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Sample records for hydrochloride mitomycin c-iohexol-lipiodol

  1. Mitomycin

    Science.gov (United States)

    Mitomycin is used in combination with other medications to treat cancer of the stomach or pancreas that ... treatment with other medications, surgery, or radiation therapy. Mitomycin is a type of antibiotic that is only ...

  2. 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 ...

  3. 40 CFR 721.5175 - Mitomycin C.

    Science.gov (United States)

    2010-07-01

    ... 40 Protection of Environment 30 2010-07-01 2010-07-01 false Mitomycin C. 721.5175 Section 721.5175... Mitomycin C. (a) Chemical substance and significant new use subject to reporting. (1) The chemical substance mitomycin C (CAS No. 5007-7) is subject to reporting under this section for the significant new...

  4. Transconjunctival penetration of mitomycin C

    OpenAIRE

    Velpandian T; Sihota Ramanjit; Sinha Ankur; Gupta Viney

    2008-01-01

    Aims: The study was performed to estimate transconjunctival penetration of mitomycin C (MMC) to Tenon′s tissue following application over the intact conjunctiva before routine trabeculectomy. Settings and Design: Institution-based case series. Materials and Methods: In 41 eyes of 41 patients, MMC (0.4 mg/ml for 3 min) was applied over the intact conjunctiva before beginning trabeculectomy. Tenon′s capsule directly beneath the site of application was excised during trabecule...

  5. Design, synthesis, and evaluation of mitomycin-tethered phosphorothioate oligodeoxynucleotides.

    Science.gov (United States)

    Huh, N; Rege, A A; Yoo, B; Kogan, T P; Kohn, H

    1996-01-01

    Mitomycin C (1) is the prototypical bioreductive alkylating agent. Studies have shown that mitomycin C and its derivatives selectively alkylate guanine residues within di- and trinucleotide DNA sequences. This investigation sought to improve the selective DNA bonding properties of the mitomycins by coupling them with antisense oligodeoxynucleotides. Two procedures were developed that allowed the attachment of a phosphorothioate oligodeoxynucleotide containing a hexylamino spacer at the 5' terminus with a C(10)-activated mitomycin. In the first procedure, decarbamoylation of 1 (NaOCH3/ benzene) afforded 10-decarbamoylmitomycin C (10), which was treated with either dimethyl sulfate or methylthiochloroformate and base to yield 10-decarbamoylporfiromycin (11) and N(1a)-[(methylthio)-carbonyl]-10-decarbamoylmitomycin C (12), respectively. Activation of the C(10) site in 11 and 12 with 1,1'-carbonyldiimidazole or with 1,1'-thiocarbonyldiimidazole provided the N(1a)-substituted mitomycin 10-decarbamoyl-10-O-carbonylimidazoles (5, 7) and 10-decarbamoyl-10-O-thiocarbonylimidazoles (6, 8), respectively. Compounds 5-8 were reacted with glycine methyl ester hydrochloride (17) and base in both methylene chloride and aqueous buffered solutions to determine the ease and efficiency in which these C(10)-activated mitomycin derivatives coupled to amines. It was found that 5-8 all reacted with 17 in methylene chloride to give the coupled products 18-21 but that improved amine coupling yields in water were observed for the 10-decarbamoyl-10-O-thiocarbonylimidazoles 6 and 8 as compared with the 10-decarbamoyl-10-O-carbonylimidazoles 5 and 7. This finding led to the coupling of the phosphorothioate oligodeoxynucleotide, H2N(CH2)6-P(S)(OH)-GGCCCCGTG-GTGGCTCCAT (22) to 8. Compound 22 complemented a 19-base sequence in the translation initiation region of the human A-raf-1 gene. Use of excess 8 (28 equiv) with 22 gave only a 36% yield of the coupled product 23, which proved difficult to

  6. Transconjunctival penetration of mitomycin C

    Directory of Open Access Journals (Sweden)

    Velpandian T

    2008-01-01

    Full Text Available Aims: The study was performed to estimate transconjunctival penetration of mitomycin C (MMC to Tenon′s tissue following application over the intact conjunctiva before routine trabeculectomy. Settings and Design: Institution-based case series. Materials and Methods: In 41 eyes of 41 patients, MMC (0.4 mg/ml for 3 min was applied over the intact conjunctiva before beginning trabeculectomy. Tenon′s capsule directly beneath the site of application was excised during trabeculectomy and was homogenized, centrifuged and MMC concentrations were analyzed using high-performance liquid chromatography (HPLC. Statistical Analysis Used: Statistical analysis was performed using stata0 8.0 version software (STATA Corporation, Houston, TX, USA. In this study, P -values less than 0.05 were considered as statistically significant. Results: The average weight of the sample of Tenon′s tissue excised was 5.51 ± 4.42 mg (range: 0.9-17.1 and the average estimated MMC concentration found to be present in Tenon′s tissue using HPLC was 18.67 ± 32.36 x 10−6 moles/kg of the tissue (range: 0.38-197.05 x 10−6 . In 36 of the 41 patients (87.80%, the MMC concentration reached above 2 x 10−6 moles/kg of the tissue concentration required to inhibit human conjunctival fibroblasts. Conclusions: Mitomycin C does permeate into the subconjunctival tissue after supraconjunctival application for 3 min. Application of MMC over the conjunctiva may be a useful alternative to subconjunctival or subscleral application during routine trabeculectomy and as an adjunct for failing blebs.

  7. 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.

  8. Mutations determining mitomycin resistance in Bacillus subtilis.

    Science.gov (United States)

    Iyer, V N

    1966-12-01

    Iyer, V. N. (Microbiology Research Institute, Canada Department of Agriculture, Ottawa, Canada). Mutations determining mitomycin resistance in Bacillus subtilis. J. Bacteriol. 92:1663-1669. 1966.-The pattern of development of genetic resistance in Bacillus subtilis to mitomycin C was studied, and spontaneous single and multistep mutants were obtained. The transmission and expression of these mutations in sensitive strains proved possible by means of genetic transformation. The mutations were genetically studied in relation to a chromosomal mutation, mac-1, which confers resistance to the macrolide antibiotic erythromycin and which has been previously localized in the early-replicating segment of the B. subtilis chromosome. The results indicate that all of three primary mutations studied in this manner, as well as a secondary and tertiary mutation derived from one of the primary mutations, are clustered in this early-replicating segment. It appears that the secondary and tertiary mutations enhance the resistance conferred by the primary mutation, apparently without themselves conferring any resistance.

  9. 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.

  10. Variability of mitomycin C adsorption by activated charcoal.

    Science.gov (United States)

    Shah, I A; Lindup, W E; McCulloch, P G

    1998-03-01

    A saline suspension of mitomycin C adsorbed on activated charcoal and administered intraperitoneally has been reported to be safe and effective in the treatment of gastric carcinoma. Activated charcoal specifically targets tumour and lymph-node tissues and the sustained higher local drug concentration is thought to be beneficial. The charcoal particles used in these suspensions have varied in size from > 147 microm to mitomycin C on activated charcoal in-vitro. Activated charcoal was ground and sieved to yield four size-fractions between 180 and 53 microm. Adsorption isotherms (n > or = 3) were constructed and applied to the Freundlich model with 0-l00 microg mL(-1) mitomycin C measured by HPLC with detection at 365 nm. Adsorption of mitomycin C by activated charcoal varied by a factor of three under identical conditions at room temperature (21 degrees C) and at 37 degrees C. The specific adsorption (microg mitomycin C (mg activated charcoal)(-1)) was generally higher at 37 degrees C than at room temperature. The variability of mitomycin C adsorption was greatly reduced by addition of the surface-active agent polyvinylpyrollidone, used to determine that adsorption of mitomycin C was independent of activated charcoal particle size. The characteristics of adsorption of mitomycin C by activated charcoal are complex and should be thoroughly investigated to discover the critical controlling factors before submitting the suspensions for further clinical evaluation.

  11. Molecular imprinted magnetic nanoparticles for controlled delivery of mitomycin C.

    Science.gov (United States)

    Türkmen, Deniz; Bereli, Nilay; Çorman, M Emin; Shaikh, Huma; Akgöl, Sinan; Denizli, Adil

    2014-10-01

    Controlled drug delivery system is a technique which has considerable recent potential in the fields of pharmacy and medicine. Mitomycin C is commonly used drug in the treatment of superficial bladder and breast cancers. In the present study, mitomycin C-imprinted magnetic poly(hydroxyethyl methacrylate)-based nanoparticles (MIMNs) were prepared using surfactant free emulsion polymerization for controlled delivery of mitomycin C. The MIMNs were characterized by fourier transform infrared spectroscopy, scanning electron microscopy, atomic force microscopy, electron spin resonance, and elemental analysis. The average particle diameter of MIMNs was about 200 nm.

  12. Structural characterization of the mitomycin 7-O-methyltransferase

    Energy Technology Data Exchange (ETDEWEB)

    Singh, Shanteri; Chang, Aram; Goff, Randal D.; Bingman, Craig A.; Grüschow, Sabine; Sherman, David H.; Phillips, Jr., George N.; Thorson, Jon S. (Michigan); (UW)

    2014-10-02

    Mitomycins are quinone-containing antibiotics, widely used as antitumor drugs in chemotherapy. Mitomycin-7-O-methyltransferase (MmcR), a key tailoring enzyme involved in the biosynthesis of mitomycin in Streptomyces lavendulae, catalyzes the 7-O-methylation of both C9{beta}- and C9{alpha}-configured 7-hydroxymitomycins. We have determined the crystal structures of the MmcR-S-adenosylhomocysteine (SAH) binary complex and MmcR-SAH-mitomycin A (MMA) ternary complex at resolutions of 1.9 and 2.3 {angstrom}, respectively. The study revealed MmcR to adopt a common S-adenosyl-L-methionine-dependent O-methyltransferase fold and the presence of a structurally conserved active site general acid-base pair is consistent with a proton-assisted methyltransfer common to most methyltransferases. Given the importance of C7 alkylation to modulate mitomycin redox potential, this study may also present a template toward the future engineering of catalysts to generate uniquely bioactive mitomycins.

  13. 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.

  14. Topical Mitomycin C in functional endoscopic sinus surgery.

    Science.gov (United States)

    Venkatraman, Vaidyanathan; Balasubramanian, Deepak; Gopalakrishnan, Suria; Saxena, Sunil Kumar; Shanmugasundaram, Nirmal

    2012-07-01

    In recent literature, there has been an interest in the use of Mitomycin C to reduce post-operative complications following endoscopic sinus surgery. We report our results on a prospective, randomized controlled trial involving 50 patients with chronic bilateral rhino sinusitis. We eliminated various confounding factors by studying a single group of patients, with symmetrical disease, without pre-existing gross anatomical abnormalities. Patients requiring revision sinus surgery were excluded. On completion of the surgery, a cotton pledget soaked in Mitomycin C was placed in one nostril (test) and saline-soaked pledget (control) was placed in the other side of the nose, both in the middle meatus. The side of the nasal cavity receiving the topical Mitomycin C was randomized. The patients were assessed periodically (first week, first month, third month and sixth month) for synechiae formation and presence or absence of their symptoms. At the first week follow up, there was a statistically significant difference in the incidence of synechiae between the saline and Mitomycin C side. Furthermore, there was a statistically significant improvement with regards to patient symptoms (nasal block and discharge) in the Mitomycin C side when compared to the saline side. At the third and sixth month, there was no difference between the two groups. The incidence of adverse tissue reaction (granulation, discharge, polypoidal mucosa and crusting) was less in the Mitomycin C side when compared to the saline side at the first month follow up. Topically applied Mitomycin C reduces the incidence of synechiae in the immediate post-operative period in patients undergoing endoscopic sinus surgery. There is also an improvement in nasal obstruction and discharge with a reduction in the incidence of adverse tissue reaction in the early post-operative period.

  15. Mitomycin C from birth to adulthood.

    Science.gov (United States)

    Serretta, Vincenzo; Scalici Gesolfo, Cristina; Alonge, Vincenza; Di Maida, Fabrizio; Caruana, Giovanni

    2016-10-04

    Mitomycin C (MMC) intravesical therapy for "superficial" papillary bladder tumors was firstly introduced in the early seventies with promising results. In the following years, several pharmacokinetic studies investigated its mechanism of action to optimize the intravesical administration. Numerous studies confirmed thereafter both the ablative and the prophylactic efficacy and the low toxicity of MMC when intravesically given. In 1984, a complete response rate of 42% in 60 patients not responsive to thiotepa was reported with intravesical MMC at the dose of 40 mg diluted in 40 ml for 8 weeks. In the following decades, many large randomized studies showed the benefit of intravesical prophylaxis with MMC versus transurethral resection (TUR) alone. Since 2002, the role of adjuvant intravesical chemotherapy and of an early MMC instillation in preventing recurrence compared with TUR alone has been confirmed by large meta-analyses and stated by the European Association of Urology (EAU) guidelines. The need for further intravesical chemotherapy after the early instillation in patients at intermediate-high risk of recurrence has been proved by several trials. Although intravesical Bacillus Calmette-Guerìn (BCG) is considered the best choice for high-risk patients and MMC for the low-risk group, both MMC and BCG can be given to prevent recurrence in intermediate-risk patients. However, the higher efficacy of BCG over MMC is evident only if maintenance regimen is administered. Despite its proven efficacy, immediate intravesical MMC is not yet fully entered in common clinical practice and efforts should be made by the urologists to optimize its adoption.

  16. Result of Intraoperative Mitomycin C Application in Dacryocystorhinostomy

    OpenAIRE

    Sheikh Sajjad Ahmad, Reyaz Ahmad Untoo

    2002-01-01

    Th is study was undertaken to evaluate the long term results 0 f intraoperative mitomyc inC app Iicat ionin dacryocystorh inostomy (DC R) surgery compared \\ ith resul ts of the conventiona I procedure. Inth is prospect ivc random ised controlled study, a tota I 01" 44 eyes diagnosed \\ ith acqu ired nasolacrimalduct obstruction \\ere randomly divided into a cOI1entional DCR group and a mitomycin C groupin \\hich mitomycin C \\3S used during OCR surger). The surgical procedures in both groups \\ere...

  17. Impact of Mitomycin-C application time on the scleral Mitomycin-C concentration.

    Science.gov (United States)

    Vass, C; Georgopoulos, M; El Menyawi, I; Radda, S; Nimmerrichter, P

    2001-04-01

    The aim of this study was to determine the effect of varying the application time of Mitomycin-C (MMC) on the scleral concentration of MMC. The sclerae of 14 human donor eyes were used for this study. The episcleral sides of the 4 scleral quadrants of each donor eye were exposed for 0.5, 1, 3 and 5 min to round, 8 mm-diameter sponges soaked with 50 microl of 0.2 mg/ml MMC. After 40-ml irrigation with saline, a central 8-mm diameter scleral disk was punched out, homogenized and analyzed with high performance liquid chromatography (HPLC). The scleral MMC concentrations (microg/g) after 0.5, 1, 3 and 5 min application times were 6.40 (+/-3.38), 9.02 (+/-2.40), 12.31 (+/-3.37), and 13.97 (+/-3.83). The differences of scleral MMC concentration in paired t-tests were statistically significant comparing 0.5 with 1 and 1 with 5 min application. However the effect was relatively small within the range of usual application times (1 to 5 min), and 64% of the MMC was delivered to the sclera within the first min.

  18. Pharmacokinetics of Mitomycin C Following Hepatic Arterial Chemoembolization With Gelfoam

    OpenAIRE

    Jin Wen Ding; Zai de Wu; Roland Andersson; Stig Bengmark

    1992-01-01

    Twelve mongrel dogs were randomly allocated into two groups using matched paired-design. Catheters were inserted into the hepatic artery, hepatic vein and the femoral vein, respectively. In the first group, gelfoam supplemented with mitomycin C (MMC) was injected into the hepatic artery, whereas the second group received a hepatic arterial injection of MMC solution alone. Simultaneous blood sampling from the hepatic and femoral veins at regular intervals was performed. MMC concent...

  19. Pharmacokinetics of Mitomycin C Following Hepatic Arterial Chemoembolization With Gelfoam

    OpenAIRE

    Ding, J. W.; Wu, Z. D.; Andersson, R.; S. Bengmark

    1992-01-01

    Twelve mongrel dogs were randomly allocated into two groups using matched paired-design. Catheters were inserted into the hepatic artery, hepatic vein and the femoral vein, respectively. In the first group, gelfoam supplemented with mitomycin C (MMC) was injected into the hepatic artery, whereas the second group received a hepatic arterial injection of MMC solution alone. Simultaneous blood sampling from the hepatic and femoral vein at regular intervals was performed. MMC concentrations in pl...

  20. Continuous hyperfractionated accelerated radiotherapy with/without mitomycin C in head and neck cancer

    NARCIS (Netherlands)

    Dobrowsky, W; Naude, J; Widder, J; Dobrowsky, E; Millesi, W; Pavelka, R; Grasl, C; Reichel, M

    1998-01-01

    Purpose: To evaluate the effect of mitomycin C to an accelerated hyperfractionated radiation therapy. The aim was to test a very short schedule with/without mitomycin C (MMC) with conventional fractionation in histologically verified squamous cell carinoma of the head and neck region. Methods and Ma

  1. Delayed healing at transurethral resection of bladder tumour sites after immediate postoperative mitomycin C instillation

    DEFF Research Database (Denmark)

    Aagaard, Mark F; Mogensen, Karin; Hermann, Gregers G

    2014-01-01

    The most common reactions to mitomycin C are dysuria and drug-related palmar and genital desquamation. This report describes two cases of delayed healing of the mucosa at resection sites after transurethral resection of bladder tumours, most likely due to immediate postoperative mitomycin C...

  2. Hyperfractionated accelerated radiochemotherapy (HFA-RCT) with mitomycin C for advanced head and neck cancer

    NARCIS (Netherlands)

    Widder, J; Dobrowsky, W; Schmid, R; Pokrajac, B; Selzer, E; Potter, R

    2004-01-01

    To investigate efficacy and feasibility of hyperfractionated accelerated radiotherapy combined with mitomycin C, patients with locally advanced unresectable squamous cell carcinomas of the head and neck region were administered 64-66 Gy in four weeks and mitomycin C (20 mg/m(2)) on day five. Twenty-

  3. Potential risk of mitomycin Cat high concentrations on peripheral nerve structure

    Institute of Scientific and Technical Information of China (English)

    Tao Sui; Jinhong Zhang; Shihao Du; Changhui Su; Jun Que; Xiaojian Cao

    2014-01-01

    Although the local application of mitomycin C may prevent epidural adhesion after laminectomy, mitomycin C can induce neurotoxicity in optic and acoustic nerves at high concentrations. To determine the safe concentration range for mitomycin C, cotton pads soaked with mitomycin C at different concentrations (0.1, 0.3, 0.5, and 0.7 mg/mL) were immediately applied for 5 minutes to the operation area of rats that had undergone laminectomy at L1. Rat sciatic nerves, instead of dorsal nerves, were used in this study. The results showed that mitomycin C at 0.1-0.5 mg/mL did not damage the structure and function of the sciatic nerve, while at 0.7 mg/mL, mitomycin C signiifcantly reduced the thickness of the sciatic nerve myelin sheath compared with lower concen-trations, though no functional change was found. These experimental ifndings indicate that the local application of mitomycin C at low concentrations is safe to prevent scar adhesion following laminectomy, but that mitomycin C at high concentrations (>0.7 mg/mL) has potential safety risks to peripheral nerve structures.

  4. Effect of beta-adrenergic stimulants on cytotoxicity of mitomycin C in HeLa cells.

    Science.gov (United States)

    Miyamoto, K; Sanae, F; Iwasaki, M; Koshiura, R

    1982-12-01

    Effects of several autonomic agents on the cytotoxicity of mitomycin C in HeLa cells were studied. When beta-adrenergic stimulants such as isoproterenol, epinephrine, terbutaline and turobuterol were added at concentrations over 10(-14) M 15 to 60 min before mitomycin C, the colony-forming ability of HeLa cells was significantly inhibited more than by mitomycin C alone. The action of isoproterenol and epinephrine on the colony-forming ability of the cells was abolished by propranolol. The intracellular cyclic AMP level of HeLa cells reached the peak of about two-fold the basal level at 30 min after the addition of 10(-8) M isoproterenol. In combination with mitomycin C, the high level of intracellular cyclic AMP induced by isoproterenol was maintained for a significantly longer period in comparison with that by isoproterenol alone, while mitomycin C alone caused essentially no change in the cyclic AMP level. The pretreatment with dibutyryl cyclic AMP also enhanced the effect of mitomycin C. From these findings, it is strongly suggested that the synergistic effect of beta-adrenergic stimulants on the cytotoxicity of mitomycin C is mediated via stimulation of the beta-adrenoceptors of HeLa cells which elevates the intracellular cyclic AMP for a long time in combination with mitomycin C.

  5. Enhancement of lutetium texaphyrin phototherapy with Mitomycin C

    Science.gov (United States)

    Thiemann, Patricia A.; Woodburn, Kathryn W.

    1998-05-01

    Lutetium texaphyrin (Lu-Tex) photodynamic therapy (PDT) relies on the presence of the water-soluble Lu-Tex, oxygen, and light (activation around 730 nm). Cytotoxic oxygen species are produced that cause irreversible damage to biological substrates. Damage may be inflicted via direct cell kill mechanisms or through vasculature effects that cause hypoxia. The addition of hypoxia enhanced drugs, such as Mitomycin C (MMC), can potentially increase the anti-tumor response. RIF-1 bearing C3H mice received 10 micrometers ol Lu-Tex/kg and were illuminated with 100 J/cm2 3 hours postinjection. Mice received MMC (2.5 or 5 mg/kg, before and after light) in conjunction with PDT and were compared to subsets of drug alone controls. A significant improvement in PDT response was observed when MMC was added to the dosing regimen; the effect was more pronounced at the highest MMC dose of 5 mg/kg: MMC prior to PDT gave a median tumor regrowth time (10X original volume) of 28 days compared to MMC and PDT alone, 16.3 and 14.9 days, respectively. The anti-tumor activity of lutetium texaphyrin induced PDT was improved by the addition of the bioreductive alkylating agent mitomycin C.

  6. Mutations induced in a shuttle vector plasmid exposed to monofunctionally activated mitomycin C.

    Science.gov (United States)

    Maccubbin, A E; Mudipalli, A; Nadadur, S S; Ersing, N; Gurtoo, H L

    1997-01-01

    Reductive activation of mitomycin C leads to its covalent binding to DNA, forming monoadducts and cross-links. The cytotoxicity of mitomycin C has been attributed to cross-link formation, whereas monoadducts are assumed to cause mutagenicity. We have developed a 32P-postlabeling technique to measure mitomycin C DNA adducts. Using this technique, we have measured monoadduct formation in the shuttle vector plasmid pSP189 and have determined mutations induced by monoadduct formation. The shuttle vector plasmid was incubated with mitomycin C under conditions favoring monofunctional activation of mitomycin C. The plasmid was then replicated in human Ad293 cells, rescued in bacteria, and analyzed for mutations in the supF tRNA gene sequence of pSP189. One major mitomycin C/DNA adduct was observed by 32P-postlabeling and was characterized as a monoadduct of guanine. When pSP189 was exposed to monofunctionally activated mitomycin C, increases in adduct levels and mutation frequency were found to be related to mitomycin C concentration. The majority of the mutations involved single bases, with base substitutions making up 59.1% of the total mutations observed. Of the base substitutions, 67.2% were transversions and 32.8% were transitions, with nearly 80% of all base substitutions involving G:C base pairs. Deletions, either as single bases or large deletions, also involved G:C base pairs the majority of the time. The observed bias of mutations at G:C and the formation of a mitomycin C/DNA monoadduct involving guanine suggests that monoadduct formation may be responsible for the mutations.

  7. 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....

  8. Mitomycin-C and 5- FU in ophthalmology: review article

    Directory of Open Access Journals (Sweden)

    M Jabbarvand Behrouz

    2009-03-01

    Full Text Available "nThe response of living tissues to the surgical trauma is associated with varying degrees of tissue repair and involves two distinct processes including replacement and regeneration. Replacement results in scar tissue formation instead of restoration of the normal architecture. However, regeneration leads to restoration of the original architecture leaving no sign of injury. Anti-proliferative agents are used to inhibit tissue responses to surgical trauma. Among them mitomycin- C and 5- FU had gained increasing applications in ophthalmic surgeries, including filtering glaucoma surgeries, laser vision correction with excimer laser by ablative surface refractive surgery, reconstructive surgeries for ocular surface disorders and removal of neoplastic tissues and secondary operations on nasolacrimal ducts. In this review article, the various aspects of applications of these agents including their mechanism of action, function, mode of application and complications in different ophthalmology fields are discussed.

  9. Ocular concentrations of mitomycin C using different delivery devices.

    Science.gov (United States)

    Mietz, H; Diestelhorst, M; Rump, A F; Theisohn, M; Klaus, W; Krieglstein, G K

    1998-01-01

    Hypotony and its sequelae are a frequent complication of trabeculectomies performed with mitomycin C (MMC), possibly related to intraocular toxicity of the substance. In an animal model with rabbits, we used different devices for the application of MMC and measured extra- and intraocular concentrations by HPLC. In addition, the concentrations of MMC remaining in the devices were determined. The devices were (1) a regular surgical sponge, (2) a scleral shield, (3) a presoaked soft contact lens, (4) a soft contact lens with MMC application, and (5) subconjunctival injection. Ocular concentrations of MMC were similar within the first 4 groups and were highest in the last. The measurements suggest that MMC penetrates intraocularly regardless of the device used. The variability of remaining MMC concentrations in the devices was lowest in the soft contact lenses suggesting an improved delivery system compared to the usually used surgical sponges.

  10. Electroporation enhances mitomycin C cytotoxicity on T24 bladder cancer cell line

    DEFF Research Database (Denmark)

    Vasquez, Juan Luis; Gehl, Julie; Hermann, Gregers G

    2012-01-01

    Intravesical mitomycin instillation combined with electric pulses is being used experimentally for the treatment of T1 bladder tumors, in patients unfit for surgery. Electroporation may enhance the uptake of chemotherapeutics by permeabilization of cell membranes. We investigated if electroporati...

  11. Trabeculectomy with Mitomycin-C versus trabeculectomy with 5-Fluorouracil for the treatment of childhood glaucoma

    Directory of Open Access Journals (Sweden)

    Osama M Badeeb

    2008-01-01

    Conclusions: 5-Fluorouracil and Mitomycin-C are equally effective as adjuncts to trabeculectomy in CG. Their use can be associated with serious complications. Further study is needed to evaluate intraoperative 5-Fluorouracil augmented trabeculectomy in CG.

  12. Mitomycin-C: 'a ray of hope' in refractory corrosive esophageal strictures.

    Science.gov (United States)

    Nagaich, N; Nijhawan, S; Katiyar, P; Sharma, R; Rathore, M

    2014-04-01

    Increasingly frequent dilation may become a self-defeating cycle in refractory stricture as recurrent trauma enhance, scar formation, and ultimately recurrence and potential worsening of the stricture. In 12 patients of caustic induced esophageal stricture, who failed to respond despite rigorous dilatation regimen for more than one year, a trial of topical mitomycin-C application to improve dilatation results was undertaken, considering the recently reported efficacy and safety of this agent. Mitomycin-C was applied for 2-3 minutes at the strictured esophageal segment after dilation with wire-guided Savary-Gilliard dilator. Patient was kept nil by mouth for 2-3 hours. After 4-6 sessions of mitomycin-C treatment, resolution of symptoms and significant improvement in dysphagia score and periodic dilatation index was seen in all 12 patients. Mitomycin-C topical application may be a useful strategy in refractory corrosive esophageal strictures and salvage patients from surgery.

  13. NEEDLE REVISION WITH MITOMYCIN-C IN ENCAPSULATED BLEBS

    Directory of Open Access Journals (Sweden)

    R Zarei

    2008-08-01

    Full Text Available "nThe most common cause of failure during the first trimester after trabeculectomy is encapsulated bleb and needling bleb revision is a less invasive method in the management of refractory cases. The purpose of this study is to determine the efficacy and safety of mitomycin-C (MMC augmented bleb revision of failed filtration surgery. This study is a before-after (paired observation. 33 patients with failed trabeculectomy because of bleb encapsulation, whose intraocular pressure (IOP was not reduced under 21 mmHg despite of medications and digital massage , underwent needling bleb revision and subconjunctival injection of 0.1 ml MMC (0.4 mg/ml.The mean follow-up time was 9.24 ± 5.27 months (1-20 months. Statistical analysis of the data included the paired two-tailed Student's t test for preoperative and postoperative IOP and number of medications. 36 needling procedures (mean, 1.09 ± 0.21 revisions per eye were performed on 33 eyes. Patients were between 10-80 years old (mean, 45.67 ± 22.41 years and mean follow-up was 9.24 ± 5.27 months. IOP decreased from 29.06 ± 5.03 mmHg to 18.21 ± 6.76 mmHg at last follow-up (P= 0.000. Antiglaucoma medications decreased from 2.18 ± 0.58 to 1.36 ± 0.29 at last follow-up (P= 0.000.Overall, 6 (18.2% of 33 cases achieved a complete success and 20 (60.6% of cases achieved a qualified success. The complications of this procedure were subconjunctival hemorrhage (17 cases, hyphema (5 cases and conjunctival button hole (2 cases. Needling bleb revision with mitomycin-C appears to be an effective and relatively safe way to revive failed filtration surgery.

  14. Relative toxicities of DNA cross-links and monoadducts: new insights from studies of decarbamoyl mitomycin C and mitomycin C.

    Science.gov (United States)

    Palom, Yolanda; Suresh Kumar, Gopinatha; Tang, Li-Qian; Paz, Manuel M; Musser, Steven M; Rockwell, Sara; Tomasz, Maria

    2002-11-01

    Mitomycin C (MC), a cytotoxic anticancer drug and bifunctional DNA DNA alkylating agent, induces cross-linking of the complementary strands of DNA. The DNA interstrand cross-links (ICLs) are thought to be the critical cytotoxic lesions produced by MC. Decarbamoyl mitomycin C (DMC) has been regarded as a monofunctional mitomycin, incapable of causing ICLs. Paradoxically, DMC is slightly more toxic than MC to hypoxic EMT6 mouse mammary tumor cells as well as to CHO cells. To resolve this paradox, EMT6 cells were treated with MC or DMC under hypoxia at equimolar concentrations and the resulting DNA adducts were analyzed using HPLC and UV detection. MC treatment generated both intrastrand and interstrand cross-link adducts and four monoadducts, as shown previously. DMC generated two stereoisomeric monoadducts and two stereoisomeric ICL adducts, all of which were structurally characterized; one was identical with that formed with MC, the other was new and unique to DMC. Overall, adduct frequencies were strikingly higher (20-30-fold) with DMC than with MC. Although DMC monoadducts greatly exceeded DMC cross-link adducts ( approximately 10:1 ratio), the latter were equal or higher in number than the cross-link adducts from MC. DMC displayed a much higher monoadduct:cross-link ratio than MC. The similar cytotoxicities of the two drug show a correlation with their similar DNA cross-link adduct frequencies, but not with their total adduct or monoadduct frequencies. This provides specific experimental evidence that the ICLs rather than the monoadducts are critical factors in the cell death induced by MC. In vitro, overall alkylation of calf thymus DNA by DMC was much less efficient than by MC. Nevertheless, ICLs formed with DMC were clearly detectable. The chemical pathway of the cross-linking was shown to be analogous to that occurring with MC. These results also suggest that the differential sensitivity of Fanconi's Anemia cells to MC and DMC is related to factors other

  15. Prevention of Intraabdominal Adhesions: An Experimental Study Using Mitomycin-C and 4% Icodextrin.

    Science.gov (United States)

    Urkan, Murat; Özerhan, İsmail Hakkı; Ünlü, Aytekin; Can, Mehmet Fatih; Öztürk, Erkan; Günal, Armağan; Yağcı, Gökhan

    2017-01-01

    Intraabdominal adhesions remain a significant cause of morbidity and mortality. Moreover, intraabdominal adhesions can develop in more than 50% of abdominal operations. We compared the anti-adhesive effects of two different agents on postoperative adhesion formation in a cecal abrasion model. Experimental animal study. Forty Wistar albino type female rats were anesthetized and underwent laparotomy. Study groups comprised Sham, Control, Mitomycin-C, 4% Icodextrin, and Mitomycin-C +4% Icodextrin groups. Macroscopic and histopathological evaluations of adhesions were performed. The frequencies of moderate and severe adhesions were significantly higher in the control group than the other groups. The mitomycin-C and Mitomycin-C +4% Icodextrin groups were associated with significantly lower adhesion scores compared to the control group and 4% Icodextrin group scores (p=0.002 and p=0.008, respectively). The adhesion scores of the Mitomycin-C group were also significantly lower than those of the 4% Icodextrin group (p=0.008). Despite its potential for bone marrow toxicity, Mitomycin-C seems to effectively prevent adhesions. Further studies that prove an acceptable safety profile relating to this promising anti-adhesive agent are required before moving into clinical trials.

  16. Pegylated liposomal mitomycin C prodrug enhances tolerance of mitomycin C: a phase 1 study in advanced solid tumor patients.

    Science.gov (United States)

    Golan, Talia; Grenader, Tal; Ohana, Patricia; Amitay, Yasmine; Shmeeda, Hilary; La-Beck, Ninh M; Tahover, Esther; Berger, Raanan; Gabizon, Alberto A

    2015-10-01

    Mitomycin C (MMC) has potent cytotoxicity but cumulative toxicity limits widespread use. In animals, pegylated liposomal mitomycin C lipid-based prodrug (PL-MLP) was well tolerated and more effective than free MMC. We evaluated PL-MLP in patients with advanced cancer. Twenty-seven patients were treated in escalating dose cohorts of 0.5-3.5 mg/kg (equivalent to 0.15-1.03 mg/kg MMC) every 4 weeks for up to 12 cycles, unless disease progression or unacceptable toxicity occurred. Pharmacokinetics were assessed during cycles 1 and 3. Per protocol maximum tolerated dose was not reached at 3.5 mg/kg. However, prolonged thrombocytopenia developed after repeated doses of 3 mg/kg or cumulative doses of 10-12 mg/kg. Dose-related grade 3 or higher adverse events included fatigue, anemia, and decreased platelets. Cmax and AUC0-∞ increased linearly over the dose range 0.5-2.0 mg/kg, and greater than linearly from 2.5 to 3.5 mg/kg; there were no significant differences in clearance of MLP between cycles 1 and 3. Median t1/2 was 23 h among dose cohorts, with no trend by dose or cycle. One patient had a partial response. Stable disease was observed in 10 patients across all dose levels. PL-MLP has a long circulation time, was well tolerated, and can be administered to heavily pretreated patients at a single dose of 3.0 mg/kg and cumulative dose of 10-12 mg/kg before development of prolonged thrombocytopenia; this is nearly threefold the equivalent dose of MMC tolerated historically. This formulation may be active in a variety of tumor types and is better tolerated than free MMC.

  17. Effect of mitomycin on normal dermal fibroblast and HaCat cell: an in vitro study

    Institute of Scientific and Technical Information of China (English)

    Yao-wen WANG; Ji-hao REN; Kun XIA; Shu-hui WANG; Tuan-fang YIN; Ding-hua XIE; Li-hua LI

    2012-01-01

    Objective: To evaluate the effects of mitomycin on the growth of human dermal fibroblast and immortalized human keratinocyte line (HaCat cell),particularly the effect of mitomycin on intracellular messenger RNA (mRNA) synthesis of collagen and growth factors of fibroblast.Methods: The normal dermal fibroblast and HaCat cell were cultured in vitro.Cell cultures were exposed to 0.4 and 0.04 mg/ml of mitomycin solution,and serum-free culture medium was used as control.The cellular morphology change,growth characteristics,cell proliferation,and apoptosis were observed at different intervals.For the fibroblasts,the mRNA expression changes of transforming growth factor (TGF)-β1,basic fibroblast growth factor (bFGF),procollagen Ⅰ,and Ⅲ were detected by reverse transcription polymerase chain reaction (RT-PCR).Results: The cultured normal human skin fibroblast and HaCat cell grew exponentially.A 5-min exposure to mitomycin at either 0.4 or 0.04 mg/ml caused marked dose-dependent cell proliferation inhibition on both fibroblasts and HaCat cells.Cell morphology changed,cell density decreased,and the growth curves were without an exponential phase.The fibroblast proliferated on the 5th day after the 5-min exposure of mitomycin at 0.04 mg/ml.Meanwhile,5-min application of mitomycin at either 0.04 or 0.4 mg/ml induced fibroblast apoptosis but not necrosis.The apoptosis rate of the fibroblast increased with a higher concentration of mytomycin (p<0.05).A 5-min exposure to mitomycin at 0.4 mg/ml resulted in a marked decrease in the mRNA production of TGF-β1,procollagen Ⅰ and Ⅲ,and a marked increase in the mRNA production of bFGF.Conclusions: Mitomycin can inhibit fibroblast proliferation,induce fibroblast apoptosis,and regulate intracellular protein expression on mRNA levels.In additon,mitomycin can inhibit HaCat cell proliferation,so epithelial cell needs more protecting to avoid mitomycin's side effect when it is applied clinically.

  18. Pharmacokinetics of mitomycin C in dogs: application of a high-performance liquid chromatographic assay.

    Science.gov (United States)

    Barbhaiya, R H; Papp, E A; Van Harken, D R; Smyth, R D

    1984-09-01

    A normal-phase high-performance liquid chromatographic (HPLC) assay was developed for the determination of mitomycin C in plasma and urine. The method involves extraction of mitomycin C from plasma or urine into ethyl acetate-2-propanol-chloroform (70:15:15) with UV detection at 365 nm. Quantitation was performed with an internal standard (porfiromycin) by the peak height ratio method. Excellent correlation was obtained between the HPLC assay and the established microbiological cup-plate bioassay. The pharmacokinetics of mitomycin C were investigated in beagle dogs following a 1-mg/kg iv (22-mg/m2) bolus dose. The plasma mitomycin C concentration versus time data were analyzed by using an open three-compartment model. The average volume of distribution was 1.90 L or 17% of body weight for the central compartment and 7.7 L or 68% of body weight for the terminal elimination phase. The volumes of distribution at steady state, calculated by model-dependent and -independent methods, compared very well with each other and were 6.5 L or 58% of body weight. Total body clearance averaged 112 mL/min, and the mean terminal plasma half-life was 53 min. The 0-24-h urinary excretion of intact mitomycin C accounted for 19% of the dose. The terminal half-life and percent urinary recovery of mitomycin C in dogs is similar to that in humans. Based on these observations, the dog appears to be a good model for studying the disposition of mitomycin C.

  19. [Intravesical therapy with mitomycin through electromotive drug administration].

    Science.gov (United States)

    Verri, Cristian; Liberati, Emanuele; Celestino, Francesco; De Carlo, Francesco; Torelli, Fiammetta; Di Stasi, Savino M

    2013-01-01

    In the management of non-muscle invasive bladder cancer (NMIBC), high-level evidence supports the widespread practice of intravesical therapy with mitomycin-C (MMC). Randomized trials showed a significant reduction in short-term recurrence compared with transurethral resection of bladder tumor (TURBT) alone, but little effect on long-term and no impact at all in preventing progression. Electromotive drug administration (EMDA®) offers a means of controlling and enhancing the tissue transport of certain drugs, in order to increase their efficacy. In both laboratory and clinical studies, intravesical electromotive drug administration (EMDA) increases MMC bladder uptake, resulting in an improved clinical efficacy in NMIBC without systemic side effects. New frameworks for treatment of NMIBC - e.g., sequential intravesical BCG and EMDA/MMC, as well as intravesical EMDA/MMC immediately before TURBT - have provided promising preliminary results with higher remission rates and longer remission times, and they are a priority to minimise the costs of disease management. These findings suggest EMDA-enhanced MMC efficacy against urothelial cancer could be a major therapeutic breakthrough in the treatment of NMIBC.

  20. Intravesical electro-osmotic administration of mitomycin C.

    Science.gov (United States)

    Di Stasi, Savino M; Verri, Cristian; Celestino, Francesco; De Carlo, Francesco; Pagliarulo, Vincenzo

    2016-10-04

    Bladder cancer is very common and most cases are diagnosed as nonmuscle invasive disease, which is characterized by its propensity to recur and progress. Intravesical therapy is used to delay recurrence and progression, while cystectomy is reserved for patients who are refractory to transurethral resection and intravesical therapy. There is an increasing interest in methods to enhance the delivery of intravesical chemotherapeutic agents to improve efficacy. In vitro and in vivo studies demonstrated that electro-osmosis of mitomycin C (MMC) is more effective in delivering this drug into the urothelium, lamina propria, and superficial muscle layers of the bladder wall than is passive transport. Higher MMC tissue concentrations might have a clinical impact in the treatment of nonmuscle invasive bladder cancer (NMIBC). In randomized trials, intravesical electro-osmotic MMC was associated with superior response rate in high-risk NMIBC cancer, compared with passive diffusion MMC transport. New strategies such as intravesical Bacillus Calmette-Guerin (BCG) combined with electro-osmotic MMC as well as intravesical pre-operative electro-osmotic MMC provided promising results in terms of higher remission rates and longer remission times.Device-assisted intravesical chemotherapy may be a useful ancillary procedure in the treatment of NMIBC. Its evaluation must be planned with respect to the technical functioning of equipment and their use for a clear purpose to avoid the financial and human costs associated with incorrect therapies.

  1. Efficacy of adjunctive mitomycin C in transcanalicular diode laser dacryocystorhinostomy.

    Science.gov (United States)

    Ozsutcu, Mustafa; Balci, Ozlem; Tanriverdi, Cafer; Demirci, Goktug

    2017-02-01

    The objective of the study was to compare the success rate of transcanalicular laser dacryocystorhinostomy (TCL-DCR) with or without the use of adjunctive mitomycin C (MMC) in cases with primary nasolacrimal duct obstruction (NLDO). This retrospective study was comprised of 68 patients with uncomplicated primary NLDO. There were two groups in the study: the Group 1 (n = 35) patients underwent TCL-DCR surgery with MMC and the Group 2 (n = 33) patients underwent TCL-DCR surgery without MMC. All patients had bicanalicular silicone tube intubation. The main outcome measures were patent osteotomy as visualized endoscopically and patent nasolacrimal irrigation. The follow-up period was 12 months. All patients had unilateral TCL-DCR with silicone tube intubation. Six months following surgery, the silicone tubes were removed. At the final evaluation, success rates were 80 % in Group 1 and 78.8 % in Group 2. There was no statistically significant difference between the two groups (p = 0.52). No complications related to MMC usage were recorded during the study period. Intraoperative use of MMC has no beneficial effect on the success rate in TCL-DCR.

  2. 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...

  3. 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...

  4. Phase II study of profiromycin vs mitomycin-C utilizing acute intermittent schedules.

    Science.gov (United States)

    Baker, L H; Izbicki, R M; Vaitkevicius, V K

    1976-01-01

    A randomized prosective study of Mitomycin-C and its N-methyl derivative, Porfiromycin, was conducted. Thirty-two patients with disseminated gastrointestinal cancer or other disseminated abdominal adenocarcinoma were treated with Mitomycin-C; 31 patients received Porfiromycin. Both drugs were given by acute intermittent bolus schedule (Mitomucin-C , 22.5 mg/M2 or Porfiromycin, 75 mg/M2 every 6--8 weeks as a single bolus i.v. injection). Eleven patients (34%) who received Mitomycin-C entered into partial remission. In 10 of the 31 patients (32%) receiving Porfiromycin, partial remission occured. Analysis by tumor type demonstrated that in the Mitomycin-C treated group responses occured in 4 of 12 patients with colorectal carcinoma, in 4 of 9 with upper GI cancers, and in 3 of 11 with ovarian cancer. Correspondingly in Porfiromycin group responses occured in 2 of 12 colorectal carcinoma patients, in 3 of 7 upper GI cancer patients, and in 5 of 12 ovarian cancer patients. Both drugs produced significant myelosuppression; however, Porfiromycin toxicity appeared more cumulative. Further clinical trial of Mitomycin in an acute intermittent bolus schedule appears justified.

  5. The inhibitor of histone deacetylases sodium butyrate enhances the cytotoxicity of mitomycin C.

    Science.gov (United States)

    Gospodinov, Anastas; Popova, Stanislava; Vassileva, Ivelina; Anachkova, Boyka

    2012-10-01

    The use of histone deacetylase inhibitors has been proposed as a promising approach to increase the cell killing effect of DNA damage-inducing drugs in chemotherapy. However, the molecular mechanism of their action remains understudied. In the present article, we have assessed the effect of the histone deacetylase inhibitor sodium butyrate on the DNA damage response induced by the crosslinking agent mitomycin C. Sodium butyrate increased mitomycin C cytotoxicity, but did not impair the repair pathways required to remove mitomycin C-induced lesions as neither the rate of nucleotide excision repair nor the homologous recombination repair rate were diminished. Sodium butyrate treatment abrogated the S-phase cell-cycle checkpoint in mitomycin C-treated cells and induced the G(2)-M checkpoint. However, sodium butyrate treatment alone resulted in accumulation of reactive oxygen species, double-strand breaks in DNA, and apoptosis. These results imply that the accumulation of reactive oxygen species-mediated increase in DNA lesion burden may be the major mechanism by which sodium butyrate enhances the cytotoxicity of mitomycin C.

  6. 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...

  7. Exploration of two methods for quantitative Mitomycin C measurement in tumor tissue in vitro and in vivo

    DEFF Research Database (Denmark)

    Fischer, Lee MacKenzie; Vásquez, Juan Luis; Gehl, Julie

    2013-01-01

    Two methods of quantifying Mitomycin C in tumor tissue are explored. A method of ultraviolet-visible absorption microscopy is developed and applied to measure the concentration of Mitomycin C in preserved mouse tumor tissue, as well as in gelatin samples. Concentrations as low as 60 μM can...... concentrations in tumor tissue....

  8. Rescue of Mitomycin C- or Psoralen-Inactivated Micrococcus Radiodurans by Additional Exposure to Radiation or Alkylating Agents

    DEFF Research Database (Denmark)

    Hansen, M. Trier

    1982-01-01

    The processing of damaged DNA was altered in a mitomycin C-sensitive mutant (mtcA) of Micrococcus radiodurans. Even though the mutant retained resistance to 254-nm UV radiation, it did not, in contrast to the wild-type strain, show any excessive DNA degradation or cell death when incubated...... with chloramphenicol after sublethal doses of either UV light or mitomycin C. The results suggest the constitutive synthesis of an enzyme system responsible for wild-type proficiency in the repair of mitomycin C-induced damage. An alternative system able to repair damage caused by mitomycin C was demonstrated...... in the mtcA background. In this strain, additional damage infficted upon the cellular DNA effected a massive rescue of cells previously inactivated by mitomycin C. Rescue was provoked by ionizing radiation, by UV light, or by simple alkylating agents. Cells treated with psoralen plus near-UV radiation could...

  9. [Response of HeLa cells to mitomycine C. I. Cell division].

    Science.gov (United States)

    Petrov, Iu P

    2013-01-01

    Using light microscopy, time-lapse imaging, and digital image analysis, the effect of mitomycine C (10 μg/ml) on HeLa-M cells has been studied. It has been shown that, after a 2 h contact with mitomycine, the cells could be separated into 2 groups: M-1--the functional cells surviving after division but non-entering mitosis any more; M-II--the cells entering mitosis but incapable to finish it; they are lost. Mitomycine C is known to specifically block DNA replication being located in the DNA minor groove. It should inhibit PHK synthesis if one follows the standard hypothesis of a transcription bubble formation. However, increasing the cell and nucleolus area during the M-I cell growth suggests that RNA and protein synthesis is not blocked. The author concludes that the presented data confirm his hypothesis about RNA synthesis in the major DNA groove (Petrov, 2006).

  10. Mitomycin C pharmacokinetics in patients with recurrent or metastatic colorectal carcinoma.

    Science.gov (United States)

    Erlichman, C; Rauth, A M; Battistella, R; Fine, S

    1987-03-01

    The pharmacokinetics of mitomycin C as a single agent have been determined in 25 treatment courses given to 18 patients with recurrent or metastatic colorectal carcinoma using a high performance liquid chromatography (HPLC) assay to analyze plasma and urine samples. The plasma pharmacokinetics conformed to a two-compartment linear model in 21 of 25 courses monitored with a mean t1/2 lambda 1 of 9.8 +/- 1.2 (SEM) min and mean t1/2 lambda z of 64.1 +/- 8.9 (SEM) min. The large variation observed in t1/2 lambda z was not related to dose or treatment, but an interaction of these two factors approached significance (p = 0.057). Renal excretion in the 12 courses in which it was determined averaged only 2.3% of the total administered dose during the first 4 h monitored and no mitomycin C metabolites were detected in plasma or urine by the HPLC technique used. The most common toxicity, thrombocytopenia, did not correlate with t1/2 lambda z or the area under the curve. This may be due to a failure to monitor active metabolites of mitomycin C; other factors besides plasma drug concentrations that mediate toxicity towards marrow elements; or the small number of courses associated with thrombocytopenia (less than 100,000/mm3). Our study indicates that an interaction of drug dose and treatment course may be associated with increasing t1/2 lambda z; the renal clearance contributes a small component of mitomycin C elimination; metabolites of mitomycin C cannot be detected by the present HPLC technique; and routine monitoring of mitomycin C using present methods cannot be recommended for clinical use to predict toxicity.

  11. Studies on synthesis and activation mechanism of mitomycin dimers connected by 1,2-dithiolane and diol linkers.

    Science.gov (United States)

    Kim, Hyoung Rae; Kim, Jae Jin; Park, Jung Jae; Lee, Sang Hyup

    2012-10-01

    We report the synthetic and mechanistic studies on a new cyclic disulfide mitomycin dimer, 7-N,7'-N'-(1″,2″-dithiolanyl-3″,5″-dimethylenyl)bismitomycin C (8), and a diol mitomycin dimer, 7-N,7'-N'-(2″,4″-dihydroxy-1″,5″-pentanediyl)bismitomycin C (9). Mitomycin 8 is a dimer connected by a 1,2-dithiolane (a five-membered cyclic disulfide) linker, and was specifically designed to undergo nucleophilic activation and double DNA alkylations leading to efficient production of DNA interstrand cross-link (DNA ISC) adducts. Disulfide cleavage in 8 would generate two thiol groups that could serve as probes to activate two mitomycin rings. At first, the target mitomycin 8 was synthesized using mitomycin A (1) and the key intermediate, cyclic disulfide (10), which was prepared through a seven-step synthetic sequence. Diol mitomycin 9 was also synthesized from 1 and diamine salt 13. Next, kinetic studies using solvolysis reaction revealed that the activation rates of 8 were much higher than those of 9 and mitomycin C (2) under nucleophilic conditions provided by Et(3)P presumably due to the presence of a cyclic disulfide unit in 8. These findings led us to propose a nucleophilic activation pathway for 8. Then, DNA ISC experiments further revealed that the levels of DNA ISC caused by 8 in the presence of Et(3)P were much higher (97%) than those by 9 (5%) and 2 (4%). More importantly, mitomycin 8 underwent much faster activation and produced slightly higher levels of DNA ISC than the previously reported mitomycins 5-7. Overall, we concluded that 8 was highly efficient for both nucleophilic activation and corresponding DNA ISC formation, and that this differentiation came from the crucial function of the cyclic disulfide unit in 8.

  12. [Metabolism of mitomycin C by human liver microsomes in vitro].

    Science.gov (United States)

    Hao, Fu-rong; Yan, Min-fen; Hu, Zhuo-han; Jin, Yi-zun

    2007-02-01

    To provide the profiles of metabolism of mitomycin C (MMC) by human liver microsomes in vitro, MMC was incubated with human liver microsomes, then the supernatant component was isolated and detected by HPLC. Types of metabolic enzymes were estimated by the effect of NADPH or dicumarol (DIC) on metabolism of MMC. Standard, reaction, background control (microsomes was inactivated), negative control (no NADPH), and inhibitor group (adding DIC) were assigned, the results were analyzed by Graphpad Prism 4. 0 software. Reaction group compared with background control and negative control groups, 3 NADPH-dependent absorption peaks were additionally isolated by HPLC after MMC were incubated with human liver microsomes. Their retention times were 10. 0, 14. 0, 14. 8 min ( named as Ml, M2, M3) , respectively. Their formation was kept as Sigmoidal dose-response and their Km were 0. 52 (95% CI, 0. 40 - 0.67) mmol x L(-1), 0. 81 (95% CI, 0. 59 - 1. 10) mmol x L(-1), 0. 54 (95% CI, 0. 41 -0. 71) mmol x L(-1) , respectively. The data indicated that the three absorption peaks isolated by HPLC were metabolites of MMC. DIC can inhibit formation of M2, it' s dose-effect fitted to Sigmoidal curve and it' s IC50 was 59. 68 (95% CI, 40. 66 - 87. 61) micromol x L(-1) , which indicated DT-diaphorase could take part in the formation of M2. MMC can be metabolized by human liver microsomes in vitro, and at least three metabolites of MMC could be isolated by HPLC in the experiment, further study showed DT-diaphorase participated in the formation of M2.

  13. Effect of Mitomycin C on Myopic versus Astigmatic Photorefractive Keratectomy

    Directory of Open Access Journals (Sweden)

    Ashwag A. Almosa

    2017-01-01

    Full Text Available Purpose. Long-term mitomycin C (MMC effects on photorefractive keratectomy (PRK were compared in simple myopic and astigmatic patients. Methods. In this observational cohort study, subjects were selected based on preoperative and postoperative data collected from medical records; they were divided into simple myopia with/without MMC and myopic astigmatism with/without MMC groups. Haze, uncorrected visual acuity (UCVA, best-corrected visual acuity (BCVA, subjective refraction, and K-reading were evaluated at 1-, 3-, 6-, and 12-month follow-ups. Results. One hundred fifty-nine eyes of 80 subjects (34 women and 46 men; mean age, 26.81 ± 7.74 years; range, 18–53 years; spherical powers, −0.50 to −8.00 DS; and cylindrical powers, −0.25 to −5.00 DC were enrolled. One year postoperatively, the simple myopia with/without MMC groups showed no difference in UCVA (P=0.187, BCVA (P=0.163, or spherical equivalent (P=0.163 and a significant difference (P=0.0495 in K-reading; the haze formation difference was nonsignificant (P=0.056. Astigmatic groups with/without MMC showed a significant difference in K-reading (P<0.0001. MMC groups had less haze formation (P<0.0001. Conclusion. PRK with intraoperative MMC application showed excellent visual outcomes. MMC’s effect on astigmatic patients was significantly better with acceptable safety and minimal side effects.

  14. Lethal effect of mitomycin C on Haemophilus influenzae

    Energy Technology Data Exchange (ETDEWEB)

    Small, G.D.; Setlow, J.K.; Kooistra, J.; Shapanka, R.

    1976-02-01

    The sensitivity of ultraviolet-sensitive strains to inactivation by mitomycin C (MC) is at the most only a factor of two greater than that of the wild type. The presence of inducible prophage has very little effect on the sensitivity. Genes which control excision of ultraviolet-induced pyrimidine dimers also control repair of MC-induced cross-links, as measured by resistance of denatured deoxyribonucleic acid (DNA) from treated cells to S1 nuclease digestion. However, endonucleolytic breaks in MC-damaged DNA, as judged by decreased single-strand molecular weight upon incubation of treated cells, are independent of these genes and probably are caused by monoadducts. After long periods of incubation there is a return to the molecular weight of untreated DNA. DNA degradation after MC treatment of various strains is not correlated with sensitivity to inactivation. Stationary-phase cells of all strains are more than twice as sensitive to MC as exponentially growing cells, and the sensitivity difference agrees with the measured difference in the number of cross-links after MC treatment of cells in the two growth stages. Evidence has been obtained that these phenomena result from differences in uptake of MC, which can be influenced by cyclic adenosine monophosphate. Small deviations in MC sensitivity from that of the wild type observed in mutants lacking the adenosine 5'-triphosphate-dependent nuclease are postulated to result from differences in MC uptake. These mutants, although no more ultraviolet sensitive than the wild type, are more sensitive to streptomycin, which also must be taken up by the cell to be effective. (auth)

  15. Validation of an HPLC-MS/MS and Wipe Procedure for Mitomycin C Contamination

    OpenAIRE

    B’Hymer, C.; Connor, T.H.; Stinson, D.; Pretty, J.R.

    2014-01-01

    A high-performance liquid chromatography-tandem mass spectrometric (HPLC-MS/MS) method was developed for the determination of mitomycin C, an anticancer drug, from contamination on various surfaces. Mitomycin C is often used in various forms of intraperitoneal chemotherapy, and operating room healthcare worker exposure to this drug is possible. The surface testing method consisted of a wiping procedure utilizing a solution of 20/45/35 (v/v/v) of acetonitrile-isopropanol-water made 0.01 M in a...

  16. A mitomycin-N6-deoxyadenosine adduct isolated from DNA.

    Science.gov (United States)

    Palom, Y; Lipman, R; Musser, S M; Tomasz, M

    1998-03-01

    A minor N6-deoxyadenosine adduct of mitomycin C (MC) was isolated from synthetic oligonucleotides and calf thymus DNA, representing the first adduct of MC and a DNA base other than guanine. The structure of the adduct (8) was elucidated using submilligram quantities of total available material. UV difference spectroscopy, circular dichroism, and electrospray mass spectroscopy as well as chemical transformations were utilized in deriving the structure of 8. A series of synthetic oligonucleotides was designed to probe the specificities of the alkylation of adenine by MC. The nature and frequency of the oligonucleotide-MC adducts formed under conditions of reductive activation of MC were determined by their enzymatic digestion to the nucleoside level followed by quantitative analysis of the products by HPLC. The analyses indicated the following: (i) (A)n sequence is favored over (AT)n for adduct formation; (ii) the alkylation favors the duplex structure; (iii) at adenine sites only monofunctional alkylation occurs; (iv) the adenine-to-alkylation frequency in the model oligonucleotides was 0.3-0.6 relative to guanine alkylation at the 5'-ApG sequence but only 0.02-0.1 relative to guanine alkylation at 5'-CpG. The 5'-phosphodiester linkage of the MC-adenine adduct is resistant to snake venom diesterase. The overall ratio of adenine to guanine alkylation in calf thymus DNA was 0.03, indicating that 8 is a minor MC-DNA adduct relative to MC-DNA adducts at guanine residues in the present experimental residues in the present experimental system. However, the HPLC elution time of 8 coincides with that of a major, unknown MC adduct detected previously in mouse mammary tumor cells treated with radiolabeled MC [Bizanek, R., Chowdary, D., Arai, H., Kasai, M., Hughes, C. S., Sartorelli, A. C., Rockwell, S., and Tomasz, M. (1993) Cancer Res. 53, 5127-5134]. Thus, 8 may be identical or closely related to this major adduct formed in vivo. This possibility can now be tested by

  17. Smac/DIABLO Promotes Mitomycin C-induced Apoptosis of Bladder Cancer T24 Cells

    Institute of Scientific and Technical Information of China (English)

    WANG Liang; ZENG Fuqing; ZHENG Liduan; TONG Qiangsong

    2006-01-01

    The enhancing effects of Smac gene on the mitomycin C-induced apoptosis of the bladder cancer cell line T24 were investigated. The Smac gene was transfected into bladder cancer cell line T24 under the induction of liposome. The intrinsic Smac level was detected by using immunohistochemistry and RT-PCR. The in vitro cellular growth activities were assayed by MTT colorimetry.Apoptosis was assayed by the flow cytometry. The results showed that as compared with the control cells, the apoptosis rate of T24 cells induced by mitomycin C was enhanced by transfected Smac gene. Flow cytometry revealed that, the apoptosis rate was 18.84% and 33.52%, and 10.72% and 26.24% respectively in blank and transfected cells treated with 0.05 or 0.005 mg/mL mitomycin C (P<0.05). It was concluded that Smac could enhance the apoptosis of T24 by mitomycin C,which could provide a useful experimental evidence for bladder cancer therapy.

  18. Multiphoton Imaging of Rabbit Cornea Treated with Mitomycin C after Photorefractive Keratectomy

    Science.gov (United States)

    Hsueh, Chiu-Mei; Lo, Wen; Wang, Tsung-Jen; Hu, Fung-Rong; Dong, Chen-Yuan

    2007-07-01

    In this work we use multiphoton microscopy to observe the post surgery structure variation of rabbit cornea after photorefractive keratectomy (PRK). In addition, we added mitomycin C (MMC) to the post surgery rabbit cornea in order to investigate the effect of MMC treatment on the postoperative regeneration.

  19. 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.

  20. 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.

  1. 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.

  2. Synthesis and mechanistic studies of a mitomycin dimer containing an eight-membered cyclic disulfide.

    Science.gov (United States)

    Park, Hyun Jung; Kim, Jae Jin; Kim, Hyoung Rae; Lee, Eun Kyung; Kim, Eun Sook; Jeong, Choon Sik; Moon, Aree; Lee, Sang Hyup

    2011-07-01

    Dimeric DNA alkylating agents have drawn significant interest because these compounds are expected to provide at least two reactive sites and as a result, generate enhanced levels of DNA interstrand cross-link (DNA ISC) adducts compared to their monomeric agents. We report the synthesis and mechanistic studies of a novel mitomycin dimer, 7-N,7'-N'-(1″,2″-dithiocanyl-3″,8″-dimethylenyl)bismitomycin C (8) connected by an eight-membered cyclic disulfide. Mitomycins require prior activation (i.e., transformation to a good electrophile) for DNA adduction and therefore, 8 was aimed to undergo facile nucleophilic activation and produce enhanced levels of DNA ISC. At the core of this function lies a cyclic disulfide in 8. It was expected that disulfide cleavage by an appropriate nucleophile would successively produce two thiols that may trigger activation of two mitomycin rings in a dimer through intramolecular cyclization to quinine rings. Compound 8 was synthesized from mitomycin A (1) and the key intermediate, cyclic disulfide (11), along with the reference diol mitomycin 7-N,7'-N'-(2″,7″-dihydroxy-1″,8″-octanediyl)bismitomycin C (23) which does not contain the disulfide unit. We found that 8 underwent significantly enhanced nucleophilic activation in the presence of Et(3)P compared with 23, and that the disulfide unit in 8 played a key role for the nucleophilic activation. Based on these findings, we proposed a mechanism for nucleophilic activation of 8. We further demonstrated that 8 generated much higher levels of DNA ISC (94%) compared with 23 (4%) and 2 (3%) in the presence of Et(3)P (and L-DTT) leading to the conclusion that 8 is more efficient for DNA ISC processes than 23 and 2 due to the role of disulfide unit.

  3. 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.

  4. Mitomycin C-DNA adducts generated by DT-diaphorase. Revised mechanism of the enzymatic reductive activation of mitomycin C.

    Science.gov (United States)

    Suresh Kumar, G; Lipman, R; Cummings, J; Tomasz, M

    1997-11-18

    Mitomycin C (MC) was reductively activated by DT-diaphorase [DTD; NAD(P)H:quinone oxidoreductase] from rat liver carcinoma cells in the presence of Micrococcus lysodeicticus DNA at pH 5.8 and 7.4. The resulting alkylated MC-DNA complexes were digested to the nucleoside level and the covalent MC-nucleoside adducts were separated, identified, and quantitatively analyzed by HPLC. In analogous experiments, two other flavoreductases, NADH-cytochrome c reductase and NADPH-cytochrome c reductase, as well as two chemical reductive activating agents Na2S2O4 and H2/PtO2 were employed as activators for the alkylation of DNA by MC. DTD as well as all the other activators generated the four known major guanine-N2-MC adducts at both pHs. In addition, at the lower pH, the guanine-N7-linked adducts of 2,7-diaminomitosene were detectable in the adduct patterns. At a given pH all the enzymatic and chemical reducing agents generated very similar adduct patterns which, however, differed dramatically at the acidic as compared to the neutral pH. Overall yield of MC adducts was 3-4-fold greater at pH 7.4 than at 5. 8 except in the case of DTD when it was 4-fold lower. Without exception, however, cross-link adduct yields were greater at the acidic pH (2-10-fold within the series). The ratio of adducts of bifunctional activation to those of monofunctional activation was 6-20-fold higher at the acidic as compared to the neutral pH. A comprehensive mechanism of the alkylation of DNA by activated MC was derived from the DNA adduct analysis which complements earlier model studies of the activation of MC. The mechanism consists of three competing activation pathways yielding three different DNA-reactive electrophiles 11, 12, and 17 which generate three unique sets of DNA adducts as endproducts. The relative amounts of these adducts are diagnostic of the relative rates of the competing pathways in vitro, and most likely, in vivo. Factors that influence the relative rates of individual pathways

  5. 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.

  6. 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.

  7. 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.

  8. 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.

  9. 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

  10. Respiration shutoff in Escherichia coli K12 strains is induced by far ultraviolet radiations and by mitomycin C.

    Science.gov (United States)

    Swenson, P A; Norton, I L

    1984-03-01

    Ultraviolet radiations (254 nm) (UV) cause respiration to shutoff in Escherichia coli B/r. It has been reported [P.A. Swenson, Photochem. Photobiol., 33 (1981) 855-859 and J. Barbé, A. Vericat and R. Guerrero, Mutation Res., 120 (1983) 1-5] that E. coli K12 strains do not shut off respiration after UV. The latter authors also reported that mitomycin C did not cause this 'SOS' response. In this paper we report that higher UV fluences than were previously used will cause respiration shutoff in K12 strain W3110 and that cyclic AMP increases the sensitivity of respiration shutoff of irradiated cell suspensions. We also report that mitomycin C shuts off respiration in this strain. Neither UV nor mitomycin C causes respiration shutoff in the recA56 derivative of W3110. Thus respiration shutoff is a recA dependent response to UV and mitomycin C in E. coli K12 strains.

  11. Addition of a hypoxic cell selective cytotoxic agent (mitomycin C or porfiromycin) to Fluosol-DA/carbogen/radiation

    Energy Technology Data Exchange (ETDEWEB)

    Holden, S.A.; Teicher, B.A. (Dana-Farber Cancer Institute, Boston (USA)); Herman, T.S. (Dana-Farber Cancer Institute, Boston (USA) Joint Center for Radiation Therapy, Boston (USA))

    1990-05-01

    In an effort to develop effictive combination treatments for use with radiation against solid tumors, the cytotoxic effects of the addition of mitomycin C or porfiromycin on treatment with Fluosol-DA/carbogen breathing and radiation in the FSaIIC tumor system were studied. In vitro mitomycin C and porfiromycin were both preferentially cytotoxic toward hypoxic FSaIIC cells. After in vivo exposure, however, the cytotoxicity of mitomycin C toward single cell tumor suspensions obtained from whole tumors was exponential over the dose range studied, but for porfiromycin a plateau in cell killing was observed. With Fluosol-DA/carbogen breathing and single dose radiaiton, addition of either mitomycin C or porfiromycin increased the tumor cell kill achieved at 5 Gy by approximately 1.2 and 1.0 logs, respectively. Less effect was seen with addition of the drugs at the 10 and 15 Gy radiation doses. In tumor growth delay experiments, the addition of either mitomycin C or porfiromycin to Fluosol-DA/carbogen breathing and radiation resulted in primarily an additive increase in tumor growth delay. The survival of Hoechst 33342 dye-selected tumor cell subpopulations indicated that Fluosol-DA/carbogen breathing increased the cytotoxicity of radiation (10 Gy) more in the bright cell subpopulation (4-fold) than in the dim cell subpopulation (2-fold) resulting in an overall 4-fold sparing of the dim subpopulation. Mitomycin C and porfiromycin were both more toxic toward the dim cell subpopulations. Addition of mitomycin C or porfiromycin to Fluosol-DA/carbogen breathing and radiation (10 Gy) resulted in a primarily additive effect of the drugs and radiation killing in both tumor cell subpopulations. Thus, with mitomycin C/Fluosol-DA/carbogen and radiation there was a 2-fold sparing of dim cells and with profiromycin in the combined treatment a 1.6-fold sparing of the dim cell population. (Abstract Truncated)

  12. Comparison of cytoreductive surgery and hyperthermic intraperitoneal chemotherapy with mitomycin or carboplatin for diffuse malignant peritoneal mesothelioma.

    Science.gov (United States)

    Shetty, Shreya J; Bathla, Lokesh; Govindarajan, Venkatesh; Thomas, Peter; Loggie, Brian W

    2014-04-01

    Diffuse malignant peritoneal mesothelioma is a rare, aggressive disease. Cytoreductive surgery (CRS) and hyperthermic intraperitoneal chemotherapy (HIPEC) have improved outcomes where systemic chemotherapy has not succeeded. In this study, we compare outcomes of patients treated with mitomycin or carboplatin as perfusate. In this retrospective study, 47 procedures (CRS + HIPEC) were conducted on 44 patients between March 2003 and August 2010 with either mitomycin or carboplatin. χ(2) and Student's t test were used for comparison of clinicopathological variables and Kaplan-Meier curves and log rank test were used to compare overall survival. Median survival of the mitomycin group was 18 months with 1- and 5-year survivals of 72.3 and 27.3 per cent, respectively. Median survival of the carboplatin group was not reached and 1- and 5-year survivals were 89.7 and 62.5 per cent, respectively (P = 0.014). Mean hospital and intensive care unit length of stay was 18.9 and 8.7 days in the mitomycin group and 12.5 and 2.3 days in the carboplatin group (P = 0.0069). Mean number of packed red blood cell units transfused was higher in the mitomycin group compared with the carboplatin group (3.54 vs 0.83, P mitomycin.

  13. 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...

  14. Liquid chromatography-thermospray mass spectrometry of DNA adducts formed with mitomycin C, porfiromycin and thiotepa.

    Science.gov (United States)

    Musser, S M; Pan, S S; Callery, P S

    1989-07-14

    High-performance liquid chromatography (HPLC) and thermospray mass spectrometry were combined for the analysis of DNA adducts formed from the interaction of the anticancer drugs mitomycin C, porfiromycin and thiotepa with calf thymus DNA. The adducts formed from reaction of mitomycin C and porfiromycin with DNA were separated from unmodified nucleosides by HPLC on a C18 column and identified by thermospray mass spectrometry. Thiotepa DNA adducts readily depurinated from DNA and were chromatographed and identified by thermospray liquid chromatography-mass spectrometry as the modified bases without the ribose moiety attached. The utility of thermospray mass spectrometry for the identification of microgram quantities of nucleoside adducts and depurinated base adducts of these anticancer drugs was demonstrated.

  15. Phellinus linteus Extract Augments the Immune Response in Mitomycin C-Induced Immunodeficient Mice

    OpenAIRE

    2007-01-01

    Phellinus linteus is a fungus distributed throughout Japan, Korea and China. Boiled water-soluble extracts from P. linteus (PLW) have shown anti-tumor and immunomodulatory properties in experiments done by intraperitoneal treatment, or in in vitro cell cultures. This is the first investigation on how oral administration of PLW influences immune responses. Here, we established immunodeficient mice by mitomycin C (MMC) and then researched how PLW influenced plaque-forming cell (PFC) production ...

  16. Transarterial chemoembolization (TACE) with mitomycin C and gemcitabine for liver metastases in breast cancer

    Energy Technology Data Exchange (ETDEWEB)

    Vogl, Thomas J.; Naguib, Nagy N.N.; Nour-Eldin, Nour-Eldin A.; Eichler, Katrin; Zangos, Stefan; Gruber-Rouh, Tatjana [Johann Wolfgang Goethe-University Frankfurt, Institute for Diagnostic and Interventional Radiology, Frankfurt am Main (Germany)

    2010-01-15

    The purpose of this study was to evaluate the efficacy of transarterial chemoembolization (TACE) using different drug combinations in the treatment of breast cancer liver metastases in terms of local tumor control and survival rate. A total of 208 patients (mean age 56.4 years, range 29-81) with unresectable hepatic metastases of breast cancer were repeatedly treated with TACE at 4-week intervals. In total, 1,068 chemoembolizations were performed (mean 5.1 sessions/patient, range 3-25). The chemotherapy protocol consisted of mitomycin-C only (8 mg/m{sup 2}; n=76), mitomycin-C with gemcitabine (n=111), and gemcitabine only (1,000 mg/m{sup 2}; n=21). Embolization was performed with lipiodol and starch microspheres. Tumor response was evaluated by MRI according to RECIST criteria. Survival rates were calculated using Kaplan-Meier method. For all protocols, local tumor control was partial response 13% (27/208), stable disease 50.5% (105/208), and progressive disease 36.5% (76/208). The 1-, 2-, and 3-year survival rates after TACE were 69, 40, and 33%. Median and mean survival times from the start of TACE were 18.5 and 30.7 months. Treatment with mitomycin-C only showed median and mean survival times of 13.3 and 24 months, with gemcitabine only they were 11 and 22.3 months, and with a combination of mitomycin-C and gemcitabine 24.8 and 35.5 months. TACE is an optional therapy for treatment of liver metastases in breast cancer patients with better results from the combined chemotherapy protocol. (orig.)

  17. Synthesis of an oligodeoxyribonucleotide adduct of mitomycin C by the postoligomerization method via a triamino mitosene

    OpenAIRE

    Champeil, Elise; Paz, Manuel M.; Ladwa, Sweta; Cristina C. Clement; ZATORSKI, ANDRZEJ; Tomasz, Maria

    2008-01-01

    The cancer chemotherapeutic agent mitomycin C (MC) alkylates and cross-links DNA monofunctionally and bifunctionally in vivo and in vitro, forming six major MC-deoxyguanosine adducts of known structures. The synthesis of one of the monoadducts (8) by the postoligomerization method was accomplished both on the nucleoside and oligonucleotide levels, the latter resulting in the site-specific placement of 8 in a 12-mer oligodeoxyribonucleotide 26. This is the first application of this method to t...

  18. Complications following Use of Intraoperative Mitomycin-C in Pterygium Surgery.

    OpenAIRE

    Imtiyaz Ahmad, Reyaz Ahmad Untoo, Sheikh Sajjad.

    2004-01-01

    This study was designed to evaluate the possible complications following the use of intraoperativemitomycin-C in patients undergoing surgery for primary pterygium. Hundred eyes of 88 patients withprimary pterygium were operated upon using ''bare sclera technique''. Intraoperatively all the patientswere applied freshly prepared mitomycin-C 0.02% (0.2 mg/ml) on the bare sclera for a period of 5 minutes,after which the eyes were thoroughly rinsed with a sterile balanced salt solution. Postoperat...

  19. Validation of an HPLC-MS/MS and wipe procedure for mitomycin C contamination.

    Science.gov (United States)

    B'Hymer, Clayton; Connor, Thomas; Stinson, Derek; Pretty, Jack

    2015-04-01

    A high-performance liquid chromatography-tandem mass spectrometric (HPLC-MS/MS) method was developed for the determination of mitomycin C, an anticancer drug, from contamination on various surfaces. Mitomycin C is often used in various forms of intraperitoneal chemotherapy, and operating room healthcare worker exposure to this drug is possible. The surface testing method consisted of a wiping procedure utilizing a solution of 20/45/35 (v/v/v) of acetonitrile-isopropanol-water made 0.01 M in ammonium citrate (apparent pH 7.0). The wipe solutions were analyzed by means of HPLC-MS/MS using a reversed-phase gradient system and electrospray ionization in positive ion mode with a triple-quadrupole MS detector. Accuracy and precision of this method were demonstrated by a series of recovery studies of both spiked solutions and extracted wipes from various surfaces (stainless steel, vinyl and Formica(®)) spiked with known levels of mitomycin C. Recoveries of spiked solutions containing the analyte demonstrate mean recoveries (accuracy) ranged from 93 to 105%. Precision as measured by the relative standard deviation (% RSD) of multiple samples (n= 10) at each concentration level demonstrated values of 7.5% or less. The recoveries from spiked surfaces varied from 30 to 99%. The limit of detection for this methodology is ∼2 ng/100 cm(2) equivalent surface area, and the limit of quantitation is ∼6 ng/100 cm(2).

  20. Induction of the Sulfolobus shibatae virus SSV1 DNA replication by mitomycin C

    Institute of Scientific and Technical Information of China (English)

    2002-01-01

    The temperate virus SSV1 from the hyperthermophilic archaeon Sulfolobus shibatae provides a useful model system for the study of archaeal DNA replication. Southern hybridization showed that SSV1 existed primarily as a provirus in its host that was grown without shaking. Upon UV or mitomycin C induction, the cellular level of free SSV1 DNA increased drastically whereas that of integrated viral DNA remained unchanged. The results of mitomycin C induction were more reproducible than those of UV induction. We found that, when the cells that had been grown without shaking were shaken, the replication of SSV1 DNA was also induced. Based on our results, we developed a method for the induction of SSV1 DNA replication by mitomycin C. When the S. shibatae virus production was induced using this method, the cellular level of free SSV1 DNA started to increase 10 h after induction, and peaked after 12-15 h. A fully induced S. shibatae cell contained ~50 molecules of free SSV1 DNA. The development of this induction method and the description of the process of SSV1 DNA replication following induction are valuable to the analysis of the origin and mode of replication of the virus.

  1. A comparative study on intraoperative mitomycin-c augmented external dacryocystorhinostomy with conventional dacryocystorhinostomy

    Directory of Open Access Journals (Sweden)

    Bharoti Sarmah Puzari

    2016-09-01

    Results: In our study we have observed that majority of cases were in 21-30 years age group with female preponderance (male vs female; 35% vs 75%. Chronic dacryocystitis was seen in majority of cases (70% followed by mucocele (26.67% and lacrimal fistula (3.33%. Major difficulties encountered during surgery and postoperatively were almost identical in both the groups. There was no case of abnormal mucosal bleeding, mucosal necrosis, delayed wound healing in patients which underwent DCR with mitomycin C use. Post-operative care and follow up were done identically in both the groups. It was seen that a total success rate of 80% was achieved in conventional group where as 96.67% success was achieved in MMC group at the end of 6 months. In case of scar prone conditions like lacrimal fistula mitomycin C use has shown to be efficacious in maintaining patency of the system after surgery. Conclusions: Distinctly higher success rate have been achieved in patients undergoing DCR with intra-operative MMC as compared to patients undergoing conventional DCR. Use of intraoperative mitomycin C can be considered safe and simple but very effective modification of conventional external DCR. [Int J Res Med Sci 2016; 4(9.000: 3879-3883

  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. 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....

  5. Dorzolamide synergizes the antitumor activity of mitomycin C against Ehrlich's carcinoma grown in mice: role of thioredoxin-interacting protein.

    Science.gov (United States)

    Ali, Belal M; Zaitone, Sawsan A; Shouman, Samia A; Moustafa, Yasser M

    2015-12-01

    The antitumor activity of carbonic anhydrase (CA) inhibitors is attributed to their ability to induce a state of intracellular acidification. In fact, acidic intracellular pH was demonstrated to upregulate several tumor suppressor proteins and increase the activity of many chemotherapies. The present study aimed to investigate the antitumor activity of the CA inhibitor, dorzolamide, in combination with mitomycin C and to study the effect of these drugs on tumoral thioredoxin-interacting protein (TXNIP) as well as tumor cell proliferation and apoptosis. Solid tumors were induced by subcutaneous inoculation of Ehrlich's ascites carcinoma (EAC) cells in female mice. Mice were treated with dorzolamide (3, 10, or 30 mg/kg/day, i.p.) and/or mitomycin C (1 mg/kg, i.p.) weekly for 3 weeks. Treatment with mitomycin C increased TXNIP level in EAC solid tumors in mice. Likewise, treatment with dorzolamide upregulated TXNIP and p53 while downregulated bcl-2. Both drug therapies increased tumoral caspase 9, caspase 3, and PARP-1 cleavage in addition to decreasing the proliferative Ki-67-stained nuclear fraction. Indeed, a synergistic effect was detected between mitomycin C and dorzolamide. The current data demonstrated that the antitumor activity of mitomycin C and dorzolamide was, at least in part, mediated through stimulating tumoral expression of TXNIP and enhancing tumor apoptosis.

  6. Electroporation enhances mitomycin C cytotoxicity on T24 bladder cancer cell line: a potential improvement of intravesical chemotherapy in bladder cancer.

    Science.gov (United States)

    Vásquez, Juan L; Gehl, Julie; Hermann, Gregers G

    2012-12-01

    Intravesical mitomycin instillation combined with electric pulses is being used experimentally for the treatment of T1 bladder tumors, in patients unfit for surgery. Electroporation may enhance the uptake of chemotherapeutics by permeabilization of cell membranes. We investigated if electroporation improves the cytotoxicity of mitomycin. In two cell lines, T24 (bladder cancer cell line) and DC3F (Chinese hamster fibroblast), exposure to different concentrations of mitomycin (0.01-2000μM) was tested with and without electroporation (6 pulses of 1kV/cm, duration: 99μs, frequency: 1Hz). Cell viability was assessed by colorimetric assay (MTT). For both cell lines, mitomycin's IC_50 was approximately 1000μM in both pulsed and unpulsed cells. On T24 cells, electroporation and mitomycin caused (relative reduction) RR of survival of: 25%, 31% and 29%, by concentrations 0μM, 500μM and 1000μM respectively. For DC3F cells, the RRs of survival were: 28%, 29%, and 33%, by concentrations 0μM, 500μM and 1000μM respectively. In conclusion, electroporation and mitomycin together are about 30% more effective than mitomycin alone. The results help to elucidate the additive effect of mitomycin and electric pulses and support the use of this combination in the treatment of bladder cancer.

  7. Selective activation of mitomycin A by thiols to form DNA cross-links and monoadducts: biochemical basis for the modulation of mitomycin cytotoxicity by the quinone redox potential.

    Science.gov (United States)

    Paz, M M; Das, A; Palom, Y; He, Q Y; Tomasz, M

    2001-08-16

    Mitomycin A (MA) but not mitomycin C (MC) cross-linked linearized (32)P-pBR322 DNA in the presence of dithiothreitol (DTT) or glutathione (GSH), as shown by a sensitive DNA cross-link assay. Incubation of calf-thymus DNA with MA and DTT or mercaptoethanol (MER) resulted in the formation of MA-DNA adducts, which were isolated from nuclease digests of the drug-DNA complexes by HPLC. The adducts were characterized by their UV absorption spectra, electrospray ionization mass spectrometry (ESIMS), and facile conversion from 7-methoxy- to 7-amino-substituted mitosene type adducts upon 10% NH(4)OH treatment, which were identical with known adducts of MC. Both DNA interstrand and intrastrand cross-link adducts, linking two deoxyguanosine residues at N(2), as well as several deoxyguanosine-N(2) monoadducts of MA, were identified. No DNA adducts were formed with MC under the same conditions. A specificity of DNA cross-link formation for the CpG sequence was observed using 12-mer synthetic oligodeoxyribonucleotides as substrates and as DNA sequence models, in analogy to the known CpG sequence specificity of MC-induced DNA cross-links. MA is known to be more cytotoxic by 2-3 orders of magnitude than MC, and this property correlates with redox potentials of MA (-0.19 V) and MA analogues that are higher than those of MC (-0.40 V) and its analogues. It is suggested that the biochemical basis for the higher cytotoxic potency of MA is MA's propensity to be reductively activated by cellular thiols while MC is resistant to thiol activation. This distinction is probably derived from the large difference between the quinone redox potentials of the two drugs.

  8. Cytomorphological Effects of Mitomycin C on Urothelial Cells: Eosinophils May Be Clue to The Drug-Induced Changes

    Directory of Open Access Journals (Sweden)

    Gulcin Guler Simsek

    2014-04-01

    Full Text Available Cytomorphological changes of mitomycin C on urothelial cells may be misinterpreted as a neoplastic process. A 60-year old male patient who was given an eight-week course of intravesical mitomycin C due to non-invasive low grade transitional cell carcinoma. During his follow-up care, the findings of a urine cytology exam were as follows: nuclear enlargement of cells, wrinkled nuclear membranes, little hyperchromasia, pleomorphism, abnormal nuclear morphology and disordered orientation of the urothelium. Furthermore, there were eosinophils nearby the atypical cells. This report aimed at reminding the cytomorphologic changes of mitomycin C may be misinterpreted as carcinoma, so the presence of eosinophils is required to predict the drug-induced changes.

  9. 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.

  10. 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...

  11. 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.

  12. 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...

  13. VEGF111b, a new member of VEGFxxxb isoforms and induced by mitomycin C, inhibits angiogenesis

    Energy Technology Data Exchange (ETDEWEB)

    Gu, Fang; Li, Xiuli [Department of Obstetrics and Gynecology, Chinese PLA General Hospital, Beijing (China); Kong, Jian [Department of Hepatobiliary Surgery, Beijing Chaoyang Hospital, Capital Medical University, Beijing (China); Pan, Bing [The Institute of Cardiovascular Sciences, Peking University Health Science Center, Key Laboratory of Molecular Cardiovascular Sciences of Education Ministry, Key Laboratory of Cardiovascular Molecular Biology and Regulatory Peptides of Health Ministry, Beijing (China); Institute of Systems Biomedicine, School of Basic Medical Sciences, Peking University Health Science Center, Key Laboratory of Molecular Cardiovascular Sciences of Education Ministry, Key Laboratory of Cardiovascular Molecular Biology and Regulatory Peptides of Health Ministry, Beijing (China); Sun, Min [Department of Obstetrics and Gynecology, Tangdu Hospital, Fourth Military Medical University, Xian (China); Zheng, Lemin, E-mail: zhengl@bjmu.edu.cn [The Institute of Cardiovascular Sciences, Peking University Health Science Center, Key Laboratory of Molecular Cardiovascular Sciences of Education Ministry, Key Laboratory of Cardiovascular Molecular Biology and Regulatory Peptides of Health Ministry, Beijing (China); Institute of Systems Biomedicine, School of Basic Medical Sciences, Peking University Health Science Center, Key Laboratory of Molecular Cardiovascular Sciences of Education Ministry, Key Laboratory of Cardiovascular Molecular Biology and Regulatory Peptides of Health Ministry, Beijing (China); Yao, Yuanqing, E-mail: yqyao@126.com [Department of Obstetrics and Gynecology, Chinese PLA General Hospital, Beijing (China)

    2013-11-08

    Highlights: •We discovered a new member of VEGFxxxb family-VEGF111b. •We found VEGF111b mRNA and protein can be induced by mitomycin C. •We confirmed VEGF111b over-expression inhibits angiogenesis. •VEGF111b inhibits angiogenesis through inhibiting VEGF-R2/PI3K/Akt and VEGF-R2/ERK1/2 phosphorylation. -- Abstract: Vascular endothelial growth factor (VEGF-A) stimulating angiogenesis is required for tumor growth and progression. The conventional VEGF-A isoforms have been considered as pro-angiogenic factors. Another family of VEGF-A isoforms generated by alternative splicing, termed VEGFxxxb isoforms, has anti-angiogenic property, exemplified by VEGF165b. Here, we identify a new number of VEGFxxx family-VEGF111b induced by mitomycin C, although not detected in mitomycin C-unexposed ovarian cancer cells. SKOV3 cells were transfected with pcDNA{sub 3.1} empty vector, pcDNA{sub 3.1}-VEGF111b or pcDNA{sub 3.1}-VEGF165b to collect conditioned mediums respectively. VEGF111b overexpression inhibits proliferation, migration and tube formation of endothelial cell by inhibiting VEGF-R2 phosphorylation and its downstream signaling, similar to VEGF165b but slightly lower than VEGF165b. The anti-angiogenic property depends on the six amino acids of exon 8b of the VEGFxxxb isoforms. Our results show that VEGF111b is a novel potent anti-angiogenic agent that can target the VEGF-R2 and its signaling pathway to inhibit ovarian tumor growth.

  14. Adjustable release of mitomycin C for inhibition of scar tissue formation after filtration surgery.

    Science.gov (United States)

    Merritt, Sonia R; Velasquez, Gia; von Recum, Horst A

    2013-11-01

    The aim of this study is to demonstrate a drug delivery system with the capacity to adjust the release of mitomycin C (MMC), based on polymer composition, and inhibit fibroblast proliferation to a better effect than is currently used in glaucoma filtration surgery. The polymer used in this work is made from the oligosaccharide cyclodextrin, from which others and we have demonstrated adjustable release of small molecule drugs due to specific molecular interactions or "affinity" between drug and the cyclodextrin polymer. To adjust release rate, cyclodextrin polymers were synthesized in either dimethylformamide (DMF) or dimethyl sulfoxide, (DMSO) at a crosslinking ratio of 1:0.16 or 1:0:32 (molecule of glucose: molecule of crosslinker). The polymers were then loaded with mitomycin C, dried, and release evaluated in a physiological environment. Drug release was determined by visible spectroscopy. Released aliquots of mitomycin C were incubated with 3T3 fibroblast cells to determine cytotoxic or inhibitory effect through a cell proliferation assay. We show that by using affinity between drug and polymer, we can adjust MMC release rates to be slower and more sustained than from conventional, diffusion-only polymers, for both the DMF polymers (p = 0.00526) and the DMSO polymers (p = 0.0113). The incorporated and released MMC maintains inhibition of fibroblast proliferation much longer than is possible with a one-time application. Affinity polymers with 1:0.16 and 1:0.32 crosslink ratio showed significant inhibition of proliferation for up to 100 h (p = 0.018 and p = 0.014 respectively). The use of our controlled drug delivery technology applied after surgery could have a greater therapeutic impact than the current one-time applications of MMC.

  15. Vincristine, adriamycin, and mitomycin (VAM) therapy for previously treated breast cancer. A preliminary report.

    Science.gov (United States)

    Oster, M W; Park, Y

    1983-01-15

    Fifteen patients with metastatic breast cancer previously treated with chemotherapy were treated with a regimen consisting of vincristine, Adriamycin, and mitomycin. Eleven patients (73%) responded with three complete and eight partial responses. The median duration of response was eight months. While all four nonresponders died within five months, the median duration of survival of responders was 18 months. Toxicity was significant but tolerable. Thus, this preliminary report suggests that this regimen is active in advanced previously treated breast cancer, providing meaningful remissions with acceptable toxicity.

  16. Application of Mitomycin C after dilation of an anastomotic stricture in a newborn with necrotizing enterocolitis

    Directory of Open Access Journals (Sweden)

    Jonathan Green

    2016-01-01

    Full Text Available Necrotizing enterocolitis (NEC is a common life-threatening condition in premature infants. Bacterial translocation, localized inflammation and subsequent perforation often require surgery for source control and definitive treatment. Small and large intestinal strictures may result from either creation of a surgical anastomosis or the disease process itself. Current methods to treat strictures include, balloon dilation and surgical resection with or without anastomosis. We report the diagnosis and surgical management of a premature infant treated for NEC, who developed an anastomotic stricture and was successfully treated with topical Mitomycin C after balloon stricturoplasty.

  17. Prevention of Adhesion after Endoscopic Sinus Surgery: Role of Mitomycin C

    Directory of Open Access Journals (Sweden)

    Mohammad-Hossein Baradaranfar

    2011-03-01

    Full Text Available Adhesions after endoscopic sinus surgery (ESS are a potential cause of surgical failure. Mitomycin-C (MMC is recently proposed as a solution for these adhesions. This study was performed to investigate the effect of Mitomycin C in reducing scar formation and adhesion in the nasal mucosa after endoscopic nasal surgery. This double blind randomized clinical trial study was performed on 37 patients with bilateral chronic rhinosinusitis. At the end of ESS, randomly impregnated mesh with MMC was placed in one side and another mesh impregnated with saline in the opposite side for 5 minutes. Patients were followed at least for three months, and the results of diagnostic endoscopy were recorded. Post operative adhesion occurred in 12 (32.4% patients (2 bilateral/10 unilateral. Among total of 14 adhesions, 4 (10.8% were in the MMC side and 10 (27% in the control side. This differences was close to statistically significant (P=0.058. MMC may reduce adhesions after ESS, but further studies with different doses, sample size and frequent use of topical MMC is recommended.

  18. Successful endoscopic management with Mitomycin C application for sinusitis with orbital cellulitis

    Directory of Open Access Journals (Sweden)

    Anil S Harugop

    2013-01-01

    Full Text Available Background: Sinusitis with orbital complication is a potentially fatal disease that has been known since the days of Hippocrates. Primary sinus infection is the most common cause of orbital cellulitis. It is an emergency that threatens not only vision but also life from complications such as meningitis, cavernous sinus thrombosis, and brain abscess. Surgical intervention is mandatory whenever antibiotic treatment fails. There are two surgical options for the drainage, an external approach via a Lynch incision and an intranasal endoscopic procedure. Materials and Methods: Five patients with orbital cellulitis secondary to acute on chronic rhinosinusitis were included in the study from the period of 2010 - 2011. All five patients did not respond to medical management and hence underwent endoscopic sinus surgery with treatment of orbital pathology. At the end of the surgical procedure Mitomycin C in a concentration of 0.4mg/ml was applied with a cottonoid for a period of 4 minutes to prevent chance of adhesion formation. Results: In this series 3 females and 2 male patient with orbital cellulitis secondary to acute on chronic rhinosinusitis underwent endoscopic sinus surgery with treatment of orbital pathology. All 5 patients showed subjective and objective improvement within one week of endoscopic management. Conclusion: Though antibiotics have altered the course of sinusitis, its grave complications still persist in our environment. The excellent results and the absence of any major complications of endoscopic sinus surgery and drainage of abscess with application of Mitomycin C can be recommended as the preferred surgical technique.

  19. Interactions of radiation and adriamycin, bleomycin, mitomycin C or cis-diamminedichloroplatinum II in intestinal crypt cells

    DEFF Research Database (Denmark)

    von der Maase, H

    1984-01-01

    The interactions of radiation and adriamycin (ADM), bleomycin (BLM), mitomycin C (MM-C), or cis-diamminedichloroplatinum II (cis-DDP) in mouse jejunal crypt cells were studied using the microcolony survival assay. ADM administered from 24 h before to 48 h after irradiation resulted in an almost...

  20. Influence of intraperitoneal therapy with mitomycin C adsorbed on activated carbon on anastomotic and wound healing in rats

    NARCIS (Netherlands)

    Jansen, M; Jansen, PL; Fass, J; Langejurgen, E; Forsch, S; Tietze, L; Schumpelick, [No Value

    2002-01-01

    In an effort to prevent intraperitoneal dissemination of gastric carcinoma, local chemotherapy with mitomycin C adsorbed to activated carbon (MMC-CH) has been implemented. Results of clinical studies showed improved survival and a reduced systemic toxicity after the use of prophylactic treatment wit

  1. [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.

  2. 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.

  3. 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

  4. 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

  5. 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.

  6. 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.

  7. 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

  8. Evidence of increased chromosomal instability in infertile males after exposure to mitomycin C and caffeine

    Institute of Scientific and Technical Information of China (English)

    Fotini Papachristou; Theodore Lialiaris; Stavros Touloupidis; Christos Kalaitzis; Constantinos Simopoulos; Nikolaos Sofikitis

    2006-01-01

    Aim: To evaluate the genetic instability of 11 fertile and 25 infertile men. Methods: The methodology of sister chromatid exchanges (SCEs) was applied to cultures of peripheral blood lymphocytes, and the levels of SCEss were analyzed as a quantitative index of genotoxicity, along with the values of the mitotic index (MI) and the proliferation rate index (PRI) as qualitative indices of cytotoxicity and cytostaticity, respectively. The genotoxic and antineoplastic agent, mitomycin C (MMC), and caffeine (CAF) - both well-known inhibitors of DNA repair mechanism - were used in an attempt to induce chromosomal instability in infertile men, so as to more easily detect the probable underlying damage on DNA. Results: Our experiments illustrated that infertile men, compared with fertile ones, demonstrated a statistically significant DNA instability in peripheral blood lymphocytes after being exposed simultaneously to MMC and CAF. Conclusion: The current study showed vividly that there was genetic instability in infertile men which probably contributes to the development of an impaired reproductive capacity.

  9. Topical mitomycin C can effectively alleviate dysphagia in children with long-segment caustic esophageal strictures.

    Science.gov (United States)

    El-Asmar, K M; Hassan, M A; Abdelkader, H M; Hamza, A F

    2015-07-01

    Caustic ingestion in children and the resulting long esophageal strictures are usually difficult to be managed, and eventually, esophageal replacement was required for cases refractory to frequent dilatation sessions. Topical mitomycin C (MMC) application has been used recently to improve the results of endoscopic dilatation for short esophageal strictures. The study aims to assess the role of MMC application in management of long-segment caustic esophageal strictures. From January 2009 to June December 2013, patients presented with long caustic esophageal stricture (>3 cm in length) were included in this study and subjected to topical MMC application after endoscopic esophageal dilatation on multiple sessions. Regular follow-up and re-evaluation were done. A dysphagia score was used for close follow-up clinically; verification was done radiologically and endoscopically. During the specified follow-up period, 21 patients with long caustic esophageal stricture were subjected to topical MMC application sessions. Clinical, radiological, and endoscopic resolution of strictures occurred in 18 patients (85.7% cure rate). Number of dilatation sessions to achieve resolution of dysphagia was (n = 14.3 ± 5.7) with application of mitomycin two to six times. There was no recurrence in short- and mid-term follow-up. No complications were encountered related to topical MMC application. MMC is a promising agent in management of long-segment caustic esophageal strictures. Long-term follow-up is needed to prove its efficacy and to evaluate potential long-term side-effects of MMC application.

  10. Reconstruction of delayed scleral flap melting with bovine pericardium after trabeculectomy with mitomycin C

    Directory of Open Access Journals (Sweden)

    Coutinho, Inês

    2017-06-01

    Full Text Available Aim: To present a challenging case of hypotony after trabeculectomy and its treatment. Case description: A 22-year-old woman with juvenile glaucoma underwent a conventional trabeculectomy with mitomycin C on the right eye (OD. In the immediate postoperative period, we observed a hyperfiltration bleb with hypotony refractory to conservative measures leading to hypotony maculopathy.A surgical revision with scleral flap resuture and conjunctival graft was performed with a satisfactory result and resolution of hypotony maculopathy. After two years, the patient complained of low visual acuity (VA of the OD. During examination, we observed a fine and avascular bleb with Seidel and visualization of the underlying uveal tissue, an intraocular pressure (IOP of 5 mmHg, and chorioretinal folds. A new revision of the trabeculectomy was performed. During the procedure, it was not possible to identify the scleral flap, so the fistula was closed with a patch of collagenous membrane derived from bovine pericardium (Tutopatch graft. A good clinical evolution occurred. After 2 months, IOP was 15 mmHg without Seidel or changes in the fundus and VA was 20/20. After of follow-up, the IOP remains stable without further complaints. Conclusion: This case illustrates the difficulties faced in the management of a common complication of trabeculectomy and highlights some of the options available for its treatment. There are few reports of scleral melting after trabeculectomy. However, trauma and scleral necrosis associated with mitomycin are listed as the main causes.The use of a scleral patch derived from bovine pericardium allows effective suturing and closure of the aqueous leak.

  11. 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...

  12. 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...

  13. 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...

  14. 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...

  15. 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...

  16. 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. ...

  17. 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)

  18. Studies on activation mechanism of a mitomycin dimer, 7-N,7'-N'-(1″,2″-dithiepanyl-3″,7″-dimethylenyl)bismitomycin C.

    Science.gov (United States)

    Kim, Jae Jin; Kim, Hyoung Rae; Lee, Sang Hyup

    2012-09-01

    We report the studies on nucleophilic activation and DNA alkylation of a cyclic disulfide mitomycin dimer, 7-N,7'-N'-(1″,2″-dithiepanyl-3″,7″-dimethylenyl)bismitomycin C (6) along with a diol mitomycin dimer, 7-N,7'-N'-(2″,6″-dihydroxy-1″,7″-heptanediyl)bismitomycin C (7). We wished to see if disulfide mitomycin 6 undergoes efficient nucleophilic activation and corresponding formation of DNA interstrand cross-link (DNA ISC) products compared to diol mitomycin 7. Mitomycin 6 is a dimer connected by a seven-membered cyclic disulfide (a 1,2-dithiepane) linker, and mitomycin 7 is also a dimer containing 2,6-dihydroxyheptane linker that was employed as a reference one to identify the effect of disulfide unit in 6. Through kinetic studies using solvolysis reaction, we found that 6 underwent much faster nucleophilic activation by Et3P compared to 7, and that the enhanced activation rates were induced by the disulfide unit in 6. These findings led us to propose a nucleophilic activation mechanism for 6. We further demonstrated that 6 produced much higher levels of DNA ISC (86%) by the action of Et3P compared with 7 (5%) and 1 (4%). Therefore, we have concluded that 6 was highly efficient for nucleophilic activation and DNA ISC formation due to the key role of cyclic disulfide unit in 6.

  19. Efficacy of Surgical Excision in Combination with Mitomycin C and Postoperative Topical 0.002% Mitomycin C Administration for Treatment of Conjunctival Intraepithelial Neoplasia

    Directory of Open Access Journals (Sweden)

    Özlen Rodop Özgür

    2011-08-01

    Full Text Available Purpose: To evaluate the efficacy of surgical excision in combination with mitomycin C (mit-C and postoperative topical mit-C 0.002% administration for the treatment of conjunctival intraepithelial neoplasia (CIN. Material and Method: Twelve eyes of twelve patients who were histopathologically diagnosed as CIN between March 2004 and July 2008 were evaluated retrospectively for their treatment modalities and results. All lesions were excised with wide margins in combination with mit-C 0.02% application for 2 minutes. Five of 12 eyes were treated with topical mit-C 0.002% eye drops four times a day for 14 days after histopathological confirmation. Large conjunctival defects in 5 eyes were reconstructed with amniotic membrane (3 eyes and autologous conjunctiva (2 eyes. Results: Seven patients were women and 5 were men, with a mean age of 68.37 (range: 30-94 years. The right eye was involved in 6 patients and the left one - in 6 patients. The conjunctival lesion was located on the nasal conjunctiva in 5 eyes and on the temporal one - in 7 eyes. Histopathological diagnosis was CIN in all cases. After a mean follow-up period of 41.75 months (between 10 and 62 months, one recurrence (8.3% was noted. This case with recurrent lesion has been previously treated with surgical excision in combination with mit-C 0.02% application and the large conjunctival defect has been reconstructed with amniotic membrane. Discussion: Surgical excision in combination with mit-C and use of additional postoperative topical mit-C 0.002% in selected cases for conjunctival intraepithelial treatment provides a safe and effective cure. (Turk J Ophthalmol 2011; 41: 138-42

  20. Expression of the dnaN and dnaQ genes of Escherichia coli is inducible by mitomycin C.

    Science.gov (United States)

    Kaasch, M; Kaasch, J; Quiñones, A

    1989-10-01

    The dnaN and dnaQ genes encode the beta subunit and the epsilon subunit of the DNA polymerase III holoenzyme. Using translational fusions to lacZ we found that DNA damage caused by mitomycin C induces expression of the dnaA and dnaQ genes. This induction was not observed in lexA and recA mutants which block the induction of the SOS response, suggesting a relationship between the mechanism(s) of genetic control of DNA polymerase III holoenzyme and the SOS regulatory network. Nevertheless, there is evidence that the mitomycin C induction of dnaN and dnaQ is not a simple lexA-regulated process, because nalidixic acid (an excellent SOS inducer) does not increase dnaN and dnaQ gene expression, and the time course of induction is abnormally slow.

  1. Superficial keratectomy and topical mitomycin C as therapy for a corneal squamous cell carcinoma in a dog.

    Science.gov (United States)

    Karasawa, K; Matsuda, H; Tanaka, A

    2008-04-01

    A 10-year-old female West Highland white terrier was presented with refractory hyperplastic keratitis of the left cornea of one month's duration. At this time, a vascularised and rough lesion 5 mm in diameter was observed on the left cornea. No other abnormality was recognised on the affected eye. The corneal neoplasm was surgically removed and histologically diagnosed as a squamous cell carcinoma. For two months after the surgery, 0.04 percent mitomycin C (MMC) eye drops were applied as adjuvant chemotherapy. Primary corneal squamous cell carcinoma with no history of keratoconjunctivitis sicca is rare in dogs. In the present report, surgical removal of the neoplasm was combined with the topical administration of the anticancer drug mitomycin C and a good prognosis was obtained. The result indicates that the combination treatment used in this case may be an appropriate therapeutic choice for corneal squamous cell carcinoma in dogs.

  2. Effects of 60Co gamma-rays, ultraviolet light, and mitomycin C on Halobacterium salinarium and Thiobacillus intermedius.

    Science.gov (United States)

    Shahmohammadi, H R; Asgarani, E; Terato, H; Ide, H; Yamamoto, O

    1997-03-01

    Lethal effects of 60Co gamma-rays, UV light, and mitomycin C on two kinds of bacteria, Halobacterium salinarium which grows in highly concentrated salt media and Thiobacillus intermedius which requires reduced sulfur compounds, were studied and compared with those on Escherichia coli B/r. D37 values for H. salinarium, T. intermedius and E. coli B/r were 393, 150, and 92 Gy, respectively, by exposure to 60Co gamma-rays. They were 212, 38, and 10 J/m2, respectively, by exposure to UV light and 2.36, 0.25, and 0.53 microgram/ml/h, respectively, by exposure to mitomycin C. Against these agents, H. salinarium was much more resistant than T. intermedius and E. coli B/r.

  3. [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.

  4. Study on the Interaction of Mitomycin C with ct-DNA by Pd-Porphin Room Temperature Phosphorescence Probe

    Institute of Scientific and Technical Information of China (English)

    2001-01-01

    Anticancer drug Mitomycin C (MMC) quenches remarkably phosphorescence and reduces lifetime of phosphorescence probe, Pd-meso-tetrakis-(4-trimethylaminophenyl)porphin (Pd-TAPP), in the presence of calf thymus DNA. These results may be attributed to the site competition of MMC with the probe and electron transfer between MMC and probe. MMC also increases polarization degree of the probe by covalent drug-DNA or DNA-drug-DNA crosslinking.

  5. Long-term outcome of mitomycin C- and 5-FU-based primary radiochemotherapy for esophageal cancer

    Energy Technology Data Exchange (ETDEWEB)

    Wolf, Maria; Zehentmayr, Franz; Niyazi, Maximilian; Ganswindt, Ute; Haimerl, Wolfgang; Belka, Claus [Dept. of Radiation Oncology, Univ. Hospital Munich, LMU (Germany); Schmidt, Michael [Inst. for Biometry and Epidemiology, Univ. Hospital Munich, LMU (Germany); Hoelzel, Dieter [Tumor Registry Munich, Univ. Hospital Munich, LMU (Germany)

    2010-07-15

    Background and purpose: for definitive radiochemotherapy, 5-fluorouracil/cisplatin protocols have been considered the standard of care for esophageal carcinoma over the last 2 decades. By contrast, most patients treated at the University Hospital, LMU Munich, Germany, received 5-fluorouracil/mitomycin C. The objective of this retrospective analysis was to determine the value of 5-fluorouracil/mitomycin-C-based therapy. Patients and methods: tumor stage, treatment received, and outcome data of patients treated for esophageal cancer between 1982 and 2007 were collected; endpoint of the analysis was overall survival. Results: 298 patients with inoperable cancer of the esophagus were identified (16.8% adenocarcinoma, 77.5% squamous cell carcinoma). At diagnosis, 61.7% (184/298) had UICC stage III-IV, 54.4% (162/298) positive lymph nodes, and 26.5% (79/298) metastatic disease. 74.5% of all patients (222/298) received radiation doses between 55 and 65 Gy, 65.8% (196/298) were subjected to concomitant chemotherapy. The median follow-up period (patients alive) was 4.1 years. A significant increase of overall survival (p < 0.0001) in the radiochemotherapy versus the radiotherapy=alone group was observed. 52% (102/196) in the 5-fluorouracil/mitomycin C group had tumor stages comparable to the RTOG 85-01 study cohort (T1-3 N0-1 M0). The median survival in this subgroup was 18.2 months, 3- and 5-year survival rates were 22.7% (21/102) and 15.0% (13/102), respectively. Conclusion: despite being nominally inferior to platinum-based radiochemotherapy, the overall survival rates are in a similar range. Thus, the mitomycin-C-based radiochemotherapy approach may considered to be as effective as the standard therapy. However, there is no randomized trial available in order to prove the equality. (orig.)

  6. 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.

  7. 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.

  8. Evidence for clinical efficacy of mitomycin C in heavily pretreated ovarian cancer patients carrying germ-line BRCA1 mutation.

    Science.gov (United States)

    Moiseyenko, Vladimir M; Chubenko, Vyacheslav A; Moiseyenko, Fedor V; Zhabina, Albina S; Gorodnova, Tatiana V; Komarov, Yuri I; Bogdanov, Alexey A; Sokolenko, Anna P; Imyanitov, Evgeny N

    2014-10-01

    Ovarian carcinomas (OC) arising in BRCA1 and BRCA2 mutation carriers demonstrate pronounced sensitivity to platinum-based therapy due to deficiency of double-strand break DNA repair. However, the choice of subsequent treatment lines for this category of women remains complicated. We considered mitomycin C for heavily pretreated hereditary OC patients, based on multiple evidence for BRCA-specific activity of this drug. Twelve patients carrying BRCA1 germ-line mutation were included in the study. All women had a history of surgical intervention followed by adjuvant platinum-based therapy; three patients also received platinating agents prior the operation. The number of preceding treatment lines for metastatic disease was one for three patients, two for four patients, three for two patients, four for two patients and six for one woman. Administration of mitomycin C (10 mg/m2, every 4 weeks) resulted in one complete response (duration 36 weeks), two partial responses (duration 36 and 48 weeks) and six instances of disease stabilization (duration 12, 16, 20, 24, 24 and 24 weeks). In addition, three patients with the stable disease showed a decline of CA-125 level. We conclude that mitomycin C may deserve further evaluation in clinical trials involving BRCA1/2-related cancers.

  9. [Response of HeLa cells to mitomycine C. III. The analysis of nucleoli of mother and daughter cells].

    Science.gov (United States)

    Petrov, Iu P; Neguliaev, Iu A; Tsupkina, N V

    2014-01-01

    The comparative analysis of the number of nucleoli in cells of the established HeLa-M line was carried out before and after exposure to mitomycin C in a concentration of 10 μg/ml for 2 h. Using time-lapse microscopy, nucleoli in mother and their respective daughter cells were computed. It has been shown that the average number of nucleoli per cell is generally higher in daughter cells than in mother cells, and a standard deviation, on the contrary, decreases. An average number of nucleoli in daughter cells, whose mother cells had been treated with mitomycin C, was higher than in corresponding cells of control group. The separate analysis has been performed for the cells having from 1 to 4 nucleoli. Nonrandom complete coincidence of the number of nucleoli in mather and daughter cells has been typicaly shown for about 1/7 of the total cell population. Mitomycin C reduces this value of about 1.5 times.

  10. 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...

  11. 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.

  12. Pre- and intraoperative mitomycin C for recurrent pterygium associated with symblepharon

    Directory of Open Access Journals (Sweden)

    Mohammed I

    2013-01-01

    Full Text Available Isyaku MohammedDepartment of Ophthalmology, Aminu Kano Teaching Hospital, Kano, NigeriaBackground: Treatment of recurrent pterygium associated with symblepharon usually involves the use of tissue grafting and/or the intraoperative application of mitomycin C (MMC. For the graft, a conjunctival/limbal autograft and/or amniotic membrane may be used. This generally requires extra technical skills and assistance, an increase in the cost and duration of surgery, and a more extensive anesthesia (a complete eye block or general anesthesia. Although widely used, safety concerns have been raised over MMC in the treatment of pterygia.Objective: The objective of this case report is to report the successful use of preoperative subconjunctival injection of low-dose (0.02% MMC one month before bare sclera excision of a multirecurrent pterygium, as well as the concomitant intraoperative application of MMC to the conjunctival fornix of the same eye after the excision of an associated symblepharon.Case report: A 31-year-old man from Kano, Northern Nigeria, presented to the eye clinic with a recurrent pterygium associated with an upper lid symblepharon in his right eye. He has had five previous pterygium excisions, with the last surgery involving conjunctival autografting and subconjunctival steroid injection. He was subsequently given 0.1 mL of 0.02% MMC as a subpterygial injection; one month later he had an alcohol-assisted bare sclera pterygium excision and a symblepharolysis with the intraoperative application of 0.02% MMC for 1 minute to the upper conjunctival fornix. Except for a Tenon granuloma that was simply excised, there has been no recurrence or other complications up to a year after surgery.Conclusion: As a cheaper and technically easier treatment option, a preoperative subconjunctival MMC injection followed by bare sclera pterygium excision was found to be effective in this patient with a recurrent pterygium. As at one-year follow-up, low

  13. Trabeculectomy with double low dose of mitomycin C – two years of follow-up

    Directory of Open Access Journals (Sweden)

    Errico D

    2011-12-01

    Full Text Available Donato Errico1, Francesca Scrimieri1, Roberta Riccardi1, Romolo Fedeli1, Giancarlo Iarossi21Opthalmology Unit, Glaucoma Service, Azienda Ospedaliera, Cardinale G Panìco, Tricase (Le, Italy; 2Department of Opthalmology, Ospedale Pediatrico Bambino Gesù, Rome, ItalyPurpose: To evaluate the efficacy and the safety of a surgical technique in which classic trabeculectomy ab externo is performed with a double application of low-dose mitomycin C (MMC in uncontrolled open-angle glaucoma (OAG patients.Method: A consecutive series of 43 white patients (43 eyes with uncontrolled primary OAG underwent trabeculectomy surgery. A double application of MMC (0.1% was performed: the first under the Tenon's capsule for 3 minutes, and the second below the scleral flap for 1 or 2 minutes, according to the risk factors. Complete success was defined as intraocular pressure (IOP <14 mmHg without any additional glaucoma surgery or medication. Qualified success was defined as IOP <14 mmHg with additional needling revision.Results: Mean preoperative IOP was 29.9 mmHg (SD 3.8 for all eyes evaluated. At 1 day postoperative, mean IOP was 6.7 mmHg (SD 1.26. At the end of the first 2 weeks postoperative, mean IOP was 8.6 mmHg (SD 1.7, at 12 months mean IOP was 11.3 mmHg (SD 1.4; P < 0.0001 and at 24 months mean IOP was 11.4 mmHg (SD 1.5; P < 0.0001. At 3 months, two eyes (5.4% underwent needling of the bleb for cystic blebs formation.Conclusion: In this study we presented the results after 2 years of follow-up of OAG undergoing trabeculectomy with dual administration of MMC (0.1 mg/mL. After 24 months, complete success was achieved in 93% of patients and a qualified success in 100% of patients.Keywords: glaucoma, trabeculectomy, mitomycin C

  14. 不同术式对翼状胬肉的治疗观察%The treatment effect of two transplantation of pteryginm combine mitomycin C

    Institute of Scientific and Technical Information of China (English)

    黄玉庚; 钱定国; 胡文禹

    2008-01-01

    Objective To compare the treatment effect of amniotie membrane transplantation(AMT) combine mitomycin C(MMC) and corneal limbal stem cell autograft transplantation combine mitomycin C surgery.Methods 234 pterygium patients(239eye) were randomly divided into two groups: routine resection and AMT combine mitomycin C,limbal epithelial autograft transplantation combine mitomycin C. Results The recrudescnce (3.25 % ) of AMT combine mitomycin C is lower than routine resection and limbal epithelial autograft transplantation combine mitomycin C(4.31% ). But there was no significant difference between these two groups. Conclusion The treatment of AMT combine mitomycin C is as good as Iimbal epithelial autograft transplantation combine mitomyein C and the recrudescnce is lower.%目的 比较翼状胬肉的常规切除+羊膜移植术(amniotic membrane transplantation,AMT)+联合丝裂霉素(MMC)(A组)及翼状胬肉的常规切除+自体角膜缘干细胞移植联合MMC(B组)进行治疗的疗效.方法 234例(239只眼),翼状胬患者随机分为两组,分别采用胬肉切除术+AMT联合MMC及翼状胬肉的常规切除+自体角膜缘干细胞移植联合MMC进行治疗,术后随访7~19个月比较复发率.结果 A组复发率3.25%,B组复发率4.31%,两组比较差异无统计学意义.结论 A组与B组效果均良好.

  15. An optimization protocol for Swiss 3T3 feeder cell growth-arrest by Mitomycin C dose-to-volume derivation strategy.

    Science.gov (United States)

    Chugh, Rishi Man; Chaturvedi, Madhusudan; Yerneni, Lakshmana Kumar

    2017-04-01

    Feeder cell functionality following growth-arrest with the cost-effective Mitomycin C vis-à-vis irradiation is controversial due to several methodological variables reported. Earlier, we demonstrated variability in growth arrested Swiss 3T3 feeder cell life-span following titration of feeder cell densities with Mitomycin C concentrations which led to the derivation of doses per cell. Alternatively, to counter the unexpected feeder regrowth at high exposure cell density, we proposed titration of a fixed density with arithmetically derived volumes of Mitomycin C solution that corresponded to permutations of specific concentrations and doses per cell. We now describe an experimental procedure of inducing differential feeder cell growth-arrest by titrating with such volumes and validating the best feeder batch through target cell growth assessment. A safe cell density of Swiss 3T3 tested for the exclusion of Mitomycin C resistant variants was titrated with a range of volumes of a Mitomycin C solution. The differentially growth-arrested feeder batches generated were tested for short-term and long-term viability and human epidermal keratinocyte growth supporting ability. The feeder cell extinction rate was directly proportional to the volume of Mitomycin C solution within a given concentration per se. The keratinocyte colony forming efficiency and the overall growth in mass cultures were maximal with a median extinction rate produced by an intermediate volume, while the faster and slower extinction rates by high and low volumes, respectively, were suboptimal. The described method could counter the inadequacies of growth-arrest with Mitomycin C.

  16. Formation of a major DNA adduct of the mitomycin metabolite 2,7-diaminomitosene in EMT6 mouse mammary tumor cells treated with mitomycin C.

    Science.gov (United States)

    Palom, Y; Belcourt, M F; Kumar, G S; Arai, H; Kasai, M; Sartorelli, A C; Rockwell, S; Tomasz, M

    1998-01-01

    Treatment of EMT6 mouse mammary tumor cells with [3H]mitomycin C (MC) results in the formation of six major DNA adducts, as described earlier using an HPLC assay of 3H-labeled products of enzymatic hydrolysis of DNA isolated from MC-treated cells. Four of these adducts were identified as monofunctional and bifunctional guanine-N2 adducts in the minor groove of DNA. In order to establish relationships between individual types of MC-DNA adducts and biological responses it is necessary to identify all of the adducts formed in cells. To this end we have now identified a predominant, previously unknown adduct formed in MC-treated EMT6 cells as a derivative not of MC, but of 2,7-diaminomitosene (2,7-DAM), the major bioreductive metabolite of MC. Rigorous proof demonstrates that it is a DNA major groove, guanine-N7 adduct of 2,7-DAM, linked at C-10 to DNA. The adduct is relatively stable at ambient temperature, but is readily depurinated upon heating. Its isolation from MC-treated cells indicates that MC is reductively metabolized to 2,7-DAM, which then undergoes further reductive activation to alkylate DNA, along with the parent MC. Low MC:DNA ratios were identified as a critical factor promoting 2,7-DAM adduct formation in an in vitro model calf thymus DNA/ MC/reductase model system, as well as in MC-treated EMT6 cells. The 2,7-DAM-guanine-N7 DNA adduct appears to be relatively noncytotoxic, as indicated by the dramatically lower cytotoxicity of 2,7-DAM in comparison with MC in EMT6 cells. Like MC, 2,7-DAM exhibited slightly greater cytotoxicity to cells treated under hypoxic as compared to aerobic conditions. However, 2,7-DAM was markedly less cytotoxic than MC under both aerobic and hypoxic conditions. Thus, metabolic reduction of MC to 2,7-DAM represents a detoxification process. The differential effects of MC-DNA and 2,7-DAM-DNA adducts support the concept that specific structural features of the DNA damage may play a critical role in the cytotoxic response to a DNA

  17. Mitomicina c en la esclerectomía profunda no perforante Mitomycin C in non-penetrating deep sclerostomy

    Directory of Open Access Journals (Sweden)

    Francisco García González

    1999-12-01

    Full Text Available Nuestro propósito en este trabajo es evaluar la eficacia de la Mitomicina C como inhibidor fibroblástico en la esclerectomía profunda no perforante (EPNP. Se realizó EPNP en 40 ojos con glaucoma crónico primario; 20 sin Mitomicina C y 20 con aplicación tópica intraoperatoria de Mitomicina C (0,5 mg/mL durante 5 min, evaluándose al 1, 6 y 12 meses. En la EPNP sin Mitomicina C la PIO se redujo de 27,40 ± 4,76 mmHg a 15,80 ± 2,50 mmHg requiriendo betabloqueadores 5 ojos (25 % a diferencia (p=,0001 de una reducción de 27,35 ± 2,91 mmHg a 7,15 ± 1,67 mmHg sin necesidad de betabloqueadores; con ampolla de filtración extensa, pálida, transparente y avascular y escasas complicaciones como hifema y dehiscencia conjuntival segmentaria. La EPNP con Mitomicina C fue más efectiva en el control de la PIO y su monodosificación tópica transoperatoria bien tolerada por los pacientes.We intend in this paper to assess the effectiveness of Mitomycin C as a fibroblastic proliferation inhibitor in the non-penetrating deep sclerostomy (NPDS. This procedure was performed in 40 eyes with primary chronic glaucoma, 20 of them were treated with intraoperative topycal Mitomycin C at 0,5 mg/mL for five minutes and 20 were not applied this drug. They were followed up and assessed one, six and twelve months after the surgery. In the NPDS without mitomycin C group, intraocular pressure was reduced from 27,40 ± 4,76 mmHg to 15,80 ± 2,50 mmHg, but 5 eyes required betablockers compared to a reduction from 27,35 ± 2,91 mmHg to 7,15 ± 1,67 mmHg without betablockers in the NPDS with Mitomycin C group, which presented and extensive, pale, transparent and avascular filtering ampulla and slight complications such as hyphema and dehiscence. The NPDS with mitomycin C was more effective in controlling intraocular pressure and transoperative topycal monodosage of this drug was well tolerated by the patients.

  18. 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.

  19. "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.

  20. 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.

  1. 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.

  2. 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.

  3. Mitomycin-C suppresses mucus secretion in an ileal neobladder rat model.

    Science.gov (United States)

    Fan, Weiwei; Yu, Yang; Shu, Junjie; Ming, Hao; Li, Weiping; Fan, Zhilu

    2015-08-01

    The aim of the present study was to investigate the mucus secretion status of mature goblet cells following the application of mitomycin-C (MMC) in ileal neobladder rat models. Bladder substitution models were established in Sprague Dawley rats, which had been divided into five groups, namely the control (sham), normal saline (NS), high-dose MMC (HMMC), low-dose MMC (LMMC) and dehydrated alcohol (DA) groups. To evaluate the total protein concentration and level of sialic acid following the therapy, urine from the rats in each group was collected on days 8, 11 and 14. In addition, to observe the variances between mucus secretion and the ileum goblet cells, immunohistochemistry and hematoxylin and eosin staining were conducted in the different groups on day 17. The results indicated that the ileal neobladder mucosas in the MMC groups were clearly undamaged, as compared with the DA group. Furthermore, the MMC and DA groups were shown to inhibit the proliferation of goblet cells. The concentration of protein and sialic acid in the LMMC group was found to be lower compared with the NS group, while the concentration in the HMMC group was considerably lower. In conclusion, HMMC was demonstrated to evidently reduce the mucin and sialic acid concentration in the urine, without visible damage to the ileal neobladder mucus membrane. Therefore, MMC may provide a novel therapeutic approach for the treatment of certain bladder conditions.

  4. Phellinus linteus Extract Augments the Immune Response in Mitomycin C-Induced Immunodeficient Mice

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    Shintaro Matsuba

    2008-01-01

    Full Text Available Phellinus linteus is a fungus distributed throughout Japan, Korea and China. Boiled water-soluble extracts from P. linteus (PLW have shown anti-tumor and immunomodulatory properties in experiments done by intraperitoneal treatment, or in in vitro cell cultures. This is the first investigation on how oral administration of PLW influences immune responses. Here, we established immunodeficient mice by mitomycin C (MMC and then researched how PLW influenced plaque-forming cell (PFC production and populations of cytokine [interferon- (IFNγ- and interleukin-4 (IL-4]-producing T lymphocytes. PLW samples were administered orally for 19 days (1, 2 or 4 g/kg/day. PFC assay was followed using Jerne's method. IFN- and IL-4-producing T lymphocyte populations were measured by flow-activated cell sorter (FACS. These assays were conducted the day after the last oral administration. MMC groups were given MMC (1 mg/kg/day intraperitoneally for 6 days with PLW administration. The number of PFC per 106 spleen cells increased significantly in the PLW (2 g/kg/day group when compared with the MMC-control (P < 0.05 while populations of IFNγ- and IL-4-producing T lymphocytes decreased by MMC treatment. However, the PLW group tended to increase more than the MMC-control. Our results indicated that PLW augments the immune response of the spleen in MMC-induced immunodeficient mice.

  5. Phellinus linteus Extract Augments the Immune Response in Mitomycin C-Induced Immunodeficient Mice.

    Science.gov (United States)

    Matsuba, Shintaro; Matsuno, Hideo; Sakuma, Masahiro; Komatsu, Yasuhiro

    2008-03-01

    Phellinus linteus is a fungus distributed throughout Japan, Korea and China. Boiled water-soluble extracts from P. linteus (PLW) have shown anti-tumor and immunomodulatory properties in experiments done by intraperitoneal treatment, or in in vitro cell cultures. This is the first investigation on how oral administration of PLW influences immune responses. Here, we established immunodeficient mice by mitomycin C (MMC) and then researched how PLW influenced plaque-forming cell (PFC) production and populations of cytokine [interferon- (IFNgamma-) and interleukin-4 (IL-4)]-producing T lymphocytes. PLW samples were administered orally for 19 days (1, 2 or 4 g/kg/day). PFC assay was followed using Jerne's method. IFN- and IL-4-producing T lymphocyte populations were measured by flow-activated cell sorter (FACS). These assays were conducted the day after the last oral administration. MMC groups were given MMC (1 mg/kg/day) intraperitoneally for 6 days with PLW administration. The number of PFC per 10(6) spleen cells increased significantly in the PLW (2 g/kg/day) group when compared with the MMC-control (P < 0.05) while populations of IFNgamma- and IL-4-producing T lymphocytes decreased by MMC treatment. However, the PLW group tended to increase more than the MMC-control. Our results indicated that PLW augments the immune response of the spleen in MMC-induced immunodeficient mice.

  6. Isolation and characterization of Chinese hamster ovary cell lines sensitive to mitomycin C and bleomycin

    Energy Technology Data Exchange (ETDEWEB)

    Robson, C.N.; Harris, A.L.; Hickson, I.D.

    1985-11-01

    Seven Chinese hamster ovary K1 cell lines exhibiting sensitivity to anticancer drugs have been isolated by a replica-plating technique. Five of the mutants are hypersensitive to the DNA cross-linking agent mitomycin C. Of these, one is also appreciably sensitive to UV light. Significant variations in their cross-sensitivity to cis-platinum(II) diammine dichloride, chlorambucil, and Adriamycin have also been observed. Two additional mutants have been isolated on the basis of sensitivity to the radiomimetic agent bleomycin. One of these shows greater than 6-fold sensitivity to bleomycin, while the other is approximately 14 times more sensitive than the parental strain to bleomycin and is also hypersensitive to a number of other DNA-damaging agents, including cis-platinum(II) diammine dichloride, chlorambucil, X-rays, and UV light. Both bleomycin-sensitive mutants also exhibit some degree of sensitivity to Adriamycin. In all cases, the cell lines have been grown in continuous culture for 3 months without evidence of reversion and should act as suitable recipients in DNA transfection experiments aimed at identifying human DNA repair genes.

  7. Protective effects of steroidal alkaloids isolated from Solanum paniculatum L. against mitomycin cytotoxic and genotoxic actions

    Directory of Open Access Journals (Sweden)

    PABLINE M. VIEIRA

    2013-06-01

    Full Text Available Solanum paniculatum L. is a plant species widespread throughout tropical America, especially in the Brazilian Cerrado region. It is used in Brazil for culinary purposes and in folk medicine to treat liver and gastric dysfunctions, as well as hangovers. Previous studies with S. paniculatum ethanolic leaf extract or ethanolic fruit extract demonstrated that they have no genotoxic activity neither in mice nor in bacterial strains, although their cytotoxicity and antigenotoxicity were demonstrated in higher doses. In order to assess the possible compounds responsible for the activities observed, we fractionated the ethanolic fruit extract of S. paniculatum, characterized by 1H and 13C NMR spectra, and evaluated two fractions containing steroidal alkaloids against mitomycin C (MMC using the mouse bone marrow micronucleus test. Swiss mice were orally treated with different concentrations (25, 50, or 100 mg.kg−1 of each fraction simultaneously with a single intraperitonial dose of MMC (4 mg.kg−1. Antigenotoxicity was evaluated by using the frequency of micronucleated polychromatic erythrocytes (MNPCE, whereas anticytotoxicity was assessed by the polychromatic and normochromatic erythrocytes ratio (PCE/NCE. Our results demonstrated that steroidal alkaloids isolated from S. paniculatum strongly protected cells against MMC aneugenic and/or clastogenic activities as well as modulated MMC cytotoxic action.

  8. Genome-Wide Mutational Signature of the Chemotherapeutic Agent Mitomycin C in Caenorhabditis elegans

    Directory of Open Access Journals (Sweden)

    Annie S. Tam

    2016-01-01

    Full Text Available Cancer therapy largely depends on chemotherapeutic agents that generate DNA lesions. However, our understanding of the nature of the resulting lesions as well as the mutational profiles of these chemotherapeutic agents is limited. Among these lesions, DNA interstrand crosslinks are among the more toxic types of DNA damage. Here, we have characterized the mutational spectrum of the commonly used DNA interstrand crosslinking agent mitomycin C (MMC. Using a combination of genetic mapping, whole genome sequencing, and genomic analysis, we have identified and confirmed several genomic lesions linked to MMC-induced DNA damage in Caenorhabditis elegans. Our data indicate that MMC predominantly causes deletions, with a 5′-CpG-3′ sequence context prevalent in the deleted regions of DNA. Furthermore, we identified microhomology flanking the deletion junctions, indicative of DNA repair via nonhomologous end joining. Based on these results, we propose a general repair mechanism that is likely to be involved in the biological response to this highly toxic agent. In conclusion, the systematic study we have described provides insight into potential sequence specificity of MMC with DNA.

  9. Involvement of apoptosis in mediating mitomycin C-induced teratogenesis in vitro.

    Science.gov (United States)

    Singh, Gyanendra; Sinha, Neeraj

    2010-05-01

    Mitomycin C (MMC) is among the most commonly used drugs worldwide and is known to cause congenital malformations and fetal death in animals. In this study, the effect of MMC on major organogenesis period and the role of apoptosis in mediating congenital malformations have been carried out. In the present study, post-implantation rat embryos of day 11 were cultured for 24 h with various concentrations of MMC, i.e. 1, 10, and 100 microg/ml cultures. The growth and developmental of each embryo was evaluated and compared with control ones for the presence of any malformations. The MMC decreased all growth and developmental parameters in a concentration-dependent manner, when compared with control. However, exposure to MMC at 1 microg/ml culture did not show any significant effect on embryonic growth and development. Parallel to this, flow cytometric analysis (cell cycle and annexin V binding) and DNA fragmentation assay were carried out followed by quantitation by 3'-OH labeling of cultured rat embryos to evaluate the role of apoptosis in bringing about MMC-induced teratogenesis. All results were found to be dose-dependent and an increase in apoptosis in embryonic tissues may be related to the increased risk of congenital malformations. The data suggested that apoptosis might be involved in mediating teratogenesis of MMC in vitro.

  10. Mitomycin C, 5-fluorouracil and radiation in advanced, locally recurrent rectal cancer.

    Science.gov (United States)

    Dobrowsky, W

    1992-02-01

    15 patients with inoperable presacral recurrent rectal cancer following surgery were treated with combined radiation and chemotherapy. Treatment consisted of split-course radiotherapy with 50 Gy in 25 fractions over 5 weeks and, after 4 weeks, an additional 20 Gy in 10 fractions over 2 weeks. At the start of treatment and following the split course, chemotherapy was administered. Mitomycin C was given on Day 1 (dose: 15 mg/m2 i.v. bolus) and 5-fluorouracil from Day 1 to Day 5 (dose: 750 mg/m2/24 h, continuous i.v. infusion). Owing to considerable, predominantly haematological and gastrointestinal toxicity, only six out of 15 patients received treatment according to the protocol. The symptomatic relief of symptoms was good. Pain was controlled in seven of eight symptomatic patients. Seven of the patients showed response according to computed tomography, but in none of these cases was a complete remission seen. After a follow-up of at least 30 months, only three patients are alive. The 1-, 2- and 3-year survival rates are 9/15, 6/15 and 3/12, respectively. The median survival is 14 months (range 4-60+ months). In comparison with historical data from the same institution, combined radio-chemotherapy did not show any prolongation of survival or increased response rate, but increased toxicity excessively, when compared with radiation alone.

  11. Deoxycholic acid-grafted PEGylated chitosan micelles for the delivery of mitomycin C.

    Science.gov (United States)

    Zhang, Xiu-Rong; Shi, Nian-Qiu; Zhao, Yang; Zhu, He-Yun; Guan, Jiao; Jin, Ying

    2015-06-01

    Mitomycin C (MTC) was incorporated to a micelle system preparing from a polymer named deoxycholic acid chitosan-grafted poly(ethylene glycol) methyl ether (mPEG-CS-DA). mPEG-CS-DA was synthesized and characterized by (1)H nuclear magnetic resonance ((1)H-NMR) and Fourier transform infrared spectroscopy. mPEG-CS-DA formed a core-shell micellar structure with a critical micelle concentration of 6.57 µg/mL. The mPEG-CS-DA micelles were spherical with a hydrodynamic diameter of about 231 nm. After poly(ethylene glycol)ylation of deoxycholic acid chitosan (CS-DA), the encapsulation efficiency and drug loading efficiency increased from 50.62% to 56.42% and from 20.51% to 24.13%, respectively. The mPEG-CS-DA micelles possessed a higher drug release rate than the CS-DA micelles. For pharmacokinetics, the area under the curve (AUC) of the mPEG-CS-DA micelles was 1.5 times higher than that of MTC injection, and these micelles can enhance the bioavailability of MTC. mPEG-CS-DA micelles reduced the distribution of MTC in almost all normal tissues and had the potential to improve the kidney toxicity caused by MTC injection.

  12. A Study of Toxic Effect of Mitomycin C on Cultured Bovine Trabecular Meshwork Cells

    Institute of Scientific and Technical Information of China (English)

    Fagang Jiang; Houren Wei; Yuanshu Lu; Ying Zhang; Yuanqing Zhou

    2000-01-01

    Purpose: To explore the toxicity of Mitomycin C (MMC) on trabecular meshwork cells.Methods: Bovine trabecular meshwork cells were cultured in vitro and exposed to MMC of different concentrations. The cellular morphology, ultrastructure, mortality and phagocytosis was studied with light microscopy, transmission electron microscopy and methods of Wright's stain, etc.Results: It was found that the toxic effect of MMC on the cells was in a dose-dependent mode. 1 × 10-2 and 1 × 10-3mg/ml of MMC caused a large part of cells dead, 1 × 10-4 and 1 × 10-5mg/ml of the drug had remarkable killing effect on the cells. 1 × 10-6mg/ml of MMC had still a mild toxicity, while 1 × 10-7 mg/ml of MMC had not any influence on cellular morphology, mortality, and phagocytosis, etc. The safe concentration on bovine trabecular meshwork cells was 1 × 10-7mg/ml and the LD50 was between 1 × 10-3and 1 × 10-4mg/ml.Conclusions: Refering to previous data, we conclude that conventional clinicalapplication of MMC might do harm to trabecular meshwork cells. Eye Science 2000; 16:38~ 42.

  13. Functional characterization of two SOS-regulated genes involved in mitomycin C resistance in Caulobacter crescentus.

    Science.gov (United States)

    Lopes-Kulishev, Carina O; Alves, Ingrid R; Valencia, Estela Y; Pidhirnyj, María I; Fernández-Silva, Frank S; Rodrigues, Ticiane R; Guzzo, Cristiane R; Galhardo, Rodrigo S

    2015-09-01

    The SOS response is a universal bacterial regulon involved in the cellular response to DNA damage and other forms of stress. In Caulobacter crescentus, previous work has identified a plethora of genes that are part of the SOS regulon, but the biological roles of several of them remain to be determined. In this study, we report that two genes, hereafter named mmcA and mmcB, are involved in the defense against DNA damage caused by mitomycin C (MMC), but not against lesions induced by other common DNA damaging agents, such as UVC light, methyl methanesulfonate (MMS) and hydrogen peroxide. mmcA is a conserved gene that encodes a member of the glyoxalases/dioxygenases protein family, and acts independently of known DNA repair pathways. On the other hand, epistasis analysis showed that mmcB acts in the same pathway as imuC (dnaE2), and is required specifically for MMC-induced mutagenesis, but not for that induced by UV light, suggesting a role for MmcB in translesion synthesis-dependent repair of MMC damage. We show that the lack of MMC-induced mutability in the mmcB strain is not caused by lack of proper SOS induction of the imuABC operon, involved in translesion synthesis (TLS) in C. crescentus. Based on this data and on structural analysis of a close homolog, we propose that MmcB is an endonuclease which creates substrates for ImuABC-mediated TLS patches.

  14. A Study of Toaic Effect of Mitomycin Con Cultured Bovine Trabecular Meshwork Cells

    Institute of Scientific and Technical Information of China (English)

    FagangJiang; HourenWei; 等

    2002-01-01

    Purpose:To explore the toxicity of Mitomycin C(MMC) on trabecular meshwork cells.Methods:Bovine trabecular meshwork cells were cultured in vitro and exposed to MMC of different concentrations.The cellular morphology,ultrastructure,mortality and phagocytosis was studied with light microscopy,transmission electron microscopy and methods of Wright's stain,etc.Results:It was found that the toxic effect of MMC on the cells was in a dose-dependent mode.1×10-2 and 1×10-3mg/ml of MMC caused a large part of cells dead,1×10-4 and 1×10-5mg/ml of the drug had remarkable dkilling effect on the cells.1×10-6mg/ml of MMC had still a mild toxicity,while 1×10-7 mg/ml of MMC had not any influence on cellular morphology,mortality,and phagocytosis,etc.The safe concentration on bovine trabecular meshwork cells was 1×10-7mg/ml and the LD50 was between 1×10-3 and 1×10-4mg/ml.Conclusions:Refering to previous data,we conclude that conventional clinical application of MMC might do harm to trabecular meshwork cells.Eye Science 2000;16:38-42.

  15. Binding of mitomycin C to blood proteins: A spectroscopic analysis and molecular docking

    Science.gov (United States)

    Jang, Jongchol; Liu, Hui; Chen, Wei; Zou, Guolin

    2009-06-01

    Mitomycin C (MMC) was the first recognized bioreductive alkylating agent, and has been widely used clinically for antitumor therapy. The binding of MMC to two human blood proteins, human serum albumin (HSA) and human hemoglobin (HHb), have been investigated by fluorescence quenching, synchronous fluorescence, circular dichroism (CD) spectroscopy and molecular docking methods. The fluorescence data showed that binding of MMC to proteins caused strong fluorescence quenching of proteins through a static quenching way, and each protein had only one binding site for the drug. The binding constants of MMC to HSA and HHb at 298 K were 2.71 × 10 4 and 2.56 × 10 4 L mol -1, respectively. Thermodynamic analysis suggested that both hydrophobic interaction and hydrogen bonding played major roles in the binding of MMC to HSA or HHb. The CD spectroscopy indicated that the secondary structures of the two proteins were not changed in the presence of MMC. The study of molecular docking showed that MMC was located in the entrance of site I of HSA, and in the central cavity of HHb.

  16. Safety and efficacy of adjunctive intranasal mitomycin C and triamcinolone in endonasal endoscopic dacryocystorhinostomy.

    Science.gov (United States)

    Li, Emmy Y; Cheng, Andy C; Wong, Alex C; Sze, Amy M; Yuen, Hunter K

    2016-02-01

    One of the common causes of failure in dacryocystorhinostomy for nasolacrimal duct obstruction (NLDO) is mucosal scarring and fibrosis around the ostium. Steroid and mitomycin C (MMC) can potentially reduce scarring by their action on the inflammatory and proliferative phase of wound healing, respectively. The purpose of this study is to evaluate the safety and efficacy of combined usage of adjunctive MMC and intranasal triamcinolone (TA) in endonasal endoscopic dacryocystorhinostomy (EE-DCR). This is a retrospective interventional case series. All patients underwent mechanical EE-DCR in two regional hospitals in Hong Kong from January 2005 to December 2006 were included. All received intraoperative MMC application for 5 min and gelfoam soaked with TA onto the ostium. Main outcome measures include the anatomical and functional success rate at follow-up at least 6 months after operation. Other outcomes include complications occurred during and after operation. A total of 73 EE-DCR were performed in 69 patients. Three patients had simultaneous bilateral DCR; one had sequential DCRs for both sides. At the last follow-up, anatomical success was achieved in 68 cases (93 %) and both anatomical with functional success in 67 cases (92 %). No major complication was observed. Minor complications included asymptomatic mucosal adhesion between the nasal septum and lateral nasal wall in one patient and moderate secondary hemorrhage in another. EE-DCR with adjunctive MMC and TA is a safe and successful procedure for the treatment of NLDO.

  17. Genome-Wide Mutational Signature of the Chemotherapeutic Agent Mitomycin C in Caenorhabditis elegans.

    Science.gov (United States)

    Tam, Annie S; Chu, Jeffrey S C; Rose, Ann M

    2015-11-12

    Cancer therapy largely depends on chemotherapeutic agents that generate DNA lesions. However, our understanding of the nature of the resulting lesions as well as the mutational profiles of these chemotherapeutic agents is limited. Among these lesions, DNA interstrand crosslinks are among the more toxic types of DNA damage. Here, we have characterized the mutational spectrum of the commonly used DNA interstrand crosslinking agent mitomycin C (MMC). Using a combination of genetic mapping, whole genome sequencing, and genomic analysis, we have identified and confirmed several genomic lesions linked to MMC-induced DNA damage in Caenorhabditis elegans. Our data indicate that MMC predominantly causes deletions, with a 5'-CpG-3' sequence context prevalent in the deleted regions of DNA. Furthermore, we identified microhomology flanking the deletion junctions, indicative of DNA repair via nonhomologous end joining. Based on these results, we propose a general repair mechanism that is likely to be involved in the biological response to this highly toxic agent. In conclusion, the systematic study we have described provides insight into potential sequence specificity of MMC with DNA.

  18. Blockage of IGF-1R signaling sensitizes urinary bladder cancer cells to mitomycin-mediated cytotoxicity

    Institute of Scientific and Technical Information of China (English)

    2001-01-01

    A major problem which is poorly understood in the management of bladder cancer is low sensitivity to chemotherapy and high recurrence after transurethral resection.Insulin-like growth factor 1 receptor(IGF-1R)signaling plays a very important role in progression,invasion and metastasis of bladder cancer cells.In this study,we investigated whether IGF-1R was involved in the growth stimulating activity and drug resistance of bladder cancer cells.The results showed: The mRNAs of IGF-1,IGF-2 and IGF-1R were strongly expressed in serum-free cultured T24 cell line,whereas normal urothelial cells did not express these factors/receptors or only in trace levels; T24 cell responded far better to growth stimulation by IGF-1 than did normal urothelial cells; blockage of IGF1R by antisense oligodeoxynucleotide(ODN)significantly inhibited the growth of T24 cell and enhanced sensitivity and apoptosis of T24 cells to mitomycin(MMC).These results suggested that blockage of IGF-IR signaling might potentially contribute to the treatment of bladder cancer cells which are insensitive to chemotherapy.

  19. Plasma mitomycin C concentrations determined by HPLC coupled to solid-phase extraction.

    Science.gov (United States)

    Paroni, R; Arcelloni, C; De Vecchi, E; Fermo, I; Mauri, D; Colombo, R

    1997-04-01

    The aim of this study was to set up a method for quantification of plasma mitomycin C (MMC) concentrations during intravesical chemotherapy delivered in the presence of local bladder hyperthermia (HT). In comparison with existing methods, this assay, characterized by relative simplicity and efficiency, resulted in the facilitation of performance with nondedicated instrumentation or nonspecialized staff. Purification from plasma matrix was carried out by solid-phase extraction under vaccuum. The purified drug was then collected directly into the vials of the HPLC autosampler. Chromatographic analysis was performed on a reversed-phase C18 column with water:acetonitrile (85:15 by vol) as the mobile phase and the UV detector set at 365 nm. The use of porfiromycin as internal standard provided a method with good within-day precision (CV 6.0% at 5 micrograms/L, n = 6), linearity (0.5-50 micrograms/L), and specificity. The lower limit of detection (< or = 0.5 microgram/L) proved to be suitable for plasma pharmacokinetics monitoring in two tested patients treated with MMC + HT for superficial bladder cancer.

  20. Determination of mitomycin C in human aqueous humor and serum by high-performance liquid chromatography.

    Science.gov (United States)

    Li, W Y; Seah, S K; Koda, R T

    1993-09-08

    Mitomycin C (MMC) is used in the treatment of disseminated adenocarcinoma of the stomach and pancreas and is used in ophthalmology as adjunctive therapy in trabeculectomy. Since only small volumes of aqueous humor are available for analysis, a sensitive method requiring limited sample preparation was developed. An internal standard, 4-aminoacetophenone, was added to aqueous humor specimens, and the solution was directly injected into the high-performance liquid chromatographic (HPLC) column. The use of a short 50-mm C18 reversed-phase column gave adequate resolution of peaks with improved sensitivity. The method was applicable for determination of MMC in serum, although solid-phase extraction for sample clean-up was required prior to injection into the HPLC column, and analytical columns of 150-250 mm were necessary for adequate resolution of peaks. The method has been validated and is linear from 6.25 to 50 ng/ml in aqueous humor and from 10 to 500 ng/ml in serum.

  1. Excimer laser phototherapeutic keratectomy in conjunction with mitomycin C in corneal macular and granular dystrophies

    Directory of Open Access Journals (Sweden)

    Erdem Yuksel

    2016-04-01

    Full Text Available ABSTRACT Purpose: To evaluate the visual outcomes, recurrence patterns, safety, and efficacy of excimer laser phototherapeutic keratectomy (PTK in conjunction with mitomycin C (MMC for corneal macular and granular diystrophies. Methods: The patients were divided into two groups. Group 1 included patients with macular corneal dystrophy (MCD that caused superficial corneal plaque opacities, and Group 2 included patients with granular corneal dystrophy (GCD. Patients in both groups were pre-, peri-, and postoperatively evaluated. The groups were compared in terms of uncorrected visual acuity (VA, best spectacle-corrected VA, presence of mild or significant recurrence, and time of recurrence. Results: Eighteen eyes (nine with MCD and nine with GCD of 18 patients (10 men and eight women were included. PTK was performed for each eye that was included in this study. The mean ablation amount was 117.8 ± 24.4 µm and 83.5 ± 45.7 µm in MCD and GCD, respectively, (p=0.18. The postoperative improvement of the mean VA was similar between the two groups before recurrences (p>0.43 and after recurrences (p>0.71. There were no statistically significant differences in the recurrence rate and the recurrence-free period for any recurrence type. Conclusion: PTK was an effective, safe, and minimally invasive procedure for patients with MCD and GCD. PTK in conjunction with MMC was similarly effective for both groups in terms of recurrence and visual outcomes.

  2. Effectiveness of scraping and mitomycin C to treat haze after myopic photorefractive keratectomy.

    Science.gov (United States)

    Spadea, Leopoldo; Verrecchia, Valerio

    2011-01-01

    To report the possibility of post myopic photorefractive keratectomy (PRK) haze treatment in a patient with expressed reluctance for any additional laser therapy. Seven months after bilateral PRK with subsequent development of corneal haze and refractive regression in both eyes, a 37-old-year male patient presented a best-spectacle corrected visual acuity (BSCVA) of 20/30 in the right eye and of 20/22 in the left eye. Both eyes were sequentially treated by scraping the stromal surface and application of mitomycin C (MMC) for 2 minutes. Both eyes had significant improvement in corneal transparency. Eighteen months after this treatment BSCVA had improved to 20/20 in each eye. No toxic effects were observed during either re-epithelialization or follow-up periods. In conclusion scraping and application of MMC could be considered a good tool in the treatment of selected cases of haze after myopic PRK, especially with patients that are reluctant to undergo a secondary laser procedure.

  3. Iatrogenic bleb formation and hypotony maculopathy following pterygium surgery with Mitomycin-C

    Directory of Open Access Journals (Sweden)

    Saeed Shokouhi-Rad

    2015-01-01

    Full Text Available Purpose: To report a case of late iatrogenic bleb formation and hypotony maculopathy after pterygium surgery applying Mitomycin C (MMC. Case Report: A 66-year-old man presented with an elevated, bleb-like, fluid-filled, cystic lesion on the nasal sclera of the right eye. The patient had undergone pterygium surgery with a combination of conjunctival autograft and adjuvant intraoperative MMC 0.02% four years before. The sclera seemed fistulized at the site of surgery and a thin layer of conjunctiva completely covered the lesion. A scleral patch graft was secured over the fistula with sutures, followed by excision of the thinned, avascular conjunctiva and advancement of the healthy adjacent conjunctiva to cover the patch graft. One month later, a small bleb re-appeared adjacent to the scleral patch graft and IOP was 2 mmHg. Argon-laser treatment of the bleb was tried to induce scarring and reduction of bleb size, and was highly effective. After one week, IOP was increased to 8 mmHg. The clinical features remained stable four months after initial presentation. Conclusion: Pterygium surgery using adjuvant MMC may result in late iatrogenic bleb formation and hypotony maculopathy. This complication can be successfully corrected surgically using a scleral patch graft combined with argon laser treatment over the inadvertent bleb.

  4. The Success Rate of Endocanalicular Laser Dacryocystorhinostomy with Two Different Mitomycin-C Application

    Directory of Open Access Journals (Sweden)

    Yesim Altay

    2014-03-01

    Full Text Available Aim: To determine the success rate of different application of mitomycin-c (mmc in endocanalicular multidiode laser dacryocystorhinostomy (ECL-DCR. Material and Method: A prospective comparative study was conducted on 89 patients with primary acquired nasolacrimal duct obstruction, undergoing ECL-DCR procedures. Group 1 was composed of 44 patients undergoing ECL-DCR with intraoperative 0.4 mg/ml mmc application for 2 minutes and group 2 was composed of 45 patients undergoing ECL-DCR with intraoperative 0.4 mg/ml mmc application for 5 minutes. Patients were followed up for at least 12 months.The main outcome measure for success was resolution or improvement of epiphora and patency of nasolacrimal duct with irrigation. Results: Final success was 26/44(%59.1 for group 1, and 36/45 (%80 for group 2.The difference was statistically significant (Chi-siquare, p=0.03. Discussion: Diode laser ECL-DCR with 0.4 mg /ml intraoperative mmc application for 5 minutes appears to be an effective treatment modality for primary nasolacrimal duct obstruction.

  5. Neoadjuvant Chemotherapy with Ifosfamide, Cisplatin, Adriamycin and Mitomycin (IMAP for High risk Adult Soft Tissue Sarcomas

    Directory of Open Access Journals (Sweden)

    Mohagheghi Mohammad Ali

    2009-05-01

    Full Text Available To define efficacy of pre-operative chemotherapy in down staging of advanced non-round cell soft tissue sarcomas. From Sep 2002 to Dec 2005, 70 patients were treated by Ifosfamid, MESNA, cisplatin, adriamycin, mitomycin and subsequent surgery. Postoperatively, patients received radiotherapy in cases of microscopically incomplete resection or local recurrence. The median age of the patients was 34 years and the median tumor size was 14 cm. According to AJCC classification 46 patients had stage 3 and 24 had stage 4 diseases. The most common subtypes were MFH and leiomyosarcoma. The most common sites of tumors were lower extremity and trunk. Toxicity grades three or higher consisted of nausea, Leucopenia and infection. About 50% of the patients received G-CSF. Response to chemotherapy was assessable in 63 patients; 9 patients achieved complete response and 16 showed partial response. Disease progressed in 8 and did not change in 37. The best response was seen with MFH, fibrosarcoma and synovial sarcoma. After chemotherapy seventy percent of patients underwent complete surgery. Disease relapsed in 41 patients and twenty two patients died of metastasis. Median survival of patients was 30 months. IMAP plus G-CSF is safe and effective as preoperative chemotherapy in some subtypes of sarcomas, although the metastasis problem has not been eliminated

  6. 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.

  7. 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...

  8. 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...

  9. 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...

  10. Nedd8-activating enzyme inhibitor MLN4924 provides synergy with mitomycin C through interactions with ATR, BRCA1/BRCA2, and chromatin dynamics pathways.

    Science.gov (United States)

    Garcia, Khristofer; Blank, Jonathan L; Bouck, David C; Liu, Xiaozhen J; Sappal, Darshan S; Hather, Greg; Cosmopoulos, Katherine; Thomas, Michael P; Kuranda, Mike; Pickard, Michael D; Liu, Ray; Bandi, Syamala; Smith, Peter G; Lightcap, Eric S

    2014-06-01

    MLN4924 is an investigational small-molecule inhibitor of the Nedd8-activating enzyme currently in phase I clinical trials. MLN4924 induces DNA damage via rereplication in most cell lines. This distinct mechanism of DNA damage may affect its ability to combine with standard-of-care agents and may affect the clinical development of MLN4924. As such, we studied its interaction with other DNA-damaging agents. Mitomycin C, cisplatin, cytarabine, UV radiation, SN-38, and gemcitabine demonstrated synergy in combination with MLN4924 in vitro. The combination of mitomycin C and MLN4924 was shown to be synergistic in a mouse xenograft model. Importantly, depletion of genes within the ataxia telangiectasia and Rad3 related (ATR) and BRCA1/BRCA2 pathways, chromatin modification, and transcription-coupled repair reduced the synergy between mitomycin C and MLN4924. In addition, comet assay demonstrated increased DNA strand breaks with the combination of MLN4924 and mitomycin C. Our data suggest that mitomycin C causes stalled replication forks, which when combined with rereplication induced by MLN4924 results in frequent replication fork collisions, leading to cell death. This study provides a straightforward approach to understand the mechanism of synergy, which may provide useful information for the clinical development of these combinations.

  11. 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…

  12. 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.

  13. Corneal melanosis successfully treated using topical mitomycin-C and alcohol corneal epitheliectomy: a 3-year follow-up case report

    Directory of Open Access Journals (Sweden)

    Mehmet Balcı

    2015-08-01

    Full Text Available ABSTRACTWe report a case of primary acquired corneal melanosis without atypia associated with corneal haze in a patient with a history of limbal malignant melanoma and the effect of mitomycin-C. A 75-year-old woman with a history of limbal malignant melanoma presented with loss of vision in right eye. Corneal examination showed a patchy melanotic pigmentation with a central haze. Topical mitomycin-C improved visual acuity and corneal haze. However, the pigmented lesions persisted, and they were removed with alcohol corneal epitheliectomy. Histopathological examination demonstrated primary acquired melanosis without atypia. The lesions were successfully removed, and there were no recurrences during the follow-up period of 36 months. The association of conjunctival and corneal melanosis without atypia is a rare condition. In addition, co-existence of central corneal haze and melanosis may decrease visual acuity. Topical mitomycin-C and alcohol corneal epitheliectomy can be useful treatments in this condition.

  14. Current treatment of nasal vestibular stenosis with CO2-laser surgery: prolonged vestibular stenting versus intraoperative mitomycin application. A case series of 3 patients.

    Science.gov (United States)

    van Schijndel, Olaf; van Heerbeek, Niels; Ingels, Koen J A O

    2014-12-01

    These case studies describe three cases of unilateral nasal vestibular stenoses caused by chemical cauterization. Each case was treated with CO2-laser surgery together with intraoperative topic application of mitomycin or prolonged vestibular stenting for prevention of restenosis. Two patients received intraoperative mitomycin application and one patient received prolonged vestibular stenting. Results were documented using high-resolution photographs. The follow up period ranged from 1 year and 3 months to 4 years and 9 months. All patients improved after CO2-laser surgery. No complications were reported. We consider CO2-laser surgery for relief of nasal vestibular stenosis as a feasible surgical technique for relieve of nasal vestibular stenosis. Prolonged vestibular stenting seems to be an important factor for the prevention of restenosis in which the value of intraoperative mitomycin application without prolonged vestibular stenting remains uncertain.

  15. Corneal melanosis successfully treated using topical mitomycin-C and alcohol corneal epitheliectomy: a 3-year follow-up case report.

    Science.gov (United States)

    Balcı, Mehmet; Yağcı, Ramazan; Güler, Emre; Haltaş, Hacer; Duman, Rahmi; Hepşen, İbrahim F

    2015-01-01

    We report a case of primary acquired corneal melanosis without atypia associated with corneal haze in a patient with a history of limbal malignant melanoma and the effect of mitomycin-C. A 75-year-old woman with a history of limbal malignant melanoma presented with loss of vision in right eye. Corneal examination showed a patchy melanotic pigmentation with a central haze. Topical mitomycin-C improved visual acuity and corneal haze. However, the pigmented lesions persisted, and they were removed with alcohol corneal epitheliectomy. Histopathological examination demonstrated primary acquired melanosis without atypia. The lesions were successfully removed, and there were no recurrences during the follow-up period of 36 months. The association of conjunctival and corneal melanosis without atypia is a rare condition. In addition, co-existence of central corneal haze and melanosis may decrease visual acuity. Topical mitomycin-C and alcohol corneal epitheliectomy can be useful treatments in this condition.

  16. Genotoxic and anti-genotoxic effects of esculin and its oligomer fractions against mitomycin C-induced DNA damages in mice.

    Science.gov (United States)

    Mokdad Bzeouich, Imen; Mustapha, Nadia; Maatouk, Mouna; Ghedira, Kamel; Ghoul, Mohamed; Chekir-Ghedira, Leila

    2016-12-01

    Mitomycin C is one of the most effective chemotherapeutic drugs against various solid tumors. However, despite its wide spectrum of clinical benefits, this agent is capable of inducing various types of genotoxicity. In this study, we investigated the effect of esculin and its oligomer fractions (E1, E2 and E3) against mitomycin C induced genotoxicity in liver and kidney cells isolated from Balb/C mice using the comet assay. Esculin and its oligomer fractions were not genotoxic at the tested doses (20 mg/kg and 40 mg/kg b.w). A significant decrease in DNA damages was observed, suggesting a protective role of esculin and its oligomer fractions against the genotoxicity induced by mitomycin C on liver and kidney cells. Moreover, esculin and its oligomer fractions did not induce an increase of malondialdehyde levels.

  17. Management experience of subglottic stenosis by endoscopic bougie dilatation with mitomycin C and review of literature: case series.

    Science.gov (United States)

    Liew, Y T; Yong, D J; Somasundran, M; Lum, C L

    2015-03-01

    The aim of the study was to examine and analyze the epidemiology and outcome of treatment for paediatric acquired subglottic stenosis treated with endoscopic bougie dilatation and topical mitomycin C. There were 15 patients identified from 2008 until 2013. All of them had acquired subglottic stenosis due to history of intubation. Majority of the patients had grade III stenosis, with the total of seven. Three patients had grade IV; three were grade II and two were grade I. All of the patients with severe stenosis (grade III and IV) needed tracheostomy while only one in mild stenosis group (grade I and II) required it for prolonged ventilation rather than obstruction due to subglottic stenosis. All of them underwent direct laryngoscopy under general anesthesia followed by endoscopic dilatation with bougie and topical mitomycin C 0.4 mg/ml for 5 min. Aim of success in our study was decannulation of tracheostomy or absence of symptoms at exertion. We achieved 6 (60 %) successful decannulation out of 10 patients with tracheostomy (excluded the patient with tracheostomy in grade I stenosis due to prolonged ventilation). As for those without tracheostomy, 3 (75 %) out of 4 patients were asymptomatic even at exertion. Average number of dilatation was 3.1 times, with mean duration of 28 min. No complications were reported in our series. One patient with grade I stenosis passed away due to severe pneumonia unrelated to the stenosis or dilatation, and she did not have any dilatation before she passed away. Multiple related risk factors were identified such as intubation, prematurity, movement of endotracheal tube, respiratory infection, traumatic intubation and gastroesophageal reflux disease. Experience of open surgical method was very limited in our centre in Sabah in East Malaysia. Endoscopic technique plays an important role in treatment of subglottic stenosis with adjunct like mitomycin C possibly booster the successful rate.

  18. New drug delivery system for corneal administration of mitomycin-C.

    Science.gov (United States)

    Pinheiro, Francisco Irochima; Araújo-Filho, Irami; Meneses do Rego, Amalia Cinthia; Pereira de Azevedo, Eduardo; Tabosa do Egito, Eryvaldo Socrates; Oréfice, Fernando; Alves de Souza Lima Filho, Acácio

    2016-08-01

    To develop a new corneal release system to deliver optimum amounts of mitomycin-C (MMC) during the perioperative period of photorefractive keratectomy (PRK). Ophthalmos S/A, São Paulo, Brazil. Experimental study. An in vitro experimental design was developed for studying a new MMC delivery system at a drug concentration of 0.02%. Whatman sterile filter paper disks with a diameter of 8.0 mm were impregnated with MMC solution. After drying, the disks were placed on agar plates seeded with Staphylococcus epidermidis; this was followed by instillation of a drop of sterile water. After 1 minute, the disks were removed and the plates were incubated for 48 hours at 35°C. The mean volume of the drops delivered from regular eyedrop bottles was determined, and the inhibition zone (in millimeters) was correlated with the amount of MMC loaded onto the disks. Analysis of the inhibition zones produced by MMC indicated that 16 μg was the optimum dose to be incorporated in the disks. The mean volume of a drop delivered from eyedrop bottles was 37.7 μL. One minute after the application of a single drop of a balanced salt solution, the system released an adequate concentration of MMC for PRK. A new delivery system for MMC was successfully developed for application during photorefractive keratectomy. Dr. de Souza Lima Filho is the managing director of Ophtalmos S/A. Drs. de Souza Lima Filho, Irochima Pinheiro, and Oréfice have exclusive rights to intellectual property of this invention secured by a patent application filed with the Instituto Nacional da Propriedade Industrial. Copyright © 2016 ASCRS and ESCRS. Published by Elsevier Inc. All rights reserved.

  19. Mitomycin C: new strategies to improve efficacy of a well-known therapy.

    Science.gov (United States)

    Ragonese, Mauro; Racioppi, Marco; Bassi, Pier Francesco; Di Gianfrancesco, Luca; Lenci, Niccolò; Filianoti, Alessio; Recupero, Salvatore M

    2016-10-04

    Mitomycin C (MMC) as an intravesical chemotherapeutic agent is a well-known option for treatment of nonmuscle invasive bladder cancer (NMIBC) recurrence; it is probably the most commonly used agent given its low rate of side effects and its efficacy.Both the American Urologic Association (AUA) and European Association of Urology (EAU) consider MMC as a standard treatment for immediate single-dose postoperative treatment and for adjuvant therapy in low and intermediate-risk NMIBC.Despite the popularity of this agent in the treatment of NMIBCs, many questions regarding the optimal approach to MMC therapy remain unanswered and the schedule widely used is empirical.Nevertheless, even when the current optimal approaches to MMC administration are used, a large proportion of NMIBCs recur.This apparent treatment resistance might be overcome by an optimization of standard MMC therapy or with a combination of MMC with other agents that have different mechanisms of action.Strategies to enhance passive delivery of MMC have been well studied and multiple measures are recommended for implementation of use in routine clinical practice.A modified scheme of instillation seems to be an easy and inexpensive alternative to increase efficacy of intravesical MMC and to also use this agent with an ablative intent.Enhancing tumor response with a sequential therapy is another option that has been investigated, mostly for chemo-immunotherapy wherein the different mechanisms of action of Bacillus of Calmette and Guerìn (BCG) and MMC are combined to achieve a higher response.

  20. Complications and outcomes of primary phacotrabeculectomy with mitomycin C in a multi-ethnic asian population.

    Directory of Open Access Journals (Sweden)

    David Z Chen

    Full Text Available To determine the occurrence of intraoperative and postoperative complications up to three years after primary phacotrabeculectomy with intraoperative use of Mitomycin C (MMC in primary open angle (POAG and primary angle closure glaucoma (PACG patients, and the effect of postoperative complications on surgical outcome.Retrospective review of 160 consecutive patients with POAG (n = 105 and PACG (n = 55, who underwent primary phacotrabeculectomy with MMC at the National University Hospital, Singapore, from January 1, 2008 to December 31, 2010. Data was collected using a standardized form that included patient demographic information, ocular characteristics and postoperative complications, including hypotony (defined as intraocular pressure < 6 mmHg, shallow anterior chamber (AC and hyphema.The mean age ± standard deviation (SD of patients was 68.2 ± 8.2 years. No patient lost light perception during duration of follow-up. 77% of the postoperative complications occurred within the first month only. The commonest complications were hypotony (n = 41, 25.6%, hyphema (n = 16, 10.0% and shallow AC (n = 16, 10.0%. Five patients (3.1% required reoperation for their complications. Early hypotony (defined as hypotony < 30 days postoperatively was an independent risk factor for surgical failure (hazard ratio [HR], 5.1; 95% CI, 1.6-16.2; p = 0.01. Hypotony with another complication was also a risk factor for surgical failure (p < 0.02.Hypotony, hyphema and shallow AC were the commonest postoperative complications in POAG and PACG patients after phacotrabeculectomy with MMC. Most complications were transient and self-limiting. Early hypotony within the first month was a significant risk factor for surgical failure.

  1. Mitomycin C-augmented trabeculectomy: subtenon injection versus soaked sponges: a randomised clinical trial.

    Science.gov (United States)

    Pakravan, Mohammad; Esfandiari, Hamed; Yazdani, Shahin; Douzandeh, Azadeh; Amouhashemi, Nassim; Yaseri, Mehdi; Pakravan, Parto

    2017-09-01

    To compare the efficacy and safety of subtenon injection of mitomycin C (MMC) with that of conventional application of MMC-soaked sponges in trabeculectomy. In this multicentre randomised clinical trial, 80 consecutive open-angle glaucoma cases were randomised into two groups; group 1 received a subtenon injection of 0.1 mL of 0.01% MMC, while group 2 received 0.02% MMC-soaked sponges. Primary outcome measure was intraocular pressure (IOP), and secondary outcome measures were endothelial cell count (ECC) changes and bleb morphology according to the Indiana Bleb Appearance Grading Scale. Outcome measures were compared at 1, 3 and 6 months postoperatively. Complete and qualified success was defined as IOP within 6-15 mm Hg without and with medications at month 6, respectively. Mean preoperative IOP was 21.8±5.1 in group 1, which reduced to 10.3±3.7 mm Hg at final visit (p<0.001). Corresponding values for group 2 were 21.8±5 and 10.8±3.5 mm Hg respectively (p<0.001). Complete success was 82.5% in both groups, and qualified success was 0 and 2.5% in groups 1 and 2, respectively. (p=0.316) The blebs tended to be more diffuse, less vascularised and shallower in group 1, at month 6 (p=0.45,<0.001 and <0.007 respectively). ECCs did not change significantly at final visit (p=0.813). Subtenon injection of MMC is a safe and effective alternative to the conventional soaked sponge method. This method produces more favourable bleb morphology after trabeculectomy. NCT02385370, Post-results. Published by the BMJ Publishing Group Limited. For permission to use (where not already granted under a licence) please go to http://www.bmj.com/company/products-services/rights-and-licensing/.

  2. Construction of humanized carcinoembryonic antigen specific single chain variable fragment and mitomycin conjugate

    Institute of Scientific and Technical Information of China (English)

    2007-01-01

    AIM: To construct a new target-oriented conjugate of humanized carcinoembryonic antigen (CEA) specific single chain variable fragment (scFv) and mitomycin (MMC) against colorectal cancer, and to investigate its influence on the growth and apoptosis of colorectal cancer cells.METHODS: The primer was designed according to the gene sequence described in reference 16, which respectively contains restriction enzyme cleavage sites BamH Ⅰ and EcoR Ⅰ in its upstream and downstream.PCR was performed with the plasmid as template containing genes of humanized anti-CEA scFv. The product was digested by BamH Ⅰ and EcoR Ⅰ, and connected to an expression vector which also has the restriction enzyme cleavage sites BamH Ⅰ and EcoR.Expression of the reaction was induced by isopropy-β-D-thiogalactoside (IPTG). Then the expression product was covalently coupled with MMC by dextran T-40. The immunoreactivity of the conjugate against colorectal cancer cells as well as CEA was measured by enzyme linked immunosorbent assay (ELISA). The inhibiting ratio of conjugate on the growth of colorectal cancer cells was also measured by ELISA. The effect of conjugate on the apoptosis of colorectal cancer cells was determined by flow cytometry (FCM).RESULTS: Restriction endonuclease cleavage and gene sequencing confirmed that the expression vector was successfully constructed. Sodium dodecyl sulfate polyacrylamide gel electropheresis (SDS-VAGE) confirmed that this vector correctly expressed the fusion protein.ELISA confirmed that the conjugate had quite a strong immunoreactivity against colorectal cancer cells and CEA. The conjugate had inhibitory effects on colorectal cancer cells in a concentration-dependent manner and could induce apoptosis of colorectal cancer cells in a concentration-dependent manner.CONCLUSION: The CEA-scFv-MMC conjugate can be successfully constructed and is able to inhibit the growth and induce apoptosis of colorectal cancer cells.

  3. Repurposing the anticancer drug mitomycin C for the treatment of persistent Acinetobacter baumannii infections.

    Science.gov (United States)

    Cruz-Muñiz, Martha Yumiko; López-Jacome, Luis Esau; Hernández-Durán, Melissa; Franco-Cendejas, Rafael; Licona-Limón, Paula; Ramos-Balderas, Jose Luis; Martinéz-Vázquez, Mariano; Belmont-Díaz, Javier A; Wood, Thomas K; García-Contreras, Rodolfo

    2017-01-01

    Acinetobacter baumannii is an emergent opportunistic bacterial pathogen responsible for recalcitrant infections owing to its high intrinsic tolerance to most antibiotics; therefore, suitable strategies to treat these infections are needed. One plausible approach is the repurposing of drugs that are already in use. Among them, anticancer drugs may be especially useful due their cytotoxic activities and ample similarities between bacterial infections and growing tumours. In this work, the effectiveness of four anticancer drugs on the growth of A. baumannii ATTC BAA-747 was evaluated, including the antimetabolite 5-fluorouracil and three DNA crosslinkers, namely cisplatin, mitomycin C (MMC) and merphalan. MMC was the most effective drug, having a minimum inhibitory concentration for 50% of growth in Luria-Bertani medium at ca. 7 µg/mL and completely inhibiting growth at 25 µg/mL. Hence, MMC was tested against a panel of 21 clinical isolates, including 18 multidrug-resistant (MDR) isolates, 3 of which were sensitive only to colistin. The minimum inhibitory concentrations and minimum bactericidal concentrations of MMC in all tested strains were found to be similar to those of A. baumannii ATCC BAA-747, and MMC also effectively killed stationary-phase, persister and biofilm cells. Moreover, MMC was able to increase survival of the insect larvae Galleria mellonella against an otherwise lethal A. baumannii infection from 0% to ≥53% for the antibiotic-sensitive A. baumannii ATCC BAA-747 strain and the MDR strains A560 and A578. Therefore, MMC is highly effective at killing the emergent opportunistic pathogen A. baumannii.

  4. Mitochondrial mutant cells are hypersensitive to ionizing radiation, phleomycin and mitomycin C

    Energy Technology Data Exchange (ETDEWEB)

    Kulkarni, Rohan; Reither, Adrian; Thomas, Robert A. [Department of Biological Sciences, Wayne State University, 5047 Gullen Mall, Suite 1370, Detroit, MI 48202 (United States); Tucker, James D., E-mail: jtucker@biology.biosci.wayne.edu [Department of Biological Sciences, Wayne State University, 5047 Gullen Mall, Suite 1370, Detroit, MI 48202 (United States)

    2009-04-26

    Mitochondrial DNA (mtDNA) is an important contributor to the ATP-generating oxidative phosphorylation complex. Single nucleotide mutations in mitochondrial genes involved in ATP synthesis result in a broad range of diseases. Leber optic atrophy and Leigh's syndrome are two such diseases arising from point mutations in the mitochondrial genome. Here, ionizing radiation, phleomycin and mitomycin C (MMC) were used to induce structural chromosomal aberrations in Leber's and Leigh's cells to investigate how these mitochondrial mutations affect the cell's DNA repair processes. Because of the energy deprivation that results from mitochondrial mutations, we hypothesized that these mutant cells would demonstrate hypersensitivity when exposed to oxidative and genotoxic stress and we also expected that these cells would not be able to repair nuclear DNA damage as efficiently as normal cells. As a consequence, these mutant cells are expected to show increased levels of DNA damage, longer cell cycle delays and increased levels of cell death. Following acute radiation exposure these mutant cells showed an increase in the number of chromosomal aberrations and decreased mitotic indices when compared with normal human lymphoblastoid cells with wild-type mtDNA. When exposed to phleomycin or MMC, the mitochondrial mutant cells again showed hypersensitivity and decreased mitotic indices compared to normal cells. These results suggest that Leber's and Leigh's cells have an impaired ability to cope with oxidative and genotoxic stress. These observations may help explain the role of ATP generation in understanding the enhanced sensitivity of mitochondrial mutant cells to cancer therapeutic agents and to adverse environmental exposure, suggesting that individuals with mtDNA mutations may be at a greater risk for cancer and other diseases that result from an accumulation of nuclear DNA damage.

  5. New Method to Prepare Mitomycin C Loaded PLA-Nanoparticles with High Drug Entrapment Efficiency

    Science.gov (United States)

    Hou, Zhenqing; Wei, Heng; Wang, Qian; Sun, Qian; Zhou, Chunxiao; Zhan, Chuanming; Tang, Xiaolong; Zhang, Qiqing

    2009-07-01

    The classical utilized double emulsion solvent diffusion technique for encapsulating water soluble Mitomycin C (MMC) in PLA nanoparticles suffers from low encapsulation efficiency because of the drug rapid partitioning to the external aqueous phase. In this paper, MMC loaded PLA nanoparticles were prepared by a new single emulsion solvent evaporation method, in which soybean phosphatidylcholine (SPC) was employed to improve the liposolubility of MMC by formation of MMC-SPC complex. Four main influential factors based on the results of a single-factor test, namely, PLA molecular weight, ratio of PLA to SPC (wt/wt) and MMC to SPC (wt/wt), volume ratio of oil phase to water phase, were evaluated using an orthogonal design with respect to drug entrapment efficiency. The drug release study was performed in pH 7.2 PBS at 37 °C with drug analysis using UV/vis spectrometer at 365 nm. MMC-PLA particles prepared by classical method were used as comparison. The formulated MMC-SPC-PLA nanoparticles under optimized condition are found to be relatively uniform in size (594 nm) with up to 94.8% of drug entrapment efficiency compared to 6.44 μm of PLA-MMC microparticles with 34.5% of drug entrapment efficiency. The release of MMC shows biphasic with an initial burst effect, followed by a cumulated drug release over 30 days is 50.17% for PLA-MMC-SPC nanoparticles, and 74.1% for PLA-MMC particles. The IR analysis of MMC-SPC complex shows that their high liposolubility may be attributed to some weak physical interaction between MMC and SPC during the formation of the complex. It is concluded that the new method is advantageous in terms of smaller size, lower size distribution, higher encapsulation yield, and longer sustained drug release in comparison to classical method.

  6. Apoptosis of human gastric cancer SGC-7901 cells induced by mitomycin combined with sulindac

    Institute of Scientific and Technical Information of China (English)

    Li Ma; Yong-Le Xie; Yi Yu; Qiu-Ning Zhang

    2005-01-01

    AIM: To investigate the effects of mitomycin (MMC)combined with sulindac on cell viability, apoptotic induction and expression of apoptosis-related gene Bcl-2 and cyclooxygenase-2 (COX-2)in gastric cancer SGC-7901cells.METHODS: Human gastric cancer SGC-7901 cells were divided into three treatment groups,namely sulindac treatment group, MMC treatment group and combined sulindac with MMC treatment group. After being treated with drugs, cell viability was examined by MTr assay.Flow cytometry was used to evaluate the cell cycle distribution and apoptotic rates. Morphology of the cells was observed under light microscope and interactive laser microscope. Expression of COX-2 and Bcl-2 was determined by immunocytochemical method.RESULTS: After exposure for 12 h to three kinds of drugs,gastric cancer SGC-7901 cells presented some morphological features of apoptosis, including cell shrinkage, nuclear condensation, DNA fragmentation and formation of apoptotic bodies. Growth inhibition was more obvious in combined sulindac with MMC treatment group and sulindac treatment group than in MMC treatment group. The apoptotic rates in co-treated cells and MMC-treated cells 24 h after treatment were 12.0% and 7.2%, respectively.After exposure for 24 h to MMC, the expression of COX-2and Bcl-2 protein was up-regulated, COX-2 levels were down-regulated but Bcl-2 gene expression was not changed significantly in combined treatment group.CONCLUSION: MMC-induced apoptosis is reduced by up-regulating the expression of COX-2 and Bcl-2 genes.MMC combined with sulindac can suppress the growth of gastric cancer cells through induction of apoptosis mediated by down-regulation of apoptosis-related Bcl-2and COX-2 gene.

  7. Synthesis of an oligodeoxyribonucleotide adduct of mitomycin C by the postoligomerization method via a triamino mitosene.

    Science.gov (United States)

    Champeil, Elise; Paz, Manuel M; Ladwa, Sweta; Clement, Cristina C; Zatorski, Andrzej; Tomasz, Maria

    2008-07-23

    The cancer chemotherapeutic agent mitomycin C (MC) alkylates and cross-links DNA monofunctionally and bifunctionally in vivo and in vitro, forming six major MC-deoxyguanosine adducts of known structures. The synthesis of one of the monoadducts (8) by the postoligomerization method was accomplished both on the nucleoside and oligonucleotide levels, the latter resulting in the site-specific placement of 8 in a 12-mer oligodeoxyribonucleotide 26. This is the first application of this method to the synthesis of a DNA adduct of a complex natural product. Preparation of the requisite selectively protected triaminomitosenes 14 and 24 commenced with removal of the 10-carbamoyl group from MC, followed by reductive conversion to 10-decarbamoyl-2,7-diaminomitosene 10. This substance was transformed to 14 or 24 in several steps. Both were successfully coupled to the 2-fluoro-O(6)-(2-trimethylsilylethyl)deoxyinosine residue of the 12-mer oligonucleotide. The N(2)-phenylacetyl protecting group of 14 after its coupling to the 12-mer oligonucleotide could not be removed by penicillinamidase as expected. Nevertheless, the Teoc protecting group of 24 after coupling to the 12-mer oligonucleotide was removed by treatment with ZnBr2 to give the adducted oligonucleotide 26. However, phenylacetyl group removal was successful on the nucleoside-level synthesis of adduct 8. Proof of the structure of the synthetic nucleoside adduct included HPLC coelution and identical spectral properties with a natural sample, and (1)H NMR. Structure proof of the adducted oligonucleotide 26 was provided by enzymatic digestion to nucleosides and authentic adduct 8, as well as MS and MS/MS analysis.

  8. Pharmacokinetics of mitomycin C after resection of peritoneal carcinomatosis and intraperitoneal chemohyperthermic perfusion.

    Science.gov (United States)

    Cerretani, D; Nencini, C; Urso, R; Giorgi, G; Marrelli, D; De Stefano, A; Pinto, E; Cioppa, T; Nastri, G; Roviello, F

    2005-12-01

    Over the last few years surgery on patients with abdominal malignancies has become more aggressive but the majority of patients present locoregional recurrence as peritoneal dissemination. Cytoreductive surgery followed by intraperitoneal chemohyperthermic perfusion (ICHP) has been described for treatment and prevention of locoregional cancer spread from various origins. This paper reports our study of the pharmacokinetics of mitomycin C (MMC) administered by intraperitoneal chemohyperthermic perfusion (ICHP) in patients with peritoneal carcinomatosis. 28 patients received MMC 20 mg/m2 intraperitoneally as a perfusion over 60 min. MMC was determined in perfusate, plasma and urine samples with a UV-HPLC method. A compartmental model was used to fit the drug concentrations in plasma and perfusate. Our results showed a mean maximum plasma concentration (Cmax) of 0.14 +/- 0.086 microg/ml with a peak time (Tmax) of 48..7 +/- 5.61 min. The mean area under the curve (AUC) and terminal half-life (t1/2) were 15.8 +/- 9.8 mg x min/L and 83.7 +/- 31.74 min respectively. Clearance (CL) was estimated by fitting the data by a compartmental model and the mean value was 72 +/- 66 L/h. The percent of the dose absorbed was very variable and ranged between 14 and 57% (mean 37 +/- 14%). The mean percentage of dose recovered unchanged in the urine during 24 hours was 7.21 +/- 3.73%. We conclude that ICHP in patients with peritoneal surface malignancies seems to have clinical value since it gives high peritoneal and tumor MMC concentrations with limited systemic exposure and toxicity.

  9. Mitigating effect of Indian propolis against mitomycin C induced bone marrow toxicity.

    Science.gov (United States)

    Kumari, Sandhya; Naik, Prashantha; Vishma, B L; Salian, Sujith Raj; Devkar, Raviraj Anand; Khan, Saleemulla; Mutalik, Srinivas; Kalthur, Guruprasad; Adiga, Satish Kumar

    2016-10-01

    A major drawback with cancer chemotherapy is its severe toxic effects on non-target tissues. Assessment of natural products for their protective effect against anticancer drugs-induced toxicity is gaining importance in cancer biology. The present study was aimed at assessing the protective effect of hydroethanolic extract of Indian propolis (HEIP) against mitomycin C (MMC)-induced genotoxicity and cytotoxicity. Swiss albino mice were injected with various doses of HEIP (100, 200, 300, 400, 600 and 800 mg/kg b. wt., i.p) 1 h prior to MMC (8 mg/kg, i.p.) injection. The geno- and cyto-toxicities were evaluated in mice by performing bone marrow micronucleus and TUNEL assays. In vitro antioxidant and lipid peroxidation inhibitory assays were carried out to understand the mechanism of the protective effects. The significant increase in the frequency of micronculeated cells (12.51 ± 0.48), apoptotic cells (23.43 ± 1.86) and reduction in P/N ratio (0.69 ± 0.04) compared with control indicated the potential geno- and cytotoxic effects of MMC in bone marrow. Pretreatment with HEIP resulted in the significant recovery of the toxic effects induced by MMC. HEIP at 400 mg/kg b. wt. was found to be the optimum dose imparting the maximum protective effects. The in vitro antioxidant and lipid peroxidation inhibitory assays suggest that the extract possesses substantial free radical scavenging activities. In conclusion, HEIP possesses substantial geno- and cyto-protective properties against MMC, which could be mediated through efficient free radical scavenging and inhibitory effect on lipid peroxidation.

  10. Synthesis of Mitomycin C and Decarbamoylmitomycin C N(2) deoxyguanosine-adducts.

    Science.gov (United States)

    Champeil, Elise; Cheng, Shu-Yuan; Huang, Bik Tzu; Conchero-Guisan, Marta; Martinez, Thibaut; Paz, Manuel M; Sapse, Anne-Marie

    2016-04-01

    Mitomycin C (MC) and Decarbamoylmitomycin C (DMC) - a derivative of MC lacking the carbamate on C10 - are DNA alkylating agents. Their cytotoxicity is attributed to their ability to generate DNA monoadducts as well as intrastrand and interstrand cross-links (ICLs). The major monoadducts generated by MC and DMC in tumor cells have opposite stereochemistry at carbon one of the guanine-mitosene bond: trans (or alpha) for MC and cis (or beta) for DMC. We hypothesize that local disruptions of DNA structure from trans or cis adducts are responsible for the different biochemical responses produced by MC and DMC. Access to DNA substrates bearing cis and trans MC/DMC lesions is essential to verify this hypothesis. Synthetic oligonucleotides bearing trans lesions can be obtained by bio-mimetic methods. However, this approach does not yield cis adducts. This report presents the first chemical synthesis of a cis mitosene DNA adduct. We also examined the stereopreference exhibited by the two drugs at the mononucleotide level by analyzing the formation of cis and trans adducts in the reaction of deoxyguanosine with MC or DMC using a variety of activation conditions. In addition, we performed Density Functional Theory calculations to evaluate the energies of these reactions. Direct alkylation under autocatalytic or bifunctional conditions yielded preferentially alpha adducts with both MC and DMC. DFT calculations showed that under bifunctional activation, the thermodynamically favored adducts are alpha, trans, for MC and beta, cis, for DMC. This suggests that the duplex DNA structure may stabilize/oriente the activated pro-drugs so that, with DMC, formation of the thermodynamically favored beta products are possible in a cellular environment.

  11. Efficacy of treatment for pterygium by autologous conjunctival transplantation and mitomycin C

    Institute of Scientific and Technical Information of China (English)

    XU Yan; ZHOU Huan-ming; LI Jun; KE Bi-lian; XU Xun

    2012-01-01

    Background The recurrence of pterygium after surgery is high.A variety of adjunctive treatment approaches have been developed to improve the clinical efficacy and many related articles have been published.This study aimed to determine the risk for postoperative pterygium recurrence comparing autologous conjunctival transplantation (ACT)versus mitomycin C (MMC).Methods Relevant literature published until December 2010 in Medline,Embase,Cochrane,Cochrane library,Science Citation Index,and Google Scholar were searched.Qualified random clinical trial (RCT) studies on the comparison of recurrence rate of pterygium after ACT and MMC treatment were included in this study.Results Eight RCTs with 663 eyes entered the final analysis.The recurrent rate of pterygium was 8.7% (30/343) for ACT and 18.75% (60/320) for MMC.Using fixed-effect meta analysis,we found that the recurrence was significantly lower after ACT than MMC treatment (odds ratio (OR)=0.40,95% confidence index (CI),0.25-0.63,P <0.0001).In sensitivity analyses,we employed random-effects model and excluded studies of low quality or studies in which MMC was administrated after the operation.All the sensitivity analyses confirmed that ACT led to lower recurrence rates than MMC.Sub-group analysis revealed that the recurrence rate was 20.2% (20/99) and 27.65% (26/94) for conjunctival autograft (CA) and MMC respectively,and no significant difference in the recurrence rate was detected (OR=0.65,95%CI 0.33-1.28,P=0.22).However,we found that conjunctival limbal autograft (CLA) had lower recurrence rate than MMC (OR=0.26,95% CI 0.14-0.48,P=0.0001).Conclusion CLA has better therapy efficacy against the recurrence of pterygium than MMC.

  12. Recurrent verrucous carcinoma of the urinary bladder after transurethral resection followed by intravesical mitomycin, and a review of the literature.

    Science.gov (United States)

    Hassan, Masroor; Qureshi, Asim; Nasir, Humaira

    2016-06-15

    Verrucous carcinoma (VC) is a locally invasive, non-metastasising well differentiated variant of squamous cell carcinoma. It is very rare in the urinary bladder and mostly associated with schistosomiasis. It has a characteristic multilobular appearance with small surface projections on contrast cystogram. Owing to its bland cytology, it is a challenging diagnosis. We report a case of VC of the bladder-unrelated to schistosomiasis and involving the prostate-that recurred after transurethral resection of the tumour and prostate followed by six doses of intravesical mitomycin. To the best of our knowledge, no such case has been reported from Pakistan. 2016 BMJ Publishing Group Ltd.

  13. Conservative treatment for late-onset bleb leaks after trabeculectomy with mitomycin C in patients with ocular surface disease

    Directory of Open Access Journals (Sweden)

    Sagara H

    2012-08-01

    Full Text Available Hideto Sagara,1,2 Tomohiro Iida,2,3 Kimimori Saito,4 Hiroki Noji,2 Masashi Ogasawara,2 Hiroshi Oyamada21The Marui Eye Clinic, Fukushima, 2Department of Ophthalmology, Fukushima Medical University School of Medicine, Fukushima, 3Tokyo Women's Medical University, Tokyo, 4Matuki Eye Clinic, Fukushima, JapanBackground: Sodium hyaluronate and autologous serum eye drops are used to treat ocular surface disease (OSD and are reported to prevent and treat late-onset bleb leaks following trabeculectomy with mitomycin C. In this study, we evaluated the efficacy of a combination of sodium hyaluronate and autologous serum eye drops and treatment for obstructive meibomian gland dysfunction as a therapy for late-onset bleb leaks after trabeculectomy with mitomycin C.Methods: This was a retrospective, interventional, nonsimultaneous study of 12 subjects (12 eyes of mean age of 64.3 ± 18.3 years with OSD and apparent late-onset bleb leaks following trabeculectomy with mitomycin C between 1998 and 2008. We compared patients diagnosed with leakages before July 2005, who had been treated with separate eye drop solutions containing 0.1% sodium hyaluronate, 50% autologous serum, and 0.3% ofloxacin (sodium hyaluronate and autologous serum group, n = 7, with patients diagnosed from August 2005 to December 2008, who were treated with a combination of eye drops (0.1% sodium hyaluronate, 50% autologous serum, and 0.08% levofloxacin hydrate and eyelid massage and warm compresses for obstructive meibomian gland dysfunction (combination eye drop group, n = 5.Results: Leakage was resolved in one patient (14.3% in the separately treated sodium hyaluronate and autologous serum eye drop group and in five patients (100% in the combination eye drop group (P = 0.015. The period after resolution of leakage with conservative treatment was 23 months in the one eye in the sodium hyaluronate and autologous serum group and 36–61 (mean 52.4 ± 10.1 months in the five eyes in the

  14. 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.

  15. 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.

  16. 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.

  17. 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.

  18. 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...

  19. 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.

  20. Effect of N-hydroxyurea, mitomycin C and actinomycin D on tumour formation on the leaves of Kalanchoe daigremontiana

    Directory of Open Access Journals (Sweden)

    Józef Koawalczyk

    2014-01-01

    Full Text Available The leaves of Kalanchoe daigremontiana wounded and infected with Agrobacterium tumefaciens were treated with single doses of inhibitors (hydroxyurea - 190, mitomycin - 0.5, actinomycin - 2 µ,g per leaf. After delaying the time' of dosage of inhibitors during five days after inoculation, changes in susceptibility of the system to antitumorous activity of analysed compounds were observed. In several hours after inoculation (period of the bacteria metabolic activity in wounds all the inhibitors prevent strongly the tumour formation. At the time between 14 and 72 hours after inoculation, including the phase of tumour induction, the system becomes sensitive to the DNA synthesis inhibitors, particularly hydroxyurea. The intensified action of actinomycin appears again only about 60 hours after inoculation and lasts till the end of experiment (the initiation of the transformed plant cell proliferation. According to the literature the antitumorous effect of inhibitors could be connected with their action on the bacteria metabolism inside the host tissue. The activities of hydroxyurea and mitomycin in the second period correspond with the intensive DNA synthesis in plant cells, which is induced by wounding. The effect of actinomycin D in 60 hours after inoculation could depend upon the inhibition of the proliferation of the transformed host cells.

  1. Genotoxicity and cytotoxicity evaluation of oenothein B and its protective effect against mitomycin C-induced mutagenic action.

    Science.gov (United States)

    Silva, Cinthia Aparecida; Silva, Carolina Ribeiro; Véras, Jefferson Hollanda; Chen-Chen, Lee; Ferri, Pedro Henrique; Santos, Suzana da Costa

    2014-06-01

    The natural product oenothein B (OeB), a dimeric macrocyclic ellagitannin, has a wide range of biological activities, such as antioxidant, anti-inflammatory, anti-viral, antifungal, and antitumor. However, investigations concerning its genotoxicity have not been carried out. This study assessed the cytotoxicity, genotoxicity, and protective effects of oenothein B using in vitro SOS-Inductest and in vivo mouse bone marrow micronucleus (MN) assay through oral and intraperitonial routes. In both assays oenothein B did not produce genotoxic effects in any of doses tested; in contrast, cytotoxic effect in cells was detected only in mice groups treated by both routes and exposed for 24 and 48h. Antigenotoxic and anticytotoxic activities of oenothein B were evaluated using both assays in combination with mitomycin C (MMC), a bioreductive alkylating agent. In the MN assay, a significant reduction was observed in MN frequency in all groups co-treated with MMC and OeB compared to those which received only MMC. Anticytotoxicity was observed in mice groups exposed to OeB and MMC for 24 and 48h. In the SOS-Inductest, oenothein B failed to show antigenotoxic and anticytotoxic effects; thus, it undoubtedly showed an in vivo protective activity against primary DNA damage induced by mitomycin C.

  2. Palliative hepatic intraarterial chemotherapy (HIC) using a novel combination of gemcitabine and mitomycin C: results in hepatic metastases

    Energy Technology Data Exchange (ETDEWEB)

    Vogl, Thomas J. [Johann Wolfgang Goethe University Clinic, Institute of Diagnostic and Interventional Radiology, Frankfurt am Main (Germany); Klinikum der Johann Wolfgang Goethe-Universitaet, Institut fuer Diagnostische und Interventionelle Radiologie, Theodor-Stern-Kai 7, Frankfurt am Main (Germany); Zangos, Stephan; Eichler, Katrin; Bauer, Ralf W. [Johann Wolfgang Goethe University Clinic, Institute of Diagnostic and Interventional Radiology, Frankfurt am Main (Germany); Selby, J.B. [Medical University of South Carolina, Institute of Radiology, Charleston, SC (United States)

    2008-03-15

    To evaluate repeated hepatic intraarterial chemotherapy (HIC) as a palliative treatment option for unresectable cholangiocarcinoma and liver metastases of various origins that were progressive under systemic chemotherapy. Between 2002 and 2006, 55 patients were treated in 4-week intervals (mean five sessions). Combined gemcitabine/mitomycin was administered intraarterially within 1 h. Tumor response was evaluated after the third session according to RECIST. Treated tumor entities were colorectal carcinoma (CRC) (n = 12), breast cancer (BC) (n = 12), cholangiocarcinoma (CCC) (n = 10), pancreatic (n = 4), ovarian (n = 3), gastric, cervical, papillary (each n = 2), prostate, esophageal carcinoma, leiomyosarcoma (each n = 1), cancer of unknown primacy (CUP) (n = 5). All patients tolerated the treatment well without any major side effects or complications. In total, there were 1 complete response (CR), 19 partial responses (PR), 19 stable (SD) and 16 progressive diseases (PD). We observed 5 PR, 3 SD and 4 PD in CRC; 1 CR, 4 PR, 6 SD in BC; and 2 PR, 2 SD and 6 PD in CCC. Median survival after first HIC was 9.7 months for CRC, 11.4 months for BC and 6.0 months for CCC. HIC with gemcitabine/mitomycin is a safe, minimally invasive, palliative treatment for hepatic metastases that are progressive under systemic chemotherapy. The treatment yields respectable tumor control rates in CRC and BC patients. (orig.)

  3. Twelve-Year Outcomes of Pterygium Excision with Conjunctival Autograft versus Intraoperative Mitomycin C in Double-Head Pterygium Surgery

    Directory of Open Access Journals (Sweden)

    Tommy C. Y. Chan

    2015-01-01

    Full Text Available Purpose. The study aims to compare the long-term outcome of conjunctival autograft (CAU and mitomycin C (MMC in double-head pterygium surgery. Methods. This is a follow-up study of a comparative interventional trial. Thirty-nine eyes of the 36 patients with double-head pterygium excision in the original study 12 years ago were recruited for clinical assessment. Seven out of the 36 patients were lost. In the original study, each eye with double-head pterygium was randomized to have pterygium excision with CAU on one “head” (temporal or nasal and MMC on the other “head.” All patients were invited for clinical assessment for conjunctival bed status and the presence of pterygium recurrence in the current study. Results. There was no significant difference between the size, morphology, and type of pterygium among the two treatment groups. The recurrence rate of CAU group and MMC group 12 years after excision was 6.3% and 28.1%, respectively (P=0.020. Among eyes without recurrence, the conjunctival bed was graded higher in the MMC group than the CAU group (P=0.024. Conclusion. The use of conjunctival autograft has a significantly lower long-term recurrence rate than mitomycin C in double-head pterygium surgery.

  4. 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.

  5. 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.

  6. 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.

  7. 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.

  8. 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.

  9. 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.

  10. 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.

  11. [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.

  12. Evaluation for safety of cultured corneal fibroblasts with cotreatment of alcohol and mitomycin C.

    Science.gov (United States)

    Kim, Tae-im; Tchah, Hungwon; Cho, Eun Hee; Kook, Michael S

    2004-01-01

    To investigate the effects of alcohol and mitomycin C (MMC) on cultured corneal fibroblast of the rabbit to determine the safety of this compound for clinical use. Corneal fibroblasts of New Zealand rabbits were cultured. Various concentrations (0%, 10%, 20%, 30%, 40%, and 60%) of ethanol were applied for 10, 20, 30, and 40 seconds to estimate dose- and time-dependent responses of cultured corneal fibroblasts. Cell viability was assessed using the MTT assay. Treated cells were additionally stained with Hoechst and annexin V for the identification of apoptosis. To investigate the coeffects of ethanol and MMC, dose and time dependency were evaluated after treatment with various concentrations of ethanol and MMC at different exposure times, and cell viability was established. To determine the latent effects of ethanol and MMC, cultured corneal fibroblasts were cotreated with various concentrations of ethanol and 0.02% MMC for various periods and washed out, and then one group was incubated for 24 hours and another group was not incubated. Cell viability was estimated, and Hoechst and annexin V staining were performed before and after incubation. To establish the pathway of cell death, caspase-3 activities were measured in cultured corneal fibroblasts treated with ethanol or MMC. Cell viability after ethanol treatment was dose and time dependent. After application of ethanol for 10 seconds, cell viability was significantly reduced with 20% ethanol (P = 0.001). At 20, 30, and 40 seconds of treatment with 10% ethanol, cell viability was significantly reduced (P corneal fibroblasts cotreated with 10% ethanol and 0.02% MMC were stained with Hoechst and annexin V. Results were similar to data obtained with ethanol-treated cells. However, after application of 20% alcohol and MMC, a significant number of cells were not viable and were detached from the well walls. Caspase-3 activity significantly increased after treatment with 30% ethanol only and 30% ethanol in conjunction

  13. Enhanced healing of mitomycin C-treated healing-impaired wounds in rats with PRP-containing fragmin/protamine microparticles (PRP&F/P MPs).

    Science.gov (United States)

    Takikawa, Megumi; Ishihara, Masayuki; Takabayashi, Yuki; Sumi, Yuki; Takikawa, Makoto; Yoshida, Ryuichi; Nakamura, Shingo; Hattori, Hidemi; Yanagibayashi, Satoshi; Yamamoto, Naoto; Kiyosawa, Tomoharu

    2015-04-13

    The purpose of this study was to evaluate the accelerating effects of platelet-rich plasma-containing (PRP&) fragmin/protamine microparticles (F/P MPs) for repairing mitomycin C-treated healing-impaired wounds. Staining with terminal deoxynucleotidyl transferase-mediated dUTP nick-end labelling (TUNEL-staining) showed that apoptosis of dermal fibroblast cells (DFCs) and epidermal keratinocyte cells (EKCs) were significantly induced in the skin of the mitomycin C-treated rats. Full-thickness skin defects were made on the back of rats and mitomycin C was applied on the wounds to prepare a healing-impaired wound. After washing out the mitomycin C, saline (control), F/P MPs alone, PRP alone, and PRP&F/P MPs were injected around the wounds. The rats were later euthanised and histological sections of the wounds were then prepared at indicated time periods after the treatment. These results indicated the numbers of large, medium, and small capillary lumens 7 days after injection of PRP&F/P MPs were significantly higher than those after injection of PRP or F/P MPs alone. Furthermore, epithelium and granulation tissue formations were significantly stimulated in the healing-impaired wounds treated with PRP&F/P MPs 3, 7 and 14 days after injection of PRP&F/P MPs.

  14. Current treatment of nasal vestibular stenosis with CO2-laser surgery; prolonged vestibular stenting versus intraoperative mitomycin application. A case series of 3 patients

    NARCIS (Netherlands)

    Schijndel, O. van; Heerbeek, N. van; Ingels, K.J.A.O.

    2014-01-01

    These case studies describe three cases of unilateral nasal vestibular stenoses caused by chemical cauterization. Each case was treated with CO2-laser surgery together with intraoperative topic application of mitomycin or prolonged vestibular stenting for prevention of restenosis. Two patients recei

  15. 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.

  16. 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.

  17. 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.

  18. 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.

  19. 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.

  20. 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...

  1. 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.

  2. 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.

  3. 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.

  4. 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.

  5. 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.

  6. 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.

  7. 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.

  8. Comparison of Subconjunctival Mitomycin C and 5-Fluorouracil Injection for Needle Revision of Early Failed Trabeculectomy Blebs

    Directory of Open Access Journals (Sweden)

    Wei Liu

    2016-01-01

    Full Text Available Background. To compare the efficacy of needle revision with 5-fluorouracil (5-FU and mitomycin C (MMC on dysfunctional filtration blebs shortly after trabeculectomy. Methods. It is a prospective randomized study comparing needle revision augmented with MMC or 5-FU for failed trabeculectomy blebs. Results. To date 71 patients (75 eyes have been enrolled, 40 eyes in the MMC group and 35 in the 5-FU group. 68 patients (72 eyes have completed 12-month follow-up, 38 eyes in the MMC group and 34 in the 5-FU group. The mean IOP before and that after needle revision in the MMC group were 26.5±4.3 mmHg and 11.3±3.4 mmHg, respectively (P0.05. Conclusions. Needle revision and subconjunctival MMC injection were more effective than needling and subconjunctival 5-FU injection for early dysfunctional filtration blebs after trabeculectomies.

  9. Cytostatic action of aspirin and its effect on mitomycin C activity. A study in vitro under irradiation

    Energy Technology Data Exchange (ETDEWEB)

    Kammerer, Cornelia; Getoff, Nikola E-mail: nikola.getoff@univie.ac.at

    2001-04-01

    Experiments in vitro using E. coli bacteria (AB 1157) proved that aspirin possesses a cytostatic ability under various experimental condition (pH=7.4) in airfree, aerated as well as in media containing N{sub 2}O (converting e{sub aq}{sup -} into OH- radicals). In the last case the highest effect of aspirin was observed. The combination of aspirin with the well-known cytostaticum, mitomycin C (MMC) leads in airfree as well as in aerated media to a significant decrease of the MMC activity. However, the mixture of aspirin and MMC in the presence of N{sub 2}O causes a synergistic effect, resulting in an enhancement of the MMC activity by a factor of 1.5. Probable reaction steps are presented and discussed. Using the pulse radiolysis method the rate constants for the reactions of e{sub aq}{sup -}, H and OH- species with aspirin were also determined.

  10. RASSF1A expression inhibits cell growth and enhances cell chemosensitivity to mitomycin in BEL-7402 hepatocellular carcinoma cells

    Institute of Scientific and Technical Information of China (English)

    GUAN Hong-geng; XUE Wan-jiang; QIAN Hai-xin; ZHOU Xiao-jun; QIN Lei; LAN Jing

    2009-01-01

    Background The antitumor role of Ras association domain family 1A (RASSFIA) gene and its potential molecular mechanisms are not well understood. The objective of this study was to observe the antitumor ability of RASSFIA in hepatoceliular carcinoma, and study the mechanisms of cell apoptosis induced by RASSFIA.Methods After stably transfecting a RASSF1A (wild-type or mutant) expression vector into the BEL-7402 hepatocellular carcinoma cell line, RT-PCR and Westem blotting was used to detect the RASSF1A expression levels in recombinant cells. The effects of wild-type RASSF1A on cell growth were observed in vitro by analyzing cell proliferation rate, cell colony formation, and in vivo by analyzing tumorigenesis in nude mice. In addition, the effect of RASSF1A gene expression on the chemosensitivity of human hepatocellular carcinoma cells to antitumor drugs was examined by inhibition of cell proliferation and the percentage of apoptotic cells.Results Wild-type RASSF1A, not the mutant, suppressed cell growth in vitro and in vivo. Re-expression of wild-type RASSF1A could enhance the inhibition of cell proliferation and the percentage of apoptotic cells following cell treatment with mitomycin, but had no significant effect when combined with adriamycin, etoposide, 5-fluorouracil and cisplatJn treatment.Conclusion Wild-type RASSF1A inhibits cell growth and enhances cell chemosensitivity to mitomycin in hepatocellular carcinoma, suggesting that RASSF1A may serve as a new target for gene therapy in hepatocellular carcinoma patients.

  11. Incorporation and release of chemically intact mitomycin C from albumin microspheres: a high performance liquid chromatography evaluation.

    Science.gov (United States)

    Allan, L; Cummings, J; Willmott, N; Whateley, T L; Smyth, J F

    1993-01-01

    Preparation of mitomycin C-loaded human serum albumin (HSA) microspheres using a new technique that avoids the use of heat denaturation, which is known chemically to degrade incorporated drug, is described. This method is based on cross-linking of protein by glutaraldehyde (2.2%) during emulsification (W/O) at room temperature. The resultant particles have a mean (s.d.) diameter of 16.9 (0.34) microns (50% weight average), contain mean (s.d.) 1.15 (0.05%) mitomycin C (MMC) (w/w, n = 17) and maintain sustained release of drug over 20 h. High performance liquid chromatography (HPLC) with diode array detection was used to study the chemical integrity of the drug. Two classes of decomposition products were evaluated: chemical degradation products and drug/nucleophile covalent adducts. The HPLC separation was validated by a number of standards of proposed degradation products. To examine incorporated drug, a complete microsphere system was solubilized with 0.4% trypsin for 24 h, while to examine released drug, microspheres were immobilized on a flow-through glass wool column and fractions were collected. No evidence of significant chemical degradation or covalent coupling to protein was detected in microsphere digests. Two candidate decomposition products, representing approximately 10% of drug released from microspheres (assuming similar molar extinction coefficients to MMC), were identified in column fractions. One of these products appeared to be a covalent adduct, the other possibly an isomeric form of intact MMC. Thus, MMC is predominantly incorporated into and released (90%) chemically intact from HSA microspheres prepared by the technique described.

  12. 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

  13. Synthesis of mPEG-Mitomycin C prodrug%聚乙二醇单甲醚偶联的丝裂霉素C前药的合成

    Institute of Scientific and Technical Information of China (English)

    陈卓; 石蕊; 谭李玉; 李梦琦

    2015-01-01

    In order to minimize the absorption into eyeball trough cornea in the application of Mitomycin C in ocular surface diseases. The PEG derivative macromolecule prodrug mPEG-MMC was synthesized by three-step reaction,based on polyethylene glycol 2000 monomethyl ether and Mitomycin C as substrates. Structure of the prodrug was characterized by UV method.%为了减少丝裂霉素 C 在眼表疾病应用时经角膜吸收导致的眼内副作用,以聚乙二醇2000单甲醚及丝裂霉素 C 为底物,经三步反应,制备了丝裂霉素 C 的聚乙二醇单甲醚衍生物高分子前药,并通过紫外法对其结构进行了表征。

  14. Structural determination of the conjugate of human serum albumin with a mitomycin C derivative, KW-2149, by matrix-assisted laser desorption/ionization mass spectrometry.

    Science.gov (United States)

    Yasuzawa, T; Tomer, K B

    1997-01-01

    A new mitomycin C derivative, KW-2149, is known to form a covalent conjugate with human serum albumin (HSA). This conjugate exhibits 1/20 of the anticellular activity of unconjugated KW-2149. Structural studies of this conjugate were carried out using a combination of enzymatic digestion, high-performance liquid chromatography (HPLC), and matrix-assisted laser desorption/ionization (MALDI) mass spectrometry. The tryptic peptide T5 (residues 21-41) was the only peptide found to be modified by KW-2149 moieties, the [(gamma-L-glutamylamino)ethyl]thio group or the (2-aminoethyl)thio group, through a disulfide bond. Although the latter peptide lost its mitomycin C moiety in the course of tryptic digestion, these data strongly suggest that KW-2149 was bound to Cys-34, the only free cysteine on HSA.

  15. 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.

  16. [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.

  17. 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.

  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. 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).

  20. 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).

  1. 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...

  2. Characterization of pegylated liposomal mitomycin C lipid-based prodrug (Promitil®) by high sensitivity differential scanning calorimetry and cryogenic transmission electron microscopy.

    Science.gov (United States)

    Wei, Xiaohui; Patil, Yogita; Ohana, Patricia; Amitay, Yasmine; Shmeeda, Hilary; Gabizon, Alberto; Barenholz, Yechezkel

    2017-01-03

    The effect of a lipidated prodrug of mitomycin C (MLP) on the membrane of a pegylated liposome formulation (PL-MLP), also known as Promitil®, was characterized through high-sensitivity differential scanning calorimetry (DSC), and cryo-TEM. The thermodynamic analysis demonstrated that MLP led to the formation of heterogeneous domains in the membrane plane of PL-MLP. MLP concentrated in prodrug-rich domains, arranged in high-ordered crystal-like structures, as suggested by the sharp and high enthalpy endotherm in the 1st heating scanning. After thiolytic cleavage of mitomycin C from MLP by dithiotreitol (DTT) treatment, the crystal-like prodrug domain disappears and a homogeneous membrane with stronger lipid interactions and higher phase transition temperature compared with the blank (MLP-free) liposomes is observed by DSC. In parallel, the rod-like discoid liposomes and the "kissing liposomes" seen by cryo-TEM in the PL-MLP formulation disappear, and liposome mean size and polydispersity increase after DTT treatment. Both MLP and the residual post-cleavage lipophilic moiety of the prodrug increased rigidity of the liposome membrane as indicated by DSC. These results confirm that MLP is inserted in the PL-MLP liposome membrane via its lipophilic anchor, and its mitomycin C moiety located mainly at the region of the phospholipid glycerol backbone and polar head-group. We hypothesize that Π-Π stacking between the planar aromatic rings of the mitomycin C moieties leads to the formation of prodrug-rich domains with highly ordered structure on the PL-MLP liposome membrane. This thermodynamically stable conformation may explain the high stability of the PL-MLP formulation. These results also provide us with an interesting example of the application of high sensitivity DSC in understanding the composition-structure-behavior dynamics of liposomal nanocarriers having a lipid-based drug as pharmaceutical ingredient.

  3. DdrA, DdrD, and PprA: components of UV and mitomycin C resistance in Deinococcus radiodurans R1.

    Directory of Open Access Journals (Sweden)

    Kathiresan Selvam

    Full Text Available Mutants created by deleting the ddrA, ddrB, ddrC, ddrD, and pprA loci of Deinococcus radiodurans R1alone and in all possible combinations of pairs revealed that the encoded gene products contribute to this species' resistance to UV light and/or mitomycin C. Deleting pprA from an otherwise wild type cell sensitizes the resulting strain to UV irradiation, reducing viability by as much as eight fold relative to R1. If this deletion is introduced into a ΔddrA or ΔddrD background, the resulting strains become profoundly sensitive to the lethal effects of UV light. At a fluence of 1000 Jm⁻², the ΔddrA ΔpprA and ΔddrD ΔpprA strains are 100- and 1000-fold more sensitive to UV relative to the strain that has only lost pprA. Deletion of ddrA results in a 100 fold increase in strain sensitivity to mitomycin C, but in backgrounds that combine a deletion of ddrA with deletions of either ddrC or ddrD, mitomycin resistance is restored to wild type levels. Inactivation of ddrB also increases D. radiodurans sensitivity to mitomycin, but unlike the ddrA mutant deleting ddrC or ddrD from a ΔddrB background further increases that sensitivity. Despite the effect that loss of these gene products has on DNA damage resistance, none appear to directly affect either excision repair or homologous recombination suggesting that they participate in novel processes that facilitate tolerance to UV light and interstrand crosslinks in this species.

  4. 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.

  5. 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.

  6. 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.

  7. 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).

  8. 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.

  9. In vitro and in vivo antimutagenic effects of DIG, a herbal preparation of Berberis vulgaris, Taraxacum officinale and Arctium lappa, against mitomycin C.

    Science.gov (United States)

    Di Giorgio, C; Boyer, L; De Meo, M; Laurant, C; Elias, R; Ollivier, E

    2015-07-01

    DIG, a liquid herbal preparation made from a mixture of diluted mother tinctures of Berberis vulgaris, Taraxacum officinale and Arctium lappa, was assessed for its antimutagenic properties against mitomycin C. The micronucleus assay on Chinese hamster ovary (CHO)-K1 cells was used to evaluate the in vitro anticlastogenic activity of DIG compared to those of separately diluted mother tinctures. The micronucleus assay was performed on mouse erythrocytes and the comet assay was performed on mouse liver, kidney, lung, brain and testicles to assess the protective effects of DIG (0.2 and 2 % at libitum) against an intraperitoneal injection of mitomycin C (1 mg Kg(-1)) in mice. DIG exerted a powerful anticlastogenic activity, under both pretreatment and simultaneous treatment conditions as assessed by the micronucleus assay in CHO-K1 cells. Its protective activity was greater than that observed for each mother tincture. DIG reduced micronuclei levels in mouse erythrocytes and suppressed >80 % of DNA strand breaks in the liver, kidney, lung, brain and testicles of mice exposed to mitomycin C.

  10. Rapamycin-enhanced mitomycin C-induced apoptotic death is mediated through the S6K1-Bad-Bak pathway in peritoneal carcinomatosis.

    Science.gov (United States)

    Song, X; Dilly, A-K; Kim, S-Y; Choudry, H A; Lee, Y J

    2014-06-05

    Peritoneal carcinomatosis (PC) is the most common secondary cancerous disease, and more effective novel regimens are needed. In this study, we identified a novel combination treatment for PC, chemotherapeutic agent mitomycin C in combination with mTOR (mammalian target of rapamycin) inhibitor rapamycin. We observed that the combination of mitomycin C and rapamycin induced synergistic cytotoxicity and apoptosis, which was mediated through an increase in caspase activation. The combination of mitomycin C and rapamycin inactivated p70 S6 ribosomal kinase (S6K1) and dephosphorylated Bad, leading to dissociation of Bcl-xL from Bak, which resulted in Bak oligomerization, mitochondria dysfunction and cytochrome c release. PF-4708671, a S6K1-specific inhibitor, enhanced the combination treatment-induced apoptosis, whereas S6K1 E389 DeltaCT-HA (S6K1 active form) dramatically decreased the induction of apoptosis. In addition, the combination treatment significantly inhibited LS174T intraperitoneal tumor growth in vivo. This study provides a preclinical rationale for apoptosis induction linked with the mTOR pathway through a combination of chemotherapeutic agents and mTOR inhibitor, and will support this combinatorial strategy to PC patients.

  11. Mitomycin C in pterygium surgery clinical observation application%丝裂霉素C在翼状胬肉手术中的疗效观察

    Institute of Scientific and Technical Information of China (English)

    唐雨生; 田静; 杨文红

    2013-01-01

      目的观察翼状胬肉手术中联合应用丝裂霉素C降低术后复发率的疗效。方法39例(47眼)翼状胬肉患者在手术显微镜下单纯切除,术区局部用0.02%丝裂霉素C,术后随访观察3个月~12个月。结果45眼达到治愈标准,2眼复发。结论翼状胬肉手术切除联合应用丝裂霉素C,术后复发率低,是一种理想的治疗方法。%Objective To observe the effect of pterygium surgery combined application mitomycin C reduce the recurrence rate of the treatment effect. Methods 39 cases (47 eyes) of pterygium resection under operating microscope simple, operation area local 0.02% mitomycin C. Postoperative follow-up of 3-12 months. Results 45 eyes to heal standard, 2 eyes recurrence. Conclusion pterygium resection combined application mitomycin C, the recurrence rate is low, which means it is a kind of ideal operation method.

  12. 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.

  13. 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

  14. 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.

  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. Observation of the dosage of mitomycin in trabeculectomy%丝裂霉素在小梁切除术中的用量观察

    Institute of Scientific and Technical Information of China (English)

    李玉茹; 刘晓瑞; 林娜

    2016-01-01

    Objective:To analyze the effect of the dosage of mitomycin on postoperative intraocular pressure control in trabeculectomy.Methods:28 patients with glaucoma(50 eyes) were given standard trabeculectomy.They were randomly divided into two groups with intraoperative application of mitomycin.15 cases(25 eyes) in the observation group were given 10 mm×8 mm size piece of cotton(containing 60 μ g mitomycin) placed under the scleral flap and between the surrounding scleral and conjunctival.13 cases(25 eyes) in the control group were given mitomycin cotton under scleral flap after standard trabeculectomy. Followed up for 6 to 24 months,the postoperative filtering bleb and intraocular pressure were observed in two groups.Results:The intraocular pressures of 2 eyes were more than 21 mmHg in the observation group;the intraocular pressures of 6 eyes were more than 21 mmHg in the control group.The observation group was significantly less than the control group(P<0.05).Conclusion:Moderate dosage of mitomycin can effectively control the success rate of trabeculectomy.%目的:分析丝裂霉素在小梁切除术中的用量对术后眼压控制的作用。方法:分析青光眼患者28例(50眼)行标准小梁切除术,术中应用丝裂霉素随机分成两组,观察组15例(25眼),术中用10 mm×8 mm 大小棉片(含丝裂霉素60μg)放于巩膜瓣下及周围的巩膜与结膜之间,对照组13例(25眼)行标准小梁切除术后常规用丝裂霉素棉片放于巩膜瓣下。随访6~24个月,观察两组术后滤过泡及眼压情况。结果:观察组2眼眼压>21 mmHg,对照组6眼>21 mmHg,观察组明显少于对照组(P<0.05)。结论:丝裂霉素用量适中可有效控制小梁切除术的成功率。

  17. 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...

  18. [Vincristine, adriamycin, mitomycin-C and UFT (VAM-UFT) therapy in progressive or recurrent breast cancer].

    Science.gov (United States)

    Yasutake, K; Imamura, Y; Yoshimura, Y; Oya, M; Matsushita, K; Hozumi, T; Katou, J; Okutani, T; Irie, K

    1989-07-01

    Since June 1984, 23 cases of progressive or recurrent breast cancers were treated with combination chemotherapy of VAM-UFT consisting of vincristine, adriamycin, mitomycin C and UFT. Clinical effects of VAM-UFT therapy were 3 CR, 12 PR, and the response rate was 65.2%. Its effective interval was 3 months. But the patients treated with over 4 cycles of VAM-UFT therapy showed an 85% response rate, with a 5-month effective interval. In each patient's background, a shorter disease free interval tended to be more highly effective, but other factors were not significant. Scirrhous carcinoma of pathology evidenced slightly high response rate. Compared with the survival time of patients treated with under 3 cycles and over 4 cycles of this therapy, the latter was significantly longer. Toxicity involved leukocytopenia (74%), thrombocytopenia (22%), anemia (30%), alopecia (91%), nausea and vomiting (87%) and stomatitis (35%), but cases in which the treatment was stopped were not observed. Therefore VAM-UFT therapy had a highly therapeutic effect, reflected in an 85% response rate, for progressive or recurrent breast cancers.

  19. Analysis of caspase-3 in ASTC-a-1 cells treated with mitomycin C using acceptor photobleaching techniques

    Science.gov (United States)

    Wang, Huiying; Chen, Tongsheng; Sun, Lei

    2008-02-01

    Caspase-3 is a key activated death protease, which catalyzes the specific cleavage of many cellular proteins and induces DNA cleavage eventually. In this report, cells were treated with mitomycin C (MMC) at different concentration and its activity was detected by cell counting kit (CCK-8). Based on results of CCK-8, cells were treated with 10μg/mL MMC and Hoechst 33258 has been used to observe cell apoptosis. Fluorescence resonance energy transfer (FRET) and confocal microscopy have been used to the effect of MMC on the caspase3 activation in living cells. Human lung adenocarcinoma cells (ASTC-a-1) was transfected with plasmid SCAT3 (pSCAT3)/CKAR FRET receptor. Acceptor photobleaching techniques of FRET plasmid has been used to destruct fluorophore of cells stably expressing SCAT3 reporter on a fluorescence confocal microscope. The activity of caspase3 can be analyzed by FRET dynamics of SCAT3 in living cells. Our results show that MM C can induce ASTC-a-1 cell apoptosis through activation of caspase3.

  20. Effect of recombinant human erythropoietin on mitomycin C-induced oxidative stress and genotoxicity in rat kidney and heart tissues.

    Science.gov (United States)

    Rjiba-Touati, K; Ayed-Boussema, I; Guedri, Y; Achour, A; Bacha, H; Abid-Essefi, S

    2016-01-01

    Mitomycin C (MMC) is an antineoplastic agent used for the treatment of several human malignancies. Nevertheless, the prolonged use of the drug may result in a serious heart and kidney injuries. Recombinant human erythropoietin (rhEPO) has recently been shown to exert an important cytoprotective effect in experimental brain injury and ischemic acute renal failure. The aim of the present work is to investigate the cardioprotective and renoprotective effects of rhEPO against MMC-induced oxidative damage and genotoxicity. Our results showed that MMC induced oxidative stress and DNA damage. rhEPO administration in any treatment conditions decreased oxidative damage induced by MMC. It reduced malondialdehyde and protein carbonyl levels. rhEPO ameliorated reduced glutathione plus oxidized glutathione modulation and the increased catalase activity after MMC treatment. Furthermore, rhEPO restored DNA damage caused by MMC. We concluded that rhEPO administration especially in pretreatment condition protected rats against MMC-induced heart and renal oxidative stress and genotoxicity.

  1. A tubular gelatin scaffold capable of the time-dependent controlled release of epidermal growth factor and mitomycin C.

    Science.gov (United States)

    Zhu, Jixiang; Yang, Fanwen; He, Fupo; Tian, Xiumei; Tang, Shuo; Chen, Xiaoming

    2015-11-01

    A tubular gelatin scaffold for the time-dependent controlled release of epidermal growth factor (EGF) and mitomycin C (MMC) was fabricated. EGF was incorporated using silk fibroin carriers, and MMC was planted using polylactide (PLA) microspheres. The relationship between scaffold properties and crosslinking degrees was evaluated. As the crosslinking degree was increased from 23.7% to 65.3%, the mechanical properties of the scaffold obviously improved, and the compressive modulus increased to approximately 65kPa. The mass degradation of the scaffold was also controlled from 9 days to approximately 1 month. In vitro release tests indicated that the scaffold mainly released EGF in the early period and MMC in the later period. Urethral epithelial cells (UECs) and urethral scar derived fibroblast cells (UFCs) were coseeded in the scaffold at a ratio of 1:1. After 9 days of coculture, immunostaining results displayed that the proportion of UECs continuously increased to approximately 71%. These changes in cell proportion were confirmed by the results of Western blot analysis. Therefore, the scaffold promoted the growth but inhibited the regeneration of UFCs. This scaffold for time-dependent controlled release of multiple biofactors may be potentially useful in urethral reconstruction and other tissue engineering studies.

  2. Mitomycin C modulates the circadian oscillation of clock gene period 2 expression through attenuating the glucocorticoid signaling in mouse fibroblasts.

    Science.gov (United States)

    Kusunose, Naoki; Matsunaga, Naoya; Kimoto, Kenichi; Akamine, Takahiro; Hamamura, Kengo; Koyanagi, Satoru; Ohdo, Shigehiro; Kubota, Toshiaki

    2015-11-06

    Clock gene regulates the circadian rhythm of various physiological functions. The expression of clock gene has been shown to be attenuated by certain drugs, resulting in a rhythm disorder. Mitomycin C (MMC) is often used in combination with ophthalmic surgery, especially in trabeculectomy, a glaucoma surgical procedure. The purpose of this study was to investigate the influence of MMC on clock gene expression in fibroblasts, the target cells of MMC. Following MMC treatment, Bmal1 mRNA levels was significantly decreased, whereas Dbp, Per1, and Rev-erbα mRNA levels were significantly increased in the mouse fibroblast cell line NIH3T3 cells. Microarray analysis was performed to explore of the gene(s) responsible for MMC-induced alteration of clock gene expression, and identified Nr3c1 gene encoding glucocorticoid receptor (GR) as a candidate. MMC suppressed the induction of Per1 mRNA by dexamethasone (DEX), ligand of GR, in NIH3T3 cells. MMC also modulated the DEX-driven circadian oscillations of Per2::Luciferase bioluminescence in mouse-derived ocular fibroblasts. Our results demonstrate a previously unknown effect of MMC in GR signaling and the circadian clock system. The present findings suggest that MMC combined with trabeculectomy could increase the risk for a local circadian rhythm-disorder at the ocular surface.

  3. Orthogonally functionalized nanoscale micelles for active targeted codelivery of methotrexate and mitomycin C with synergistic anticancer effect.

    Science.gov (United States)

    Li, Yang; Lin, Jinyan; Wu, Hongjie; Chang, Ying; Yuan, Conghui; Liu, Cheng; Wang, Shuang; Hou, Zhenqing; Dai, Lizong

    2015-03-02

    The design of nanoscale drug delivery systems for the targeted codelivery of multiple therapeutic drugs still remains a formidable challenge (ACS Nano, 2013, 7, 9558-9570; ACS Nano, 2013, 7, 9518-9525). In this article, both mitomycin C (MMC) and methotrexate (MTX) loaded DSPE-PEG micelles (MTX-M-MMC) were prepared by self-assembly using the dialysis technique, in which MMC-soybean phosphatidylcholine complex (drug-phospholipid complex) was encapsulated within MTX-functionalized DSPE-PEG micelles. MTX-M-MMC could coordinate an early phase active targeting effect with a late-phase synergistic anticancer effect and enable a multiple-responsive controlled release of both drugs (MMC was released in a pH-dependent pattern, while MTX was released in a protease-dependent pattern). Furthermore, MTX-M-MMC could codeliver both drugs to significantly enhance the cellular uptake, intracellular delivery, cytotoxicity, and apoptosis in vitro and improve the tumor accumulation and penetration and anticancer effect in vivo compared with either both free drugs treatment or individual free drug treatment. To our knowledge, this work provided the first example of the systemically administrated, orthogonally functionalized, and self-assisted nanoscale micelles for targeted combination cancer chemotherapy. The highly convergent therapeutic strategy opened the door to more simplified, efficient, and flexible nanoscale drug delivery systems.

  4. Pharmacokinetics of intraarterial mitomycin C in hypoxic hepatic infusion with embolization in the treatment of liver metastases.

    Science.gov (United States)

    Cerretani, Daniela; Roviello, Franco; Pieraccini, Massimo; Civeli, Letizia; Correale, Pierpaolo; Francini, Guido; Marrelli, Daniele; De Manzoni, Giovanni; Pinto, Enrico; Giorgi, Giorgio

    2002-07-01

    1. The pharmacokinetics of mitomycin C (MMC) was evaluated during hypoxic hepatic infusion (HHMI) with arterial embolization for the treatment of unresectable liver metastases. 2. Ten patients with hepatic metastases from colorectal cancer were considered. Antiblastic infusion with MMC (20 mg/m2 at 30 ml/min) was initiated after 10 min of hepatic arterial occlusion. Peripheral venous blood samples were collected at different time intervals. MMC was assayed by high-pressure liquid chromatography (HPLC), and pharmacokinetic parameters were determined using an open, two-compartment model and linear kinetics. 3. Cmax of MMC during HHMI was 708 +/- 336.6 ng/ml, and tmax was 9.3 +/- 1.1 min. The plasma concentration-time curve showed a t1/2 alpha ranging from 1.5 to 9 min, followed by a t1/2 beta ranging from 31 to 93 min. The Cltot was 35.5 l/h/m2 with an area under the plasma concentration-time curve (AUC) ranging from 251 to 850 micrograms h/l. The same AUC parameter standardized for the amount of MMC was 15.5 mg-1. The HHMI model that we used revealed a significant increase in Cltot and a reduction in AUC when compared to the locoregional intraarterial and peripheral intravenous models (p < .001). 4. The reduction in AUC following HHMI explains the limited systemic toxicity in treated patients, with a greater total tumor exposure to the drug and improved drug activation.

  5. Simultaneous determination of the peptide-mitomycin KW-2149 and its metabolites in plasma by high-performance liquid chromatography.

    Science.gov (United States)

    Zhang, Z D; Guetens, G; De Boeck, G; Van Cauwenberghe, K; Maes, R A; Ardiet, C; van Oosterom, A T; Highley, M; de Bruijn, E A; Tjaden, U R

    2000-03-10

    A gradient high-performance liquid chromatographic (HPLC) method is described for the quantification of KW-2149 and its two major metabolites in plasma. The method involves a sample clean-up by solid-phase extraction on C18 columns, separation of the respective compounds by HPLC on a YMC ODS-AQ column (5-microm particle size, 150x6 mm I.D.), using a methanol-water gradient system as an eluent, and measurement by UV absorbance detection at 375 nm. The limits of quantitation were 10 ng/ml for KW-2149 and M-16, and 15 ng/ml for M-18. Recoveries from plasma were higher than 92% on C18 extraction columns. Intra-day precision, expressed as %C.V., was between 1.4 and 6.5%. Intra-day accuracy ranged from 94 to 107%. Precision and accuracy of variability of inter-assays increased somewhat; however, were still within acceptable ranges. The ability of the method to quantify KW-2149 and two major metabolites simultaneously, with precision, accuracy and sensitivity, make it useful in monitoring the fate of this new mitomycin in cancer patients.

  6. Use of high-performance liquid chromatography to detect hydroxyl and superoxide radicals generated from mitomycin C.

    Science.gov (United States)

    Pritsos, C A; Constantinides, P P; Tritton, T R; Heimbrook, D C; Sartorelli, A C

    1985-11-01

    Distinguishing between short-lived reactive oxygen species like hydroxyl and superoxide radicals is difficult; the most successful approaches employ electron spin resonance (ESR) spin-trapping techniques. Using the spin trap 5,5-dimethyl-l-pyrroline N-oxide (DMPO) to selectively trap various radicals in the presence and absence of ethanol, an HPLC system which is capable of separating the hydroxyl- and superoxide-generated DMPO adduct species has been developed. The radical-generated DMPO adducts were measured with an electrochemical detector attached to the HPLC system and confirmed by spin-trapping techniques. The HPLC separation was carried out on an ODS reverse-phase column with a pH 5.1 buffered 8.5% acetonitrile mobile phase. The advantage of the HPLC system described is that it permits the separation and detection of hydroxyl and superoxide radicals without requiring ESR instrumentation. The antineoplastic bioreductive alkylating agent mitomycin C, when activated by NADPH-cytochrome c reductase, was shown to generate both hydroxyl and superoxide radicals.

  7. Proteasomal inhibition sensitizes cervical cancer cells to mitomycin C-induced bystander effect: the role of tumor microenvironment.

    Science.gov (United States)

    Singh, S V; Ajay, A K; Mohammad, N; Malvi, P; Chaube, B; Meena, A S; Bhat, M K

    2015-10-22

    Inaccessibility of drugs to poorly vascularized strata of tumor is one of the limiting factors in cancer therapy. With the advent of bystander effect (BE), it is possible to perpetuate the cellular damage from drug-exposed cells to the unexposed ones. However, the role of infiltrating tumor-associated macrophages (TAMs), an integral part of the tumor microenvironment, in further intensifying BE remains obscure. In the present study, we evaluated the effect of mitomycin C (MMC), a chemotherapeutic drug, to induce BE in cervical carcinoma. By using cervical cancer cells and differentiated macrophages, we demonstrate that MMC induces the expression of FasL via upregulation of PPARγ in both cell types (effector cells) in vitro, but it failed to induce bystander killing in cervical cancer cells. This effect was primarily owing to the proteasomal degradation of death receptors in the cervical cancer cells. Pre-treatment of cervical cancer cells with MG132, a proteasomal inhibitor, facilitates MMC-mediated bystander killing in co-culture and condition medium transfer experiments. In NOD/SCID mice bearing xenografted HeLa tumors administered with the combination of MMC and MG132, tumor progression was significantly reduced in comparison with those treated with either agent alone. FasL expression was increased in TAMs, and the enhanced level of Fas was observed in these tumor sections, thereby causing increased apoptosis. These findings suggest that restoration of death receptor-mediated apoptotic pathway in tumor cells with concomitant activation of TAMs could effectively restrict tumor growth.

  8. Effect and Mechanism of Mitomycin C Combined with Recombinant Adeno-Associated Virus Type II against Glioma

    Directory of Open Access Journals (Sweden)

    Hong Ma

    2013-12-01

    Full Text Available The effect of chemotherapy drug Mitomycin C (MMC in combination with recombinant adeno-associated virus II (rAAV2 in cancer therapy was investigated, and the mechanism of MMC affecting rAAV2’s bioactivity was also studied. The combination effect was evaluated by the level of GFP and TNF expression in a human glioma cell line, and the mechanism of MMC effects on rAAV mediated gene expression was investigated by AAV transduction related signal molecules. C57 and BALB/c nude mice were injected with rAAV-EGFP or rAAV-TNF alone, or mixed with MMC, to evaluate the effect of MMC on AAV-mediated gene expression and tumor suppression. MMC was shown to improve the infection activity of rAAV2 both in vitro and in vivo. Enhancement was found to be independent of initial rAAV2 receptor binding stage or subsequent second-strand synthesis of target DNA, but was related to cell cycle retardation followed by blocked genome degradation. In vivo injection of MMC combined with rAAV2 into the tumors of the animals resulted in significant suppression of tumor growth. It was thus demonstrated for the first time that MMC could enhance the expression level of the target gene mediated by rAAV2. The combination of rAAV2 and MMC may be a promising strategy in cancer therapy.

  9. Effect of mitomycin C on the activation of adenylate cyclase in rat ascites hepatoma AH130 cells.

    Science.gov (United States)

    Miyamoto, K; Matsunaga, T; Sanae, F; Koshiura, R

    1986-09-01

    Isoproterenol (IPN)-stimulated activity of adenylate cyclase was enhanced in a dose-dependent manner by exposure of AH130 cells to mitomycin C (MMC). The enhancement was also observed in prostaglandin E1-, guanine nucleotide analog-, NaF-, cholera toxin- and forskolin-stimulated activities of the enzyme but not in manganese-stimulated activity. In addition, even when the cells pretreated with islet-activating protein were exposed to MMC, IPN-stimulated activity of adenylate cyclase was enhanced. Anaerobic exposure of AH130 cells to MMC somewhat inhibited IPN-stimulated activity of adenylate cyclase in contrast with aerobic exposure. Exposure of cells to adriamycin also caused enhancement of IPN-stimulated activity of adenylate cyclase but exposure to nitrogen mustard inhibited the enzyme stimulation by IPN. The enhancing effect of MMC was lost by the combined treatment with alpha-tocopherol. From these results, it was shown that MMC modulated the activity of adenylate cyclase, probably through alterations in membrane structure.

  10. 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...

  11. 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...

  12. 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...

  13. 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...

  14. 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.

  15. 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...

  16. 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.

  17. 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.

  18. 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 ...

  19. 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.

  20. 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.

  1. 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.

  2. 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.

  3. 丝裂霉素C在鼻腔泪囊吻合术中的应用%Application of mitomycin C in dacryocystorhinostomy

    Institute of Scientific and Technical Information of China (English)

    盛张兴; 邵利琴; 向远波

    2012-01-01

    To evaluate the application of mitomycin C in dacryocystorhinostomy.MethodsOne hundred andforty patients with chronic dacryocystitis were randomly assigned to endoscopic surgery and traditional surgical modality. Two groups were further divided into mitomycin C subgroup and control subgroup. The cure rates of subgroups were observed and compared.ResultsThe cure rates of control and mitomycin subgroups with traditional modality were 76.47% and 97.22% re-spectively; the cure rates of control and mitomycin subgroups with endoscopic surgery were 81.58% and 97.62% respectively. There were no statistical differences in cure rate between endoscopic and traditional groups; while there were significant differences in cure rate between control and mitomycin subgroups in both surgical modality groups.ConclusionNasal endoscopic dacryocystorhinostomy is safe and efficient for chronic dacryocystitis and the application of mitomycin C may further improve the surgical cure rate.%目的 探讨丝裂霉素C 在鼻腔泪囊吻合术中临床应用.方法 回顾分析140 例慢性泪囊炎患者,按治疗方法不同随机分为外路鼻腔泪囊吻合术组与鼻内镜下鼻腔泪囊吻合术组,两组按术中是否应用丝裂霉素棉片又分别分为对照组和治疗组.随访两组手术效果.结果 其中外路鼻腔泪囊吻合术对照组治愈率为76.47%;治疗组治愈率为97.22%.鼻内镜下鼻腔泪囊对照组治愈率为81.58%;治疗组治愈率为97.62%.两个不同手术方式组间手术治愈率无统计学差异性.两组内对照组与治疗组间手术治愈率均存在统计学上差异性.结论 鼻内镜下鼻腔泪囊吻合术治疗慢性泪囊炎是安全、有效的,且该术式与传统外路鼻腔泪囊吻合术相比具有较好的优势,应用丝裂霉素于慢性泪囊炎治疗是安全且有效的,能明显提高手术的成功率.

  4. [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.

  5. 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.

  6. 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.

  7. 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.

  8. 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.

  9. 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.

  10. 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.

  11. 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.

  12. 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

  13. 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.

  14. 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.

  15. [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.

  16. 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.

  17. 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.

  18. 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.

  19. 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.

  20. 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.

  1. Efficacy of pterygium excision combining with Mitomycin C%翼状胬肉切除联合丝裂霉素 C 疗效观察

    Institute of Scientific and Technical Information of China (English)

    张记梅

    2013-01-01

      目的探讨翼状胬肉切除联合应用丝裂霉素 C(MMC)治疗翼状胬肉的疗效.方法36例(40眼)原发性翼状胬肉患者在手术显微镜下分离球结膜与病变组织,切除胬肉组织,在结膜下放置0.2 mg/mL 的丝裂霉素 C 棉片,彻底冲洗,将球结膜固定到浅层巩膜上,角膜缘裸露3 mm×4 mm.结果术后随访6个月~24个月,术后2眼复发,复发率5%.结论翼状胬肉显微手术切除联合应用丝裂霉素 C,术后复发率低,是一种安全有效的方法.%Objective Explore the efficacy of pterygium using pterygium excision combined with mitomycin C (MMC).Methods 36 patients (40 eyes) were operated,separation bulbar conjunctiva and diseased tissue, excision of pterygium tissue under the operating microscope, 0.2 mg/mL mitomycin C cotton pad placed under the conjunctiva, rinse thoroughly, conjunctiva ball fixed to the superficial scleral limbus bare 3 mm×4 mm. Results The patients are followed up for 6 months to 24 months, two eyes recurrence after surgery, the recurrence rate is 5% . Conclusion Pterygium microsurgical resection of the joint application of mitomycin C, the recurrence rate is low, and it's a safe and effective method.

  2. 鸦胆子油乳联合丝裂霉素治疗恶性胸腔积液的研究%The application of Yadanzhi grease combined with mitomycin in the treatment of malignant pleural effusion

    Institute of Scientific and Technical Information of China (English)

    徐春华

    2011-01-01

    Objective To observe the curative effects on malignant pleural effusion treated with Yedanzhi (YDZ) grease and mitomycin(MMC). Methods Sixty-seven in patients suffering from malignant pleural effusion were divided into three groups randotnly:24 patients in the treatment group were treated with mitomycin 6 mg and YDZ 60 ml ,22 patients were treated with YDZ and 21 patients were treated with mitomycin. The doses were given one time every week, for 2 ~ 3 weeks. Results The total effective rates in the treatment group, YDZ group and mitomycin group were respectively 83.3% ,59. 1 % and 57. 1% respectively ( P < 0. 05 ). Conclusion The effect of using YDZ and mitomycin together in treatment of malignant pleural effusion is superior to using only YDZ or mitomycin.%目的 研究鸦胆子油乳联用丝裂霉素治疗恶性胸腔积液的疗效.方法 选样67例患有恶性胸腔积液的住院患者,分别胸腔内注射鸦胆子油乳、丝裂霉素与单用鸦胆子油乳、丝裂霉素,每周1次,连续注射2~3周.结果 鸦胆子油乳联用丝裂霉素组治疗有效率83.3% ,鸦胆子油乳组59.1% ,丝裂霉素组57.1%(P<0.05).结论 鸦胆子油乳联用丝裂霉素治疗恶性胸腔积液的疗效明显优于单用鸦胆子油乳、丝裂霉素.

  3. Persistent hypotony after primary trabeculectomy with mitomycin C Hipotonia persistente depois de trabeculectomia primária com mitomicina C

    Directory of Open Access Journals (Sweden)

    Viviane R.F. Guedes

    2000-06-01

    Full Text Available Purpose: To describe the clinical findings and treatment modalities of persistent hypotony following primary trabeculectomy with mitomycin C. Methods: We retrospectively analyzed 9 eyes with persistent hypotony, which was defined as intraocular pressure less than or equal to 5 mmHg for more than 2 months. Results: Mean hypotony duration was 7.4 months (standard deviation (SD ± 6.7 months, range 2 to 23 months. Associated findings included choroidal detachment (2 eyes and maculopathy (5 eyes. All patients who developed maculopathy were relatively young (mean age = 37 years old, SD ± 16, range 18 to 79 years. Treatments included bandaged contact lens, autologous blood injection, phacoemulsification, resuturing of the scleral flap, scleral patch graft, and Simmons' shell. After treatment, intraocular pressure (IOP raised in all patients (mean final IOP = 11.1 mmHg, SD ± 3.5. On the first day of hypotony, the mean IOP was 3 mmHg (SD ±1.7. At the last follow up, visual acuity (VA was unchanged in 3 eyes, worsened in 2 eyes (by 2 Snellen lines, and improved (by 1 to 4 Snellen lines in 4 eyes. Of those eyes whose VA improved, 3 had undergone phacoemulsification. Conclusion: Hypotony after trabeculectomy with mitomycin C can be reversed with possible improvement in vision.Objetivo: Descrever os achados clínicos e as modalidades de tratamento da hipotonia persistente após trabeculectomia primária com mitomicina C. Método: Foram retrospectivamente analisados 9 olhos com hipotonia persistente, a qual foi definida como pressão intra-ocular igual ou menor que 5 mmHg por mais que 2 meses. Resultado: Tempo médio de duração da hipotonia foi de 7.4 meses, desvio padrão ± 6.7 meses. Complicações associadas à hipotonia incluíram descolamento de coróide (2 olhos, maculopatia (5 olhos. Todos os pacientes que desen-volveram maculopatia eram relativamente novos (idade media de 37 anos, desvio padrão ±16. Tratamentos incluíram lente de contato

  4. Experimental research on the effect of mitomycin C fibrin gel on spinal peridural scar tissue in rats.

    Science.gov (United States)

    Liu, Wenping

    2014-09-01

    This paper aimed to study the best working concentration of mitomycin C (MMC) fibrin gel on spinal peridural scar tissue in rats and the sustained release function of peridural adhesion after laminectomy of rats. 96 SD rats were divided into four groups. They were conducted L1 laminectomy and sprayed FG-MMC. The concentration of MMC was detected and the best working concentration of MMC was selected. Then other 48 SD rats were divided into four groups to construct L1 vertebral plate excision model. Materials were drawn 4 weeks after the operation for Rydell grading. In addition, we observed HE staining and fibroblast proliferation and collagen distribution situation after Masson staining. And concentration of hydroxyproline was also detected. The best working concentration of MMC experiment showed that except experimental group C, the other groups all appeared drug release peak in the 4th week after the operation. MMC concentration of group C appeared drug release peak in the 5th week besides the 2nd week. Moreover, adhesion of endorhachis and peripheral tissue in group A was the most obvious while the group C was the weakest. Experiment on the slow-release effect of different adhesion materials on peridural adhesion showed that compared to the contrast group and group F, Rydell grading in group E and G was Level 0 and with low adhesion degree, little fibroblast and fibrocyte, low collagen content, regular collagen fibers arrangement and no inflammatory cells after HE staning and Masson staining. In addition, content of hydroxyproline(HOP) decreased significantly especially the group of FG-MMC mixture. It was concluded that MMC fibrin gel mixture had a good slow-release effect on adhesion of spinal peridural scar tissue in rats and the best working concentration was 0.5 mg FG-MMC/ml.

  5. Sustained Release of Mitomycin C from Its Conjugate with Single-Walled Carbon Nanotubes Associated by Pegylated Peptide.

    Science.gov (United States)

    Ohta, Takahisa; Hashida, Yasuhiko; Yamashita, Fumiyoshi; Hashida, Mitsuru

    2016-01-01

    A novel sustained release formulation of mitomycin C (MMC) was developed by employing single-walled carbon nanotubes (SWCNTs) wrapped by designed peptide with polyethylene glycol (PEG) modification (pegylation) as a nano-scale molecular platform. The amino groups of polycationic and amphiphilic H-(-Cys-Trp-Lys-Gly-)(-Lys-Trp-Lys-Gly-)6-OH [CWKG(KWKG)6] peptide associated with SWCNTs were modified using PEG with 12 units (PEG12) to improve the dispersion stability of the composite. Then thiol groups of peptide were conjugated with MMC using N-ε-maleimidocaproic acid (EMCA) as a linker via transformation of aziridine group of MMC. The obtained SWCNTs-CWKG(KWKG)6-(PEG)12-C6-MMC composites particularly that with 13.6% PEG modification extent of amino groups, showed good dispersion stability both in water and in a cell culture medium for 24 h. The release of MMC from SWCNTs-CWKG(KWKG)6-(PEG)12-C6-MMC was confirmed to follow first-order kinetics being accelerated by the pH increase in good agreement with the results observed for MMC-dextran conjugate with the same conjugation structure. The SWCNTs-CWKG(KWKG)6-(PEG)12 composite exhibited a considerably low cytotoxicity against cultured human lung adenocarcinoma epithelial cell line (A549). In contrast, SWCNTs-CWKG(KWKG)6-(PEG)12-C6-MMC demonstrated delayed but relatively corresponding antitumor activity with free MMC at the same concentration. The results suggested the potential role of SWCNTs-CWKG(KWKG)6-(PEG)12 as a carrier for a controlled release drug delivery system (DDS).

  6. LASEK for the correction of hyperopia with mitomycin C using SCHWIND AMARIS excimer laser: one-year follow-up

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    Khosrow Jadidi

    2015-11-01

    Full Text Available AIM: To evaluate the efficacy, safety and predictability of laser-assisted sub-epithelial keratectomy(LASEKfor the correction of hyperopia using the SCHWIND AMARIS platform.METHODS: This retrospective single-surgeon study includes 66 eyes of 33 patients with hyperopia who underwent LASEK with mitomycin C(MMC. The median age of patients was 35.42±1.12y(ranging 18 to 56y. In each patient LASEK was performed using SCHWIND AMARIS excimer laser. Postoperatively clinical outcomes were evaluated in terms of predictability, safety, efficacy, subjective and objective refractions, uncorrected visual acuity(UCVA, best spectacle-corrected visual acuity(BSCVAand adverse events. RESULTS: The mean baseline refraction was 3.2±1.6 diopters(D(ranging 0 to 7 D. The mean pre-operative and postoperative spherical equivalent(SEwere 2.34±1.76(ranging -1.25 to 7 Dand 0.30±0.84(ranging -0.2 to 0.8 Drespectively(P=0.001. The mean hyperopia was 0.63±0.84 D(ranging -1.75 to 2.76 D6 to 12mo postoperatively. Likewise, the mean astigmatism was 0.68±0.43 D(range 0 to 2 Dwith 51(77.3%and 15(22.7%eyes within ±1 and ±0.50 D respectively. The safety index and efficacy index were 1.08 and 1.6 respectively.CONCLUSION:LASEK using SCHWIND AMARIS with MMC yields good visual and refractive results for hyperopia. Moreover, there were no serious complications.

  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. Label-free structural characterization of mitomycin C-modulated wound healing after photorefractive keratectomy by the use of multiphoton microscopy

    Science.gov (United States)

    Lo, Wen; Wang, Tsung-Jen; Chen, Wei-Liang; Hsueh, Chiu-Mei; Chen, Shean-Jen; Chen, Yang-Fang; Chou, Hsiu-Chu; Lin, Pi-Jung; Hu, Fung-Rong; Dong, Chen-Yuan

    2010-05-01

    We applied multiphoton autofluorescence (MAF) and second-harmonic generation (SHG) microscopy to monitor corneal wound healing after photorefractive keratectomy (PRK). Our results show that keratocyte activation can be observed by an increase in its MAF, while SHG imaging of corneal stroma can show the depletion of Bowman's layer after PRK and the reticular collagen deposition in the wound healing stage. Furthermore, quantification of the keratocyte activation and collagen deposition in conjunction with immunohistochemistry and histological images demonstrate the effectiveness of mitomycin C (MMC) in suppressing myofibroblast proliferation and collagen regeneration in the post-PRK wound healing process.

  9. 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.

  10. 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.

  11. 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.

  12. 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.

  13. Transarterial chemoperfusion with gemcitabine and mitomycin C in pancreatic carcinoma: Results in locally recurrent tumors and advanced tumor stages; Transarterielle Chemoperfusion mit Gemcitabine und Mitomycin C bei Pankreaskarzinom: Ergebnisse bei Rezidivtumoren und fortgeschrittenen Tumorstadien

    Energy Technology Data Exchange (ETDEWEB)

    Vogl, T.J.; Zangos, S.; Heller, M.; Hammerstingl, R.M.; Bauer, R.W. [Inst. fuer Diagnostische und Interventionelle Radiologie, J. W. Goethe-Univ. Frankfurt (Germany); Boecher, E. [Klinik Paradise, Medizinische Klinik, Soest (Germany); Jacob, U. [Leonardisklinik, Onkologische Fachklinik, Bad Heilbrunn (Germany)

    2007-11-15

    Purpose: The purpose of this study was to evaluate local transarterial chemoperfusion (TACP) in locally recurrent pancreatic carcinoma and advanced tumor stages which did not respond to prior systemic chemotherapy. The tumor response, survival, and pain response were retrospectively analyzed. Materials and method: Forty outpatients (median age 62 years, range 36 - 79) were treated with a minimum of 3 (mean 6, range 3 - 12) applications per patient in four-week intervals. Twenty-eight patients were in advanced tumor stages, and 12 patients had locally recurrent tumors. Gemcitabine (1,000 mg/m{sup 2}) and mitomycin C (8.5 mg/m{sup 2}) were administered within 1 hour through a celiac trunk catheter. The tumor response (diameter, volume) was measured using MRI or CT and classified according to RECIST. The pain response was defined as a reduction of pain intensity of more than 50% on a visual analog scale, or a reduction of more than 50% in analgesics consumption, or a switch to a less potent analgesic agent. Results: The treatment was tolerated well by all patients. No clinically relevant problems or grade III or IV toxicity according to CTC (Common Toxicity Criteria) were observed. Tumor-related pain was relieved in 20/32 (62.5%) cases. Radiologically, 'complete response' was found in 3/40 (7.5%), 'partial response' in 9/40 (22.5%), 'stable disease' in 16/40 (40%), and 'progressive disease' in 12/40 (30%) of the patients. The median survival period since initial diagnosis and first TACP was 16.4 months and 8.1 months, respectively. Locally recurrent tumors showed better, but still not significant results regarding tumor response (41.7% vs. 25%) as well as survival (14.4 vs. 7 months) compared to advanced tumor stages. Responders (CR + PR) showed a significant survival advantage compared to patients with tumor progression (13.0 vs. 6.0 months; p = 0.013). (orig.)

  14. Mitomycin-treated undifferentiated embryonic stem cells as a safe and effective therapeutic strategy in a mouse model of Parkinson's disease.

    Directory of Open Access Journals (Sweden)

    Mariana eAcquarone

    2015-04-01

    Full Text Available Parkinson’s disease (PD is an incurable progressive neurodegenerative disorder. Clinical presentation of PD stems largely from the loss of dopaminergic neurons in the nigrostriatal dopaminergic pathway, motivating experimental strategies aimed at replacing dopaminergic innervation by cellular therapy. Transplantation of dopaminergic neurons derived from embryonic stem cells significantly improves motor functions in rodent and non-human primate models of PD. However, protocols to generate dopaminergic neurons from embryonic stem cells generally meet with low efficacy and high risk of teratoma development upon transplantation. To address these issues, we have pre-treated undifferentiated mouse embryonic stem cells (mESCs with the DNA alkylating agent mitomycin C (MMC before transplantation. MMC treatment of cultures prevented tumor formation in a 12-week follow-up after mESCs were injected in nude mice. In 6-OH-dopamine-lesioned mice, intrastriatal injection of MMC-treated mESCs markedly improved motor function without tumor formation for as long as 15 months. Furthermore, we show that halting mitotic activity of undifferentiated mESCs induces a four-fold increase in dopamine release following in vitro differentiation. Our findings indicate that treating mESCs with mitomycin C prior to intrastriatal transplant is an effective strategy that could be further investigated as a novel alternative for treatment of Parkinson's disease.

  15. Vincristine, doxorubicin and mitomycin (VAM) in patients with advanced breast cancer previously treated with cyclophosphamide, methotrexate and fluorouracil (CMF). A clinical trial of the Piedmont Oncology Association (POA).

    Science.gov (United States)

    Shipp, S K; Muss, H B; Westrick, M A; Cooper, M R; Jackson, D V; Richards, F C; White, D R; Stuart, J J; Christian, R M; Ramseur, W

    1983-01-01

    Thirty-six evaluable patients with advanced breast cancer who had failed prior CMF therapy [15 (42%) as adjuvant treatment and 21 (58%) for advanced disease] were treated with a combination of vincristine, doxorubicin, and mitomycin (VAM). There was one CR and 10 PR, giving a response rate of 31% (P, 95% confidence interval, 15%-47%). Response was not significantly related to age, performance status, disease-free interval, dominant site of disease, number of sites of disease, or estrogen receptor status. The median duration of response was 5 months for patients attaining CR or PR and 4.6 months for patients with stable disease. The median survival for patients with CR or PR of 7.9 months was not better than for those with stable disease (8.0 months), but both groups had significantly longer survival than those with initial progression. Patients who received VAM after failing adjuvant CMF had a 53% response rate (8 of 15), as against a 14% response rate (3 of 21) in those failing CMF for advanced disease (P less than 0.05). In spite of this difference, the survival distributions for these two groups were not significantly different. Myelosuppression was moderate and no cardiac toxicity was seen. The addition of mitomycin to vincristine and doxorubicin in previously treated patients does not appear to improve the results obtained with vincristine and doxorubicin alone.

  16. Replication of simian virus 40 in simian virus 40-transformed hamster kidney cells induced by mitomycin C or /sup 60/Co. gamma. irradiation

    Energy Technology Data Exchange (ETDEWEB)

    Rakusanova, T.; Smales, W.P.; Kaplan, J.C.; Black, P.H.

    1978-07-15

    Several clones of simian virus 40 (SV40)-transformed hamster kidney cells, which are heterogeneous for induction of infectious SV40, have been studied. SV40 yields are low after induction with /sup 60/Co ..gamma.. irradiation or mitomycin C. In order to clarify the mechanism(s) by which virus is produced in induced cells, we analyzed the replication of viral DNA and production of virion (V) antigen and infectious virus after induction in various clones as well as in lytically infected permissive cells. Cells replicating SV40 DNA or synthesizing V antigen were visualized by in situ hybridization and immunofluorescence techniques, respectively. Only some cells in induced cultures were found to produce SV40 and those which did were less efficient than lytically infected monkey cells. Mitomycin C or /sup 60/Co ..gamma.. irradiation acted by inducing more cells to replicate virus rather than by increasing the amount of SV40 released from individual cells. A greater proportion of cells could be induced to replicate SV40 DNA than to synthesize V antigen in all induced clones studied. Also, SV40 DNA replication was induced at lower doses of ..gamma.. irradiation than the production of either V antigen or infectious virus suggesting that synthesis of late virus protein is more restricted in induced cells than is replication of SV40 DNA. These findings indicate that one of the effects of induction treatments on SV40-transformed hamster cells is an enhancement of the cells' capacity to support SV40 replication.

  17. Physical and Chemical Characterization of Poly(hexamethylene biguanide Hydrochloride

    Directory of Open Access Journals (Sweden)

    Luiz Henrique C. Mattoso

    2011-06-01

    Full Text Available We present the characterization of commercially available Poly(hexamethylene biguanide hydrochloride (PHMB, a polymer with biocidal activity and several interesting properties that make this material suitable as a building block for supramolecular chemistry and “smart” materials. We studied polymer structure in water solution by dynamic light scattering, surface tension and capacitance spectroscopy. It shows typical surfactant behavior due to amphiphilic structure and low molecular weight. Spectroscopic (UV/Vis, FT-NIR and thermal characterization (differential scanning calorimetry, DSC, and thermogravimetric analysis, TGA were performed to give additional insight into the material structure in solution and solid state. These results can be the foundation for more detailed investigations on usefulness of PHMB in new complex materials and devices.

  18. β-Cyclodextrin-promazine hydrochloride interaction: Conductometric and viscometric studies

    Directory of Open Access Journals (Sweden)

    Mohd. Sajid Ali

    2015-01-01

    Full Text Available Herein we have studied the interaction of β-cyclodextrin (β-CD with the amphiphilic drug promazine hydrochloride (PMZ by using conductimetry and viscometry. From the observed results it was concluded that critical micelle concentration (cmc of the pure drug was lower than the apparent critical micelle concentration (cmc∗ of the drug in the presence of β-CD. The cmc∗ increased on increasing the concentration of β-CD due to the encapsulation of the amphiphilic drug to the hydrophobic cavities of the β-CD which delayed the micelle formation. Viscosity of the solution decreased drastically on the addition of β-CD which further increased on increasing the drug solution. Free energies of micellization (ΔGmic were calculated with the help of degrees of micelle ionization and cmc obtained from the specific conductivity−[PMZ] plots. Micellization was found to be less spontaneous in the presence of cyclodextrin.

  19. Permanent-wave dermatitis: contact allergy to cysteamine hydrochloride.

    Science.gov (United States)

    Landers, Maeran C; Law, Sandra; Storrs, Frances J

    2003-09-01

    Cysteamine hydrochloride (CHC) is a newly recognized sensitizer found in permanent-wave solutions. We report the case of a hairdresser who was found to be allergic to CHC. Our allergic patient was patch-tested to various chemicals found in permanent-wave solutions, including CHC (1.0% in petrolatum). Patch-test reactions were positive to CHC, glyceryl thioglycolate, diglyceryl thioglycolate, p-phenylenediamine (PPD), and PPD through a piece of latex glove. Sixty-four controls to CHC (1.0% in petrolatum) had negative results. Household-weight latex gloves were protective against CHC allergy. Persons with CHC-waved hair were not allergic. CHC contained in "neutral" permanent-wave preparations has been used in American beauty salons since 1993. We briefly discuss the introduction and significance of CHC in permanent waves.

  20. Betahistine hydrochloride in Méniére's disease.

    Science.gov (United States)

    Frew, I J; Menon, G N

    1976-08-01

    A double-blind, placebo-controlled, cross-over clinical trial was performed to assess the effect of betahistine hydrochloride (Serc) in Ménière's disease. The diagnosis was based on paroxysmal attacks of rotational vertigo, with tinnitus, and a fluctuating sensori-neural deafness, together with the results of auditory and vestigular tests. Twenty-eight patients were admitted to the trial over 3 years. Twenty-two patients completed the trial. In total, they received betahistine 32 mg daily, for a period of 16 weeks, and placebo also for the same length of time, preceded in every case by a 4-week pre-treatment period. Daily symptom score cards were kept. There was a statistically significant improvement in favour of the drug with regard to vertigo, tinnitus and deafness. Vertigo was the most responsive symptom. No adverse reactions were observed.

  1. [Characteristics and selectivity of photocatalytic-degradation of tetracycline hydrochloride].

    Science.gov (United States)

    Song, Chen-Yi; Yin, Da-Qiang

    2014-02-01

    The photocatalytic-degradation behavior of tetracycline hydrochloride (TTC) was studied. The catalyst used was photosensitive semiconductor titanium dioxide (TiO2). The results showed that the photocatalytic degradation of TTC was well fitted to first order reaction kinetics model, and the adsorption was the control step of the whole photocatalytic-degradation process, indicating that the main degradation path was the photocatalytic reaction of TTC adsorbed on the surface of TiO2. Besides, through photocatalytic-degradation of the mixed solution of TTC and sulfamethoxazole or amoxicillin, the degradation of the two antibiotics showed obvious selectivity when the pH, TiO2 dosage and other conditions were changed.

  2. FORMULATION AND EVALUATION OF SUSTAINED RELEASE PELLETS OF TRAMADOL HYDROCHLORIDE

    Directory of Open Access Journals (Sweden)

    Baskara Haripriya

    2013-02-01

    Full Text Available The aim of the present research is to develop and evaluate a better sustained release multiple unit pellets (MUP formulation of Tramadol hydrochloride. Dissolution and diffusion controlled systems have classically been of primary importance in oral delivery of medication because of their relative ease of production and cost compared with other methods of sustained or controlled delivery. Most of these systems are solids, although a few liquids and suspension have been recently introduced. The present work aimed at developing SR pellets of Tramadol HCl by Wurster process. FTIR studies showed no unacceptable extra peaks which confirm the absence of chemical interaction between the drug and polymer. Angle of repose, tapped density, bulk density values for the formulations were within the range which indicates that pellets prepared by Wurster process were satisfactory for further studies. The percentage drug content of Tramadol was determined by extraction with methanol and analyzed by using UV-visible spectrophotometer at 271nm.

  3. Design and Evaluation of Chronomodulated Drug Delivery of Tramadol Hydrochloride.

    Science.gov (United States)

    Alekya, Thota; Narendar, Dudhipala; Mahipal, Donthi; Arjun, Narala; Nagaraj, Banala

    2017-09-26

    Rheumatoid arthritis is an auto immune disease which requires chronotherapy as it occurs during early morning. Tramadol hydrochloride (TH) is an analgesic drug, used to treat rheumatoid arthritis. The aim of the present investigation was to develop chronomodulated drug delivery system of tramadol hydrochloride such that it releases the drug early in the morning, during which the symptoms of rheumatoid arthritis worsen. To develop chronomodulated drug delivery system of TH, initially core tablets of TH were prepared using three different supradisintegrants followed by coating with pH dependent polymer of Eudragit S100. The prepared core tablets are evaluated for physical parameters and an optimal system was identified. Further, coating composition of Eudragit S100 was optimized and coating tablets of TH was prepared. The prepared coated tablets were evaluated for weight variation, hardness, drug content and in vitro release studies in 0.1N HCl, pH 6.8 phosphate buffer and pH 7.4 phosphate buffer. Formulation with 7.5% of coating solution (ES2) had shown a significant drug release after a lag time of 3 h (in pH 6.8 medium), 6 h (in pH 6.8 medium) and 8 h (in pH 7.4 medium), respectively. DSC studies revealed that no interaction between core and coated materials with drug was observed. Thus, chronomodulated drug delivery system of TH was formulated and assuming that if a tablet is administered around 9 pm to 10 pm, the drug release starts after a lag time of 6 h i. e., around 3am to 4 am. © Georg Thieme Verlag KG Stuttgart · New York.

  4. Sinomenine Hydrochloride Protects against Polymicrobial Sepsis via Autophagy

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    Yu Jiang

    2015-01-01

    Full Text Available Sepsis, a systemic inflammatory response to infection, is the major cause of death in intensive care units (ICUs. The mortality rate of sepsis remains high even though the treatment and understanding of sepsis both continue to improve. Sinomenine (SIN is a natural alkaloid extracted from Chinese medicinal plant Sinomenium acutum, and its hydrochloride salt (Sinomenine hydrochloride, SIN-HCl is widely used to treat rheumatoid arthritis (RA. However, its role in sepsis remains unclear. In the present study, we investigated the role of SIN-HCl in sepsis induced by cecal ligation and puncture (CLP in BALB/c mice and the corresponding mechanism. SIN-HCl treatment improved the survival of BALB/c mice that were subjected to CLP and reduced multiple organ dysfunction and the release of systemic inflammatory mediators. Autophagy activities were examined using Western blotting. The results showed that CLP-induced autophagy was elevated, and SIN-HCl treatment further strengthened the autophagy activity. Autophagy blocker 3-methyladenine (3-MA was used to investigate the mechanism of SIN-HCl in vitro. Autophagy activities were determined by examining the autophagosome formation, which was shown as microtubule-associated protein light chain 3 (LC3 puncta with green immunofluorescence. SIN-HCl reduced lipopolysaccharide (LPS-induced inflammatory cytokine release and increased autophagy in peritoneal macrophages (PM. 3-MA significantly decreased autophagosome formation induced by LPS and SIN-HCl. The decrease of inflammatory cytokines caused by SIN-HCl was partially aggravated by 3-MA treatment. Taken together, our results indicated that SIN-HCl could improve survival, reduce organ damage, and attenuate the release of inflammatory cytokines induced by CLP, at least in part through regulating autophagy activities.

  5. Sinomenine hydrochloride protects against polymicrobial sepsis via autophagy.

    Science.gov (United States)

    Jiang, Yu; Gao, Min; Wang, Wenmei; Lang, Yuejiao; Tong, Zhongyi; Wang, Kangkai; Zhang, Huali; Chen, Guangwen; Liu, Meidong; Yao, Yongming; Xiao, Xianzhong

    2015-01-23

    Sepsis, a systemic inflammatory response to infection, is the major cause of death in intensive care units (ICUs). The mortality rate of sepsis remains high even though the treatment and understanding of sepsis both continue to improve. Sinomenine (SIN) is a natural alkaloid extracted from Chinese medicinal plant Sinomenium acutum, and its hydrochloride salt (Sinomenine hydrochloride, SIN-HCl) is widely used to treat rheumatoid arthritis (RA). However, its role in sepsis remains unclear. In the present study, we investigated the role of SIN-HCl in sepsis induced by cecal ligation and puncture (CLP) in BALB/c mice and the corresponding mechanism. SIN-HCl treatment improved the survival of BALB/c mice that were subjected to CLP and reduced multiple organ dysfunction and the release of systemic inflammatory mediators. Autophagy activities were examined using Western blotting. The results showed that CLP-induced autophagy was elevated, and SIN-HCl treatment further strengthened the autophagy activity. Autophagy blocker 3-methyladenine (3-MA) was used to investigate the mechanism of SIN-HCl in vitro. Autophagy activities were determined by examining the autophagosome formation, which was shown as microtubule-associated protein light chain 3 (LC3) puncta with green immunofluorescence. SIN-HCl reduced lipopolysaccharide (LPS)-induced inflammatory cytokine release and increased autophagy in peritoneal macrophages (PM). 3-MA significantly decreased autophagosome formation induced by LPS and SIN-HCl. The decrease of inflammatory cytokines caused by SIN-HCl was partially aggravated by 3-MA treatment. Taken together, our results indicated that SIN-HCl could improve survival, reduce organ damage, and attenuate the release of inflammatory cytokines induced by CLP, at least in part through regulating autophagy activities.

  6. Formulation optimization of propranolol hydrochloride microcapsules employing central composite design

    Directory of Open Access Journals (Sweden)

    Shivakumar H

    2008-01-01

    Full Text Available A central composite design was employed to produce microcapsules of propranolol hydrochloride by o/o emulsion solvent evaporation technique using a mixture of cellulose acetate butyrate as coat material and span-80 as an emulsifier. The effect of formulation variables namely levels of cellulose acetate butyrate (X 1 and percentage of Span-80 (X 2 on encapsulation efficiency (Y 1 , drug release at the end of 1.5 h (Y 2 , 4 h (Y 3 , 8 h (Y 4 , 14 h (Y 5 , and 24 h (Y 6 were evaluated using the F test. Mathematical models containing only the significant terms were generated for each response parameter using multiple linear regression analysis and analysis of variance. Both the formulation variables exerted a significant influence (P < 0.05 on Y 1 whereas the cellulose acetate butyrate level emerged as the lone factor which significantly influenced the other response parameters. Numerical optimization using desirability approach was employed to develop an optimized formulation by setting constraints on the dependent and independent variables. The experimental values of Y 1 , Y 2 , Y 3 , Y 4 , Y 5 , and Y 6 for the optimized formulation was found to be 92.86±1.56% w/w, 29.58±1.22%, 48.56±2.56%, 60.85±2.35%, 76.23±3.16% and 95.12±2.41%, respectively which were in close agreement with those predicted by the mathematical models. The drug release from microcapsules followed first order kinetics and was characterized by Higuchi diffusion model. The optimized microcapsule formulation developed was found to comply with the USP drug release test-1 for extended release propranolol hydrochloride capsules.

  7. Biowaiver monographs for immediate release solid oral dosage forms: ciprofloxacin hydrochloride.

    Science.gov (United States)

    Olivera, M E; Manzo, R H; Junginger, H E; Midha, K K; Shah, V P; Stavchansky, S; Dressman, J B; Barends, D M

    2011-01-01

    Literature data relevant to the decision to allow a waiver of in vivo bioequivalence (BE) testing for the approval of new multisource and reformulated immediate release (IR) solid oral dosage forms containing ciprofloxacin hydrochloride as the only active pharmaceutical ingredient (API) are reviewed. Ciprofloxacin hydrochloride's solubility and permeability, its therapeutic use and index, pharmacokinetics, excipient interactions and reported BE/bioavailability (BA) problems were taken into consideration. Solubility and BA data indicate that ciprofloxacin hydrochloride is a BCS Class IV drug. Therefore, a biowaiver based approval of ciprofloxacin hydrochloride containing IR solid oral dosage forms cannot be recommended for either new multisource drug products or for major scale-up and postapproval changes (variations) to existing drug products.

  8. Co-Amorphous Combination of Nateglinide-Metformin Hydrochloride for Dissolution Enhancement

    National Research Council Canada - National Science Library

    Wairkar, Sarika; Gaud, Ram

    The aim of the present work was to prepare a co-amorphous mixture (COAM) of Nateglinide and Metformin hydrochloride to enhance the dissolution rate of poorly soluble Nateglinide. Nateglinide (120 mg...

  9. Myocardial perfusion imaging with higenamine hydrochloride stress studies in diagnosis of coronary artery disease

    Institute of Scientific and Technical Information of China (English)

    周维

    2013-01-01

    Objective To evaluate the stress test efficacy and safety of higenamine hydrochloride,MPI studies were performed in patients with coronary artery disease. Methods Sixty-eight patients with suspected coronary artery

  10. Synthesis of 2-Heterocyclomethyl-5-diphenylmethylenecyclopentanone Hydrochlorides and their Inhibitory Effect on Tumor Cell Growth

    Institute of Scientific and Technical Information of China (English)

    Yun Hai ZHANG; Lin Xiang ZHAO; Zhen Jun BIAN; Rui WANG; Fu Yuan SUN

    2006-01-01

    Sixteen new 2-heterocyclomethyl-5-diphenylmethylenecyclopentanone hydrochlorides were designed and synthesized. The growth inhibitory effect of these compounds in vitro was conducted using a MTT assay in human breast cancer T47D cells.

  11. The effect of tramadol hydrochloride on early life stages of fish.

    Science.gov (United States)

    Sehonova, Pavla; Plhalova, Lucie; Blahova, Jana; Berankova, Petra; Doubkova, Veronika; Prokes, Miroslav; Tichy, Frantisek; Vecerek, Vladimir; Svobodova, Zdenka

    2016-06-01

    The aim of this study was to perform the fish embryo acute toxicity test (FET) on zebrafish (Danio rerio) and the early-life stage toxicity test on common carp (Cyprinus carpio) with tramadol hydrochloride. The FET was performed using the method inspired by the OECD guideline 236. Newly fertilized zebrafish eggs were exposed to tramadol hydrochloride at concentrations of 10; 50; 100 and 200μg/l for a period of 144h. An embryo-larval toxicity test on C. carpio was performed according to OECD guideline 210 also with tramadol hydrochloride at concentrations 10; 50; 100 and 200μg/l for a period of 32 days. Hatching was significantly influenced in both acute and subchronic toxicity assays. Subchronic exposure also influenced early ontogeny, both morphometric and condition characteristics and caused changes in antioxidant enzyme activity. The LOEC value was found to be 10μg/l tramadol hydrochloride.

  12. Effects of drotaverine hydrochloride on viability of rat cultured cerebellar granulocytes.

    Science.gov (United States)

    Demushkin, V P; Zhavoronkova, E V; Khaspekov, L G

    2012-02-01

    The neurocytotoxic effect of drotaverine hydrochloride was studied in culture of rat cerebellar granulocytes. Incubation of cells with 100 and 250 μM drotaverine reduced neuronal survival to 60 and 4%, respectively.

  13. Thiamine hydrochloride: An efficient catalyst for one-pot synthesis of quinoxaline derivatives at ambient temperature

    Indian Academy of Sciences (India)

    Omprakash B Pawar; Fulchand R Chavan; Venkat S Suryawanshi; Vishnu S Shinde; Narayan D Shinde

    2013-01-01

    Quinoxaline derivatives have been synthesized in high to excellent yields in the presence of thiamine hydrochloride (VB1) as an inexpensive, non-toxic and metal ion free catalyst at ambient temperature.

  14. 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.

  15. 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

  16. Synthesis and Characterization of Impurities of Barnidipine Hydrochloride, an Antihypertensive Drug Substance

    OpenAIRE

    Zhi-Gang Cheng; Xu-Yong Dai; Li-Wei Li; Qiong Wan; Xiang Ma; Guang-Ya Xiang

    2014-01-01

    Barnidipine hydrochloride is a long term dihydropyridine calcium channel blocker used for the treatment of hypertension. During the process development of barnidipine hydrochloride, four barnidipine impurities were detected by high-performance liquid chromatography (HPLC) with an ordinary column (Agilent ZORBAX Eclipse XDB-C18, 150 mm × 4.6 mm, 5 µm). All these impurities were identified, synthesized, and subsequently characterized by their respective spectral data (MS, 1H-NMR, and 13C-NMR)...

  17. Synthesis and Characterization of Impurities of Barnidipine Hydrochloride, an Antihypertensive Drug Substance

    OpenAIRE

    Cheng, Zhi-Gang; Dai, Xu-Yong; Li, Li-Wei; Wan, Qiong; Ma, Xiang; Xiang, Guang-Ya

    2014-01-01

    Barnidipine hydrochloride is a long term dihydropyridine calcium channel blocker used for the treatment of hypertension. During the process development of barnidipine hydrochloride, four barnidipine impurities were detected by high-performance liquid chromatography (HPLC) with an ordinary column (Agilent ZORBAX Eclipse XDB-C18, 150 mm × 4.6 mm, 5 µm). All these impurities were identified, synthesized, and subsequently characterized by their respective spectral data (MS, 1H-NMR, and 13C-NMR). ...

  18. Co-Amorphous Combination of Nateglinide-Metformin Hydrochloride for Dissolution Enhancement.

    Science.gov (United States)

    Wairkar, Sarika; Gaud, Ram

    2016-06-01

    The aim of the present work was to prepare a co-amorphous mixture (COAM) of Nateglinide and Metformin hydrochloride to enhance the dissolution rate of poorly soluble Nateglinide. Nateglinide (120 mg) and Metformin hydrochloride (500 mg) COAM, as a dose ratio, were prepared by ball-milling technique. COAMs were characterized for saturation solubility, amorphism and physicochemical interactions (X-ray powder diffraction (XRPD), differential scanning calorimetry (DSC), Fourier transform infrared spectroscopy (FTIR)), SEM, in vitro dissolution, and stability studies. Solubility studies revealed a sevenfold rise in solubility of Nateglinide from 0.061 to 0.423 mg/ml in dose ratio of COAM. Solid-state characterization of COAM suggested amorphization of Nateglinide after 6 h of ball milling. XRPD and DSC studies confirmed amorphism in Nateglinide, whereas FTIR elucidated hydrogen interactions (proton exchange between Nateglinide and Metformin hydrochloride). Interestingly, due to low energy of fusion, Nateglinide was completely amorphized and stabilized by Metformin hydrochloride. Consequently, in vitro drug release showed significant increase in dissolution of Nateglinide in COAM, irrespective of dissolution medium. However, little change was observed in the solubility and dissolution profile of Metformin hydrochloride, revealing small change in its crystallinity. Stability data indicated no traces of devitrification in XRPD of stability sample of COAM, and % drug release remained unaffected at accelerated storage conditions. Amorphism of Nateglinide, proton exchange with Metformin hydrochloride, and stabilization of its amorphous form have been noted in ball-milled COAM of Nateglinide-Metformin hydrochloride, revealing enhanced dissolution of Nateglinide. Thus, COAM of Nateglinide-Metformin hydrochloride system is a promising approach for combination therapy in diabetic patients.

  19. SIMULTANEOUS ESTIMATION OF DICLOFENAC SODIUM AND TOLPERISONE HYDROCHLORIDE IN COMBINED PHARMACEUTICAL FORMULATION

    OpenAIRE

    Bhavesh Gevriya* and R.C. Mashru

    2013-01-01

    Three simple, rapid, precise and accurate spectrophotometric methods have been developed for simultaneous analysis of Tolperisone Hydrochloride (TOL) and Diclofenac Sodium (DIC) in their combined dosage form. Method A, Simultaneous equation method (Vierodt’s method) applies measurement of absorptivities at two wavelengths, 261.00 nm (λmax of Tolperisone Hydrochloride) and 279.00 nm, (λmax of Diclofenac Sodium) in zero order spectra. The concentrations can be calculated from the derived equati...

  20. SPECTROPHOTOMETRIC METHOD FOR SIMULTANEOUS ESTIMATION OF TOLPERISONE HYDROCHLORIDE AND DICLOFENAC SODIUM IN SYNTHETIC MIXTURE

    OpenAIRE

    Patel Satish A; Hariyani Kaushik P

    2012-01-01

    The present manuscript describes simple, sensitive, rapid, accurate, precise and economical spectrophotometric method for the simultaneous determination of Diclofenac sodium and Tolperisone hydrochloride in bulk and synthetic mixture. The method is based on the simultaneous equations for analysis of both the drugs using methanol as solvent. Diclofenac sodium has absorbance maxima at 281 nm and Tolperisone hydrochloride has absorbance maxima at 255 nm in methanol. The linearity was obtained in...

  1. The effect of L-ornithine hydrochloride ingestion on human growth hormone secretion after strength training

    OpenAIRE

    2010-01-01

    This study aimed to examine the effect of L-ornithine hydrochloride ingestion on serum growth hormone secretion response after strength training in young men who did not regularly engage in high intensity exercise. Ten healthy young males without workout habits (age: 22.2 +/- 1.0 yr). Subjects performed biceps curl strength training after L-ornithine hydrochloride and placebo ingestions. They participated in both of the above conditions randomly with a week interval in between. Serum growth h...

  2. Targeting of pegylated liposomal mitomycin-C prodrug to the folate receptor of cancer cells: Intracellular activation and enhanced cytotoxicity.

    Science.gov (United States)

    Patil, Yogita; Amitay, Yasmine; Ohana, Patricia; Shmeeda, Hilary; Gabizon, Alberto

    2016-03-10

    Mitomycin C (MMC) is a powerful anti-bacterial, anti-fungal and anti-tumor antibiotic, often active against multidrug resistant cells. Despite a broad spectrum of antitumor activity, MMC clinical use is relatively limited due to its fast clearance and dose-limiting toxicity. To exploit the potential antitumor activity of MMC and reduce its toxicity we have previously developed a formulation of pegylated liposomes with a lipophilic prodrug of MMC (PL-MLP), activated by endogenous reducing agents which are abundant in the tumor cell environment in the form of different thiols. PL-MLP has minimal in vitro cytotoxicity unless reducing agents are added to the cell culture to activate the prodrug. In the present study, we hypothesized that targeting PL-MLP via folate receptors will facilitate intracellular activation of prodrug and enhance cytotoxic activity without added reducing agents. We grafted a lipophilic folate conjugate (folate-PEG(5000)-DSPE) to formulate folate targeted liposomes (FT-PL-MLP) and examined in vitro cell uptake and cytotoxic activity in cancer cell lines with high folate receptors (HiFR). 3H-cholesterol-hexadecyl ether (3H-Chol)-radiolabeled liposomes were prepared to study liposome-cell binding in parallel to cellular uptake of prodrug MLP. 3H-Chol and MLP cell uptake levels were 4-fold and 9-fold greater in KB HiFR cells when FT-PL-MLP is compared to non-targeted PL-MLP liposomes. The cytotoxic activity of FT-PL-MLP liposomes was significantly increased up to ~5-fold compared with PL-MLP liposomes in all tested HiFR expressing cell lines. The enhanced uptake and intracytoplasmic liposome delivery was confirmed by confocal fluorescence studies with Rhodamine-labeled liposomes. In vivo, no significant differences in pharmacokinetics and biodistribution were observed when PL-MLP was compared to FT-PL-MLP by the intravenous route. However, when liposomes were directly injected into the peritoneal cavity of mice with malignant ascites of J6456 Hi

  3. 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.

  4. A Randomized Clinical Trial of Berberine Hydrochloride in Patients with Diarrhea-Predominant Irritable Bowel Syndrome.

    Science.gov (United States)

    Chen, Chunqiu; Tao, Chunhua; Liu, Zhongchen; Lu, Meiling; Pan, Qiuhui; Zheng, Lijun; Li, Qing; Song, Zhenshun; Fichna, Jakub

    2015-11-01

    We aimed to evaluate clinical symptoms in diarrhea predominant irritable bowel syndrome (IBS-D) receiving berberine hydrochloride in a randomized double-blind placebo-controlled clinical trial. Overall, 196 patients with IBS-D were recruited for this study; consequently, 132 patients randomized to receive daily 400 mg of berberine hydrochloride, delivered twice daily or placebo for 8 weeks followed by a 4-week washout period. After a 2-week run-in period, diarrhea, abdominal pain, urgent need for defecation frequency and any adverse events were recorded daily. Prior to administration of the medication and after completing the treatment, assessment of IBS symptom scores, depression and anxiety scale scores and the IBS scale for quality of life (QOL) was carried out. The effects of berberine hydrochloride on IBS-D, defined by a reduction of diarrhea frequency (P = 0.032), abdominal pain frequency (P berberine group than the placebo group in the 8 weeks of treatment. A trend of improvement (P berberine hydrochloride for IBS symptom score, depression score and anxiety score and the IBSQOL, compared with placebo. At last, berberine hydrochloride was well tolerated. So we concluded that berberine hydrochloride is well tolerated and reduces IBS-D symptoms, which effectively improved patients QOL.

  5. Using crystal structure prediction to rationalize the hydration propensities of substituted adamantane hydrochloride salts.

    Science.gov (United States)

    Mohamed, Sharmarke; Karothu, Durga Prasad; Naumov, Panče

    2016-08-01

    The crystal energy landscapes of the salts of two rigid pharmaceutically active molecules reveal that the experimental structure of amantadine hydrochloride is the most stable structure with the majority of low-energy structures adopting a chain hydrogen-bond motif and packings that do not have solvent accessible voids. By contrast, memantine hydrochloride which differs in the substitution of two methyl groups on the adamantane ring has a crystal energy landscape where all structures within 10 kJ mol(-1) of the global minimum have solvent-accessible voids ranging from 3 to 14% of the unit-cell volume including the lattice energy minimum that was calculated after removing water from the hydrated memantine hydrochloride salt structure. The success in using crystal structure prediction (CSP) to rationalize the different hydration propensities of these substituted adamantane hydrochloride salts allowed us to extend the model to predict under blind test conditions the experimental crystal structures of the previously uncharacterized 1-(methylamino)adamantane base and its corresponding hydrochloride salt. Although the crystal structure of 1-(methylamino)adamantane was correctly predicted as the second ranked structure on the static lattice energy landscape, the crystallization of a Z' = 3 structure of 1-(methylamino)adamantane hydrochloride reveals the limits of applying CSP when the contents of the crystallographic asymmetric unit are unknown.

  6. RP-HPLC estimation of imipramine hydrochloride and diazepam in tablets

    Directory of Open Access Journals (Sweden)

    D Srikantha

    2015-01-01

    Full Text Available A simple and rapid reversed phase-high performance liquid chromatographic method was developed for simultaneous determination of imipramine hydrochloride and diazepam in pharmaceutical formulations. The elution was done in isocratic mode utilizing a mobile phase consisting of methanol:water:0.1M sodium acetate (30:50:20 v/v/v on Chromosil C18 column with a flow rate of 1.0 ml/min and with detection at 243 nm. The measured retention time was 3.33±0.02 min for imipramine hydrochloride and 4.64±0.02 min for diazepam. Linearity was measured in the range 25-150 μg/ml for imipramine hydrochloride (r 2 =0.999 and in the range 5-30 μg/ml for diazepam (r 2 =0.9994, respectively. The limits of detection and quantitation were 0.03 and 0.1 μg/ml for imipramine hydrochloride and 0.02 and 0.07 μg/ml for diazepam. Satisfactory validation was also obtained from recovery (100.95-101.52% for imipramine hydrochloride and 99.47-100.33% for diazepam studies, intraday and interday precision (<2% and robustness results. The reported method was the first study of these drugs in combination and could be employed for routine quantitative determination of imipramine hydrochloride and diazepam in tablets.

  7. HPLC method validation for modernization of the tetracycline hydrochloride capsule USP monograph

    Directory of Open Access Journals (Sweden)

    Emad M. Hussien

    2014-12-01

    Full Text Available This paper is a continuation to our previous work aiming at development and validation of a reversed-phase HPLC for modernization of tetracycline-related USP monographs and the USP general chapter . Previous results showed that the method is accurate and precise for the assay of tetracycline hydrochloride and the limit of 4-epianhydrotetracycline impurity in the drug substance and oral suspension monographs. The aim of the current paper is to examine the feasibility of the method for modernization of USP tetracycline hydrochloride capsule monograph. Specificity, linearity, accuracy and precision were examined for tetracycline hydrochloride assay and 4-epianhydrotetracycline limit. The method was linear in the concentration range from 80% to 160% (r>0.9998 of the assay concentration (0.1 mg/mL for tetracycline hydrochloride and from 50% to 150% (r>0.997 of the acceptance criteria specified in tetracycline hydrochloride capsule monograph for 4-epianhydrotetracycline (NMT 3.0%. The recovery at three concentration levels for tetracycline hydrochloride assay was between 99% and 101% and the RSD from six preparations at the concentration 0.1 mg/mL is less than 0.6%. The recovery for 4-epianhydrotetracycline limit procedure over the concentration range from 50% to 150% is between 96% and 102% with RSD less than 5%. The results met the specified acceptance criteria.

  8. SPECTROPHOTOMETRIC METHOD FOR SIMULTANEOUS ESTIMATION OF TOLPERISONE HYDROCHLORIDE AND DICLOFENAC SODIUM IN SYNTHETIC MIXTURE

    Directory of Open Access Journals (Sweden)

    Patel Satish A

    2012-09-01

    Full Text Available The present manuscript describes simple, sensitive, rapid, accurate, precise and economical spectrophotometric method for the simultaneous determination of Diclofenac sodium and Tolperisone hydrochloride in bulk and synthetic mixture. The method is based on the simultaneous equations for analysis of both the drugs using methanol as solvent. Diclofenac sodium has absorbance maxima at 281 nm and Tolperisone hydrochloride has absorbance maxima at 255 nm in methanol. The linearity was obtained in the concentration range of 2-20 μg/ml and 2-20 μg/ml for Diclofenac sodium and Tolperisone hydrochloride, respectively. The concentrations of the drugs were determined by using simultaneous equations at both the wavelengths. The mean recovery was 100.6 ± 0.41 and 99.64 ± 0.50 for Diclofenac sodium and Tolperisone hydrochloride, respectively. The method was successfully applied to laboratory prepared synthetic mixture because no interference from the mixture excipients was found. The suitability of this method for the quantitative determination of Diclofenac sodium and Tolperisone hydrochloride was proved by validation. The proposed method was found to be simple and sensitive for the routine quality control application of Diclofenac sodium and Tolperisone hydrochloride in combination. The results of analysis have been validated statistically and by recovery studies.

  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. Comparison between lignocaine hydrochloride and ropivacaine hydrochloride as lumbosacral epidural anaesthetic agents in goats undergoing laparoscopy assisted embryo transfer

    Directory of Open Access Journals (Sweden)

    Anubhav Khajuria

    2014-10-01

    Full Text Available Goats (n=12 undergoing laparoscopy assisted embryo transfer were randomly allotted to two groups (I and II and injected lignocaine hydrochloride (4mg/kg or ropivacaine hydrochloride (1mg/kg at the lumbosacral epidural space. The animals were held with raised hind quarters for first three minutes following injection. Immediately after induction of regional anaesthesia, they were restrained in dorsal recumbency in Trendelenburg position in a cradle. Laparoscopy was performed after creating pneumoperitoneum using filtered room air. The mean (± S.E induction time in animals of group I was significantly shorter (5.33 ± 0.61 min than those belonging to group II (12.66 ±1.99 min. Complete analgesia developed throughout the hind quarters and abdomen for 30 min and 60 min in group I and II animal’s respectively. Unlike animals of group I, group II goats continued to show moderate analgesia for 180 minutes. The motor activity returned after a lapse of 130.00 ± 12.64 min and 405.00 ± 46.31 min respectively. Occasional vocalization and struggling was noticed in two goats one from each group irrespective of the surgical manipulations during laparoscopy. The rectal temperature and respiration rates showed only non-significant increase, but the heart rate values were significantly higher (P < 0.5 up to 150 min in animals of both the groups when compared to their baseline values. From this study, it was concluded that both anaesthetic agents produced satisfactory regional anaesthesia in goats undergoing laparoscopy. However, considering the very long delay in regaining the hind limb motor activity, the use of ropivacaine may not be recommended for this purpose. Supplementation of sedative/tranquilizer with lumbosacral epidural anaesthesia needs evaluation.

  11. Biowaiver monographs for immediate release solid oral dosage forms based on biopharmaceutics classification system (BCS) literature data: verapamil hydrochloride, propranolol hydrochloride, and atenolol.

    Science.gov (United States)

    Vogelpoel, H; Welink, J; Amidon, G L; Junginger, H E; Midha, K K; Möller, H; Olling, M; Shah, V P; Barends, D M

    2004-08-01

    Literature data related to the Biopharmaceutics Classification System (BCS) are presented on verapamil hydrochloride, propranolol hydrochloride, and atenolol in the form of BCS-monographs. Data on the qualitative composition of immediate release (IR) tablets containing these active substances with a Marketing Authorization (MA) in the Netherlands (NL) are also provided; in view of these MA's the assumption was made that these tablets were bioequivalent to the innovator product. The development of a database with BCS-related data is announced by the International Pharmaceutical Federation (FIP).

  12. An enantioselective synthesis of S-[gamma]-[(4-trifluoromethyl)phenoxy]benzenepropanamine-[3-[sup 14]C] hydrochloride, an important metabolite of fluoxetine hydrochloride

    Energy Technology Data Exchange (ETDEWEB)

    Wheeler, W.J. (Lilly (Eli) and Co., Indianapolis, IN (United States). Lilly Research Labs.)

    1992-06-01

    The S-enantiomer of [gamma]-[(4-trifluoromethyl)phenoxy]benzenepropanamine-[3-[sup 14]C] hydrochloride has been prepared in eight steps from acetophenone-[carbonyl-[sup 14]C]. The key step in the synthesis involved the enantioselective reduction of R-2-chloroacetophenone-[1-[sup 14]C]with (-)-diisopinocampheyl-chloroborane in an 86.5% yield. The chlorohydrin was converted to R-phenyloxirane-[1-[sup 14]C], which was subsequently converted to the corresponding R-cyanohydrin by reaction with TMS-CN/CaO. Borane reduction and arylation, followed by salt formation yielded S-[gamma]-[(4-trifluoromethyl)phenoxy]benzenepropanamine-[3-[sup 14]C] hydrochloride. (author).

  13. 光谱法研究丝裂霉素、血清白蛋白 以及金属离子间的相互作用%Studies of Interaction of Mitomycin C and Serum Albumin by Spectrum Method

    Institute of Scientific and Technical Information of China (English)

    张勇; 张贵珠; 王月梅; 卢继新

    2000-01-01

    The interaction of Mitomycin C, which is an antitumour antibiotic, and serum albumin has been studied by using fluorescence spectropho tometry. The binding constant of Mitomycin C and bovine serum albumin has been o btained, and the effects of some metal ions on the binding constan were also exp lored.%用荧光光谱法研究了抗癌药物丝裂霉素(Mitomycin C) 与血清白蛋白的相互作用,以及一些金属离子对丝裂霉素与牛血清白蛋白(BSA)相互作用的影响。

  14. Eradication of Biofilm-like Microcolony Structures of Borrelia burgdorferi by Daunomycin and Daptomycin but not Mitomycin C in Combination with Doxycycline and Cefuroxime

    Directory of Open Access Journals (Sweden)

    Jie eFeng

    2016-02-01

    Full Text Available Lyme disease, caused by Borrelia burgdorferi, is the most common vector-borne disease in the United States and Europe. While the majority of Lyme disease patients can resolve their symptoms if treated promptly, 10-20% of patients suffer from prolonged symptoms called post-treatment Lyme disease syndrome (PTLDS. Although the cause for PTLDS is unclear, one possibility is the presence of bacterial persisters not effectively cleared by the current Lyme antibiotics. Recent studies identified several drug candidates including daptomycin, daunomycin, doxorubicin, and mitomycin C that had good activity against B. burgdorferi persisters. However, their relative activities against B. burgdorferi persisters have not been evaluated under the same conditions. In this study, we tested the anti-persister activities of these drugs against both 7-day and 15-day old stationary phase cultures of B. burgdorferi individually as well as in combination with Lyme antibiotics doxycycline and cefuroxime (Ceftin. Our findings demonstrate daunomycin and daptomycin were more active than mitomycin C in single drug comparison at 10 and 20 µM, as well as in drug combinations with doxycycline and cefuroxime. In addition, daunomycin was more active than doxorubicin which correlated with their ability to stain and accumulate in B. burgdorferi. The two drug combination of doxycycline and cefuroxime was unable to eradicate biofilm-like microcolonies of B. burgdorferi persisters. However, the addition of either daunomycin or daptomycin to the doxycycline + cefuroxime combination completely eradicated the biofilm-like structures and produced no visible bacterial regrowth after 7 days and 21 days, while the addition of doxorubicin was unable to prevent regrowth at either 7 day or 21 day subculture. Mitomycin C in combination with doxycycline and cefuroxime caused no regrowth at 7 days but visible spirochetal regrowth occurred after 21 day subculture. Furthermore, we found that

  15. Application of mitomycin in glaucoma surgery in%丝裂霉素在抗青光眼术中的应用

    Institute of Scientific and Technical Information of China (English)

    魏冉

    2015-01-01

    Objective To explore the application effect of mitomycin in glaucoma surgery in safety and. Methods 36 cases of 42 eyes of glaucoma patients with 0.5mg per milliliter of mitomycin solution soaked 4×4mm cotton sheet into the scleral flap in under 3 minutes, into a piece of cotton under the same size of conjunctival flap for 2 minutes, and then use the 200mL physiological saline solution scleral flap and conjunctival flap remaining under repeated washing, small beam organization under the scleral flap resection in 2×1mm, corresponding scleral iridectomy. Results 42 eyes after follicular lichen, dispersion, pale, no neovascularization, discharge of intraocular pressure at 0.8~2.3kPa, the average 1.66kPa. Conclusion Using mitomycin as auxiliary medicine in anti glaucoma operation, avoids the disadvantages of repeated subconjunctival injection, easy to accept the patient.%目的:探讨丝裂霉素在抗青光眼术中的应用疗效与安全性。方法36例(42只眼)青光眼患者术中用0.5 mg/mL的丝裂霉素溶液浸泡过的4×4 mm棉片放入巩膜瓣下3 min,用同样大小的棉花片放入结膜瓣下2 min,然后用200 mL生理盐水反复冲洗巩膜瓣及结膜瓣下残存的药液,在巩膜瓣下切除2×1 mm的小梁组织,做相应巩膜周边切除。结果42只眼术后滤泡扁平,弥散,色苍白,无新生血管长入,出院时眼压在0.8~2.3 kPa,平均1.66 kPa。结论采用丝裂霉素作为抗青光眼术中的辅助药物,避免了反复球结膜下注射的弊端,患者容易接受。

  16. Simultaneous Integrated Boost–Intensity Modulated Radiation Therapy With Concomitant Capecitabine and Mitomycin C for Locally Advanced Anal Carcinoma: A Phase 1 Study

    Energy Technology Data Exchange (ETDEWEB)

    Deenen, Maarten J. [Division of Clinical Pharmacology, Department of Medical Oncology, The Netherlands Cancer Institute, Amsterdam (Netherlands); Dewit, Luc [Department of Radiotherapy, The Netherlands Cancer Institute, Amsterdam (Netherlands); Boot, Henk [Division of Gastroenterology and Hepatology, Department of Medical Oncology, The Netherlands Cancer Institute, Amsterdam (Netherlands); Beijnen, Jos H. [Department of Pharmacy and Pharmacology, Slotervaart Hospital, Amsterdam (Netherlands); Faculty of Science, Department of Pharmaceutical Sciences, Division of Pharmaco-epidemiology and Clinical Pharmacology, Utrecht University, Utrecht (Netherlands); Schellens, Jan H.M. [Division of Clinical Pharmacology, Department of Medical Oncology, The Netherlands Cancer Institute, Amsterdam (Netherlands); Faculty of Science, Department of Pharmaceutical Sciences, Division of Pharmaco-epidemiology and Clinical Pharmacology, Utrecht University, Utrecht (Netherlands); Cats, Annemieke, E-mail: a.cats@nki.nl [Division of Gastroenterology and Hepatology, Department of Medical Oncology, The Netherlands Cancer Institute, Amsterdam (Netherlands)

    2013-04-01

    Purpose: Newer radiation techniques, and the application of continuous 5-FU exposure during radiation therapy using oral capecitabine may improve the treatment of anal cancer. This phase 1, dose-finding study assessed the feasibility and efficacy of simultaneous integrated boost–intensity modulated radiation therapy (SIB-IMRT) with concomitant capecitabine and mitomycin C in locally advanced anal cancer, including pharmacokinetic and pharmacogenetic analyses. Methods and Materials: Patients with locally advanced anal carcinoma were treated with SIB-IMRT in 33 daily fractions of 1.8 Gy to the primary tumor and macroscopically involved lymph nodes and 33 fractions of 1.5 Gy electively to the bilateral iliac and inguinal lymph node areas. Patients received a sequential radiation boost dose of 3 × 1.8 Gy on macroscopic residual tumor if this was still present in week 5 of treatment. Mitomycin C 10 mg/m{sup 2} (maximum 15 mg) was administered intravenously on day 1, and capecitabine was given orally in a dose-escalated fashion (500-825 mg/m{sup 2} b.i.d.) on irradiation days, until dose-limiting toxicity emerged in ≥2 of maximally 6 patients. An additional 8 patients were treated at the maximum tolerated dose (MTD). Results: A total of 18 patients were included. The MTD of capecitabine was determined to be 825 mg/m{sup 2} b.i.d. The predominant acute grade ≥3 toxicities included radiation dermatitis (50%), fatigue (22%), and pain (6%). Fifteen patients (83% [95%-CI: 66%-101%]) achieved a complete response, and 3 (17%) patients a partial response. With a median follow-up of 28 months, none of the complete responders, and 2 partial responders had relapsed. Conclusions: SIB-IMRT with concomitant single dose mitomycin C and capecitabine 825 mg/m{sup 2} b.i.d. on irradiation days resulted in an acceptable safety profile, and proved to be a tolerable and effective treatment regimen for locally advanced anal cancer.

  17. 丝裂霉素C在青光眼治疗中的应用分析%To Explore the Mitomycin C Application in Treatment of Glaucoma

    Institute of Scientific and Technical Information of China (English)

    鲁孝辉

    2015-01-01

    目的:探究青光眼患者采用丝裂霉素C治疗的方法和效果。方法选取2013年7月~2014年8月收治的34例青光眼患者进行治疗,随机分组,实验组20例选择丝裂霉素C和小梁切除术的治疗,对照组14例患者金给予小梁切除术的治疗,不叫治疗效果。结果实验组治疗有效率为95.0%,对照组治疗有效率为78.57%,P<0.05,差异具有统计学意义。结论青光眼患者在治疗中采取小梁切除术和丝裂霉素,安全性高,效果显著,术后的并发症较少,操作简便。%Objective To explore mitomycin C application method and its effect in treatment of patients with glaucoma.MethodsGather 34 glaucoma patients who are received and treated in hospital from July 2013 to August 2014 and separate them into two groups at random, 20 patients in study group are given mitomycin C medication combined with trabeculectomy operation treatment, while 14 patients in control group are given trabeculectomy operation treatment only, and then compare treatment effects between two groups. Results Treatment efifcacy in study group is up to 95.0%; while treatment efifcacy in control group is 78.57%, there is a differential between two groups and such a differential has statistic value (P<0.05).Conclusion Mitomycin C medication combined with trabeculectomy operation treatment is of efifcacy and safety in treatment of glaucoma patient,besides, such a treatment method is easy to operate and has few complications.

  18. Single-step transepithelial ASLA (SCHWIND with mitomycin-C for the correction of high myopia: long term follow-up

    Directory of Open Access Journals (Sweden)

    Aslanides IM

    2014-12-01

    Full Text Available Ioannis M Aslanides, Panagiotis N Georgoudis, Vasilis D Selimis, Achyut N Mukherjee Emmetropia Mediterranean Eye Institute, Heraklion, Crete, Greece Purpose: We wanted to compare the outcomes of single-step modified transepithelial photorefractive keratectomy (tPRK termed a SCHWIND all surface laser ablation (ASLA versus conventional alcohol-assisted photorefractive keratectomy (PRK and laser-assisted in situ keratomileusis (LASIK for the correction of higher myopia of 6.00 diopters (D or more, in an area with high risk of haze due to high intensity of sunlight.Methods: We used a prospective interventional cohort with matched retrospective control groups. Patients with >6 D myopia and <3.5 D of astigmatism were included. All treatments were performed with the SCHWIND Amaris system using aspheric ablation profiles. Mitomycin C was used in all PRK and ASLA cases. Outcomes were postoperative refraction, visual acuity, stability, and complications. The follow-up period was up to 12 months.Results: In total, 101 eyes were included after exclusions. Mean preoperative spherical equivalent refraction was −7.9 D, −8.2 D, and −7.4 D in the ASLA (n=41, PRK (n=29, and LASIK (n=31 groups. Mean postoperative spherical equivalent at 12 months postoperatively was −0.1 (standard deviation [SD]: 0.34, −0.2 (SD: 0.59, and −0.08 (SD: 0.36 in the ASLA, PRK, and LASIK groups, with 91.4%, 85.7%, and 83.9% within 0.5 D of target, respectively. Refractive outcomes and regression at 12 months did not vary among groups (P>0.05. Mean logMAR (logarithm of the minimum angle of resolution uncorrected distance visual acuity at 12 months was 0.00 (SD: 0.05, 0.06 (SD: 0.1, and 0.05 (SD: 0.09 in the ASLA, PRK, and LASIK groups, with significantly better vision in the tPRK group versus LASIK (P=0.01 and PRK (P=0.01 groups.Conclusion: ASLA (SCHWIND tPRK with mitomycin C for high myopia demonstrates comparable refractive outcomes to LASIK and PRK, with relatively

  19. [Treatment of 9 squamous epithelial carcinoma in situ lesions of the conjunctiva (CIN) with mitomycin C eyedrops in cytological and DNA image cytometric control].

    Science.gov (United States)

    Cartsburg, O; Kersten, A; Sundmacher, R; Nadjari, B; Pomjanski, N; Böcking, A

    2001-06-01

    Conjunctival intraepithelial neoplasia (CIN) is a frequent conjunctival tumor. Following excision alone recurrences are frequent. An effective postsurgical recurrence prevention is therefore highly desirable. In this study we aimed to evaluate the effectivity of postsurgical chemotherapy of conjunctival squamous cell carcinoma in situ (CIN) with mitomycin C eyedrops. We introduced the otherwise established diagnostic tools of cytology and DNA-image-cytometry to the diagnosis and therapy-monitoring of CIN. We treated 9 patients with CIN. For diagnosis the results of cytology and cytometry of presurgically obtained brush smears were compared with the histologic evaluation of the excised tissue. After surgery, we administered topical chemotherapy with mitomycin C eye drops 0.02% (MMC). Conjunctival brush smears were again evaluated by cytology and DNA-image-cytometry for postsurgical therapy monitoring. The clinical diagnosis of CIN was fully confirmed by cytology, DNA-image-cytometry and histology respectively in 7 patients. In one patient, the results of the applied diagnostic methods differed in results: Histologic evaluation indicated a moderate dysplasia but DNA-image-cytometry showed significant DNA-aneuploidy unequivocally indicating neoplasia like squamous cell carcinoma. In another patient the preoperatively obtained conjunctival brush smears could not properly analyzed by cytometry but clinical diagnosis was confirmed by histology. MMC-therapy was well tolerated except for a self-limited conjunctivitis. A complete remission of CIN was obtained in 8 of 9 patients (89%) who were free of CIN recurrences during a follow-up period of 27.2 months (11-48). Only one patient suffered from a recurrence 14 months after surgery and after 2 MMC-cycles. Adjuvant topical mitomycin C appears to be effective in the prevention of recurrences of conjunctival CIN after surgical removal. Our results indicate that at least 4 cycles of topical MMC are required to prevent local

  20. Stability-indicating HPTLC determination of ambroxol hydrochloride in bulk drug and pharmaceutical dosage form.

    Science.gov (United States)

    Jain, P S

    2010-01-01

    A simple, selective, precise, and stability-indicating high-performance thin-layer chromatographic (HPTLC) method for the analysis of ambroxol hydrochloride both as a bulk drug and in formulations was developed and validated. The method employed HPTLC aluminium plates precoated with silica gel 60F-254 as the stationary phase. The solvent system consisted of methanol-triethylamine (4:6 v/v). The system was found to give a compact spot for ambroxol hydrochloride (R(f) value of 0.53 +/- 0.02). Densitometric analysis of ambroxol hydrochloride was carried out in the absorbance mode at 254 nm. The linear regression analysis data for the calibration plots showed good linear relationship with r(2) = 0.9966 +/- 0.0013 with respect to peak area in the concentration range 100-1000 ng/spot. The mean value +/- standard deviation of slope and intercept were 164.85 +/- 0.72 and 1168.3 +/- 8.26 with respect to peak area. The method was validated for precision, recovery, and robustness. The limits of detection and quantitation were 10 and 30 ng/spot, respectively. Ambroxol hydrochloride was subjected to oxidation and thermal degradation. The drug undergoes degradation under oxidation and heat conditions. This indicates that the drug is susceptible to oxidation and heat. Statistical analysis proves that the method is repeatable, selective, and accurate for the estimation of said drug. Stability indicating of new chemical entities is an important part for the drug development of ambroxol hydrochloride and for its estimation in plasma and other biological fluids; the novel Statistical analysis proves that the method is repeatable and selective for the analysis of ambroxol hydrochloride as bulk drug and in pharmaceutical formulations. The proposed developed HPTLC method can be applied for identification and quantitative determination of ambroxol hydrochloride in bulk drug and dosage forms. This work is to determine the purity of the drug available from the various sources by detecting

  1. 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.

  2. High Performace Liquid Chromtographic Determination of Nicardipine Hydrochloride in Human Plasma

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    Y. S. R. Krishnaiah

    2004-01-01

    Full Text Available A sensitive high-performance liquid chromatographic method was developed for the estimation of nicardipine hydrochloride in human plasma. Varying amount of nicardipine hydrochloride (2.5 to 150 ng/0.5 mL and fixed quantity (100 ng/0.5 mL of nifedipine (internal standard was added to blank human plasma, and a single step extraction was carried out with ethyl acetate. The mixture was centrifuged, ethyl acetate layer separated, dried and reconstituted with 100 μL of acetonitrile. Twenty microliters of this solution was injected into a reverse phase C-18 column using a mobile phase consisting of acetonitrile: 0.02 M potassium dihydrogen phosphate (pH 4.0 in the ratio of 60:40 v/v and the eluents were monitored at 239 nm. The method was validated for its linearity, precision and accuracy. The calibration curve was linear in the range of 5-150 ng/0.5 mL of plasma and the lower detection limit was 2.5 ng/0.5 mL of plasma. The intra- and inter-day variation was found to be less than 2.5% indicating that the method is highly precise. The mean recovery of nicardipine hydrochloride from plasma samples was 89.6±2.60%. The proposed HPLC method was applied for the estimation of nicardipine hydrochloride in human plasma after oral administration of an immediate release nicardipine hydrochloride capsule (dose 30 mg to 6 adult male volunteers. There was no interference of either the drug metabolites or other plasma components with the proposed HPLC method for the estimation of nicardipine hydrochloride in human plasma. Due to its simplicity, sensitivity, high precision and accuracy, the proposed HPLC method may be used for biopharmaceutical and pharmacokinetic evaluation of nicardipine hydrochloride and its formulations in humans

  3. Human serum paraoxonase-1 (hPON1): in vitro inhibition effects of moxifloxacin hydrochloride, levofloxacin hemihidrate, cefepime hydrochloride, cefotaxime sodium and ceftizoxime sodium.

    Science.gov (United States)

    Türkeş, Cüneyt; Söyüt, Hakan; Beydemir, Şükrü

    2015-01-01

    In this study, we investigated the effects of antibacterial drugs (moxifloxacin hydrochloride, levofloxacin hemihidrate, cefepime hydrochloride, cefotaxime sodium and ceftizoxime sodium) on human serum paraoxonase-1 (hPON1) enzyme activity from human serum in vitro conditions. For this purpose, hPON1 enzyme was purified from human serum using simple chromatographic methods. The antibacterial drugs exhibited inhibitory effects on hPON1 at low concentrations. Ki constants were calculated to be 2.641 ± 0.040 mM, 5.525 ± 0.817 mM, 35.092 ± 1.093 mM, 252.762 ± 5.749 mM and 499.244 ± 10.149 mM, respectively. The inhibition mechanism of moxifloxacin hydrochloride was competitive, whereas levofloxacin hemihidrate, cefepime hydrochloride, cefotaxime sodium and ceftizoxime sodium were noncompetitive inhibitors.

  4. 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、

  5. One-electron oxidation of mitomycin C and its corresponding peroxyl radicals. A steady-state and pulse radiolysis study

    Science.gov (United States)

    Getoff, Nikola; Solar, Sonja; Quint, Ruth M.

    1997-12-01

    The one-electron oxidation of Mitomycin C (MMC) as well as the formation of the corresponding peroxyl radicals were investigated by both steady-state and pulse radiolysis. The steady-state MMC-radiolysis by OH-attack followed at both absorption bands showed different yields: at 218 nm G i (-MMC) = 3.0 and at 364 nm G i (-MMC) = 3.9, indicating the formation of various not yet identified products, among which ammonia was determined, G(NH 3) = 0.81. By means of pulse radiolysis it was established a total κ (OH + MMC) = (5.8 ± 0.2) × 10 9 dm 3 mol -1 s -1. The transient absorption spectrum from the one-electron oxidized MMC showed absorption maxima at 295 nm ( ɛ = 9950 dm 3 mol -1 cm t-1 ), 410 nm ( ɛ = 1450 dm 3 mol -1 cm -1) and 505 nm ( ɛ = 5420 dm 3 mol -1 cm -1). At 280-320 and 505 nm and above they exhibit in the first 150 μs a first order decay, κ1 = (0.85 ± 0.1) × 10 3 s -1, and followed upto ms time range, by a second order decay, 2 κ = (1.3 ± 0.3) × 10 8 dm 3 mol -1 s -1. Around 410 nm the kinetics are rather mixed and could not be resolved. The steady-state MMC-radiolysis in the presence of oxygen featured a proportionality towards the absorbed dose for both MMC-absorption bands, resulting in a G i (-MMC) = 1.5. Among several products ammonia-yield was determined G(NH 3) = 0.52. The formation of MMC-peroxyl radicals was studied by pulse radiolysis, likewise in neutral aqueous solution, but saturated with a gas mixture of 80% N 2O and 20% O 2. The maxima of the observed transient spectrum are slightly shifted compared to that of the one-electron oxidized MMC-species, namely: 290 nm ( ɛ = 10100 dm 3 mol -1 cm -1), 410 nm ( ɛ = 2900 dm 3 mol -1 cm -1) and 520 nm ( ɛ = 5500 dm 3 mol -1 cm -1). The O 2-addition to the MMC-one-electron oxidized transients was found to be at 290 to 410 nm gk(MMC·OH + O 2) = 5 × 10 7 dm 3 mol -1 s -1, around 480 nm κ = 1.6 × 10 8 dm 3 mol -1 s -1 and at 510 nm and above, κ = 3 × 10 8 dm 3 mol -1 s -1. The

  6. Application of mitomycin C in dacryocystorhinostomy%絲裂霉素C在泪囊鼻腔吻合術中的應用

    Institute of Scientific and Technical Information of China (English)

    李自立; 馬雅玲

    2002-01-01

    目的探討絲裂霉素C(mitomycin C,MMC)在泪囊鼻腔吻合術中的作用效果.方法封31例36眼慢性泪囊炎行泪囊腔吻合術,術中一次性使用0.4g/L的MMC.結果術後随訪3~31個月,治愈率爲97.2%,吻合口開通率爲100%.結論MMC可作爲治疗慢性泪囊炎的一種安全、簡單、有效的輔助藥物,明顯提高了手術成功率.

  7. N-hydroxyurea, mitomycin C and actinomycin D activity in the process of tumour formation on the primary leaves of the 'Pinto' bean

    Directory of Open Access Journals (Sweden)

    Aldona Rennert

    2014-01-01

    Full Text Available Mitomycin C (MC, N-hydroxyurea (HU and actinomycin D (AD inhibit tumour formation on the primary leaves of Pinto beans. Agrobacterium tumefaciens was inoculated into bean leaves with application of the above named inhibitors at various times. It was found that MC action is strongest during inoculation and immediately after it, the maximal effect of HU take place within 12 h after inoculation, whereas the antitumour action of AD starts as late as 12 h after leaf inoculation. In view of the different degree of susceptibility of bacteria and plant cells to the inhibitors applied, the above described results allowed to distinguish three critical periods in the process of tumour formation in the tested host-pathogen system.

  8. Estudio comparativo del uso de mitomicina C en el pterigium recidivante Comparative study of the use of mitomycin C in recurrent pterygium

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    Belmary Aragonés Cruz

    2008-12-01

    Full Text Available INTRODUCCIÓN: El pterigium constituye un problema en la práctica oftalmológica por su alta prevalencia y elevada frecuencia de recidiva. El propósito de este estudio fue el de comparar la técnica quirúrgica de injerto autólogo de conjuntiva con células límbicas más mitomicina C, con la de injerto de membrana amniótica con mitomicina C, en pterigium recidivante, en cuanto a la tasa de recidiva, complicaciones posoperatorias inmediatas, y tiempo libre de recidiva (meses. MÉTODOS: Se realizó un ensayo clínico controlado prospectivo con n= 57 pacientes portadores de pterigium recidivante. Se conformaron 2 grupos: grupo 1, injerto de conjuntiva antólogo con células límbicas más mitomicina C; y el grupo 2, injerto de membrana amniótica más mitomicina C. Se comparó el comportamiento de las técnicas empleadas a partir de sus resultados. El seguimiento fue ± de 1-6 meses. RESULTADOS: La agudeza visual mejoró en 60 % de los casos. La recidiva fue de 2 % para el grupo 1 y de 6 % para el grupo 2. CONCLUSIONES: El método de injerto conjuntival con limbo resultó más efectivo para el tratamiento del pterigium recidivante. Él método de membrana amniótica constituye una alternativa para el tratamiento de casos en los cuales no sea viable la aplicación de de injerto antólogo.INTRODUCTION: Pterygium is a problem in ophthalmology practice because of its high prevalence and frequency of recurrence. The objectives of this study was to compare the surgical technique of autologous conjuctival graft with limbal cells plus mitomycin C with that of amniotic membrane graft treated with mitomycin C in recurrent pterygium in terms of recurrence rates, immediate postoperative complications and recurrence-free time (months. METHODS: A prospective controlled clinical assay was carried out in 57 patients suffering recurrent pterygium. They were divided into two groups; the group 1 that had autologous conjuctival graft with limbal cells plus

  9. Cinchocaine hydrochloride determination by atomic absorption spectrometry and spectrophotometry.

    Science.gov (United States)

    Abdel-Ghani, Nour T; Youssef, Ahmed F A; Awady, Mohamed A

    2005-05-01

    Two sensitive spectrophotometric and atomic absorption spectrometric procedures have been developed for determination of cinchocaine hydrochloride (Cin.Cl) in pure form and in pharmaceutical formulation. The spectrophotometric method was based on formation of an insoluble colored ion-associate between the cited drug and tetrathiocyanatocobaltate (CoTC) or hexathiocyanatochromate (CrTC) which dissolved and extracted in an organic solvent. The optimal experimental conditions for quantitative extraction such as pH, concentration of the reagents and solvent were studied. Toluene and iso-butyl alcohol proved to be the most suitable solvents for quantitative extraction of Cin-CoTC and Cin-CrTC ion-associates with maximum absorbance at 620 and 555 nm, respectively. The optimum concentration ranges, molar absorptivities, Ringbom ranges and Sandell sensitivities were also evaluated. The atomic absorption spectrometric method is based on measuring of the excess cobalt or chromium in the aqueous solution, after precipitation of the drug, at 240.7 and 357.9 nm, respectively. Linear application ranges, characteristic masses and detection limits were 57.99-361.9, 50.40 and 4.22 microg ml(-1) of Cin.Cl, in case of CoTC, while 37.99-379.9, 18.94 and 0.81 microg ml(-1) in case of CrTC.

  10. 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.

  11. 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.

  12. Prednisone and vardenafil hydrochloride for refractory levamisole-induced vasculitis.

    Science.gov (United States)

    Mandrell, Joshua; Kranc, Christina L

    2016-08-01

    Levamisole is an immunomodulatory drug that was previously used to treat various medical conditions, including parasitic infections, nephrotic syndrome, and colorectal cancer. Over the last few years, increasing amounts of levamisole have been used as an adulterant in cocaine. Levamisole-cut cocaine has become a concern because it is known to cause a necrotizing purpuric rash, autoantibody production, and life-threatening leukopenia. Mixed histologic findings of vasculitis and thrombosis are characteristic of levamisole-induced purpura. The recommended management of levamisole-induced vasculitis currently involves withdrawal of the culprit along with supportive treatment. We describe a patient with levamisole-induced vasculitis who continued to develop skin lesions despite self-reported cocaine cessation. Complete resolution of cutaneous disease occurred with the addition of oral prednisone and vardenafil hydrochloride, suggesting the possibility of a new treatment option in patients with refractory disease. In addition, we review the clinical presentation, disease course, diagnostic approach, laboratory findings, histology, and management of levamisole-induced vasculitis. The harmful effects of levamisole-cut cocaine are serious enough that public alerts have been issued to increase awareness. Clinicians should consider the possibility of levamisole exposure in cocaine users presenting with any combination of fever, neutropenia, and necrotic skin lesions, especially in acral areas including the ears.

  13. Conformation and interactions of dopamine hydrochloride in solution

    Energy Technology Data Exchange (ETDEWEB)

    Callear, Samantha K.; Imberti, Silvia [ISIS Facility, STFC Rutherford Appleton Laboratory, Harwell Oxford, Didcot OX11 0QX (United Kingdom); Johnston, Andrew; McLain, Sylvia E. [Biochemistry Department, University of Oxford, South Parks Road, Oxford OX1 3QU (United Kingdom)

    2015-01-07

    The aqueous solution of dopamine hydrochloride has been investigated using neutron and X-ray total scattering data together with Monte-Carlo based modelling using Empirical Potential Structure Refinement. The conformation of the protonated dopamine molecule is presented and the results compared to the conformations found in crystal structures, dopamine-complexed protein crystal structures and predicted from theoretical calculations and pharmacophoric models. It is found that protonated dopamine adopts a range of conformations in solution, highlighting the low rotational energy barrier between different conformations, with the preferred conformation being trans-perpendicular. The interactions between each of the species present (protonated dopamine molecules, water molecules, and chloride anions) have been determined and are discussed with reference to interactions observed in similar systems both in the liquid and crystalline state, and predicted from theoretical calculations. The expected strong hydrogen bonds between the strong hydrogen bond donors and acceptors are observed, together with evidence of weaker CH hydrogen bonds and π interactions also playing a significant role in determining the arrangement of adjacent molecules.

  14. FORMULATION AND EVALUATION OF EXTENDED RELEASE TABLETS OF TRAMADOL HYDROCHLORIDE

    Directory of Open Access Journals (Sweden)

    Chilvalvar Sapnil

    2013-10-01

    Full Text Available The objective of this research work was to develop extended release tablets (Twice in a day of Tramadol Hydrochloride using different Hydrophilic polymers like HPMC K15M, HPMC K4M, Metalose 60SH50, Carbopol 971P, Sodium alginate, Xanthan gum by direct compression method. Various amounts of polymers was used in the twenty four proposed formulations (F1 to F24 for the study of release rate retardant effect at 10 %, 15 %, 20 %, 25 % of total weight of tablet matrix respectively. Then the tablets were evaluated in terms of their physical parameters (weight variation, hardness, friability and thickness, drug content and in-vitro release studies. All the formulations showed compliance with pharmacopoeial standards. The in-vitro dissolution study were conducted using USP dissolution apparatus type-II (paddle method in 900 ml 0.1 N HCl for first 2 h and remaining 10 h performed in 6.8 pH phosphate buffer at 100 rpm for a total period of 12 h. Based on the dissolution data comparison with innovator product, formulation F14 was found as the best formulation. The drug release of formulation F14 followed First Order kinetic model and the mechanism was found to be non-Fickian/anomalous according to Korsmeyer-Peppas equation.

  15. FORMULATION DEVELOPMENT OF ISOXSUPRINE HYDROCHLORIDE MODIFIED RELEASE MATRIX TABLETS

    Directory of Open Access Journals (Sweden)

    Ketan Patel

    2012-01-01

    Full Text Available The objective of the present investigation was to study the effect of critical formulation parameters affecting release of isoxsuprine hydrochloride from matrix tablets using combination of polyethylene oxide (PEO and dicalcium phosphate (DCP. The powder blend consisting of drug and excipients was analyzed for angle of repose, Carr’s index and Hausner’s ratio. The tablets were prepared by direct compression method. To assess the compressional behavior of the drug-excipient blend, the tablets were analyzed for friability and crushing strength. The in vitro drug release study was carried out in distilled water. The powder blend exhibited satisfactorily flow as measured by angle of repose, Carr’s index and Hausner’s ratio. The formulation ingredients showed satisfactory tableting properties (friability <1%, crushing strength ≥ 4 kgf. The drug release was modified on addition of PEO and DCP. Addition of 5 to 25% DCP in the formulation of matrix tablets caused apparent difference in the drug dissolution in distilled water. However, the difference was insignificant as analyzed by analysis of variance (ANOVA and similarity factor ( f2. The drug release from the tablets was best explained by Weibull model. Unified Weibull model was evolved to predict drug release from the formulated batches. The findings of this investigation can be extended to industry to cut down the cost of formulation and to by-pass the existing patents employing hydrophilic matrixing agents, at least for selective drugs.

  16. Solvent screening and crystal habit of metformin hydrochloride

    Science.gov (United States)

    Benmessaoud, Ibtissem; Koutchoukali, Ouahiba; Bouhelassa, Mohamed; Nouar, Abderrahim; Veesler, Stéphane

    2016-10-01

    A multi-well setup with video-microscopy was used to study the influence of solvent on solubility, nucleation, and crystallization of an Active Pharmaceutical Ingredient (API): metformin hydrochloride (MET.HCl). Starting with 13 solvents covering a wide variety of polarity and proticity, we found 63 crystallization medium for MET.HCl solid generation: good solvents, good co-solvents and anti-solvent systems. For toxicological reasons, we limited the number of crystallization medium to 18: 3 good solvents (class 3), 3 good co-solvent systems and 12 anti-solvent systems. In order to study the influence of crystallization medium on nucleation temperature, crystal habit and polymorphism of MET.HCl, crystallization was studied by a cooling temperature method. Different crystal habits were observed by optical and scanning electron microscopies, and solid phase were characterized by X-ray powder diffraction, indicating that all the crystals correspond to the thermodynamic stable polymorphic form A of MET.HCl. Finally, the enthalpy of fusion and the melting temperature of MET.HCl were determined by DSC and confirmed the X-ray powder diffraction results.

  17. Facile colorimetric methods for the quantitative determination of tetramisole hydrochloride

    Science.gov (United States)

    Amin, A. S.; Dessouki, H. A.

    2002-10-01

    A facile, rapid and sensitive methods for the determination of tetramisole hydrochloride in pure and in dosage forms are described. The procedures are based on the formation of coloured products with the chromogenic reagents alizarin blue BB (I), alizarin red S (II), alizarin violet 3R (III) and alizarin yellow G (IV). The coloured products showed absorption maxima at 605, 468, 631 and 388 nm for I-IV, respectively. The colours obtained were stable for 24 h. The colour system obeyed Beer's law in the concentration range 1.0-36, 0.8-32, 1.2-42 and 0.8-30 μg ml -1, respectively. The results obtained showed good recoveries with relative standard deviations of 1.27, 0.96, 1.13 and 1.35%, respectively. The detection and determination limits were found to be 1.0 and 3.8, 1.2 and 4.2, 1.0 and 3.9 and finally 1.4 and 4.8 ng ml -1 for I-IV complexes, respectively. Applications of the method to representative pharmaceutical formulations are represented and the validity assessed by applying the standard addition technique, which is comparable with that obtained using the official method.

  18. Trans-ungual delivery of itraconazole hydrochloride by iontophoresis.

    Science.gov (United States)

    Kushwaha, Avadhesh; Jacob, Melissa; Shiva Kumar, H N; Hiremath, Shobharani; Aradhya, Sacchidanand; Repka, Michael A; Murthy, S Narasimha

    2015-01-01

    Itraconazole (ITR) is a potent antifungal drug. However, poor aqueous solubility limits its permeation ability across the human nail plate. Therefore, in this project, ITR was converted to hydrochloride salt (ITR-HCl) to improve its solubility and to render it amenable to iontophoresis. ITR-HCl was characterized by spectroscopic methods and antifungal efficacy was evaluated in comparison to the base. In vitro and ex vivo transport studies (passive and iontophoresis) were carried out across the porcine hoof membrane and excised human cadaver toe using two different protocols; continuous delivery of drug for 24 h and pulsed delivery of drug for 3 days (8 h/day). The antifungal efficacy of ITR-HCL was comparable to ITR. Iontophoresis was found to be more effective than passive mode of delivery of ITR-HCL. In both iontophoresis as well as passive mode of delivery, the pulsed protocol resulted in more ungual and trans-ungual delivery of drug than continuous protocol. ITR-HCL could be delivered into and across the nail plate by iontophoresis. Human cadaver toe appears to be a good model to investigate the ungual delivery of drugs.

  19. [POLYHEXAMETHYLENE BIGUANID HYDROCHLORIDE (BIGUANELLE) THERAPY OF BACTERIAL VAGINOSIS].

    Science.gov (United States)

    Kovachev, S; Ganovska, A; Sultanov, E; Ivanova, S; Gizdov, N; Nikolova, L; Iliev, V

    2016-01-01

    The aim of our study was to determine the efficacy and tolerability of local therapy with polyhexamethylene biguanid hydrochloride (BIGUANELLE) in women with anaerobic vaginal infection. We include in our study 23 women (18-50) with established by AMSEL criteria bacterial vaginosis. In all of the women at the beginning and at the end of the survey was performed gynecological examination and microbiological research (AMSEL). The therapeutic scheme at all women is with a single vaginal application of gynecological solution BIGUANELLE. Effectiveness of the treatment was evaluated according to clinical complaints and microbiological research (Amsel criteria: Ph 4.5 >; KOH (+); "clue cells"; specific vaginal fluorine). Tolerability of patients to treatment was assessed by questionnaire. Clinical complaints of patients after the therapy decreased as follows: vaginal fluorine with 73.9%; odor--75%; pruritus--50%; discomfort--90%. Microbiological research and their evaluation by AMSEL, showed the therapeutic efficacy of the therapy in 16 (69.6%) of all (n-23) patients. At 7 (30.4%) women, the treatment remained without effect. At questionnaire answers, 73.9% patients were satisfied with the application of BIGUANELLE, 95.6% of them have implemented it easily, 95.6% of women believe that BIGUANELLE is more convenient to use in comparison with similar products which have a daily application, and none of the patients (100%) have any complaints in applying this gynecological solution. BIGUANELLE showed good clinical efficacy in the treatment of bacterial vaginosis. It is easily applied and well tolerated by the patients.

  20. 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.

  1. 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.

  2. Cisplatin, tegafur-uracil and leucovorin plus mitomycin C: an acceptably effective and toxic regimen for patients with recurrent or metastatic nasopharyngeal carcinoma

    Directory of Open Access Journals (Sweden)

    Chia-Hsun Hsieh

    2013-10-01

    Full Text Available Background: This prospective phase II clinical trial evaluated the efficacy and toxicity of cisplatin, oral tegafur-uracil, leucovorin, and mitomycin C in patients with recurrent or metastatic nasopharyngeal carcinoma. Methods: Patients with histologically proven non-keratinizing or undifferentiated nasopharyngeal carcinoma were prospectively enrolled from April 2002 to June 2005. Cisplatin 50 mg/m 2 on day 1, 22 and mitomycin C 6 mg/m 2 on day 1 were administered. Oral tegafur-uracil 300 mg/m 2 /day and oral leucovorin 60 mg/day were given on day 1-14 and day 22-35, respectively. Each cycle was repeated every 6 weeks. Primary and secondary endpoints are response rate and toxic profiles with survivals, respectively. Results: Twenty-two patients with the median age of 47 (35-69 years were enrolled in the study. Sixteen (72.7% patients had undifferentiated nasopharyngeal carcinoma. The regimen was well-tolerated by all patients with the exception of one patient (4.6% who experienced grade IV anorexia, and two patients (9.1% who had grade IV vomiting. There was no treatment-related death. The overall response rate was 59.1%, including 3 (13.6% complete remissions. The median duration of response was 15.9 months, the median time to tumor progression was 10.0 months, and the median overall survival was 16.0 months. Conclusion: This outpatient chemotherapy regimen is acceptably effective and toxic among patients with recurrent or metastatic nasopharyngeal carcinoma.

  3. Enhanced sensitivity to mitomycin C by abating heat shock protein 70 expression in human bladder cancer cell line of BIU-87

    Institute of Scientific and Technical Information of China (English)

    HE Ling-feng; GUAN Kao-peng; YAN Zheng; YE Hai-yun; XU Ke-xin; REN Liang; HOU Shu-kun

    2005-01-01

    Background Bladder cancer is a relatively common tumor in the urinary system, in which mitomycin C (MMC)-based chemotherapy or combination chemotherapy has been mainly used to treat patients with advanced bladder cancer. The prognosis of patients with advanced bladder cancer is still extremely poor in spite of recent therapeutic advances. To improve the prognosis, the sensitivity of tumor cells to mitomycin C by the induction of apoptosis with the abating heat shock protein 70 (HSP70) expression in human bladder cancer cell lines of BIU-87 was investigated. Methods HSP70 expression was abated in BIU-87 cells by HSP mRNA antisense oligomers. MTT assay and the clone-forming test were used for evaluating the sensitivity of cells to MMC. Apoptosis was assessed using both fluorescent microscopy after staining the cells with Hoechst 33258 and DNA fragment ladder agarose electrophoresis. Thirty-two male six-week-old BALB/c nude mice, at the beginning of the experiment, were used to evaluate the effect of antisense oligomers (ASO) on the tumor formation in vivo. Results HSP70 expression in BIU-87 was effectively abated by HSP70 mRNA antisense oligomers. The percentage of apoptotic cells in ASO group was greater than in sense oligomers (SO) [P50%) was more than that of ASO or MMC group alone (all P<0.05). Conclusions The abating level of HSP70 expression can strengthen the sensitivity of BIU-87 to MMC. One of this effect might be related to the induction of apoptosis by abating HSP70 expression.

  4. 丝裂霉素C眼用凝胶的制备及质量控制%Preparation and Quality Control of Mitomycin C Ophthalmic Gel

    Institute of Scientific and Technical Information of China (English)

    毕宏生; 苏卫华; 郭俊国; 刘大美; 吴建峰

    2011-01-01

    制备丝裂霉素C眼用凝胶剂并建立其质量控制方法.以丝裂霉素为主药,以卡波姆和羧甲基纤维素( HPMC K4M)为基质制备眼用凝胶,采用HPLC法测定制剂中丝裂霉素C的含量.所制得的眼用凝胶为淡紫色透明状,丝裂霉素C在21 - 210μg/ml范围内呈良好的线性关系,A=0.482C+ 0.009,精密度RSD为0.049%,稳定性RSD为1.28%.该法制备工艺简单,质量可控,有关项目符合眼用凝胶的质量要求.%To prepare mitomycin C ophthalmic gel and the establishment of its quality control methods. Eyegel was prepared based on mitiomycin medicine and taking Carbomer and carboxymethyl cellulose (HPMC K4M) as a substrate. Mitonycin c content was determinated wing HPLC. The obtained eye gel is transparent lavender, within the scope of mitomycin C in 21 ~ 210μg/ml good linear relationship, A = 0.482C + 0.009, precision RSD of 0.049%, stable of the RSD is 1.28%.Hie preparation process is simple, quality control, the project meets the quality requirements of the eye gel.

  5. Prospective randomized trial comparing mitomycin, cisplatin, and protracted venous-infusion fluorouracil (PVI 5-FU) With epirubicin, cisplatin, and PVI 5-FU in advanced esophagogastric cancer.

    Science.gov (United States)

    Ross, P; Nicolson, M; Cunningham, D; Valle, J; Seymour, M; Harper, P; Price, T; Anderson, H; Iveson, T; Hickish, T; Lofts, F; Norman, A

    2002-04-15

    We report the results of a prospectively randomized study that compared the combination of epirubicin, cisplatin, and protracted venous-infusion fluorouracil (PVI 5-FU) (ECF) with the combination of mitomycin, cisplatin, and PVI 5-FU (MCF) in previously untreated patients with advanced esophagogastric cancer. Five hundred eighty patients with adenocarcinoma, squamous carcinoma, or undifferentiated carcinoma were randomized to receive either ECF (epirubicin 50 mg/m(2) every 3 weeks, cisplatin 60 mg/m(2) every 3 weeks and PVI 5-FU 200 mg/m(2)/d) or MCF (mitomycin 7 mg/m(2) every 6 weeks, cisplatin 60 mg/m(2) every 3 weeks, and PVI 5-FU 300 mg/m(2)/d) and analyzed for survival, response, toxicity, and quality of life (QOL). The overall response rate was 42.4% (95% confidence interval [CI], 37% to 48%) with ECF and 44.1% (95% CI, 38% to 50%) with MCF (P =.692). Toxicity was tolerable, and there were only two toxic deaths. ECF resulted in more grade 3/4 neutropenia and grade 2 alopecia, but MCF caused more thrombocytopenia and plantar-palmar erythema. Median survival was 9.4 months with ECF and 8.7 months with MCF (P =.315); at 1 year, 40.2% (95% CI, 34% to 46%) of ECF and 32.7% (95% CI, 27% to 38%) of MCF patients were alive. Median failure-free survival was 7 months with both regimens. Global QOL scores were better with ECF at 3 and 6 months. This study confirms response, survival, and QOL benefits of ECF observed in a previous randomized study. The equivalent efficacy of MCF was demonstrated, but QOL was superior with ECF. ECF remains one of the reference treatments for advanced esophagogastric cancer.

  6. 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.

  7. RP-HPLC estimation of venlafaxine hydrochloride in tablet dosage forms

    Directory of Open Access Journals (Sweden)

    Baldania S

    2008-01-01

    Full Text Available A simple, specific, accurate, and precise reverse phase high performance liquid chromatographic method was developed and validated for the estimation of venlafaxine hydrochloride in tablet dosage forms. A Phenomenex Gemini C-18, 5 µm column having 250 x 4.6 mm i.d. in isocratic mode, with mobile phase containing methanol: 0.05 M potassium dihydrogen orthophosphate (70:30, v/v; pH 6.2 was used. The flow rate was 1.0 ml/min and effluents were monitored at 226 nm. Carbamazepine was used as an internal standard. The retention time of venlafaxine hydrochloride and carbamazepine were 3.7 min and 5.3 min, respectively. The method was validated for specificity, linearity, accuracy, precision, limit of quantification, limit of detection, robustness and solution stability. Limit of detection and limit of quantification for estimation of venlafaxine hydrochloride were found to be 100 ng/ml and 300 ng/ml, respectively. Recoveries of venlafaxine hydrochloride in tablet formulations were found to be in the range of 99.02-101.68%. Proposed method was successfully applied for the quantitative determination of venlafaxine hydrochloride in tablet dosage forms.

  8. FORMULATION AND EVALUATION OF S-(--AMLODIPINE BESYLATE AND NEBIVOLOL HYDROCHLORIDE TABLETS

    Directory of Open Access Journals (Sweden)

    Shaikh S.A

    2010-06-01

    Full Text Available The objective of the present study was to develop a tablet formulation of S-(-- amlodipine besylate chiral separation drug and nebivolol hydrochloride for better management of hypertension, while reducing or avoiding undesirable adverse effects, which are often associated with administration of a racemic mixture of amlodipine. The composition containing the optically pure S-(-- isomer of amlodipine 2.5 mg has calcium channel blocking activity and, nebivolol hydrochloride 5 mg has beta-receptor blocking activity.The study was also carried out to design a suitable dissolution medium for S-(- - amlodipine besylate and nebivolol hydrochloride. Amlodipine besylate and nebivolol hydrochloride had maximum solubility in pH 1.2 and thus pH 1.2 was selected as the most suitable media for S-(- - amlodipine besylate and nebivolol hydrochloride dissolution studies. The RSD below 2% indicated insignificant batch-to-batch variation. The accelerated stability study of the optimized formulation was performed as the ICH guidelines. The results indicated no change in optical rotation of S-(- - amlodipine besylate. Hence, combination of two drugs can be formulated into the tablet by wet granulation technique having satisfactory release profile.

  9. Design and development of polyethylene oxide based matrix tablets for verapamil hydrochloride

    Directory of Open Access Journals (Sweden)

    S Vidyadhara

    2013-01-01

    Full Text Available In the present investigation an attempt has been made to increase therapeutic efficacy, reduced frequency of administration and improved patient compliance by developing controlled release matrix tablets of verapamil hydrochloride. Verapamil hydrochloride was formulated as oral controlled release matrix tablets by using the polyethylene oxides (Polyox WSR 303. The aim of this study was to investigate the influence of polymer level and type of fillers namely lactose (soluble filler, swellable filler (starch 1500, microcrystalline cellulose and dibasic calcium phosphate (insoluble fillers on the release rate and mechanism of release for verapamil hydrochloride from matrix tablets prepared by direct compression process. Higher polymeric content in the matrix decreased the release rate of drug. On the other hand, replacement of lactose with anhydrous dibasic calcium phosphate and microcrystalline cellulose has significantly retarded the release rate of verapamil hydrochloride. Biopharmaceutical evaluation of satisfactory formulations were also carried out on New Zealand rabbits and parameters such as maximum plasma concentration, time to reach peak plasma concentration, area under the plasma concentration time curve (0-t and area under first moment curve (0-t were determined. In vivo pharmacokinetic study proves that the verapamil hydrochloride from matrix tablets showed prolonged release and were be able to sustain the therapeutic effect up to 24 h.

  10. Application of near-infrared reflectance spectrometry to the analytical control of pharmaceuticals: ranitidine hydrochloride tablet production.

    Science.gov (United States)

    Dreassi, E; Ceramelli, G; Corti, P; Perruccio, P L; Lonardi, S

    1996-02-01

    The possibility of applying near-infrared reflectance spectrometry to the control of the production cycle of ranitidine hydrochloride tablets was investigated. The results were good for the identification of ranitidine hydrochloride drug substance, mixtures for tablets, cores and coated tablets. The determination of the compound and of its water content also gave satisfactory results.

  11. 75 FR 31790 - Determination That Cysteine Hydrochloride Injection, USP, 7.25%, Was Not Withdrawn From Sale for...

    Science.gov (United States)

    2010-06-04

    ... HUMAN SERVICES Food and Drug Administration Determination That Cysteine Hydrochloride Injection, USP, 7... determination that Cysteine Hydrochloride Injection, USP, 7.25% (Cysteine HCl), was not withdrawn from sale for... applications (ANDAs) for Cysteine HCl if all other legal and regulatory requirements are met. FOR...

  12. 40 CFR Appendix A to Subpart Ddd... - Free Formaldehyde Analysis of Insulation Resins by the Hydroxylamine Hydrochloride Method

    Science.gov (United States)

    2010-07-01

    ... Insulation Resins by the Hydroxylamine Hydrochloride Method A Appendix A to Subpart DDD of Part 63 Protection... Part 63—Free Formaldehyde Analysis of Insulation Resins by the Hydroxylamine Hydrochloride Method 1. Scope The method in this appendix was specifically developed for water-soluble phenolic resins that...

  13. Biowaiver monographs for immediate release solid oral dosage forms: amitriptyline hydrochloride.

    Science.gov (United States)

    Manzo, R H; Olivera, M E; Amidon, G L; Shah, V P; Dressman, J B; Barends, D M

    2006-05-01

    Literature data relevant to the decision to allow a waiver of in vivo bioequivalence (BE) testing for the approval of immediate release (IR) solid oral dosage forms containing amitriptyline hydrochloride are reviewed. Its therapeutic uses, its pharmacokinetic properties, the possibility of excipient interactions and reported BE/bioavailability (BA) problems are also taken into consideration. Literature data indicates that amitriptyline hydrochloride is a highly permeable active pharmaceutical ingredient (API). Data on the solubility according to the current Biopharmaceutics Classification System (BCS) were not fully available and consequently amitriptyline hydrochloride could not be definitively assigned to either BCS Class I or BCS Class II. But all evidence taken together, a biowaiver can currently be recommended provided that IR tablets are formulated with excipients used in existing approved products and that the dissolution meets the criteria defined in the Guidances.

  14. 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

  15. Synthesis, spectral, and anti-microbial studies of thioiminium iodides and amine hydrochlorides.

    Science.gov (United States)

    Britto, Sebastian; Renaud, Philippe; Nallu, Maruthai

    2014-01-01

    To avoid the undesired deprotonation during the addition of organolithium and organomagnesium reagents to ketones, the thioiminium salts, easily prepared from lactams and amides are converted into 2,2-disubstituted and 2-monosubstituted amines by reaction with simple nucleophiles such as organocerium and organocopper reagents. The reaction of thioiminium iodides with organocerium reagents derived by transmetalation of corresponding lithium reagents with anhydrous cerium(III) chloride has been investigated. These thioiminium iodides act as good electrophiles and accept alkylceriums towards bisaddition. The newly synthesized amines have been characterized by 1H and 13C NMR, IR and mass spectra. The amines have been converted into their hydrochlorides and characterized by COSY. These hydrochlorides have been subjected to antimicrobial screening with clinically isolated microorganisms, Staphylococcus aureus, Klebsiella pneumoniae, Pseudomonas aeruginosa, Salmonella typhi and Candida albicans. The hydrochlorides show quite good activity against these bacteria and fungus. Copyright © 2013 Elsevier B.V. All rights reserved.

  16. The effects of clomipramine hydrochloride in cats with psychogenic alopecia: a prospective study.

    Science.gov (United States)

    Mertens, Petra A; Torres, Sheila; Jessen, Carl

    2006-01-01

    A double-blind, placebo-controlled clinical trial was conducted to determine the efficacy of clomipramine hydrochloride in cats with psychogenic alopecia. Twenty-five cats were randomly assigned to receive clomipramine hydrochloride (0.5 mg/kg orally q 24 hours) or placebo for 56 days. Eleven cats in each group completed the trial. The results of this study showed that clomipramine hydrochloride failed to demonstrate significant changes in the number of grooming bouts, hair regrowth, and the area of alopecia in cats with psychogenic alopecia when compared to a placebo. It was uncertain whether these results reflected a lack of drug efficacy, insufficient treatment duration, or an insufficient number of cases enrolled.

  17. Protective effects of glucosamine hydrochloride against free radical-induced erythrocytes damage.

    Science.gov (United States)

    Jamialahmadi, Khadijeh; Arasteh, Omid; Matbou Riahi, Maryam; Mehri, Soghra; Riahi-Zanjani, Bamdad; Karimi, Gholamreza

    2014-07-01

    Glucosamine (GlcN) is an important precursor in the biochemical synthesis of glycosylated proteins and lipids in human body. It gains importance because of its contribution to human health and its multiple biological and therapeutic effects. In this study, the in vitro oxidative hemolysis of rat erythrocyte was used as a model to study the potential protective effect of glucosamine hydrochloride against free radical-induced damage of biological membranes. Glucosamine hydrochloride exhibited dose-dependent DPPH antioxidant activity. Oxidative hemolysis and lipid/protein peroxidation of erythrocytes induced by a water-soluble free radical initiator 2,2'-azobis (2-amidinopropane) dihydrochloride (AAPH) were significantly suppressed by GlcN in a time and dose dependent manner. GlcN also prevented the depletion of cytosolic antioxidant glutathione (GSH) in erythrocytes. These results indicated that glucosamine hydrochloride efficiently protected erythrocytes against free radicals and it could be recommended as a pharmaceutical supplement to alleviate oxidative stress.

  18. Simultaneous determination of salbutamol sulphate and bromhexine hydrochloride in tablets by reverse phase liquid chromatography

    Directory of Open Access Journals (Sweden)

    Pai P. N. S.

    2009-01-01

    Full Text Available A simple reverse phase liquid chromatographic method has been developed and subsequently validated for simultaneous determination of salbutamol sulphate and bromhexine hydrochloride. The separation was carried out using a mobile phase consisting of acetonitrile, methanol and phosphate buffer, pH 4 in the ratio 60:20:20 v/v. The column used was SS Wakosil-II C-18 with a flow rate of 1 ml/min and UV detection at 224 nm. The described method was linear over a concentration range of 10-110 µg/ml and 20-140 µg/ml for the assay of salbutamol sulphate and bromhexine hydrochloride, respectively. The mean recovery was found to be 95-105% for salbutamol sulphate and 96.2-102.1% for bromhexine hydrochloride when determined at five different levels.

  19. Management of attention-deficit hyperactivity disorder in adults: focus on methylphenidate hydrochloride

    Directory of Open Access Journals (Sweden)

    Rajasree Nair

    2009-08-01

    Full Text Available Rajasree Nair, Shannon B MossBaylor Family Medicine Residency at Garland, Garland, Texas, USAAbstract: Attention-deficit hyperactivity disorder (ADHD is one of the most common psychiatric disorders in young adults and causes significant psychosocial impairment and economic burden to society. Because of the paucity of long-term evidence and lack of national guidelines for diagnosis and management of adult ADHD, most of the data are based on experience derived from management of childhood ADHD. This article reviews the current evidence for the diagnosis and management of adult ADHD with special emphasis on the role of methylphenidate hydrochloride preparations in its treatment. Methylphenidate hydrochloride, a stimulant that acts through the dopaminergic and adrenergic pathways, has shown more than 75% efficacy in controlling the symptoms of adult ADHD. Although concern for diversion of the drug exists, recent data have shown benefits in preventing substance use disorders in patients with adult ADHD.Keywords: adult ADHD, treatment, stimulants, methylphenidate hydrochloride

  20. 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%.

  1. 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.

  2. Formulation and evaluation of S-(--Amlodipine besylate and nebivolol hydrochloride tablets

    Directory of Open Access Journals (Sweden)

    S A Shaikh

    2010-01-01

    The study was also carried out to design a suitable dissolution medium for S-(- - amlodipine besylate and nebivolol hydrochloride. Amlodipine besylate and nebivolol hydrochloride had maximum solubility in pH 1.2 and thus pH 1.2 was selected as the most suitable media for S-(- - amlodipine besylate and nebivolol hydrochloride dissolution studies. The RSD below 2% indicated insignificant batch-to-batch variation. The accelerated stability study of the optimized formulation was performed as the ICH guidelines. The results indicated no change in optical rotation of S-(- - amlodipine besylate. Hence, combination of two drugs can be formulated into the tablet by wet granulation technique having satisfactory release profile.

  3. Thermal Analysis Investigation of Dapoxetine and Vardenafil Hydrochlorides using Molecular Orbital Calculations.

    Science.gov (United States)

    Attia, Ali Kamal; Souaya, Eglal R; Soliman, Ethar A

    2015-11-01

    Thermal analysis techniques have been used to study the thermal behavior of dapoxetine and vardenafil hydrochlorides and confirmed using semi-empirical molecular orbital calculations. Thermogravimetric analysis, derivative thermogravimetry, differential thermal analysis and differential scanning calorimetry were used to determine the thermal behavior and purity of the drugs under investigation. Thermodynamic parameters such as activation energy, enthalpy, entropy and Gibbs free energy were calculated. Thermal behavior of DAP and VAR were confirmed using by semi-empirical molecular orbital calculations. The purity values were found to be 99.97% and 99.95% for dapoxetine and vardenafil hydrochlorides, respectively. The purity of dapoxetine and vardenafil hydrochlorides is similar to that found by reported methods according to DSC data. Thermal analysis justifies its application in quality control of pharmaceutical compounds due to its simplicity, sensitivity and low operational costs.

  4. 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

  5. Compatibility of verapamil hydrochloride injection in commonly used large-volume parenterals.

    Science.gov (United States)

    Cutie, M R; Lordi, N G

    1980-05-01

    The visual and chemical compatibilities of verapamil hydrochloride injection in 10 commonly used large-volume solutions packaged in glass, polyolefin, or polyvinyl chloride containers were studied. The mixtures, each containing 40 mg/liter of verapamil hydrochloride, were stored away from light for up to 48 hours at 25 degrees C. The solutions were examined visually for haze, precipitate formation, color change, and evolution of gas immediately after mixing and at 0.25, 1, 3, 8, 24, and 48 hours. Spectrophotometry and thin-layer chromatography were used to test for drug decomposition or chemical incompatibilities. All test methods used showed that no significant degradation of verapamil hydrochloride had taken place in the solutions or through contact with the containers. Slightly higher spectrophotometric readings for dextrose-containing solutions, though within experimental error, could have indicated the presence of dextrose degradation products. Evidence from this study suggests that verapamil hydrocholoride is compatible with the large-volume parenterals studied.

  6. DEVELOPMENT AND VALIDATION OF SPECTROPHOTOMETRIC METHOD FOR SIMULTANEOUS DETERMINATION OF PROPRANOLOL HYDROCHLORIDE AND FLUNARIZINE DIHYDROCHLORIDE IN THEIR COMBINED DOSAGE FORMULATION

    Directory of Open Access Journals (Sweden)

    A.K. Doshi*, B.N. Patel and C.N. Patel

    2012-06-01

    Full Text Available A simple, accurate and precise spectrophotometric method has been developed for simultaneous estimation of Propranolol hydrochloride and Flunarizine dihydrochloride in combined dosage form. Simultaneous equation method is employed for simultaneous determination of Propranolol hydrochloride and Flunarizine dihydrochloride from combined dosage forms. In this method, the absorbance was measured at 289 nm for Propranolol hydrochloride and 253 nm for Flunarizine dihydrochloride. Linearity was observed in range of 24-64 μg/ml and 6-16 μg/ml for Propranolol hydrochloride and Flunarizine dihydrochloride respectively. Recovery studies confirmed the accuracy of proposed method and results were validated as per ICH guidelines. The method can be used for routine quality control of pharmaceutical formulation containing Propranolol hydrochloride and Flunarizine dihydrochloride.

  7. [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.

  8. Safety and efficacy of tramadol hydrochloride on treatment of premature ejaculation

    Institute of Scientific and Technical Information of China (English)

    Bayoumy I Eassa; Mohamed A El-Shazly

    2013-01-01

    Premature ejaculation (PE) is the most common sexual disorder.It affects 20%-30% of adult men; the aetiology of this condition has not yet been elucidated.The aim of this study is to evaluate the efficacy,safety,tolerability,undesirable effects and improved satisfaction with sexual intercourse with tramadol hydrochloride at different dosages for the treatment of PE.A total of 300 patients who presented with lifelong (primary) PE were included in this study.The study was performed for 28 weeks,in which placebo (starch tablet) was given for 4 weeks,and active ingredient (tramadol hydrochloride) was administered at different therapeutic dosages for 24 weeks.Patients were divided into three equal groups,each consisting of 100 patients.The first group (A) was given tramadol hydrochloride capsule 25 mg.The second group (B) was given tramadol hydrochloride capsule 50 mg.The third group (C) was given tramadol hydrochloride capsule 100 mg.All of the 300 participants included completed the study voluntarily.The age of the patients varied from 25 to 50 years.After the treatment period,the recorded data were collected for each group and analysed.The results showed a highly significant increase in the mean intravaginal ejaculatory latency time (IELT) in all groups compared to baseline data (P<0.0001).We concluded that using tramadol hydrochloride at different doses on demand for the treatment of PE is effective,safe and tolerable,with minimal undesirable effects,and approval for this indication should be sought.

  9. BRAIN TARGETING OF FLUNARIZINE HYDROCHLORIDE BY SOLID LIPID NANOPARTICLES FOR PROPHYLAXIS OF MIGRAINE

    Directory of Open Access Journals (Sweden)

    Mandal Surjyanarayan

    2011-09-01

    Full Text Available Flunarizine hydrochloride, a piperazine derivative, is a selective Ca++ channel blocker coupled with its antihistaminic property claimed to be effective in prophylaxis of migraine. Oral bioavailability of Flunarizine hydrochloride is very low (less then 18% due to poor water solubility and extensive first pass metabolism. Hence the aim of the present study was to develop Flunaruzine hydrochloride loaded sold lipid nanoparticles to improve drug diffusion profile and hence the oral bioavailability. Flunarizine hydrochloride nanosuspension stabilised by poloxamer F-68 was first prepared by high speed homogenization and was lyophilized to obtain nanoparticle using mannitol (1:1 w/v as cryoprotectant. Developed nanoparticle was characterized for its particle size and size distribution, drug content and % drug entrapment. In vitro dissolution study using dissolution bag (12000 D and ex vivo study in rat ileum were carried out using simulated intestinal fluid as dissolution medium. Droplet size, Zeta potential, % drug content and % drug entrapment of the nanoparticles of the Flunarizine hydrochloride were found to be 282±50nm with PdI=0.424±0.028, 34.9±7.36mV, 98.3±0.26% and 67±0.55% respectively. In vitro, ex vivo permeation study revealed that cumulative percentage drug permeated was found to be 75.66±0.9% and 69±1.4% in 8 hrs. Data of the ex vivo release study indicated that drug release was controlled by combination of lipid swelling, erosion and diffusion through the hydrated lipid matrix. From the results it could be considered that the developed Flunarizine hydrochloride nanoparticles may be an alternative for the prophylaxis of migraine.

  10. Effect of Clenbuterol Hydrochloride on the in vitro Development of Mouse Embryo

    Institute of Scientific and Technical Information of China (English)

    2002-01-01

    Objective To investigate the effect of clenbuterol hydrochloride on the in vitro devel-opment of both 1-cell and 2-cell mouse embryos.Methods The cultural systems of both 1-cell and 2-cell mouse embryo were used todetermine the effect of clenbuterol hydrochloride at doses of 1 ng/mL, 3 ng/mL, and10 ng/mL on developmental rates of mouse embryos.Results When 1-cell embryos cultured with 1 ng/mL of clenbuterol hydrochloride,developmental rates from the 4-cell stage to blastocyst stage were significantly lowerthan those in the control group (P< 0. 05), but on dosages of 3 ng/mL and 10ng/mL,the inhibiting effects on embryo development were significantly increased (P< 0. 01).When 2-cell embryos cultured with 1 ng/mL of clenbuterol hydrochloride, obvious dif-ferences in developmental rates were not found between the 2-cell embryo group and thecontrol (P> 0. 05). However, at levels of 3 ng/mL and 10 ng/mL, significant de-crease of developmental rates in 2-cell embryos was observed from the 4-cell and fromthe 8-cell stage, respectively (P< 0. 05). Embryos cultured with clenbuterol hydrochlo-ride appeared to have more granules, fragments and degeneration than those in thecontrol.Conclusion Clenbuterol hydrochloride has a toxic effect on the mouse embryos, and theeffect is in a dose-dependent. 1-cell mouse embryos cultured with clenbuterolhydrochloride could be easily inhibited at 2-cell stage, but the effect of clenbuterolhydrochloride on development of the late 2-cell embryos would be reduced.

  11. SIMULTANEOUS ESTIMATION OF DICLOFENAC SODIUM AND TOLPERISONE HYDROCHLORIDE IN COMBINED PHARMACEUTICAL FORMULATION

    Directory of Open Access Journals (Sweden)

    Bhavesh Gevriya* and R.C. Mashru

    2013-01-01

    Full Text Available Three simple, rapid, precise and accurate spectrophotometric methods have been developed for simultaneous analysis of Tolperisone Hydrochloride (TOL and Diclofenac Sodium (DIC in their combined dosage form. Method A, Simultaneous equation method (Vierodt’s method applies measurement of absorptivities at two wavelengths, 261.00 nm (λmax of Tolperisone Hydrochloride and 279.00 nm, (λmax of Diclofenac Sodium in zero order spectra. The concentrations can be calculated from the derived equations. Method B, Q-Absorbance equation method. It involves formation of Q-absorbance equation at 233.50 nm (isoabsorptive point and 261.00 nm (λmax of Tolperisone Hydrochloride in zero order spectra. Method C, Zero crossing first derivative spectrophotometry involves measurement of absorbance at 249.20 nm (for Tolperisone Hydrochloride and 227.40 nm (for Diclofenac Sodium in first derivative spectra. Developed methods were validated according to ICH guidelines. The calibration graph follows Beer’s law in the range of 6.0 to 18.0 μg/ml for Tolperisone Hydrochloride and 2.0 to 6.0 μg/ml for Diclofenac Sodium with R square value greater than 0.999. Accuracy of all methods was determined by recovery studies and showed % recovery between 98 to 102%. Intraday and interday precision was checked for all methods and mean %RSD was found to be less than 2 for all the methods. The methods were successfully applied for estimation of Tolperisone Hydrochloride and Diclofenac Sodium in marketed formulation.

  12. 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.

  13. Formulation and evaluation of micro hydrogel of Moxifloxacin hydrochloride.

    Science.gov (United States)

    Nanjwade, Basavaraj K; Deshmukh, Rucha V; Gaikwad, Kishori R; Parikh, Kemy A; Manvi, F V

    2012-06-01

    The field of ocular drug delivery is one of the interesting and challenging endeavors facing the pharmaceutical scientist. Novel approaches for ophthalmic drug delivery need to be established to increase the ocular bioavailability by overcoming the inherent drawbacks of conventional dosage forms. In situ hydrogels are instilled as drops into the eye and undergoes a sol-to-gel transition in the cul-de-sac, improved ocular bioavailability by increasing the duration of contact with corneal tissue, thereby reducing the frequency of administration. The purpose of the present work was to develop an ophthalmic drug delivery system using three different gelling agents with different mechanisms for in situ gelation of Moxifloxacin hydrochloride, a fluoroquinolone antibiotic. polyox (a pH-sensitive gelling agent), sodium alginate (an ion-sensitive gelling agent), and poloxamer (a temperature-sensitive gelling agent) were employed for the formation of in situ hydrogel along with HPMC K4M as viscofying agent, which increases the residence time of the drug in the ocular cavity. The promising formulations MF(4), MF(5), and MF(9) were evaluated for pH, drug content, in vitro gelation, in vitro drug release, in vivo drug release, ocular irritation, and stability. Percent drug content of 98.2, 98.76, and 99.43%; viscosity of 15.724 × 100, 16.108 × 100, and 15.213 × 100 cP at 20 rpm, cumulative percent release of 75.364, 74.081, and 71.752%, and C (max) of 1,164.16, 1,187.09, and 1,220.58 ng/ml was observed for formulation MF(4), MF(5), and MF(9), respectively. The developed formulations were therapeutically efficacious, stable, and non-irritant and provided sustained release of the drug over 8 h.

  14. Biowaiver monographs for immediate release solid oral dosage forms: ranitidine hydrochloride.

    Science.gov (United States)

    Kortejärvi, H; Yliperttula, M; Dressman, J B; Junginger, H E; Midha, K K; Shah, V P; Barends, D M

    2005-08-01

    Literature and experimental data relevant to the decision to allow a waiver of in vivo bioequivalence testing for the approval of immediate release (IR) solid oral dosage forms containing ranitidine hydrochloride are reviewed. According to the current Biopharmaceutics Classification System (BCS), ranitidine hydrochloride should be assigned to Class III. However, based on its therapeutic and therapeutic index, pharmacokinetic properties and data related to the possibility of excipient interactions, a biowaiver can be recommended for IR solid oral dosage forms that are rapidly dissolving and contain only those excipients as reported in this study.

  15. Development and validation of a dissolution test for diltiazem hydrochloride in immediate release capsules

    Directory of Open Access Journals (Sweden)

    Taciane Ferreira Mendonça

    2011-01-01

    Full Text Available This work describes the development and validation of a dissolution test for 60 mg of diltiazem hydrochloride in immediate release capsules. The best dissolution in vitro profile was achieved using potassium phosphate buffer at pH 6.8 as the dissolution medium and paddle as the apparatus at 50 rpm. The drug concentrations in the dissolution media were determined by UV spectrophotometry and HPLC and a statistical analysis revealed that there were significant differences between HPLC and spectrophotometry. This study illustrates the importance of an official method for the dissolution test, since there is no official monograph for diltiazem hydrochloride in capsules.

  16. Synthesis and Characterization of Impurities of Barnidipine Hydrochloride, an Antihypertensive Drug Substance

    Directory of Open Access Journals (Sweden)

    Zhi-Gang Cheng

    2014-01-01

    Full Text Available Barnidipine hydrochloride is a long term dihydropyridine calcium channel blocker used for the treatment of hypertension. During the process development of barnidipine hydrochloride, four barnidipine impurities were detected by high-performance liquid chromatography (HPLC with an ordinary column (Agilent ZORBAX Eclipse XDB-C18, 150 mm × 4.6 mm, 5 µm. All these impurities were identified, synthesized, and subsequently characterized by their respective spectral data (MS, 1H-NMR, and 13C-NMR. The identification of these impurities should be useful for quality control in the manufacture of barnidipine.

  17. Synthesis and characterization of impurities of barnidipine hydrochloride, an antihypertensive drug substance.

    Science.gov (United States)

    Cheng, Zhi-Gang; Dai, Xu-Yong; Li, Li-Wei; Wan, Qiong; Ma, Xiang; Xiang, Guang-Ya

    2014-01-21

    Barnidipine hydrochloride is a long term dihydropyridine calcium channel blocker used for the treatment of hypertension. During the process development of barnidipine hydrochloride, four barnidipine impurities were detected by high-performance liquid chromatography (HPLC) with an ordinary column (Agilent ZORBAX Eclipse XDB-C18, 150 mm×4.6 mm, 5 µm). All these impurities were identified, synthesized, and subsequently characterized by their respective spectral data (MS, 1H-NMR, and 13C-NMR). The identification of these impurities should be useful for quality control in the manufacture of barnidipine.

  18. 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.

  19. Effect of Modulated Alternating and Direct Current Iontophoresis on Transdermal Delivery of Lidocaine Hydrochloride

    OpenAIRE

    Gaurav Bhatia; Banga, Ajay K.

    2014-01-01

    The objective of this study was to investigate the iontophoretic delivery of lidocaine hydrochloride through porcine skin and to compare the effects of modulated alternating and direct current iontophoresis. Continuous and modulated iontophoresis was applied for one hour and two hours (0-1 h and 4-5th h) using a 1% w/v solution of lidocaine hydrochloride. Tape stripping was done to quantify the amount of drug permeated into stratum corneum and skin extraction studies were performed to determi...

  20. 丝裂霉素C血管外渗致皮肤损伤的防治实验研究%An experimental investigation on prevention of skin injury induced by extravascular mitomycin C

    Institute of Scientific and Technical Information of China (English)

    范淑英; 张玉英; 郭文君; 魏志新

    2001-01-01

    Objective To explored the pathologic changes in skin injury induced by Mitomycin C Extravasation and to explore the preventive method. Method The 0.2mg mitomycin C Were injected into subcutaneous in lower extremity of rat, 30min late, 0.8ml blockade solution (consist of 0.2% lidocaine, gentamycin and dexamethasone) were injected into subcutaneous and ZuSanli point of lower extremity. Pathologic changes of skin injury tissue were observed. Result When mitomycin C Were injected into subcutaneous in 5~8 days late,group A showed the inflammatory infiltration and ulcer formation in part of injection, group B showed mild inflammatory and was no ulcer formation in part of injection. Conclusion The point blockade treatment was a effective preventing skin injury induced by extravascular mitomycin C.%目的探讨丝裂霉素C血管外渗致皮肤损伤的形态学变化及防治措施。方法在大鼠后下肢皮下注射0.2mg丝裂霉素C,30 min后,分别在注射部位皮下和相当于足三里穴位处注射0.8ml封闭液(0.2%利多卡因10ml,庆大霉素8万单位,地塞米松5mg混匀即用),观察局部病理形态学变化。结果皮下注射组5~8d后,局部可见明显溃疡形成,而穴位封闭组病变轻微,无溃疡形成。结论穴位局部封闭有防治丝裂霉素血管外渗所致皮肤损伤的作用。

  1. 内镜下扩张联合注射丝裂霉素治疗食管良性狭窄的疗效评价%Endoscopic dilation combined with intramuscular injection of mitomycin C for benign esophageal strictures

    Institute of Scientific and Technical Information of China (English)

    张银; 刘莉; 王敏; 陈建平; 范志宁; 王翔

    2015-01-01

    Objective To evaluate the safety and efficacy of an endoscopic dilation in association with the intramuscular injection of either mitomycin C for benign esophageal strictures. Methods A total of 89 patients with benign esophageal strictures were retrospectively divided into 3 groups, including 30 cases of dilation combined with mitomycin C injection (mitomycin C group) , 29 of dilation combined with dexamethasone injection (dexamethasone group) and 30 of dilation with saline injection (dilation group). The successful rate, complications and the clinical effect in the 3 groups were compared. Results The 89 patients all successfully received the procedure, with the endoscopic and clinical release. No massive hemorrhage occurred. In mitomycin C group, 1 case with major complication (perforation) and 7 minor complication occurred;9 and 7 cases with minor complication occurred in dexamethasone group and dilation group, respectively. There were no significant difference of the complications in the 3 groups (P0.05).术后食管通畅时间丝裂霉素组为(5.25±1.18)个月,激素组为(4.46±1.53)个月,单纯扩张组为(3.03±1.62)个月,3组间差异有统计学意义(P<0.05).结论 内镜下扩张联合注射丝裂霉素、地塞米松及单纯扩张治疗食管良性狭窄均安全有效,但联合注射药物治疗效果优于单纯扩张,且以联合注射丝裂霉素治疗效果更优.

  2. Dexmethylphenidate--Novartis/Celgene. Focalin, D-MPH, D-methylphenidate hydrochloride, D-methylphenidate, dexmethylphenidate, dexmethylphenidate hydrochloride.

    Science.gov (United States)

    2002-01-01

    Celgene has developed a chirally pure form of methylphenidate (Ritalin), called dexmethylphenidate [d-methylphenidate, d-methylphenidate hydrochloride, d-MPH; Focalin]. The drug has been launched in the USA and is undergoing registration in Canada for the treatment of children with attention-deficit hyperactivity disorder (ADHD). Dexmethylphenidate is the single isomer version of racemic methylphenidate (Ritalin), which contains the active d isomer of Ritalin. Dexmethylphenidate acts via the inhibition of reuptake of norepinephrine and dopamine. Research is ongoing to further clarify the mode of therapeutic action in ADHD. Dexmethylphenidate was developed with the aim of reducing drug load, adverse events and drug interactions. Dexmethylphenidate provides effective management of attention-deficit hyperactivity disorder at half the dose of Ritalin. In April 2000, worldwide rights (excluding Canada) to dexmethylphenidate were granted to Novartis. Celgene has also granted Novartis rights to all related intellectual properties and patents. Novartis will fund all remaining development and marketing expenses required for regulatory approval and commercialisation of dexmethylphenidate. Crystaal Corporation, the marketing division of Biovail Corporation International, has exclusive Canadian marketing rights for all formulations of dexmethylphenidate. Novartis launched dexmethylphenidate (Focalin) in the USA during Q1 2002. It is available as a D-shaped tablet (2.5, 5 and 10 mg doses). Novartis had planned to use the tradename Ritadex, however the FDA recommended an alternative name due to potential prescribing errors with Ritalin. The finalized tradename to be used is Focalin. In July 2001, a new drug submission was filed with Canada's Therapeutic Products Programme for dexmethylphenidate in the treatment of attention-deficit disorder and attention-deficit hyperactivity disorder. Novartis is also developing an extended-release version of chirally pure dexmethylphenidate

  3. Photorefractive Keratectomy with Adjunctive Mitomycin C for Residual Error after Laser-Assisted In Situ Keratomileusis Using the Pulzar 213 nm Solid-State Laser: Early Results.

    Science.gov (United States)

    Ng-Darjuan, Maya Fe; Evangelista, Raymond P; Agahan, Archimedes Lee D

    2013-01-01

    Purpose. To evaluate the accuracy, efficacy, stability, and safety of photorefractive keratectomy (PRK) enhancement using the Pulzar 213 nm solid-state laser (SSL) with adjunctive Mitomycin C in eyes previously treated with laser assisted in situ keratomileusis (LASIK) with residual error of refraction. Methods. This is a prospective noncomparative case series of 16 eyes of 12 patients who underwent PRK for residual refractive error after primary LASIK. Mitomycin C 0.02% was used after the PRK to prevent haze formation. Outcomes measured were pre- and postoperative manifest refraction spherical equivalent (MRSE), uncorrected (UDVA) and best-corrected distance visual acuity (CDVA), and slit lamp evidence of corneal complications. Results. The mean UDVA improved from 20/70 preoperatively to 20/30 postoperatively. The average gain in lines for the UDVA was 2.38. After six months of followup, the postoperative MRSE within 0.50 D in 56% (9) of eyes and 94% (15) eyes were within 1.0 diopters of the intended correction. No eyes developed haze all throughout the study. Conclusion. PRK enhancement with adjunctive use of Mitomycin C for the correction of residual error of refraction after LASIK using the Pulzar 213 nm solid-state laser is an accurate, effective, and safe procedure.

  4. 丝裂霉素C治疗眼部手术后结膜植入性囊肿的临床观察%Clinical observation of Mitomycin C in curing implantantion cyst of conjunctiva after operation

    Institute of Scientific and Technical Information of China (English)

    孟凡华

    2012-01-01

    OBJECTIVE To observe the clinical efficacy of Mitomycin C in treating implantation cyst of conjunctiva after operation. METHODS Twenty-eight cases of implantation cyst of conjunctiva were given drainage through marginal incision and cleaned with 0.02% Mitomycin C. RESULTS Followed up for 3 months to 2 years, 28 cases were all cured. CONCLUSIONS Mitomycin C is a simple and efficient application in curing implantation cyst of conjunctiva.%目的 探究丝裂霉素C治疗眼部手术后结膜植入性囊肿的治疗效果.方法 对28例眼部手术后发生的球结膜植入性囊肿,采取囊肿一侧边缘切口放液,而后用0.02%丝裂霉素C擦拭囊壁治疗.结果 随访3个月~2年,28例患者全部治愈.结论 丝裂霉素C治疗结膜植入性囊肿简单有效,适合临床使用.

  5. 丝裂霉素加顺铂治疗难治性晚期乳腺癌%Phase Ⅱ study of mitomycin C and cisplatin in heavily pretreated advanced breast cancer

    Institute of Scientific and Technical Information of China (English)

    胡夕春; 郭海宜; 赵欣民

    2006-01-01

    Objective: The mitomycin C and cisplatin combination was investigated in patients with advanced breast cancer who had been exposed to anthracyclines, vinorelbine and taxanes. Methods: Three-weekly regimen consisted of mitomycin,6 mg/m2 administered intravenously on day 1, and cisplatin, 25 mg/m2 intravenously on day 1-3. Results: Thirty-eight patients aged 25-75 years (median, 46 years) were treated with an overall response rate of 31.6%. The median time to progression(TTP) was 4.0 months. Median TTP for 12 patients with a complete or partial response was 9.0 months, while stable disease and progression of disease 4.0 months, ,P=-0.002. Grade 3/4 side effects of neutropenia, thrombocytopenia and nausea/vomiting were documented in 4 (10.5%), 4 (10.5%) and 3 (7.9%) patients, respectively. The median overall survival was 13+ months. Conclusion: Mitomycin C/cisplatin doublet showed antitumor activity for anthracycline-, vinorelbine- and taxane-resistant breast cancer comparable to other regimens. This well-tolerated regimen provides an affordable option for patients in China.

  6. Spotlight on anagrelide hydrochloride for the treatment of essential thrombocythemia

    Directory of Open Access Journals (Sweden)

    Sarma A

    2017-01-01

    Full Text Available Anita Sarma,1 Donal P Mclornan,1,2 Claire N Harrison2 1Department of Haematology, King’s College Hospital NHS Foundation Trust, 2Department of Haematology, Guy’s and St Thomas’ NHS Foundation Trust, London, UK Abstract: Anagrelide (ANA hydrochloride is an oral imidazoquinazoline registered as an orphan drug in Europe. It is indicated as a second-line agent for the reduction of thrombocytosis in high-risk essential thrombocythemia (ET in Europe and in any myeloproliferative neoplasm-associated thrombocytosis and for the amelioration of thrombo-hemorrhagic events in the context of myeloproliferative neoplasm in the USA and Japan. The compound has been in clinical use for almost two decades with approval in the European Union (EU for over a decade. The licensed indication encompasses the apparently specific action of the drug to reduce the platelet count; however, the precise mode of action of ANA remains unclear. Here, we review the current data from two large phase 3 studies, PT-1 and ANAHDRET, and a phase 4 post-approval observational study EXELS. All of these studies were conducted in the EU and therefore pertain to ET as the only licensed indication. Data from these studies suggest that ANA is on the whole as effective as the most commonly used agent hydroxycarbamide (HC. Although ANA, when compared to HC, appears to be slightly less effective in preventing arterial thrombosis and myelofibrotic transformation, it is associated with lower risk of venous thrombosis. Since the initial data from the PT-1 study, a caution has been recommended for the combined use of ANA and aspirin as this may provoke excess hemorrhage. ET is a clinically and biologically heterogeneous condition, and these biological variations may in part explain some of the clinical differences observed in various studies in response to specific treatments. No new toxicities of ANA have emerged in the past decade, which means that clinicians and patients can be reassured

  7. Pharmaceutical development of an amorphous solid dispersion formulation of elacridar hydrochloride for proof-of-concept clinical studies.

    Science.gov (United States)

    Sawicki, E; Schellens, J H M; Beijnen, J H; Nuijen, B

    2017-04-01

    A novel tablet formulation containing an amorphous solid dispersion (ASD) of elacridar hydrochloride was developed with the purpose to resolve the drug's low solubility in water and to conduct proof-of-concept clinical studies. Elacridar is highly demanded for proof-of-concept clinical trials that study the drug's suitability to boost brain penetration and bioavailability of numerous anticancer agents. Previously, clinical trials with elacridar were performed with a tablet containing elacridar hydrochloride. However, this tablet formulation resulted in poor and unpredictable absorption which was caused by the low aqueous solubility of elacridar hydrochloride. Twenty four different ASDs were produced and dissolution was compared to crystalline elacridar hydrochloride and a crystalline physical mixture. The formulation with highest dissolution was characterized for amorphicity. Subsequently, a tablet was developed and monitored for chemical/physical stability for 12 months at +15-25 °C, +2-8 °C and -20 °C. The ASD powder was composed of freeze dried elacridar hydrochloride-povidone K30-sodium dodecyl sulfate (1:6:1, w/w/w), appeared fully amorphous and resulted in complete dissolution whereas crystalline elacridar hydrochloride resulted in only 1% dissolution. The ASD tablets contained 25 mg elacridar hydrochloride and were stable for at least 12 months at -20 °C. The ASD tablet was considered feasible for proof-of-concept clinical studies and is now used as such.

  8. LASEK con mitomicina C en altos defectos refractivos miópicos Use of LASEK with Mitomycin C to treat high myopic defects

    Directory of Open Access Journals (Sweden)

    Abel Cabrera Martínez

    2009-12-01

    Full Text Available OBJETIVO: Valorar los resultados refractivos en pacientes con altos defectos refractivos miópicos operados por queratomileusis subepitelial asistida con láser combinando el uso de mitomicina C (LASEK+MC. MÉTODOS: Se realizó un estudio prospectivo, de corte transversal en un total de 47 ojos. La muestra fue seleccionada del total de pacientes que acudió a nuestro -Servicio de Cirugía Implanto-refractiva. Teniendo en cuenta el consentimiento informado previo, se aplicó la técnica referida para la corrección de a ametropía, empleándose la mitomicina C de producción nacional al 0,02 % durante dos minutos en el transoperatorio. Para valorar los resultados del estudio se realizaron varios exámenes antes y después de operados los pacientes. RESULTADOS: Los resultados refractivos encontrados en los pacientes operados fueron muy alentadores, se logró corregir la totalidad de los defectos refractivos y se obtuvo una calidad visual muy favorable según test visuales realizados. Además, se obtuvo un índice de complicaciones muy bajo. CONCLUSIONES: La cirugía corneal con láser mediante LASEK+MC, demostró ser una técnica muy confiable y segura. Se obtuvo resultados refractivos muy alentadores, en pacientes con altos defectos refractivos miópicos, cuya calidad de vida, consecuentemente, fue muy superior.OBJECTIVE: To assess the refractive outcome in patients with high refractive myopic defects who were operated on by laser-assisted subepithelial keratomileusis plus Mitomycin C (LASEK + MC. METHODOS: A prospective cross-sectional study was performed in 47 eyes. The sample was selected from the whole number of patients who went to our Implant-Refractive Surgery Department. Taking into account their previous informed consent, the referred technique was used to correct ametropy by additionally using Cuban-made 0,02 % Mitomycin C for two minutes in the transoperative stage. To evaluate the outcome of the study, several tests were conducted

  9. Carbon dioxide-water oxygen isotope fractionation factor using chlorine trifluoride and guanidine hydrochloride techniques

    Energy Technology Data Exchange (ETDEWEB)

    Dugan, J.P. Jr.; Borthwick, J.

    1986-12-01

    A new value for the CO/sub 2/-H/sub 2/O oxygen isotope fractionation factor of 1.04145 +/- 0.000 15 (2sigma) has been determined. The data have been normalized to the V-SMOW/V-SLAP scale and were obtained by measuring isotopic compositions with the guanidine hydrochloride and chlorine trifluoride techniques.

  10. 77 FR 53892 - Determination That ALOXI (Palonosetron Hydrochloride) Capsules, 0.5 Milligram (Base), Were Not...

    Science.gov (United States)

    2012-09-04

    ...) Capsules, 0.5 Milligram (Base), Were Not Withdrawn From Sale for Reasons of Safety or Effectiveness AGENCY... determined that ALOXI (palonosetron hydrochloride (HCl)) Capsules, 0.5 milligram (mg) (base), were not... abbreviated new drug applications (ANDAs) for palonosetron HCl capsules, 0.5 mg (base), if all other legal and...

  11. Biowaiver monographs for immediate release solid oral dosage forms: mefloquine hydrochloride.

    Science.gov (United States)

    Strauch, S; Jantratid, E; Dressman, J B; Junginger, H E; Kopp, S; Midha, K K; Shah, V P; Stavchansky, S; Barends, D M

    2011-01-01

    Literature data relevant to the decision to allow a waiver of in vivo bioequivalence (BE) testing for the approval of immediate release solid oral dosage forms containing mefloquine hydrochloride as the only active pharmaceutical ingredient (API) are reviewed. The solubility and permeability data of mefloquine hydrochloride as well as its therapeutic use and therapeutic index, its pharmacokinetic properties, data related to the possibility of excipient interactions and reported BE/bioavailability studies were taken into consideration. Mefloquine hydrochloride is not a highly soluble API. Since no data on permeability are available, it cannot be classified according to the Biopharmaceutics Classification System with certainty. Additionally, several studies in the literature failed to demonstrate BE of existing products. For these reasons, the biowaiver cannot be justified for the approval of new multisource drug products containing mefloquine hydrochloride. However, scale-up and postapproval changes (HHS-FDA SUPAC) levels 1 and 2 and most EU type I variations may be approvable without in vivo BE, using the dissolution tests described in these regulatory documents.

  12. An investigation on in vitro and in vivo antimicrobial properties of the antidepressant: amitriptyline hydrochloride

    Directory of Open Access Journals (Sweden)

    Anurup Mandal

    2010-10-01

    Full Text Available The antidepressant drug amitriptyline hydrochloride was obtained in a dry powder form and was screened against 253 strains of bacteria which included 72 Gram positive and 181 Gram negative bacteria and against 5 fungal strains. The minimum inhibitory concentration (MIC was determined by inoculating a loopful of an overnight peptone water culture of the organism on nutrient agar plates containing increasing concentrations of amitriptyline hydrochloride (0, 10 µg/mL, 25 µg/mL, 50 µg/mL, 100 µg/mL, 200 µg/mL. Amitriptyline hydrochloride exhibited significant action against both Gram positive and Gram negative bacteria at 25-200 µg/mL. In the in vivo studies it was seen that amitriptyline hydrochloride at a concentration of 25 µg/g and 30 µg/g body weight of mouse offered significant protection to Swiss strain of white mice when challenged with 50 median lethal dose (MLD of a virulent strain of Salmonella typhimurium NCTC 74. The in vivo data were highly significant (p<0.001 according to the chi-square test.

  13. Oral Midodrine Hydrochloride for Prevention of Orthostatic Hypotension during Early Mobilization after Hip Arthroplasty

    DEFF Research Database (Denmark)

    Jans, Øivind; Mehlsen, Jesper; Kjærsgaard-Andersen, Per

    2015-01-01

    or older and scheduled for total hip arthroplasty under spinal anesthesia to either 5 mg midodrine hydrochloride or placebo orally 1 h before mobilization at 6 and 24 h postoperatively. The primary outcome was the prevalence of OH (decrease in systolic or diastolic arterial pressures of > 20 or 10 mm...

  14. DENATURATION OF NATIVE AND DEGLYCOSYLATED α-GALACTOSIDASES FROM Penicillium canescens BY GUANIDINE HYDROCHLORIDE

    Directory of Open Access Journals (Sweden)

    Borzova N. V.

    2015-08-01

    Full Text Available The aim of this work was the study of native and galactosidases from Penicillium canescens under denaturing conditions caused by guanidine hydrochloride. Calculation of kinetics and constants of enzymes inactivation was carried out on using experimental kinetic curves of enzyme denaturation. We observed significant differences in the kinetics of inactivation of native and deglycosylated α-galactosidases from P. canescens caused by guanidine hydrochloride. Native enzyme was stable within the selected range of guanidine hydrochloride concentrations (from 0.1 to 3.0 M, retaining no less than 50% of the initial enzyme activity for 3 days. Deglycosylated enzyme preparations were less stable and they lost their activity within 5–30 minutes, when they were treated with guanidine hydrochloride in concentrations above 1 M. Dissociation rate constant of native and deglycosylated forms of the enzyme differed by 10 to 100 folds. It was shown that subunit interactions play a major role in the process of inactivation of the enzyme, and the carbohydrate component is essential for stabilizing of subunit bonds and maintaining conformational stability of the enzyme under denaturing conditions of chemical agents.

  15. Effect of magnesium stearate concentration on dissolution properties of ranitidine hydrochloride coated tablets.

    Science.gov (United States)

    Uzunović, Alija; Vranić, Edina

    2007-08-01

    Most pharmaceutical formulations also include a certain amount of lubricant to improve their flowability and prevent their adhesion to the surfaces of processing equipment. Magnesium stearate is an additive that is most frequently used as a lubricant. Magnesium stearate is capable of forming films on other tablet excipients during prolonged mixing, leading to a prolonged drug liberation time, a decrease in hardness, and an increase in disintegration time. It is hydrophobic, and there are many reports in the literature concerning its adverse effect on dissolution rates. The objective of this study was to evaluate the effects of two different concentrations of magnesium stearate on dissolution properties of ranitidine hydrochloride coated tablet formulations labeled to contain 150 mg. The uniformity content was also checked. During the drug formulation development, several samples were designed for choice of the formulation. For this study, two formulations containing 0,77 and 1,1% of magnesium stearate added in the manufacture of cores were chosen. Fraction of ranitidine hydrochloride released in dissolution medium was calculated from calibration curves. The data were analyzed using pharmacopeial test for similarity of dissolution profiles ( f2 equation), previously proposed by Moore and Flanner. Application of f2 equation showed differences in time-course of ranitidine hydrochloride dissolution properties. The obtained values indicate differences in drug release from analyzed ranitidine hydrochloride formulations and could cause differences in therapeutic response.

  16. Efficacy of epinastine hydrochloride for antigen-provoked nasal symptoms in subjects with orchard grass pollinosis.

    Science.gov (United States)

    Gotoh, Minoru; Hashiguchi, Kazuhiro; Okubo, Kimihiro

    2011-03-01

    Among the gramineae species, orchard grass is a typical causative pollen that provokes seasonal rhinitis. The purpose of this study was to examine the protective efficacy of epinastine hydrochloride for signs and symptoms caused by repeated nasal provocation with discs containing orchard grass pollen. A single-dose, placebo-controlled, double-blind, crossover clinical study was conducted in subjects with orchard grass pollinosis. The pollen challenge was conducted with the use of provocation discs containing orchard grass pollen. Epinastine hydrochloride suppressed nasal symptoms caused by nasal provocation tests using orchard grass pollen discs. Among the nasal symptoms, the number of sneezing was significantly inhibited 30 minutes and 60 minutes after the administration of epinastine hydrochloride, as compared with placebo. There were no adverse reactions to the study drugs. Our results suggest that nasal provocation tests with discs containing orchard grass pollen is a useful method for evaluating the onset of action of antiallergic drugs. As compared with placebo, epinastine hydrochloride decreased early-phase sneezing and the total nasal symptom score after repeated nasal provocations with orchard grass pollen discs.

  17. 77 FR 14810 - Determination That DURANEST (Etidocaine Hydrochloride) Injection, 0.5%, and Five Other DURANEST...

    Science.gov (United States)

    2012-03-13

    ... contains the same active ingredient in the same strength and dosage form as the ``listed drug,'' which is a.... Drug Applicant date NDA 17-751...... DURANEST AstraZeneca August 30, 1976. (epinephrine Pharmaceutical.... (epinephrine Pharmaceutical. bitartrate; etidocaine hydrochloride) Injection 1.5%. The drug products listed...

  18. 1,2-Bis (pyridin-2-ylmethyl)sulfanyl ethane and its dimorphic hydrochloride salt

    DEFF Research Database (Denmark)

    Lennartson, A.; McKenzie, C. J.

    2011-01-01

    and are held together by C-H center dot center dot center dot N and C-H center dot center dot center dot S interactions, resulting in the formation of a three-dimensional network structure. In addition, two polymorphs of the corresponding hydrochloride salt, 2-[(2-[(pyridin-1-ium-2-ylmethyl...

  19. 40 CFR 721.5775 - Phenol, 5-amino-2,4-dicholoro-, hydrochloride.

    Science.gov (United States)

    2010-07-01

    ... 40 Protection of Environment 30 2010-07-01 2010-07-01 false Phenol, 5-amino-2,4-dicholoro... Specific Chemical Substances § 721.5775 Phenol, 5-amino-2,4-dicholoro-, hydrochloride. (a) Chemical substance and significant new uses subject to reporting. (1) The chemical substance identified as phenol,...

  20. A Parent Guide To Understanding the Effects of Ritalin (Methylphenidate Hydrochloride).

    Science.gov (United States)

    Villegas, Orlando; And Others

    This guide provides information to help parents decide whether their child with attention deficit hyperactivity disorder (ADHD) should take methylphenidate hydrochloride (Ritalin). Information is provided in a question-and-answer format on various concerns, including: the meaning of ADHD, whether Ritalin is overprescribed, when this medication is…

  1. Minocycline hydrochloride as a soft sclerotizing agent for symptomatic simple renal and hepatic cysts.

    Science.gov (United States)

    Danza, F M; Falcione, M; Bordonaro, V; Infante, A; Paladini, A; Bonomo, L

    2017-01-01

    To present the results of our ten-year case series in simple hepatic and renal cysts sclerosis using minocycline hydrochloride as a sclerotizing agent, evaluating the effectiveness, the safety and the feasibility of this agent for percutaneous sclerotherapy for symptomatic cysts. We retrospectively evaluated our archives of patients treated (54 patients with 60 renal cysts, 21 patients with 24 hepatic cysts) for symptomatic abdominal cysts. These patients were treated with ultrasound guided drainage and subsequent minocycline hydrochloride instillation. In large or recurrent cysts, we repeated the treatment for the second time. The patients were evaluated at 6 and 12 months; some patients underwent later, additional examinations and we also reviewed these exams for any eventual long-term relapse. The percentage of sclerosis success was found to be 100% for hepatic cysts and 86% for renal cysts. We also found that minimal complications were encountered. Minocycline hydrochloride has proven to be an effective sclerotizing agent. In our cases, symptoms disappeared in 100% of patients with hepatic cysts and in 93% of patients with renal cysts. It is also a safe sclerotizing agent, as demonstrated by the few complications encountered. Percutaneous sclerosis with Minocycline hydrochloride is a very effective and promising nonsurgical treatment for patients with symptomatic simple cysts, and it can be performed without major complications.

  2. The Impact of Hydrochloride Heroin on Mental Flexibility, Abstract Reasoning, Impulsivity, and Attention

    Directory of Open Access Journals (Sweden)

    Zahra Alam Mehrjerdi

    2011-04-01

    Full Text Available Introduction: Drug addiction could lead to severe impairments in executive and neurocognitive functions but study on the impact of hydrochloride heroin on executive functions has remained in infancy in Iran. The aim of this study was to examine the relationship between addiction to hydrochloride heroin and executive functioning in several cognitive domains including mental flexibility, abstract reasoning, impulsivity, and attention. Methods: A total of 60 cases of young male addicts aged 18 to 21 were recruited from outpatient addiction clinics in Karaj city and were matched with 60 non-drug using controls. A test battery including the Wisconsin Card Sorting Test (WCST, Porteus Maze Test (PMQS, Serial Seven Subtraction Test (SSST, and Color Trails Test (CTT were administered respectively. Results: The patient group showed more problems in impulse control compared with the control group, while mental flexibility, abstract reasoning and attention were not affected. Discussion: The findings indicated that addiction to hydrochloride heroin had a negative effect on impulse control. This issue could reflect the role of impaired inhibitory control on drug-seeking behaviors and relapse. Special treatment programs must be tailored to control impulsivity among addicts to hydrochloride heroin during treatment.

  3. Solubility, dissolution rate and phase transition studies of ranitidine hydrochloride tautomeric forms.

    Science.gov (United States)

    Mirmehrabi, M; Rohani, S; Murthy, K S K; Radatus, B

    2004-09-10

    Understanding the polymorphic behavior of pharmaceutical solids during the crystallization process and further in post-processing units is crucial to meet medical and legal requirements. In this study, an analytical technique was developed for determining the composition of two solid forms of ranitidine hydrochloride using two peaks of Fourier transform infrared (FTIR) spectra without the need to grind the samples. Solubility studies of ranitidine hydrochloride showed that Form 2 has a higher solubility than Form 1. Solution-mediated transformation is very slow and occurs from Form 2 to Form 1 and not the reverse. No solid-solid transformation was observed due to grinding or compressing the pure samples of either forms and of a 50/50 wt.% mixture. Grinding was found to be a proper technique for increasing the bulk solid density of the ranitidine hydrochloride without the risk of solid-solid transformation. Dissolution rate found to be equally fast for both forms. The solubility data were modeled using the group contribution parameters and UNIversal QUAsi-Chemical (UNIQUAC) theory. There was a good agreement between the experimental solubility data of ranitidine hydrochloride and the results of UNIQUAC equation.

  4. SPECTROPHOTOMETRIC ESTIMATION OF BUSPIRONE HYDROCHLORIDE IN BULK AND ITS PHARMACEUTICAL FORMULATION

    Directory of Open Access Journals (Sweden)

    B.DHANDAPANI,

    2010-05-01

    Full Text Available Three simple, accurate, rapid and sensitive methods developed for the determination of buspirone hydrochloride in bulk drug and in its tablets by UV Spectroscopy (Method – A – Water as a Solvent, UV Spectroscopy (Method – B – Methanol as a Solvent, and Colorimetry (Method - C. In Method A buspirone hydrochloride estimated at 236 nm using distilled water as a solvent. The linearity was observed in the concentration range of 5 – 25 μg/ml with correlation co efficient of 0.9866. In Method B methanol used as a solvent. The linearity wasobserved in the concentration range of 10 – 50 μg/ml with correlation co efficient of 0.9905. In Method C buspirone hydrochloride is a colorless compound undergoes oxidation with 0.005M Potassium ermanganate Solution in the presence of 0.5M Sodium Hydroxide gives Pink color. The intensity of color directly proportional to theconcentration of buspirone hydrochloride and its found that intensity of color stable for 20mins and the absorbance was measured at 610 nm with different time intervals with the linearity range and correlation co -efficient of 10 – 50 μg/ml and 0.9924. The result of analysis for all the methods was validated statistically and by ecovery studies.

  5. Complexation of roxatidine acetate hydrochloride with beta-cyclodextrin: NMR spectroscopic study.

    Science.gov (United States)

    Ali, S M; Maheshwari, A; Asmat, F

    2004-08-01

    A NMR spectroscopic study of mixtures of varying ratios of roxatidine acetate hydrochloride (RAH) and beta-cyclodextrin (beta-CD) in D2O revealed the formation of a 1:1 inclusion compound. The aromatic ring of RAH selectively penetrates the beta-CD cavity in preference to the piperidine ring.

  6. Usefulness of vernakalant hydrochloride injection for rapid conversion of atrial fibrillation

    DEFF Research Database (Denmark)

    Pratt, Craig M.; Roy, Dennis; Torp-Pedersen, Christian

    2010-01-01

    The objective of the present study was to assess the safety and effectiveness of vernakalant hydrochloride injection (RSD1235), a novel antiarrhythmic drug, for the conversion of atrial fibrillation (AF) or atrial flutter to sinus rhythm (SR). Patients with either AF or atrial flutter were random...

  7. 1,2-Bis (pyridin-2-ylmethyl)sulfanyl ethane and its dimorphic hydrochloride salt

    DEFF Research Database (Denmark)

    Lennartson, A.; McKenzie, C. J.

    2011-01-01

    and are held together by C-H center dot center dot center dot N and C-H center dot center dot center dot S interactions, resulting in the formation of a three-dimensional network structure. In addition, two polymorphs of the corresponding hydrochloride salt, 2-[(2-[(pyridin-1-ium-2-ylmethyl...

  8. Interactions of biocidal guanidine hydrochloride polymer analogs with model membranes: a comparative biophysical study

    Institute of Scientific and Technical Information of China (English)

    Zhongxin Zhou; Anna Zheng; Jianjiang Zhong

    2011-01-01

    Four synthesized biocidal guanidine hydrochloride polymers with different alkyl chain length,including polyhexamethylene guanidine hydrochloride and its three new analogs,were used to investigate their interactions with phospholipids vesicles mimicking bacterial membrane.Characterization was conducted by using fluorescence dye leakage,isothermal titration calorimetry,and differential scanning calorimetry.The results showed that the gradually lengthened alkyl chain of the polymer increased the biocidal activity,accompanied with the increased dye leakage rate and the increased binding constant and energy change value of polymer-membrane interaction.The polymer-membrane interaction induced the change of pretransition and main phase transition (decreased temperature and increased width) of phospholipids vesicles,suggesting the conformational change in the phospholipids headgroups and disordering in the hydrophobic regions of lipid membranes.The above information revealed that the membrane disruption actions of guanidine hydrochloride polymers are the results of the polymer's strong binding to the phospholipids membrane and the subsequent perturbations of the polar headgroups and hydrophobic core region of the phospholipids membrane.The alkyl chain structure significantly affects the binding constant and energy change value of the polymer-membrane interactions and the perturbation extent of the phospholipids membrane,which lead to the different biocidal activity of the polymer analogs.This work provides important information about the membrane disruption action mechanism of biocidal guanidine hydrochloride polymers.

  9. 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.

  10. Zilpaterol hydrochloride affects cellular muscle metabolism and lipid components of ten different muscles in feedlot heifers

    Science.gov (United States)

    This study determined if zilpaterol hydrochloride (ZH) altered muscle metabolism and lipid components of ten muscles. Crossbred heifers were either supplemented with ZH (n = 9) or not (Control; n = 10). Muscle tissue was collected (adductor femoris, biceps femoris, gluteus medius, infraspinatus, lat...

  11. 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.

  12. Vernakalant hydrochloride for rapid conversion of atrial fibrillation - A phase 3, randomized, placebo-controlled trial

    DEFF Research Database (Denmark)

    Roy, D.; Pratt, C.M.; Torp-Pedersen, C.;

    2008-01-01

    Background - The present study assessed the efficacy and safety of vernakalant hydrochloride ( RSD1235), a novel compound, for the conversion of atrial fibrillation ( AF). Methods and Results - Patients were randomized in a 2: 1 ratio to receive vernakalant or placebo and were stratified by AF du...

  13. Application of new membrane selective electrodes for the determination of drotaverine hydrochloride in tablets and plasma.

    Science.gov (United States)

    El-Saharty, Y S; Metwaly, F H; Refaat, M; El-Khateeb, S Z

    2006-06-07

    The construction and electrochemical response characteristics of poly vinyl chloride (PVC) membrane sensors for the determination of drotaverine hydrochloride were described. The sensors are based on the use of the ion association complexes of drotaverine cation with sodium phosphotungestate (Dro-PTA) or ammonium reineckate (Dro-R) counter anions as ion exchange sites in the PVC matrix. The performance characteristics of these sensors, which were evaluated according to IUPAC recommendations, reveal a fast, stable and linear response for drotaverine over the concentration range 10(-5) to 10(-2) M with cationic slopes of 49.55 and 51.36 mV per concentration decade. The direct potentiometric determination of drotaverine hydrochloride using the proposed sensors gave average recoveries of 99.95+/-0.71 and 100.04+/-0.60 for Dro-PTA and Dro-R, respectively. The sensors are used for determination of drotaverine hydrochloride in tablets, in its mixture with caffeine and paracetamol and in plasma. Validation of the method shows suitability of the proposed sensors for use in the quality control assessment of drotaverine hydrochloride. The developed method was found to be simple, accurate and precise when compared with a reported HPLC method.

  14. Effect of carrier excipient and processing on stability of indorenate hydrochloride/excipient mixtures.

    Science.gov (United States)

    Villalobos-Hernández, J R; Villafuerte-Robles, L

    2001-11-01

    The purpose of this investigation was to determine the solid-state chemical stability of a model drug, indorenate hydrochloride, as a function of carrier excipient and mixing process. Physical mixtures and granules were prepared by tumble mixing and alcoholic granulation with and without binder. Stability of the mixtures was estimated using differential scanning calorimetry and isothermal degradation studies at 40, 50, and 60 degrees C. Average first-order degradation constants at 25 degrees C, extrapolated from isothermal studies, were much lower for indorenate hydrochloride after tumbling mixing with microcrystalline cellulose (3.45 x 10(-5) day-1) than those obtained after tumbling mixing with lactose (112.0 x 10(-5) day-1). Distribution of the drug on the excipient's surface, through granulation with and without Povidone, increased the average drug degradation rates in granules with microcrystalline cellulose (36.2 x 10(-5) day-1) as well as in granules with lactose (326 x 10(-5) day-1). Partially amorphous lactose (spray-dried lactose) showed higher average degradation rates (310.5 x 10(-5) day-1) than crystalline lactose (199.3 x 10(-5) day-1). It appears that the amorphous portion of the drug as well as that of reacting excipients play a major role in affecting the reaction rate. The calorimetric studies showed a strong solid-solid interaction between indorenate hydrochloride and lactose, suggesting chemical incompatibility. This strong solid-solid interaction was characterized by disappearance of typical transition peaks of lactose at temperatures above 200 degrees C and the development of new peaks at about 130-170 degrees C. No major changes in transition peaks were observed in mixtures of microcrystalline cellulose and indorenate hydrochloride, suggesting chemical compatibility. Calorimetric results allow the prediction of the chemical incompatibility between indorenate hydrochloride and lactose observed in isothermal degradation studies.

  15. 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.

  16. Toxicity of naproxen sodium and its mixture with tramadol hydrochloride on fish early life stages.

    Science.gov (United States)

    Sehonova, Pavla; Plhalova, Lucie; Blahova, Jana; Doubkova, Veronika; Prokes, Miroslav; Tichy, Frantisek; Fiorino, Emma; Faggio, Caterina; Svobodova, Zdenka

    2017-08-31

    Pharmaceuticals occur in water bodies as a consequence of their incomplete removal during waste water treatment processes. The occurence of pharmaceuticals in surface waters as well as their possible impact on aquatic vertebrates have received considerable attention in recent years. However, there is still a lack of informations on the chronic effects of widely used drugs as well as their possible mixture toxicity on non-target aquatic vertebrates as well as their possible mixture toxicity. The aim of this study was to assess the effects of naproxen sodium on early life stages of fish and evaluate its mixture toxicity with tramadol hydrochloride, which was assessed in our earlier study as a single substance. Two embryo-larval toxicity tests with common carp (Cyprinus carpio) were performed according to the OECD guideline 210 (Fish, Early-life Stage Toxicity Test) in order to assess the subchronic toxicity of naproxen sodium and tramadol hydrochlorid-naproxen sodium mixture at the concentrations of 10; 50; 100 and 200 μg/L. These experiments were conducted for 32 days. The subchronic exposure to naproxen sodium and naproxen sodium and tramadol hydrochloride mixture had a strong effect on the early life stages of common carp. Hatching, developmental rate, morphology, histopathology and, in the case of the naproxen sodium and tramadol hydrochloride mixture, mortality were influenced. The bioindicators of oxidative stress were also influenced. The LOEC was determined at 10 μg/L for both naproxen sodium and naproxen sodium and tramadol hydrochloride mixture. Copyright © 2017. Published by Elsevier Ltd.

  17. The protecting effects and mechanism of betaine hydrochloride on hepatic ischemia-reperfusion injury in rats

    Institute of Scientific and Technical Information of China (English)

    XIN Xiao-ming; MA Lian-long; GAO Yong-feng; WANG Hao; WANG Xiao-dan; ZHU Yu-yun; GAO Yun-sheng

    2008-01-01

    Objective To study the protecting effects and mechanism of betaine hydrochloride on hepatic ischemia-reperfusion injury in rats. Methods Fourty SD rats were randomly divided into 5 groups (8 animals in each group) : sham-operated control group (A), hepatic ischemia-reperfusion group (B), 200 mg·kg-1 400 mg·kg-1 800 mg·kg-1 betaine hydrochloride + hepatic ischemia-reperfusion group (C、D、E). betaine hydrochloride was administered to animals byoral route in group C、D、E for 7 days before ischemia. A、B group was administered with NS. Made the animal model of part hepatic ischemia-reperfusion. Serum alanine aminotransferase (ALT), aspartate aminotransferase (AST) levels in the blood and themalondialdehyde (MDA), superoxide dismutase (SOD), protein content in hepatic tissue were determined after the liver had been reperfused for 24 hours; the hepatic tissue was examined under lightmieroscope and the cell apoptosis was demonstrated with flow cytometry. Results ALT, AST, MDA increased and SOD decreased significantly in B group when compared those in the A group (P<0.05), Hepatic apoptosis was significantly increased; ALT, AST, MDA decreased and SOD increased significantly in betaine hydrochloride 200 mg·kg-1(C) group when compared those in the B group(P<0.05). Hepatic apoptosis was significantly lower, The histologic changes of the liver tissue under lightmicroscope in the C group was more easer than in the I/R group (B). Conclusions Betaine hydrochloride has the ability to scavenge oxygen free radical (OFR), reduce lipid peroxidation and inhibition of apoptosis. So it can protect the rats liver damaged by ischemia-reperfusion.

  18. Effects of Xiaoaiping injection combined with mitomycin on lung cancer cells in vitro%消癌平辅助丝裂霉素对肺癌细胞化疗增效的研究

    Institute of Scientific and Technical Information of China (English)

    谢泽新; 杨杨; 王金烁

    2016-01-01

    Objective To observe the effects of Xiaoaiping injection combined with mitomycin on cell proliferation, cell cycle, cell apoptosis and expressions of related genes (CyclinD1,P53 mRNA) of lung cancer-A549 cells in vitro,and to explore potential action mechanism.Methods The inhibitory effects of Xiaoaiping injection (2,8,21μl/ml) combined with mitomycin (2μg/nl) were detected by MTT (combination treatment group A,B,C),moreover, control group, Xiaoaiping group and mitomycin group were established.The cell cycle and cell apoptosis of lung cancer-A549 cells in vitro were detected by cytometry,and the expression levels of CyclinD1 and P53 mRNA were measured by RT-PCR.Results The results by MTT showed that the optical density value (OD) on 24h,48h,72h in combination treatment group A,B,C was significantly higher than that in mitomycin group ( P <0.05).The results by cytometry showed that as compared with control group,the lung cancer cells were blocked at G0/G1 phase in Xiaoaiping group and mitomycin group ( P <0.05).There were significant differences in the cell ratio at G0 /G1 phase and cell apoptosis rate between combination treatment groups and mitomycin group ( P <0.05).The expression levels of P53 mRNA in Xiaoaiping group and mitomycin group were significantly increased,as compared with those in control group ( P <0.05).Moreover the expression levels of P53 mRNA in combination treatment groups were significantly higher than those in mitomycin group ( P <0.05).The expression levels of Cyclin D1 in Xiaoaiping group and mitomycin group were significantly decreased,as compared with those in control group ( P <0.05).Furthermore the expression levels of Cyclin D1 in combination treatment groups were significantly decreased,as compared with those in mitomycin group ( P <0.05).Conclusion Xiaoaiping injection combined with mitomycin can enhance the efficiency of chemotherapy on lung cancer-A549 cells in vitro,and the action mechanism may be correlated to up -regulating the

  19. Effects of mitomycin C on apoptosis of hypertrophic scar fibroblasts%丝裂霉素C影响增生性瘢痕成纤维细胞的凋亡

    Institute of Scientific and Technical Information of China (English)

    吴晓明; 孙奎; 张宏霞; 孙喜平; 耿琪瑛; 李树松

    2012-01-01

    BACKGROUND: Mitomycin C has been gradually used in hyperplastic scar therapy. But the molecular mechanism underlying the effects of mitomycin C on hyperplastic scar via cell apoptosis is reported few. OBJECTIVE: To explore the effects of mitomycin C on fibroblasts apoptosis in hypertrophic scar. METHODS: Hypertrophic scar fibroblasts were cultured in vitro with five different concentrations of mitomycin C (2.5, 12.5, 50, 100, 200 mg/L). Cell cycle distribution and apoptosis of fibroblasts were detected by Annexin V-PI, and the protein expression levels of Bax and Bcl-2 in fibroblasts were detected with Western blotting. RESULTS AND CONCLUSION: Mitomycin C blocked the growth of hyperplastic scar fibroblasts in G0/G1 period, and induced apoptosis of hyperplastic scar fibroblasts in an obvious concentration-dependent manner. Bax protein expression levels increased and Bcl-2 protein expression levels decreased in hyperplastic scar fibroblasts after treated with 2.5-200 mg/L mitomycin C for 24 hours (P < 0.05). These findings indicate that mitomycin C has the possibility to promote fibroblasts apoptosis through increasing Bax expression and decreasing Bcl-2 expression in hyperplastic scar fibroblasts.%背景:丝裂霉素C已逐渐开始应用于治疗增生性瘢痕领域中,但针对丝裂霉素C通过细胞凋亡作用于增生性瘢痕分子机制报道很少.目的:探讨丝裂霉素C对增生性瘢痕成纤维细胞凋亡的影响.方法:应用2.5,12.5,50,100和200 mg/L 丝裂霉素C作用于体外培养的增生性瘢痕成纤维细胞,采用流式细胞仪检测成纤维细胞的周期分布和凋亡情况;通过Western blot法检测细胞中Bax和Bcl-2蛋白表达水平.结果与讨论:丝裂霉素C可使增生性瘢痕成纤维细胞的生长阻滞于G0/G1期,并且能够诱导增生性瘢痕成纤维细胞发生凋亡,有着明显的浓度依赖性.经2.5~200 mg/L丝裂霉素C作用24 h后,增生性瘢痕成纤维细胞中Bax蛋白表达增高,Bcl-2

  20. Mitomycin-treated undifferentiated embryonic stem cells as a safe and effective therapeutic strategy in a mouse model of Parkinson's disease.

    Science.gov (United States)

    Acquarone, Mariana; de Melo, Thiago M; Meireles, Fernanda; Brito-Moreira, Jordano; Oliveira, Gabriel; Ferreira, Sergio T; Castro, Newton G; Tovar-Moll, Fernanda; Houzel, Jean-Christophe; Rehen, Stevens K

    2015-01-01

    Parkinson's disease (PD) is an incurable progressive neurodegenerative disorder. Clinical presentation of PD stems largely from the loss of dopaminergic neurons in the nigrostriatal dopaminergic pathway, motivating experimental strategies of replacement based on cell therapy. Transplantation of dopaminergic neurons derived from embryonic stem cells significantly improves motor functions in rodent and non-human primate models of PD. However, protocols to generate dopaminergic neurons from embryonic stem cells generally meet with low efficacy and high risk of teratoma formation upon transplantation. To address these issues, we have pre-treated undifferentiated mouse embryonic stem cells (mESCs) with the DNA alkylating agent mitomycin C (MMC) before transplantation. MMC treatment of cultures prevented tumorigenesis in a 12 week follow-up after mESCs were injected in nude mice. In 6-OH-dopamine-lesioned mice, intrastriatal injection of MMC-treated mESCs markedly improved motor function without tumor formation for as long as 15 months. Furthermore, we show that halting mitotic activity of undifferentiated mESCs induces a four-fold increase in dopamine release following in vitro differentiation. Our findings indicate that treating mESCs with MMC prior to intrastriatal transplant is an effective to strategy that could be further investigated as a novel alternative for treatment of PD.

  1. Prolonged rest period enables the detection of micronucleated hepatocytes in the liver of young adult rats after a single dose of diethylnitrosamine or mitomycin C.

    Science.gov (United States)

    Shimada, Keisuke; Yamamoto, Mika; Takashima, Miyuki; Seki, Jiro; Miyamae, Yoichi; Wakata, Akihiro

    2015-09-01

    A repeated-dose micronucleus assay utilizing young adult rat hepatocytes was recently developed to evaluate the genotoxicity. In this assay, accumulation of micronucleated hepatocytes (MNHEPs) induced by repeated dosing of genotoxic chemicals is considered to be a key factor in the detection of micronuclei induction. Then, we hypothesized that the period following chemical exposure enable the detection of MNHEP induction in young adult rats, namely that MNHEPs can be generated from chromosomally damaged cells and accumulate following initiation of chemical exposure until sampling. We therefore measured MNHEP induction at 2 or 4 weeks after a single oral administration of 12.5, 50, or 100mg/kg of diethylnitrosamine (DEN) or an intraperitoneal administration of 0.5, 1.0, or 2.0mg/kg of mitomycin C (MMC) to young adult rats. Results showed a statistically significant, dose-dependent increase in the numbers of MNHEPs in DEN- or MMC-treated rats, indicating that prolonged rest period following a single dose of a genotoxic chemical enables the detection of MNHEP induction in the liver of young adult rats. From these results, a single oral administration of 50mg/kg of DEN with a 2- or 4- week rest period can be used as a positive control in repeated-dose liver micronucleus assays. This procedure is superior in terms of labor saving and animal welfare to repeated dosing of DEN.

  2. Controlled release of 5-fluorouracil or mitomycin-c from polymer matrix: Preparation by radiation polymerization and in vivo evaluation of the anticancer drug/polymer composites

    Science.gov (United States)

    Li, Ximing; Shen, Weiming; Liu, Chengjie; Nishimoto, Sei-Ichi; Kagiya, Tsutomu

    Polymer tablets containing anticancer drugs such as 5-fluorouracil (5-FU) and mitomycin-C (MMC) have been prepared to evaluate the drug-release characteristics in vitro and the effect on local control of mouse solid tumors in vivo. Radiation-induced polymerization of hydrophilic monomers (2-hydroxyethyl methacrylate and related monomers) at low temperature (-80°C) was performed to immobilize 5-FU or MMC in the polymer matrix. The drug was dispersed as microcrystallines within the polymer matrix. The rate of drug release in vitro in buffer solution (pH7.0, 37°C) increased with increase in hydrophilicity of polymer matrix. Appropriate amount of crosslinks within the polymer matrix, as formed by ethylene glycol dimethacrylate (2G) added in the polymerization system, was effective to control the rate of drug release. The drug release became faster upon the addition of increasing amount of water in the radiation-induced polymerization. The tablet consisting of drug/polymer was buried surgically near solid tumors of striate muscle sarcoma (S180) transplanted to Kunming mice and the therapeutic effect of slow releasing drugs was evaluated in vivo by reference to intraperitoneal (i.p.) injection of the corresponding drugs. The slow releasing drugs led to high chemotherapeutic gain for local control of solid tumors with remarkable reduction of toxic side effect of the drugs.

  3. Identification of Escherichia coli ygaQ and rpmG as novel mitomycin C resistance factors implicated in DNA repair.

    Science.gov (United States)

    Bolt, Edward L; Jenkins, Tabitha; Russo, Valeria Moreira; Ahmed, Sharlene; Cavey, James; Cass, Simon D

    2015-12-24

    Using the ASKA (A Complete Set of Escherichia coli K-12 ORF Archive) library for genome-wide screening of E. coli proteins we identified that expression of ygaQ and rpmG promotes mitomycin C resistance (MMC(R)). YgaQ mediated MMC(R) was independent of homologous recombination involving RecA or RuvABC, but required UvrD. YgaQ is an uncharacterized protein homologous with α-amylases that we identified to have nuclease activity directed to ssDNA of 5' flaps. Nuclease activity was inactivated by mutation of two amino acid motifs, which also abolished MMC(R). RpmG is frequently annotated as a bacterial ribosomal protein, although forms an operon with MutM glycosylase and a putative deubiquitinating (DUB) enzyme, YicR. RpmG associated MMC(R) was dependent on MutM. MMC(R) from RpmG resembles DNA repair phenotypes reported for 'idiosyncratic ribosomal proteins' in eukaryotes.

  4. Effect of mitomycin C therapy on dacryocystorhinostomy%丝裂霉素应用于鼻腔泪囊吻合术疗效探讨

    Institute of Scientific and Technical Information of China (English)

    鄢秀菊; 吴成富

    2002-01-01

    目的探讨丝裂霉紊C(mitomycin C,MMC)对泪囊鼻腔吻合术的效果.方法将41只眼慢性泪囊炎随机分为MMC组18只眼和对照组23只眼,MMC组术中应用0,4mg/ml MMC,对照组采用常规泪囊鼻腔吻合术,术后平均随访30个月.结果治愈率:MMC组与对照组分别为94.11%,78.26%,(P<0.05).结论 MMC可作为治疗慢性泪囊炎的一种安全、简单、有效的辅助药物,应用于鼻腔泪囊吻合术中,大大提高了新造孔道通畅的可能性.

  5. 人肝脏微粒体在体外对丝裂霉素C的代谢%Metabolism of mitomycin C by human liver microsomes in vitro

    Institute of Scientific and Technical Information of China (English)

    郝福荣; 严敏芬; 胡卓汉; 金一尊

    2007-01-01

    丝裂霉素C(mitomycin C,MMC)是一种醌类DNA烷化剂,是生物还原活性物的代表之一,也是临床常用的化疗药物,被广泛用于治疗膀胱癌、乳腺癌、头颈部癌、非小细胞肺癌等。作为MMC与肝脏药物代谢酶相互作用的两个方面,作者曾发表了MMC对肝脏3种细胞色素P450同工酶活性影响的报道。已往关于MMC代谢酶学的研究材料主要使用动物肝脏微粒体及纯化酶、体外肿瘤细胞系和/或肿瘤组织,而人肝脏药物代谢酶对MMC代谢的研究尚未见报道。本实验用体外方法初步研究了人肝脏微粒体对MMC的代谢作用。

  6. Functional hyper-IL-6 from vaccinia virus-colonized tumors triggers platelet formation and helps to alleviate toxicity of mitomycin C enhanced virus therapy

    Directory of Open Access Journals (Sweden)

    Sturm Julia B

    2012-01-01

    Full Text Available Abstract Background Combination of oncolytic vaccinia virus therapy with conventional chemotherapy has shown promise for tumor therapy. However, side effects of chemotherapy including thrombocytopenia, still remain problematic. Methods Here, we describe a novel approach to optimize combination therapy of oncolytic virus and chemotherapy utilizing virus-encoding hyper-IL-6, GLV-1h90, to reduce chemotherapy-associated side effects. Results We showed that the hyper-IL-6 cytokine was successfully produced by GLV-1h90 and was functional both in cell culture as well as in tumor-bearing animals, in which the cytokine-producing vaccinia virus strain was well tolerated. When combined with the chemotherapeutic mitomycin C, the anti-tumor effect of the oncolytic virotherapy was significantly enhanced. Moreover, hyper-IL-6 expression greatly reduced the time interval during which the mice suffered from chemotherapy-induced thrombocytopenia. Conclusion Therefore, future clinical application would benefit from careful investigation of additional cytokine treatment to reduce chemotherapy-induced side effects.

  7. 术前与术中应用丝裂霉素C对复发性翼状胬肉的疗效比较%Comparison of the curative effects of preoperative and intraoperative application of mitomycin C on recurrent pterygi-um

    Institute of Scientific and Technical Information of China (English)

    高建伟; 张阿芳

    2014-01-01

    Objective To observe the efficacy of subconjunctival injection of mitomycin C one day before surgery in the man-agement of recurrent pterygium. Methods Thirty-eight eyes with recurrent ptergium were randomly divided into two groups,the mitomycin injection group(19 eyes)and the mitomycin application group(19 eyes). The mitomycin injection group underwent preoperative subconjunctival injection of mitomycin C in low dose(0. 1 ml of 0. 15 mg/ml)1 day before bare sclera pterygium excision surgery. The mitomycin application group underwent bare sclera pterygium excision with topical application of mitomycin C(same concentration). Results After one year of followed-up,1 of 19 eyes(5%)in the mitomycin injiection group and 5 of 19 eyes(21%)in the mitomycin application group were free of reoccurrence,the difference was statistically significant( P﹤0. 05). As regards postoperative comlications,delayed epithelization(more than 2 weeks)occurred in 2 eyes(11%)in the mit-omycin injection group and in 5 eyes(26%)in the mitomycin application group. Scleral thinning was reported in 1 eye(5%)in the mitomycin application group which resolved within 3 weeks after surgery. Conclusion Preoperative subconjunctival injection of mitomycin C in low dose(0. 1 ml of 0. 15 mg/ml)1 day before pterygium surgery is a simple and effective modality for man-agement of recurrent pterygium. It has the advantage of low recurrence and complications rate.%目的:观察术前1天局部注射丝裂霉素C对复发性翼状胬肉的疗效。方法38例复发性翼状胬肉患者分为注射组和贴敷组,注射组19例在翼状胬肉切除术前1天将低浓度(0.15 mg/ml)丝裂霉素C溶液0.1 ml注入瘤体内,贴敷组19例在翼状胬肉切除术中将同样剂量的丝裂霉素C溶液棉片置于裸露巩膜区3 min。结果经过1年随访,注射组复发1例(5%),贴敷组复发4例(21%),两组比较差异有统计学意义( P﹤0.05)。术后并发症:注射组中2

  8. Multimorphologies of hydrochloride polyaniline synthesized by conventional and interfacial polymerization

    Science.gov (United States)

    Ferreira, André A.; Sanches, Edgar A.

    2017-09-01

    The aim of this paper is to analyze the structure and morphology of the hydrochloride Polyaniline Emeraldine-salt form (PANI-ES) synthesized by conventional (PANI-ES/C1 and PANI-ES/C2) and interfacial (PANI-ES/I1 and PANI/ES/I2) polymerization using HCl 1 M and 2 M. The X-ray diffraction patterns (XRD) of PANI-ES/I1 and PANI-ES/I2 have presented higher crystallinity. Furthermore, the peak located at 2θ = 18.3° has not been reported in scientific literature. PANI-ES/C1 and PANI-ES/C2 presented closed crystallinity percentage around 50 (±2) %, while PANI-ES/I1 and PANI-ES/I2 presented, respectively, 55 (±2) % and 63 (±2) % of crystallinity. However, PANI-ES/C2, PANI-ES/I1 and PANI-ES/I2 have presented larger ;b; unit cell parameter, from 8.9021 Å (PANI-ES/C1) to ∼16.2931 Å, due to the more efficient doping of the chloride ions. Fourier-transform Infrared Spectroscopy technique (FTIR) was useful to evaluate significant changes in the quinoid (Q) and benzenoid (B) bands: PANI-ES/C1 and PANI-ES/C2 presented the ratio Q/B, respectively, 0.4 and 0.6, indicating that the doping level by exposure to a higher dopant concentration has increased. An even more intense dopant action was verified in PANI-ES/I1 and PANI-ES/I2, presenting Q/B ratios of 0.7 and 0.9, respectively. These results reveal the more efficient doping level provided by the interfacial polymerization. Scanning Electron Microscopy (SEM) images showed that PANI-ES/C1 presented short nanofibers, while PANI-ES/C2 showed nanofibers length and diameter, respectively, around 61% and 13% higher than those found in PANI-ES/C1. However, PANI-ES/I1 and PANI-ES/I2 presented four different types of morphologies (nanoplates, nanorods, nanofibers and nanoflowers) due to the peculiarity of this polymerization method. The difference of length and diameter between PANI-ES/C1 and PANI-ES/I2 nanofibers reaches 64% and 52%, respectively. Thermogravimetric Analysis (TGA) showed that the event related to the dopant release

  9. Does yohimbine hydrochloride facilitate fear extinction in virtual reality treatment of fear of flying? A randomized placebo-controlled trial

    NARCIS (Netherlands)

    Meyerbroeker, K.; Powers, M.B.; van Stegeren, A.; Emmelkamp, P.M.G.

    2012-01-01

    BACKGROUND: Research suggests that yohimbine hydrochloride (YOH), a noradrenaline agonist, can facilitate fear extinction. It is thought that the mechanism of enhanced emotional memory is stimulated through elevated noradrenaline levels. This randomized placebo-controlled trial examined the

  10. Antioxidant and antimicrobial activity of Maillard reaction products from xylan with chitosan/chitooligomer/glucosamine hydrochloride/taurine model systems.

    Science.gov (United States)

    Wu, Shuping; Hu, Jiao; Wei, Liuting; Du, Yumin; Shi, Xiaowen; Zhang, Lina

    2014-04-01

    The structure, UV absorbance, browning intensity, fluorescence changes, antioxidant activity and antimicrobial assessment of Maillard reaction products (MRPs) derived from xylan with chitosan, chitooligomer, glucosamine hydrochloride and taurine model systems were evaluated. The results revealed that all MRPs had similar infrared spectra and molecular structures. MRPs from different model systems on the UV absorbance at 294 nm after heated 90 min and browning intensity at 420 nm showed the similar law: xylan-taurine > xylan-glucosamine hydrochloride > xylan-chitooligomer > xylan-chitosan, and the order of DPPH scavenging activity of MRPs was as follows: xylan-chitosan > xylan-chitooligomer > xylan-glucosamine hydrochloride > xylan-taurine, which revealed that the properties of MRPs were closely related to molecular weight of model systems. Moreover, the highest radical scavenging activity of MRPs from xylan with chitosan/chitooligomer/glucosamine hydrochloride/taurine model systems was 65.9%, 63.7%, 46.4% and 42.5%, respectively.

  11. Application of physiologically based pharmacokinetic modeling in predicting drug–drug interactions for sarpogrelate hydrochloride in humans

    Directory of Open Access Journals (Sweden)

    Min JS

    2016-09-01

    Full Text Available Jee Sun Min,1 Doyun Kim,1 Jung Bae Park,1 Hyunjin Heo,1 Soo Hyeon Bae,2 Jae Hong Seo,1 Euichaul Oh,1 Soo Kyung Bae1 1Integrated Research Institute of Pharmaceutical Sciences, College of Pharmacy, The Catholic University of Korea, Bucheon, 2Department of Pharmacology, College of Medicine, The Catholic University of Korea, Seocho-gu, Seoul, South Korea Background: Evaluating the potential risk of metabolic drug–drug interactions (DDIs is clinically important. Objective: To develop a physiologically based pharmacokinetic (PBPK model for sarpogrelate hydrochloride and its active metabolite, (R,S-1-{2-[2-(3-methoxyphenylethyl]-phenoxy}-3-(dimethylamino-2-propanol (M-1, in order to predict DDIs between sarpogrelate and the clinically relevant cytochrome P450 (CYP 2D6 substrates, metoprolol, desipramine, dextromethorphan, imipramine, and tolterodine. Methods: The PBPK model was developed, incorporating the physicochemical and pharmacokinetic properties of sarpogrelate hydrochloride, and M-1 based on the findings from in vitro and in vivo studies. Subsequently, the model was verified by comparing the predicted concentration-time profiles and pharmacokinetic parameters of sarpogrelate and M-1 to the observed clinical data. Finally, the verified model was used to simulate clinical DDIs between sarpogrelate hydrochloride and sensitive CYP2D6 substrates. The predictive performance of the model was assessed by comparing predicted results to observed data after coadministering sarpogrelate hydrochloride and metoprolol. Results: The developed PBPK model accurately predicted sarpogrelate and M-1 plasma concentration profiles after single or multiple doses of sarpogrelate hydrochloride. The simulated ratios of area under the curve and maximum plasma concentration of metoprolol in the presence of sarpogrelate hydrochloride to baseline were in good agreement with the observed ratios. The predicted fold-increases in the area under the curve ratios of metoprolol

  12. A randomized, crossover design study of sevelamer carbonate powder and sevelamer hydrochloride tablets in chronic kidney disease patients on haemodialysis

    OpenAIRE

    Fan, Stanley; Ross, Calum; Mitra, Sandip; Kalra, Philip; Heaton, Jeremy; Hunter, John; Plone, Melissa; Pritchard, Nick

    2009-01-01

    Background. Sevelamer carbonate is an improved, buffered form of sevelamer hydrochloride developed for the treatment of hyperphosphataemia in CKD patients. Sevelamer carbonate formulated as a powder for oral suspension presents a novel, patient-friendly alternative to tablet phosphate binders. This study compared the safety and efficacy of sevelamer carbonate powder with sevelamer hydrochloride tablets in CKD patients on haemodialysis. Methods. This was a multi-centre, open-label, randomized,...

  13. Berberine hydrochloride attenuates lipopolysaccharide-induced endometritis in mice by suppressing activation of NF-κB signal pathway.

    Science.gov (United States)

    Fu, Kaiqiang; Lv, Xiaopei; Li, Weishi; Wang, Yu; Li, Huatao; Tian, Wenru; Cao, Rongfeng

    2015-01-01

    Endometritis is a common disease in animal production and influences breeding all over the world. Berberine is one of the main alkaloids isolated from Rhizoma coptidis. Previous reports showed that berberine has anti-inflammatory potential. However, there have been a limited number of published reports on the anti-inflammatory effect of berberine hydrochloride on LPS-induced endometritis. The purpose of the present study was to investigate the effects of berberine hydrochloride on LPS-induced mouse endometritis. Berberine hydrochloride was administered intraperitoneally at 1h before and 12h after LPS induction. Then, a biopsy was performed, and uterine myeloperoxidase (MPO) and nitric oxide (NO) concentrations were determined. Tumor necrosis factor-α (TNF-α) and interleukin-1β (IL-1β) levels in the uterus homogenate were measured by ELISA. The extent of IκB-α and P65 phosphorylation was detected by Western blot. The results showed that berberine hydrochloride significantly attenuated neutrophil infiltration, suppressed myeloperoxidase activity and decreased NO, TNF-αand IL-1βproduction. Furthermore, berberine hydrochloride inhibited the phosphorylation of the NF-κB p65 subunit and the degradation of its inhibitor, IκBα. These findings suggest that berberine hydrochloride exerts potent anti-inflammatory effects on LPS-induced mouse endometritis and might be a potential therapeutic agent for endometritis.

  14. Formulation and evaluation of hydroxyzine hydrochloride sustained release microspheres by ionotropic gelation technique using Carbopol 934P

    Directory of Open Access Journals (Sweden)

    Soumyadeep Ghosh

    2014-01-01

    Full Text Available Preparation of sustained release microspheres of hydroxyzine hydrochloride by ionotropic gelation technique and evaluation. Microspheres of hydroxyzine hydrochloride were prepared by ionotropic gelation method using sodium alginate, Carbopol 934P and calcium chloride. The powders were evaluated for their flow properties. Hydroxyzine hydrochloride microspheres were characterized by Fourier transform infrared and in vitro dissolution studies. The drug release study of hydroxyzine hydrochloride microspheres was evaluated using basket type dissolution test apparatus. The release rate of Hydroxyzine hydrochloride microspheres was studied for 12 h in pH 7.4 phosphate buffer media. From the five batches F5 batch showed good release behavior 91.08% of drug is released over 12 h, and r2 = 0.987 in zero-order kinetics. The microspheres were prepared without the use of organic solvents. Microspheres of hydroxyzine hydrochloride decrease the incidence of side effects and also improve patient compliance by reducing the number of dosing and by reducing the fluctuations of drug in the blood. This entire attributed attitude proves that microsphere technology from novel drug delivery can be very much effective in reducing dosage frequency, dose dumping, and better patient compliance and economical to the patient. In the future, natural, biodegradable polymers can be used to improve therapeutic efficacy of the drug and further minimizing side-effects.

  15. [A prospective multicenter randomized controlled clinical study on the efficacy and safety of Guaifenesin compound pseudoephedrine hydrochloride oral solution].

    Science.gov (United States)

    Lu, Quan

    2010-03-01

    To evaluate efficacy and safety of Guaifenesin compound pseudoephedrine hydrochloride oral solution for the treatment of cough, expectoration, nasal congestion and runny nose in children. This was a prospective multicenter randomized single-blind, parallel-controlled clinical study. A total of 10 centers participated in this study, the actual number of cases in line with the program was 412, of whom 205 cases in trial group were treated with Guaifenesin compound pseudoephedrine hydrochloride oral solution, and 207 cases in control group with ambroxol hydrochloride oral solution, treatment of both groups persisted for 7 days. The improvement rate of each single symptom and the combined symptoms and the overall effective rate were compared between the two groups. The adverse drug reactions and compliance were assessed as well. The treatment of both groups showed efficacy. Except sputum stickiness, the improvement of all symptoms in trial group was superior to that in the control group on the 3rd day after treatment (P Guaifenesin compound pseudoephedrine hydrochloride oral solution was 82.9% and the overall efficacy rate was 89.3%. Guaifenesin compound Pseudoephedrine hydrochloride oral solution had higher compliance and its adverse event rate was merely 0.92%. Guaifenesin compound pseudoephedrine hydrochloride oral solution showed significant efficacy and safety in children for treatment of cough, expectoration, nasal congestion and runny nose caused by common cold or acute tracheobronchitis.

  16. 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).

  17. Determination of ivabradine hydrochloride in Ivabradine Hydrochloride Tablets by HPLC%HPLC法测定盐酸伊伐布雷定片含量

    Institute of Scientific and Technical Information of China (English)

    杨晓莉; 张琼; 李辉

    2012-01-01

    Objective To establish an HPLC method for the determination of ivabradine hydrochloride in Ivabradine Hydrochloride Tablets. Methods The column C18 Inertsil ODS-3(250 mm ×4. 6 mm,5 μm) was used. The mobile phase consisted of buffer phos-phate(pH7. 6)- acetonitrile(60 : 40) ,flow rate was 1. 0 mL o min-1 ,the detection wavelength was set at 286 nm,and the column temperature was 25 ℃. Results The linearity of peak area was good when the sample content was in the range of 2. 32-16. 25 μg(r= 0. 999 9). The average recovery was 101. 3% with RSD 1. 2%(n = 9). Conclusions The method is accurate,reliable and simple,and it can be used in the determination of ivabradine hydrochloride in Ivabradine Hydrochloride Tablets.%目的 建立HPLC法测定盐酸伊伐布雷定片的含量.方法 采用C18 Inertsil ODS-3(250 mm ×4.6 mm,5 μm)色谱柱,流动相为磷酸盐缓冲液(pH7.6)-乙腈(60∶40),流速为1.0 mL·min-1,检测波长为286 nm,柱温25 ℃.结果 盐酸伊伐布雷定线性范围为2.32~16.25 μg,峰面积与进样量线性关系良好(r=0.999 9);平均回收率为101.3%,其RSD为1.2% (n=9).结论 该方法准确、可靠、简便,适用于盐酸伊伐布雷定片的含量测定.

  18. Preparation and characterisation of mucoadhesive nasal gel of venlafaxine hydrochloride for treatment of anxiety disorders

    Directory of Open Access Journals (Sweden)

    Shyamoshree Basu

    2012-01-01

    Full Text Available The aim of the present study is to prepare and evaluate mucoadhesive nasal gels of venlafaxine hydrochloride. Mucoadhesive nasal gels were prepared using polymers like carbopol 934 and sodium alginate and characterized in terms of viscosity, texture profile analysis, ex vivo drug permeation profiles and histopathological studies. The results show that values of viscosity, hardness and adhesiveness increase while those of cohesiveness decrease with corresponding increase in concentration of the polymers. Ex vivo drug permeation profiles showed that formulation containing 5% sodium alginate provided a better controlled release of the drug than the other formulations over a period of 12 h. Histopathological studies assured that gels containing different polymers did not produce any significant change in the nasal mucosae of goat even after 12 h permeation study. Mucoadhesive nasal gel of venlafaxine hydrochloride is a novel dosage form which delivers the drug directly into systemic circulation and provides controlled release of the drug.

  19. SIMULTANEOUS ESTIMATION & VALIDATION OF PARACETAMOL, PHENYLEPHRINE HYDROCHLORIDE AND CHLORPHENIRAMINE MALEATE IN TABLETS BY SPECTROPHOTOMETRIC METHOD

    Directory of Open Access Journals (Sweden)

    R. SAWANT, R. JOSHI, P. LANKE L. BHANGALE

    2013-09-01

    Full Text Available The present work describes two methods for simultaneous estimation of phenylephrine hydrochloride and chlorpheniramine maleate in pure and solid dosage forms. First method employs the application of simultaneous equation and second, is a multi-wavelength spectrophotometric analysis method. Both methods utilize 0.1N NaOH as solvent. Simultaneous equation develops using 256.8 nm, 236.8 nm and 222.4 nm as the max of paracetamol, phenylephrine hydrochloride and chlorpheniramine maleate respectively. Calibration curves were linear over the concentration ranges of 0-35 μg/mL for all drugs. The results demonstrated that the procedure is accurate, precise and reproducible (relative standard deviation < 1 %, while being simple, cheap and less time consuming, and hence can be suitably applied for simultaneous determination of three drugs in laboratory prepared mixtures and in commercial tablet preparation.

  20. Electron paramagnetic resonance and FT-IR spectroscopic studies of glycine anhydride and betaine hydrochloride

    Science.gov (United States)

    Halim Başkan, M.; Kartal, Zeki; Aydın, Murat

    2015-12-01

    Gamma irradiated powders of glycine anhydride and betaine hydrochloride have been investigated at room temperature by electron paramagnetic resonance (EPR). In these compounds, the observed paramagnetic species were attributed to the R1 and R2 radicals, respectively. It was determined that the free electron interacted with environmental protons and 14N nucleus in both radicals. The EPR spectra of gamma irradiated powder samples remained unchanged at room temperature for two weeks after irradiation. Also, the Fourier Transform Infrared (FT-IR), FT-Raman and thermal analyses of both compounds were investigated. The functional groups in the molecular structures of glycine anhydride and betaine hydrochloride were identified by vibrational spectroscopies (FT-IR and FT-Raman).

  1. Double-blind study of benzydamine hydrochloride, a new treatment for sore throat.

    Science.gov (United States)

    Wethington, J F

    1985-01-01

    Forty-four patients with sore throat participated in a placebo-controlled, double-blind clinical trial of benzydamine hydrochloride administered as a gargle. After medical evaluation and throat culture, 21 patients were treated with a solution containing benzydamine and 23 patients with a placebo solution. Statistical analysis of scores from patients' diaries showed that benzydamine solution afforded significantly greater (P less than 0.001) relief of pain and dysphagia at 24 hours than did the placebo solution. Physician evaluations at 24 hours showed that the benzydamine solution had significantly greater effect than did placebo on hyperemia (P less than 0.004) and edema (P less than 0.005). Side effects were minimal and of no clinical significance. The findings indicate that benzydamine hydrochloride is safe and effective therapy for the signs and symptoms of sore throat.

  2. Development and Evaluation of Extended Release Formulation of Tramadol Hydrochloride Based on Osmotic Technology

    Directory of Open Access Journals (Sweden)

    Patel JB

    2013-05-01

    Full Text Available Extended release formulation of Tramadol Hydrochloride based on osmotic technology was developedand evaluated. Target release profile was selected and different variables were optimized to achieve it.Formulation variables such as osmotic agent, plasticizer and coating thickness of semi-permeablemembrane were found to markedly affect drug release. Tramadol hydrochloride release was directlyproportional to the level of osmogent and plasticizer but inversely proportional to the level of coatingthickness of semi-permeable membrane. Drug release from developed formulation was independent ofpH and agitation intensity but dependent on osmotic pressure of release media. The optimizedformulation was compared with marketed product CONTRAMAL SR and accelerated stability studywas also carried out for 6 months.

  3. Spectroscopic Study on Interaction of β-Cyclodextrin with Triprolidine Hydrochloride

    Institute of Scientific and Technical Information of China (English)

    ALI Syed Mashhood; ASMAT Fahmeena

    2006-01-01

    The complexation of triprolidine hydrochloride (TRP) and β-cyclodextrin (β-CD) in deuterium oxide was investigated by 400 MHz 1H NMR spectroscopy. The 800 MHz 2D ROESY data reveaed that two 1 : 1 and one 2: 1β-CD-TRP inclusion complexes were formed. Both aromatic moieties (p-tolyl and pyridyl ring) has entered into the β-CD cavity, confirming the existence of two different equilibria for 1: 1 inclusion complexes in which p-tolyl ring of the guest is more tightly held by the host cavity. The ROE intermolecular interactions provided the plausible structures of these 1: 1 and 2: 1 stoichiometric inclusion complexes of β-CD-triprolidine hydrochloride in solution.

  4. 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.

  5. Transdermal delivery of betahistine hydrochloride using microemulsions: physical characterization, biophysical assessment, confocal imaging and permeation studies.

    Science.gov (United States)

    Hathout, Rania M; Nasr, Maha

    2013-10-01

    Transdermal delivery of betahistine hydrochloride encapsulated in various ethyl oleate, Capryol 90(®), Transcutol(®) and water microemulsion formulations was studied. Two different kinds of phase diagrams were constructed for the investigated microemulsion system. Pseudoplastic flow that is preferable for skin delivery was recorded for the investigated microemulsions. A balanced and bicontinuous microemulsion formulation was suggested and showed the highest permeation flux (0.50±0.030mgcm(-2)h(-1)). The effect of the investigated microemulsions on the skin electrical resistance was used to explain the high permeation fluxes obtained. Confocal laser scanning microscopy was used to confirm the permeation enhancement and to reveal the penetration pathways. The results obtained suggest that the proposed microemulsion system highlighted in the current work can serve as a promising alternative delivery means for betahistine hydrochloride.

  6. Formulation and evaluation of bilayer tablet for bimodal release of venlafaxine hydrochloride

    OpenAIRE

    2015-01-01

    The aim of the present research was to develop a bilayer tablet of venlafaxine hydrochloride for bimodal drug release. In the present investigation authors have tried to explore fenugreek mucilage (FNM) for bioadhesive sustained release layer. The attempt has been made to combine FNM with well studied bioadhesive polymers like hydroxy propyl methyl cellulose (HPMC), Carbopol, and Xanthan Gum. The formulations were evaluated for swelling Index, ex vivo bioadhesion, water uptake studies, in vit...

  7. Derivatives of benzimidazole: vasodilator activity of 2-(p-chloro-alpha-hydroxybenzyl)-benzimidazole hydrochloride. Preliminary study.

    Science.gov (United States)

    Demenge, P; Carraz, G; Luu Duc, C; Silice, C

    1979-01-01

    The effects of 2-(p-chloro-alpha-hydroxybenzyl)-benzimidazole hydrochloride (HBBPC) have been studied in the rabbit and rat. Most of these studies were performed comparatively with reference vasodilators and papaverine. HBBPC vasodilator activity is nearly the same as that of papaverine in the isolated rabbit ear. The characteristic of the vasoactive action of HBBPC seems to reside in its duration. The mechanism of action of HBBPC seems of peripheral type, that is to say it acts on the vascular smooth muscle.

  8. Pupil Dilation with Intracameral Epinephrine Hydrochloride during Phacoemulsification and Intraocular Lens Implantation

    Science.gov (United States)

    Yu, A-Yong; Guo, Hua; Wang, Qin-Mei; Bao, Fang-Jun; Huang, Jing-Hai

    2016-01-01

    Objective. To investigate mydriatic effect of intracamerally injected epinephrine hydrochloride during phacoemulsification and intraocular lens (IOL) implantation. Methods. Eighteen cataract patients for bilateral phacoemulsification were enrolled. To dilate pupil, one eye was randomly selected to receive intracamerally 1 mL epinephrine hydrochloride 0.001% for 1 minute after corneal incision (intracameral group), and the contralateral eye received 3 drops of compound tropicamide 0.5% and phenylephrine 0.5% at 5-minute intervals 30 minutes before surgery (topical group). Pupil diameters were measured before corneal incision, before ophthalmic viscoelastic device (OVD) injection, after OVD injection, before IOL implantation, and at the end of surgery. Results. At each time point, the mean pupil diameter in the intracameral group was 2.20 ± 0.08, 5.09 ± 0.20, 6.76 ± 0.19, 6.48 ± 0.18, and 5.97 ± 0.24 mm, respectively, and in the topical group it was 7.98 ± 0.15, 7.98 ± 0.15, 8.53 ± 0.14, 8.27 ± 0.16, and 7.93 ± 0.20 mm, respectively. The topical group consistently had larger mydriatic effects than the intracameral group (P < 0.05). The onset of mydriatic effect was rapid in the intracameral group. There was no difference in surgical performance or other parameters between groups. Conclusions. Intracameral epinephrine hydrochloride appears to be an alternative to the mydriatic modalities for phacoemulsification and IOL implantation. In comparison with topical mydriatics, intracameral epinephrine hydrochloride offers easier preoperative preparation, more rapid pupil dilation, and comparable surgical performance. PMID:26904274

  9. A validated high performance thin layer chromatography method for determination of yohimbine hydrochloride in pharmaceutical preparations

    OpenAIRE

    Badr, Jihan M.

    2013-01-01

    Background: Yohimbine is an indole alkaloid used as a promising therapy for erectile dysfunction. A number of methods were reported for the analysis of yohimbine in the bark or in pharmaceutical preparations. Materials and Method: In the present work, a simple and sensitive high performance thin layer chromatographic method is developed for determination of yohimbine (occurring as yohimbine hydrochloride) in pharmaceutical preparations and validated according to International Conference of Ha...

  10. Evaluation of gum damar as a novel microencapsulating material for ibuprofen and diltiazem hydrochloride

    OpenAIRE

    Morkhade D; Joshi S

    2007-01-01

    A natural gum, damar was investigated as a novel microencapsulating material for sustained drug delivery. Microparticles were prepared by oil-in-oil emulsion solvent evaporation method. Ibuprofen and diltiazem hydrochloride were used as model drugs. Microparticles were evaluated for particle size, encapsulation efficiency and in vitro drug release kinetics. Images of the microparticles were obtained by bright field microscopy. The effect of different gum:drug ratios and solubility of drug on ...

  11. DEVELOPMENT AND EVALUATION OF MICROBALLOONS OF PIOGLITAZONE HYDROCHLORIDE USING EUDRAGIT S-100

    OpenAIRE

    Nishant S. Gandhi et al.

    2012-01-01

    ABSTRACTKeywords:Pioglitazone hydrochloride,Eudragit S-100,Solvent diffusion evaporation,Floating microspheres,Polymer: Drug ratioCorrespondence to Author:Nishant GandhiOld Power House Road, Ramnagar, Gondia, Maharashtra, IndiaVarious approaches have been used to retain the dosage form in the stomach as a way of increasing the gastric residence time (GRT), including floatation systems; high-density systems; mucoadhesive systems; magnetic systems; unfoldable, extendible, or swellable systems;...

  12. Ion activated in situ gel system for ophthalmic delivery of moxifloxacin hydrochloride

    OpenAIRE

    Mali, Mahesh N.; Ashok A. Hajare

    2010-01-01

    Rapid precorneal elimination of drug is a major limitation of conventional ophthalmic formulations. An ion activated in situ gel forming systems of an antibacterial agent moxifloxacin hydrochloride for instillation as drops into eye undergoing a sol to gel transition in the cul-de-sac was formulated. Sodium alginate was used as the gelling agent in combination with hydroxypropylmethyl cellulose. Formulations were evaluated for gelling capacity, pH, in vitro release, rheological study, Draize ...

  13. 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

  14. Formulation and development of industry feasible proniosomal transdermal drug delivery system of granisetron hydrochloride

    OpenAIRE

    Bhushan Arun Patil; Prashant Keshav Puranik; Shankar Dadasaheb Pol; Prajakta Kalidas Khobragade; Pritee Shamrao Ramteke; Rajashree Gopal Palasakar; Nitiraj Ransing-Patil

    2015-01-01

    Proniosomes gel is semisolid liquid crystal products of nonionic surfactants, which converted into niosomes upon hydration. A proniosome based transdermal drug delivery system of granisetron hydrochloride (GRA HCL) developed by coacervation phase separation method. Formulation optimized by use of 3 2 full factorial design. Span 60 and cholesterol selected as independent variables, while entrapment efficiency (EE) and flux selected as dependent variables. Proniosomes evaluated for EE, in vitro...

  15. Development and In Vitro Characterization of Sustained Release Pellets of Venlafaxine Hydrochloride

    OpenAIRE

    P.REMYA; N. Damodharan; Dinesh Kumar, S.; V. Sowjanya

    2012-01-01

    The present study was undertaken with development and in-vitro characterization of sustained release pellets of venlafaxine hydrochloride by wruster process technique .which release the drug in sustained manner over a period of 20 hours. The different viscosity grades of polymers are HPMC-E6, Ethyl cellulose 7cps, MCC-101 were preparation of granules or pellets by wurster coating .The granules were prepared and evaluated for Angle of repose, bulk density, tapped density, cars index, moisture ...

  16. 经鼻泪道扩张联合丝裂霉素C治疗鼻泪管阻塞%Nasolacrimal duct dilating with mitomycin C for nasolacrimal duct obstruction

    Institute of Scientific and Technical Information of China (English)

    秦民安; 冯梅艳

    2009-01-01

    目的 评价经鼻泪道扩张联合丝裂霉素C(MMC)治疗鼻泪管阻塞的疗效和临床应用价值.方法 将60例鼻泪管阻塞患者随机分为丝裂霉紊组(A组)和硅胶管组(B组),经鼻泪道扩张后A组局部使用MMC,B组逆行置入硅胶管,随访6个月,观察治疗成功率.结果 经鼻泪道扩张联合MMC与逆行置入硅胶管术的疗效差异无统计学意义(P=0.058).结论 经鼻泪道扩张联合MMC治疗鼻泪管阻塞可取得与逆行置入硅胶管术相似的临床疗效,具有操作简便、费用低廉、治疗时间短、创伤小、恢复快等优点.%Objective To investigate the efficacy and practicability of through nasolacrimal duct dilating with mitomycin C in treatment of nasolaerimal duet obstruction. Methods 60 patients were randomly divided into two groups: Group A received mit-omyein C and Group B received a silicone stent.After nasolacrimal duct dilating, mitomycin C was used in Group A, and a sili-cone stent was retrogradely placed in Group B. Results Followed up for 6 months, efficacy of the two groups was not significant-ly different through a Chi square test. Conclusion Nasolacrimal duct dilating with mitomycin C has similar clinical efficacy with retrograde placement of a silicone stem. It has many advantages, such as simple operation, cheap charge, short treatment-time, small trauma, and quick resumption.

  17. Clinical Observation on Adjustable Suture Trabeculectomy With Mitomycin Combination Therapy for Glaucoma%可调整缝线小梁切除术与丝列霉素联合治疗青光眼临床观察

    Institute of Scientific and Technical Information of China (English)

    何海侠

    2016-01-01

    Objective To study the effect of adjustable suture trabeculectomy with mitomycin combination therapy in patients with glaucoma.Methods 76 patients with glaucoma (76 eyes) were divided into treatment group and control group, respectively received traditional trabeculectomy with adjustable suture trabeculectomy and mitomycin combination therapy.Results In the treatment group, shallow anterior chamber intraocular pressure levelⅠgrade proportion and postoperative complications were better than control group (P<0.05).Conclusion The glaucoma patients receiving adjustable suture trabeculectomy with mitomycin combination therapy have distinct curative effect.%目的:研究可调整缝线小梁切除术与丝裂霉素联合治疗青光眼患者的疗效。方法随机将76例青光眼患者(76眼)分成治疗组与对照组,分别行传统小梁切除术与可调整缝线小梁切除术与丝裂霉素联合治疗。结果治疗组平均眼压水平、浅前房Ⅰ级比例以及术后并发症等均优于对照组(P<0.05)。结论治疗青光眼患者应用可调整缝线小梁切除术与丝裂霉素联合疗法,疗效显著。

  18. Mitomycin Irrigation of Bladder Combined with Bladder Mucosa Electrocautery Treating Glandular Cystitis%丝裂霉素膀胱灌注联合膀胱黏膜电灼术治疗腺性膀胱炎

    Institute of Scientific and Technical Information of China (English)

    岳俊敏; 范锐; 张林超

    2013-01-01

    Objective:To observe the curative effects on mitomycin irrigation of bladder combined with bladder mucosa electrocau-tery treating glandular cystitis. Methods:38 patients with glandular cystitis proceeded bladder mucosa electrocautery with spinal-epi-dural anesthesia, 20mg mitomycin or 20ml physiological saline perfused the bladder 7 days later, catheter was removed after kept for 2 hours. Results:32 cases were cured, 6 cases were recurrent, and the curative rate was 84.2%with cystoscoping after 6 months of operation. Conclusion:Therapy of mitomycin bladder perfusion combined with bladder mucosa electrocautery treating glandular cystitis is curative effective of low cost.%  目的:观察丝裂霉素膀胱灌注联合膀胱黏膜电灼术治疗腺性膀胱炎的疗效。方法:38例腺性膀胱炎患者均行腰硬联合麻醉下膀胱黏膜电灼术,术后7天膀胱灌注20mg丝裂霉素/20ml生理盐水,保留2小时后拔除尿管。结果:术后6个月复查膀胱镜,治愈32例,复发6例,治愈率84.2%。结论:丝裂霉素膀胱灌注联合膀胱黏膜电灼术治疗腺性膀胱炎疗效好,费用低廉。

  19. 小梁切除术联合丝裂霉素C治疗青光眼临床意义探析%The Clinical Significance of Treatment of Glaucoma With Trabeculectomy and Mitomycin C

    Institute of Scientific and Technical Information of China (English)

    付宇鹏

    2015-01-01

    Objective To explore the clinical significance of treatment of glaucoma with trabeculectomy and mitomycin C. Methods Randomly selected 70 cases of patients with glaucoma in our hospital from October 2012 to October 2013 as the research objects. Divided into two groups randomly,control group and experimental group,each team with 35 cases,the patients in control group were treated with trabeculectomy,the others in experimental group were treated with trabeculectomy and mitomycin C. Compared the effects. Results The success rate of experimental group was much higher. The difference was significant(P<0.05). Conclusion The treatment of glaucoma with trabeculectomy and mitomycin C is effect.%目的:探析小梁切除术联合丝裂霉素C治疗青光眼临床意义。方法我院在2012年10月~2013年10月抽取了70例青光眼患者作为研究对象,对其进行随机分组,分别是对照组与实验组两组,每组35例。对照组给予小梁切除术进行治疗,实验组给予小梁切除术联合丝裂霉素C进行治疗。对比两组的效果。结果实验组治疗成功率高于对照组,差异有统计学意义,P<0.05。结论小梁切除术联合丝裂霉素C对治疗青光眼具有很好的治疗效果。

  20. A comparative study of the safety and efficacy effect of 5-fluorouracil or mitomycin C mounted biological delivery membranes in a rabbit model of glaucoma filtration surgery

    Directory of Open Access Journals (Sweden)

    Wu ZH

    2013-03-01

    Full Text Available Zhihong Wu,1 Shuning Li,2 Ningli Wang,2 Wanshun Liu,3 Wen Liu3 1General Hospital of Armed Police Forces, Beijing, People’s Republic of China; 2Beijing Tongren Eye Center, Capital Medical University, Beijing, People’s Republic of China 3Ocean University of China, Qingdao, People’s Republic of China Purpose: To investigate the potential usage of biological delivery membranes containing mitomycin C (MMC or 5-fluorouracil (5-FU in the construction of glaucoma-filtering blebs, and to evaluate their safety and efficacy. Methods: Chitosan was selected as the biological membrane carrier to prepare sustained-released membranes. Twelve micrograms of 5-FU or MMC was covalently conjugated onto the membranes by solvent volatilization. Rabbits underwent glaucoma filtration surgery and were randomly allocated into one of the four treatment regimens: glaucoma filtration operation with no implantation of chitosan membrane group (as control, drug-free chitosan membrane implantation group (blank/placebo group, membrane containing 5-FU treatment group (5-FU group, and membrane containing MMC treatment group (MMC group. Each group consisted of 12 rabbits. Intraocular pressure (IOP was measured and evaluated over a 28-day period follow-up preoperatively, then after surgery on days 1, 3, 5, 7, 14, 21, and 28 by Tono-Pen. The aqueous humor was analyzed in each experimental and control groups at days 4, 6, 8, 10, 12, 14, 16, and 20 after operation. Bleb survival and anterior segment were examined with a slit lamp microscope and photographed simultaneously. Two rabbits from each group were killed on day 28 and eight eye samples obtained for histopathological study. Corneas and lenses were examined by transmission and scanning electron microscopy. Results: Both 5-FU and MMC significantly prolonged bleb survival compared with control groups. The filtering bleb’s survival period was significantly more prolonged in the MMC and 5-FU groups (maintained 14 days than the