteristics in plasma, blood and erythrocyte, and one-compartment model provided the best fit for pharmacokinetic profiles of thiamine. The transformation process of benfotiamine to thiamine produced large amount of hippuric acid. No accumulation of hippuric acid was observed after multiple-dose of benfotiamine. Compared to thiamine hydrochloride, the bioavailability of thiamine in plasma and TDP in erythrocyte after oral administration of benfotiamine were 1147.3 ± 490.3% and 195.8 ± 33.8%, respectively. The absorption rate and extent of benfotiamine systemic availability of thiamine were significantly increased indicating higher bioavailability of thiamine from oral dose of benfotiamine compared to oral dose of thiamine hydrochloride.

  7. Stability-Indicating TLC-densitometric determination of nebivolol hydrochloride in bulk and pharmaceutical dosage form.

    Science.gov (United States)

    Shirkhedkar, Atul A; Bugdane, Prasad M; Surana, Sanjay J

    2010-02-01

    A simple, selective, precise, and stability-indicating high-performance thin-layer chromatographic (HPTLC) method for densitometric determination of nebivolol hydrochloride both as a bulk drug and in formulation was developed and validated as per the international conference on harmonization guidelines (ICH). The method employed TLC aluminium plates precoated with silica gel 60F254 as the stationary phase. The solvent system consisted of toluene-methanol-triethylamine (3.8:1.2:0.2 v/v/v). Densitometry analysis of nebivolol hydrochloride was carried out in the absorbance mode at 281 nm. The system was found to give compact spot for nebivolol hydrochloride (R(f) value of 0.33 +/- 0.02). The linear regression analysis data for the calibration plots showed good relationship with r(2)= 0.9994 +/- 0.0002 in the concentration range 500-3000 ng/spot. The mean value +/- SD of slope and intercept were 3.761 +/- 0.017 and 127.39 +/- 19.53 with respect to peak area. The limits of detection (LOD) and limit of quantitation (LOQ) were 63.10 ng/spot and 191.23 ng/ spot, respectively. Nebivolol hydrochloride was subjected to acid and alkali hydrolysis, oxidation, thermal degradation, and photodegradation. All the peaks of degradation products were well-resolved from the standard drug with significantly different R(f) values. Statistical analysis proves that the method is repeatable, selective and accurate for the estimation of said drug. The proposed developed HPTLC method can be applied for identification and quantitative determination of nebivolol hydrochloride in the bulk and pharmaceutical dosage form.

  8. A validated stability-indicative UPLC method for nilotinib hydrochloride for the determination of process-related and degradation impurities.

    Science.gov (United States)

    Kondra, Sudhakar Babu; Madireddy, Venkataramanna; Chilukuri, Mohanareddy; Papadasu, Narayanareddy; Jonnalagadda, Latha

    2014-09-01

    A novel stability-indicating ultra performance liquid chromatographic (UPLC) method has been developed for quantitative determination of nilotinib hydrochloride in active pharmaceutical ingredients along with four impurities (imp-1, imp-2, imp-3 and imp-4). The method is applicable to the quantification of related compounds and assay of nilotinib hydrochloride drug. Efficient chromatographic separation was achieved on a Shim-pack XR-ODS II, 75 × 3.0 mm, 1.8-µm column with a gradient mobile phase combination. Quantification was carried at 260 nm at a flow rate of 0.6 mL min(-1). Stress degradation conditions were established for nilotinib hydrochloride by subjecting it to acid, base, oxidation, humidity, thermal and photolysis. The stress samples were assayed against a qualified reference standard and the mass balance was found close to 97.0%. The developed UPLC method was validated according to the present International Conference on Harmonisation guidelines for specificity, detection limit, quantitation limit, linearity, accuracy, precision, intermediate precision and robustness. The resolution between nilotinib hydrochloride and four potential impurities is found to be >2.0. Regression analysis shows as r value (correlation coefficient) of >0.999 for nilotinib hydrochloride and four potential impurities.

  9. Direct, preparative enantioselective chromatography of propranolol hydrochloride and thioridazine hydrochloride using carbon dioxide-based mobile phases.

    Science.gov (United States)

    Geiser, F; Schultz, M; Betz, L; Shaimi, M; Lee, J; Champion, W

    1999-12-31

    In this paper, we describe the direct, preparative enantioselective chromatography of racemic (rac)-propranolol hydrochloride (HCI) and rac-thioridazine.HCl using Chiralpak AD chiral stationary phase and mobile phase systems containing carbon dioxide and methanol without the use of basic or acidic additives. Isolated fractions of propranolol.HCl were positively identified by mass spectrometry, Beilstein flame test, melting point, and chemical analysis to be HCI enantiomers of propranolol-HCl salts exhibited characteristic mass spectra peaks at 36 and 38 mass-to-charge ratio in the expected 3:1 isotopic ratio for the solute that were absent in the mass spectra for the free-base forms. To our knowledge, the direct, preparative enantioselective isolation of HCI enantiomeric salts of rac-propranolol and of rac-thioridazine have not been previously demonstrated and published.

  10. Spectrophotometric Method for Estimation of Tamsulosin Hydrochloride in Pharmaceutical Dosage Form Using Bromate-Bromide and Methyl Orange Reagent

    Directory of Open Access Journals (Sweden)

    Bharatkumar Ganeshbhai Chaudhari

    2012-09-01

    Full Text Available A simple, rapid, accurate and precise assay procedure based on Spectrophotometric method has been developed for the estimation of Tamsulosin hydrochloride in Pharmaceutical formulation. The method was based on the bromination of Tamsulosin hydrochloride with a known excess amount of Bromate-bromide mixture in acidic medium followed by the determination of surplus bromine by reacting with dye methyl orange and measuring the absorbance at 513 nm. Validation was carried out in compliance with International Conference on Harmonization guidelines. Linear regression analysis of method showed good linearity with the correlation co-efficient (r of 0.9978 with respect to absorbance in the concentration range of 2-12 μg/mL and the mean recovery for Tamsulosin hydrochloride was 99.65% ± 0.47 . The proposed method can be successfully applied for the analysis of tablet formulations.

  11. Clinical, histological, and immunohistochemical markers of resistance to Methyl-aminolevulinate Photodynamic therapy in Bowen's disease.

    Science.gov (United States)

    Gracia-Cazaña, T; Salazar, N; Vera-Álvarez, J; Aguilera, J; López-Navarro, N; Herrera-Ceballos, E; González, S; Juarranz, Á; Gilaberte, Y

    2017-09-08

    Bowen's disease (BD) is an intraepidermic squamous cell carcinoma (SCC), which principally appears on photoexposed areas.(1) Methyl-aminolevulinate (MAL) photodynamic therapy (PDT) is an excellent option for the treatment of BD (strength of recommendation, A; quality of evidence, 1). However, despite good response rates, some tumors prove non-responsive due to primary or acquired resistance.(2) The present study sought to identify clinical, histological, and molecular variables implicated in the response to MAL-PDT in BD. This article is protected by copyright. All rights reserved. This article is protected by copyright. All rights reserved.

  12. A terapia fotodinâmica com ácido 5-aminolevulínico como modalidade de tratamento para neoplasias cutâneas não-melanoma Topical 5-aminolevulinic acid photodynamic therapy as a treatment modality for nonmelanoma skin cancer

    Directory of Open Access Journals (Sweden)

    Lília Bernardini Antunes de Felício

    2008-08-01

    Full Text Available FUNDAMENTOS: A terapia fotodinâmica baseia-se na associação de fonte de luz e fotossensibilizador para destruir seletivamente as células. OBJETIVO: Avaliar os efeitos imediatos e tardios, a resposta clínica e os resultados estéticos da terapia fotodinâmica com ácido 5-aminolevulínico em neoplasias cutâneas não-melanoma. MÉTODOS: Trinta e quatro lesões, sendo 19 disceratoses de Bowen e 15 carcinomas basocelulares, foram submetidas à aplicação tópica e oclusiva do ácido 5-aminolevulínico a 20%, por seis horas, e posteriormente a sessão única de laser de diodo (630nm. RESULTADOS: Foram registrados: sensação de queimação durante as sessões; eritema, edema e erosões, nas primeiras 72 horas; cicatrização em média de quatro semanas; resultados estéticos variáveis de excelentes a bons. Aos três meses, a resposta clínica foi de 91,2%, sendo reduzida, aos 18 meses, para 73,3%, de modo similar tanto para disceratose de Bowen (72,2% quanto para carcinoma basocelular (75%. Foi evidenciada relação de tendência linear entre a redução da freqüência da resposta clínica e o aumento da dimensão das neoplasias cutâneas não-melanoma (pBACKGROUND: Photodynamic therapy is based on the association of a light source and photosensitizer in order to selectively destroy cells. OBJECTIVE: To evaluate the short and long-term effects, clinical response, and cosmetic outcome of the photodynamic therapy with 5-aminolaevulinic acid for non-melanoma skin cancer. METHODS: TThirty-four non-melanoma skin cancer - 19 Bowen’s diseases and 15 basal cell carcinomas, were submitted to a single 6-hour topical and occlusive application of 20% 5-aminolaevulinic acid, and were later exposed to 630 nm diode laser single session. RESULTS: Burning sensation during the session; erythema, edema and erosions in the first 72 hours; healing process after 4 weeks on average and excellent or good cosmetic results were observed. After 3 months, tumor

  13. [Antiseptics on the base of Octenidine Hydrochloride].

    Science.gov (United States)

    Malinovskií, N N; Reshetnikov, E A; Rubashnaia, I E; Mal'nikova, G N; Mitiukov, A P

    1997-01-01

    Comparative evaluation of laboratory and clinical investigation of antiseptic preparations on the base of octenidin-hydrochloride and bigluconate chlorhexidine in 537 patients was carried out. Statistically valid decrease in dissemination through the operation field and surgical wound after application of octenidin containing solutions was determined. It was established as well that these preparations were more effective fools of protection of the operation wound from its microbial contamination in comparison with antiseptic solutions widely spread to date in surgical practice.

  14. 抗抑郁药Duloxetine Hydrochloride

    Institute of Scientific and Technical Information of China (English)

    艾建国; 晋展

    2003-01-01

    @@ 日本Shionogi公司获得了Eli Lilly公司的授权,对其研制的一种对5-羟色胺(5-HT)和去甲肾上腺素(NE)的摄取有双重抑制作用的化合物Duloxetine Hydrochloride (Cymbalta(R),LY-264453,LY-248686)进行了进一步的开发.

  15. Effect of iptakalim hydrochloride on hemodynamics

    Institute of Scientific and Technical Information of China (English)

    Qing-leiZHU; HaiWANG; Wen-binXIAO

    2004-01-01

    AIM: To study the effect of iptakalim hydrochloride (Ipt) on hemodynamics. METHODS: Effect of Ipt on hemodynamics were studied in anesthetized nomotensive dogs, conscious nomotensive rats (NTR), and stroke prone spontaneously hypertensive rats (SHRsp), respectively. RESULTS: In pentobarbital anesthetized nomotensive dogs, Ipt at doses of 0.125, 0.25, 0.5,1.0, and 2.0 mg/kg iv could dose-dependently decrease blood pressure (BP), with the decrease of systolic BP equivalent

  16. Cartap hydrochloride poisoning: a case report

    OpenAIRE

    Sumesh Raj; Sheetal S.

    2014-01-01

    Cartap hydrochloride is a thiocarbamate insecticide used for control of chewing and sucking insects of all stages of development, on many crops. It is an analogue of nereistoxin. Poisoning with cartap is very rarely reported from India. We report a 46 year old man who consumed cartap with alcohol, presented with nausea & vomiting and improved with supportive measures. [Int J Res Med Sci 2014; 2(1.000): 360-361

  17. Low-dose methotrexate enhances aminolevulinate-based photodynamic therapy in skin carcinoma cells in vitro and in vivo.

    Science.gov (United States)

    Anand, Sanjay; Honari, Golara; Hasan, Tayyaba; Elson, Paul; Maytin, Edward V

    2009-05-15

    To improve treatment efficacy and tumor cell selectivity of delta-aminolevulinic acid (ALA)-based photodynamic therapy (PDT) via pretreatment of cells and tumors with methotrexate to enhance intracellular photosensitizer levels. Skin carcinoma cells, in vitro and in vivo, served as the model system. Cultured human SCC13 and HEK1 cells, normal keratinocytes, and in vivo skin tumor models were preconditioned with methotrexate for 72 h and then incubated with ALA for 4 h. Changes in protoporphyrin IX (PpIX) levels and cell survival after light exposure were assessed. Methotrexate preconditioning of monolayer cultures preferentially increased intracellular PpIX levels 2- to 4-fold in carcinoma cells versus normal keratinocytes. Photodynamic killing was synergistically enhanced by the combined therapy compared with PDT alone. Methotrexate enhancement of PpIX levels was achieved over a broad methotrexate concentration range (0.0003-1.0 mg/L; 0.6 nmol/L-2 mmol/L). PpIX enhancement correlated with changes in protein expression of key porphyrin pathway enzymes, approximately 4-fold increase in coproporphyrinogen oxidase and stable or slightly decreased expression of ferrochelatase. Differentiation markers (E-cadherin, involucrin, and filaggrin) were also selectively induced by methotrexate in carcinoma cells. In vivo relevance was established by showing that methotrexate preconditioning enhances PpIX accumulation in three models: (a) organotypic cultures of immortalized keratinocytes, (b) chemically induced skin tumors in mice; and (c) human A431 squamous cell tumors implanted subcutaneously in mice. Combination therapy using short-term exposure to low-dose methotrexate followed by ALA-PDT should be further investigated as a new combination modality to enhance efficacy and selectivity of PDT for epithelial carcinomas.

  18. Vitamin D Combined with Aminolevulinate (ALA)-Mediated Photodynamic Therapy (PDT) for Human Psoriasis: A Proof-of-Principle Study.

    Science.gov (United States)

    Maytin, Edward V; Honari, Golara; Khachemoune, Amor; Taylor, Charles R; Ortel, Bernhard; Pogue, Brian W; Sznycer-Taub, Nathaniel; Hasan, Tayyaba

    2012-09-01

    We previously showed that select agents (methotrexate or Vitamin D), when administered as a preconditioning regimen, are capable of promoting cellular differentiation of epithelial cancer cells while simultaneously enhancing the efficacy of 5-aminolevulinic acid (ALA)-mediated photodynamic therapy (PDT). In solid tumors, pretreatment with Vitamin D simultaneously promotes cellular differentiation and leads to selective accumulation of target porphyrins (mainly protoporphyrin IX, PpIX) within diseased tissue. However, questions of whether or not the effects upon cellular differentiation are inexorably linked to PpIX accumulation, and whether these effects might occur in hyperproliferative noncancerous tissues, have remained unanswered. In this paper, we reasoned that psoriasis, a human skin disease in which abnormal cellular proliferation and differentiation plays a major role, could serve as a useful model to test the effects of pro-differentiating agents upon PpIX levels in a non-neoplastic setting. In particular, Vitamin D, a treatment for psoriasis that restores (increases) differentiation, might increase PpIX levels in psoriatic lesions and facilitate their responsiveness to ALA-PDT. This concept was tested in a pilot study of 7 patients with bilaterally-matched psoriatic plaques. A regimen in which calcipotriol 0.005% ointment was applied for 3 days prior to ALA-PDT with blue light, led to preferential increases in PpIX (~130%), and reductions in thickness, redness, scaling, and itching in the pretreated plaques. The results suggest that a larger clinical trial is warranted to confirm a role for combination treatments with Vitamin D and ALA-PDT for psoriasis.

  19. RNA is required for enzymatic conversion of glutamate to delta-aminolevulinate by extracts of Chlorella vulgaris.

    Science.gov (United States)

    Weinstein, J D; Beale, S I

    1985-05-15

    Formation of delta-aminolevulinic acid (ALA) from glutamete catalyzed by a soluble extract from the unicellular green alga, Chlorella vulgaris, was abolished after incubation of the cell extract with bovine pancreatic ribonuclease A (RNase). Cell extract was prepared for the ALA formation assay by high-speed centrifugation and gel-filtration through Sephadex G-25 to remove insoluble and endogenous low-molecular-weight components. RNA hydrolysis products did not affect ALA formation, and RNase did not affect the ability of ATP and NADPH to serve as reaction substrates, indicating that the effect of RNase cannot be attributed to degradation of reaction substrates or transformation of a substrate or cofactor into an inhibitor. The effect of RNase was blocked by prior addition of placental RNase inhibitor (RNasin) to the cell extract, but RNasin did not reverse the effect of prior incubation of the cell extract with RNase, indicating that RNase does not act by degrading a component generated during the ALA-forming reaction, but instead degrades an essential component already present in active cell extract at the time the ALA-forming reaction is initiated. After inactivation of the cell extract by incubation with RNase, followed by administration of RNasin to block further RNase action, ALA-forming activity could be restored to a higher level than originally present by addition of a C. vulgaris tRNA-containing fraction isolated from an active ALA-forming preparation by phenol extraction and DEAE-cellulose chromatography. Baker's yeast tRNA, wheat germ tRNA, Escherichia coli tRNA, and E. coli tRNAglu type II were unable to reconstitute ALA-forming activity in RNase-treated cell extract, even though the cell extract was capable of catalyzing the charging of some of these RNAs with glutamate.

  20. Gastroretentive drug delivery system of ranitidine hydrochloride: formulation and in vitro evaluation.

    Science.gov (United States)

    Dave, Brijesh S; Amin, Avani F; Patel, Madhabhai M

    2004-04-08

    The purpose of this research was to prepare a gastroretentive drug delivery system of ranitidine hydrochloride. Guar gum, xanthan gum, and hydroxypropyl methylcellulose were evaluated for gel-forming properties. Sodium bicarbonate was incorporated as a gas-generating agent. The effects of citric acid and stearic acid on drug release profile and floating properties were investigated. The addition of stearic acid reduces the drug dissolution due to its hydrophobic nature. A 3(2) full factorial design was applied to systemically optimize the drug release profile. The amounts of citric acid anhydrous (X1) and stearic acid (X2) were selected as independent variables. The times required for 50% (t50) and 80% drug dissolution (t80), and the similarity factor f2 were selected as dependent variables. The results of the full factorial design indicated that a low amount of citric acid and a high amount of stearic acid favors sustained release of ranitidine hydrochloride from a gastroretentive formulation. A theoretical dissolution profile was generated using pharmacokinetic parameters of ranitidine hydrochloride. The similarity factor f2 was applied between the factorial design batches and the theoretical dissolution profile. No significant difference was observed between the desired release profile and batches F2, F3, F6, and F9. Batch F9 showed the highest f2 (f2 = 75) among all the batches, and this similarity is also reflected in t50 (approximately 214 minutes) and t80 (approximately 537 minutes) values. These studies indicate that the proper balance between a release rate enhancer and a release rate retardant can produce a drug dissolution profile similar to a theoretical dissolution profile.

  1. Stability of paclitaxel with ondansetron hydrochloride or ranitidine hydrochloride during simulated Y-site administration.

    Science.gov (United States)

    Burm, J P; Jhee, S S; Chin, A; Moon, Y S; Jeong, E; Nii, L; Fox, J L; Gill, M A

    1994-05-01

    The stability of paclitaxel with either ondansetron hydrochloride or ranitidine hydrochloride during simulated Y-site injection at room temperature was studied. Triplicate test solutions of paclitaxel 0.3 and 1.2 mg/mL were admixed 1:1 with ondansetron 0.03 and 0.3 mg/mL (as the hydrochloride salt) or ranitidine 0.5 and 2.0 mg/mL (as the hydrochloride salt). Also, paclitaxel 1.2 mg/mL was admixed 1:1:1 with ondansetron 0.3 mg/mL and ranitidine 2.0 mg/mL. The solutions were stored in glass containers at room temperature, and samples were removed at zero, one, two, and four hours for immediate assay. At the time of the assay and before any dilution, each sample was visually inspected for clarity, color, and precipitation, and the pH was determined. Drug concentrations were measured by stability-indicating high-performance liquid chromatographic procedures. Throughout the study, more than 90% of the initial concentrations of paclitaxel, ondansetron, and ranitidine remained in the solutions. No precipitates, color changes, or haziness was seen. The changes in pH were minor. Paclitaxel in concentrations of 0.3 and 1.2 mg/mL was stable when mixed with either ondansetron (0.03 or 0.3 mg/mL, as the hydrochloride salt) or ranitidine (0.5 or 2.0 mg/mL, as the hydrochloride salt) and stored in glass containers for four hours. Paclitaxel 1.2 mg/mL was also stable when mixed with both ondansetron 0.3 mg/mL and ranitidine 2.0 mg/mL and stored in glass containers for four hours.

  2. Simultaneous determination of pseudoephedrine hydrochloride and cetrizine hydrochloride by reverse phase high performance liquid chromatography

    Directory of Open Access Journals (Sweden)

    Nalini C

    2006-01-01

    Full Text Available A reversed phase high performance liquid chromatographic method has been developed using Shimadzu HPLC-VP series, LC-10 ATV pump, SPD10 AVP and C8 column, for simultaneous determination of pseudoephedrine hydrochloride and cetrizine hydrochloride in three marketed tablet formulations (extended release. The mobile phase consists of phosphate buffer of pH 7.0 and acetonitrile HPLC grade in the ratio of 1:1. The flow rate was maintained at 1 ml/min and the ultraviolet detection was done at 242 nm, which is the isosbestic point. Linearity coefficients, assay values, recovery studies and repeatability studies showed that the method is accurate and precise.

  3. Simultaneous Determination of Sitagliptin Phosphate Monohydrate and Metformin Hydrochloride in Tablets by a Validated UPLC Method.

    Science.gov (United States)

    Malleswararao, Chellu S N; Suryanarayana, Mulukutla V; Mukkanti, Khagga

    2012-01-01

    A novel approach was used to develop and validate a rapid, specific, accurate and precise reverse phase ultra performance liquid chromatographic (UPLC) method for the simultaneous determination of Sitagliptin phosphate monohydrate and Metformin hydrochloride in pharmaceutical dosage forms. The chromatographic separation was achieved on Aquity UPLC BEH C8 100 × 2.1 mm, 1.7 μm, column using a buffer consisting of 10 mM potassium dihydrogen phosphate and 2 mM hexane-1-sulfonic acid sodium salt (pH adjusted to 5.50 with diluted phosphoric acid) and acetonitrile as organic solvent in a gradient program. The flow rate was 0.2 mL min(-1) and the detection wavelength was 210 nm. The limit of detection (LOD) for Sitagliptin phosphate monohydrate and Metformin hydrochloride was 0.2 and 0.06 μg mL(-1), respectively. The limit of quantification (LOQ) for Sitagliptin phosphate monohydrate and Metformin hydrochloride was 0.7 and 0.2 μg mL(-1), respectively. This method was validated with respect to linearity, accuracy, precision, specificity and robustness. The method was also found to be stability-indicating.

  4. DEVELOPMENT AND VALIDATION OF STABILITY-INDICATING TLC-DENSITOMETRY METHOD FOR THE SIMULTANEOUS DETERMINATION OF EPERISONE HYDROCHLORIDE AND PARACETAMOL IN BULK AND TABLET DOSAGE FORM

    Directory of Open Access Journals (Sweden)

    Pritam S. Jain

    2013-08-01

    Full Text Available A rapid and reproducible stability indicating TLC-densitometric method was developed for the determination of eperisone hydrochloride and paracetamol in presence of their degraded products in bulk drugs and pharmaceutical formulations. Uniform degradation conditions were maintained by refluxing reaction mixtures for 8 h at 60°C including acidic, alkaline hydrolysis. Oxidation at room temperature, photochemical and dry heating degradation studies were also carried out. A sensitive and robust stability indicating TLC-densitometric method for simultaneous quantification of eperisone hydrochloride and paracetamol in bulk drugs and pharmaceutical formulations has been developed and validated. Separation was done on TLC aluminum sheets, pre-coated with silica gel 60F-254 using ethyl acetate: toluene: methanol (2:2:1 v/v/v. Spots at Rf 0.42 ± 0.04 and Rf 0.60 ± 0.02 were recognized as paracetamol and eperisone hydrochloride, respectively. Densitometric analysis of chromatoplates was carried out in absorbance mode at isobastic point 260 nm. The developed method was optimized and validated as per ICH guidelines. Method was found linear over the concentration range of 100-350 ng / spot for eperisone hydrochloride and 600-2100 ng / spot for paracetamol with the correlation coefficient (r2 of 0.999 and 0.999 for eperisone hydrochloride and paracetamol, respectively. The developed TLC method can be applied for routine analysis of eperisone hydrochloride and paracetamol in presence of their degraded products in their combined pharmaceutical formulations.

  5. Fenton degradation of Cartap hydrochloride: identification of the main intermediates and the degradation pathway.

    Science.gov (United States)

    Tian, Kaixun; Ming, Cuixiang; Dai, Youzhi; Honore Ake, Kouassi Marius

    2015-01-01

    The advanced oxidation of Cartap hydrochloride (Cartap) promoted by the Fenton system in an aqueous medium was investigated. Based on total organic carbon, chemical oxygen demand and high-performance liquid chromatography, the oxidation of Cartap is quite efficient by the Fenton system. Its long chain is easily destroyed, but the reaction does not proceed to complete mineralization. Ion chromatography detection indicated the formation of acetic acid, propionic acid, formic acid, nitrous acid and sulfuric acid in the reaction mixtures. Further evidence of nitrogen monoxide and sulfur dioxide formation was obtained by using a flue gas analyzer. Monitoring by gas chromatograph-mass spectrometer demonstrated the formation of oxalic acid, ethanol, carbon dioxide, and L-alanine ethylamide. Based on these experimental results, plausible degradation pathways for Cartap mineralization in an aqueous medium by the Fenton system are proposed.

  6. Stability-Indicating RP-HPLC Method for Determination of Guanfacine Hydrochloride in Bulk Drugs and in Pharmaceutical Dosage Form

    Directory of Open Access Journals (Sweden)

    Vinod K. Ahirrao

    2011-04-01

    Full Text Available A novel stability-indicating RP-HPLC method was developed and validated for quantitative determination of guanfacine hydrochloride in bulk drug and in pharmaceutical dosage form. An isocratic, reversed phase HPLC method was developed to separate the drug from the degradation products, using Apollo, C18 (250mm x 4.6mm, 5µm column with mobile phase of 50mM Ammonium acetate (volatile buffer and acetonitrile (65:35, v/v. UV detection has been done at wavelength 220 nm. The guanfacine hydrochloride was subjected to the stress conditions of hydrolysis (acid, base, oxidation, photolysis and thermal degradation. The stressed samples were analyzed by the proposed method. The analyte peak shape was excellent. The described method shows excellent linearity over a range of 30 – 450 µg/mL. The correlation coefficient for guanfacine hydrochloride was 0.999. The limit of detection for Guanfacine hydrochloride is 0.011 µg/mL and the limit of quantification is 0.038 µg/mL respectively.Degradation was observed for guanfacine hydrochloride in base, thermal and in 30% H2O2 conditions. The drug was found to be stable in the other stress conditions attempted. The degradation products were well resolved from main peak. The percentage recovery of guanfacine hydrochloride was ranged from (99.2% to 100.5% in pharmaceutical dosage form. The developed method was validated with respect to the linearity, accuracy (recovery, precision, specificity and robustness. The forced degradation studies prove the stability indicating power of the method.

  7. 21 CFR 520.1660b - Oxytetracycline hydrochloride capsules.

    Science.gov (United States)

    2010-04-01

    ... 21 Food and Drugs 6 2010-04-01 2010-04-01 false Oxytetracycline hydrochloride capsules. 520.1660b Section 520.1660b Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES... Oxytetracycline hydrochloride capsules. (a) Specifications. The drug is in capsule form with each capsule...

  8. 21 CFR 520.2345a - Tetracycline hydrochloride capsules.

    Science.gov (United States)

    2010-04-01

    ... 21 Food and Drugs 6 2010-04-01 2010-04-01 false Tetracycline hydrochloride capsules. 520.2345a... Tetracycline hydrochloride capsules. (a) Specifications. Each capsule contains 50, 100, 125, 250, or 500... as in paragraph (c) of this section: (1) No. 000009: 250 mg per capsule. (2) No. 000069: 125, 250, or...

  9. 21 CFR 520.1242f - Levamisole hydrochloride gel.

    Science.gov (United States)

    2010-04-01

    ... 21 Food and Drugs 6 2010-04-01 2010-04-01 false Levamisole hydrochloride gel. 520.1242f Section 520.1242f Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES... Levamisole hydrochloride gel. (a) Specifications. The drug is a gel containing 11.5 percent...

  10. 21 CFR 520.1242 - Levamisole hydrochloride oral dosage forms.

    Science.gov (United States)

    2010-04-01

    ... 21 Food and Drugs 6 2010-04-01 2010-04-01 false Levamisole hydrochloride oral dosage forms. 520.1242 Section 520.1242 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL DRUGS, FEEDS, AND RELATED PRODUCTS ORAL DOSAGE FORM NEW ANIMAL DRUGS § 520.1242 Levamisole hydrochloride oral dosage...

  11. 21 CFR 520.1242e - Levamisole hydrochloride effervescent tablets.

    Science.gov (United States)

    2010-04-01

    ... 21 Food and Drugs 6 2010-04-01 2010-04-01 false Levamisole hydrochloride effervescent tablets. 520.1242e Section 520.1242e Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL DRUGS, FEEDS, AND RELATED PRODUCTS ORAL DOSAGE FORM NEW ANIMAL DRUGS § 520.1242e Levamisole hydrochloride...

  12. 21 CFR 522.1222 - Ketamine hydrochloride injectable dosage forms.

    Science.gov (United States)

    2010-04-01

    ... 21 Food and Drugs 6 2010-04-01 2010-04-01 false Ketamine hydrochloride injectable dosage forms. 522.1222 Section 522.1222 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN... ANIMAL DRUGS § 522.1222 Ketamine hydrochloride injectable dosage forms. ...

  13. Vibrational spectra of pilocarpine hydrochloride crystals

    Energy Technology Data Exchange (ETDEWEB)

    Bento, R.R.F. [Universidade Federal de Mato Grosso (UFMT), Cuiaba, MT (Brazil). Inst. de Fisica; Freire, P.T.C. [Universidade Federal do Ceara (UFC), Fortaleza, CE (Brazil). Dept. de Fisica]. E-mail: tarso@fisica.ufc.br; Teixeira, A.M.R.; Silva, J.H. [Universidade Regional do Cariri, Crato, CE (Brazil). Dept. Ciencias Fisicas e Biologicas; Lima Junior, J.A. [Universidade Estadual do Ceara (UECE), Limoeiro do Norte, CE (Brazil); Oliveira, M.C.F. de; Andrade-Neto, M. [Universidade Federal do Ceara (UFC), Fortaleza, CE (Brazil). Dept. de Quimica Organica e Inorganica; Romero, N.R. [Universidade Federal do Ceara (UFC), Fortaleza, CE (Brazil). Dept. de Farmacia; Pontes, F.M. [Universidade Estadual Paulista, Bauru, SP (Brazil). Faculdade de Ciencias

    2009-03-15

    Pilocarpine is a natural substance with potential application in the treatment of several diseases. In this work Fourier Transform (FT)-Raman spectrum and the Fourier Transform infra red (FT-IR) spectrum of pilocarpine hydrochloride C{sub 11} H{sub 17} N{sub 2} O{sup +}{sub 2} .Cl{sup -1} were investigated at 300 K. Vibrational wavenumber and wave vector have been predicted using density functional theory (B3LYP) calculations with the 6-31 G(d,p) basis set. A comparison with experiment allowed to assign most of the normal modes of the crystal. (author)

  14. Fractionated PDT with 5-aminolevulinic acid: effective, cost effective, and patient friendly

    Science.gov (United States)

    de Vijlder, Hannah C.; Middelburg, Tom A.; de Bruijn, Henriette S.; Robinson, Dominic J.; Neumann, H. A. Martino; de Haas, Ellen R. M.

    2009-06-01

    PDT with ALA and MAL is established as a relatively effective treatment for non-melanoma skin cancer and premalignancies. PDT is often repeated, because a single treatment gives poor long term results. Preclinical studies showed that ALA-PDT applying a fractionated illumination scheme with a small first light fraction and a second larger light fraction separated by a dark interval of two hours resulted in a significant increase in efficacy. Whereas the efficacy was not enhanced by fractionating MAL-PDT, indicating that ALA-PDT mechanism is not the same as MAL-PDT mechanism. The increase in efficacy using fractionated PDT was confirmed clinically. A randomized comparative clinical study comparing fractionated ALA-PDT versus non-fractionated ALA-PDT in the treatment of superficial basal cell carcinoma showed a significant higher response rate in the lesions treated with fractionated ALA-PDT after a follow-up of one year ( pMAL-PDT treatments separated by one week), both reducing direct and indirect costs and the burden to the patient.

  15. Raman spectroscopy of bladder tissue in the presence of 5-aminolevulinic acid

    NARCIS (Netherlands)

    Grimbergen, M. C. M.; van Swol, C. F. P.; van Moorselaar, Rj. A.; Uff, J.; Mahadevan-Jansen, A.; Stone, N.

    2009-01-01

    Raman spectroscopy has the ability to provide differential diagnosis of different cancers with high sensitivity and specificity. A major limitation in its clinical application is the weak nature of Raman signal, which inhibits scanning large surface areas of tissues. In bladder cancer diagnosis, flu

  16. OPTIMIZATIONS FOR 5-AMINOLEVULINIC ACID BASED PHOTODYNAMIC THERAPY IN PURGING LEUKEMIA CELL HL60

    Institute of Scientific and Technical Information of China (English)

    2005-01-01

    Photodynamictherapy(PDT),whichinvolves administrationofatumorlocalizing photosensiti zingagentthatmayrequiremetabolizingsynthesis(i.e.,aprodrug),followedbyactivationofthea gentbylightofaspecificwavelength.Thistherapy resultsinasequenceofphotochemicalandphotobio logicprocessthatcausesirreversiblephotodamageto tumortissue.SeveralphotosensitizersinPDThavesofar beenappliedtoeradicateresidualtumorcellsinau tograftsandtoreducecontaminationoftumorcells inhemopathy[1-3].However,alltheexogenous photosensitizershavea...

  17. Effects of 5-aminolevulinic acid-mediated sonodynamic therapy on macrophages

    OpenAIRE

    Cheng J; Sun X; Guo S; Chen H.; Jin Y; Li B; Li Q; Wang H; Wang Z.; Zhou Q; Wang P; Zhang Z; Cao W.; Tian Y

    2013-01-01

    Jiali Cheng,1,* Xin Sun,1,2,* Shuyuan Guo,1,* Wei Cao,1 Haibo Chen,1 Yinghua Jin,1 Bo Li,1 Qiannan Li,1 Huan Wang,1 Zhu Wang,3 Qi Zhou,3 Peng Wang,3 Zhiguo Zhang,3 Wenwu Cao,3,4 Ye Tian1,21Division of Cardiology, the First Affiliated Hospital, Cardiovascular Institute, Harbin Medical University, Harbin, People’s Republic of China; 2Division of Pathophysiology, the State-Province Key Laboratories of Biomedicine-Pharmaceutics of China, Key Laboratory of Cardiovascular Research, Minist...

  18. Increased brain edema following 5-aminolevulinic acid mediated photodynamic in normal and tumor bearing rats

    Science.gov (United States)

    Hirschberg, Henry; Angell-Petersen, Even; Spetalen, Signe; Mathews, Marlon; Madsen, Steen J.

    2007-02-01

    Introduction: Failure of treatment for high grade gliomas is usually due to local recurrence at the site of surgical resection indicating that a more aggressive form of local therapy, such as PDT, could be of benefit. PDT causes damage to both tumor cells as well as cerebral blood vessels leading to degradation of the blood brain barrier with subsequent increase of brain edema. The increase in brain edema following ALA-PDT was evaluated in terms of animal survival, histopatological changes in normal brain and tumor tissue and MRI scanning. The effect of steroid treatment, to reduce post-treatment PDT induced edema, was also examined. Methods:Tumors were established in the brains of inbred BD-IX and Fisher rats. At various times following tumor induction the animals were injected with ALA ip. and four hours later light treatment at escalating fluences and fluence rates were given. Nontumor bearing control animals were also exposed to ALA-PDT in a similar manner to evaluate damage to normal brain and degree of blood brain barrier (BBB) disruption. Results: Despite a very low level of PpIX production in normal brain, with a 200:1 tumor to normal tissue selectivity ratio measured at a distance of 2 mm from the tumor border, many animals succumbed shortly after treatment. A total radiant energy of 54 J to non-tumor bearing animals resulted in 50% mortality within 5 days of treatment. Treatment of tumor bearing animals with moderate fluence levels produced similar brain edema compared to higher fluence levels. ALA PDT in nontumor bearing animals produced edema that was light dose dependent. PDT appeared to open the BBB for a period of 24-48 hrs after which it was restored. The addition of post operative steroid treatment reduced the incident of post treatment morbidity and mortality. Conclusions: T2 and contrast enhanced T1 MRI scanning proved to be a highly effective and non-evasive modality in following the development of the edema reaction and the degree and time course of BBB dysfunction thus allowing the use of fewer animals.

  19. Ultraviolet spectrophotometric method for analytical determination of mianserin hydrochloride in coated tablets and comparison with LC

    Directory of Open Access Journals (Sweden)

    Letícia Lenz Sfair

    2015-12-01

    Full Text Available abstract Ultraviolet spectrophotometric (UV and Liquid Chromatographic (LC methods for the determination of mianserin hydrochloride in pharmaceutical formulation were developed and validated. The various parameters, such as specificity, linearity, precision and accuracy were studied according to International Conference on Harmonization (ICH, 2005. For UV method, mianserin hydrochloride was determinate at 278 nm using HCl 0.1 M as the solvent. The response was linear in the concentration range of 20.0 - 140.0 µg/mL (r = 0.9998. Precision data evaluated by relative standard deviation was lower than 2%. The UV method was simple, rapid and low cost. Chromatographic analyses were performed in an Ace C18 column and the mobile phase was composed of methanol, 50 mM monobasic potassium phosphate buffer and 0.3% triethylamine solution adjusted to pH 7.0 with phosphoric acid 10% (85:15. LC method was specific, linear, precise, exact and robust. The results confirmed that the both methods are valid and useful to the routine quality control of mianserin hydrochloride in coated tablets. Statistical analysis by Student´s t-test showed no significant difference between the results obtained by UV and LC methods.

  20. The relation between methyl aminolevulinate concentration and inflammation after photodynamic therapy in healthy volunteers

    DEFF Research Database (Denmark)

    Fabricius, Susanne; Lerche, Catharina Margrethe; Philipsen, Peter Alshede;

    2013-01-01

    Inflammation and pain are well known adverse-effects in photodynamic therapy (PDT). There is currently a tendency towards introducing lower concentrations of the photosensitizer than used in the standard treatment for various indications. The aim of this study was to investigate whether reduced...... concentrations of methyl aminolevulinate (MAL) can reduce inflammation (erythema) during PDT treatment. We measured the formation of protoporphyrin IX (PpIX) using fluorescence and monitored both erythema and pain during and after PDT treatment with conventional 16% MAL and threee reduced concentrations of 2, 0.......75, and 0.25% in twenty-four healthy volunteers. We found that lowering the MAL concentration reduced PpIX fluorescence and erythema after PDT treatment. There was a strong correlation (R(2) = 0.70) between the PpIX fluorescence and erythema after treatment. A further increase in erythema after PDT...

  1. Daylight photodynamic therapy with methyl-aminolevulinate for the treatment of actinic cheilitis.

    Science.gov (United States)

    Fai, Dario; Romanello, Eugenio; Brumana, Marta Benedetta; Fai, Carlotta; Vena, Gino Antonio; Cassano, Nicoletta; Piaserico, Stefano

    2015-01-01

    Actinic cheilitis (AC) is a common premalignant condition that requires an effective treatment to reduce the risk of malignant transformation. Photodynamic therapy (PDT) has been recently added to the armamentarium available for AC treatment. Daylight PDT (D-PDT) is a novel PDT modality in which the activation of the topical photosensitizer is induced by the exposure to natural daylight instead of artificial light sources without preliminary occlusion. This simplified procedure was found to be more tolerated as compared to conventional PDT. We report our preliminary experience on the use of D-PDT using methyl-aminolevulinate cream in 10 patients with refractory AC of the lower lip. Patients received two consecutive D-PDT sessions with an interval of 7-14 days. At 3 months after therapy, a complete response was observed in seven patients, with sustained results in five patients over an observational period of 6-12 months. Treatment was well tolerated.

  2. [Neuropharmacological studies on tolperisone hydrochloride (author's transl)].

    Science.gov (United States)

    Fujii, Y; Ishii, Y; Suzuki, T; Murayama, S

    1979-10-01

    Neuropharmacological properties of tolperisone hydrochloride (2,4'-dimethyl-3-piperidinopropiophenone hydrochloride) were investigated in mice, rats and cats. Tolperisone inhibited the spontaneous movement and methamphetamine-induced hyperactivity in mice and the ED50 was approx. 50 mg/kg, s.c. At this dose, tolperisone did not prolong the pentobarbital-induced sleeping time. Tolperisone inhibited convulsions induced by pentylenetetrazol, nicotine and maximum electric shock, but did not affect convulsions induced by strychnine and picrotoxin. Tolperisone induced muscle relaxation in mice and rats in several pharmacological tests, but did not affect neuro-muscular transmission. Tolperisone did not affect conditioned avoidance response in rats and methamphetamine-induced rotational behaviour in nigro-lesioned rats. Tolperisone reduced decerebrated rigidity in cats with i.v. administration of 5 approximately 10 mg/kg and intraduodenal administration of 50 approximately 100 mg/kg. Tolperisone elicited a slight drowsy pattern in the spontaneous EEG of cats at 5 approximately 10 mg/kg, i.v., and inhibited the EEG arousal response and pressor response to stimulation of mesencephalic reticular formation or posterior hypothalamic area. These results suggest that inhibition of the activity in the gamma pathway descending from the mesencephalic reticular formation may be involved in the mechanism of muscle relaxant action of tolperisone.

  3. Responses to hexyl 5-aminolevulinate-induced photodynamic treatment in rat bladder cancer model

    Science.gov (United States)

    Arum, Carl-Jørgen; Gederas, Odrun; Larsen, Eivind; Randeberg, Lise; Zhao, Chun-Mei

    2010-02-01

    OBJECTIVES: In this study, we evaluated histologically the effects of hexyl 5-aminolevulinateinduced photodynamic treatment in the AY-27 tumor cell induced rat bladder cancer model. MATERIAL & METHODS: The animals (fischer-344 female rats) were divided into 2 groups, half of which were orthotopically implanted with 400,000 syngeniec AY-27 urothelia1 rat bladder cancer cells and half sham implanted. 14 days post implantation 6 rats from each group were treated with hexyl 5-aminolevulinate-induced photodynamic treatment (8mM HAL and light fluence of 20 J/cm2). Additional groups of animals were only given HAL instillation, only light treatment, or no treatment. All animals were sacrificed 7 days after the PDT/only HAL/only light or no treatment. Each bladder was removed, embedded in paraffin and stained with hematoxylin, eosin, and saferin for histological evaluation at high magnification for features of tissue damage by a pathologist blinded to the sample source. RESULTS: In all animals that were AY-27 implanted and not given complete PDT treatment, viable tumors were found in the bladder mucosa and wall. In the animals treated with complete HAL-PDT only 3 of 6 animals had viable tumor. In the 3 animals with viable tumor it was significantly reduced in volume compared to the untreated animals. It was also noted that in the PDT treated animals there was a significantly increased inflammatory response (lymphocytic and mononuclear cell infiltration) in the peri-tumor area compared to implanted animals without complete HAL-PDT. CONCLUSION: Our results suggest that hexyl 5-aminolevulinate-induced photodynamic treatment in a rat bladder cancer model involves both direct effects on cell death (necrosis and apoptosis) and indirect effects to evoke the host immune-response, together contributing to tumor eradication.

  4. Stability studies of lincomycin hydrochloride in aqueous solution and intravenous infusion fluids

    Directory of Open Access Journals (Sweden)

    Czarniak P

    2016-03-01

    Full Text Available Petra Czarniak, Michael Boddy, Bruce Sunderland, Jeff D Hughes School of Pharmacy, Curtin University, Perth, WA, Australia Purpose: The purpose of this study was to evaluate the chemical stability of Lincocin® (lincomycin hydrochloride in commonly used intravenous fluids at room temperature (25°C, at accelerated-degradation temperatures and in selected buffer solutions.Materials and methods: The stability of Lincocin® injection (containing lincomycin 600 mg/2 mL as the hydrochloride stored at 25°C±0.1°C in sodium lactate (Hartmann’s, 0.9% sodium chloride, 5% glucose, and 10% glucose solutions was investigated over 31 days. Forced degradation of Lincocin® in hydrochloric acid, sodium hydroxide, and hydrogen peroxide was performed at 60°C. The effect of pH on the degradation rate of lincomycin hydrochloride stored at 80°C was determined.Results: Lincomycin hydrochloride was found to maintain its shelf life at 25°C in sodium lactate (Hartmann’s solution, 0.9% sodium chloride solution, 5% glucose solution, and 10% glucose solution, with less than 5% lincomycin degradation occurring in all intravenous solutions over a 31-day period. Lincomycin hydrochloride showed less rapid degradation at 60°C in acid than in basic solution, but degraded rapidly in hydrogen peroxide. At all pH values tested, lincomycin followed first-order kinetics. It had the greatest stability near pH 4 when stored at 80°C (calculated shelf life of 4.59 days, and was least stable at pH 2 (calculated shelf life of 0.38 days.Conclusion: Lincocin® injection was chemically found to have a shelf life of at least 31 days at 25°C when added to sodium lactate (Hartmann’s solution, 0.9% sodium chloride solution, 5% glucose solution, and 10% glucose solution. Solutions prepared at approximately pH 4 are likely to have optimum stability. Keywords: lincomycin, stability, pH, intravenous fluids, IV additives

  5. Identification of polymorphism in ethylone hydrochloride: synthesis and characterization.

    Science.gov (United States)

    Maheux, Chad R; Alarcon, Idralyn Q; Copeland, Catherine R; Cameron, T Stanley; Linden, Anthony; Grossert, J Stuart

    2016-08-01

    Ethylone, a synthetic cathinone with psychoactive properties, is a designer drug which has appeared on the recreational drug market in recent years. Since 2012, illicit shipments of ethylone hydrochloride have been intercepted with increasing frequency at the Canadian border. Analysis has revealed that ethylone hydrochloride exists as two distinct polymorphs. In addition, several minor impurities were detected in some seized exhibits. In this study, the two conformational polymorphs of ethylone hydrochloride have been synthesized and fully characterized by FTIR, FT-Raman, powder XRD, GC-MS, ESI-MS/MS and NMR ((13) C CPMAS, (1) H, (13) C). The two polymorphs can be distinguished by vibrational spectroscopy, solid-state nuclear magnetic resonance spectroscopy and X-ray diffraction. The FTIR data are applied to the identification of both polymorphs of ethylone hydrochloride (mixed with methylone hydrochloride) in a laboratory submission labelled as 'Ocean Snow Ultra'. The data presented in this study will assist forensic scientists in the differentiation of the two ethylone hydrochloride polymorphs. This report, alongside our recent article on the single crystal X-ray structure of a second polymorph of this synthetic cathinone, is the first to confirm polymorphism in ethylone hydrochloride. © 2015 Canada Border Services Agency. Drug Testing and Analysis published by John Wiley & Sons, Ltd. © 2015 Canada Border Services Agency. Drug Testing and Analysis published by John Wiley & Sons, Ltd.

  6. SIMULTANEOUS ESTIMATION AND VALIDATION OF VARDENAFIL AND DAPOXETINE HYDROCHLORIDE IN PHARMACEUTICAL FORMULATION BY THIN LAYER CHROMATOGRAPHIC DENSITOMETRIC METHOD

    Directory of Open Access Journals (Sweden)

    Bhavin Chapla

    2012-05-01

    Full Text Available The present manuscript describes new, simple, accurate, and precise high performance thin layer chromatography method for the simultaneous determination of Vardenafil and Dapoxetine in combined tablet dosage form. Chromatographic separation of the drugs was performed on aluminium plates pre coated with silica gel 60 F254 as the stationary phase and the solvent system consisted of Chloroform: Methanol: Acetonitrile: Formic acid (4: 0.8: 4: 1 v/v/v/v. Densitometric evaluation of the separated zones was performed at 232 nm. The two drugs were satisfactorily resolved with Rf values 0.47 and 0.79 for Vardenafil and Dapoxetine Hydrochloride, respectively. The linear regression data for the calibration plots showed good relationship with r2 = 0.9995 from 150-750 ng/spot for Vardenafil and r2 = 0.9980 from 450-2250 ng/spot for Dapoxetine Hydrochloride. The methods were validated for precision, accuracy, and recovery. The percentage recovery for Vardenafil was found to be 99.58 – 100.72 % and 99.97 – 100.21% for Dapoxetine Hydrochloride. The limits of detection and quantification were 21.86 and 66.25 ng/spot per spot for Vardenafil and 128.58. and 389.64 ng/spot per spot for Dapoxetine Hydrochloride, respectively.

  7. Capillary electrophoresis coupled with electrochemiluminescence for determination of cloperastine hydrochloride

    Institute of Scientific and Technical Information of China (English)

    2008-01-01

    Objective To investigate the electrochemiluminescence (ECL) behavior of cloperastine hydrochloride. Methods ECL intensity of tris (2,2′-bipyridyl) rutheniumo(Ⅱ) was enhanced, the method for the determination of cloperastine hydrochloride was established using capillary electrophoresis (CE) coupled with electrochemilumolinescence (ECL) detection. Results Under the optimum conditions, ECL intensity varied linearly with cloperastine hydrochloride concentration from 7.0×10-6g/mL to 1.0×10-4g/mL. The detection l...

  8. COMPARISON OF DROTAVERINE HYDROCHLORIDE AND VALETHAMATE BROMIDE ON CERVICAL DILATATION

    Directory of Open Access Journals (Sweden)

    Mallika Selvaraj

    2016-06-01

    Full Text Available AIM To compare the two drugs drotaverine hydrochloride and valethamate bromide and their effects on cervical dilatation and labour duration. METHODOLOGY It is a prospective study undertaken at Government Rajaji Hospital on 150 randomly selected primigravidae patients. RESULTS The duration of active phase of first stage of labour was significantly reduced (p value 0.003, rate of cervical dilatation was higher (p value 0.0001 with drotaverine hydrochloride. CONCLUSION Drotaverine hydrochloride is a safe, potent and effective drug to be used in the active phase of labour.

  9. Leishmania spp: Delta-aminolevulinate-inducible neogenesis of porphyria by genetic complementation of incomplete heme biosynthesis pathway

    Science.gov (United States)

    Dutta, Sujoy; Furuyama, Kazumichi; Sassa, Shigeru; Chang, Kwang-Poo Chang

    2008-01-01

    To further develop the Leishmania model for porphyria based on their deficiencies in heme biosynthesis, three Old World species were doubly transfected as before for Leishmania amazonensis with cDNAs, encoding the 2nd and 3rd enzymes in the pathway. Expression of the transgenes was verified immunologically at the protein level and functionally by uroporphyrin neogenesis that occurs only after exposure of the double-transfectants to delta-aminolevulinate. All species examined were equally deficient in heme biosynthesis, as indicated by the accumulation of uroporphyrin as the sole porphyrin and the production of coproporphyrin upon further transfection of one representative species with the downstream gene. The results obtained thus demonstrate that at least the first five enzymes for heme biosynthesis are absent in all species examined, rendering their transfectants inducible with aminolevulinate to accumulate porphyrins and thus useful as cellular models for human porphyrias. PMID:18164705

  10. Magnetic resonance imaging study of the transport phenomena of solvent into the gel layer of hypromellose matrices containing tetracycline hydrochloride.

    Science.gov (United States)

    Tritt-Goc, Jadwiga; Kowalczuk, Joanna; Pislewski, Narcyz

    2003-11-01

    Magnetic resonance imaging was used to study the diffusion of a water solution of hydrochloric acid into hypromellose (hydroxypropylmethylcellulose) matrices. Spatially resolved information was obtained about the self-diffusion coefficient and spin-spin relaxation time of solvent protons in the gel layer of hypromellose matrices loaded with different amounts of tetracycline hydrochloride. The data showed the influence of the drug concentration on the diffusion and spin-spin relaxation. Higher drug concentrations in the hypromellose matrix led to greater swelling of the matrix and faster diffusion of the water molecules inside the gel layer of the polymer. The observed differences between the radial and axial diffusion were interpreted in terms of the stresses imposed in the axial direction during the compression of the samples. The spin-spin and diffusion profiles indicated that the diffusion of a water solution of hydrochloric acid into hypromellose, pure and loaded with different amounts of tetracycline hydrochloride, was characterized as a Case II mechanism.

  11. Lack of association of delta-aminolevulinate dehydratase polymorphisms with blood lead levels and hemoglobin in Romanian women from a lead-contaminated region.

    Science.gov (United States)

    Rabstein, Sylvia; Unfried, Klaus; Ranft, Ulrich; Illig, Thomas; Kolz, Melanie; Mambetova, Chinara; Vlad, Mariana; Roman, Cecilia; Weiss, Tobias; Becker, Doreen; Brüning, Thomas; Pesch, Beate

    2008-01-01

    As part of a project on environmental pollution, this study aimed to evaluate associations between blood lead (BPb) levels, hemoglobin (Hb) content, and single-nucleotide polymorphisms (SNPs) of delta-aminolevulinic acid dehydratase (ALAD) gene in 129 unrelated women from Romania. Five SNPs (rs1805313, rs2228083, rs1805312, rs1800435, rs1139488) were analyzed with respect to haplotype structure and impact on BPb levels and Hb content with proportional odds and analysis of covariance models. Combinations of SNPs were rare (16%). Low haplotype diversity was found with seven haplotypes. One rare haplotype implied the C allele of rs1800435, often referred to as the ALAD2 allele (frequency 8.6%). The putative risk genotype (CC) occurred in only one woman with BPb below 0.5 microg/dl. Median BPb was 4.8 microg/dl and differed markedly by community with a level of 12.5 microg/dl near a mining-spill region. Hb was regular (interquartile range 12.3-13.7 g/dl) and not correlated with BPb, although quantitatively lower in women living near the spill region. No significant associations were found for BPb or Hb with SNPs, haplotypes, or diplotypes. BPb levels were higher in this region than in populations from industrialized countries but without hematotoxic effects. An impact of ALAD2 on BPb or Hb was not seen in these women.

  12. 度洛西汀联合硫辛酸治疗糖尿病周围神经病变性疼痛的疗效观察%Therapeutic effect analysis of duloxetine hydrochloride combined with alpha-lipoic acid in treatment of diabetic peripheral neuropathic pain

    Institute of Scientific and Technical Information of China (English)

    沈柿芬; 郭道骝

    2016-01-01

    目的:探讨度洛西汀联合硫辛酸治疗糖尿病周围神经病变性疼痛的有效性及安全性。方法:将78例糖尿病周围神经病变性疼痛患者随机分为两组,西汀组口服度洛西汀,联合组口服度洛西汀和静脉滴注硫辛酸,比较两组疗效。结果:两组治疗后正中神经感觉传导速度(median nerve conduction velocity,MNCV)、腓总神经感觉传导速度(phil nerve conduction velocity,PNCV)、尺神经感觉传导速度(ulnar nerve conduction velocity,UNCV)均显著提高(P0.05);两组治疗前、治疗8周后胆固醇(TC)、甘油三酯(TG)、丙氨酸氨基转移酶(ALT)、门冬氨酸氨基转移酶(AST)、血肌酐(SCr)指标水平均无显著性变化(P>0.05)。结论:度洛西汀联合硫辛酸治疗糖尿病周围神经病变性疼痛,能有效改善患者神经功能,减轻疼痛症状,且安全可靠。%Objective:By comparing duloxetine combination with alpha-lipoic acid and duloxetine in the therapeutic effect of painful diabetic neuropathy, to explore the efficacy and safety of duloxetine combination with alpha-lipoic acid treatment on diabetic peripheral neuropathic pain (DPNP) is optimal.Methods:78 cases with painful diabetic neuropathy of type 2 diabetes were recruited from our department and randomly divided into two groups, which were duloxetine in combination with alpha-lipoic acid group and duloxetine treatment group.Results: Compared to baseline, median nerve sensory conduction velocity (MNCV), Phil nerve conduction velocity (PNCV) and ulnar nerve conduction velocity (UNCV) of both groups were better (P0.05). Before treatment, no statistically signiifcant differences were detected in total cholesterol (TC), triglycerides (TG), alanine aminotransferase (ALT), aspartate aminotransferase (AST), and serum creatinine (SCr) between two groups (P>0.05).Conclusion:Duloxetine hydrochloride combined with alpha-lipoic acid has a good

  13. 盐酸吡哆辛在石墨烯-碳纳米管/聚烟酸复合修饰电极上的电化学行为研究及其测定%Electrochemical Behavior and Determination of Pyridoxine Hydrochloride at Graphene-Carbon Nanotubes/Poly(nicotinic acid) Modified Electrode

    Institute of Scientific and Technical Information of China (English)

    何凤云; 俞静; 刘欢; 顾小燕; 唐鹏鹏; 周宏; 陈昌云; 陆国飞

    2014-01-01

    Graphene ( GN) and multiwalled carbon nanotubes ( MWCNT) composites were coated on glassy carbon electrode ( GCE ) and then poly ( nicotinic acid ) ( PNA ) was electrodeposited on the modified electrode. The electrochemical behavior of pyridoxine hydrochloride ( VB6 ) was investigated at the modified electrode by cyclic voltammetry ( CV ) and differential pulse voltammetry ( DPV ) . Results showed the oxidation current of VB6 at the GN-MWCNT/PNA/GCE was obviously larger than that at GCE, PNA/GCE and GN/MWCNT/GCE. The oxidation process of VB6 was an irreversible diffusion-controlled process involving one electron and two protons. The liner range between the peak current intensity of DPV and the concentration of VB6 was 0 . 05-200 μmol/L with a detection limit of 0 . 02 μmol/L ( S/N=3 ) . The modified electrode showed a good reproducibility with a relative standard deviation of 3 . 1% ( n=8 ) . The proposed method was applied to the analysis of vitamin B6 in vitamin B6 tablets and compound vitamin B tablets with recoveries between 96 . 1%-104 . 5%.%通过滴涂和电聚合的方法制备了石墨烯( GN)-多壁碳纳米管( MWCNTs)/聚烟酸( PNA)修饰玻碳电极。利用循环伏安法和差分脉冲伏安法考察了盐酸吡哆辛( VB6)在此修饰电极上的电化学行为和测定方法。结果表明,VB6在此修饰电极上有一明显的不可逆氧化峰(Epa=1.049 V),该电极与 GCE、PNA/GCE以及GN/MWCNT/GCE相比,VB6的氧化峰电流显著提高,电极反应为扩散控制的一电子两质子反应。利用差分脉冲伏安法对VB6进行测定,线性范围为0.05~200μmol/L,检出限为0.02μmol/L,相对平均偏差为3.1%(n=8)。本方法可用于测定VB6片和B族维生素片中的VB6含量测定,加标回收率为在96.1%~104.5%之间。

  14. Dyeing Characteristics of Chitosan Biguanidine Hydrochloride Treated Wool Fabrics

    Institute of Scientific and Technical Information of China (English)

    2010-01-01

    Chitosan biguanidine hydrochloride(CGH) has been synthesized by the guanidineylation reaction of chitosan with dicyandiamide.The structures of CGH were characterized by Fourier transform infrared spectroscopy and 13CNMR spectra.In this paper,we used citric acid(CA) as a crosslinking agent,mixed with CGH to perform a pad-drycure treatment on wool fabric to study reaction mechanism during crosslinking with the help of Fourier transform infrared spectroscopy(FT-IR) and scanning electron microscopy(SEM).Dyeing characteristics of CGH treated wool fabric was assessed.The effects of CGH concentration,curing temperature,dipping time,pH value on color yield of reactive dyes on wool fibres were investigated.Fastness properties of the modified wool fabric to laundering and crocking have also been discussed.Fourier transform infrared spectroscopy(FT-IR) showed that CA produce esterification with the-OH group of the wool and transamidation with the-NH2 group of the CGH to form a crosslink.Scanning electron microscopy(SEM) analysis showed the CGH firmly attached to the surface of wool fibre.It was found that the CGH pretreated wool fabrics had significantly improved dyeability characteristics.It is worthwhile to mention that the CGH treated samples have antibacterial potential due to the antibacterial property of chitosan molecules and guanidinium salts.

  15. DESIGN OF GASTRO RETENTIVE DRUG DELIVERY SYSTEM OF DILTIAZEM HYDROCHLORIDE

    Directory of Open Access Journals (Sweden)

    L. K. Omray

    2014-02-01

    Full Text Available Gastro retentive drug delivery system of diltiazem hydrochloride was designed and evaluated for its effectiveness for the management of mild to moderate hypertension. Gastro retentive drug delivery system were prepared using polyvinyl alcohol and sodium carboxy methyl cellulose as the polymers and sodium bicarbonate as a gas generating agent for the reduction of floating lag time. Gastro retentive drug delivery system tablets were prepared by wet granulation method by compression in tablet compression machine. Formulations DL1, DL2, DL3, DL4 and DL5 were developed which differed in the ratio of polyvinyl alcohol and sodium carboxy methyl cellulose polymers. All the formulations were evaluated for hardness, weight variation, friability, drug content, swelling index, buoyancy studies and in vitro drug release study. In vitro drug release study was performed using United State Pharmacopoeia 23 type 2 dissolution test apparatus employing paddle stirrer at 50 r/pm. Dissolution medium was 900 ml of 0.1N hydrochloric acid at 37ºC ± 3ºC. Formulations DL3 was found to be better as compared to other formulation.

  16. Development and evaluation of microporous osmotic tablets of diltiazem hydrochloride.

    Science.gov (United States)

    Bathool, Afifa; Gowda, D V; Khan, Mohammed S; Ahmed, Ayaz; Vasudha, S L; Rohitash, K

    2012-04-01

    Microporous osmotic tablet of diltiazem hydrochloride was developed for colon targeting. These prepared microporous osmotic pump tablet did not require laser drilling to deliver the drug to the specific site of action. The tablets were prepared by wet granulation method. The prepared tablets were coated with microporous semipermeable membrane and enteric polymer using conventional pan coating process. The incorporation of sodium lauryl sulfate (SLS), a leachable pore-forming agent, could form in situ delivery pores while coming in contact with gastrointestinal medium. The effect of formulation variables was studied by changing the amounts of sodium alginate and NaCMC in the tablet core, osmogen, and that of pore-forming agent (SLS) used in the semipermeable coating. As the amount of hydrophilic polymers increased, drug release rate prolonged. It was found that drug release was increased as the concentration of osmogen and pore-former was increased. Fourier transform infrared spectroscopy and Differential scanning calorimetry results showed that there was no interaction between drug and polymers. Scanning electron microscopic studies showed the formation of pores after predetermined time of coming in contact with dissolution medium. The formation of pores was dependent on the amount of pore former used in the semipermeable membrane. in vitro results showed acid-resistant, timed release at an almost zero order up to 24 hours. The developed osmotic tablets could be effectively used for prolonged delivery of Diltiazem HCl.

  17. Development and evaluation of microporous osmotic tablets of diltiazem hydrochloride

    Directory of Open Access Journals (Sweden)

    Afifa Bathool

    2012-01-01

    Full Text Available Microporous osmotic tablet of diltiazem hydrochloride was developed for colon targeting. These prepared microporous osmotic pump tablet did not require laser drilling to deliver the drug to the specific site of action. The tablets were prepared by wet granulation method. The prepared tablets were coated with microporous semipermeable membrane and enteric polymer using conventional pan coating process. The incorporation of sodium lauryl sulfate (SLS, a leachable pore-forming agent, could form in situ delivery pores while coming in contact with gastrointestinal medium. The effect of formulation variables was studied by changing the amounts of sodium alginate and NaCMC in the tablet core, osmogen, and that of pore-forming agent (SLS used in the semipermeable coating. As the amount of hydrophilic polymers increased, drug release rate prolonged. It was found that drug release was increased as the concentration of osmogen and pore-former was increased. Fourier transform infrared spectroscopy and Differential scanning calorimetry results showed that there was no interaction between drug and polymers. Scanning electron microscopic studies showed the formation of pores after predetermined time of coming in contact with dissolution medium. The formation of pores was dependent on the amount of pore former used in the semipermeable membrane. in vitro results showed acid-resistant, timed release at an almost zero order up to 24 hours. The developed osmotic tablets could be effectively used for prolonged delivery of Diltiazem HCl.

  18. Spectrophotometric methods for the determination of ritodrine hydrochloride and its application to pharmaceutical preparations.

    Science.gov (United States)

    Revanasiddappa, H D; Manju, B

    2001-08-01

    Two simple and sensitive spectrophotometric methods are described for the determination of ritodrine hydrochloride (RTH) in both pure and dosage forms. The methods are based on the interaction of diazotised p-nitroaniline (DPNA) and sulphanilic acid (DSNA) with RTH in an alkaline medium. The resulting azo dyes are measured at 480 nm (for the DPNA method) and at 440 nm (for the DSNA method) and are stable for more than 1 h. The optimum reaction conditions and other analytical parameters are evaluated. A study of the effect of commonly associated excipients and additives do not interfere with the determinations. Statistical analysis of results indicates that the methods are precise and accurate.

  19. Distribution of non-tasters for phenylthiocarbamide and high sensitivity to quinine hydrochloride of the non-tasters in Japanese.

    Science.gov (United States)

    Sato, T; Okada, Y; Miyamoto, T; Fujiyama, R

    1997-10-01

    The percentage of non-tasters for phenylthiocarbamide in 915 Japanese students was 9.4%. The thresholds of the edge and back of the tongue to quinine hydrochloride were significantly smaller in the non-tasters than in the tasters. The thresholds of any tongue portions to NaCl, acetic acid or sucrose did not differ between the tasters and the non-tasters.

  20. UPLC and LC-MS studies on degradation behavior of irinotecan hydrochloride and development of a validated stability-indicating ultra-performance liquid chromatographic method for determination of irinotecan hydrochloride and its impurities in pharmaceutical dosage forms.

    Science.gov (United States)

    Kumar, Navneet; Sangeetha, Dhanaraj; Reddy, Sunil P

    2012-10-01

    The objective of the current investigation was to study the degradation behavior of irinotecan hydrochloride under different International Conference on Harmonization (ICH) recommended stress conditions using ultra-performance liquid chromatography and liquid chromatography-mass spectrometry and to establish a validated stability-indicating reverse-phase ultra-performance liquid chromatographic method for the quantitative determination of irinotecan hydrochloride and its seven impurities and degradation products in pharmaceutical dosage forms. Irinotecan hydrochloride was subjected to the stress conditions of oxidative, acid, base, hydrolytic, thermal and photolytic degradation. Irinotecan hydrochloride was found to degrade significantly in oxidative and base hydrolysis and photolytic degradation conditions. The degradation products were well resolved from the main peak and its impurities, thus proving the stability-indicating power of the method. Chromatographic separation was achieved on a Waters Acquity BEH C8 (100 × 2.1 mm) 1.7-µm column with a mobile phase containing a gradient mixture of solvent A (0.02M KH(2)PO(4) buffer, pH 3.4) and solvent B (a mixture of acetonitrile and methanol in the ratio of 62:38 v/v). The mobile phase was delivered at a flow rate of 0.3 mL/min with ultraviolet detection at 220 nm. The run time was 8 min, within which irinotecan and its seven impurities and degradation products were satisfactorily separated. The developed method was validated as per ICH guidelines with respect to specificity, linearity, limit of detection, limit of quantification, accuracy, precision and robustness. This method was also suitable for the assay determination of irinotecan hydrochloride in pharmaceutical dosage forms.

  1. A novel formulation for mebeverine hydrochloride.

    Science.gov (United States)

    Abdel-Hamid, Sameh M; Abdel-Hady, Seham E; El-Shamy, Abdel-Hamid A; El-Dessouky, Hadir F

    2007-10-01

    The antispasmodic drug mebeverine hydrochloride was formulated into a film-forming gel to be used as a topical local anesthetic. A mixture of cellulose derivatives was used as a base. Additives were used to enhance the release as well as the residence time. Formulations were characterized in terms of drug release, mucoadhesion and rheology. Clinically, the selected formula has shown faster onset (p = 0.0156), longer duration (p = 0.0313), better film residence (p = 0.0313), and no foreign body sensation (p = 0.0313) in comparison to Solcoseryl dental paste. Histopathological examination showed no change in inflammatory cells count, concluding that this topical anesthetic is efficacious and safe orally.

  2. Effect of sertraline hydrochloride on dialysis hypotension.

    Science.gov (United States)

    Dheenan, S; Venkatesan, J; Grubb, B P; Henrich, W L

    1998-04-01

    Hemodialysis hypotension (HH) is a very common disorder and has a multifactorial etiology. Autonomic dysfunction occurs in up to 50% of patients with end-stage renal disease (ESRD) and plays a key role in HH in some patients. Sertraline hydrochloride, a central nervous system serotonin reuptake inhibitor, has been shown to be an effective treatment of hypotension caused by autonomic dysfunction in disorders such as neurocardiogenic syncope and idiopathic orthostatic hypotension. This study sought to determine whether sertraline was effective in ameliorating HH. A retrospective chart analysis was performed that included nine consecutive patients (aged > or = 54 years, time on hemodialysis > or = 2.2 years) placed on sertraline (50 to 100 mg/d) for depression who also had HH (defined as prehemodialysis systolic blood pressure [SBP] or = 40 mm Hg decrease in SBP during hemodialysis, SBP sertraline. The data from a 6-week pre-sertraline period were compared with the data from a 6-week sertraline period (defined as 6 weeks after drug begun). Blood pressure medications were unchanged during the trial period of sertraline. However, nadir mean arterial pressure recorded during a given dialysis session in the pre-sertraline period (55+/-4 mm Hg) was significantly lower than that recorded in the sertraline period (68+/-5 mm Hg; P sertraline period was significantly lower than that during the pre-sertraline period (mean, 0.6+/-0.2 episodes per session v 1.4+/-0.3 episodes per session; P sertraline period was also significantly less than that during the pre-sertraline period (mean, 1.7+/-0.8 interventions v 11.0+/-3.0 interventions; P sertraline hydrochloride reduces HH in some patients with ESRD. A possible mechanism for this effect is sertraline-induced attenuation of the paradoxical sympathetic withdrawal that may underlie HH in some patients with ESRD.

  3. Dyeing Characteristics of Chitosan Biguanidine Hydrochloride Treated Wool Fabrics

    Institute of Scientific and Technical Information of China (English)

    ZHAO Xue; HE JIN-xin

    2010-01-01

    @@ Chitosan biguanidine hydrochloride(CGH)has been synthesized by the guanidineylation reaction of chitosan with dicyandiamide.The structures of CGH were characterized by Fourier transform infrared spectroscopy and 13CNMR spectra.

  4. Non-pigmented fixed drug eruption induced by eprazinone hydrochloride.

    Science.gov (United States)

    Tanabe, Kenichi; Tsuboi, Hiromi; Maejima, Hideki; Arai, Satoru; Katsuoka, Kensei

    2005-12-01

    A 68-year-old woman developed an upper respiratory tract infection in November 2002 and was treated with eprazinone hydrochloride, serrapeptase, carbocysteine and clarithromycin. Three days after the start of treatment, the patient noted erythema on her axilla, buttock and inguinal regions. The erythema subsided in 7 days although slight pigmentation remained. However, 7 days later the pigmentation completely disappeared. Oral eprazinone hydrochloride was given as a challenge, and 1 day later the erythema re-appeared in the same areas as on initial presentation (axilla, buttock, and inguinal regions). A fixed erythema without lasting pigmentation is attributed to eprazinone hydrochloride. Therefore, the patient was diagnosed as having a nonpigmented fixed drug eruption associated with eprazinone hydrochloride.

  5. Antifungal activity of hydrochloride salts of tylophorinidine and tylophorinine.

    Science.gov (United States)

    Dhiman, Mini; Parab, Rajashri R; Manju, Sreedharannair L; Desai, Dattatraya C; Mahajan, Girish B

    2012-09-01

    The antimicrobial efficacy of two phenanthroindolizidine alkaloids, tylophorinidine hydrochloride (TdnH) and tylophorinine hydrochloride (TnnH), isolated from the plant Tylophora indica (local name, Antamul) was evaluated. These were screened for in vitro antifungal and antibacterial activities. Both compounds exhibited potent antifungal activity displaying minimum inhibitory concentrations (MIC) in the range of 2-4 microg/mL for TdnH and 0.6-2.5 microg/mL for TnnH against Candida species.

  6. Treatment of allergic conjunctivitis with olopatadine hydrochloride eye drops

    OpenAIRE

    Eiichi Uchio

    2008-01-01

    Eiichi UchioDepartment of Ophthalmology, Fukuoka University School of Medicine, Fukuoka, JapanAbstract: Olopatadine hydrochloride exerts a wide range of pharmacological actions such as histamine H1 receptor antagonist action, chemical mediator suppressive action, and eosinophil infiltration suppressive action. Olopatadine hydrochloride 0.1% ophthalmic solution (Patanol®) was introduced to the market in Japan in October 2006. In a conjunctival allergen challenge (CAC) test, olopatadine...

  7. COMPARISON OF DROTAVERINE HYDROCHLORIDE AND VALETHAMATE BROMIDE ON CERVICAL DILATATION

    OpenAIRE

    Mallika Selvaraj; Sumathi

    2016-01-01

    AIM To compare the two drugs drotaverine hydrochloride and valethamate bromide and their effects on cervical dilatation and labour duration. METHODOLOGY It is a prospective study undertaken at Government Rajaji Hospital on 150 randomly selected primigravidae patients. RESULTS The duration of active phase of first stage of labour was significantly reduced (p value 0.003), rate of cervical dilatation was higher (p value 0.0001) with drotaverine hydrochloride. CONCLUS...

  8. Simultaneous Spectrophotometric Determination of Drotaverine Hydrochloride and Paracetamol in Tablet

    OpenAIRE

    Mahaparale Sonali; Telekone R; Raut R; Damle S; Kasture P

    2010-01-01

    Two simple, accurate and reproducible spectrophotometric methods; Q analysis and first order derivative method have been described for the simultaneous estimation of drotaverine hydrochloride and paracetamol in combined tablet dosage form. Absorption maxima of drotaverine hydrochloride and paracetamol in distilled water were found to be 303.5 nm and 243.5 nm respectively. Beer′s law was obeyed in the concentration range 5-50 µg/ml for drotaverine and 5-60 µg/ml for paracetamo...

  9. Development of LC Method for the Simultaneous Determination of Antidepressant Drug Combination Melitracen Hydrochloride and Flupentixol Dihydrochloride in their Combined Dosage Form

    Directory of Open Access Journals (Sweden)

    Usmangani K. Chhalotiya

    2011-01-01

    Full Text Available A simple, specific and stability-indicating reversed-phase high-performance liquid chromatographic method was developed for the simultaneous determination of melitracen hydrochloride and flupentixol dihydrochloride in tablet dosage form. A Brownlee C-18, 5 μm column having 250×4.6 mm i.d. in isocratic mode, with mobile phase containing 0.025 M potassium dihydrogen phosphate: methanol (10 : 90, v/v; pH 7.3 was used. The flow rate was 1.0 mL/min, and effluents were monitored at 230 nm. The retention times of melitracen hydrochloride and flupentixol dihydrochloride were 7.75 min and 5.50 min, respectively. The linearity for melitracen hydrochloride and flupentixol dihydrochloride were in the range of 0.5–60 μg/mL. The recoveries obtained for melitracen hydrochloride and flupenthixol dihydrochloride was 99.81–100.77% and 99.42–100.12%, respectively. Both the drugs were subjected to acid and alkali hydrolysis, chemical oxidation, and dry heat degradation and photodegradation. The proposed method was validated and successfully applied to the estimation of melitracen hydrochloride and flupentixol dihydrochloride in combined tablet dosage form.

  10. Development and Validation of a Stability-Indicating RP-UPLC Method for the Estimation of Impurities in Cinacalcet Hydrochloride API and its Formulation.

    Science.gov (United States)

    Sunil Reddy, Pingili; Raju, Thummala Veera Raghava; Raju, Penmetsa Satyanarayana; Varma, Nadimpalli Sunil; Babu, Kondra Sudhakar

    2015-01-01

    A sensitive, stability-indicating, gradient reversed-phase ultra-performance liquid chromatography method has been developed for the quantitative estimation of cinacalcet hydrochloride impurities in active pharmaceutical ingredients and pharmaceutical formulations. Efficient chromatographic separation was achieved on an Acquity BEH Shield RP18, 100 × 2.1 mm, 1.7 µm column with the mobile phase containing pH 6.6 phosphate buffer and acetonitrile. The flow rate of the mobile phase was 0.3 mL min(-1) with a column temperature of 35°C and detection wavelength at 223 nm. The relative response factor values of (+)-R-1-(1-Naphthyl)ethylamine, regioisomer, diastereomer isomer-1, and diastereomer isomer-2 were 1.79, 0.99, 0.89, and 0.88, respectively. The cinacalcet hydrochloride formulation sample was subjected to the stress conditions of acid, base, oxidative, hydrolytic, thermal, humidity, and photolytic degradation. Cinacalcet hydrochloride was found to degrade significantly under the peroxide stress conditions. The degradation products were well-resolved from cinacalcet hydrochloride and its impurities. The peak purity test results confirmed that the cinacalcet hydrochloride peak was homogenous in all stress samples and the mass balance was found to be more than 96%, thus proving the stability-indicating power of the method. The developed method was validated according to ICH guidelines.

  11. Preparation and Identification of Major Impurity A in Pyridoxine Hydrochloride%维生素B6中关键杂质A的制备与分析

    Institute of Scientific and Technical Information of China (English)

    徐勇智; 范卫东; 章根宝; 党登峰

    2011-01-01

    Impurity A in European pharmacopoeia for pyridoxine hydrochloride was synthesized from pyridoxine hydrochloride with the presence of sulfuric acid, and its structure was characterized by lH NMR, MS, FT-IR, HPLC. This study provides a convenient method to prepare impurity A reference substance, which can be used for quality control of pyridoxine hydrochloride.%以维生素B6为起始原料,在硫酸存在下合成了欧洲药典中的维生素B6杂质A,并通过1H NMR、MS、FT-IR、HPLC方法对其结构进行鉴定,为生产维生素B6质量控制提供了一种简便的杂质标准物制备方法.

  12. A Post Hoc Analysis of D-Threo-Methylphenidate Hydrochloride (Focalin) Versus D,l-Threo-Methylphenidate Hydrochloride (Ritalin)

    Science.gov (United States)

    Weiss, Margaret; Wasdell, Michael; Patin, John

    2004-01-01

    Objective: To evaluate clinical measures of the benefit/risk ratio in a post hoc analysis of a clinical trial of d-threo-methylphenidate hydrochloride (d-MPH) and d,l-threo-methylphenidate hydrochloride (d,l-MPH). Method: Data from a phase III clinical trial was used to compare equimolar doses of d-MPH and d,l-MPH treatment for…

  13. Simultaneous determination of nortriptyline hydrochloride and fluphenazine hydrochloride in microgram quantifies from low dosage forms by liquid chromatography-UV detection

    Institute of Scientific and Technical Information of China (English)

    Safwan Ashour; Nuha Kattan

    2012-01-01

    A novel method for the simultaneous high-performance liquid chromatographic determi- nation of nortriptyline hydrochloride and fluphenazine hydrochloride was developed and validated. Fhivastatin sodium was used as internal standard. The determination was performed on a Hypersil Gold Cs column (250 mm × 4.6 mm i.d., 5 μm particle size) at 25 ℃; the mobile phase, consisting of a mixture of formic acid (0.1 M, pH 2.16)-methanol (33:67, v/v), was delivered at a fow rate of 1.1 mL/min and detector wavelength at 251 rim. The retention time of nortriptyline, fluphenazine and fluvastatin was found to be 5.11, 8.05 and 11.38 min, respectively. Linearity ranges were 5.0-1350.0 and 10.0-1350.0 μg/ mL with limit of detection values of 0.72 and 0.31μg/mL, for nortriptyline and fluphenazine, respectively. Results of assay and recovery studies were statistically evaluated for its accuracy and precision. Correlation coefficients (r2) of the regression equations were greater than 0.999 in all cases. According to the validation results, the proposed method was found to be specific, accurate, precise and could be applied to the simultaneous quantitative analysis of nortriptyline and fluphenazine.

  14. Positive response of a recurrent keloid scar to topical methyl aminolevulinate-photodynamic therapy.

    Science.gov (United States)

    Nie, Zhuxiang; Bayat, Ardeshir; Behzad, Farhad; Rhodes, Lesley E

    2010-12-01

    A 36-year-old Caucasian female of Iranian origin presented with a persistently raised dermal lesion under her chin, confirmed histologically to be a keloid scar. There was a 4-year history of a negative response to a range of conventional treatments including topical silicone gel sheets, steroid creams, steroid injections and surgical excision. In view of treatment failure and an in vitro study indicating a positive effect of photodynamic therapy (PDT)on keloid fibroblasts, we treated our patient's lesion with five sessions of methyl aminolevulinate photodynamic therapy (MAL-PDT) over a period of 5 months. Following this treatment regime, her keloid scar had considerably reduced in size and become flattened.The surface of the keloid also became smooth, with attenuation in erythema at the margin as well as an improvement in the colour of the scar, which was better matched to the surrounding skin. There was no recurrence at 1-year follow-up and this treatment resulted in an overall acceptable cosmetic outcome. This case report presents PDT as a potential treatment option for persistent keloid lesions unresponsive to conventional scar modulation therapies and suggests a need for further research in this area.

  15. Acne treatment by methyl aminolevulinate photodynamic therapy with red light vs. intense pulsed light.

    Science.gov (United States)

    Hong, Jong Soo; Jung, Jae Yoon; Yoon, Ji Young; Suh, Dae Hun

    2013-05-01

    Various methods of photodynamic therapy (PDT) for acne have been introduced. However, comparative studies among them are still needed. We performed this study to compare the effect of methyl aminolevulinate (MAL) PDT for acne between red light and intense pulsed light (IPL). Twenty patients were enrolled in this eight-week, prospective, split-face study. We applied MAL cream over the whole face with a three-hour incubation time. Then patients were irradiated with 22 J/cm(2) of red light on one-half of the face and 8-10 J/cm(2) of IPL on the other half during each treatment session. We performed three treatment sessions at two-week intervals and followed-up patients until four weeks after the last session. Inflammatory and non-inflammatory acne lesions were reduced significantly on both sides. The red light side showed a better response than the IPL side after the first treatment. Serious adverse effects after treatment were not observed. MAL-PDT with red light and IPL are both an effective and safe modality in acne treatment. Red light showed a faster response time than IPL. After multiple sessions, both light sources demonstrated satisfactory results. We suggest that reducing the total dose of red light is desirable when performing MAL-PDT in Asian patients with acne compared with Caucasians.

  16. Aminolevulinate dehydrogenase polymorphisms did not modified lead serum and memory relationship

    Directory of Open Access Journals (Sweden)

    Lantip Rujito

    2012-12-01

    Full Text Available Background Lead accumulation in the blood widely known affecting the formation of heme and oxygen transport processes in vital organs, Leading to organ failure including the brain synapses. Lead affinity has been recognized influenced by constitutional genotype of aminolevulinate dehydrogenase (ALAD, which encodes for heme synthesis. This research aimed to determine the relationship between plumbum (Pb and short term memory on each ALAD gene genotyping (ALAD 1-1, ALAD 1-2 or ALAD 2-2 in gas station workers. Methods Seventy six probands from gas station workers were recruited to participate in this research. Each probands was carried out ALAD genotyping using polymerase chain reaction-restriction fragment length polymorphism (PCR-RFLP method, lead serum level using atomic absorbent spectrophotometer (AAS, and short term memory was measurement by intelligence structure test (IST. Results Proportion of d ALAD 1-1, 1-2, and 2-2 were 91.8%, 8.2% and 0% respectively. Lead serum showed 15.84 ppb in homozygous 1-1, and 20.79 ppb in heterozygous. Short term memory in the probands varied from 85 until 117, with average in 99.71. There was significant negative relationship between lead serum and short term memory (r=-0.24; p=0.038. However, we could not find any significant correlation in each d ALAD genotypes. Conclusion The d ALAD genotypes did not modified the relationship between serum lead level and short term memory in gas station workers.

  17. Identification of regulatory sequences in the gene for 5-aminolevulinate synthase from rat.

    Science.gov (United States)

    Braidotti, G; Borthwick, I A; May, B K

    1993-01-15

    The housekeeping enzyme 5-aminolevulinate synthase (ALAS) regulates the supply of heme for respiratory cytochromes. Here we report on the isolation of a genomic clone for the rat ALAS gene. The 5'-flanking region was fused to the chloramphenicol acetyltransferase gene and transient expression analysis revealed the presence of both positive and negative cis-acting sequences. Expression was substantially increased by the inclusion of the first intron located in the 5'-untranslated region. Sequence analysis of the promoter identified two elements at positions -59 and -88 bp with strong similarity to the binding site for nuclear respiratory factor 1 (NRF-1). Gel shift analysis revealed that both NRF-1 elements formed nucleoprotein complexes which could be abolished by an authentic NRF-1 oligomer. Mutagenesis of each NRF-1 motif in the ALAS promoter gave substantially lowered levels of chloramphenicol acetyltransferase expression, whereas mutagenesis of both NRF-1 motifs resulted in the almost complete loss of expression. These results establish that the NRF-1 motifs in the ALAS promoter are critical for promoter activity. NRF-1 binding sites have been identified in the promoters of several nuclear genes encoding mitochondrial proteins concerned with oxidative phosphorylation. The present studies suggest that NRF-1 may co-ordinate the supply of mitochondrial heme with the synthesis of respiratory cytochromes by regulating expression of ALAS. In erythroid cells, NRF-1 may be less important for controlling heme levels since an erythroid ALAS gene is strongly expressed and the promoter for this gene apparently lacks NRF-1 binding sites.

  18. Aminolevulinate dehydrogenase polymorphisms did not modified lead serum and memory relationship

    Directory of Open Access Journals (Sweden)

    Lantip Rujito

    2015-12-01

    Full Text Available BACKGROUND Lead accumulation in the blood widely known affecting the formation of heme and oxygen transport processes in vital organs, Leading to organ failure including the brain synapses. Lead affinity has been recognized influenced by constitutional genotype of aminolevulinate dehydrogenase (ALAD, which encodes for heme synthesis. This research aimed to determine the relationship between plumbum (Pb and short term memory on each ALAD gene genotyping (ALAD 1-1, ALAD 1-2 or ALAD 2-2 in gas station workers. METHODS Seventy six probands from gas station workers were recruited to participate in this research. Each probands was carried out ALAD genotyping using polymerase chain reaction-restriction fragment length polymorphism (PCRRFLP method, lead serum level using atomic absorbent spectrophotometer (AAS, and short term memory was measurement by intelligence structure test (IST. RESULTS Proportion of δ ALAD 1-1, 1-2, and 2-2 were 91.8%, 8.2% and 0% respectively. Lead serum showed 15.84 ppb in homozygous 1-1, and 20.79 ppb in heterozygous. Short term memory in the probands varied from 85 until 117, with average in 99.71. There was significant negative relationship between lead serum and short term memory (r=-0.24; p=0.038. However, we could not find any significant correlation in each δ ALAD genotypes. CONCLUSION The δ ALAD genotypes did not modified the relationship between serum lead level and short term memory in gas station workers.

  19. Liver δ-Aminolevulinate Dehydratase Activity is Inhibited by Neonicotinoids and Restored by Antioxidant Agents

    Directory of Open Access Journals (Sweden)

    Elisa Sauer

    2014-11-01

    Full Text Available Neonicotinoids represent the most used class of insecticides worldwide, and their precursor, imidacloprid, is the most widely marketed. The aim of this study was to evaluate the effect of imidacloprid on the activity of hepatic δ-aminolevulinate dehydratase (δ-ALA-D, protective effect of potential antioxidants against this potential effect and presence of chemical elements in the constitution of this pesticide. We observed that δ-ALA-D activity was significantly inhibited by imidacloprid at all concentrations tested in a dose-dependent manner. The IC50 value was obtained and used to evaluate the restoration of the enzymatic activity. δ-ALA-D inhibition was completely restored by addition of dithiotreitol (DTT and partly by ZnCl2, demonstrating that the inhibition occurs by oxidation of thiol groups and by displacement of the Zn (II, which can be explained by the presence of chemical elements found in the constitution of pesticides. Reduced glutathione (GSH had the best antioxidant effect against to δ-ALA-D inhibition caused by imidacloprid, followed by curcumin and resveratrol. It is well known that inhibition of the enzyme δ-ALA-D may result in accumulation of its neurotoxic substrate (δ-ALA, in this line, our results suggest that further studies are needed to investigate the possible neurotoxicity induced by neonicotinoids and the involvement of antioxidants in cases of poisoning by neonicotinoids.

  20. A SIMPLE AND-SENSITIVE STABILITY-INDICATING UHPLC-DAD METHOD FOR THE DETERMINATION OF CEFETAMET PIVOXIL HYDROCHLORIDE.

    Science.gov (United States)

    Garbacki, Piotr; Cielecka-Piontek, Judyta; Zalewski, Przemysław; Oszczapowicz, Irena; Jelińska, Anna

    2016-01-01

    A fast and sensitive UHPLC-DAD method was developed and subsequently validated for determination of cefetamet pivoxil hydrochloride in the presence of its degradation products. The chromatographic separation was carried out on a Waters Acquity BEH C18, (2.1 x 100 mm, 1.7 µm) column. The mobile phase was composed of 0.1% formic acid and acetonitrile (40 : 60, v/v) at the flow rate 0.7 mL/min. The detection wavelength was 265 nm and the temperature was 30 °C. Cefetamet pivoxil hydrochloride was susceptible to degradation under the influence of sodium hydroxide, hydrochloric acid and in the conditions of increased temperature and relative humidity. However, it was stable after irradiation, in increased temperature in dry air and in the presence of oxidizing agent. The developed UHPLC-DAD method was linear over the concentration range of 10-240 µg/mL (r2 = 0.9999; n = 12). The obtained RSD values were less than 2%, demonstrating that the described procedure is precise. The accuracy was also confirmed (mean recoveries were 97.79-102.08%). Under applied chromatographic conditions LOD and LOQ values were 2.08 mg/mL and 6.29 mg/mL, respectively. The proposed method was successfully applied in determination of cefetamet pivoxil hydrochloride in aqueous solutions as well as in the solid state.

  1. Development of duloxetine hydrochloride loaded mesoporous silica nanoparticles: characterizations and in vitro evaluation.

    Science.gov (United States)

    Ganesh, Mani; Ubaidulla, Udhumansha; Hemalatha, Pushparaj; Peng, Mei Mei; Jang, Hyun Tae

    2015-08-01

    This study investigated the potential use of mesoporous silica nanoparticles (MSNs) as a carrier for duloxetine hydrochloride (DX), which is prone to acid degradation. Sol-gel and solvothermal methods were used to synthesize the MSNs, which, after calcination and drug loading, were then characterized using X-ray diffraction (XRD), Brunauer-Emmett-Teller (BET) technique, thermogravimetric analysis (TGA), Fourier transform infrared (FT-IR) spectroscopy, scanning electron microscopy (SEM), differential scanning calorimetry (DSC), and diffuse reflectance ultraviolet-visible (DRS-UV-Vis) spectroscopy. Releases of DX from the MSNs were good in pH 7.4 (90%) phosphate buffer but poor in acidic pH (40%). In a comparative release study between the MSNs in phosphate buffer, TW60-3DX showed sustained release for 140 h, which was higher than the other nanoparticles. The mechanism of DX release from the MSNs was studied using Peppas kinetics model. The "n" value of all three MSNs ranged from 0.45 to 1 with a correlation coefficient (r (2)) >0.9, which indicated that the release of the drug from the system follows the anomalous transport or non-Fickian diffusion. The results supported the efficacy of mesoporous silica nanoparticles synthesized here as a promising carrier for duloxetine hydrochloride with higher drug loading and greater pH-sensitive release.

  2. In vitro evaluation of the stability of ranitidine hydrochloride in total parenteral nutrient mixtures.

    Science.gov (United States)

    Williams, M F; Hak, L J; Dukes, G

    1990-07-01

    The stability of ranitidine hydrochloride in various total parenteral nutrient (TPN) solutions was studied, as well as the effect of ranitidine on the stability of lipid emulsion and amino acids in these solutions. Ranitidine hydrochloride 25 mg/mL was added to each of the following mixtures to make final concentrations of approximately 50 and 100 mg/L: (1) TPN solution containing 4.5% amino acids, 22.7% dextrose, and electrolytes; (2) 10% lipid emulsion; (3) TPN solution containing 3.7% amino acids, 18.5% dextrose, 3.7% lipid emulsion, and electrolytes (all-in-one mixture); and (4) 0.9% sodium chloride injection. Mixtures were tested at room temperature and at 4 degrees C and were either protected from or exposed to fluorescent light. Sampling was done at 0, 12, 24, 36, and 48 hours, and the ranitidine concentration was determined by high-performance liquid chromatography. Samples were also analyzed for lipid particle size distribution and for amino acid content. At 48 hours, the all-in-one mixtures retained 86.0% to 91.4% of the initial ranitidine concentration. With one exception (ranitidine 50 mg/L in 0.9% sodium chloride injection, stored at room temperature and not protected from light), all other solutions retained at least 90% of the initial concentration at 48 hours. No visible changes in color and minimal changes in pH values were noted. There were no important changes in lipid particle-size distribution; 96% of all particles counted from any mixture were smaller than 1.44 microns in diameter at 48 hours. Ranitidine did not have an effect on amino acid concentrations in these mixtures.(ABSTRACT TRUNCATED AT 250 WORDS)

  3. Iontophoretic transdermal delivery of buspirone hydrochloride in hairless mouse skin.

    Science.gov (United States)

    Al-Khalili, Mohammad; Meidan, Victor M; Michniak, Bozena B

    2003-01-01

    The transdermal delivery of buspirone hydrochloride across hairless mouse skin and the combined effect of iontophoresis and terpene enhancers were evaluated in vitro using Franz diffusion cells. Iontophoretic delivery was optimized by evaluating the effect of drug concentration, current density, and pH of the vehicle solution. Increasing the current density from 0.05 to 0.1 mA/cm2 resulted in doubling of the iontophoretic flux of buspirone hydrochloride, while increasing drug concentration from 1% to 2% had no effect on flux. Using phosphate buffer to adjust the pH of the drug solution decreased the buspirone hydrochloride iontophoretic flux relative to water solutions. Incorporating buspirone hydrochloride into ethanol:water (50:50 vol/vol) based gel formulations using carboxymethylcellulose and hydroxypropylmethylcellulose had no effect on iontophoretic delivery. Incorporation of three terpene enhancers (menthol, cineole, and terpineol) into the gel resulted in a synergistic effect when combined with iontophoresis. Menthol was the most active enhancer, and when combined with iontophoresis it was possible to deliver 10 mg/cm2/day of buspirone hydrochloride.

  4. HPLC法测定馥感啉口服液中盐酸麻黄碱和盐酸伪麻黄碱的含量%Determination of Ephedrine Hydrochloride and Pseudoephedrine Hydrochloride in Fuganlin Oral Liquid by HPLC

    Institute of Scientific and Technical Information of China (English)

    曾永长; 张莉; 曾晓燕; 陈艺文

    2015-01-01

    目的:采用高效液相色谱法建立同时测定馥感啉口服液中盐酸麻黄碱和盐酸伪麻黄碱含量的检测方法。方法使用Phenomenex Synergi Polar-RP柱(250 mm×4.6 mm,4μm),以甲醇-0.092%磷酸溶液(含0.04%三乙胺和0.02%二正丁胺)(1.5∶98.5)为流动相,流速:1.0 mL·min-1,检测波长为210 nm。结果盐酸麻黄碱和盐酸伪麻黄碱在进样1~100μg·mL-1范围内线性关系良好,平均回收率(n=6)分别为97.43%(RSD=0.80%)、98.59%(RSD=1.77%)。结论该方法操作简便、分离度好、稳定可靠,可同时快速测定盐酸麻黄碱和盐酸伪麻黄碱,为馥感啉口服液的质量评价提供科学依据。%Objective To establish a HPLC method to determine the content of ephedrine hydrochloride and pseudoephedrine hydrochloride in Fuganlin oral liquid. Methods The chromatographic conditions was as follows:Phenomenex Synergi Polar-RP column(250 mm ×4.6 mm, 4 μm), methanol-0.092 % phosphoric acid solution (containing 0.04 % triethylamine and 0.02 % di-n-butylamine)(1.5∶98.5)as the mobile phase, flow rate being 1.0 mL ·min-1, detection wavelength set as 210 nm. Results The linear range of ephedrine hydrochloride and pseudoephedrine hydrochloride was 1~100 μg·mL-1,and the average recovery(n=6)was 97.43 % (RSD=0.80 %) and 98.59 %(RSD=1.77 %)respectively. Conclusion The method is simple,accurate and reliable,and can be used for the simultaneous determination of ephedrine hydrochloride and pseudoephedrine hydrochloride,which will provide a scientific basis for quality evaluation of Fuganlin oral liquid.

  5. Compatibility of cholecalciferol, haloperidol, imipramine hydrochloride, levodopa/carbidopa, lorazepam, minocycline hydrochloride, tacrolimus monohydrate, terbinafine, tramadol hydrochloride and valsartan in SyrSpend SF PH4 oral suspensions.

    Science.gov (United States)

    Polonini, H C; Silva, S L; Cunha, C N; Brandão, M A F; Ferreira, A O

    2016-04-01

    A challenge with compounding oral liquid formulations is the limited availability of data to support the physical, chemical and microbiological stability of the formulation. This poses a patient safety concern and a risk for medication errors. The objective of this study was to evaluate the compatibility of the following active pharmaceutical ingredients (APIs) in 10 oral suspensions, using SyrSpend SF PH4 (liquid) as the suspending vehicle: cholecalciferol 50,000 IU/mL, haloperidol 0.5 mg/mL, imipramine hydrochloride 5.0 mg/mL, levodopa/carbidopa 5.0/1.25 mg/mL, lorazepam 1.0 mg/mL, minocycline hydrochloride 10.0 mg/mL, tacrolimus monohydrate 1.0 mg/mL, terbinafine 25.0 mg/mL, tramadol hydrochloride 10.0 mg/mL and valsartan 4.0 mg/mL. The suspensions were stored both refrigerated (2 - 8 degrees C) and at controlled room temperature (20 - 25 degrees C). This is the first stability study for these APIs in SyrSpend SF PH4 (liquid). Further, the stability of haloperidol,ilmipramine hydrochloride, minocycline, and valsartan in oral suspension has not been previously reported in the literature. Compatibility was assessed by measuring percent recovery at varying time points throughout a 90 days period. Quantification of the APIs was performed by high performance liquid chromatography (HPLC-UV). Given the percentage of recovery of the APIs within the suspensions, the beyond-use date of the final preparations was found to be at least 90 days for most suspensions both refrigerated and at room temperature. Exceptions were: Minocycline hydrochloride at both storage temperatures (60 days), levodopa/carbidopa at room temperature (30 days), and lorazepam at room temperature (60 days). This suggests that compounded suspensions of APIs from different pharmacological classes in SyrSpend SF PH4 (liquid) are stable.

  6. 78 FR 2416 - Notice of Issuance of Final Determination Concerning Rybix® (Tramadol Hydrochloride) Tablets

    Science.gov (United States)

    2013-01-11

    ... (Tramadol Hydrochloride) Tablets AGENCY: U.S. Customs and Border Protection, Department of Homeland Security... (tramadol hydrochloride) tablets. Based upon the facts presented, CBP has concluded in the final determination that India is the country of origin of the Rybix (tramadol hydrochloride) tablets for purposes of...

  7. Spectrophotometric determination of meclizine hydrochloride and pyridoxine hydrochloride in laboratory prepared mixtures and in their pharmaceutical preparation

    Science.gov (United States)

    Ibrahim, Maha M.; Elzanfaly, Eman S.; El-Zeiny, Mohamed B.; Ramadan, Nesreen K.; Kelani, Khadiga M.

    2017-05-01

    In this paper, three rapid, simple, accurate and precise spectrophotometric methods were developed for the determination of meclizine hydrochloride in the presence of pyridoxine hydrochloride without previous separation. The methods under study are dual wavelength (DWL), ratio difference (RD) and continuous wavelet transform (CWT). On the other hand, pyridoxine hydrochloride (PYH) was determined directly at 291 nm. The methods obey Beer's law in the range of (5-50 μg/mL) for both compounds. All the methods were validated according to the ICH guidelines where the accuracy was found to be 98.29, 99.59, 100.42 and 100.62% for DWL, RD, CWT and PYH; respectively. Moreover the precision of the methods were calculated in terms of %RSD and it was found to be 0.545, 0.372, 1.287 and 0.759 for DWL, RD,CWT and PYH; respectively. The selectivity of the proposed methods was tested using laboratory prepared mixtures and assessed by applying the standard addition technique. So, they can be used for the routine analysis of pyridoxine hydrochloride and meclizine hydrochloride in quality-control laboratories.

  8. Metabolomic Analyses of Blood Plasma after Oral Administration of D-Glucosamine Hydrochloride to Dogs

    Directory of Open Access Journals (Sweden)

    Saburo Minami

    2012-08-01

    Full Text Available D-Glucosamine hydrochloride (GlcN∙HCl is an endogenous amino monosaccharide synthesized from glucose that is useful in the treatment of joint diseases in both humans and animals. The aim of this study was to examine amino acid metabolism in dogs after oral administration of GlcN∙HCl. Accelerated fumarate respiration and elevated plasma levels of lactic acid and alanine were observed after administration. These results suggest that oral administration of GlcN∙HCl induces anaerobic respiration and starvation in cells, and we hypothesize that these conditions promote cartilage regeneration. Further studies are required to evaluate the expression of transforming growth factor-beta (TGF-β.

  9. Stability of ranitidine hydrochloride in total parenteral nutrient solution.

    Science.gov (United States)

    Walker, S E; Bayliff, C D

    1985-03-01

    The stability of ranitidine hydrochloride was studied in a standard total parenteral nutrition (TPN) solution. The Canadian formulation of ranitidine hydrochloride (25 mg/mL) was added in 100-, 200-, and 300-mg doses to approximately 1200 mL of a TPN solution and allowed to stand at room temperature (23 degrees C) for seven days. During this time, samples were drawn at least once a day, and the ranitidine concentration was determined by high-performance liquid chromatography. The ranitidine concentration declined at roughly the same rate regardless of the initial concentration. During the study period, each of the three different concentrations declined to less than 70% of the initial concentration. Approximately 10% of the initial concentration was lost in 48 hours. Ranitidine hydrochloride admixtures were stable for up to 48 hours at room temperature in this standard TPN solution.

  10. Temperature-dependent THz vibrational spectra of clenbuterol hydrochloride

    Science.gov (United States)

    Yang, YuPing; Lei, XiangYun; Yue, Ai; Zhang, Zhenwei

    2013-04-01

    Using the high-resolution Terahertz Time-domain spectroscopy (THz-TDS) and the standard sample pellet technique, the far-infrared vibrational spectra of clenbuterol hydrochloride (CH), a β 2-adrenergic agonist for decreasing fat deposition and enhancing protein accretion, were measured in temperature range of 77-295 K. Between 0.2 and 3.6 THz (6.6-120.0 cm-1), seven highly resolved spectral features, strong line-narrowing and a frequency blue-shift were observed with cooling. However, ractopamine hydrochloride, with some structural and pharmacological similarities to clenbuterol hydrochloride, showed no spectral features, indicating high sensitivity and strong specificity of THz-TDS. These results could be used for the rapid and nondestructive CH residual detection in food safety control.

  11. Simultaneous spectrophotometric determination of drotaverine hydrochloride and paracetamol in tablet.

    Science.gov (United States)

    Mahaparale, Sonali; Telekone, R S; Raut, R P; Damle, S S; Kasture, P V

    2010-01-01

    Two simple, accurate and reproducible spectrophotometric methods; Q analysis and first order derivative method have been described for the simultaneous estimation of drotaverine hydrochloride and paracetamol in combined tablet dosage form. Absorption maxima of drotaverine hydrochloride and paracetamol in distilled water were found to be 303.5 nm and 243.5 nm respectively. Beer's law was obeyed in the concentration range 5-50 mug/ml for drotaverine and 5-60 mug/ml for paracetamol. In Q analysis method, two wavelengths were selected at isobestic point (277 nm) and lambda(max) of paracetamol (243.5 nm). In first order derivative method, zero crossing point for drotaverine hydrochloride and paracetamol were selected at 303.5 nm and 243.5 nm, respectively. The results of two methods were validated statistically and recovery studies were found to be satisfactory.

  12. Simultaneous spectrophotometric determination of drotaverine hydrochloride and paracetamol in tablet

    Directory of Open Access Journals (Sweden)

    Mahaparale Sonali

    2010-01-01

    Full Text Available Two simple, accurate and reproducible spectrophotometric methods; Q analysis and first order derivative method have been described for the simultaneous estimation of drotaverine hydrochloride and paracetamol in combined tablet dosage form. Absorption maxima of drotaverine hydrochloride and paracetamol in distilled water were found to be 303.5 nm and 243.5 nm respectively. Beer′s law was obeyed in the concentration range 5-50 µg/ml for drotaverine and 5-60 µg/ml for paracetamol. In Q analysis method, two wavelengths were selected at isobestic point (277 nm and λmax of paracetamol (243.5 nm. In first order derivative method, zero crossing point for drotaverine hydrochloride and paracetamol were selected at 303.5 nm and 243.5 nm, respectively. The results of two methods were validated statistically and recovery studies were found to be satisfactory.

  13. Splenic fibrosis and sarcomas in F344 rats fed diets containing aniline hydrochloride, p-chloroaniline, azobenzene, o-toluidine hydrochloride, 4,4'-sulfonyldianiline, or D & C red No. 9.

    Science.gov (United States)

    Goodman, D G; Ward, J M; Reichardt, W D

    1984-07-01

    In six carcinogenicity bioassays, male and female F344 rats were fed diets containing aniline hydrochloride (CAS: 142-04-1; hydrochloride benzenamide), p-chloroaniline (CAS: 106-47-8), azobenzene (CAS: 103-33-3), o-toluidine hydrochloride (CAS: 636-21-5), dapsone (CAS: 80-08-0; 4,4'-sulfonyldianiline), or D & C red No. 9 [CAS: D85500000; 5-chloro-2-[2-hydroxy-1-naphthalenyl)azo)-4-methylbenzenesulfon ic acid, barium salt]. The rats, from 6 weeks to 2 years old, were given the compounds at two dose levels, the estimated maximum tolerated dose and one-half that dose. In all six bioassays, dose-dependent incidences of splenic sarcomas and fibrosis were seen, with the highest incidences in male rats. Fibrosis occurred in the splenic parenchyma and/or the capsule. Fatty infiltration also was seen in the spleen. Sarcomas appeared to arise in the splenic red pulp or splenic capsule, usually in association with areas of parenchymal and capsular fibrosis and pigmentation. Larger tumors metastasized to the peritoneal cavity and abdominal organs. In some rats there was marked osseous metaplasia when the primary tumor metastasized to peritoneal surfaces. Other, less common, splenic neoplasms included hemangiosarcoma and hemangiopericytoma. Some rats had such extensive peritoneal involvement that the site of origin of their sarcoma was difficult to determine.

  14. 5-Aminolevulinate production by Escherichia coli containing the Rhodobacter sphaeroides hemA gene

    Energy Technology Data Exchange (ETDEWEB)

    Van Der Werf, M.J. [Michigan State Univ., East Lansing, MI (United States); Zeikus, J.G. [Michigan State Univ., East Lansing, MI (United States)]|[MBI International, Lansing, MI (United States)

    1996-10-01

    The Rhodobacter sphaeroides hemA gene codes for 5-aminolevulinate (ALA) synthase. This enzyme catalyzes the pyridoxal phosphate-dependent condensation of succinyl coenzyme A and glycine-forming ALA. The R. sphaeroides hemA gene in the pUC18/19 vector system was transformed into Escherichia coli. The effects of both genetic and physiological factors on the expression of ALA synthase and the production of ALA were studied. ALA synthase activity levels were maximal when hemA had the same transcription direction as the lac promoter. The distance between the lac promoter and hemA affected the expression of ALA synthase on different growth substrates. The E. coli host strain used had an enormous effect on the ALA synthase activity level and on the production of ALA, with E. coli DH1 being best suited. The ALA synthase activity level was also dependent on the carbon source. Succinate, L-malate, fumarate, and L-aspartate gave the highest levels of ALA synthase activity, while the use of lactose as a carbon source resulted in a repression of ALA synthase. After growth on succinate, ALA synthase represented {approx}5% of total cellular protein. The ALA synthase activity level was also dependent on the pH of the medium, with maximal activity occurring at pH 6.5. ALA production by whole cells was limited by the availability of glycine, and the addition of 2 g of glycine per liter to the growth medium increased the production of ALA fivefold, to 2.25 mM. In recombinant E. coli extracts, up to 22 mM ALA was produced from succinate, glycine, and ATP. 58 refs., 4 figs., 7 tabs.

  15. Spectrophotometric determination of ritodrine and isoxsuprine hydrochlorides using 4-aminoantipyrine.

    Science.gov (United States)

    Revanasiddappa, H D; Manju, B G

    2000-01-01

    A simple, accurate, and rapid method for the quantitative determination of ritodrine hydrochloride (RTH) and isoxsuprine hydrochloride (ISH) in both pure and dosage forms, is described. The method is based on the development of pink colored product as a result of the condensation of 4-aminoantipyrine with phenols in the presence of an alkaline oxidizing agent. The resulting products are measured at 510 nm for both drugs, with molar absorptivities of 0.98 x 10(4) and 1.20 x 10(4) L/mol x cm for RTH and ISH, respectively. A study of the effect of commonly associated excipients revealed that they did not cause interference.

  16. Enantiomeric Separation of Meptazinol Hydrochloride by Capillary Electrophoresis

    Institute of Scientific and Technical Information of China (English)

    YUYun-qiu; CHENYan; LINi; QIUZhui-bai

    2004-01-01

    Aim To establish a capillary electrophoresis method for enantiomerie separation of meptazinol hydrochloride. Methods The separation conditions such as cyclodextrin(CD)type, buffer pH, concentration of 2,3,6-O-triInethyl-β-cyclodextrin and organic additives were optimized. An optimum concentration was 30 mmol·L-1 phosphate (pH 7.02)with 10% (W/V) TM-β-CD and 2% acetonitrile. Results Basehne resolution of the enantiomer was readily achieved using 2,3,6-O-trimethyl-β-cyclodextrin. Conclusion This is a convenient method for fast enantiomeric resolution of meptazinol hydrochloride.

  17. [Effect of topical exhedrine hydrochloride on muco-ciliary transport].

    Science.gov (United States)

    Grammatica, L; Fiorella, R

    1983-07-30

    The time of nasal M.C.T. (Mucus Ciliar Transport) was studied by the indirect objective method of bleu-sky in 30 healthy subjects before and after the application of efedrina hydrochloride in water solution associated with timolo, eucaliptolo, mentolo essence of canfora monobramata and clorbutamolo. The time of nasal M.C.T., regular in the 87% of the subjects during the first determination was found extended in almost all of the cases after the application of vasoconstrictor (85%). This experimental data may be caused both by a direct effect of efedrina hydrochloride and by the substances associated in the solution and their physical characteristics.

  18. Low-dose Methotrexate Enhances Aminolevulinate-based Photodynamic Therapy in Skin Carcinoma Cells In-vitro and In-vivo

    Science.gov (United States)

    Anand, Sanjay; Honari, Golara; Hasan, Tayyaba; Elson, Paul; Maytin, Edward V.

    2009-01-01

    Purpose To improve treatment efficacy and tumor cell selectivity of δ-aminolevulinic acid (ALA)-based photodynamic therapy (PDT), via pretreatment of cells and tumors with methotrexate (MTX) to enhance intracellular photosensitizer levels. Experimental Design Skin carcinoma cells, in-vitro and in-vivo, served as the model system. Cultured human SCC13 and HEK1 cells, normal keratinocytes, and in-vivo skin tumor models (see below) were preconditioned with MTX for 72 h, then incubated with ALA for 4 h. Changes in PpIX levels and in cell survival after light exposure were assessed. Results MTX-preconditioning of monolayer cultures preferentially raised intracellular PpIX levels 2- to 4-fold in carcinoma cells versus normal keratinocytes. Photodynamic killing was synergistically enhanced by the combined therapy, compared to PDT alone. MTX enhancement of PpIX levels was achieved over a broad MTX concentration range (0.0003 – 1.0 mg/L; 0.6 nM – 2 mM). PpIX enhancement correlated with changes in protein expression of key porphyrin pathway enzymes, i.e. ~4-fold increase in coproporphyrinogen oxidase, and stable or slightly decreased expression of ferrochelatase. Differentiation markers (E-cadherin, involucrin, filaggrin) were also selectively induced by MTX in carcinoma cells. In-vivo relevance was established by showing that MTX preconditioning enhances PpIX accumulation in three models: (1) organotypic cultures of immortalized keratinocytes; (2) chemically-induced skin tumors in mice; and (3) human A431 squamous cell tumors implanted subcutaneously in mice. Conclusion Combination therapy using short-term exposure to low-dose MTX followed by ALA-PDT should be further investigated as a new combination modality to enhance efficacy and selectivity of PDT for epithelial carcinomas. PMID:19447864

  19. Preparation and adsorption behavior of berberine hydrochloride imprinted polymers by using silica gel as sacrificed support material

    Science.gov (United States)

    Li, Hui; Li, Yuzhuo; Li, Zhiping; Peng, Xiyang; Li, Yanan; Li, Gui; Tan, Xianzhou; Chen, Gongxi

    2012-03-01

    Preparation of berberine hydrochloride (B-Cl) imprinted polymers (MIPs) based on surface imprinting technique with silica gel as sacrificial support material was performed successfully by using B-Cl as template, methacrylic acid (MAA) and ethylene glycol dimethacrylate (EGDMA) as functional monomer and cross-linker, respectively. The prepared polymers were characterized by Fourier transmission infrared spectrometry (FTIR) and scanning electron microscopy (SEM). Adsorption behavior of the MIPs for the template and its structural analogues was investigated. Sites distribution on the surface of MIPs was explored by using different isotherm adsorption models and thermodynamic parameters for the adsorption of B-Cl on the MIPs determined. Sample application and reusability for the MIPs was also evaluated. Results indicated the strong adsorption and high selectivity of the MIPs for B-Cl. Saturated adsorption capacity reached 27.2 μmol g-1 and the selectivity coefficient of the MIPs for B-Cl relative to jatrorrhizine hydrochloride (J-Cl) and palmatine palmatus hydrochloride (P-Cl) are 3.70 and 6.03, respectively. In addition, the MIPs were shown with good reusability and selectively retention ability in sample application.

  20. Preparation and adsorption behavior of berberine hydrochloride imprinted polymers by using silica gel as sacrificed support material

    Energy Technology Data Exchange (ETDEWEB)

    Li Hui, E-mail: lihuijsdx@163.com [Key Laboratory of Plant Resource Conservation and Utilization, Jishou University, Hunan Jishou, 416000 (China); Li Yuzhuo [Key Laboratory of Plant Resource Conservation and Utilization, Jishou University, Hunan Jishou, 416000 (China); Li Zhiping [College of Chemistry and Chemical Engineering, Jishou University, Hunan Jishou, 416000 (China); Peng Xiyang; Li Yanan; Li Gui; Tan Xianzhou; Chen Gongxi [Key Laboratory of Plant Resource Conservation and Utilization, Jishou University, Hunan Jishou, 416000 (China)

    2012-03-01

    Preparation of berberine hydrochloride (B-Cl) imprinted polymers (MIPs) based on surface imprinting technique with silica gel as sacrificial support material was performed successfully by using B-Cl as template, methacrylic acid (MAA) and ethylene glycol dimethacrylate (EGDMA) as functional monomer and cross-linker, respectively. The prepared polymers were characterized by Fourier transmission infrared spectrometry (FTIR) and scanning electron microscopy (SEM). Adsorption behavior of the MIPs for the template and its structural analogues was investigated. Sites distribution on the surface of MIPs was explored by using different isotherm adsorption models and thermodynamic parameters for the adsorption of B-Cl on the MIPs determined. Sample application and reusability for the MIPs was also evaluated. Results indicated the strong adsorption and high selectivity of the MIPs for B-Cl. Saturated adsorption capacity reached 27.2 {mu}mol g{sup -1} and the selectivity coefficient of the MIPs for B-Cl relative to jatrorrhizine hydrochloride (J-Cl) and palmatine palmatus hydrochloride (P-Cl) are 3.70 and 6.03, respectively. In addition, the MIPs were shown with good reusability and selectively retention ability in sample application.

  1. A comparative study on the aggregating effects of guanidine thiocyanate, guanidine hydrochloride and urea on lysozyme aggregation

    Energy Technology Data Exchange (ETDEWEB)

    Emadi, Saeed, E-mail: emadi@iasbs.ac.ir; Behzadi, Maliheh

    2014-08-08

    Highlights: • Lysozyme aggregated in guanidine thiocyanate (1.0 and 2.0 M). • Lysozyme aggregated in guanidine hydrochloride (4 and 5 M). • Lysozyme did not aggregated at any concentration (0.5–5 M) of urea. • Unfolding pathway is more important than unfolding per se in aggregation. - Abstract: Protein aggregation and its subsequent deposition in different tissues culminate in a diverse range of diseases collectively known as amyloidoses. Aggregation of hen or human lysozyme depends on certain conditions, namely acidic pH or the presence of additives. In the present study, the effects on the aggregation of hen egg-white lysozyme via incubation in concentrated solutions of three different chaotropic agents namely guanidine thiocyanate, guanidine hydrochloride and urea were investigated. Here we used three different methods for the detection of the aggregates, thioflavin T fluorescence, circular dichroism spectroscopy and atomic force microscopy. Our results showed that upon incubation with different concentrations (0.5, 1.0, 2.0, 3.0, 4.0, 5.0 M) of the chemical denaturants, lysozyme was aggregated at low concentrations of guanidine thiocyanate (1.0 and 2.0 M) and at high concentrations of guanidine hydrochloride (4 and 5 M), although no fibril formation was detected. In the case of urea, no aggregation was observed at any concentration.

  2. [Simultaneous determination of ephedrine hydrochloride, D-pseudoephedrine and amygdalin in xiao'er pingchuan qutan granule by HPLC].

    Science.gov (United States)

    Yang, De-Bin; Tong, Yan; Ma, Zhen-Shan; Wang, Lin; Dong, Mei-Hong; Li, Yan-Ling; Wang, Jin-Yu

    2013-03-01

    To establish an HPLC method for the determination of ephedrine hydrochloride, D-pseudo-ephedrine and amygdalin in Xiao'er Pingchuan Qutan granule. Pheny ether chromatographic column (4.6 mm x 250 mm, 5 microm) was adopted, with acetonitrile-0.1% phosphoric acid (containing 0.1% three ethylamine) (3:97) as the mobile phase. The UV detection wavelength was at 210 nm, with the flow rate of 1 mL x min(-1), and column temperature was at 35 degrees C. The linearity of ephedrine hydrochloride, D-pseudo-ephedrine and amygdalin ranged between 0.078 60-3.144 microg (r = 1.000 0), 0.103 4-2.068 microg (r = 0.999 7) and 0.430 5-3.157 microg (r = 0.999 8), respectively. Their average recoveries were 98.46% (RSD 1.1%), 103.0% (RSD 1.5%) and 97.15% (RSD 2.1%), respectively. The method is simple, stable and reliable that it can be used to determine the content of ephedrine hydrochloride, D-pseudo-ephedrine and amygdalin in Xiao'er Pingchuan Qutan granule.

  3. Stability-indicating LC method for the estimation of bendamustine hydrochloride and its related impurities.

    Science.gov (United States)

    Kasa, Srinivasulu; Raja Sekhar Reddy, M; Kadaboina, Raja Sekhar; Murki, Veerender; Mulukutla, Venkata Suryanarayana

    2014-08-01

    A novel, simple, sensitive and stability-indicating high-performance liquid chromatography method was developed and validated for the quantification of impurities (process related and degradants) and the assay determination of Bendamustine hydrochloride. A chromatographic separation of Bendamustine and its impurities was achieved with an Inertsil ODS-2 analytical column, 250 × 4.6 mm, 5 µm, using gradient elution with mobile phase A consisting of a mixture of water and trifluoroacetic acid (1000:1, v/v) and mobile phase B consisting of acetonitrile. The instrumental settings included a flow rate of 1.0 mL/min, column temperature of 27°C and a detector wavelength of 233 nm, using a photodiode array detector. The tailing factor for Bendamustine was 1.10. Bendamustine hydrochloride was exposed to thermal, photolytic, hydrolytic and oxidative stress conditions and the stressed samples were analyzed by the proposed method. Peak homogeneity data of Bendamustine were obtained by using a photodiode array detector in the stressed sample chromatograms, which demonstrated the specificity of the method for estimation in the presence of degradants. The developed method was validated for parameters such as precision, accuracy, linearity, limit of detection, limit of quantification, ruggedness and robustness. The stability tests were also performed on drug substances as per International Conference on Harmonization guidelines.

  4. Development and validation of RP-HPLC method for the estimation of ivabradine hydrochloride in tablets

    Directory of Open Access Journals (Sweden)

    Seerapu Sunitha

    2010-01-01

    Full Text Available A simple, sensitive, precise and robust reverse-phase high-performance liquid chromatographic method for analysis of ivabradine hydrochloride in pharmaceutical formulations was developed and validated as per ICH guidelines. The separation was performed on SS Wakosil C18AR, 250Χ4.6 mm, 5 μm column with methanol:25 mM phosphate buffer (60:40 v/v, adjusted to pH 6.5 with orthophosphoric acid, added drop wise, as mobile phase. A well defined chromatographic peak of Ivabradine hydrochloride was exhibited with a retention time of 6.55±0.05 min and tailing factor of 1.14 at the flow rate of 0.8 ml/min and at ambient temperature, when monitored at 285 nm. The linear regression analysis data for calibration plots showed good linear relationship with R=0.9998 in the concentration range of 30-210 μg/ml. The method was validated for precision, recovery and robustness. Intra and Inter-day precision (% relative standard deviation were always less than 2%. The method showed the mean % recovery of 99.00 and 98.55 % for Ivabrad and Inapure tablets, respectively. The proposed method has been successfully applied to the commercial tablets without any interference of excipients.

  5. Charge-assisted bond N(+)H mediates the gelation of amorphous lurasidone hydrochloride during dissolution.

    Science.gov (United States)

    Qian, Shuai; Wang, Shanshan; Li, Zhen; Wang, Xiaojie; Ma, Di; Liang, Shujun; Gao, Yuan; Zhang, Jianjun; Wei, Yuanfeng

    2017-02-25

    Lurasidone hydrochloride (LH), the hydrochloride form of lurasidone with a charge-assisted bond N(+)H, is an atypical antipsychotropic agent for the treatment of schizophrenia. As a BCS class II drug, LH has a low oral bioavailability mainly due to its poor water solubility and low dissolution. In order to improve its solubility, amorphization of LH was performed and characterized. Unexpectedly, the dissolution rate of amorphous LH was much lower than that of crystalline LH. In addition, the amorphous LH powders quickly aggregated when contacting the dissolution media (water, 37°C), and formed a sticky gel adhering on the paddle. The follow-up polarized light microscope, XRPD, DSC, and FTIR analysis found that amorphous LH transformed to crystalline LH during dissolution. On the other hand, no such gelation phenomenon of amorphous lurasidone was observed under the same dissolution condition. However, the gel would reform when dropping concentrated hydrochloric acid slowly into the bottom of the medium during the dissolution of amorphous lurasidone, and XRPD/DSC/FTIR results indicated that the regenerated gel was consisted of crystalline LH, suggesting that the charge-assisted bond N(+)H in the structure of LH mediated the gel formation of amorphous LH during its dissolution process.

  6. [Radiolytic Decomposition of Ciprofloxacin Hydrochloride in Aqueous Solution Using γ Irradiation].

    Science.gov (United States)

    Zhu, Sheng-nan; Guo, Zhao-bing; Zhao, Yong-fu; Ge, Xin; Wei, Ying; Chen, Shu; Wang, Jing

    2015-04-01

    Effects of initial concentrations, pH values, different additives and composite pollutants on ciprofloxacin hydrochloride removal using γ irradiation were investigated. The experiments results showed γ irradiation could effectively remove ciprofloxacin hydrochloride; low initial concentration and strongly acidic condition were favorable for CIP removal using γ irradiation; the degradation of CIP was inhibited upon the addition of CO3(2-) and methanol, which indicated that the degradation of CIP might be mainly ascribed to *OH oxidation and the direct decomposition of CIP molecules induced by irradiation. BrO3- showed a synergistic effect with CIP in degradation of the composite pollutants when mixed together with CIP for γ irradiation, and the removal rates of both pollutants were improved. At an absorbed dose of 400 Gy, the removal rates of CIP and BrO3- were increased by 18.74% and 1.81%, respectively. The removal rates of TOC and COD were 15.22% and 61.44%, respectively, when the 100 mg x L(-1) CIP was degraded by γ irradiation at the absorbed dose of 6 000 Gy.

  7. Formulation and Evaluation of Multilayered Tablets of Pioglitazone Hydrochloride and Metformin Hydrochloride

    Directory of Open Access Journals (Sweden)

    Y. Ankamma Chowdary

    2014-01-01

    Full Text Available In the treatment of type 2 diabetes mellitus a continuous therapy is required which is a more complex one. As in these patients there may be a defect in both insulin secretion and insulin action exists. Hence, the treatment depends on the pathophysiology and the disease state. In the present study, multilayered tablets of pioglitazone hydrochloride 15 mg and metformin hydrochloride 500 mg were prepared in an attempt for combination therapy for the treatment of type 2 diabetes mellitus. Pioglitazone HCl was formulated as immediate release layer to show immediate action by direct compression method using combination of superdisintegrants, namely, crospovidone and avicel PH 102. Crospovidone at 20% concentration showed good drug release profile at 2 hrs. Metformin HCl was formulated as controlled release layer to prolong the drug action by incorporating hydrophilic polymers such as HPMC K4M by direct compression method and guar gum by wet granulation method in order to sustain the drug release from the tablets and maintain its integrity so as to provide a suitable formulation. The multilayered tablets were prepared after carrying out the optimization of immediate release layer and were evaluated for various precompression and postcompression parameters. Formulation F13 showed 99.97% of pioglitazone release at 2 hrs in 0.1 N HCl and metformin showed 98.81% drug release at 10 hrs of dissolution in 6.8 pH phosphate buffer. The developed formulation is equivalent to innovator product in view of in vitro drug release profile. The results of all these evaluation tests are within the standards. The procedure followed for the formulation of these tablets was found to be reproducible and all the formulations were stable after accelerated stability studies. Hence, multilayered tablets of pioglitazone HCl and metformin HCl can be a better alternative way to conventional dosage forms.

  8. Determination of Dyclonine Hydrochloride by a HPLC Method and Camphor and Menthol by a GC Method in Compound Lotion

    Directory of Open Access Journals (Sweden)

    Suying Ma

    2013-01-01

    Full Text Available A high performance liquid chromatographic (HPLC method with UV detector for the determination of dyclonine hydrochloride and a gas chromatography (GC method with flame ionization detector (FID for the determination of camphor and menthol in lotion were developed. The developed HPLC method involved using a SinoChoom ODS-BP C18 reversed-phase column (5 μm, 4.6 mm × 200 mm and mobile phase consisting of acetonitrile : water : triethylamine in a ratio of 45 : 55 : 1.0; pH was adjusted to 3.5 with glacial acetic acid. The developed GC method for determination of camphor and menthol involved using an Agilent 19091J-413 capillary chromatographic column (30 m × 320 μm × 0.25 μm. The two methods were validated according to official compendia guidelines. The calibration of dyclonine hydrochloride for HPLC method was linear over the range of 20–200 μg/mL. The retention time was found at 6.0 min for dyclonine hydrochloride. The calibration of camphor and menthol of GC method was linear over the range of 10–2000 μg/mL. The retention time was found at 2.9 min for camphor and 3.05 min for menthol. The proposed HPLC and GC methods were proved to be suitable for the determination of dyclonine hydrochloride, camphor, and menthol in lotion.

  9. Diffusion Coefficients ofl-Lysine Hydrochloride and l-Arginine Hydrochloride in Their Aqueous Solutions at 25℃

    Institute of Scientific and Technical Information of China (English)

    2000-01-01

    The diffusion coefficients** ofl-lysine hydrochloride andl-arginine hydrochloride in their aqueous solu- tions at 25℃ were determined by the metallic diaphragm cell method which is characterized by accuracy, promptness and convenience. Meanwhile, the densities and viscosities of the solutions were also determined. Based on all these data a semi-empirical model for correlating the diffusion coefficients of solid organic salts in their aqueous solutions at 25℃ was proposed. The fitting result of this model is comparatively satisfactory. Compared to a former model, Gordon Model, this model can avoid a number of difficulties and arduous work.

  10. The clinical efficacy of topical methyl-aminolevulinate photodynamic therapy in moderate to severe actinic keratoses of the face and scalp.

    NARCIS (Netherlands)

    Kleinpenning, M.M.; Kerkhof, P.C.M. van de; Gerritsen, M.J.P.

    2010-01-01

    INTRODUCTION: Since actinic keratoses (AKs) often appear in areas with field cancerization, photodynamic therapy (PDT) may have significant advantages over the standard treatment options. Objectives: Clinical efficacy of PDT with topical methyl aminolevulinate (MAL-PDT) in field cancerization was ev

  11. Comparison of topical methyl aminolevulinate photodynamic therapy with cryotherapy or Fluorouracil for treatment of squamous cell carcinoma in situ: Results of a multicenter randomized trial.

    NARCIS (Netherlands)

    Morton, C.; Horn, M.; Leman, J.; Tack, B.; Bedane, C.; Tjioe, M.; Ibbotson, S.; Khemis, A.; Wolf, P.

    2006-01-01

    OBJECTIVE: To compare the efficacy, tolerability, and cosmetic outcome of photodynamic therapy (PDT) using topical methyl aminolevulinate with cryotherapy or topical fluorouracil for treatment of squamous cell carcinoma in situ. DESIGN: Randomized, placebo-controlled study, with follow-up at 3 and 1

  12. Daylight photodynamic therapy with methyl aminolevulinate cream as a convenient, similarly effective, nearly painless alternative to conventional photodynamic therapy in actinic keratosis treatment

    DEFF Research Database (Denmark)

    Rubel, D M; Spelman, L; Murrell, D F

    2014-01-01

    BACKGROUND: Daylight photodynamic therapy (DL-PDT) of actinic keratosis (AK) has shown preliminary efficacy and safety results comparable to conventional photodynamic therapy (c-PDT), using methyl aminolevulinate (MAL) cream. OBJECTIVES: To demonstrate the efficacy and safety of DL-PDT vs. c...

  13. Release Characteristics of Diltiazem Hydrochloride Wax-Matrix ...

    African Journals Online (AJOL)

    Michael Horsfall

    diltiazem hydrochloride-wax matrix granules with sintering. ... The drug release was by Higuchi controlled diffusion mechanism and it followed ... of plastic matrix tablets. Polymer films with different permeability have been .... More so, with increase in temperature and ..... characterization of ibuprofen-cetyl alcohol beads by.

  14. Surface tension of compositions of polyhexametyleneguanidine hydrochloride - surfactants

    Directory of Open Access Journals (Sweden)

    S. Kumargaliyeva

    2012-12-01

    Full Text Available We made up songs bactericidal polyhexamethyleneguanidine hydrochloride (metacyde with the surface-active substances - anionic sodium dodecylsulfate, cationic cetylpyridinium bromide, and nonionic Tween-80 and measured the surface tension of water solutions. The study showed that the composition metacyde with surface-active agents have a greater surface activity than the individual components.

  15. 21 CFR 524.1982 - Proparacaine hydrochloride ophthalmic solution.

    Science.gov (United States)

    2010-04-01

    ... 21 Food and Drugs 6 2010-04-01 2010-04-01 false Proparacaine hydrochloride ophthalmic solution. 524.1982 Section 524.1982 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN... longterm toxicity of proparacaine is unknown. Prolonged use may possibly delay wound healing. (d...

  16. Acute generalized exanthematous pustulosis caused by terazosin hydrochloride.

    Science.gov (United States)

    Speck, Laura M; Wilkerson, Michael G; Perri, Anthony J; Kelly, Brent C

    2008-04-01

    Acute generalized exanthematous pustulosis (AGEP) is a rare cutaneous eruption mainly provoked by drugs. A case of AGEP in a 74-year-old male that was attributed to the ingestion of terazosin hydrochloride is presented. This is the first reported case of this association in medical literature. The history, clinical presentation, and pathogenesis of AGEP are discussed.

  17. Cradle-to-gate life cycle inventory of vancomycin hydrochloride.

    Science.gov (United States)

    Ponder, Celia; Overcash, Michael

    2010-02-15

    A life cycle analysis on the cradle-to-gate production of vancomycin hydrochloride, which begins at natural resource extraction and spans through factory (gate) production, not only shows all inputs, outputs, and energy usage to manufacture the product and all related supply chain chemicals, but can highlight where process changes would have the greatest impact on raw material and energy consumption and emissions. Vancomycin hydrochloride is produced by a low-yield fermentation process that accounts for 47% of the total cradle-to-gate energy. The fermentation step consumes the most raw materials and energy cradle-to-gate. Over 75% of the total cradle-to-gate energy consumption is due to steam use; sterilization within fermentation is the largest user of steam. Aeration and agitation in the fermentation vessels use 65% of the cradle-to-gate electrical energy. To reduce raw materials, energy consumption, and the associated environmental footprint of producing vancomycin hydrochloride, other sterilization methods, fermentation media, nutrient sources, or synthetic manufacture should be investigated. The reported vancomycin hydrochloride life cycle inventory is a part of a larger life cycle study of the environmental consequences of the introduction of biocide-coated medical textiles for the prevention of MRSA (methicillin-resistant Staphylococcus aureus) nosocomial infections.

  18. Asymmetric Synthesis of (+)-(11 R,12S)-Mefloquine Hydrochloride

    Institute of Scientific and Technical Information of China (English)

    2008-01-01

    The asymmetric synthesis of (+)-(11R,12S)-mefloquine hydrochloride, an antimalarial drug, was accomplished from commercially available 2-trifluoromethylaniline, ethyl 4,4,4-trifluoroacetoacetate and cyclopentanone in 7 steps with a 14% overall yield. The key steps were proline-catalyzed asymmetric direct aldol reaction and Beck-mann rearrangement. The absolute configuration was assigned by a Mosher's method.

  19. Amitriptyline-related peripheral neuropathy relieved during pyridoxine hydrochloride administration.

    Science.gov (United States)

    Meadows, G G; Huff, M R; Fredericks, S

    1982-11-01

    Tricyclic antidepressants rarely cause peripheral neuropathy. In fact, this class of drugs has been used to control the symptoms of pain and paresthesia that accompany peripheral neuropathy. We report peripheral paresthesias that occurred in a 39-year-old female during five years of amitriptyline administration. The patient's symptoms were relieved by oral pyridoxine hydrochloride, associated with elevated plasma pyridoxal phosphate.

  20. Simple spectrophotometric methods for determination of fluoxetine and clomipramine hydrochlorides in dosage forms and in some post-mortem biological fluids samples

    Directory of Open Access Journals (Sweden)

    Emam A. Ali

    2016-12-01

    Full Text Available Sensitive, simple and rapid spectrophotometric methods for micro determination of fluoxetine hydrochloride (FLU and clomipramine hydrochloride (CLO. The methods are based on the reaction between the examined drugs and acid dyes, namely; bromocresol green (BCG, phenol red (PhR and metanil yellow (MY producing yellow ion-pair complexes followed by their extraction with methylene chloride and measured at 412, 407 and 409 nm for FLU with BCG, PhR and MY, respectively; whereas for CLO at 409, 406 and 407 nm, respectively. All variables that affect the performance of the proposed methods were carefully studied and optimized. Beer’s law was obeyed in the concentration ranges 0.86–24.32 μg/mL, 8.64–41.30 μg/mL, 0.86–34.76 μg/mL for FLU and 1.75–24.55 μg/mL, 7.0–50 μg/mL, 1.65–34.78 μg/mL for CLO using BCG, PhR and MY respectively. The methods were validated in terms of accuracy and precision. The proposed methods were successfully applied to the determination of fluoxetine hydrochloride and clomipramine hydrochloride in pure samples, pharmaceutical formulations, spiked post-mortem urine and blood samples.

  1. Micellization behavior of mixtures of amphiphilic promazine hydrochloride and cationic aniline hydrochloride in aqueous and electrolyte solutions

    Energy Technology Data Exchange (ETDEWEB)

    Rub, Malik Abdul; Azum, Naved; Asiri, Abdullah M. [King Abdulaziz University, Jeddah (Saudi Arabia); Khan, Farah [Aligarh Muslim University, Aligarh (India); Al-Sehemi, Abdullah G. [Research Center for Advanced Materials Science, King Khalid University, Abha (Saudi Arabia)

    2015-10-15

    We studied the influence of cationic hydrotrope aniline hydrochloride on the micellization behavior of cationic amphiphilic phenothiazine drug promazine hydrochloride in the presence and absence of 50mmol kg{sup -1} NaCl. The experimental critical micelle concentration (CMC) values came out to be lower than ideal CMC (CMCid) values, signifying attractive interactions between the two components in mixed micelles. NaCl further decreases the CMC of pure PMZ and aniline hydrochloride as well as their mixture due to screening of the electrostatic repulsion among the polar head groups. The bulk properties of solution were examined by using different theoretical models for justification and comparison of results. The micellar mole fraction of aniline hydrochloride (X{sup Rub}{sub ,} X{sup M}{sub 1}, X{sup Rod}{sub 1} and X{sup id}{sub 1}) was evaluated by different proposed models, showing greater contribution of hydrotrope in mixed micelle. The negative values of interaction parameter (β) indicate synergistic interactions and negative values of β further decrease by the addition of salt in mixed systems. From the CMC values as a function of temperature, various thermodynamic properties have been evaluated and discussed in detail.

  2. Chemical Immobilization of Sloth Bears (Melursus ursinus) with Ketamine Hydrochloride and Xylazine Hydrochloride: Hematology and Serum Biochemical Values.

    Science.gov (United States)

    Veeraselvam, M; Sridhar, R; Perumal, P; Jayathangaraj, M G

    2014-01-01

    The present study was conducted to define the physiological responses of captive sloth bears immobilized with ketamine hydrochloride and xylazine hydrochloride and to determine and compare the values of hematology and serum biochemical parameters between sexes. A total of 15 sloth bears were immobilized using combination of ketamine hydrochloride and xylazine hydrochloride drugs at the dose rate of 5.0 milligram (mg) per kg body weight and 2.0 mg per kg body weight, respectively. The use of combination of these drugs was found satisfactory for the chemical immobilization of captive sloth bears. There were no significant differences observed in induction time and recovery time and physiological parameters such as heart rate, respiratory rate, and rectal temperature between sexes. Health related parameters comprising hematological values like packed cell volume (PCV), hemoglobin (Hb), red blood cell count (RBC), erythrocyte indices, and so forth and biochemical values like total protein, blood urea nitrogen (BUN), creatinine, alkaline amino-transferase (ALT), aspartate amino-transferase (AST), and so forth were estimated in 11 (5 males and 6 females) apparently healthy bears. Comparison between sexes revealed significant difference in PCV (P sloth bears for appropriate line treatment.

  3. Chemical Immobilization of Sloth Bears (Melursus ursinus with Ketamine Hydrochloride and Xylazine Hydrochloride: Hematology and Serum Biochemical Values

    Directory of Open Access Journals (Sweden)

    M. Veeraselvam

    2014-01-01

    Full Text Available The present study was conducted to define the physiological responses of captive sloth bears immobilized with ketamine hydrochloride and xylazine hydrochloride and to determine and compare the values of hematology and serum biochemical parameters between sexes. A total of 15 sloth bears were immobilized using combination of ketamine hydrochloride and xylazine hydrochloride drugs at the dose rate of 5.0 milligram (mg per kg body weight and 2.0 mg per kg body weight, respectively. The use of combination of these drugs was found satisfactory for the chemical immobilization of captive sloth bears. There were no significant differences observed in induction time and recovery time and physiological parameters such as heart rate, respiratory rate, and rectal temperature between sexes. Health related parameters comprising hematological values like packed cell volume (PCV, hemoglobin (Hb, red blood cell count (RBC, erythrocyte indices, and so forth and biochemical values like total protein, blood urea nitrogen (BUN, creatinine, alkaline amino-transferase (ALT, aspartate amino-transferase (AST, and so forth were estimated in 11 (5 males and 6 females apparently healthy bears. Comparison between sexes revealed significant difference in PCV (P<0.05 and mean corpuscular hemoglobin concentration (MCHC (P<0.05. The study might help to evaluate health profiles of sloth bears for appropriate line treatment.

  4. 盐酸氨基葡萄糖片高效液相色谱测定方法的改进%Improvement on Determination of Glucosamine Hydrochloride in Glucosamine Hydrochloride Tablets by HPLC

    Institute of Scientific and Technical Information of China (English)

    吴学军; 金鹏飞; 邹定; 姜文清; 胡欣; 孙春华

    2012-01-01

    Objective To improve an HPLC method for the determination of glucosamine hydrochloride in Glucosamine Hydrochloride Tablets. Methods An Alltima C18 column (250 mm × 4. 6 mm, 5 μm) was used for the separation, with 10 mm ammonium dihydrogen phosphate - acetonitrile (95 : 5) as the mobile phase at the flow rate of 0.5 mL/min. The detection wavelength was 194 nm. Results This method showed good linearity with a correlation coefficient (r) of 0.999 5; the specificity study showed satisfactory resolutions between glucosamine hydrochloride, excipients, forced degradation products and common acid radical negative ions; the precisions and stability were satisfactory with all RSDs below 2% ; and the spiked recovery ranged from 99.52% to 101. 2%. Conclusion This method is superior to the standard method, and could be used for the determination of glucosamine hydrochloride in Glucosamine Hydrochloride Tablets.%目的 改进盐酸氨基葡萄糖片的高效液相色谱测定方法.方法 采用AlhimaC18色谱柱(250mm×4.6mm,5μm),以10mmol/L磷酸二氢铵溶液一乙腈(95:5,V/V)为流动相,流速为0.5 mL/min,检测渡长为194nm.结果 改进方法后,盐酸氨基葡萄糖的线性关系良好,r=0.999 5;方法专属性强,盐酸氨基葡萄糖和辅料、降解产物、常见酸根离子之间都有良好分离度;方法精密度和稳定性良好.RSD均小于2%;加样回收率良好,百分回收率在99.52%-101.2%之间.结论 改进后的方法优于国家食品药品监督管理局注册标准中的方法,可作为盐酸氨基葡萄糖片的含量测定方法.

  5. Bioadhesive ranitidine hydrochloride for gastroretention with controlled microenvironmental pH.

    Science.gov (United States)

    Adhikary, Anuradha; Vavia, Pradeep R

    2008-08-01

    Ranitidine hydrochloride is a H(2) receptor blocker used in the treatment of gastric ulcers. Pharmacological factors, in addition to the dosage regimen, favor development of a sustained-release system for ranitidine especially in the therapeutic condition of erosive esophagitis. This investigation delves into the development of bioadhesive type of gastroretentive formulation (tablets) of ranitidine. The effect of mucoadhesive polymers such as Carbopol, hydroxypropyl methyl cellulose, and dextrose were studied. Mucoadhesion, in vitro drug release profile, water uptake, and swelling of the tablet were evaluated. Alkalizing agents were incorporated in an attempt to maintain an alkaline microenvironment within the tablet and improve the stability of the drug in acidic medium. The stability was evaluated using dye test and degradation studies. The drug release profiles were fit into various kinetic models.

  6. [Qualitative and quantitative analysis of fluoxetine hydrochloride by 19F NMR].

    Science.gov (United States)

    Yang, Bai-Qin; Kong, Er-Li; Xue, Xiao-Di; Zhao, Shou-Qian; Lin, Shrong-Shi

    2012-05-01

    The chemical shift of fluoxetine hydrochloride appears at delta 14.15 in 19F NMR analysis. The delta moved upfield slightly from 14.158 to 14.145 when the concentration of solution became diluted from 2.00 to 0.05 mmol x L(-1). Spiking test was suggested to confirm the existence of the compound for qualitative analysis. 19F NMR detection sensitivity test illustrated that a concentration of 17 mg in 1 L water could be detected while the sample was scanned 500 times with optimum parameters. In quantitative analysis, standard curve of concentration versus fluorine signal intensity was proposed to determine the amount of fluoxetine. Long capillary tube containing trifluoroacetic acid was used as internal standard for the integration measurements and straight line was obtained with good fitting. Direct additions of trifluoroethanol to fluoxetine solutions gave a poorer standard curve.

  7. Rapid quantification of the metabolite of valacyclovir hydrochloride in human plasma by liquid chromatography-tandem mass spectrometry

    Institute of Scientific and Technical Information of China (English)

    2010-01-01

    Objective To establish a rapid,sensitive and selective liquid chromatography-tandem mass spectrometry (LC-MS/MS) method for the determination of acyclovir (the metabolite of valacyclovir hydrochloride) in human plasma. Methods After addition of ganciclovir as internal standard (IS),plasma samples were prepared by one-step protein precipitation using acetonitrile as precipitant,followed by an isocratic elution with 0.1% formic acid solution-methanol (95∶5,v/v) on an Agilent ZORBAX SB-C18 (150mm×2.1mm i.d.,3....

  8. Determination of Ephedrine Hydrochloride and Pseudoephedrine Hydrochloride in Heat Oral Solution for Children by HPLC%HPLC法测定小儿清热止咳口服液中盐酸麻黄碱和盐酸伪麻黄碱的含量

    Institute of Scientific and Technical Information of China (English)

    覃晓媚; 韦薇; 黄妹春; 周征福; 陆红萍; 陈晓军; 黄园

    2012-01-01

    The HPLC determination method was used to detect the ephedrine hydrochloride and pseudoephedrine hydrochloride in heat oral solution for children by C18 ( 4. 6 mmX 250mm, 5jum ) and methanol-0. 02mol/L sodium dihydrogen phosphate ( with 0. 2% triethylamine,adjusted with phosphoric acid pH = 2. 5,9 : 91 ) were used as the mobile phase. The flow was set at 1.0ml · min-1,and the detection wavelength was 210nm. The precision and stability were fine in those conditions. The calibration curve was linear over the range of 0. 102 ~1. 02jig for ephedrine hydrochloride ( r =0. 9999 ) and 0.1016~1. 6256jj.g for pseudoephedrine hydrochloride ( r =0. 9999 ). The average recovery rates ( n =6 ) was 97. 62% for ephedrine hydrochloride and 97. 55% for pseudoephedrine hydrochloride. The proposed method can be used in simultaneously quantitative analysis of ephedrine hydrochloride and pseudoephedrine hydrochloride in heat oral solution for children.%采用C18色谱柱(4.6 mmX250mm,5μm),以甲醇-0.02mol/L磷酸二氢钠溶液(含0.2%三乙胺,磷酸调pH值2.5,9:91)为流动相,流速1.0ml.rnin-1,检测波长210nm,建立反相高效液相色谱法测定小儿清热止咳口服液中盐酸麻黄碱和盐酸伪麻黄碱含量.结果表明,盐酸麻黄碱在0.102~1.02μg范围内与峰面积呈良好线性关系,r=0.9999,平均加样回收率为97.62%,RSD为1.56%(n=6);盐酸伪麻黄碱在0.1016~1.6256μg范围内与峰面积呈良好线性关系,r=0.9999,平均加样回收率为97.55%,RSD为1.84%(n=6).本方法分离度好,具有良好的重复性,可以同时测定小儿清热止咳口服液中盐酸麻黄碱和盐酸伪麻黄碱的含量.

  9. A Convenient Synthesis of Amino Acid Methyl Esters

    Directory of Open Access Journals (Sweden)

    Yaowu Sha

    2008-05-01

    Full Text Available A series of amino acid methyl ester hydrochlorides were prepared in good toexcellent yields by the room temperature reaction of amino acids with methanol in thepresence of trimethylchlorosilane. This method is not only compatible with natural aminoacids, but also with other aromatic and aliphatic amino acids.

  10. Transdermal delivery of ondansetron hydrochloride: effects of vehicles and penetration enhancers.

    Science.gov (United States)

    Gwak, Hye Sun; Oh, Ik Sang; Chun, In Koo

    2004-02-01

    The effects of vehicles and penetration enhancers on the in vitro permeation of ondansetron hydrochloride (OS) across dorsal hairless mouse skins were investigated. Various types of vehicles, including ester, alcohol, and ether and their mixtures were used, and then a series of fatty acids and fatty alcohols were employed as enhancers. Among pure vehicles used, water and ethanol showed high permeation fluxes, which were 48.2+/-23.7 and 41.9+/-17.9 microg/cm2 per h, respectively. Even though propylene glycol monocaprylate (PGMC) alone did not show a high permeation rate, the skin permeability of OS was increased by the addition of diethylene glycol monoethyl ether (DGME); the highest flux was achieved at 40% of DGME. Also, the combination of PGMC and ethanol (80:20) or PGMC and propylene glycol (PG) (60:40) increased the permeation flux by six- and two-fold, respectively, compared to PGMC alone. The synergistic enhancement was also obtained by using PG-oleyl alcohol (OAl) cosolvent. The greatest flux was attained by the addition of unsaturated fatty acids at 3% concentration to PG. The enhancement factors with the addition of oleic acid or linoleic acid to PG were about 1250 and 450, respectively. But saturated fatty acids failed to show a significant enhancing effect. When the PGMC-DGME (60:40) cosolvent system was used as a vehicle, all fatty acids, including unsaturated fatty acids, failed to show significant enhancing effects. The results indicate that the combinations of oleic acid, linoleic acid, or oleyl alcohol with PG, or PGMC-DGME (60:40) cosolvent could be used for the design of the OS transdermal system.

  11. A novel validated RP-HPLC-DAD method for the simultaneous estimation of Metformin Hydrochloride and Canagliflozin in bulk and pharmaceutical tablet dosage form with forced degradation studies

    Directory of Open Access Journals (Sweden)

    Uttam Prasad Panigrahy

    2015-09-01

    Full Text Available A novel approach was used to develop and validate a rapid isocratic Reversed Phase-High Performance Liquid Chromatographic method for the simultaneous estimation of Metformin Hydrochloride and Canagliflozin in bulk and pharmaceutical tablet dosage form with forced degradation studies. The separation was performed by using Kromasil C18 column (250mm×4.6 mm, 5mm particle size, Waters Alliance e2695 HPLC system with 2998 PDA detector and mobile phase contained a mixture of 0.01M Ammonium acetate (pH adjusted to 3.5 with orthophosphoric acid and Acetonitrile (65:35, v/v. The flow rate was set to 1ml/min with responses measured at 254nm. The retention time of Metformin Hydrochloride and Canagliflozin was 2.440min and 3.713min respectively with resolution of 8.95.Linearity was established in the range of 50-300µg/ml for Metformin Hydrochloride and 5-30µg/ml for Canagliflozin with correlation coefficients (r2=0.999. The percentage recoveries were between (99.45%-100.65% and (99.95%-100.74% for Metformin Hydrochloride and Canagliflozin respectively. Validation parameters were evaluated according to the International Conference on Harmonization (ICH Q2 R1 guidelines. The forced degradation studies were performed by using HCl, NaOH, H2O2, thermal, UV radiation and water. Metformin Hydrochloride and Canagliflozin are more sensitive towards oxidative degradation condition. The developed method was successfully applied for the quantification and hyphenated instrumental analysis.

  12. A validated stability-indicating high performance liquid chromatographic method for moxifloxacin hydrochloride and ketorolac tromethamine eye drops and its application in pH dependent degradation kinetics

    Directory of Open Access Journals (Sweden)

    Jayant B Dave

    2013-01-01

    Full Text Available Background and Aim: A fixed dose combination of moxifloxacin hydrochloride and ketorolac tromethamine is used in ratio of 1:1 as eye drops for the treatment of the reduction of post operative inflammatory conditions of the eye. A simple, precise, and accurate High Performance Liquid Chromatographic (HPLC method was developed and validated for determination of moxifloxacin hydrochloride and ketorolac tromethamine in eye drops. Materials and Methods: Isocratic HPLC separation was achieved on a ACE C 18 column (C 18 (5 μm, 150 mm×4.6 mm, i.d. using the mobile phase 10 mM potassium di-hydrogen phosphate buffer pH 4.6-Acetonitrile (75:25 v/v at a flow rate of 1.0 mL/min. The detection was performed at 307 nm. Drugs were subjected to acid, alkali and neutral hydrolysis, oxidation and photo degradation. Moreover, the proposed HPLC method was utilized to investigate the pH dependent degradation kinetics of moxifloxacin hydrochloride and ketorolac tromethamine in buffer solutions at different pH values like 2.0, 6.8 and 9.0. Results and Conclusion: The retention time (t R of moxifloxacin hydrochloride and ketorolac tromethamine were 3.81±0.01 and 8.82±0.02 min, respectively. The method was linear in the concentration range of 2-20 μ/mL each for moxifloxacin hydrochloride and ketorolac tromethamine with a correlation coefficient of 0.9996 and 0.9999, respectively. The method was validated for linearity, precision, accuracy, robustness, specificity, limit of detection and limit of quantitation. The drugs could be effectively separated from different degradation products and hence the method can be used for stability analysis. Different kinetics parameters like apparent first-order rate constant, half-life and t 90 (time for 90% potency left were calculated.

  13. Development and validation of a rapid RP-UPLC method for the simultaneous estimation of bambuterol hydrochloride and montelukast sodium from tablets

    Directory of Open Access Journals (Sweden)

    R Yanamandra

    2012-01-01

    Full Text Available A rapid, simple, sensitive and selective analytical method was developed by using reverse phase ultra performance liquid chromatographic technique for the simultaneous estimation of bambuterol hydrochloride and montelukast sodium in combined tablet dosage form. The developed method is superior in technology to conventional high performance liquid chromatography with respect to speed, resolution, solvent consumption, time, and cost of analysis. Elution time for the separation was 6 min and ultra violet detection was carried out at 210 nm. Efficient separation was achieved on BEH C18 sub-2-μm Acquity UPLC column using 0.025% (v/v trifluoro acetic acid in water and acetonitrile as organic solvent in a linear gradient program. Resolutions between bambuterol hydrochloride and montelukast sodium were found to be more than 31. The active pharmaceutical ingredient was extracted from tablet dosage from using a mixture of methanol, acetonitrile and water as diluent. The calibration graphs were linear for bambuterol hydrochloride and montelukast sodium in the range of 6.25-37.5 μg/ml. The percentage recoveries for bambuterol hydrochloride and montelukast sodium were found to be in the range of 99.1-100.0% and 98.0-101.6%, respectively. The test solution was found to be stable for 7 days when stored in the refrigerator between 2-8Ί. Developed UPLC method was validated as per International Conference on Harmonization specifications for method validation. This method can be successfully employed for simultaneous estimation of bambuterol hydrochloride and montelukast sodium in bulk drugs and formulations.

  14. HPLC法测定盐酸曲马多葡萄糖注射液中盐酸曲马多的含量%Determination of Tramadol Hydrochloride in tRAMADOL Hydrochloride Glucose Injections by HPLC

    Institute of Scientific and Technical Information of China (English)

    赵峰辉; 李新图; 陈建中; 陈跃; 汪变; 文桂芳

    2013-01-01

    目的:建立HPLC法测定盐酸曲马葡萄糖注射液中盐酸曲马多的含量.方法:色谱柱:Bondysil-C18(250 mm×4.6 mm,5 μm),流动相:醋酸-冰醋酸钠缓冲液(pH4.5)-甲醇(65:35),流速:1.0 ml·min-1,柱温:35℃,检测波长:271 nm,进样量:20 μl.结果:盐酸曲马多质量浓度线性范围为10~140μg·ml-1(r=0.999 0),平均回收率为99.9%(RSD=0.80%,n=9).结论:本方法简便、灵敏、准确.%Objective: To establish an HPLC method for the determination of tramadol hydrochloride in tramadol hydrochloride glucose injections. Method: The analysis was performed on a Bondysil-C18( 250 mm ×4.6 mm,5 μm )column. The mobile phase was acetic acid-sodium glacial acetic acid buffer ( pH 4.5) and methanol ( 65: 35 ). The flow rate was 1.0 ml · min-1, the column temperature was 30℃ , the detection wavelength was 271 nm, and the injection volume was 20 μl. Result: The linear range of tramadol hydrochloride was 10-140 μg · ml-1( r = 0.999 0 ), and the average recovery was 99.9% with RSD of 0.80%( n = 9 ). Conclusion: The method is simple, sensitive and accurate.

  15. Differential effect of buffering agents on the crystallization of gemcitabine hydrochloride in frozen solutions.

    Science.gov (United States)

    Patel, Mehulkumar; Munjal, Bhushan; Bansal, Arvind K

    2014-08-25

    The purpose of this study was to evaluate the differential effect of buffering agents on the crystallization of gemcitabine hydrochloride (GHCl) in frozen solutions. Four buffering agents, viz. citric acid (CA), malic acid (MA), succinic acid (SA) and tartaric acid (TA) were selected and their effect on GHCl crystallization was monitored using standard DSC and low temperature XRD. Onset of GHCl crystallization during heating run in DSC was measured to compare the differential effect of buffering agents. Glass transition temperature (Tg'), unfrozen water content in the freeze concentrate and crystallization propensity of the buffering agents was also determined for mechanistic understanding of the underlying effects. CA and MA inhibited while SA facilitated crystallization of GHCl even at 25 mM concentration. Increasing the concentration enhanced their effect. However, TA inhibited GHCl crystallization at concentrations crystallization could be explained by consideration of two opposing factors: (i) their own crystallization tendency and (ii) unfrozen water content in the freeze concentrate. In conclusion, it was established that API crystallization in frozen solution is affected by the type and concentration of the buffering agents.

  16. Fundamentals of ionic conductivity relaxation gained from study of procaine hydrochloride and procainamide hydrochloride at ambient and elevated pressure.

    Science.gov (United States)

    Wojnarowska, Z; Swiety-Pospiech, A; Grzybowska, K; Hawelek, L; Paluch, M; Ngai, K L

    2012-04-28

    The pharmaceuticals, procaine hydrochloride and procainamide hydrochloride, are glass-forming as well as ionically conducting materials. We have made dielectric measurements at ambient and elevated pressures to characterize the dynamics of the ion conductivity relaxation in these pharmaceuticals, and calorimetric measurements for the structural relaxation. Perhaps due to their special chemical and physical structures, novel features are found in the ionic conductivity relaxation of these pharmaceuticals. Data of conductivity relaxation in most ionic conductors when represented by the electric loss modulus usually show a single resolved peak in the electric modulus loss M(")(f) spectra. However, in procaine hydrochloride and procainamide hydrochloride we find in addition another resolved loss peak at higher frequencies over a temperature range spanning across T(g). The situation is analogous to many non-ionic glass-formers showing the presence of the structural α-relaxation together with the Johari-Goldstein (JG) β-relaxation. Naturally the analogy leads us to name the slower and faster processes resolved in procaine hydrochloride and procainamide hydrochloride as the primary α-conductivity relaxation and the secondary β-conductivity relaxation, respectively. The analogy of the β-conductivity relaxation in procaine HCl and procainamide HCl with JG β-relaxation in non-ionic glass-formers goes further by the finding that the β-conductivity is strongly related to the α-conductivity relaxation at temperatures above and below T(g). At elevated pressure but compensated by raising temperature to maintain α-conductivity relaxation time constant, the data show invariance of the ratio between the β- and the α-conductivity relaxation times to changes of thermodynamic condition. This property indicates that the β-conductivity relaxation has fundamental importance and is indispensable as the precursor of the α-conductivity relaxation, analogous to the relation found

  17. Disposable screen-printed sensors for determination of duloxetine hydrochloride

    Directory of Open Access Journals (Sweden)

    Alarfaj Nawal A

    2012-01-01

    Full Text Available Abstract A screen-printed disposable electrode system for the determination of duloxetine hydrochloride (DL was developed using screen-printing technology. Homemade printing has been characterized and optimized on the basis of effects of the modifier and plasticizers. The fabricated bi-electrode potentiometric strip containing both working and reference electrodes was used as duloxetine hydrochloride sensor. The proposed sensors worked satisfactorily in the concentration range from 1.0 × 10-6-1.0 × 10-2 mol L-1 with detection limit reaching 5.0 × 10-7 mol L-1 and adequate shelf life of 6 months. The method is accurate, precise and economical. The proposed method has been applied successfully for the analysis of the drug in pure and in its dosage forms. In this method, there is no interference from any common pharmaceutical additives and diluents. Results of the analysis were validated statistically by recovery studies.

  18. Linear scleroderma after contusion and injection of mepivacaine hydrochloride.

    Science.gov (United States)

    Ueda, Takashi; Niiyama, Shiro; Amoh, Yasuyuki; Katsuoka, Kensei

    2010-05-15

    A 36-year-old woman initially was treated for a contusion by local injection of mepivacaine hydrochloride into the left dorsum of the foot. Approximately 3 months after the injury and injection, linear sclerotic plaques originating from the site of contusion and injection were recognized. These progressed in extent and severity over a period of 3 years, when she presented to our clinic. By biopsy, swelling of collagen fibers in the lower dermis was revealed and the condition was diagnosed as linear scleroderma. Our present case had multiple linear sclerotic plaques of the left lower extremity, the distribution of which was consistent with Blaschko lines. It was also revealed that the initial sclerotic plaque was at the site of the contusion and local mepivacaine hydrochloride injection. Our present case is interesting in that the findings suggest a correlation between linear scleroderma plaque occurrence and the contusion or injection of mepivacaine.

  19. OPTIMIZATION OF CONCENTRATION OF POLYHEXANIDE HYDROCHLORIDE IN MULTIPURPOSE SOLUTION.

    OpenAIRE

    Arora, A.; Ali, A.; M.T.Zzaman; Chauhan, S.; V.Handa

    2010-01-01

    There are a number of foreign pathogenic microorganisms like viruses, bacteria, yeast, fungi and protozoa which can inadvertently be introduced into eye via contact lens and hence disinfection is a vital part. Multifunctional solutions are generally intended to combine the action of cleaning disinfecting, rinsing lubricating deproteinising and soaking in one single product.In order to optimization of concentration of Polyhexanide hydrochloride in multipurpose solution some microbiological stu...

  20. FORMULATION AND EVALUATION OF FLOATING TABLETS OF TIZANIDINE HYDROCHLORIDE

    Directory of Open Access Journals (Sweden)

    Adimoolam Senthil

    2011-08-01

    Full Text Available The objective of the present investigation was to develop floating matrix tablets of tizanidine hydrochloride for prolongation of gastric residence time in order to overcome its low bioavailability (34–40% and short biological half life (4.2 h. Tizanidine hydrochloride floating tablets were prepared by the direct compression method, using different viscosity grades of hydroxypropylmethylcellulose (HPMC K4M and K15M. Tizanidine hydrochloride is an orally administered prokinetic agent that facilitates or restores motility throughout the length of the gastrointestinal tract. Tablets were evaluated for various physical parameters and floating properties. Further, tablets were studied for in-vitro drug release characteristics in 12 hours. Drug release from floating matrix tablets was sustained over 12 h with buoyant properties. DSC study revealed that there was no drug and excipient interaction. Based on the release kinetics, all formulations best fitted the Higuchi, first-order model and non-Fickian as the mechanism of drug release. The optimized formulation (F9 released 75% of drug at the end of 10 hours by in-vitro release study.

  1. Clinical effect of venlafaxine combined with methylphenidate hydrochloride on narcolepsy

    Directory of Open Access Journals (Sweden)

    YAN Bin

    2013-11-01

    Full Text Available This study aims to explore the clinical effect of venlafaxine sustained-release capsules combined with methylphenidate hydrochloride tablets on narcolepsy. Thirty-eight cases of narcoleptic patients were randomly divided into venlafaxine combined with methylphenidate hydrochloride treatment group (observation group, N = 19 and methylphenidate hydrochloride and clomipramine treatment group (control group, N = 19. After a total of 12-week treatment, clinical curative effect and adverse drug reactions were observed in 2 groups of patients. The results showed that effective rate of the treatment for excessive daytime sleepiness (EDS in observation group was higher than that of the control group (15/19 vs 8/19, P = 0.044, and effective rate of the treatment for cataplexy in observation group was higher than that of the control group (13/19 vs 6/19, P = 0.048. The rate of adverse drug reactions in observation group was lower than that in the control group (χ2 = 8.889, P = 0.003. It was indicated that venlafaxine combined with methylphenidate had good curative effect on narcolepsy with EDS and cataplexy symptoms.

  2. Mucoadhesive microspheres of propranolol hydrochloride for nasal delivery

    Directory of Open Access Journals (Sweden)

    Dandagi P

    2007-01-01

    Full Text Available Gelatin A microspheres of propranolol hydrochloride for intranasal systemic delivery were developed with the aim to avoid first pass metabolism, to improve the patient compliance, to use an alternative therapy to conventional dosage form, to achieve controlled blood level profiles, and to improve the therapeutic efficacy of propranolol hydrochloride in the treatment of various cardiovascular disorders and as a prophylactic for migraine. Gelatin A microspheres were prepared by emulsion crosslinking method using glutaradehyde as a crosslinking agent. Gelatin and chitosan were used as polymer and co polymer respectively. All the prepared microspheres were evaluated for physical characteristics, such as particle size, incorporation efficiency, swelling index, in vitro bioadhesion using rat jejunum and in vitro drug release in pH 6.6 phosphate buffer. Average particle size of microspheres was found to be in the size range 1-50 mm. Increase in drug and polymer concentration in the formulation increased incorporation efficiency. All the microsphers showed good bioadhesive properties and swelling indices and good sustained release of drug. The data indicates that propranolol hydrochloride release followed Higuchi′s matrix and Peppa′s model. Stability studies showed stability of formulation at all the conditions to which they were subjected.

  3. A novel kind of TSV slurry with guanidine hydrochloride

    Science.gov (United States)

    Jiao, Hong; Yuling, Liu; Baoguo, Zhang; Xinhuan, Niu; Liying, Han

    2015-10-01

    The effect of a novel alkaline TSV (through-silicon-via) slurry with guanidine hydrochloride (GH) on CMP (chemical mechanical polishing) was investigated. The novel alkaline TSV slurry was free of any inhibitors. During the polishing process, the guanidine hydrochloride serves as an effective surface-complexing agent for TSV CMP applications, the removal rate of barrier (Ti) can be chemically controlled through tuned selectivity with respect to the removal rate of copper and dielectric, which is helpful to modifying the dishing and gaining an excellent topography performance in TSV manufacturing. In this paper, we mainly studied the working mechanism of the components of slurry and the skillful application guanidine hydrochloride in the TSV slurry. Project supported by the Major National Science and Technology Special Projects (No. 2009ZX02308), the Fund Project of Hebei Provincial Department of Education, China (No. QN2014208), the Natural Science Foundation of Hebei Province, China (No. E2013202247), and Colleges and Universities Scientific research project of Hebei Province, China (No. Z2014088).

  4. Spectrophotometric estimation of betahistine hydrochloride in tablet formulations

    Directory of Open Access Journals (Sweden)

    Amit Kumar

    2010-01-01

    Full Text Available Aim: The study aims to develop simple, sensitive, rapid, accurate and precise spectrophotometric method for estimation of Betahistine hydrochloride in tablet dosage forms. Materials and Methods: For method I and II, in a series of 10 ml volumetric flask, aliquots of standard drug solution (100 μg/ml in double distilled water were transferred and diluted with same so as to give several dilutions in concentration range of 15-90 μg/ml and 10-80 μg/ml respectively of betahistine hydrochloride. To 5 ml of each dilution taken in a separating funnel, (5 ml of methyl orange for method I and 5 ml of bromo phenol blue for method II reagent and 5 ml of chloroform was added. Reaction mixture was shaken gently for 5 min and allowed to stand so as to separate aqueous and chloroform layer. Absorbance maxima measured at 421.6 nm and 412 nm for method I and II respectively. Results: The recovery studies were found close to 100 % that indicates accuracy and precision of the proposed methods. The statistical analysis was carried out and results of which were found satisfactory. Standard deviation values were found low that indicated reproducibility of the proposed methods. Conclusion: Based on results the developed methods could be used for routine estimation of betahistine hydrochloride from tablet formulations.

  5. Preparation and Characterization of Chitosan Hydrochloride

    Institute of Scientific and Technical Information of China (English)

    FENG; HuiXia

    2001-01-01

    Chitin 1 is a biodegradable and nontoxic polysaccharide widely spread among marine and terrestrial invertebrates and fungi. It is usually obtained from waste materials of the sea food-processing industry, mainly shells of crab, shrimp, prawn and krill. Native chitin occurs in such natural composite materials usually combined with inorganics, proteins, lipids and pigments. Its isolation calls for chemical treatments to eliminate these contaminants, some of which maybe coimmercially explored. By treating crude chitin with aqueous 40~50% sodium hydroxide at 110~115℃ chitosan is obtained. However, the fully deacetylated product is rarely obtained due to the risks of side reactions and chain deplolymerization. Chitosan and chitin are closely related since both are linear polysaccharides containing 2-acetamido-2-deoxy-D-glucopyranose and 2-amino-2-deoxy-D-glucopyranose units joined by β (1→4) glycosidic bonds. They can be distinguished by their contents of the above-mentioned units and by their solubilities in aqueous media. The acetylated units predominate in chitin while chitosan chains contain mostly deacetylated units. Chitin is soluble in a very limited number of solvents while chitosan is soluble in aqueous dilute solutions of a number of mineral and organic acids, being the most common ones, the hydrochloric and acetic acids. In aqueous dilute acid media chitosan forms salts, producing polyelectrolyte chains bearing positive charges on the nitrogen atoms of their amine groups. In fact the salt of chitosan may be formed in a separate step or as a consequence of the presence of acid in the water suspension of the neutralized form of chitosan.  ……

  6. Preparation and Characterization of Chitosan Hydrochloride

    Institute of Scientific and Technical Information of China (English)

    2001-01-01

    @@ Chitin 1 is a biodegradable and nontoxic polysaccharide widely spread among marine and terrestrial invertebrates and fungi. It is usually obtained from waste materials of the sea food-processing industry, mainly shells of crab, shrimp, prawn and krill. Native chitin occurs in such natural composite materials usually combined with inorganics, proteins, lipids and pigments. Its isolation calls for chemical treatments to eliminate these contaminants, some of which maybe coimmercially explored. By treating crude chitin with aqueous 40~50% sodium hydroxide at 110~115℃ chitosan is obtained. However, the fully deacetylated product is rarely obtained due to the risks of side reactions and chain deplolymerization. Chitosan and chitin are closely related since both are linear polysaccharides containing 2-acetamido-2-deoxy-D-glucopyranose and 2-amino-2-deoxy-D-glucopyranose units joined by β (1→4) glycosidic bonds. They can be distinguished by their contents of the above-mentioned units and by their solubilities in aqueous media. The acetylated units predominate in chitin while chitosan chains contain mostly deacetylated units. Chitin is soluble in a very limited number of solvents while chitosan is soluble in aqueous dilute solutions of a number of mineral and organic acids, being the most common ones, the hydrochloric and acetic acids. In aqueous dilute acid media chitosan forms salts, producing polyelectrolyte chains bearing positive charges on the nitrogen atoms of their amine groups. In fact the salt of chitosan may be formed in a separate step or as a consequence of the presence of acid in the water suspension of the neutralized form of chitosan.

  7. Use of xylazine hydrochloride-ketamine hydrochloride for immobilization of wild leopards (Panthera pardus fusca) in emergency situations.

    Science.gov (United States)

    Belsare, Aniruddha V; Athreya, Vidya R

    2010-06-01

    In India, leopards (Panthera pardus fusca) inhabit human-dominated landscapes, resulting in encounters that require interventions to prevent harm to people, as well as the leopards. Immobilization is a prerequisite for any such intervention. Such emergency field immobilizations have to be carried out with limited tools, often amidst large uncontrollable crowds. An effective and practicable approach is discussed, based on 55 wild leopard immobilizations undertaken between January 2003 and April 2008. A xylazine hydrochloride (1.4 +/- 0.3 mg/kg)--ketamine hydrochloride (5 +/- 2 mg/kg) mixture was used for immobilization of leopards, based on estimated body weight. When weight could not be estimated, a standard initial dose of 50 mg of xylazine--150 mg of ketamine was used. Supplemental doses (50-75 mg) of only ketamine were used as required. No life-threatening adverse effects of immobilization were documented for at least 1 mo postimmobilization.

  8. A Validated Stability-indicating Reverse Phase HPLC Assay Method for the Determination of Memantine Hydrochloride Drug Substance with UV-Detection Using Precolumn Derivatization Technique

    Directory of Open Access Journals (Sweden)

    Bhavil Narola

    2010-07-01

    Full Text Available This present paper deals with the development and validation of a stability indicating high performance liquid chromatographic method for the quantitative determination of Memantine hydrochloride. Memantine hydrochloride was derivatized with 0.015 M 9-fluorenylmethyl chloroformate (FMOC and 0.5 M borate buffer solution by keeping it at room temperature for about 20 minutes and the chromatographic separation achieved by injecting 10 µL of the derivatized mixture into a Waters HPLC system with photodiode array detector using a kromasil C18 column (150 × 4.6 mm, 5 µ. The mobile phase consisting of 80% acetonitrile and 20% phosphate buffer solution and a flow rate of 2 milliliter/minute. The Memantine was eluted at approximately 7.5 minutes. The volume of FMOC used in derivatization, concentration of FMOC and derivatization time was optimized and used. Forced degradation studies were performed on bulk sample of Memantine hydrochloride using acid (5.0 Normal (N hydrochloric acid, base (1.0 N sodium hydroxide, oxidation (30% hydrogen peroxide, thermal (105°C, photolytic and humidity conditions. The developed LC method was validated with respect to specificity, precision (% RSD about 0.70%, linearity (linearity of range about 70–130 µg/mL, ruggedness (Overall % RSD about 0.35%, stability in analytical solution (Cumulative % RSD about 0.11% after 1450 min. and robustness.

  9. Synthesis of silver nanoparticles in the presence of diethylaminoethyl-dextran hydrochloride polymer and their SERS activity

    Science.gov (United States)

    Mikac, L.; Jurkin, T.; Štefanić, G.; Ivanda, Mile; Gotić, Marijan

    2017-09-01

    The silver nanoparticles (AgNPs) were synthesized upon γ-irradiation of AgNO3 precursor suspensions in the presence of diethylaminoethyl-dextran hydrochloride (DEAE-dextran) cationic polymer as a stabilizer. The dose rate of γ-irradiation was 32 kGy h-1, and absorbed doses were 30 and 60 kGy. The γ-irradiation of the precursor suspension at acidic or neutral pH conditions produced predominantly the silver(I) chloride (AgCl) particles, because of the poor solubility of AgCl already present in the precursor suspension. The origin of AgCl in the precursor suspension was due to the presence of chloride ions in DEAE-dextran hydrochloride polymer. The addition of ammonia to the precursor suspension dissolved the AgCl precipitate, and the γ-irradiation of such colourless suspension at alkali pH produced a stable aqueous suspension with rather uniform spherical AgNPs of approximately 30 nm in size. The size of AgNPs was controlled by varying the AgNO3/DEAE-dextran concentration in the suspensions. The surface-enhanced Raman scattering (SERS) activities of synthesized AgNPs were examined using organic molecules rhodamine 6G, pyridine and 4-mercaptobenzoic acid (4-MBA). The NaBH4 was used as SERS aggregation agent. The SERS results have shown that in the presence of synthesized AgNPs, it was possible to detect low concentration of tested compounds.

  10. Floating matrix dosage form for propranolol hydrochloride based on gas formation technique: development and in vitro evaluation.

    Science.gov (United States)

    Chaturvedi, Kiran; Umadevi, S; Vaghani, Subhash

    2010-01-01

    Gastroretentive tablets of propranolol hydrochloride were developed by direct compression method using citric acid and sodium bicarbonate as the effervescent base. Hydroxypropyl methylcellulose; HPMC K15M was used to prepare the floating tablets to retard the drug release for 12h in stomach. Na-carboxymethyl cellulose (NaCMC) or carbopol 934P was added to alter the drug release profile or the dimensional stability of the formulation. Dicalcium phosphate (DCP) was used as filler. Formulations were evaluated for floating lag time, duration of floating, dimensional stability, drug content and in vitro drug release profile. The formulations were found to have floating lag time less than 1min. It was found that the dimensional stability of the formulations increase with increasing concentration of the swelling agent. The release mechanism of propranolol hydrochloride from floating tablets was evaluated on the basis of Peppas and Higuchi model. The ânâ value of the formulations ranged from 0.5201 to 0.7367 (0.5DCP, 3.75% citric acid and 18.75% sodium bicarbonate seemed most desirable. FTIR, DSC and XRPD studies indicated the absence of any significant chemical interaction within dug and excipients. Stability study of optimized formulation revealed no significant change and found to be stable.

  11. Quantitative fluorescence using 5-aminolevulinic acid–induced protoporphyrin IX biomarker as a surgical adjunct in low-grade glioma surgery

    Science.gov (United States)

    Valdés, Pablo A.; Jacobs, Valerie; Harris, Brent T.; Wilson, Brian C.; Leblond, Frederic; Paulsen, Keith D.; Roberts, David W.

    2015-01-01

    OBJECT Previous studies in high-grade gliomas (HGGs) have indicated that protoporphyrin IX (PpIX) accumulates in higher concentrations in tumor tissue, and, when used to guide surgery, it has enabled improved resection leading to increased progression-free survival. Despite the benefits of complete resection and the advances in fluorescence-guided surgery, few studies have investigated the use of PpIX in low-grade gliomas (LGGs). Here, the authors describe their initial experience with 5-aminolevulinic acid (ALA)–induced PpIX fluorescence in a series of patients with LGG. METHODS Twelve patients with presumed LGGs underwent resection of their tumors after receiving 20 μg/kg of ALA approximately 3 hours prior to surgery under an institutional review board–approved protocol. Intraoperative assessments of the resulting PpIX emissions using both qualitative, visible fluorescence and quantitative measurements of PpIX concentration were obtained from tissue locations that were subsequently biopsied and evaluated histopathologically. Mixed models for random effects and receiver operating characteristic curve analysis for diagnostic performance were performed on the fluorescence data relative to the gold-standard histopathology. RESULTS Five of the 12 LGGs (1 ganglioglioma, 1 oligoastrocytoma, 1 pleomorphic xanthoastrocytoma, 1 oligodendroglioma, and 1 ependymoma) demonstrated at least 1 instance of visible fluorescence during surgery. Visible fluorescence evaluated on a specimen-by-specimen basis yielded a diagnostic accuracy of 38.0% (cutoff threshold: visible fluorescence score ≥ 1, area under the curve = 0.514). Quantitative fluorescence yielded a diagnostic accuracy of 67% (for a cutoff threshold of the concentration of PpIX [CPpIX] > 0.0056 μg/ml, area under the curve = 0.66). The authors found that 45% (9/20) of nonvisibly fluorescent tumor specimens, which would have otherwise gone undetected, accumulated diagnostically significant levels of CPpIX that were

  12. A Novel, Rapid, and Validated Stability-Indicating UPLC Method for the Estimation of Drotaverine Hydrochloride and Ibuprofen Impurities in Oral Solid Dosage Form.

    Science.gov (United States)

    Vijay Kumar, Rekulapally; Rao, Vinay U; Anil Kumar, N; Venkata Subbaiah, B

    2015-01-01

    A novel, stability-indicating, reversed-phase ultra-performance liquid chromatographic (RP-UPLC) method was developed for the determination of pure drotaverine hydrochloride and ibuprofen in the presence of their impurities and degradation products. The method was developed using a Waters UPLC BEH C18, 100 × 2.1 mm, 1.7 µm column with a flow rate of 0.3 mL/min and detector wavelength at 210 nm. The mobile phase consisted of potassium dihydrogen orthophosphate buffer and acetonitrile. Drotaverine hydrochloride and ibuprofen were subjected to the stress conditions of oxidative, acid, base, photolytic, and thermal degradation. Degradation products resulting from the stress studies were well-resolved, thus confirming the test method as stability-indicating. Validation of the method was carried out as per International Conference on Harmonization guidelines.

  13. Synthesis and activity of (R)-(-)-m-trimethylacetoxy-alpha-[(methylamino)methyl]benzyl alcohol hydrochloride: a prodrug form of (R)-(-)-phenylephrine.

    Science.gov (United States)

    Yuan, S S; Bador, N

    1976-06-01

    Optically pure (R)-(-)-m-trimethylacetoxy-alpha-[(methylamino)methyl]benzyl alcohol hydrochloride was synthesized by the following sequence: (R)-(-)-phenylephrine was condensed with acetone in the presence of calcium carbide to give an oxazolidine derivative and then treated with thallous ethoxide in ether followed by trimethylacetyl chloride to yield the phenolic ester. Finally, the oxazolidine ring was cleaved by one equivalent of hydrogen chloride in ethanol. Condensation of phenylephrine with benzaldehyde, with or without solvents, gave either 1,1,2-trimethyl-4,6-dihydroxy-1,2,3,4-tetrahydroisoquinoline or a mixture of side-chain oxazolidine and the tetrahydroisoquinoline. Condensation of epinephrine with opianic acid in pyridine also gave a tetrahydroisoquinoline only. When applied on rabbit eyes, the prodrug (R)-(-)-m-trimethylacetoxy-alpha[(methylamino)methyl]benzyl alcohol hydrochloride exhibited an unexpected, three times higher mydriatic activity than the corresponding racemic prodrug and was 15 times more active than the parent, (R)-(-)-phenylephrine.

  14. Four new mutations in the erythroid-specific 5-aminolevulinate synthase (ALAS2) gene causing X-linked sideroblastic anemia: increased pyridoxine responsiveness after removal of iron overload by phlebotomy and coinheritance of hereditary hemochromatosis.

    Science.gov (United States)

    Cotter, P D; May, A; Li, L; Al-Sabah, A I; Fitzsimons, E J; Cazzola, M; Bishop, D F

    1999-03-01

    X-linked sideroblastic anemia (XLSA) in four unrelated male probands was caused by missense mutations in the erythroid-specific 5-aminolevulinate synthase gene (ALAS2). All were new mutations: T647C, C1283T, G1395A, and C1406T predicting amino acid substitutions Y199H, R411C, R448Q, and R452C. All probands were clinically pyridoxine-responsive. The mutation Y199H was shown to be the first de novo XLSA mutation and occurred in a gamete of the proband's maternal grandfather. There was a significantly higher frequency of coinheritance of the hereditary hemochromatosis (HH) HFE mutant allele C282Y in 18 unrelated XLSA hemizygotes than found in the normal population, indicating a role for coinheritance of HFE alleles in the expression of this disorder. One proband (Y199H) with severe and early iron loading coinherited HH as a C282Y homozygote. The clinical and hematologic histories of two XLSA probands suggest that iron overload suppresses pyridoxine responsiveness. Notably, reversal of the iron overload in the Y199H proband by phlebotomy resulted in higher hemoglobin concentrations during pyridoxine supplementation. The proband with the R452C mutation was symptom-free on occasional phlebotomy and daily pyridoxine. These studies indicate the value of combined phlebotomy and pyridoxine supplementation in the management of XLSA probands in order to prevent a downward spiral of iron toxicity and refractory anemia.

  15. High-performance liquid chromatographic determination of memantine hydrochloride in rat plasma using sensitive fluorometric derivatization.

    Science.gov (United States)

    Xie, Mei-Fen; Zhou, Wei; Tong, Xin-Yi; Chen, Yi-Le; Cai, Yi; Li, Yan; Duan, Geng-Li

    2011-02-01

    In this study, we investigated a simple, sensitive and reliable liquid chromatography-fluorescence detection method for the determination of memantine hydrochloride in rat plasma which was based on derivatization with 9-fluorenylmethyl chloroformate (FMOC-Cl). For the first time, FMOC-Cl was introduced into derivatization of memantine hydrochloride in rat plasma. The amino groups of memantine hydrochloride and amantadine hydrochloride (internal standard) were trapped with FMOC-Cl to form memantine hydrochloride-FMOC-Cl and amantadine hydrochloride-FMOC-Cl compositions, which can be very compatible for LC-FLD. Precipitation of plasma proteins by acetonitrile was followed by vortex mixing and centrifugation. Chromatographic separation was performed on a C(18) column (DIAMONSIL 150 × 4.6 mm, id 5 μm) with a mobile phase consisting of acetonitrile and water at a flow rate of 1.0 mL/min. The retention times of memantine hydrochloride-FMOC-Cl and amantadine hydrochloride-FMOC-Cl compositions were 23.69 and 40.27 min, respectively. Optimal conditions for the derivatization of memantine hydrochloride were also described. The limit of quantification (LOQ) was 25 ng/mL for memantine hydrochloride in plasma, the linear range was 0.025-5.0 μg/mL in plasma with a correlation coefficient (r) of 0.9999. The relative standard deviations (RSDs) of intra-day and inter-day assays were 4.46-12.19 and 5.23-11.50%, respectively. The validated method was successfully applied to the determination of memantine hydrochloride in rat plasma samples.

  16. Stability-indicating high performance thin layer chromatography determination of Paroxetine hydrochloride in bulk drug and pharmaceutical formulations.

    Science.gov (United States)

    Venkatachalam, A; Chatterjee, Vidya S

    2007-08-29

    A simple selective precise and stability-indicating high performance thin layer chromatographic method of analysis of Paroxetine hydrochloride both as a bulk drug and in formulations was developed and validated. The method employed TLC (Thin Layer Chromatography) aluminum precoated with silica gel 60F-254 as the stationary phase. The solvent system consisted of butanol:acetic acid:water (8:2:0.5, v/v/v). This system was found to give compact spots for Paroxetine HCl (Rf, retardation factor, value-0.48+/-0.02). Paroxteine HCl was subjected to acid and alkali hydrolysis, oxidation and photodegradation, where the degraded product was well separated from the pure drug. Densitometric analysis of Paroxetine hydrochloride was carried out in the absorbance mode at 295 nm. The linear regression analysis data for the calibration spots showed good relationship with (regression) r2 = 0.9903 in the amount range of 300-1500 ng (nanogram) per spot. The mean value of co-relation co-efficient, slope and intercept were 0.9903+/-0.001, 5.38+/-0.058 and 182.5+/-2.16 respectively. The method was validated for precision, recovery and robustness. The limits of detection and quantitation were 50 and 150 ng, respectively. The drug does not undergo degradation with oxidation, but gets affected in acidic and alkaline conditions. The acid and alkali degradation showed extra peaks at 0.4 and 0.08 Rf, respectively. This indicates that the drug is susceptible to acidic and alkaline medium. As the method could effectively separate the drug from its degradation products, it can be employed as a stability-indicating one.

  17. Photodynamic therapy (PDT) and photodiagnosis (PD) using endogenous photosensitization induced by 5-aminolevulinic acid (ALA): current clinical and development status

    Science.gov (United States)

    Marcus, Stuart L.; Sobel, Russel S.; Golub, Allyn L.; Carroll, Ronald L.; Lundahl, Scott L.; Shulman, D. Geoffrey

    1996-04-01

    Exogenous provision of ALA to many tissues results in the accumulation of sufficient quantities of the endogenous photosensitizer protoporphyrin IX, (PpIX), to produce a photodynamic effect. Therefore, ALA may be considered the only current PDT agent in clinical development which is a biochemical precursor of a photosensitizer. Topical ALA application, followed by exposure to activating light (ALA PDT), has been reported effective for the treatment of a variety of dermatologic diseases including cutaneous T-cell lymphoma, superficial basal cell carcinoma, Bowen's disease, and actinic (solar) keratoses, and is also being examined for treatment of acne and hirsutism. PpIX induced by ALA application also may serve as a fluorescence detection marker for photodiagnosis (PD) of malignant and pre- malignant conditions of the urinary bladder and other organs. Local internal application of ALA has also been used for selective endometrial ablation in animal model systems and is beginning to be examined in human clinical studies. Systemic, oral administration of ALA has been used for ALA PDT of superficial head and neck cancer, various gastrointestinal cancers, and the condition known as Barrett's esophagus. This brief paper reviews the current clinical and development status of ALA PDT.

  18. The effects of visual fluorescence marking induced by 5-aminolevulinic acid for endoscopic diagnosis of urinary bladder cancer

    Science.gov (United States)

    Daniltchenko, Dmitri I.; Koenig, Frank; Schnorr, Dietmar; Valdman, Alexander; Al-Shukri, Salman; Loening, Stefan A.

    2003-10-01

    During cystoscopy procedure, fluorescence diagnostics induced by 5-ALA improves visual detection of the bladder cancer. Macroscopic ALA-fluorescence allows visualizing of small flat tumors, carcinoma in situ, true neoplasm margins and dysplasias of the bladder. Following ALA instillation, cystoscopy has been performed under both standard and blue light illumination. Totally, 153 biopsies have been carried out at 53 patients with suspicion of bladder cancer. The results were compared to ALA-fluorescence data. In 13% of the patients, bladder cancer and dysplasia were found out in addition, due to red fluorescence. The sensitivity and specificity of ALA-fluorescence technique aggregated 96% and 52% respectively. The sensitivity and specificity of 5-ALA-fluorescent detection exceeded standard endoscopy under white light on 20%. The new method does not exclude a false positive and a false negative fluorescent luminescence. The ALA-based fluorescence detection system enhances the diagnosis of malignant/dysplastic bladder lesions significantly.

  19. Treatment of Sweat gland carcinoma with Topical Aminolevulinic Acid Photodynamic therapy: An effective treatment method to improve surgical outcomes.

    Science.gov (United States)

    He, Xian; Yang, Yadong; Yang, Yang; Wang, Yuanyuan; Wang, Wensheng; Song, Yanying; Zeng, Yongfang; Yang, Yunchuan; Zhang, Xingcun; Li, Guoling; Gao, Yang; Lu, Yuangang

    2017-03-01

    Sweat gland carcinoma is an extremely rare skin cancer, which is hard to diagnose and completely resect without causing functional and cosmetic problems. Moreover, the high rate of recurrence is hard to handle in the treatment of sweat gland carcinoma. Photodynamic therapy is a novel treatment protocol which can selectively destroy tumor cells with good functional and cosmetic outcomes. This is a case about a 53 years old patient with sweat gland carcinoma on his right foot, which received surgery and photodynamic therapy. There is no recurrence one year after treatment of surgery and photodynamic therapy. Excision combined with photodynamic therapy during operation is a promising strategy towards tumors which are hard to resect thoroughly and have a high risk of recurrence. Copyright © 2016 Elsevier B.V. All rights reserved.

  20. Treatment of hidradenitis suppurativa with intralesional photodynamic therapy with 5-aminolevulinic acid and 630nm laser beam.

    Science.gov (United States)

    Suárez Valladares, María Jesús; Eiris Salvado, Noemi; Rodríguez Prieto, Manuel Angel

    2017-03-01

    Hidradenitis suppurativa (HS) is a chronic relapsing inflammatory skin disease with multiple treatment options that have been used with mixed results. To evaluate the effectiveness, safety and tolerability of intralesional photodynamic therapy (I-PDT) in the management of HS. Also, to assess the effect of this technique on the different areas treated. Case series of 38 HS patients treated with I-PDT between 2011-2015 following a standardized protocol to assess response at the treated areas RESULTS: 29 patients achieved a complete response, while persistence was noted on 8 cases and only 1 suffered a recurrence. Difference between basal (median 28.5) and final (0) Hidradenitis Severity Score showed a significant reduction of 24.5 points (ptreatment option for localized HS lesions, achieving a high rate of remission with an adequate maintenance of response i and few complications. Copyright © 2016 Japanese Society for Investigative Dermatology. Published by Elsevier B.V. All rights reserved.

  1. Induced Protoporphyrin IX Accumulation by the δ-Aminolevulinic Acid in Bacteria and its Potential Use in the Photodynamic Therapy

    Science.gov (United States)

    Brígido-Aparicio, Cyntiha; Ramón-Gallegos, Eva; Arenas-Huertero, Francisco Jesús; Uribe-Hernández, Raúl

    2008-08-01

    The increasing incident of resistant strains to antibiotic has encouraged the search of new antibacterial treatments, such as the photodynamic therapy. In recent years, photodynamic therapy has demonstrated being a good technology for the treatment of recurrent bacteria infection. PDT presents a hopeful approach to eliminate Gram positive and negative bacteria in immunological compromised patients. This therapy uses a laser in combination with a photosensibilizer in presence of intracellular molecular oxygen. The process generates an effect of phototoxicity in bacterial cells. The aim of this work was to determine the in vitro conditions to accumulate PpIX in effective concentrations in Staphylococcus aureus ATCC25923 and Streptococcus pyogenes, which are responsible of human cutaneous diseases. A cellular suspension of both strains was prepared in TSB to obtain growth in Log-phase, then, the suspensions were adjusted to a final concentration of 2.61×108 cells/mL. The strains were exposed to increasing concentrations from 0 to 160μg/mL of δ-ALA in order to determinate the concentration that induces the biggest accumulation of PpIX. PpIX was measured using the Piomelli method modified for bacteria. The concentration selected was 40 mg/mL of ALA. It was found that in basal concentration of δ-ALA (0 μg/mL) both strains accumulated similar amount of PpIX. In concentrations of 5 mg/mL of δ-ALA it was observed a significant (p<0.001) increment in PpIX concentration. Finally it was realized a kinetic to determinate the optimal accumulation over the time at 0, 5, 10, 15 and 30 min, and 1, 2, 4, 8, 16 and 32 h. It was found that the ideal time for PDT application, in both strains, was 24 h because in smaller times there was not statistically significant difference. The S. aureus ATCC25923 accumulated significantly the biggest concentration of PpIX with regard to S. pyogenes. In conclusion, it was found that the optimal conditions to apply PDT will be to expose both strains to 40 mg/mL of ALA and to irradiate at 24 h after the exposition.

  2. Stability Indicating HPLC Method for Estimation of S-amlodipine besylate and Nebivolol hydrochloride in Bulk Drugs and Marketed Formulation

    Directory of Open Access Journals (Sweden)

    G.V.S Kumar

    2012-10-01

    Full Text Available A simple, precise and stability indicating reversed phase liquid chromatographic method was developed and validated for estimation of s-amlodipine besylate and nebivolol hydrochloride in bulk drug and marketed formulation. The separation was achieved on Zorbax C8 G (250mm x 4.6mm, 5µm analytical column with mobile phase comprising of 0.05M Potassium di hydrogen phosphate: Acetonitrile (pH 3.0 (60:40v/v at isocratic flow of 1.0ml/min with UV detection at 269 nm. The retention times of s-amlodipine besylate and nebivolol hydrochloride was found to be 5.2 and 6.8 minutes respectively. The method was successfully validated in accordance to ICH guidelines for accuracy, precision, specificity, linearity, ruggedness and robustness. The linear regression analysis data for calibration plots showed good linear relationship in the concentration range 0.125-0.375μg/mL for s-amlodipine besylate and 0.25-0.75 for nebivolol hydrochloride. The drugs were exposed to acidic, basic, oxidation, thermal and photolytic stress degradation conditions. The resultant stressed samples were analyzed by the proposed method and was established to provide high resolution among the degradation products and the analytes. All the peaks of degraded product were resolved from the active pharmaceutical ingredient with significantly different retention time and the peak purity of analyte peaks in the stressed samples was confirmed by photodiode array detector. The method could effectively separate the drug from its degradation product; it can be employed as a stability- indicating one.

  3. 78 FR 27971 - Determination That REV-EYES (Dapiprazole Hydrochloride Ophthalmic Solution), 0.5%, Was Not...

    Science.gov (United States)

    2013-05-13

    ... HUMAN SERVICES Food and Drug Administration Determination That REV-EYES (Dapiprazole Hydrochloride... determined that REV-EYES (dapiprazole hydrochloride ophthalmic solution), 0.5%, was not withdrawn from sale... refer to a listed drug. REV-EYES (dapiprazole hydrochloride ophthalmic solution), 0.5%, is the...

  4. 21 CFR 524.1484d - Neomycin sulfate, hydrocortisone acetate, tetracaine hydrochloride ear ointment.

    Science.gov (United States)

    2010-04-01

    ..., tetracaine hydrochloride ear ointment. 524.1484d Section 524.1484d Food and Drugs FOOD AND DRUG..., tetracaine hydrochloride ear ointment. (a) Specifications. The product contains 5 milligrams of neomycin... a lesser degree, chronic otitis externa in dogs and cats. In treatment of ear canker and...

  5. 21 CFR 520.1242b - Levamisole hydrochloride tablet or oblet (bolus).

    Science.gov (United States)

    2010-04-01

    ... 21 Food and Drugs 6 2010-04-01 2010-04-01 false Levamisole hydrochloride tablet or oblet (bolus). 520.1242b Section 520.1242b Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL DRUGS, FEEDS, AND RELATED PRODUCTS ORAL DOSAGE FORM NEW ANIMAL DRUGS § 520.1242b Levamisole hydrochloride tablet...

  6. 21 CFR 520.1242c - Levamisole hydrochloride and piperazine dihydrochloride.

    Science.gov (United States)

    2010-04-01

    ... 21 Food and Drugs 6 2010-04-01 2010-04-01 false Levamisole hydrochloride and piperazine dihydrochloride. 520.1242c Section 520.1242c Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) ANIMAL DRUGS, FEEDS, AND RELATED PRODUCTS ORAL DOSAGE FORM NEW ANIMAL DRUGS § 520.1242c Levamisole hydrochloride...

  7. Effects of metomindate hydrochloride and tricaine methanesulfonate on the short term cortisol response in channel catfish

    Science.gov (United States)

    The effects of metomidate hydrochloride and tricaine methanesulfonate (MS-222) on cortisol stress response of channel catfish, Ictalurus punctatus, were examined during 10 minutes of sedation. Channel catfish were assigned to three treatments: 1. Metomidate hydrochloride (12.5 mg/L), 2. MS-222 (100...

  8. A practical synthesis of sarpogrelate hydrochloride and in vitro platelet aggregation inhibitory activities of its analogues

    Institute of Scientific and Technical Information of China (English)

    2010-01-01

    A convenient approach for the preparation of sarpogrelate hydrochloride was developed.Two series of sarpogrelate hydrochloride analogues were designed and synthesized in order to improve their platelet aggregation inhibitory activities, biological tests suggested that these compounds have platelet aggregation inhibitory activities to some extent.

  9. 40 CFR Appendix B to Subpart Nnn... - Free Formaldehyde Analysis of Insulation Resins by Hydroxylamine Hydrochloride

    Science.gov (United States)

    2010-07-01

    ... Insulation Resins by Hydroxylamine Hydrochloride B Appendix B to Subpart NNN of Part 63 Protection of...—Free Formaldehyde Analysis of Insulation Resins by Hydroxylamine Hydrochloride 1. Scope This method was specifically developed for water-soluble phenolic resins that have a relatively high free-formaldehyde...

  10. HPLC法测定鼻炎糖浆中盐酸麻黄碱和盐酸伪麻黄碱的含量%Determination of ephedrine hydrochloride and pseudoephedrine hydrochloride in Biyan Syrup by HPLC

    Institute of Scientific and Technical Information of China (English)

    冉亚东; 原欢欢; 官柳

    2014-01-01

    目的:建立高效液相色谱法测定鼻炎糖浆中盐酸麻黄碱和盐酸伪麻黄碱含量的测定方法。方法采用Agilent Zorbax SB-C18色谱柱(4.6 mm ×250 mm,5μm),乙腈-0.2%磷酸溶液(含0.2%三乙胺)(2:98)为流动相,流速:1.0 mL ·min-1,检测波长206 nm,柱温:25℃。结果盐酸麻黄碱进样量在0.124~1.86μg范围内与峰面积呈良好线性(r=0.9999),平均回收率为99.99%,RSD=1.24%(n=6);盐酸伪麻黄碱进样量在0.1038~1.557μg范围内与峰面积呈良好线性(r=0.9999),平均回收率为99.33%,RSD=1.93%(n=6)。结论该方法准确、重复性好,可用于鼻炎糖浆中盐酸麻黄碱和盐酸伪麻黄碱的测定。%Objective To establish an HPLC method for the determination of ephedrine hydrochloride and pseudo-ephedrine hydrochloride in Biyan Syrup. Methods The Agilent Zorbax SB-C18(4. 6 mm × 250 mm,5 μm)column was used. The mobile phase consisted of acetonitrile-0. 20% phosphoric acid(containing 0. 2% triethylamine)(2:98)with the flow rate of 1. 0 mL·min-1 . The detection wavelength was 206 nm and the column temperature was 25 ℃. Results The linear range of ephedrine hydrochloride and pseudoephedrine hydrochloride was 0. 124~1. 86μg(r=0. 999 9)and 0. 103 8~1. 557 μg(r=0. 999 9)with the average recovery of 99. 99%(RSD=1. 24%,n=6)and 99. 33%(RSD=1. 93%,n=6),respectively. Conclusion The method was accurate and reproducible. It can be used for the determination of ephed-rine hydrochloride and pseudoephedrine hydrochloride in Biyan Syrup.

  11. Neuroprotection against vascular dementia after acupuncture combined with donepezil hydrochloride: P300 event related potential

    Directory of Open Access Journals (Sweden)

    Qiang Liu

    2016-01-01

    Full Text Available Acupuncture can be used to treat various nervous system diseases. Here, 168 vascular dementia patients were orally administered donepezil hydrochloride alone (5 mg/day, once a day for 56 days, or combined with acupuncture at Shenting (DU24, Tianzhu (BL10, Sishencong (Extra, Yintang (Extra, Renzhong (DU26, Neiguan (PC6, Shenmen (HT7, Fengchi (GB20, Wangu (GB12 and Baihui (DU20 (once a day for 56 days. Compared with donepezil hydrochloride alone, P300 event related potential latency was shorter with an increased amplitude in patients treated with donepezil hydrochloride and acupuncture. Mini-Mental State Examination score was also higher. Moreover, these differences in P300 latency were identified within different infarcted regions in patients treated with donepezil hydrochloride and acupuncture. These findings indicate that acupuncture combined with donepezil hydrochloride noticeably improves cognitive function in patients with vascular dementia, and exerts neuroprotective effects against vascular dementia.

  12. Neuroprotection against vascular dementia after acupuncture combined with donepezil hydrochloride:P300 event related potential

    Institute of Scientific and Technical Information of China (English)

    Qiang Liu; Xiu-juan Wang; Zhe-cheng Zhang; Rong Xue; Ping Li; Bo Li

    2016-01-01

    Acupuncture can be used to treat various nervous system diseases. Here, 168 vascular dementia patients were orally administered donepezil hydrochloride alone (5 mg/day, once a day for 56 days), or combined with acupuncture atShenting (DU24),Tianzhu (BL10),Sishencong (Extra), Yintang (Extra),Renzhong (DU26),Neiguan (PC6),Shenmen (HT7),Fengchi (GB20),Wangu (GB12) andBaihui (DU20) (once a day for 56 days). Compared with donepezil hydrochloride alone, P300 event related potential latency was shorter with an increased ampli-tude in patients treated with donepezil hydrochloride and acupuncture. Mini-Mental State Examination score was also higher. Moreover, these differences in P300 latency were identiifed within different infarcted regions in patients treated with donepezil hydrochloride and acupuncture. These ifndings indicate that acupuncture combined with donepezil hydrochloride noticeably improves cognitive function in patients with vascular dementia, and exerts neuroprotective effects against vascular dementia.

  13. Liquid Chromatographic Methods for the Determination of Vildagliptin in the Presence of its Synthetic Intermediate and the Simultaneous Determination of Pioglitazone Hydrochloride and Metformin Hydrochloride

    OpenAIRE

    El-Bagary, Ramzia I.; Elkady, Ehab F.; Ayoub, Bassam M.

    2011-01-01

    Two reversed-phase liquid chromatographic (RP-LC) methods are described for the determination of two binary mixtures of hypoglycemic agents. In the first method, vildagliptin (VDG) was determined in the presence of 3-amino-1-adamantanol (AAD), a synthetic intermediate and impurity of VDG. In the second method, pioglitazone hydrochloride (PGZ) and metformin hydrochloride (MET) were simultaneously determined in their binary mixture. Chromatographic separation in the two methods was achieved on ...

  14. Chitosan coated vancomycin hydrochloride liposomes: Characterizations and evaluation.

    Science.gov (United States)

    Yang, Zhenlei; Liu, Junli; Gao, Jinhua; Chen, Shilei; Huang, Guihua

    2015-11-10

    The present work evaluated the feasibility of chitosan coated liposomes (c-Lips) for the intravenous delivery of vancomycin hydrochloride (VANH), a water-soluble antibiotic for the treatment of gram-positive bacterial infections like osteomyelitis, arthritis, endocarditis, pneumonia, etc. The objective of this research was to develop a suitable drug delivery system in vivo which could improve therapeutic efficacy and decrease side effects especially nephrotoxicity. Firstly, the vancomycin hydrochloride liposomes (VANH-Lips) were prepared by modified reverse phase evaporation method, then the chitosan wrapped vancomycin hydrochloride liposomes (c-VANH-Lips) nanosuspension was formulated by the method of electrostatic deposition. Based on the optimized results of single-factor screening experiment, the c-VANH-Lips were found to be relatively uniform in size (220.40 ± 3.56 nm) with a narrow polydispersity index (PI) (0.21 ± 0.03) and a positive zeta potential (25.7 ± 1.12 mV). The average drug entrapment efficiency (EE) and drug loading (DL) were 32.65 ± 0.59% and 2.18 ± 0.04%, respectively. The in vitro release profile of c-VANH-Lips possessed a sustained release Characterization and the release behavior was in accordance with the Weibull equation. Hemolysis experiments showed that its intravenous injection had preliminary safety. In vivo, after intravenous injection to mice, c-VANH-Lips showed a longer retention time and higher AUC values compared with the VANH injection (VANH-Inj) and VANH-Lips. In addition, biodistribution results clearly demonstrated that c-VANH-Lips preferentially decreased the drug distribution in kidney of mice after intravenous injection. These results revealed that injectable c-VANH-Lips may serve as a promising carrier for VANH to increase therapeutic efficacy on gram-positive bacterial infections and reduce nephrotoxicity, which provides significantly clinical value for long-term use of VANH.

  15. Multicomposite ultrathin capsules for sustained ocular delivery of ciprofloxacin hydrochloride.

    Science.gov (United States)

    Bhadra, Dipankar; Gupta, Girish; Bhadra, Sulekha; Umamaheshwari, R B; Jain, Narendra

    2004-07-16

    The present work is intended to develop a sustained bioadhesive drug delivery system for delivery of Ciprofloxacin Hydrochloride in Cul-de-Sac for sustained and effective antimicrobial chemotherapy. For this, ultrathin multicomposite capsular systems were selected. Multicomposite ultrathin capsules are molecular assemblies of tailored architecture having layer-by-layer adsorption of oppositely charged macromolecules onto colloidal particles. In the present study colloidal calcium phosphate core and gluateraldehyde fixed RBCs were used as core on which alginate (-vely charged) and polyallylamine hydrochloride (+vely charged) polyelectrolyte coating was deposited alternatively upto 10th layer. The coating in each subsequent layer was determined by changes in zeta potential. Ciprofloxacin hydrochloride was loaded in the capsules by incubation with the capsules suspended in phosphate buffer saline pH 7.4. The cores of the capsules were then removed by treatment with 0.1N HCl for calcium phosphate core and by sodium hypochlorite for RBC cored capsules. The hollow ciprofloxacin HCl loaded capsules were the evaluated in-vitro for pattern of layer-by-layer drug loading, drug release, stability at various temperatures and ionic concentrations and corneal retention. The core removal process was found to have minimal effects on drug loading in capsules. The drug loading was found to be higher for RBC cored hollow capsules and hence release rate was lower as compared to calcium cored hollow capsules. Draize test for corneal irritancy proved that the capsules were not irritating. The capsules were found to deliver the ciprofloxacin in cul-de-sac of rabbit's eyes for prolonged period. Based on corneal retention studies and tear drug concentration, the capsules can be considered for suitable and safe use for sustained ocular delivery of drugs.

  16. Indirect Electrochemical Oxidation of 4-Amino-dimethyl-aniline Hydrochloride

    Institute of Scientific and Technical Information of China (English)

    2006-01-01

    The indirect electrochemical oxidation of 4-amino-dimethyl-aniline hydrochloride containing wastewater generated from vanillin production is presented. Experiments were conducted at a constant current density of 30 mA/cm2 via a Ti/Ru-Ti-Sn ternary oxide coated anode and an undivided reactor. During the various stages of the electrolysis, parameters such as the values of chemical oxygen demand (COD) and total organic carbon (TOC) were determined in order to evaluate the feasibility of the electrochemical treatment. The energy consumption and the current efficiency during the electrolysis were calculated. The present study proves the effectiveness of the electrochemical treatment for wastewater resulted from vanillin production.

  17. Verapamil hydrochloride release characteristics from new copolymer zwitterionic matrix tablets.

    Science.gov (United States)

    Kostova, Bistra; Kamenska, Elena; Ivanov, Ivo; Momekov, George; Rachev, Dimitar; Georgiev, George

    2008-01-01

    The aim of this study was to synthesize stable copolymer (vinyl acetate-co-3-dimethyl[methacryloyloxyethyl] ammonium propane sulfinate) zwitterionic latex with different compositions for the first time by emulsifier-free emulsion copolymerization. Throughout the course of the study, a proposal was made for the explanation of the relationship between the "overshooting" phenomenon (a swelling kinetics with a maximum) and the specific self-association of the zwitterionic copolymers. The zwitterionic monomer unit mole fraction, pH, and ionic strength effects on this relationship, on the swelling kinetics of the zwitterionic copolymers, and on the sustained verapamil hydrochloride release from the model tablets were established by the study's authors.

  18. Biodegradation of drotaverine hydrochloride by free and immobilized cells of Rhodococcus rhodochrous IEGM 608.

    Science.gov (United States)

    Ivshina, I B; Vikhareva, E V; Richkova, M I; Mukhutdinova, A N; Karpenko, Ju N

    2012-10-01

    Drotaverine [1-(3,4-diethoxybenzylidene)-6,7-diethoxy-1,2,3,4-tetrahydroisoquinoline] hydrochloride, an antispasmodic drug derived from benzylisoquinoline was evaluated for its biodegradability using a bacterial strain Rhodococcus rhodochrous IEGM 608. The experiments were performed under aerobic conditions with rhodococci cultures able to degrade drotaverine. In the presence of glucose, the removal efficiency of drotaverine by free Rhodoccocus cells pre-grown with isoquinoline was above 80 % (200 mg/l, initial concentration) after 25 days. Rhodococcus immobilization on hydrophobized sawdust enhanced the biodegradation process, with the most marked drotaverine loss being observed during the first 5 days of fermentation. High metabolic activity of rhodococcal cells towards drotaverine was confirmed respirometrically. GC-MS analysis of transformation products resulting from drotaverine biodegradation revealed 3,4-diethoxybenzoic acid, 3,4-diethoxybenzaldehyde and 3,4-diethoxybenzoic acid ethyl ester which were detected in the culture medium until drotaverine completely disappeared. Based on these major and other minor metabolites, putative pathways for drotaverine biodegradation were proposed. The obtained data broadened the spectrum of organic xenobiotics oxidized by Rhodoccocus bacteria and proved their potential in decontamination of natural ecosystems from pharma pollutants.

  19. Lanthanum carbonate versus sevelamer hydrochloride: improvement of metabolic acidosis and hyperkalemia in hemodialysis patients.

    Science.gov (United States)

    Filiopoulos, Vassilis; Koutis, Ioannis; Trompouki, Sofia; Hadjiyannakos, Dimitrios; Lazarou, Dimitrios; Vlassopoulos, Dimosthenis

    2011-02-01

    Sevelamer hydrochloride (SH) has been reported to aggravate metabolic acidosis and hyperkalemia. This study was performed to evaluate acid-base status and serum potassium changes after replacing SH with lanthanum carbonate (LC) in hemodialysis patients. SH was prescribed for 24 weeks in 14 stable hemodialysis patients and replaced by LC in a similar treatment schedule. Laboratory tests, including indices of acid-base status, nutrition, bone/mineral metabolism, and dialysis adequacy, were performed monthly during the study. Dialysate bicarbonate, potassium and calcium concentrations remained constant. Serum bicarbonate and pH rose, and serum potassium dropped significantly under LC. Alkaline phosphatase also decreased significantly under LC. No significant differences were observed in the other studied parameters between the two treatment periods. Control of serum phosphate was similar under both phosphate-binders and no differences were observed in calcium, Ca × P product, CRP, or lipid levels. Dialysis adequacy was constantly kept within K/DOQI target-range. Although full compliance to treatment was reported, three patients on LC complained of gastrointestinal upset and/or a metallic taste, and four had difficulty chewing the LC tablet. LC improves metabolic acidosis and hyperkalemia in hemodialysis patients previously under SH. Although both medications are well-tolerated, the gastrointestinal side-effects appear to occur more frequently with LC; a fact that, together with difficulties in chewing the tablet, may result in decreased compliance.

  20. Stability of polymorphic forms of ranitidine hydrochloride.

    Science.gov (United States)

    Wu, V; Rades, T; Saville, D J

    2000-07-01

    , resulted in a preferential loss of form II (compared to form I). Loss was greater at 30 degrees C/75% RH than at 20 degrees C/75% RH. Form II was also preferentially lost under low humidity conditions created by a saturated solution of potassium carbonate (45% RH) at the elevated temperature of 42 degrees C. This environment was shown to be acidic.

  1. RP-HPLC analytical method development and optimization for quantification of donepezil hydrochloride in orally disintegrating tablet.

    Science.gov (United States)

    Liew, Kai Bin; Peh, Kok Khiang; Fung Tan, Yvonne Tze

    2013-09-01

    An easy, fast and validated RV-HPLC method was invented to quantify donepezil hydrochloride in drug solution and orally disintegrating tablet. The separation was carried out using reversed phase C-18 column (Agilent Eclipse Plus C-18) with UV detection at 268 nm. Method optimization was tested using various composition of organic solvent. The mobile phase comprised of phosphate buffer (0.01M), methanol and acetonitrile (50:30:20, v/v) adjusted to pH 2.7 with phosphoric acid (80%) was found as the optimum mobile phase. The method showed intraday precision and accuracy in the range of 0.24% to -1.83% and -1.83% to 1.99% respectively, while interday precision and accuracy ranged between 1.41% to 1.81% and 0.11% to 1.90% respectively. The standard calibration curve was linear from 0.125 μg/mL to 16 μg/mL, with correlation coefficient of 0.9997±0.00016. The drug solution was stable under room temperature at least for 6 hours. System suitability studies were done. The average plate count was > 2000, tailing factor method was used to assay donepezil hydrochloride in tablet and dissolution study of in-house manufactured donepezil orally disintegrating tablet and original Aricept.

  2. Analgesic effects of meloxicam, morphine sulfate, flunixin meglumine, and xylazine hydrochloride in African-clawed frogs (Xenopus laevis).

    Science.gov (United States)

    Coble, Dondrae J; Taylor, Douglas K; Mook, Deborah M

    2011-05-01

    We evaluated analgesic use and analgesiometry in aquatic African-clawed frogs (Xenopus laevis). We used the acetic acid test (AAT) to assess the analgesic potential of systemic xylazine hydrochloride, meloxicam, flunixin meglumine, and morphine sulfate after injection into the dorsal lymph sac. Flunixin meglumine provided better analgesia than did the other drugs, most evident at 5 and 9 h after administration. Because the AAT was associated with the development of dermal lesions, we discontinued use of this assay and chose the Hargreaves test as an alternative method of measuring nociception in Xenopus. This assay is commonly performed in rodents, but its efficacy in an aquatic species such as Xenopus was unknown prior to this study. We found that the Hargreaves test was an effective measure of nociception in Xenopus, and we used it to evaluate the effectiveness of the nonopiod agents xylazine hydrochloride, meloxicam, and flunixin meglumine both in the absence of surgery and after surgical oocyte harvest. Similar to findings from the AAT, flunixin meglumine provided better analgesia in the Hargreaves test than did the other agents when analyzed in the absence of surgical intervention. Results were equivocal after oocyte harvest. Although surgical oocyte harvest is a common procedure in Xenopus, and currently there are no published recommendations for analgesia after this invasive surgery. Future studies are needed to clarify the efficacy of nonsteroidal antiinflammatory drugs for that purpose.

  3. Fluorescence studies of the effect of pH, guanidine hydrochloride and urea on equinatoxin II conformation.

    Science.gov (United States)

    Malavasic, M; Poklar, N; Macek, P; Vesnaver, G

    1996-04-01

    The solvent denaturation of equinatoxin II (EqTxII) in aqueous solutions of urea, guanidine hydrochloride (Gu-HCl) and at various pH values was examined by monitoring changes in the protein intrinsic emission fluorescence spectra and in the fluorescence spectra of the added external probe ANS. It has been observed that EqTxII denaturation is reflected in a strong red shift of intrinsic fluorescence emission maxima accompanied by a simultaneous decrease in fluorescence intensity and that guanidine hydrochloride is significantly more powerful denaturant than urea or changing of pH. Comparison of intrinsic fluorescence spectra of EqTxII denatured by one of the three denaturing agents has shown that the fully denatured states of the protein in Gu-HCl and urea are similar and substantially different from those induced by changing of pH. Furthermore, according to the measurements of the ANS-fluorescence in EqTxII solutions as a function of pH the protein exists at pH values below 2.0 in an acid-denatured compact state.

  4. Determination of losartan potassium, quinapril hydrochloride and hydrochlorothiazide in pharmaceutical preparations using derivative spectrophotometry and chromatographic-densitometric method.

    Science.gov (United States)

    Stolarczyk, Mariusz; Maślanka, Anna; Apola, Anna; Krzek, Jan

    2013-01-01

    Two methods, spectrophotometric and chromatographic-densitometric ones, were developed for determination of losartan potassium, quinapril hydrochloride and hydrochlorothiazide in pharmaceutical preparations. Spectrophotometric method involved derivative spectrophotometry and zero order spectrophotometry. The measurements were carried out at lambda = 224.0 nm for quinapril, lambda = 261.0 nm for hydrochlorothiazide and lambda = 270.0 nm for losartan when the derivative spectrophotometry was applied and lambda = 317.0 nm when zero order spectrophotometry was applied for the determination of hydrochlorothiazide. In chromatographic-densitometric studies high performance thin layer chromatography (HPTLC) plates were used as stationary phase and a mixture of solvents n-butanol : acetic acid : water (15 : 5 : 1, v/v/v) as mobile phase. Under the established conditions good resolution of examined constituents was obtained. Retardation factor for quinapril hydrochloride was R(f) - 0.70, for losartan potassium R(f) - 0.85 and for hydrochlorothiazide R(f) - 0.78. The developed methods are characterized by high sensitivity and accuracy. For quantitative analysis, densitometric measurements were carried out at lambda = 218.0 nm for quinapril, lambda = 275.0 nm for hydrochlorothiazide and = 232.0 nm for losartan.

  5. Analgesic Effects of Meloxicam, Morphine Sulfate, Flunixin Meglumine, and Xylazine Hydrochloride in African-Clawed Frogs (Xenopus laevis)

    Science.gov (United States)

    Coble, Dondrae J; Taylor, Douglas K; Mook, Deborah M

    2011-01-01

    We evaluated analgesic use and analgesiometry in aquatic African-clawed frogs (Xenopus laevis). We used the acetic acid test (AAT) to assess the analgesic potential of systemic xylazine hydrochloride, meloxicam, flunixin meglumine, and morphine sulfate after injection into the dorsal lymph sac. Flunixin meglumine provided better analgesia than did the other drugs, most evident at 5 and 9 h after administration. Because the AAT was associated with the development of dermal lesions, we discontinued use of this assay and chose the Hargreaves test as an alternative method of measuring nociception in Xenopus. This assay is commonly performed in rodents, but its efficacy in an aquatic species such as Xenopus was unknown prior to this study. We found that the Hargreaves test was an effective measure of nociception in Xenopus, and we used it to evaluate the effectiveness of the nonopiod agents xylazine hydrochloride, meloxicam, and flunixin meglumine both in the absence of surgery and after surgical oocyte harvest. Similar to findings from the AAT, flunixin meglumine provided better analgesia in the Hargreaves test than did the other agents when analyzed in the absence of surgical intervention. Results were equivocal after oocyte harvest. Although surgical oocyte harvest is a common procedure in Xenopus, and currently there are no published recommendations for analgesia after this invasive surgery. Future studies are needed to clarify the efficacy of nonsteroidal antiinflammatory drugs for that purpose. PMID:21640031

  6. Visible Spectrophotometric determination of Chlorpheniramine maleate and Diphenhydramine hydrochloride in raw and dosage form using Potassium permanganate

    Directory of Open Access Journals (Sweden)

    Mohammed Al Bratty

    2016-05-01

    Full Text Available Two simple, rapid and sensitive spectrophotometric methods developed for Chlorpheniramine Maleate (CPM and Diphenhydramine Hydrochloride (DPH determination in pure and pharmaceutical preparation using Potassium Permanganate. The solvent system used was potassium permanganate. The method developed by adding a known amount of permanganate to CPM and DPH in acid and alkaline medium, the unreacted permanganate was determined at 550 nm; method A and bluish green colour of Manganate at 610 nm; method B. In method A decrease in absorbance or method B increase in absorbance as concentrations of CPM and DPH was measured. Beer’s law was obeyed at a range of 2.5 to 20 μg / ml in both the methods A and B. The method was validated as per International Council for Harmonisation guideline. The proposed methods were effectively used for the determination of CPM and DPH in commercially available syrup. The average percentages of recoveries of CPM were 99.20 ± 1.29% (method A, 100.6% ± 1.43% (method B; DPH 98.50 ± 1.29% (method A and 100.20 ± 1.43% (method B. The methods were efficiently validated and used for quantitative determination of Chlorpheniramine maleate and Diphenhydramine Hydrochloride in pure and syrup preparations.

  7. Effects of betaine hydrochloride on ruminal fermentation in vitro%甜菜碱盐酸盐对人工瘤胃发酵参数的影响

    Institute of Scientific and Technical Information of China (English)

    张善芝; 韩兆玉

    2012-01-01

    采用人工瘤胃体外发酵方法对培养液中甜菜碱盐酸盐不同质量浓度(0、16.7和33.4 mg· L-1)下,各时间段(3、6、12、18和24h)的体外产气量、pH值、干物质降解率、氨态氮(NH3-N)、挥发性脂肪酸(VFA)、乳酸和菌体蛋白含量的测定,探讨甜菜碱盐酸盐对人工瘤胃发酵功能的影响.结果显示:培养液中甜菜碱盐酸盐的质量浓度为33.4 mg· L-1时,瘤胃液中乙酸、丙酸、丁酸、总VFA的浓度显著升高(P<0.01),干物质降解率显著提高(P<0.01),乳酸浓度显著降低(P<0.05);而甜菜碱盐酸盐对瘤胃液pH值、产气量、菌体蛋白含量、NH3-N浓度无显著影响.结论:甜菜碱盐酸盐可改善人工瘤胃发酵性能.%Mixed ruminal liquid and artifial saliva were cultured in anaerobious environment for 24 h in vitro. The betaine hydrochloride was added to the media at different concentrations(0,16. 7 and 33. 4 mg·L-1 ) ,and the gas production in vitro,pH value, the degradation of dry matter, NH3 -N, volatile fatty acids ( VFA ) , lactic acid and bacteria protein productions were detected. The results showed that,when the concentration was 33.4 mg·L-1 ,betaine hydrochloride could increase the concentration of acetic acid,propionate acid,butyric acid and total volatile fatty acids(tVFA) (P0. 05) adding betaine hydrochloride on pH value, gas yield, bacteria protein and NH3 -N concentrations in rumen. Conclusion: the betaine hydrochloride promoted the ruminal fermentation in vitro.

  8. Effect of an oxygen pressure injection (OPI) device on the oxygen saturation of patients during dermatological methyl aminolevulinate photodynamic therapy.

    Science.gov (United States)

    Blake, E; Allen, J; Thorn, C; Shore, A; Curnow, A

    2013-05-01

    Methyl aminolevulinate photodynamic therapy (MAL-PDT) (a topical treatment used for a number of precancerous skin conditions) utilizes the combined interaction of a photosensitizer (protoporphyrin IX (PpIX)), light of the appropriate wavelength, and molecular oxygen to produce singlet oxygen and other reactive oxygen species which induce cell death. During treatment, localized oxygen depletion occurs and is thought to contribute to decreased efficacy. The aim of this study was to investigate whether an oxygen pressure injection (OPI) device had an effect on localized oxygen saturation levels and/or PpIX fluorescence of skin lesions during MAL-PDT. This study employed an OPI device to apply oxygen under pressure to the skin lesions of patients undergoing standard MAL-PDT. Optical reflectance spectrometry and fluorescence imaging were used to noninvasively monitor the localized oxygen saturation and PpIX fluorescence of the treatment area, respectively. No significant changes in oxygen saturation were observed when these data were combined for the group with OPI and compared to the group that received standard MAL-PDT without OPI. Additionally, no significant difference in PpIX photobleaching or clinical outcome at 3 months between the groups of patients was observed, although the group that received standard MAL-PDT demonstrated a significant increase (pMAL-PDT. Further investigation is therefore required to find a more effective method of MAL-PDT enhancement.

  9. Long-term follow-up of metil aminolevulinate (MAL)-PDT in difficult-to-treat cutaneous Bowen's disease.

    Science.gov (United States)

    Cavicchini, Stefano; Serini, Stefano Maria; Fiorani, Roberta; Girgenti, Valentina; Ghislanzoni, Massimo; Sala, Francesco

    2011-08-01

    Bowen's disease (BD) is a form of intraepidermal squamous cell carcinoma, which is clinically characterized by gradually enlarging, well-demarcated erythematous plaques with irregular borders and surface crusting or scaling, affecting primarily the elderly. BD often presents with lesions difficult to treat with standard therapy as surgery, cryosurgery, or 5-fluorouracil (5-FU) for the risk of significantly poor cosmetic outcome, failure rate, and adverse events, related mainly to the age of the patients. Topical PDT with methyl aminolevulinate (MAL) represents a valid and approved therapy for BD lesions in many cases, especially for lesions located at poor healing sites or for large patches of disease, due to its high efficacy coupled with good tolerability and tissue-sparing attitude. In this study, we sought to investigate the efficacy, safety, and cosmetic outcome of MAL-PDT in a series of patients with BD lesions which were challenging to treat for clinical, surgical, and patient-related reasons, such as size of the lesion, difficult surgical approach for anatomical sites, or age of patients and request of the best cosmetic result. We also performed a long-term follow-up to assess recurrence rates and eventual late-onset adverse events.

  10. [Examination of effectiveness of olopatadine hydrochloride in atopic dermatitis].

    Science.gov (United States)

    Shimizu, Tadamichi; Mashiko, Maki; Shimizu, Hiroshi

    2005-02-01

    Subjective/objective symptoms (itching, papula, erythema, lichenification, desquamation, scratching, erosion) and the levels of IgE, LDH, interleukin (IL) -6, thymus and activation-regulated chemokine (TARC) were compared before and after administering olopatadine hydrochloride (ALLELOCK tablets) to 17 atopic dermatitis (AD) patients. Subject/objective symptoms improved significantly after administering the agent, and the total dosage of the combined topical steroids was also significantly decreased after administration (p<0.05), although IgE, IL-6 and LDH levels did not change, TARC was significantly decreased (p<0.05). The correlation between the levels of IgE, IL-6, LDH and TARC before and after the administration was examined. There was a positive correlation between IgE and TARC (r=0.62, p<0.01) and between IL-6 and TARC (r=0.78, p<0.01). Olopatadine hydrochloride is therefore useful in improving the symptoms in AD, and TARC may be used as an indicator of the symptom improvement.

  11. Growth of glycine ethyl ester hydrochloride and its characterizations

    Science.gov (United States)

    Venkatesan, G.; Pari, S.

    2016-11-01

    Single crystal of glycine ethyl ester hydrochloride by slow evaporation method is reported. The grown crystal characterized by single crystal X-ray diffraction, FT-IR, UV-Vis-NIR and fluorescence spectroscopy. It is established that the crystal falls under the monoclinic system and space group P21/c with the cell parameters as: a=8.565 Å, b=12.943 Å, c=6.272 Å, α=γ=90°, β=103.630º. UV-Vis-NIR spectrum shows indirect allowed transition with a band gap of 5.21 eV and other optical properties are measured. The crystal is also shown to have a high transmittance in the visible region. The third order nonlinear property and optical limiting have been investigated using Z-Scan technique. Complex impedance spectrum measured at the dc conductivity. Dependence of dielectric constant, dielectric loss and ac conductivity on frequency at different temperature of applied ac field is analyzed. The mechanical behavior has been assessed by Vickers microhardness indenter. The thermal behavior of glycine ethyl ester hydrochloride was analyzed using TG/DTA thermal curves. From the thermal study, the material was found to possess thermal stability up to 174 °C. The predicted NLO properties, UV-Vis transmittance and Z-scan studies indicate that is an attractive material for photonics optical limiting applications.

  12. SPECTROPHOTOMETRIC, ATOMIC ABSORPTION AND CONDUCTOMETRIC ANALYSIS OF TRAMADOL HYDROCHLORIDE

    Directory of Open Access Journals (Sweden)

    Sara M. Anis

    2011-09-01

    Full Text Available Six simple and sensitive spectroscopic and conductometric procedures (A-F were developed for the determination of tramadol hydrochloride. Methods A, B and C are based on the reaction of cobalt (II thiocyanate with tramadol to form a stable ternary complex, which could be measured by spectrophotometric (method A, atomic absorption (method B or conductometric (method C procedures. Methods D and E depend on the reaction of molybdenum thiocyanate with tramadol to form a stable ternary complex, measured by spectrophotometric means (method D or by atomic absorption procedures (method E, while method F depends on the formation of an ion pair complex between the studied drug and bromothymol blue which is extractable into methylene chloride. Tramadol hydrochloride could be assayed in the range of 80-560 and 40-–220 μg ml-1, 1-15 mg ml-1 and 2.5-22.5, 1.25-11.25 and 5-22 μg ml-1 using methods A,B,C,D,E and F, respectively. Various experimental conditions were studied. The results obtained showed good recoveries. The proposed procedures were applied successfully to the analysis of tramadol in its pharmaceutical preparations and the results were favorably comparable with the official method.

  13. FORMULATION AND DISSOLUTION STUDY OF DILTIAZEM HYDROCHLORIDE IMMEDIATE RELEASE TABLETS

    Directory of Open Access Journals (Sweden)

    BRAHMAIAH BONTHAGARALA

    2014-08-01

    Full Text Available Objective: The main aim and objective of the work is to formulate immediate release tablets using different direct compression vehicles (DCV’S in different ratios. Methods: In the present study, design of oral immediate release tablets of Diltiazem hydrochloride by direct compression technique was carried out. Results: The main motive is to compare the dissolution profile of these formulations and conclude the best formulation which release drug at a faster rate . To determine the best fit dissolution profile for the dosage forms. Diltiazem hydrochloride tablets were formulated by using microcrystalline cellulose (diluent, potato starch, acacia (binder and magnesium stearate (lubricant. The granules were compressed into tablets and were subjected to dissolution studies. The dissolution profile of the formulation F2 was found to have better dissolution rate compared to others. Conclusion: The Invitro dissolution studies of all the formulations were conducted and the results were obtained, it was concluded that formulation F2 was the best with fast release of drug compared to others.

  14. Modulation of venlafaxine hydrochloride release from press coated matrix tablet

    Directory of Open Access Journals (Sweden)

    Gohel M

    2008-01-01

    Full Text Available The aim of present study was to prepare novel modified release press coated tablets of venlafaxine hydrochloride. Hydroxypropylmethylcellulose K4M and hydroxypropylmethylcellulose K100M were used as release modifier in core and coat, respectively. A 3 2 full factorial design was adopted in the optimization study. The drug to polymer ratio in core and coat were chosen as independent variables. The drug release in the first hour and drug release rate between 1 and 12 h were chosen as dependent variables. The tablets were characterized for dimension analysis, crushing strength, friability and in vitro drug release. A check point batch, containing 1:2.6 and 1:5.4 drug to polymer in core and coat respectively, was prepared. The tablets of check point batch were subjected to in vitro drug release in dissolution media with pH 5, 7.2 and distilled water. The kinetics of drug release was best explained by Korsmeyer and Peppas model (anomalous non-Fickian diffusion. The systematic formulation approach enabled us to develop modified release venlafaxine hydrochloride tablets.

  15. TRIMETAZIDINE HYDROCHLORIDE TRANSDERMAL PATCH: FORMULATION AND IN-VITRO EVALUATION

    Directory of Open Access Journals (Sweden)

    Sarfaraz Md

    2012-07-01

    Full Text Available The present study was carried out to formulate and evaluate matrix-type transdermal formulations containing trimetazidine hydrochloride with polymers such as carboxymethyl chitosan and hydroxypropylmethylcellulose (HPMC 5cps by solvent evaporation technique with glycerin, as plasticizer. The prepared patches were tested for their physicochemical characteristics such as thickness, weight variation, drug content uniformity, folding endurance and tensile strength. The partition coefficient study was performed using n-octanol as the organic phase and phosphate buffer pH 7.4 as an aqueous phase and it was found to be 1.01. In-vitro release studies of trimetazidine hydrochloride-loaded patches in phosphate buffer (pH, 7.4 exhibited drug release in the range of 89.40 to 92.10 % in 24 hrs. The parameter flux (J was calculated and it was in the range of 1.325 to 2.898 mg/cm2/hr. Based on optimization studies, patches containing carboxymethyl chitosan patches were chosen as optimized formulation. Skin irritation studies were performed on optimized transdermal patch and were found to be free of irritation. The patches were subjected to short term stability studies and were found stable. FTIR studies revealed no interactions between drug and excipients. Data of in vitro release from optimized patches were fit in to different equations and kinetic models such as zero order, first-order, Higuchi and Korsmeyer-Peppas models to explain release kinetics.

  16. 维拉佐酮盐酸盐%vilazodone hydrochloride

    Institute of Scientific and Technical Information of China (English)

    李赛

    2011-01-01

    由Trovis Pharma LLC制药公司研制的维拉佐酮盐酸盐(vilazodone hydrochloride)于2011年1月21日由FDA批准上市,商品名为Viibryd,用于治疗成年人重度抑郁症(major depressive disorder,MDD)[1].Viibryd将以10 mg、20 mg和40 mg片剂上市.Viibryd中文化学名称:5-[4-[4-(5-氰基-1H-吲哚-3-基)丁基]-1-哌嗪基]-2-苯并呋喃草酰胺盐酸盐;英文化学名称:5-[4-[4-(5-cyano-1 H-indol-3-yl)butyl]-1 -piperaz-inyl]-2-benzofurancarboxamide hydrochloride;分子式:C26-H27N5O2 ·HCl;分子量:477.99;CAS登记号:163521-08-2.

  17. Structural characterisation and dehydration behaviour of siramesine hydrochloride.

    Science.gov (United States)

    Zimmermann, Anne; Tian, Fang; de Diego, Heidi Lopez; Frydenvang, Karla; Rantanen, Jukka; Elema, Michiel Ringkjøbing; Hovgaard, Lars

    2009-10-01

    In this study the crystal structures of siramesine hydrochloride anhydrate alpha-form and siramesine hydrochloride monohydrate were determined, and this structural information was used to explain the physicochemical properties of the two solid forms. In the crystal structure of the monohydrate, each water molecule is hydrogen bonded to two chloride ions, and thus the water is relatively strongly bound in the crystal. No apparent channels for dehydration were observed in the monohydrate structure, which could allow transmission of structural information during dehydration. Instead destructive dehydration occurred, where the elimination of water from the monohydrate resulted in the formation of an oily phase, which subsequently recrystallised into one or more crystalline forms. Solubility and intrinsic dissolution rate of the anhydrate alpha-form and the monohydrate in aqueous media were investigated and both were found to be lower for the monohydrate compared to the anhydrate alpha-form. Finally, the interactions between water molecules and chloride ions in the monohydrate as well as changes in packing induced by water incorporation could be detected by spectroscopic techniques.

  18. OPTIMIZATION OF CONCENTRATION OF POLYHEXANIDE HYDROCHLORIDE IN MULTIPURPOSE SOLUTION.

    Directory of Open Access Journals (Sweden)

    A. Arora

    2010-01-01

    Full Text Available There are a number of foreign pathogenic microorganisms like viruses, bacteria, yeast, fungi and protozoa which can inadvertently be introduced into eye via contact lens and hence disinfection is a vital part. Multifunctional solutions are generally intended to combine the action of cleaning disinfecting, rinsing lubricating deproteinising and soaking in one single product.In order to optimization of concentration of Polyhexanide hydrochloride in multipurpose solution some microbiological studies were performed by taking five microorganisms which are more prevalent in the infected eye condition. The nutrient agar and sabourad's agar media were used for bacteria and yeast mould respectively. The media were prepared as per I.P and sterilised by autoclaving and poured into Petri plates. The media when cooled to 42°C, 0.5 ml of the culture was added.The optimum concentration of Polyhexanide hydrochloride is 0.0002% which is an effective concentration against five microorganisms that are most prevalent in the infected eye condition.It was concluded that the multipurpose solution containing 2.0 g/ml of polyhexanide were found to be better in terms of antimicrobial activity

  19. Modulation of venlafaxine hydrochloride release from press coated matrix tablet.

    Science.gov (United States)

    Gohel, M C; Soni, C D; Nagori, S A; Sarvaiya, K G

    2008-01-01

    The aim of present study was to prepare novel modified release press coated tablets of venlafaxine hydrochloride. Hydroxypropylmethylcellulose K4M and hydroxypropylmethylcellulose K100M were used as release modifier in core and coat, respectively. A 3(2) full factorial design was adopted in the optimization study. The drug to polymer ratio in core and coat were chosen as independent variables. The drug release in the first hour and drug release rate between 1 and 12 h were chosen as dependent variables. The tablets were characterized for dimension analysis, crushing strength, friability and in vitro drug release. A check point batch, containing 1:2.6 and 1:5.4 drug to polymer in core and coat respectively, was prepared. The tablets of check point batch were subjected to in vitro drug release in dissolution media with pH 5, 7.2 and distilled water. The kinetics of drug release was best explained by Korsmeyer and Peppas model (anomalous non-Fickian diffusion). The systematic formulation approach enabled us to develop modified release venlafaxine hydrochloride tablets.

  20. Formulation and evaluation of transdermal patches of papaverine hydrochloride

    Directory of Open Access Journals (Sweden)

    Shah Samip

    2010-01-01

    Full Text Available Transdermal patches of papaverine hydrochloride were prepared by the solvent casting method using ethyl cellulose: PVP, PVA: PVP and Eudragit RL-100: Eudragit RS-100 using different ratios. The physicochemical parameters such as flexibility, thickness, smoothness, weight variation, moisture content, hardness and tensile strength were evaluated for the prepared patches. The formulation exhibited flexibility, uniform thickness and weight, smoothness, good drug content (92 to 96%, and little moisture content. The in vitro diffusion studies were carried out using modified Keshery-Chein cell using cellophane as the diffusion membrane and the formulation followed the Higuchi diffusion mechanism. The formulation containing PVA: PVP as polymers showed faster release rate (hydrophilic polymers compared to Eudragit RL-100: Eudragit RS-100 (hydrophobic polymers or combination of hydrophilic and hydrophobic polymers (ethyl cellulose and PVP. The stability studies indicated that all the patches maintained good physicochemical properties and drug content after storing the patches in different storage conditions. Compatibility studies indicated that there was no interaction between the drug and polymers. In vivo studies showed that papaverine hydrochloride helps in decreasing the effect of isoproterenol-induced myocardial necrosis. Hence, the aim of the present study was to prepare the sustained release formulation (Transdermal patches of the drug using different blend of polymers. The formulated patches containing the hydroplilic polymers showed best release rate of drug.

  1. Formulation and evaluation of tramadol hydrochloride rectal suppositories

    Directory of Open Access Journals (Sweden)

    Saleem M

    2008-01-01

    Full Text Available Rectal suppositories of tramadol hydrochloride were prepared using different bases and polymers like PEG, cocoa butter, agar and the effect of different additives on in vitro release of tramadol hydrochloride was studied. The agar-based suppositories were non-disintegrating/non-dissolving, whereas PEGs were disintegrating/dissolving and cocoa butter were melting suppositories. All the prepared suppositories were evaluated for various physical parameters like weight variation, drug content and hardness. The PEG and cocoa butter suppositories were evaluated for macromelting range, disintegration and liquefaction time. In vitro release study was performed by USP type I apparatus. The prepared suppositories were within the permissible range of all physical parameters. In vitro drug release was in the order of PEG>Agar>cocoa butter. Addition of PVP, HPMC in agar suppositories retards the release. The mechanism of drug release was diffusion controlled and follows first order kinetics. The results suggested that blends of PEG of low molecular weight (1000 with high molecular weight (4000 and 6000 in different percentage and agar in 10% w/w as base used to formulate rapid release suppositories. The sustained release suppositories can be prepared by addition of PVP, HPMC in agar-based suppositories and by use of cocoa butter as base.

  2. A novel and rapid microbiological assay for ciprofloxacin hydrochloride

    Institute of Scientific and Technical Information of China (English)

    Edith Cristina Laignier Cazedey; Hérida Regina Nunes Salgado

    2013-01-01

    The present work reports a simple, fast and sensitive microbiological assay applying the turbidimetric method for the determination of ciprofloxacin hydrochloride (CIPRO HCl) in ophthalmic solutions. The validation method yielded good results and included excellent linearity, precision, accuracy and specificity. The bioassay is based on the inhibitory effect of CIPRO HCl upon the strain of Staphylococcus epidermidis ATCC 12228 used as the test microorganism. The results were treated statistically by analysis of variance (ANOVA) and were found to be linear (r¼0.9994, in the range of 14.0-56.0 mg/mL), precise (intraday RSD%¼2.06;interday RSD%¼2.30) and accurate (recovery ¼ 99.7%). The turbidimetric assay was compared to the UV spectrophotometric and HPLC methods for the same drug. The turbidimetric bioassay described on this paper for determination of ciprofloxacin hydrochloride in ophthalmic solution is an alternative to the physicochemical methods disclosed in the literature and can be used in quality control routine.

  3. Growth of glycine ethyl ester hydrochloride and its characterizations

    Energy Technology Data Exchange (ETDEWEB)

    Venkatesan, G.; Pari, S., E-mail: sparimyur@gmail.com

    2016-11-15

    Single crystal of glycine ethyl ester hydrochloride by slow evaporation method is reported. The grown crystal characterized by single crystal X-ray diffraction, FT-IR, UV–Vis–NIR and fluorescence spectroscopy. It is established that the crystal falls under the monoclinic system and space group P21/c with the cell parameters as: a=8.565 Å, b=12.943 Å, c=6.272 Å, α=γ=90°, β=103.630º. UV–Vis–NIR spectrum shows indirect allowed transition with a band gap of 5.21 eV and other optical properties are measured. The crystal is also shown to have a high transmittance in the visible region. The third order nonlinear property and optical limiting have been investigated using Z-Scan technique. Complex impedance spectrum measured at the dc conductivity. Dependence of dielectric constant, dielectric loss and ac conductivity on frequency at different temperature of applied ac field is analyzed. The mechanical behavior has been assessed by Vickers microhardness indenter. The thermal behavior of glycine ethyl ester hydrochloride was analyzed using TG/DTA thermal curves. From the thermal study, the material was found to possess thermal stability up to 174 °C. The predicted NLO properties, UV–Vis transmittance and Z-scan studies indicate that is an attractive material for photonics optical limiting applications.

  4. Intestinal Anisakiasis Treated Successfully with Prednisolone and Olopatadine Hydrochloride

    Directory of Open Access Journals (Sweden)

    Hideki Toyoda

    2016-02-01

    Full Text Available The clinical characteristic of gastrointestinal anisakiasis is severe abdominal pain after eating raw fish. Intestinal anisakiasis is more uncommon than gastric anisakiasis. Most patients with intestinal anisakiasis need hospitalization because anisakiasis can cause intestinal obstruction, ileus, peritonitis or intestinal perforation. We report a case of intestinal anisakiasis. A 43-year-old woman presented with symptoms of intermittent abdominal pain 2 days after eating raw fish. Her brother had eaten the same food and had been suffering from gastric anisakiasis. Abdominal ultrasonography in this patient showed localized jejunal wall thickening with dilated lumen of proximal jejunum and ascites. According to the clinical course and examinations, she was diagnosed with intestinal anisakiasis. Administration of prednisolone 5 mg/day and olopatadine hydrochloride 10 mg/day improved her symptoms quickly without hospitalization. Prednisolone was administered for 10 days, and olopatadine hydrochloride was administered for a total of 6 weeks according to ultrasonographic findings. Six months after the treatment, the abdominal ultrasonography demonstrated normal findings. This case demonstrates that ultrasonography was quite useful for the diagnosis and surveillance of intestinal anisakiasis. Furthermore, treatment with corticosteroid and an antiallergic agent could be an option for patients with intestinal anisakiasis.

  5. Structural characterization of anhydrous naloxone- and naltrexone hydrochloride by high resolution laboratory X-ray powder diffraction and thermal analysis.

    Science.gov (United States)

    Sugimoto, Kunihisa; Dinnebier, Robert E; Zakrzewski, Marek

    2007-12-01

    The crystal structures of the analgesic compounds anhydrous naloxone and naltrexone hydrochloride were determined ab initio from high resolution laboratory X-ray powder diffraction data. Both compounds crystallize in the orthorhombic space group P2(1)2(1)2(1) with lattice parameters of a = 14.6588(10) A, b = 17.4363(9) A, c = 7.96200(22) A, and V = 2035.06(23) A(3) for naloxone hydrochloride and a = 15.4560(5) A, b = 14.9809(4) A, c = 7.84121(18) A, and V = 1815.58(11) A(3) for naltrexone hydrochloride. The crystal structure of anhydrous naloxone hydrochloride forms one-dimensional chains through hydrogen bonds. In the crystal structure of anhydrous naltrexone hydrochloride, two-dimensional sheets are formed by hydrogen bonds. The dehydration processes of naloxone hydrochloride dehydrate and naltrexone hydrochloride tetrahydrate was analyzed by DTA, DSC, TG, and MG.

  6. Ambulant photodynamic therapy of superficial malignomas with 5-ALA in combination with folic acid and use of noncoherent light.

    Science.gov (United States)

    Jindra, R H; Kubin, A; Kolbabek, H; Alth, G; Dobrowsky, W

    1999-01-01

    This study reports our first results of ambulant photodynamic treatment with 5-aminolevulinic acid (5-ALA) in combination with folic acid and subsequent illumination with a noncoherent light source. The compound was topically applied to avoid total body skin sensitivity which occurs in the case of systemic administration. If no therapeutic response could be proved, we added folic acid to 5-ALA for a further treatment attempt. Illumination was performed by broad band red thermic light to also excitate reaction products with absorption bands located near to that of the sensitizer. As a result, we observed a response in all cases, however, in some cases only after the addition of folic acid.

  7. Efficacy of benzydamine hydrochloride dripping at endotracheal tube cuff for prevention of postoperative sore throat.

    Science.gov (United States)

    Nimmaanrat, Sasikaan; Chokkijchai, Kedsirin; Chanchayanon, Thavat

    2013-10-01

    Postoperative sore throat (POST) is a frequent consequence following ETT intubation, which may negatively affect the postoperative course and patient satisfaction. Benzydamine hydrochloride is a topically-applied non-steroidal anti-inflammatory drug (NSAID). The authors evaluated the analgesic effect of benzydamine hydrochloride dripping on the ETT cuff on POST. Eighty-six patients participated in this randomized controlled trial. They were assigned into either the benzydamine hydrochloride or the control group. The whole ETT cuff was dripped either with 3 ml (4.5 mg) of benzydamine hydrochloride or nothing five minutes prior to anesthesia induction. The incidence and severity of POST at 0, 2, 4, 6, 12 and 24 hours postoperatively were assessed. The potential adverse effects of benzydamine hydrochloride (throat numbness throat burning sensation, dry mouth, and thirst) were also evaluated. Twenty-five patients (58.14%) in each group had POST (p-value = 1). The severity of POST (calculated from affected patients) in both groups at different time points was not significantly different. Patients in the benzydamine hydrochloride group did not have a higher incidence of adverse effects. We found that dripping benzydamine hydrochloride on the ETT cuff neither reduced the incidence of POST nor increased the incidence of adverse effects in comparison with no intervention.

  8. Developmental rates of immatures of three Chrysomya species (Diptera: Calliphoridae) under the effect of methylphenidate hydrochloride, phenobarbital, and methylphenidate hydrochloride associated with phenobarbital.

    Science.gov (United States)

    Rezende, Fábio; Alonso, Marcela A; Souza, Carina M; Thyssen, Patrícia J; Linhares, Arício X

    2014-05-01

    Entomotoxicology is focused on obtaining data on necrophagous entomofauna, for criminal investigations purposes. This study aimed to evaluate the effect of different concentrations of methylphenidate hydrochloride, phenobarbital, and their association on the developmental rate, larval and pupal survivorship, and the interval of emergence of adults of Chrysomya albiceps (Wiedemann), Chrysomya megacephala (Fabricius), and Chrysomya putoria (Wiedemann) (Diptera: Calliphoridae). Considering the therapeutic dose (TD) of methylphenidate hydrochloride (0.29 mg/Kg), the concentrations tested were 10× TD, 50× TD, and 100× TD. For phenobarbital, the concentrations used were 1× TD (=150 mg/Kg), 3.3× TD, and 6.7× TD. For the association of the drugs, the combinations used were 10× TD-methylphenidate hydrochloride plus 1× TD-phenobarbital, 50× TD-methylphenidate hydrochloride plus 3.3× TD-phenobarbital, and 100× TD-methylphenidate hydrochloride plus 6.7× TD-phenobarbital. The control group, without addition of drug, was maintained under the same conditions of temperature (25 ± 1 °C), humidity (70 ± 10%), and photoperiod (12 h). Specimens of each group were weighed every 12 h until pupariation. The developmental rate of the three Chrysomya species immatures was monitored. For C. albiceps the developmental time was delayed in 24 h for methylphenidate hydrochloride group and in 12 h for the phenobarbital and the drugs association groups. The effect was observed only at specific ages for C. megacephala, without altering the developmental time. For C. putoria, the developmental time was delayed in 12 h for methylphenidate hydrochloride group and in 24 h for the phenobarbital and the drugs association groups. The emergence interval was similar among all experimental groups, but larval and pupal viabilities were affected in different ways.

  9. Comparative effects of zilpaterol hydrochloride and ractopamine hydrochloride on live performance and carcass characteristics of calf-fed Holstein steers.

    Science.gov (United States)

    Brown, T R; Sexten, A K; Lawrence, T E; Miller, M F; Thomas, C L; Yates, D A; Hutcheson, J P; Hodgen, J M; Brooks, J C

    2014-09-01

    Holstein steers (n = 2,275) were assigned to 1 of 3 treatments: 1) a control diet containing no β-agonists, 2) a diet that contained zilpaterol hydrochloride (ZH; 8.3 mg/kg [100% DM basis]) for 20 d with a 3-d withdrawal period before harvest, and 3) a diet that contained ractopamine hydrochloride (RH; 30.1 mg/kg [100% DM basis]) for 28 d before harvest. No differences (P ≥ 0.18) were detected between treatments for initial BW, BW at d 28, or DMI. Final BW, BW gain for the last 28 d, total BW gain, ADG for the last 28 d, and overall ADG were greater (P Feeding either β-agonist to calf-fed Holstein steers increased live performance through increased BW, BW gain, and ADG. Furthermore, supplementing calf-fed Holstein steers with ZH provides greater improvements in HCW, LM area, and yield grade components, with a slight decrease in quality grade when compared to calf-fed Holstein steers supplemented with RH.

  10. Antitumor efficacy of poly(dimer acid-dodecanedioic acid) copolymer in mice bearing Sarcoma-180 tumor.

    Science.gov (United States)

    Guo, Wen-Xun; Shi, Zongli; Zeng, Fan-Bing; Liang, Kui; Chen, Xian-Hong; Ai, Yong-Ping; Fang, Min; Sun, Xiao; Zhang, Zhi; Hu, Li-Xin

    2007-08-01

    The drug release profiles of poly(dimer acid-dodecanedioic acid) P(DA-DDDA) copolymer containing 5% adriamycin hydrochloride (ADM) in vitro were evaluated. The biocompatibility of P(DA-DDDA) under mice skin was also evaluated, macroscopic observation and microscopic analysis demonstrated that the copolymer is biocompatible and well tolerated in vivo. Antitumor efficacy of P(DA-DDDA) copolymers containing 5% adriamycin hydrochloride (ADM) implanted subcutaneously in mice bearing Sarcoma-180 tumor exhibited increased volume doubling time (VDT) (31 +/- 1.5 days) compared to plain subcutaneous injection of ADM (7 +/- 0.9 days). The studies suggest that P(DA-DDDA) copolymer as an effective carrier for antineoplastic drug like adriamycin hydrochloride has a very good prospect in the treatment of noumenon tumors.

  11. In Vivo Non-Invasive Evaluation of Actinic Keratoses Response to Methyl-Aminolevulinate-Photodynamic Therapy (MAL-PDT) by Reflectance Confocal Microscopy

    OpenAIRE

    Marina Venturini; Arianna Zanca; Piergiacomo Calzavara-Pinton

    2014-01-01

    Photodynamic therapy (PDT) with methyl-aminolevulinate (MAL) is an approved non-invasive treatment option for actinic keratoses (AKs). In vivo reflectance confocal microscopy (RCM) is a non-invasive tool for real-time imaging of epidermis and superficial dermis in vivo that has been previously reported to facilitate the in vivo evaluation of skin lesions, including AKs. The aim of this study was to investigate the use of in vivo RCM in evaluating AKs response to MAL-PDT. For this reason a tot...

  12. Release behavior and kinetic evaluation of berberine hydrochloride from ethyl cellulose/chitosan microspheres

    Science.gov (United States)

    Zhou, Hui-Yun; Cao, Pei-Pei; Zhao, Jie; Wang, Zhi-Ying; Li, Jun-Bo; Zhang, Fa-Liang

    2014-12-01

    Novel ethyl cellulose/chitosan microspheres (ECCMs) were prepared by the method of w/o/w emulsion and solvent evaporation. The microspheres were spherical, adhesive, and aggregated loosely with a size not bigger than 5 μm. The drug loading efficiency of berberine hydrochloride (BH) loaded in microspheres were affected by chitosan (CS) concentration, EC concentration and the volume ratio of V(CS)/ V(EC). ECCMs prepared had sustained release efficiency on BH which was changed with different preparation parameters. In addition, the pH value of release media had obvious effect on the release character of ECCMs. The release rate of BH from sample B was only a little more than 30% in diluted hydrochloric acid (dHCl) and that was almost 90% in PBS during 24 h. Furthermore, the drug release data were fitted to different kinetic models to analyze the release kinetics and the mechanism from the microspheres. The released results of BH indicated that ECCMs exhibited non-Fickian diffusion mechanism in dHCl and diffusion-controlled drug release based on Fickian diffusion in PBS. So the ECCMs might be an ideal sustained release system especially in dHCl and the drug release was governed by both diffusion of the drug and dissolution of the polymeric network.

  13. A degradation study of cefepime hydrochloride in solutions under various stress conditions by TLC-densitometry.

    Science.gov (United States)

    Dąbrowska, Monika; Starek, Małgorzata; Krzek, Jan; Papp, Elżbieta; Król, Piotr

    2015-03-01

    A rapid, accurate and sensitive thin-layer chromatography (TLC) method with densitometric detection has been developed and validated for the determination of cefepime in pharmaceuticals. Chromatographic separation was achieved on a silica gel TLC F254 plates with a mobile phase consisting of ethanol-2-propanol-glacial acetic acid 99.5%-water (4:4:1:3, v/v). Densitometric detection was carried out at wavelength of 266 nm in reflectance/absorbance mode. The validation of the method was found to be satisfactory with high accuracy (from 99.24 to 101.37%) and precision (RSD from 0.06 to 0.36%). Additionally, the stability of cefepime in solution was investigated, including the effect of pH, temperature and incubation time. Favorable retention parameters (Rf , Rs, α) were obtained under the developed conditions, which guaranteed good separation of the studied components. The degradation process of cefepime hydrochloride was described by kinetic and thermodynamic parameters (k, t0.1 , t0.5 and Ea ). Moreover, the chemical properties of degradation products were characterized by the Rf values, absorption spectra, HPLC-MS/MS and TLC-densitometry analysis. As the method could effectively separate the active substance from its main degradation product (1-methylpyrrolidine), it can be employed as a method to indicate the stability of this drug. Copyright © 2014 John Wiley & Sons, Ltd.

  14. Simultaneous determination of amlodipine besylate and benazepril hydrochloride in pharmaceutical dosage form by LC.

    Science.gov (United States)

    Kasawar, Gajanan B; Farooqui, Mazahar N

    2009-12-01

    A rapid, precise, specific, and accurate ultra performance liquid chromatography (UPLC) method has been developed and subsequently validated for simultaneous determination of amlodipine present as amlodipine basylate (AB) and benazepril hydrochloride (BH) in capsule dosage form. The chromatographic separation was achieved on an Acquity UPLC, BEH C8 (100 mm x 2.1 mm, 1.7 microm) column using a photodiode array detector. The mobile phase used consisted of a mixture of phosphate buffer pH 3.0 (0.01 M aqueous potassium dihydrogen phosphate, pH 3.0 adjusted with orthophosphoric acid) and solvent mixture (equal mixture of acetonitrile and methanol) in the ratio of 45:55 (v/v) at a flow rate of 0.3 mL/min. The described method was linear over ranges of 5.21-15.63 microg/mL for AB and 20.24-60.72 microg/mL for BH. The mean recoveries were 100.47 and 99.97% for AB and BH, respectively. The lower limit of quantification was determined on the basis of signal-to-noise ratio method; it is 0.01 microg/mL for AB and 0.019 microg/mL for BH.

  15. Electrospinning of PLGA/gum tragacanth nanofibers containing tetracycline hydrochloride for periodontal regeneration.

    Science.gov (United States)

    Ranjbar-Mohammadi, Marziyeh; Zamani, M; Prabhakaran, M P; Bahrami, S Hajir; Ramakrishna, S

    2016-01-01

    Controlled drug release is a process in which a predetermined amount of drug is released for longer period of time, ranging from days to months, in a controlled manner. In this study, novel drug delivery devices were fabricated via blend electrospinning and coaxial electrospinning using poly lactic glycolic acid (PLGA), gum tragacanth (GT) and tetracycline hydrochloride (TCH) as a hydrophilic model drug in different compositions and their performance as a drug carrier scaffold was evaluated. Scanning electron microscopy (SEM) results showed that fabricated PLGA, blend PLGA/GT and core shell PLGA/GT nanofibers had a smooth and bead-less morphology with the diameter ranging from 180 to 460 nm. Drug release studies showed that both the fraction of GT within blend nanofibers and the core-shell structure can effectively control TCH release rate from the nanofibrous membranes. By incorporation of TCH into core-shell nanofibers, drug release was sustained for 75 days with only 19% of burst release within the first 2h. The prolonged drug release, together with proven biocompatibility, antibacterial and mechanical properties of drug loaded core shell nanofibers make them a promising candidate to be used as drug delivery system for periodontal diseases.

  16. Application of potassium permanganate to spectrophotometric assay of metoclopramide hydrochloride in pharmaceuticals

    Science.gov (United States)

    Devi, O. Zenita; Basavaiah, K.; Vinay, K. B.

    2012-01-01

    Two simple, sensitive, and cost-effective spectrophotometric methods are described for the determination of metoclopramide hydrochloride (MCP) in pharmaceutical dosage forms. The methods are based on a redox reaction between MCP and KMnO4 in alkaline and acid media. Direct spectrophotometry (method A) involves treating MCP with permanganate in an NaOH medium and measuring a bluish green product at 610 nm. In indirect spectrophotometry (method B), MCP is treated with a fixed concentration of KMnO4 in an H2SO4 medium, and after a specified time, the unreacted KMnO4 is measured at 545 nm. Under optimum assay conditions, Beer's law is obeyed over the ranges of 0.75-12.0 and 2.5-30.0 g/ml for methods A and B, respectively. Molar absorptivity values are calculated to be 2.33•104 and 2.66•104 l/mol cm for methods A and B, respectively, and corresponding Sandell's sensitivity values are 0.015 and 0.013 g/cm2. Limits of detection (LOD) and quantification (LOQ) are also reported. The applicability of the developed methods was demonstrated by the determination of MCP in tablet and injection forms. The accuracy and reliability of the proposed methods were further ascertained by recovery studies via standard addition technique.

  17. Simultaneous determination of phenylephrine hydrochloride, guaifenesin, and chlorpheniramine maleate in cough syrup by gradient liquid chromatography.

    Science.gov (United States)

    Amer, Sawsan M; Abbas, Samah S; Shehata, Mostafa A; Ali, Nahed M

    2008-01-01

    A simple and reliable high-performance liquid chromatographic method was developed for the simultaneous determination of mixture of phenylephrine hydrochloride (PHENYL), guaifenesin (GUAIF), and chlorpheniramine maleate (CHLO) either in pure form or in the presence of methylparaben and propylparaben in a commercial cough syrup dosage form. Separation was achieved on a C8 column using 0.005 M heptane sulfonic acid sodium salt (pH 3.4 +/- 0.1) and acetonitrile as a mobile phase by gradient elution at different flow rates, and detection was done spectrophotometrically at 210 nm. A linear relationship in the range of 30-180, 120-1800, and 10-60 microg/mL was obtained for PHENYL, GUAIF, and CHLO, respectively. The results were statistically analyzed and compared with those obtained by applying the British Pharmacopoeia (2002) method and showed that the proposed method is precise, accurate, and can be easily applied for the determination of the drugs under investigation in pure form and in cough syrup formulations.

  18. Stability-Indicating LC Method for the Determination of Prasugrel Hydrochloride in Pharmaceutical Dosage Form.

    Science.gov (United States)

    Ahirrao, Vinod K; Patil, Chabutai S; Bembalkar, Saroj B; Ubale, Sanjay B; Marathe, Rajendra P; Nawale, Rajesh B; Landge, Mahadev G; Pawar, Rajendra P

    2012-01-01

    A simple, rapid and precise method was developed for the quantitative estimation of prasugrel hydrochloride in pharmaceutical dosage form. A chromatographic separation of prasugrel and its degradants was achieved with Zorbax XDB C(8), 150 × 4.6 mm, 3.5μm analytical column using aqueous solution of 0.05 M ammonium acetate pH 4.5 with acetic acid-acetonitrile (40:60 v/v). The instrumental settings include flow rate of 1.0 ml/min, column temperature at 30°C and detector wavelength of 254 nm using a photodiode array detector. Theoretical plates for prasugrel were 7023. Tailing factor for prasugrel was 1.11. Prasugrel was exposed to thermal, photolytic, hydrolytic and oxidative stress conditions, and the stressed samples were analyzed by the proposed method. Peak homogeneity data of prasugrel was obtained using photodiode array detector in the stressed sample chromatograms, which demonstrated the specificity of the method for the estimation in presence of degradants. The described method showed excellent linearity over a range of 10-300 μg/ml for prasugrel. The correlation coefficient is 0.999. The relative standard deviation of peak area for six measurements is always less than 2%. Overall, the proposed method was found to be suitable and accurate for quantitative determination and stability study of prasugrel in pharmaceutical dosage form.

  19. Development and Characterization of Novel Floating-Mucoadhesive Tablets Bearing Venlafaxine Hydrochloride

    Directory of Open Access Journals (Sweden)

    Raghvendra Misra

    2016-01-01

    Full Text Available The present investigation is concerned about the development of floating bioadhesive drug delivery system of venlafaxine hydrochloride which after oral administration exhibits a unique combination of floating and bioadhesion to prolong gastric residence time and increase drug bioavailability within the stomach. The floating bioadhesive tablets were prepared by the wet granulation method using different ratios of hydroxypropyl methyl cellulose (HPMC K4MCR and Carbopol 934PNF as polymers. Sodium bicarbonate (NaHCO3 and citric acid were used as gas (CO2 generating agents. Tablets were characterized for floating properties, in vitro drug release, detachment force, and swelling index. The concentration of hydroxypropyl methyl cellulose and Carbopol 934PNF significantly affects the in vitro drug release, floating properties, detachment force, and swelling properties of the tablets. The optimized formulation showed the floating lag time 72±2.49 seconds and duration of floating 24.50±0.74 hr. The in vitro release studies and floating behavior were studied in simulated gastric fluid (SGF at pH 1.2. Different drug release kinetics models were also applied. The in vitro drug release from tablets was sufficiently sustained (more than 18 hr and the Fickian transports of the drug from the tablets were confirmed. The radiological evidence suggests that the tablets remained buoyant and altered position in the stomach of albino rabbit and mean gastric residence time was prolonged (more than > 6 hr.