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Sample records for active pharmaceutical ingredients

  1. Separation of Chiral Active Pharmaceutical Ingredients

    DEFF Research Database (Denmark)

    Chaaban, Joussef Hussein

    is regarded as a first step towards a fully continuous PC process. The current knowledge of the importance of crystallization processes in the pharmaceutical industry and the complex thermodynamic and kinetic phenomena accompanied with the separation of chiral compounds are addressed. The experimental work...... public demand, and fierce competition have forced the pharmaceutical industry to redevelop existing methods or develop completely new methods to produce pharmaceuticals consisting of APIs of the desired enantiomer. PC is one of several methods used industrially to obtain pure enantiomers by separation...... covers laboratory studies and the theoretical work is based on the experimental data and observations. A large fraction of active pharmaceutical ingredients (APIs) are enantiomers and the desired biological activity is provided only by one of the enantiomers. Strict regulatory requirements, increasing...

  2. Optimised crystal morphologies for active pharmaceutical ingredients and related studies

    OpenAIRE

    Horgan, Danielle E.

    2015-01-01

    The majority of active pharmaceutical ingredients (APIs) are crystalline solids in their pure forms. Crystalline solids have definable morphologies, i.e. shape and size. Crystal morphology is determined by both the internal structure of the crystals and external factors during growth from solution. The morphology of a crystal batch can affect key processes during manufacturing. Companies generally accept whatever morphology the manufacturing process provides and deal with any subsequent probl...

  3. Impurity profile tracking for active pharmaceutical ingredients: case reports.

    Science.gov (United States)

    Zhou, Lili; Mao, Bing; Reamer, Robert; Novak, Tom; Ge, Zhihong

    2007-06-28

    Tracking the impurity profile of an active pharmaceutical ingredient (API) is a very important task for all stages of drug development. A systematic approach for tracking impurity profile of API is described. Various real pharmaceutical applications are presented through successful examples of impurity profile tracking for three different novel APIs. These include MK-0969, an M3 antagonist; MK-0677, an oral-active growth hormone secretagogue and API-A, a cathepsin K inhibitor. A general strategy including selection of a reversed phase high performance liquid chromatographic (RP-HPLC) impurity profile method based on screening various stationary phases and changing the pH of the mobile phase and elucidation of impurity structures through the utilization of LC-MS, preparative-LC and NMR is demonstrated. A series of studies were conducted on the peak purity check by using the LC-UV diode-array and LC-MS detections. The advantages and disadvantages of each technique in the evaluation of peak purity are discussed. PMID:17142001

  4. Interactions and incompatibilities of pharmaceutical excipients with active pharmaceutical ingredients: a comprehensive review.

    Directory of Open Access Journals (Sweden)

    Sonali S. Bharate

    2010-12-01

    Full Text Available Studies of active drug/excipient compatibility represent an important phase in the preformulation stage of the development of all dosage forms. The potential physical and chemical interactions between drugs and excipients can affect the chemical nature, the stability and bioavailability of drugs and, consequently, their therapeutic efficacy and safety. The present review covers the literaturereports of interaction and incompatibilities of commonly used pharmaceutical excipients with different active pharmaceutical ingredients in solid dosage forms. Examples of active drug/excipientinteractions, such as transacylation, the Maillard browning reaction, acid base reactions and physical changes are discussed for different active pharmaceutical ingredients belonging to different therapeuticcategories viz antiviral, anti-inflammatory, antidiabetic, antihypertensive, anti-convulsant, antibiotic,bronchodialator, antimalarial, antiemetic, antiamoebic, antipsychotic, antidepressant, anticancer, anticoagulant and sedative/hypnotic drugs and vitamins. Once the solid-state reactions of a pharmaceutical system are understood, the necessary steps can be taken to avoid reactivity and improve the stability of drug substances and products.

  5. Terahertz study on porosity and mass fraction of active pharmaceutical ingredient of pharmaceutical tablets.

    Science.gov (United States)

    Bawuah, Prince; Tan, Nicholas; Tweneboah, Samuel Nana A; Ervasti, Tuomas; Axel Zeitler, J; Ketolainen, Jarkko; Peiponen, Kai-Erik

    2016-08-01

    In this study, terahertz time-domain spectroscopic (THz-TDS) technique has been used to ascertain the change in the optical properties, as a function of changing porosity and mass fraction of active pharmaceutical ingredient (API), of training sets of pharmaceutical tablets. Four training sets of pharmaceutical tablets were compressed with microcrystalline cellulose (MCC) excipient and indomethacin API by varying either the porosity, height, and API mass fraction or all three tablet parameters. It was observed, as far as we know, for the first time, that the THz time-domain and frequency-domain effective refractive index, as well as, the frequency-domain effective absorption coefficient both show linear correlations with the porosity and API mass fraction for training sets of real pharmaceutical tablets. We suggest that, the observed linear correlations can be useful in basic research and quality inspection of pharmaceutical tablets. Additionally, we propose a novel optical strain parameter, based on THz measurement, which yields information on the conventional strain parameter of a tablet as well as on the change of fill fraction of solid material during compression of porous pharmaceutical tablets. We suggest that the THz measurement and proposed method of data analysis, in addition to providing an efficient tool for basic research of porous media, can serve as one of the novel quality by design (QbD) implementation techniques to predict critical quality attributes (CQA) such as porosity, API mass fraction and strain of flat-faced pharmaceutical tablets before production. PMID:27288937

  6. Life cycle analysis within pharmaceutical process optimization and intensification: case study of active pharmaceutical ingredient production.

    Science.gov (United States)

    Ott, Denise; Kralisch, Dana; Denčić, Ivana; Hessel, Volker; Laribi, Yosra; Perrichon, Philippe D; Berguerand, Charline; Kiwi-Minsker, Lioubov; Loeb, Patrick

    2014-12-01

    As the demand for new drugs is rising, the pharmaceutical industry faces the quest of shortening development time, and thus, reducing the time to market. Environmental aspects typically still play a minor role within the early phase of process development. Nevertheless, it is highly promising to rethink, redesign, and optimize process strategies as early as possible in active pharmaceutical ingredient (API) process development, rather than later at the stage of already established processes. The study presented herein deals with a holistic life-cycle-based process optimization and intensification of a pharmaceutical production process targeting a low-volume, high-value API. Striving for process intensification by transfer from batch to continuous processing, as well as an alternative catalytic system, different process options are evaluated with regard to their environmental impact to identify bottlenecks and improvement potentials for further process development activities.

  7. Effects of active pharmaceutical ingredients mixtures in mussel Mytilus galloprovincialis.

    Science.gov (United States)

    Gonzalez-Rey, M; Mattos, J J; Piazza, C E; Bainy, A C D; Bebianno, M J

    2014-08-01

    Active pharmaceutical ingredients (APIs) are emergent environmental contaminants widely detected in surface waters as result of incomplete waste water treatment plant (WWTP) removal processes and improper disposal. The assessment of potential effects of APIs on non-target organisms is still scarce since besides presenting multiple chemical structures, properties and modes of action, these compounds occur as complex mixtures. This study comprises a 15-day exposure of mussels Mytilus galloprovincialis to mixtures (at environmentally relevant nominal concentrations) of non-steroidal inflammatory drugs ibuprofen (IBU) and diclofenac (DCF) (250 ng L(-1) each) and selective serotonin reuptake inhibitor (SSRI) fluoxetine (FLX) (75 ng L(-1)) (MIX 1) along with the addition of classical pro-oxidant copper (Cu) (5 μg L(-1)) (MIX 2). The goals included the assessment of oxidative stress, neurotoxic and endocrine effects on this sentinel species applying both a multibiomarker and gene expression (here and later gene expression is taken as synonym to gene transcription, although it is acknowledged that it is also affected by, e.g. translation, and mRNA and protein stability) analysis approaches. The results revealed a swifter antioxidant response in digestive glands than in gills induced by MIX 1, nevertheless the presence of Cu in MIX 2 promoted a higher lipid peroxidation (LPO) induction. Neither mixture altered acetylcholinesterase (AChE) activity, while both triggered the formation of vitellogenin-like proteins in females confirming the xenoestrogenic effect of mixtures. All these results varied with respect to those obtained in previous single exposure essays. Moreover, RT-PCR analysis revealed a catalase (CAT) and CYP4Y1 gene expression down- and upregulation, respectively, with no significant changes in mRNA levels of genes encoding superoxide dismutase (SOD) and glutathione-S-transferase (GST). Finally, this study highlights variable tissue and time-specific biomarker

  8. Crystal solvates of active pharmaceutical ingredients actual for industry of Latvia

    OpenAIRE

    Veldre, Kaspars

    2013-01-01

    Crystal solvates of active pharmaceutical ingredients actual for industry of Latvia ABSTRACT This doctoral thesis project is focused on investigation of active pharmaceutical ingredients (API), which are important for industry of Latvia. Crystal solvate search and screening was performed for compounds described and novel crystalline forms were obtained. Stability in acquisition, production and storage conditions was evaluated. Crystal structure determination was performed for selected A...

  9. Tregitope Peptides: The Active Pharmaceutical Ingredient of IVIG?

    Directory of Open Access Journals (Sweden)

    Anne S. De Groot

    2013-01-01

    Full Text Available Five years ago, we reported the identification and characterization of several regulatory T-cell epitopes (now called Tregitopes that were discovered in the heavy and light chains of IgG (De Groot et al. Blood, 2008. When added ex vivo to human PBMCs, these Tregitopes activated regulatory T cells (Tregs, increased expression of the transcription factor FoxP3, and induced IL-10 expression in CD4+ T cells. We have now shown that coadministration of the Tregitopes in vivo, in a number of different murine models of autoimmune disease, can suppress immune responses to antigen in an antigen-specific manner, and that this response is mediated by Tregs. In addition we have shown that, although these are generally promiscuous epitopes, the activity of individual Tregitope peptides is restricted by HLA. In this brief report, we provide an overview of the effects of Tregitopes in vivo, discuss potential applications, and suggest that Tregitopes may represent one of the “active pharmaceutical ingredients” of IVIg. Tregitope applications may include any of the autoimmune diseases that are currently treated almost exclusively with intravenous immunoglobulin G (IVIG, such as Chronic Inflammatory Demyelinating Polyneuropathy (CIDP and Multifocal Motor Neuropathy (MMN, as well as gene therapy and allergy where Tregitopes may provide a means of inducing antigen-specific tolerance.

  10. Oxidation of Mixed Active Pharmaceutical Ingredients in Biologically Treated Wastewater by ClO2

    DEFF Research Database (Denmark)

    Moradas, Gerly; Fick, Jerker; Ledin, Anna;

    2011-01-01

    Biologically treated wastewater containing a mixture of 53 active pharmaceutical ingredients (APIs)was treated with 0-20 mg/l chlorine dioxide (ClO2) solution. Wastewater effluents were taken from two wastewater treatment plants in Sweden, one with (low COD) and one without (high COD) extended...

  11. Kinetics of the esterification of active pharmaceutical ingredients containing carboxylic Acid functionality in polyethylene glycol

    DEFF Research Database (Denmark)

    Schou-Pedersen, Anne Marie V; Hansen, Steen Honoré; Moesgaard, Birthe;

    2014-01-01

    Polyethylene glycols (PEGs) are attractive as excipients in the manufacture of drug products because they are water soluble and poorly immunogenic. They are used in various pharmaceutical preparations. However, because of their terminal hydroxyl groups, PEGs can participate in esterification...... reactions. In this study, kinetics of two active pharmaceutical ingredients, cetirizine and indomethacin possessing carboxylic acid functionality, has been studied in PEG 400 and PEG 1000 at 50°C, 60°C, 70°C, and 80°C. HPLC-UV was applied for the determination of concentrations in the kinetic studies...

  12. Oxidation of Mixed Active Pharmaceutical Ingredients in Biologically Treated Wastewater by ClO2

    OpenAIRE

    Moradas, Gerly; Fick, Jerker; Ledin, Anna; Jansen, Jes la Cour; Andersen, Henrik Rasmus

    2011-01-01

    Biologically treated wastewater containing a mixture of 53 active pharmaceutical ingredients (APIs)was treated with 0-20 mg/l chlorine dioxide (ClO2) solution. Wastewater effluents were taken from two wastewater treatment plants in Sweden, one with (low COD) and one without (high COD) extended nitrogen removal. The removal of the APIs varied from no significant removal at the highest dose of ClO2 (20 mg/l) to 90% removal at a dose of 0.5 mg/l of the oxidant. From the low COD effluent, only 4 ...

  13. Isolation and characterization of process related impurities in anastrozole active pharmaceutical ingredient

    Energy Technology Data Exchange (ETDEWEB)

    Hiriyanna, S. G.; Basavaiah, K. [University of Mysore, Manasagangothri, Mysore (India). Dept. of Chemistry]. E-mail: hiriyannag@gmail.com

    2008-07-01

    Three impurities ranging from 0.08%-0.12% by peak area in anastrozole active pharmaceutical ingredient were detected by simple isocratic reverse-phase high performance liquid chromatography (HPLC). These impurities were isolated by prep-HPLC and were characterized by LC- MS/MS, GCMS and NMR experimental data. Based on the results obtained from different spectroscopic experiments, these impurities have been characterized as 2,2'-(5-((4H-1,2,4-triazol-4-yl)methyl)-1,3-phenylene)bis(2-methyl propanenitrile) (Impurity I), 2,2'-(5-methyl-1,3-phenylene)bis(2-methylpropanenitrile) (Impurity II) and 2,2'-(5-(bromomethyl)-1,3-phenylene)bis(2-methylpropanenitrile) (Impurity III). (author)

  14. Application of instrumented nanoindentation in preformulation studies of pharmaceutical active ingredients and excipients.

    Science.gov (United States)

    Egart, Mateja; Janković, Biljana; Srčič, Stane

    2016-09-01

    Nanoindentation allows quantitative determination of a material's response to stress such as elastic and plastic deformation or fracture tendency. Key instruments that have enabled great advances in nanomechanical studies are the instrumented nanoindenter and atomic force microscopy. The versatility of these instruments lies in their capability to measure local mechanical response, in very small volumes and depths, while monitoring time, displacement and force with high accuracy and precision. This review highlights the application of nanoindentation for mechanical characterization of pharmaceutical materials in the preformulation phase (primary investigation of crystalline active ingredients and excipients). With nanoindentation, mechanical response can be assessed with respect to crystal structure. The technique is valuable for mechanical screening of a material at an early development phase in order to predict and better control the processes in which a material is exposed to stress such as milling and compression. PMID:27383883

  15. Direct analysis of palladium in active pharmaceutical ingredients by anodic stripping voltammetry.

    Science.gov (United States)

    Rosolina, Samuel M; Chambers, James Q; Xue, Zi-Ling

    2016-03-31

    Anodic stripping voltammetry, a classical electroanalytical method has been optimized to analyze trace Pd(II) in active pharmaceutical ingredient matrices. The electroanalytical approach with an unmodified glassy carbon electrode was performed in both aqueous and 95% DMSO/5% water (95/5 DMSO/H2O) solutions, without pretreatment such as acid digestion or dry ashing to remove the organics. Limits of detection (LODs) in the presence of caffeine and ketoprofen were determined to be 11 and 9.6 μg g(-1), with a relative standard deviation (RSD) of 5.7% and 2.3%, respectively. This method is simple, highly reproducible, sensitive, and robust. The instrumentation has the potential to be portable and the obviation of sample pretreatment makes it an ideal approach for determining lost catalytic metals in pharmaceutical-related industries. Furthermore, the simultaneous detection of Pd(II) with Cd(II) and Pb(II) in the low μg L(-1) range indicates that this system is capable of simultaneous multi-analyte analysis in a variety of matrices. PMID:26965326

  16. Consequences of New Approach to Chemical Stability Tests to Active Pharmaceutical Ingredients.

    Science.gov (United States)

    Jamrógiewicz, Marzena

    2016-01-01

    There is a great need of broaden look on stability tests of active pharmaceutical ingredients (APIs) in comparison with current requirements contained in pharmacopeia. By usage of many modern analytical methods the conception of monitoring the changes of APIs during initial stage of their exposure to harmful factors has been developed. New knowledge must be acquired in terms of identification of each degradation products, especially volatile ones. Further research as toxicology prediction during in silico studies of determined and identified degradation products is necessary. In silico methods are known as computational toxicology or computer-assisted technologies which are used for predicting toxicology of pharmaceutical substances such as impurities or degradation products. This is a specialized software and databases intended to calculate probability of genotoxicity or mutagenicity of these substances through a chemical structure-based screening process and algorithm specific to a given software program. Applying of new analytical approach is proposed as the usage of PAT tools, XRD, HS-SPME GC-MS/MS, LC-MS/MS for stability testing. Described improvements should be taken into account in case of each drug existing already in the market as well as being implemented as new one. PMID:26955356

  17. Core-Shell Composite Hydrogels for Controlled Nanocrystal Formation and Release of Hydrophobic Active Pharmaceutical Ingredients.

    Science.gov (United States)

    Badruddoza, Abu Zayed Md; Godfrin, P Douglas; Myerson, Allan S; Trout, Bernhardt L; Doyle, Patrick S

    2016-08-01

    Although roughly 40% of pharmaceuticals being developed are poorly water soluble, this class of drugs lacks a formulation strategy capable of producing high loads, fast dissolution kinetics, and low energy input. In this work, a novel bottom-up approach is developed for producing and formulating nanocrystals of poorly water-soluble active pharmaceutical ingredients (APIs) using core-shell composite hydrogel beads. Organic phase nanoemulsion droplets stabilized by polyvinyl alcohol (PVA) and containing a model hydrophobic API (fenofibrate) are embedded in the alginate hydrogel matrix and subsequently act as crystallization reactors. Controlled evaporation of this composite material produces core-shell structured alginate-PVA hydrogels with drug nanocrystals (500-650 nm) embedded within the core. Adjustable loading of API nanocrystals up to 83% by weight is achieved with dissolution (of 80% of the drug) occurring in as little as 30 min. A quantitative model is also developed and experimentally validated that the drug release patterns of the fenofibrate nanocrystals can be modulated by controlling the thickness of the PVA shell and drug loading. Thus, these composite materials offer a "designer" drug delivery system. Overall, our approach enables a novel means of simultaneous controlled crystallization and formulation of hydrophobic drugs that circumvents energy intensive top-down processes in traditional manufacturing. PMID:27249402

  18. Estimation of active pharmaceutical ingredients content using locally weighted partial least squares and statistical wavelength selection.

    Science.gov (United States)

    Kim, Sanghong; Kano, Manabu; Nakagawa, Hiroshi; Hasebe, Shinji

    2011-12-15

    Development of quality estimation models using near infrared spectroscopy (NIRS) and multivariate analysis has been accelerated as a process analytical technology (PAT) tool in the pharmaceutical industry. Although linear regression methods such as partial least squares (PLS) are widely used, they cannot always achieve high estimation accuracy because physical and chemical properties of a measuring object have a complex effect on NIR spectra. In this research, locally weighted PLS (LW-PLS) which utilizes a newly defined similarity between samples is proposed to estimate active pharmaceutical ingredient (API) content in granules for tableting. In addition, a statistical wavelength selection method which quantifies the effect of API content and other factors on NIR spectra is proposed. LW-PLS and the proposed wavelength selection method were applied to real process data provided by Daiichi Sankyo Co., Ltd., and the estimation accuracy was improved by 38.6% in root mean square error of prediction (RMSEP) compared to the conventional PLS using wavelengths selected on the basis of variable importance on the projection (VIP). The results clearly show that the proposed calibration modeling technique is useful for API content estimation and is superior to the conventional one. PMID:22001843

  19. Direct analysis of palladium in active pharmaceutical ingredients by anodic stripping voltammetry.

    Science.gov (United States)

    Rosolina, Samuel M; Chambers, James Q; Xue, Zi-Ling

    2016-03-31

    Anodic stripping voltammetry, a classical electroanalytical method has been optimized to analyze trace Pd(II) in active pharmaceutical ingredient matrices. The electroanalytical approach with an unmodified glassy carbon electrode was performed in both aqueous and 95% DMSO/5% water (95/5 DMSO/H2O) solutions, without pretreatment such as acid digestion or dry ashing to remove the organics. Limits of detection (LODs) in the presence of caffeine and ketoprofen were determined to be 11 and 9.6 μg g(-1), with a relative standard deviation (RSD) of 5.7% and 2.3%, respectively. This method is simple, highly reproducible, sensitive, and robust. The instrumentation has the potential to be portable and the obviation of sample pretreatment makes it an ideal approach for determining lost catalytic metals in pharmaceutical-related industries. Furthermore, the simultaneous detection of Pd(II) with Cd(II) and Pb(II) in the low μg L(-1) range indicates that this system is capable of simultaneous multi-analyte analysis in a variety of matrices.

  20. Dissolution enhancement of active pharmaceutical ingredients by therapeutic deep eutectic systems.

    Science.gov (United States)

    Aroso, Ivo M; Silva, João C; Mano, Francisca; Ferreira, Ana S D; Dionísio, Madalena; Sá-Nogueira, Isabel; Barreiros, Susana; Reis, Rui L; Paiva, Alexandre; Duarte, Ana Rita C

    2016-01-01

    A therapeutic deep eutectic system (THEDES) is here defined as a deep eutectic solvent (DES) having an active pharmaceutical ingredient (API) as one of the components. In this work, THEDESs are proposed as enhanced transporters and delivery vehicles for bioactive molecules. THEDESs based on choline chloride (ChCl) or menthol conjugated with three different APIs, namely acetylsalicylic acid (AA), benzoic acid (BA) and phenylacetic acid (PA), were synthesized and characterized for thermal behaviour, structural features, dissolution rate and antibacterial activity. Differential scanning calorimetry and polarized optical microscopy showed that ChCl:PA (1:1), ChCl:AA (1:1), menthol:AA (3:1), menthol:BA (3:1), menthol:PA (2:1) and menthol:PA (3:1) were liquid at room temperature. Dissolution studies in PBS led to increased dissolution rates for the APIs when in the form of THEDES, compared to the API alone. The increase in dissolution rate was particularly noticeable for menthol-based THEDES. Antibacterial activity was assessed using both Gram-positive and Gram-negative model organisms. The results show that all the THEDESs retain the antibacterial activity of the API. Overall, our results highlight the great potential of THEDES as dissolution enhancers in the development of novel and more effective drug delivery systems. PMID:26586342

  1. Active pharmaceutical ingredient (API) production involving continuous processes – A process system engineering (PSE)-assisted design framework

    DEFF Research Database (Denmark)

    Cervera Padrell, Albert Emili; Skovby, Tommy; Kiil, Søren;

    2012-01-01

    kg of product – was reduced to half of its initial value, with potential for further reduction. The case-study includes reaction steps typically used by the pharmaceutical industry featuring different characteristic reaction times, as well as L–L separation and distillation-based solvent exchange......A systematic framework is proposed for the design of continuous pharmaceutical manufacturing processes. Specifically, the design framework focuses on organic chemistry based, active pharmaceutical ingredient (API) synthetic processes, but could potentially be extended to biocatalytic...... the detailed design and analysis. Examples from the literature of PSE methods and tools applied to pharmaceutical process design and novel pharmaceutical production technologies are provided along the text, assisting in the accumulation and interpretation of process knowledge. Different criteria are suggested...

  2. Development of a solvate as an active pharmaceutical ingredient: Developability, crystallisation and isolation challenges

    Science.gov (United States)

    Douillet, Julien; Stevenson, Neil; Lee, Mei; Mallet, Franck; Ward, Richard; Aspin, Peter; Dennehy, Daniel Robert; Camus, Laure

    2012-03-01

    The preclinical development of an active pharmaceutical ingredient (API) begins with the selection of a solid state form. A solvate may be selected for development if it is sufficiently stable and if the solvent quantity administered to the patient is lower than the tolerated potential daily exposure (PDE). The selection and process development of a solvate is presented here. The initial crystallisation process gave poor control over the particle size distribution (PSD) and inclusion of additional crystallisation solvent in the crystal lattice. These two API attributes were controlled using micronised seeds and optimising the crystallisation conditions. After filtration, slurry washing with a second solvent was used to replace the high boiling point crystallisation solvent to improve the drying efficiency. The slurry washing was modelled and studied in the laboratory to control the level of unbound crystallisation solvent in the API. The API desolvation during slurry washing was studied by considering thermodynamics, by construction of the ternary phase diagram, and kinetics aspects. This work provides useful approaches and considerations to assess the risks specific to the controlled production of a solvate that are rarely presented in the literature.

  3. Approaches to the Development of Human Health Toxicity Values for Active Pharmaceutical Ingredients in the Environment.

    Science.gov (United States)

    Sorell, Tamara L

    2016-01-01

    Management of active pharmaceutical ingredients (API) in the environment is challenging because these substances represent a large and diverse group of compounds. Advanced wastewater treatment technologies that can remove API tend to be costly. Because of the potential resources required to address API in the environment, there is a need to establish environmental benchmarks that can serve as targets for treatment and release. To date, there are several different approaches that have been taken to derive human health toxicity values for API. These methods include traditional risk assessment approaches that calculate "safe" doses using experimental data and uncertainty (safety) factors; point of departure (POD), which starts from a therapeutic human dose and applies uncertainty factors; and threshold of toxicological concern (TTC), a generic approach that establishes threshold values across broad classes of chemicals based on chemical structure. To evaluate the use of these approaches, each of these methods was applied to three API commonly encountered in the environment: acetaminophen, caffeine, and chlorpromazine. The results indicate that the various methods of estimating toxicity values produce highly varying doses. Associated doses are well below typical intakes, or toxicity thresholds cannot be derived due to a lack of information. No uniform approach can be applied to establishing thresholds for multiple substances. Rather, an individualized approach will need to be applied to each target API.

  4. Prioritization methodology for the monitoring of active pharmaceutical ingredients in hospital effluents.

    Science.gov (United States)

    Daouk, Silwan; Chèvre, Nathalie; Vernaz, Nathalie; Bonnabry, Pascal; Dayer, Pierre; Daali, Youssef; Fleury-Souverain, Sandrine

    2015-09-01

    The important number of active pharmaceutical ingredients (API) available on the market along with their potential adverse effects in the aquatic ecosystems, lead to the development of prioritization methods, which allow choosing priority molecules to monitor based on a set of selected criteria. Due to the large volumes of API used in hospitals, an increasing attention has been recently paid to their effluents as a source of environmental pollution. Based on the consumption data of a Swiss university hospital, about hundred of API has been prioritized following an OPBT approach (Occurrence, Persistence, Bioaccumulation and Toxicity). In addition, an Environmental Risk Assessment (ERA) allowed prioritizing API based on predicted concentrations and environmental toxicity data found in the literature for 71 compounds. Both prioritization approaches were compared. OPBT prioritization results highlight the high concern of some non steroidal anti-inflammatory drugs and antiviral drugs, whereas antibiotics are revealed by ERA as potentially problematic to the aquatic ecosystems. Nevertheless, according to the predicted risk quotient, only the hospital fraction of ciprofloxacin represents a risk to the aquatic organisms. Some compounds were highlighted as high-priority with both methods: ibuprofen, trimethoprim, sulfamethoxazole, ritonavir, gabapentin, amoxicillin, ciprofloxacin, raltegravir, propofol, etc. Analyzing consumption data and building prioritization lists helped choosing about 15 API to be monitored in hospital wastewaters. The API ranking approach adopted in this study can be easily transposed to any other hospitals, which have the will to look at the contamination of their effluents.

  5. Co-crystallization: An approach to improve the performance characteristics of active pharmaceutical ingredients

    Directory of Open Access Journals (Sweden)

    Jignasa Ketan Savjani

    2015-01-01

    Full Text Available Co-crystal chemistry has recently attracted supramolecular scientists. Co-crystals are comprising of hydrogen boding assembly between different molecules. Many issues related to performance characteristics of an active pharmaceutical ingredient (API can be resolved using co-crystallization approach. Proper understanding of crystal structure of an API is required for successful formation of co-crystals with the selected co-former. This review article focus on explanation about co-crystals, intellectual property rights, their advantages and limitations. Co-crystallization can be achieved using different methods like co-grinding slurry based, solvent evaporation method, etc. Methods of co-crystallization are simple and increase the purity of the final product. Co-crystallization can be applied to the drugs prescribed in combination therapy. Stoichiometric composition of different drugs used in combination therapy can be co-crystallize to form one solid state form. Physicochemical properties of APIs such as solubility and stability can be improved using co-crystallization approach. With due regards co-crystallization should be used with caution because of some issues during manufacturing of final product.

  6. The significance of different health institutions and their respective contributions of active pharmaceutical ingredients to wastewater.

    Science.gov (United States)

    Herrmann, Manuel; Olsson, Oliver; Fiehn, Rainer; Herrel, Markus; Kümmerer, Klaus

    2015-12-01

    Active pharmaceutical ingredients (APIs) have been frequently found in the environment. It is, however, still not quite clear who is mainly responsible for API emissions. Hospitals have been considered to be the main contributing point sources for wastewater (WW) discharge of APIs. However, recent studies have shown that the contribution of hospitals to the input of APIs into the aquatic environment is quite low. Due to demographic change and the increase of psychiatric diseases, health institutions (HIs) such as psychiatric hospitals and nursing homes are likely to be important sources as well, but no data is available in this respect. This study aims to assess the impact of HIs and to provide a methodology to measure their respective contributions. Drawing on pharmaceutical consumption data for the years 2010, 2011, and 2012, this study identified API usage patterns for a psychiatric hospital (146 beds), a nursing home (286 inhabitants), and a general hospital (741 beds), the latter of which comprises three separate locations. All the HIs are located in two sub-regions of a county district with about 400,000 citizens in southwestern Germany. A selection of neurological drugs was quantified in the sewer of these facilities to evaluate the correlation between consumption and emission. The API contribution of HIs was assessed by comparing the specific consumption in the facilities with the consumption in households, expressed as the emission potential (IEP). The study shows that the usage patterns of APIs in the psychiatric hospital and the nursing home were different from the general hospital. Neurological drugs such as anticonvulsants, psycholeptics, and psychoanaleptics were mainly consumed in the psychiatric hospital and the nursing home (74% and 65%, respectively). Predicted and average measured concentrations in the effluent of the investigated HIs differed mostly by less than one order of magnitude. Therefore, the consumption-based approach is a useful method

  7. Role of herbal bioactives as a potential bioavailability enhancer for Active Pharmaceutical Ingredients.

    Science.gov (United States)

    Ajazuddin; Alexander, Amit; Qureshi, Azra; Kumari, Leena; Vaishnav, Pramudita; Sharma, Mukesh; Saraf, Swarnlata; Saraf, Shailendra

    2014-09-01

    The current review emphasizes on the herbal bioenhancers which themselves do not possess inherent pharmacological activity of their own but when co-administered with Active Pharmaceutical Ingredients (API), enhances their bioavailability and efficacy. Herbal bioenhancers play a crucial role in enhancing the bioavailability and bioefficacy of different classes of drugs, such as antihypertensives, anticancer, antiviral, antitubercular and antifungal drugs at low doses. This paper highlights various natural compounds that can be utilized as an efficient bioenhancer. Several herbal compounds including piperine, quercetin, genistein, naringin, sinomenine, curcumin, and glycyrrhizin have demonstrated capability to improve the pharmacokinetic parameters of several potent API. This article also focuses on various United States patents on herbal bioenhancers, which has proved to be beneficial in improving oral absorption of nutraceuticals like vitamins, minerals, amino acids and certain herbal compounds. The present paper also describes proposed mechanism of action, which mainly includes absorption process, drug metabolism, and action on drug target. The herbal bioenhancers are easily available, safe, free from side effects, minimizes drug toxicity, shortens the duration of treatment, lowers the drug resistance problems and minimizes the cost of treatment. Inspite of the fact that herbal bioenhancers provide an innovative concept for enhancing the bioavailability of several potent drugs, there are numerous bioenhancers of herbal origin that are yet to be explored in several vital areas. These bioenhancers must also be implied to enhance the bioavailability and bioefficacy through routes other than the oral route of drug delivery. There is a vast array of unexploited plants which can be investigated for their drug bioenhancing potency. The toxicity profiles of these herbal bioenhancers must not be overlooked. Researches must be carried out to solve these issues and to

  8. 78 FR 3900 - Generic Drug User Fee-Active Pharmaceutical Ingredient and Finished Dosage Form Facility Fee...

    Science.gov (United States)

    2013-01-17

    ...The Food and Drug Administration (FDA) is announcing the rate for the generic drug active pharmaceutical ingredient (API) and finished dosage form (FDF) facilities user fees for fiscal year (FY) 2013. The Federal Food, Drug, and Cosmetic Act (the FD&C Act), as amended by the Generic Drug User Fee Amendments of 2012 (GDUFA), enacted the Food and Drug Administration Safety and Innovation Act, as......

  9. Active pharmaceutical ingredients detected in herbal food supplements for weight loss samples on the Dutch market

    NARCIS (Netherlands)

    Reeuwijk, N.M.; Venhuis, B.J.; Kaste, de D.; Hoogenboom, L.A.P.; Rietjens, I.; Martena, M.J.

    2014-01-01

    Herbal food supplements claiming to reduce weight may contain active pharmacological ingredients (APIs) that can be used for the treatment of overweight and obesity. The aim of this study was to determine whether herbal food supplements for weight loss on the Dutch market contain APIs with weight lo

  10. Determination of platinum group metal catalyst residues in active pharmaceutical ingredients by means of total reflection X-ray spectrometry

    Science.gov (United States)

    Marguí, Eva; Queralt, Ignasi; Hidalgo, Manuela

    2013-08-01

    The control of metal catalyst residues (i.e., platinum group metals (PGMs)) in different stages of the manufacturing processes of the active pharmaceutical ingredients (APIs) and, especially, in the final product is crucial. For API specimens, there are strict guidelines to limit the levels of metal residues based on their individual levels of safety concern. For PGMs the concentration limit has been established at 10 mg/kg in the API. Therefore great effort is currently being devoted to the development of new and simple procedures to control metals in pharmaceuticals. In the present work, an analytical methodology based on benchtop total reflection X-ray fluorescence spectrometry (TXRF) has been developed for the rapid and simple determination of some PGM catalyst impurities (Rh, Pd, Ir and Pt) in different types of API samples. An evaluation of different sample treatments (dissolution and digestion of the solid pharmaceutical samples) has been carried out and the developed methodologies have been validated according to the analytical parameters to be considered and acceptance criteria for PGM determination according to the United States Pharmacopeia (USP). Limits of quantification obtained for PGM metals were in the range of 2-4 mg/kg which are satisfactory according to current legislation. From the obtained results it is shown that the developed TXRF method can be implemented in the pharmaceutical industries to increase productivity of the laboratory; offering an interesting and complementary analytical tool to other atomic spectroscopic methods.

  11. Characterizing Active Pharmaceutical Ingredient Binding to Human Serum Albumin by Spin-Labeling and EPR Spectroscopy.

    Science.gov (United States)

    Hauenschild, Till; Reichenwallner, Jörg; Enkelmann, Volker; Hinderberger, Dariush

    2016-08-26

    Drug binding to human serum albumin (HSA) has been characterized by a spin-labeling and continuous-wave (CW) EPR spectroscopic approach. Specifically, the contribution of functional groups (FGs) in a compound on its albumin-binding capabilities is quantitatively described. Molecules from different drug classes are labeled with EPR-active nitroxide radicals (spin-labeled pharmaceuticals (SLPs)) and in a screening approach CW-EPR spectroscopy is used to investigate HSA binding under physiological conditions and at varying ratios of SLP to protein. Spectral simulations of the CW-EPR spectra allow extraction of association constants (KA ) and the maximum number (n) of binding sites per protein. By comparison of data from 23 SLPs, the mechanisms of drug-protein association and the impact of chemical modifications at individual positions on drug uptake can be rationalized. Furthermore, new drug modifications with predictable protein binding tendency may be envisaged. PMID:27460503

  12. Quantification of potential impurities by a stability indicating UV-HPLC method in niacinamide active pharmaceutical ingredient.

    Science.gov (United States)

    Thomas, Saji; Bharti, Amber; Tharpa, Kalsang; Agarwal, Ashutosh

    2012-02-23

    A sensitive, stability indicating reverse phase UV-HPLC method has been developed for the quantitative determination of potential impurities of niacinamide active pharmaceutical ingredient. Efficient chromatographic separation was achieved on C18 stationary phase in isocratic mode using simple mobile phase. Forced degradation study confirmed that the newly developed method was specific and selective to the degradation products. Major degradation of the drug substance was found to occur under oxidative stress conditions to form niacinamide N-oxide. The method was validated according to ICH guidelines with respect to specificity, precision, linearity and accuracy. Regression analysis showed correlation coefficient value greater than 0.999 for niacinamide and its six impurities. Detection limit of impurities was in the range of 0.003-0.005% indicating the high sensitivity of the newly developed method. Accuracy of the method was established based on the recovery obtained between 93.3% and 113.3% for all impurities.

  13. Direct detection and identification of active pharmaceutical ingredients in intact tablets by helium plasma ionization (HePI mass spectrometry

    Directory of Open Access Journals (Sweden)

    Athula B. Attygalle

    2014-06-01

    Full Text Available A simple modification converts an electrospray ion source to an ambient-pressure helium plasma ionization source without the need of additional expensive hardware. Peaks for active ingredients were observed in the spectra recorded from intact pharmaceutical tablets placed in this source. A flow of heated nitrogen was used to thermally desorb analytes to gas phase. The desorption temperatures were sometimes as low as 50 °C. For example, negative-ion spectra recorded from an aspirin tablet showed peaks at m/z 137 (salicylate anion and 179 (acetylsalicylate anion which were absent in the background spectra. The overall ion intensity increased as the desorption gas temperature was elevated. Within the same acquisition experiment, both positive- and negative-ion signals for acetaminophen were recorded from volatiles emanating from Tylenol tablets by switching the polarity of the capillary back and forth. Moreover, different preparations of acetaminophen tablets could be distinguished by their ion-intensity thermograms.

  14. Direct detection and identification of active pharmaceutical ingredients in intact tablets by helium plasma ionization (HePI) mass spectrometry

    Institute of Scientific and Technical Information of China (English)

    Athula B. Attygalle; Freneil B. Jariwala; Julius Pavlov; Zhihua Yang; Jason A. Mahr; Mabel Oviedo

    2014-01-01

    A simple modification converts an electrospray ion source to an ambient-pressure helium plasma ionization source without the need of additional expensive hardware. Peaks for active ingredients were observed in the spectra recorded from intact pharmaceutical tablets placed in this source. A flow of heated nitrogen was used to thermally desorb analytes to gas phase. The desorption temperatures were sometimes as low as 50 1C. For example, negative-ion spectra recorded from an aspirin tablet showed peaks at m/z 137 (salicylate anion) and 179 (acetylsalicylate anion) which were absent in the background spectra. The overall ion intensity increased as the desorption gas temperature was elevated. Within the same acquisition experiment, both positive- and negative-ion signals for acetaminophen were recorded from volatiles emanating from Tylenol tablets by switching the polarity of the capillary back and forth. Moreover, different preparations of acetaminophen tablets could be distinguished by their ion-intensity thermograms.

  15. Optimization of HS-GC-FID-MS Method for Residual Solvent Profiling in Active Pharmaceutical Ingredients Using DoE.

    Science.gov (United States)

    Poceva Panovska, Ana; Acevska, Jelena; Stefkov, Gjoshe; Brezovska, Katerina; Petkovska, Rumenka; Dimitrovska, Aneta

    2016-02-01

    Within this research, a headspace (HS) gas chromatography-flame ionization detector-mass spectrometry method was developed for profiling of residual solvents (RSs) in active pharmaceutical ingredients (APIs). Design of experiment was used for optimization of sample preparation, as well as for robustness testing of the method. HS equilibration temperature and dilution medium were detected as parameters with greater impact on the sensitivity, compared with the time used for equilibration of the samples. Regardless of the sample solubility, the use of water for sample preparation was found to be crucial for better sensitivity. The use of a well-designed strategy for method development and robustness testing, additional level of identification confidence, as well as use of internal standard provided a strong and reliable analytical tool for API fingerprinting, thus enabling the authentication of the substance based on the RS profile. PMID:26290585

  16. An Introduction to the Prequalification of Active Pharmaceutical Ingredients%WHO原料药预认证项目简介

    Institute of Scientific and Technical Information of China (English)

    杜雯君; 梁毅

    2012-01-01

    Search the WHO website for guidanc e and technical documents for Prequalification of Active Pharmaceutical Ingredients,and translate and compile the program.Conclusion:Learn the relevant regulations of international organization and requirements of technology in depth,to form the system of drug management which meets the international standards,only in this way can we enter the international market as soon as possible.%检索WHO药品预认证项目技术指南,翻译并整理原料药预认证项目的工作程序。结论:只有深入学习国际组织相关法规和技术要求、建立符合国际标准的监管体系,才能有效推进我国制药产品早日进入国际市场。

  17. Determination of platinum group metal catalyst residues in active pharmaceutical ingredients by means of total reflection X-ray spectrometry

    Energy Technology Data Exchange (ETDEWEB)

    Marguí, Eva, E-mail: eva.margui@udg.edu [Department of Chemistry, University of Girona, Campus Montilivi, 17071 Girona (Spain); Queralt, Ignasi, E-mail: iqueralt@ictja.csic.es [Laboratory of X-ray Analytical Applications, Institute of Earth Sciences “Jaume Almera”, CSIC, Solé Sabarís s/n, 08028 Barcelona (Spain); Hidalgo, Manuela, E-mail: manuela.hidalgo@udg.edu [Department of Chemistry, University of Girona, Campus Montilivi, 17071 Girona (Spain)

    2013-08-01

    The control of metal catalyst residues (i.e., platinum group metals (PGMs)) in different stages of the manufacturing processes of the active pharmaceutical ingredients (APIs) and, especially, in the final product is crucial. For API specimens, there are strict guidelines to limit the levels of metal residues based on their individual levels of safety concern. For PGMs the concentration limit has been established at 10 mg/kg in the API. Therefore great effort is currently being devoted to the development of new and simple procedures to control metals in pharmaceuticals. In the present work, an analytical methodology based on benchtop total reflection X-ray fluorescence spectrometry (TXRF) has been developed for the rapid and simple determination of some PGM catalyst impurities (Rh, Pd, Ir and Pt) in different types of API samples. An evaluation of different sample treatments (dissolution and digestion of the solid pharmaceutical samples) has been carried out and the developed methodologies have been validated according to the analytical parameters to be considered and acceptance criteria for PGM determination according to the United States Pharmacopeia (USP). Limits of quantification obtained for PGM metals were in the range of 2–4 mg/kg which are satisfactory according to current legislation. From the obtained results it is shown that the developed TXRF method can be implemented in the pharmaceutical industries to increase productivity of the laboratory; offering an interesting and complementary analytical tool to other atomic spectroscopic methods. - Highlights: • A TXRF method for PGM catalyst residue determination in API samples is presented. • Analysis can be performed using 10 μL of the internal standardized dissolved API. • The method is rapid, simple and suitable according to the USP requirements.

  18. Determination of platinum group metal catalyst residues in active pharmaceutical ingredients by means of total reflection X-ray spectrometry

    International Nuclear Information System (INIS)

    The control of metal catalyst residues (i.e., platinum group metals (PGMs)) in different stages of the manufacturing processes of the active pharmaceutical ingredients (APIs) and, especially, in the final product is crucial. For API specimens, there are strict guidelines to limit the levels of metal residues based on their individual levels of safety concern. For PGMs the concentration limit has been established at 10 mg/kg in the API. Therefore great effort is currently being devoted to the development of new and simple procedures to control metals in pharmaceuticals. In the present work, an analytical methodology based on benchtop total reflection X-ray fluorescence spectrometry (TXRF) has been developed for the rapid and simple determination of some PGM catalyst impurities (Rh, Pd, Ir and Pt) in different types of API samples. An evaluation of different sample treatments (dissolution and digestion of the solid pharmaceutical samples) has been carried out and the developed methodologies have been validated according to the analytical parameters to be considered and acceptance criteria for PGM determination according to the United States Pharmacopeia (USP). Limits of quantification obtained for PGM metals were in the range of 2–4 mg/kg which are satisfactory according to current legislation. From the obtained results it is shown that the developed TXRF method can be implemented in the pharmaceutical industries to increase productivity of the laboratory; offering an interesting and complementary analytical tool to other atomic spectroscopic methods. - Highlights: • A TXRF method for PGM catalyst residue determination in API samples is presented. • Analysis can be performed using 10 μL of the internal standardized dissolved API. • The method is rapid, simple and suitable according to the USP requirements

  19. Acceleration of Anti-Markovnikov Hydroamination in the Synthesis of an Active Pharmaceutical Ingredient

    DEFF Research Database (Denmark)

    Mitic, Aleksandar; Skovby, Tommy; Dam-Johansen, Kim;

    2016-01-01

    Slow chemical reactions are a big challenge in the modern pharmaceutical industry. Their accelerations together with the introduction of continuous manufacturing modes are major drivers for future development. One example reaction is hydroamination, a reaction between unsaturated hydrocarbons...

  20. Supramolecular hydrogen-bonding patterns of co-crystals containing the active pharmaceutical ingredient (API) phloroglucinol and N-heterocycles.

    Science.gov (United States)

    Cvetkovski, Aleksandar; Bertolasi, Valerio; Ferretti, Valeria

    2016-06-01

    The active pharmaceutical ingredient phloroglucinol (PHL) has been taken as an illustrative molecule to explore the intermolecular interactions which can be established with other molecular entities to build PHL pharmaceutical co-crystals. The crystal structures of five newly synthesized co-crystals are reported, where PHL is crystallized with N-heterocycles, namely 2-hydroxy-6-methylpyridine (1), 2,4-dimethyl-6-hydroxypyrimidine (2), 4-phenylpyridine (3), 2-hydroxypyridine (4) and 2,3,5,6-tetramethylpyrazine (5). The structural characteristics of these co-crystals, as far as the hydrogen-bonding networks and the crystalline architectures are concerned, are strongly dependent on the chemical features of the coformer molecules, as well as on their size and shape. A detailed analysis of the intermolecular interactions established in all the PHL co-crystals of known structures has allowed the recognition of some regularities in the packing modes that can be useful in the design of new supramolecular adducts forming predictable structural motifs. PMID:27240764

  1. Direct Determination of ECD in ECD Kit: A Solid Sample Quantitation Method for Active Pharmaceutical Ingredient in Drug Product

    Directory of Open Access Journals (Sweden)

    Ming-Yu Chao

    2011-01-01

    Full Text Available Technetium-99m ethyl cysteinate dimer (Tc-99m-ECD is an essential imaging agent used in evaluating the regional cerebral blood flow in patients with cerebrovascular diseases. Determination of active pharmaceutical ingredient, that is, L-Cysteine, N, N′-1,2-ethanediylbis-, diethyl ester, dihydrochloride (ECD in ECD Kit is a relevant requirement for the pharmaceutical quality control in processes of mass fabrication. We here presented a direct solid sample determination method of ECD in ECD Kit without sample dissolution to avoid the rapid degradation of ECD. An elemental analyzer equipped with a nondispersive infrared detector and a calibration curve of coal standard was used for the quantitation of sulfur in ECD Kit. No significant matrix effect was found. The peak area of coal standard against the amount of sulfur was linear over the range of 0.03–0.10 mg, with a correlation coefficient ( of 0.9993. Method validation parameters were achieved to demonstrate the potential of this method.

  2. A Tape Method for Fast Characterization and Identification of Active Pharmaceutical Ingredients in the 2-18 THz Spectral Range

    Science.gov (United States)

    Kissi, Eric Ofosu; Bawuah, Prince; Silfsten, Pertti; Peiponen, Kai-Erik

    2015-03-01

    In order to find counterfeit drugs quickly and reliably, we have developed `tape method' a transmission spectroscopic terahertz (THz) measurement technique and compared it with a standard attenuated total reflection (ATR) THz spectroscopic measurement. We used well-known training samples, which include commercial paracetamol and aspirin tablets to check the validity of these two measurement techniques. In this study, the spectral features of some active pharmaceutical ingredients (APIs), such as aspirin and paracetamol are characterized for identification purpose. This work covers a wide THz spectral range namely, 2-18 THz. This proposed simple but novel technique, the tape method, was used for characterizing API and identifying their presence in their dosage forms. By comparing the spectra of the APIs to their dosage forms (powder samples), all distinct fingerprints present in the APIs are also present in their respective dosage forms. The positions of the spectral features obtained with the ATR techniques were akin to that obtained from the tape method. The ATR and the tape method therefore, complement each other. The presence of distinct fingerprints in this spectral range has highlighted the possibility of developing fast THz sensors for the screening of pharmaceuticals. It is worth noting that, the ATR method is applicable to flat faced tablets whereas the tape method is suitable for powders in general (e.g. curved surface tablets that require milling before measurement). Finally, we have demonstrated that ATR techniques can be used to screen counterfeit antimalarial tablets.

  3. A Hybrid MPC-PID Control System Design for the Continuous Purification and Processing of Active Pharmaceutical Ingredients

    Directory of Open Access Journals (Sweden)

    Maitraye Sen

    2014-05-01

    Full Text Available In this work, a hybrid MPC (model predictive control-PID (proportional-integral-derivative control system has been designed for the continuous purification and processing framework of active pharmaceutical ingredients (APIs. The specific unit operations associated with the purification and processing of API have been developed from first-principles and connected in a continuous framework in the form of a flowsheet model. These integrated unit operations are highly interactive along with the presence of process delays. Therefore, a hybrid MPC-PID is a promising alternative to achieve the desired control loop performance as mandated by the regulatory authorities. The integrated flowsheet model has been simulated in gPROMSTM (Process System Enterprise, London, UK. This flowsheet model has been linearized in order to design the control scheme. The ability to track the set point and reject disturbances has been evaluated. A comparative study between the performance of the hybrid MPC-PID and a PID-only control scheme has been presented. The results show that an enhanced control loop performance can be obtained under the hybrid control scheme and demonstrate that such a scheme has high potential in improving the efficiency of pharmaceutical manufacturing operations.

  4. A systematic methodology for the design of continuous active pharmaceutical ingredient production processes

    DEFF Research Database (Denmark)

    Cervera Padrell, Albert Emili; Gani, Rafiqul; Kiil, Søren;

    2011-01-01

    Continuous pharmaceutical manufacturing (CPM) has emerged as a powerful technology to obtain higher reaction yields and improved separation efficiencies, potentially leading to simplified process flowsheets, reduced total costs, lower environmental impacts, and safer and more flexible production....... However, the change from batch-wise production towards continuous operation and the definition of flexible design spaces requires a high degree of process knowledge. Process Systems Engineering (PSE) offers multiple methods and tools which can assist in efficient knowledge acquisition, structuring...... and representation, as well as on how to employ this knowledge for process (re-)design. The aim of this paper is to introduce a methodology that systematically identifies already existing PSE methods and tools which can assist in the design of CPM processes. This methodology has been applied to a process...

  5. Characterization of solid polymer dispersions of active pharmaceutical ingredients by 19F MAS NMR and factor analysis

    Science.gov (United States)

    Urbanova, Martina; Brus, Jiri; Sedenkova, Ivana; Policianova, Olivia; Kobera, Libor

    In this contribution the ability of 19F MAS NMR spectroscopy to probe structural variability of poorly water-soluble drugs formulated as solid dispersions in polymer matrices is discussed. The application potentiality of the proposed approach is demonstrated on a moderately sized active pharmaceutical ingredient (API, Atorvastatin) exhibiting extensive polymorphism. In this respect, a range of model systems with the API incorporated in the matrix of polvinylpyrrolidone (PVP) was prepared. The extent of mixing of both components was determined by T1(1H) and T1ρ(1H) relaxation experiments, and it was found that the API forms nanosized domains. Subsequently it was found out that the polymer matrix induces two kinds of changes in 19F MAS NMR spectra. At first, this is a high-frequency shift reaching 2-3 ppm which is independent on molecular structure of the API and which results from the long-range polarization of the electron cloud around 19F nucleus induced by electrostatic fields of the polymer matrix. At second, this is broadening of the signals and formation of shoulders reflecting changes in molecular arrangement of the API. To avoid misleading in the interpretation of the recorded 19F MAS NMR spectra, because both the contributions act simultaneously, we applied chemometric approach based on multivariate analysis. It is demonstrated that factor analysis of the recorded spectra can separate both these spectral contributions, and the subtle structural differences in the molecular arrangement of the API in the nanosized domains can be traced. In this way 19F MAS NMR spectra of both pure APIs and APIs in solid dispersions can be directly compared. The proposed strategy thus provides a powerful tool for the analysis of new formulations of fluorinated pharmaceutical substances in polymer matrices.

  6. Measurement of low amounts of amorphous content in hydrophobic active pharmaceutical ingredients with dynamic organic vapor sorption.

    Science.gov (United States)

    Müller, Thorsten; Schiewe, Jörg; Smal, Rüdiger; Weiler, Claudius; Wolkenhauer, Markus; Steckel, Hartwig

    2015-05-01

    Today, a variety of devices for dry powder inhalers (DPIs) is available and many different formulations for optimized deposition in the lung are developed. However, during the production of powder inhalers, processing steps may induce changes to both, the carrier and active pharmaceutical ingredients (APIs). It is well known that standard pharmaceutical operations may lead to structural changes, crystal defects and amorphous regions. Especially operations such as milling, blending and even sieving generate these effects. These disorders may induce re-crystallization and particle size changes post-production which have a huge influence on drug delivery and product stability. In this study, pilot tests with a polar solvent (water) and hydrophilic drug (Salbutamol sulfate) were performed to receive a first impression on further possible implementation of hydrophobic samples with organic solvents. Thereafter, a reliable method for the accurate detection of low amounts of amorphous content is described up to a limit of quantification (LOQ) of 0.5% for a hydrophobic model API (Ciclesonide). The organic vapor sorption method which is a gravimetric method quantifies exactly these low amounts of amorphous content in the hydrophobic powder once the suitable solvent (isopropanol), the correct p/p0 value (0.1) and the exact temperature (25°C) have been found. Afterward it was possible to quantitate low amorphous amounts in jet-milled powders (0.5-17.0%). In summary, the data of the study led to a clearer understanding in what quantity amorphous parts were generated in single production steps and how variable these parts behave to fully crystalline material. Nevertheless it showed how difficult it was to re-crystallize hydrophobic material with water vapor over a short period. For the individual samples it was possible to determine the single humidity at which the material starts to re-crystallize, the behavior against different nonpolar solvents and the calculation of the

  7. Quantitation of active pharmaceutical ingredients and excipients in powder blends using designed multivariate calibration models by near-infrared spectroscopy.

    Science.gov (United States)

    Li, Weiyong; Worosila, Gregory D

    2005-05-13

    This research note demonstrates the simultaneous quantitation of a pharmaceutical active ingredient and three excipients in a simulated powder blend containing acetaminophen, Prosolv and Crospovidone. An experimental design approach was used in generating a 5-level (%, w/w) calibration sample set that included 125 samples. The samples were prepared by weighing suitable amount of powders into separate 20-mL scintillation vials and were mixed manually. Partial least squares (PLS) regression was used in calibration model development. The models generated accurate results for quantitation of Crospovidone (at 5%, w/w) and magnesium stearate (at 0.5%, w/w). Further testing of the models demonstrated that the 2-level models were as effective as the 5-level ones, which reduced the calibration sample number to 50. The models had a small bias for quantitation of acetaminophen (at 30%, w/w) and Prosolv (at 64.5%, w/w) in the blend. The implication of the bias is discussed. PMID:15848006

  8. Development and validation of a stability-indicating reverse phase ultra performance liquid chromatographic method for the estimation of nebivolol impurities in active pharmaceutical ingredients and pharmaceutical formulation.

    Science.gov (United States)

    Thummala, Veera Raghava Raju; Lanka, Mohana Krishna

    2015-10-01

    A sensitive, stability-indicating gradient reverse phase ultra performance liquid chromatographic method has been developed for the quantitative estimation of nebivolol impurities in active pharmaceutical ingredient (API) and pharmaceutical formulation. Efficient chromatographic separation was achieved on an Acquity BEH C18 column (100 mm x 2.1 mm, 1.7 μm) with mobile phase of a gradient mixture. The flow rate of the mobile phase was 0.18 mL/min with column temperature of 30 degrees C and detection wavelength of 281 nm. The relative response factor values of (R*)-2-( benzylamino)-1-((S*)-6-fluorochroman-2-yl) ethanol ((R x S*) NBV-), (R)-1-((R)-6-fluorochroman-2-yl)-2-((S)-2-((S)-6-fluoro-chroman-2-yl)-2-hydroxyethyl-amino) ethanol ((RRSS) NBV-3), 1-(chroman-2-yl)-2-(2-(6-fluorochroman-2-yl)-2-hydroxyethyl amino) ethanol (monodesfluoro impurity), (S)-1-((R)-6-fluorochroman-2-yl)-2-((R)-2 (S*)-6-fluoro-chroman-2-yl)-2-hydroxyethylamino) ethanol hydrochloride ((RSRS) NBV-3) and (R*)-1-((S*)-6-fluorochroman-2-yl)-2-((S*)-2-((S*)-6-fluoro-chroman-2-yl)-2-hydroxyethylamino) ethanol ((R* S* S* S*) NBV-2) were 0.65, 0.91, 0.68, 0.92 and 0.91 respectively. Nebivolol formulation sample was subjected to the stress conditions of acid, base, oxidative, hydrolytic, thermal, humidity and photolytic degradation. Nebivolol was found to degrade significantly under peroxide stress condition. The degradation products were well resolved from nebivolol and its impurities. The peak purity test results confirmed that the nebivolol peak was homogenous and pure in all stress samples and the mass balance was found to be more than 98%, thus proving the stability-indicating power of the method. The developed method was validated according to International Conference on Hormonization (ICH) guidelines with respect to specificity, linearity, limits of detection and quantification, accuracy, precision and robustness. PMID:26930962

  9. Capillary-induced Homogenization of Matrix in Paper: A Powerful Approach for the Quantification of Active Pharmaceutical Ingredients Using Mass Spectrometry Imaging

    Science.gov (United States)

    de Menezes, Maico; de Oliveira, Diogo Noin; Catharino, Rodrigo Ramos

    2016-07-01

    Herein we present a novel approach for the quantification of active pharmaceutical ingredients (APIs) using mass spectrometry imaging. This strategy uses a filter paper previously “eluted” with a MALDI matrix solution as a support for analyte application. Samples are submitted to mass spectrometry imaging (MSI) and quantification through characteristic fingerprints is ultimately performed. Results for the content of rosuvastatin from a known formulation are comparable to those obtained with a validated HPLC method.

  10. Capillary-induced Homogenization of Matrix in Paper: A Powerful Approach for the Quantification of Active Pharmaceutical Ingredients Using Mass Spectrometry Imaging

    Science.gov (United States)

    de Menezes, Maico; de Oliveira, Diogo Noin; Catharino, Rodrigo Ramos

    2016-01-01

    Herein we present a novel approach for the quantification of active pharmaceutical ingredients (APIs) using mass spectrometry imaging. This strategy uses a filter paper previously “eluted” with a MALDI matrix solution as a support for analyte application. Samples are submitted to mass spectrometry imaging (MSI) and quantification through characteristic fingerprints is ultimately performed. Results for the content of rosuvastatin from a known formulation are comparable to those obtained with a validated HPLC method. PMID:27439589

  11. Impact of alternative solid state forms and specific surface area of high-dose, hydrophilic active pharmaceutical ingredients on tabletability.

    Science.gov (United States)

    Paluch, Krzysztof J; Tajber, Lidia; Corrigan, Owen I; Healy, Anne Marie

    2013-10-01

    In order to investigate the effect of using different solid state forms and specific surface area (TBET) of active pharmaceutical ingredients on tabletability and dissolution performance, the mono- and dihydrated crystalline forms of chlorothiazide sodium and chlorothiazide potassium (CTZK) salts were compared to alternative anhydrous and amorphous forms, as well as to amorphous microparticles of chlorothiazide sodium and potassium which were produced by spray drying and had a large specific surface area. The tablet hardness and tensile strength, porosity, and specific surface area of single-component, convex tablets prepared at different compression pressures were characterized. Results confirmed the complexity of the compressibility mechanisms. In general it may be concluded that factors such as solid-state form (crystalline vs amorphous), type of hydration (presence of interstitial molecules of water, dehydrates), or specific surface area of the material have a direct impact on the tabletability of the powder. It was observed that, for powders of the same solid state form, those with a larger specific surface area compacted well, and better than powders of a lower surface area, even at relatively low compression pressures. Compacts prepared at lower compression pressures from high surface area porous microparticles presented the shortest times to dissolve, when compared with compacts made of equivalent materials, which had to be compressed at higher compression pressures in order to obtain satisfactory compacts. Therefore, materials composed of nanoparticulate microparticles (NPMPs) may be considered as suitable for direct compaction and possibly for inclusion in tablet formulations as bulking agents, APIs, carriers, or binders due to their good compactibility performance. PMID:23961942

  12. Encapsulation of active ingredients

    NARCIS (Netherlands)

    Gotlieb, K.F.; Schijndel, van R.J.G.; Soest, van J.J.G.

    1999-01-01

    Microspheres having a particle size of 50 nm to 1 nm and a polydispersity of less than 40%, consisting of a chemically cross-linked starch shell containing an active ingredient, are obtained by preparing an oil-in-water emulsion of the active ingredient in a hydrophobic phase and starch or a dispers

  13. Encapsulation of active ingredients

    NARCIS (Netherlands)

    Soest, van J.J.G.; Schijndel, van R.J.G.; Gotlieb, K.F.

    2000-01-01

    Microspheres having a particle size of 50 nm to 1 nm and a polydispersity of less than 40%, consisting of a chemically cross-linked starch shell containing an active ingredient, are obtained by preparing an oil-in-water emulsion of the active ingredient in a hydrophobic phase and starch or a dispers

  14. Encapsulation of active ingredients

    NARCIS (Netherlands)

    Soest, van J.J.G.; Schijndel, van R.J.G.; Gotlieb, K.F.

    2002-01-01

    Microspheres having a particle size of 50 nm to 1 nm and a polydispersity of less than 40%, consisting of a chemically cross-linked starch shell containing an active ingredient, are obtained by preparing an oil-in-water emulsion of the active ingredient in a hydrophobic phase and starch or a dispers

  15. Encapsulation of active ingredients

    OpenAIRE

    Soest, van, A.J.; Schijndel, van, AWM Jos; Gotlieb, K.F.

    2002-01-01

    Microspheres having a particle size of 50 nm to 1 nm and a polydispersity of less than 40%, consisting of a chemically cross-linked starch shell containing an active ingredient, are obtained by preparing an oil-in-water emulsion of the active ingredient in a hydrophobic phase and starch or a dispersion of a solid active ingredient and starch in water, incorporating the oil-in-water emulsion or solid dispersion in an outer hydrophobic phase, particles of the oil-in-water emulsion or solid disp...

  16. A survey of the syntheses of active pharmaceutical ingredients for antiretroviral drug combinations critical to access in emerging nations.

    Science.gov (United States)

    Pinheiro, Eloan Dos Santos; Antunes, Octavio Augusto Ceva; Fortunak, Joseph M D

    2008-09-01

    irrelevant, except for "advanced salvage" drugs such as enfuvirtide. In resource-poor settings cost is a huge factor that limits drug access, resulting in high rates of new infection and subsequent mortality. IP coverage, where granted, can keep access prices for essential ARVs higher than would otherwise be the case. Large, innovator companies have made drugs available at prices very close to the cost of manufacturing for "lowest income" countries. Generic providers in India and elsewhere provide the largest supply of drugs for the developing world. The recent issuance of Voluntary and Compulsory Licenses (VLs, CLs) through the World Trade Organization's TRIP (Treaty Respecting Intellectual Property) provisions arguably contribute to bringing down access prices. The utilization of improved science, pooled purchasing and intelligent procurement practices all definitely contribute to access. This work surveys the production processes for several critical ARVs. These are discussed in terms of scale up, raw material/intermediates and active pharmaceutical ingredient (API) costs. In some cases new routes to APIs or critical intermediates are needed. Based on potential new chemistries, there are significant opportunities to reduce cost for a number of critical ARVs. PMID:18571246

  17. 离子液体在活性药物成分中的应用%The application of ionic liquids in active pharmaceutical ingredients

    Institute of Scientific and Technical Information of China (English)

    孟坤燕; 齐明辉; 陈宜俍; 赵文杰; 任国宾

    2011-01-01

    离子液体具有独特的可调节的理化性能,近年来离子液体在活性药物成分中的应用成为国际上研究的前沿和热点.该文在介绍离子液体特性的基础上,综述了离子液体形式的活性药物成分的制备、表征和研究意义.%Ionic liquids (Ils) possess unique tunable physical and chemical properties. Recently, the application of Ils in active pharmaceutical ingredients (APIs) has become the frontier of international pharmaceutical research. The synthesis, characterization and significance of Ils-APIs are summarized based on the properties of Ils.

  18. Analytical method (HPLC, validation used for identification and assay of the pharmaceutical active ingredient, Tylosin tartrate for veterinary use and its finite product Tilodem 50, hydrosoluble powder

    Directory of Open Access Journals (Sweden)

    Maria Neagu

    2010-12-01

    Full Text Available In SC DELOS IMPEX ’96 SRL the quality of the active pharmaceutical ingredient (API for the finite product Tilodem 50 - hydrosoluble powder was acomkplished in the respect of last European Pharmacopoeia.The method for analysis used in this purpose was the compendial method „Tylosin tartrate for veterinary use” in EurPh. in vigour edition and represent a variant developed and validation „in house”.The parameters which was included in the methodology validation for chromatographic method are the followings: Selectivity, Linearity, Linearity range, Detection and Quantification limits, Precision, Repeatability (intra day, Inter-Day Reproductibility, Accuracy, Robustness, Solutions’ stability and System suitability. According to the European Pharmacopoeia, the active pharmaceutical ingredient is consistent, in terms of quality, if it contains Tylosin A - minimum 80% and the amount of Tylosin A, B, C, D, at minimum 95%. Identification and determination of each component separately (Tylosin A, B, C, D is possible by chromatographic separation-HPLC. Validation of analytical methods is presented below.

  19. Continuous Hydrolysis and Liquid–Liquid Phase Separation of an Active Pharmaceutical Ingredient Intermediate Using a Miniscale Hydrophobic Membrane Separator

    DEFF Research Database (Denmark)

    Cervera Padrell, Albert Emili; Morthensen, Sofie Thage; Lewandowski, Daniel Jacob;

    2012-01-01

    capillary pressure (Laplace pressure) combined with a large number of pores per unit area offering low pressure drop. The separation device can easily be operated by means of a back-pressure regulator ensuring flow-independent separation efficiency. Simple monitoring and control strategies as well as...... scaling-up/out approaches are proposed, concluding that membrane-based L-L separation may become a standard unit operation for continuous pharmaceutical manufacturing....... a PTFE membrane with 28 cm2 of active area. A less challenging separation of water and toluene was achieved at total flow rates as high as 80 mL/min, with potential to achieve even higher flow rates. The operability and flexibility of the membrane separator and a plate coalescer were compared...

  20. The slow relaxation dynamics in active pharmaceutical ingredients studied by DSC and TSDC: Voriconazole, miconazole and itraconazole.

    Science.gov (United States)

    Ramos, Joaquim J Moura; Diogo, Hermínio P

    2016-03-30

    The slow molecular mobility of three active pharmaceutical drugs (voriconazole, miconazole and itraconazole) has been studied by differential scanning calorimetry (DSC) and thermally stimulated depolarization currents (TSDC). This study yielded the main kinetic features of the secondary relaxations and of the main (glass transition) relaxation, in particular their distribution of relaxation times. The dynamic fragility of the three glass formers was determined from DSC data (using two different procedures) and from TSDC data. According to our results voriconazole behaves as a relatively strong liquid, while miconazole is moderately fragile and itraconazole is a very fragile liquid. There are no studies in this area published in the literature relating to voriconazole. Also not available in the literature is a slow mobility study by dielectric relaxation spectroscopy in the amorphous miconazole. Apart from that, the results obtained are in reasonable agreement with published works using different experimental techniques.

  1. Monitoring and Control of a Continuous Grignard Reaction for the Synthesis of an Active Pharmaceutical Ingredient Intermediate Using Inline NIR spectroscopy

    DEFF Research Database (Denmark)

    Cervera Padrell, Albert Emili; Nielsen, Jesper; Jønch Pedersen, Michael;

    2012-01-01

    Inline near-infrared (NIR) spectroscopy has been used to monitor a continuous synthesis of an active pharmaceutical ingredient (API) intermediate by a Grignard alkylation reaction. The reaction between a ketone substrate and allylmagnesium chloride may form significant impurities with excess...... to the stoichiometric ratio, leading the path to full process automation. The feedback control loop relies on NIR transmission measurements performed in a flow cell where, in contrast to labor-intensive offline HPLC analytical methods, the whole reaction product can be scanned in real time without sample dilution...... information about its dynamic behavior. This information is very useful for process control design, assessment of analytical tools and definition of sampling times. In this work, a systematic procedure for chemometric model building is followed, after which a discussion is made on some of the potential...

  2. Determination of everolimus in everolimus active pharmaceutical ingredient by HPLC%HPLC法测定依维莫司原料药中依维莫司

    Institute of Scientific and Technical Information of China (English)

    孙莉君; 沈海梅; 马海霞; 董大伟; 王越; 杨静

    2015-01-01

    Objective To establish an HPLC method for determination of everolimus in everolimus active pharmaceutical ingredient. Methods The separation was performed on a Hypersil-ODS C18column with acetonitrile - water (70∶30) as mobile phases. The detection wavelength was set at 276 nm. The column temperature was 50℃. The flow rate was 0.8 mL/min with injection volume of 10μL.Results Everolimus had good linearity in the ranges of 63 — 1 008μg/mL (r= 0.999 7). The average recovery was 100.45% with RSD 0.64% (n=9).Conclusion The method is simple and specific, and can be used effectively for quality control of everolimus active pharmaceutical ingredient.%目的:建立HPLC法测定依维莫司原料药中依维莫司。方法采用Hypersil-ODS C18色谱柱(250 mm×4.6 mm,5μm);流动相:乙腈–水(70∶30);检测波长:276 nm;柱温:50℃;体积流量:0.8 mL/min;进样量:10μL。结果依维莫司在63~1008μg/mL线性关系良好(r=0.9997),平均回收率为100.45%,RSD值为0.64%(n=9)。结论所建立的操作简便,专属性强,可用于依维莫司原料药的质量控制。

  3. Monitoring the dissolution of Active Pharmaceutical Ingredient and TPGS in real time via IR spectroscopy during the manufacturing of liquid dosage formulation.

    Science.gov (United States)

    Šašić, Slobodan; Palm, Andrew S; Tang, Degui

    2012-11-01

    Infrared spectroscopy is used to monitor the dissolution of the Active Pharmaceutical Ingredient (API) and an excipient (vitamin E - TPGS) during manufacturing of a liquid pharmaceutical formulation. The goal of the analysis is to explore options for real-time, on screen, and quantitative monitoring of these two components by using an iC10 instrument. As is common, the first step in the approach is to create respective calibration models for the two components and then apply those models on the spectra obtained from scale-up batches. Interestingly, while the API dissolves at the room temperature, TPGS dissolves at an acceptable rate at 50 °C so both temperatures have to be considered. It is shown that univariate models of sufficient accuracy can be developed with a straightforward applicability to the scale-up batches spectra and providing reasonably accurate estimates of the API and TPGS concentrations. Some limitations of the software on the employed instrument may diminish the prospect for the quantitative analysis of the components of interest in this formulation. PMID:22871426

  4. Development of Genotoxic Impurities Control in Active Pharmaceutical Ingredient%原料药中基因毒性杂质控制的研究进展

    Institute of Scientific and Technical Information of China (English)

    王萍; 徐彩虹; 陈仙; 胡爱玲; 楼朝; 金秀芳; 龚俊强; 陈轶群

    2015-01-01

    目的 介绍原料药(active pharmaceutical ingredient,API)中基因毒性杂质控制的法规要求、评估方法和控制方法.方法 通过学习欧美法规发展历史,理解国际高端市场对基因毒性杂质控制的监管期望,提出原料药中基因毒性杂质风险评估方法.结果与结论 企业基于半定量评估,结合清除研究数据,建立科学的控制策略,使实际工艺中所有可能涉及的基因毒性杂质风险得到明确鉴别和控制,是达到监管期望的有效途径.

  5. Influence of Process Parameters on Content Uniformity of a Low Dose Active Pharmaceutical Ingredient in a Tablet Formulation According to GMP

    Directory of Open Access Journals (Sweden)

    Muselík Jan

    2014-09-01

    Full Text Available The article describes the development and production of tablets using direct compression of powder mixtures. The aim was to describe the impact of filler particle size and the time of lubricant addition during mixing on content uniformity according to the Good Manufacturing Practice (GMP process validation requirements. Processes are regulated by complex directives, forcing the producers to validate, using sophisticated methods, the content uniformity of intermediates as well as final products. Cutting down of production time and material, shortening of analyses, and fast and reliable statistic evaluation of results can reduce the final price without affecting product quality. The manufacturing process of directly compressed tablets containing the low dose active pharmaceutical ingredient (API warfarin, with content uniformity passing validation criteria, is used as a model example. Statistic methods have proved that the manufacturing process is reproducible. Methods suitable for elucidation of various properties of the final blend, e.g., measurement of electrostatic charge by Faraday pail and evaluation of mutual influences of researched variables by partial least square (PLS regression, were used. Using these methods, it was proved that the filler with higher particle size increased the content uniformity of both blends and the ensuing tablets. Addition of the lubricant, magnesium stearate, during the blending process improved the content uniformity of blends containing the filler with larger particles. This seems to be caused by reduced sampling error due to the suppression of electrostatic charge.

  6. Development Of New Visible Spectrophotometric Methods For Quantitative Determination Of Almotriptan Malate As An Active Pharmaceutical Ingredient In Formulations

    Directory of Open Access Journals (Sweden)

    U. Viplava Prasad

    2012-06-01

    Full Text Available Purpose: The aim of the investigation was to see the simple and sensitive visible spectrophotometric methods for the determination of the almotriptan malate in bulk and tablet dosage forms. Methods: Two simple, sensitive and cost effective visible spectrophotometric methods (M1-M2 were developed for the estimation of almotriptan malate in bulk and dosage forms. The first method (M1 is based on the formation of blue reduced product by treating drug with Folin Ciocalteu (FC reagent in the presence of sodium carbonate solution with an absorption maximum of 770nm. The second method (M2 is based on the complex formation product by drug with 1, 10-phenanthroline in the presence of Fe (III as an oxidant in phosphoric acid medium with an absorption maximum of 510nm. Results: Beer’s law obeyed in the concentration range of 4-12μg/ml and 1-5 μg/ml for methodM1 and M2 respectively. No interference was observed from the usually existing additives in pharmaceutical formulations and the applicability of the methods was examined by analyzing AXERT tablets containing AM. Conclusion: The reported methods for its assay involve sophisticated equipment, which are very costly and pose problems of maintenance. To overcome these problems, the use of visible spectrophotometric technique is justifiable. The statistical data proved the accuracy, reproducibility and the precision of the proposed methods.

  7. Identification, synthesis and characterization of an unknown process related impurity in eslicarbazepine acetate active pharmaceutical ingredient by LC/ESI–IT/MS, 1H, 13C and 1H–1H COSY NMR

    OpenAIRE

    Saji Thomas; Saroj Kumar Paul; Subhash Chandra Joshi; Vineet Kumar; Ashutosh Agarwal; Dharam Vir

    2014-01-01

    A new impurity was detected during high performance liquid chromatographic (HPLC) analysis of eslicarbazepine acetate active pharmaceutical ingredient. The structure of unknown impurity was postulated based on liquid chromatography mass spectrometry using electrospray ionization and ion trap analyzer (LC/ESI–IT/MS) analysis. Proposed structure of impurity was unambiguously confirmed by synthesis followed by characterization using 1H, 13C nuclear magnetic resonance spectrometry (NMR), 1H–1H co...

  8. HPLC法测定达格列净原料药中有关物质%Determination of related substances in dapagliflozin active pharmaceutical ingredients by HPLC

    Institute of Scientific and Technical Information of China (English)

    陈稳; 郑津津; 王晨

    2015-01-01

    Objective To establish a method for determination of related substances in dapagliflozin active pharmaceutical ingredients.Methods HPLC method was adopted. The determination was carried out on Diamonsil C18 column (250 mm × 4.6 mm, 5 µm). The mobile phase consisted of 0.02 mol/L sodium dihydrogen phosphate - methanol - tetrahydrofuran (60∶35∶5) at a flow rate of 1.0 mL/min. The detective wavelength was set at 220 nm, the column temperature was at 35℃, and the injection volume was 10μL.Results Dapagliflozin and its related substances had good separation. The LOQ of the related substances, such as Z1, Z2, F1, F2, and F3 were1.34, 1.54, 1.42, 1.71, and 2.11 ng, respectively. The average recoveries were 98.9%, 97.6%, 103.2%, 102.4%, and 102.8% with RSD values of 1.8%, 1.3%, 1.5%, 0.7%, and 1.7%, respectively.Conclusion The method is sensitive and accurate, and can be used for quality control of related substances in dapagliflozin active pharmaceutical ingredients.%目的:建立达格列净原料药中有关物质的测定方法。方法采用 HPLC法。Diamonsil C18色谱柱(250 mm×4.6 mm,5μm);以0.02 mol/L磷酸二氢钠水溶液–甲醇–四氢呋喃(60∶35∶5)为流动相;体积流量1.0 mL/min;检测波长220 nm;柱温35℃;进样量为10μL。结果达格列净与各杂质的分离度良好,杂质Z1、Z2、F1、F2、F3的定量限分别为3.22、3.83、3.65、4.33、4.92 ng,平均回收率分别为98.9%、97.6%、103.2%、102.4%、102.8%,RSD值分别为1.8%、1.3%、1.5%、0.7%、1.7%。结论本方法检测灵敏度高,精密度好,可以用于达格列净原料药中有关物质的质量控制。

  9. Determination of related substances in ambrisentan active pharmaceutical ingredients%HPLC法测定安立生坦原料药中有关物质

    Institute of Scientific and Technical Information of China (English)

    陈保来; 李家春; 仲艳; 郭庆明; 沈旺; 王振中; 萧伟

    2015-01-01

    目的:建立安立生坦原料药中有关物质的测定方法。方法采用HPLC法。Waters Atlantis T3色谱柱(250 mm×4.6 mm,5μm);以0.02%三氟乙酸水溶液–0.01%三氟乙酸乙腈溶液为流动相,进行梯度洗脱;柱温30℃;体积流量1.0 mL/min;自动进样器控温5℃;检测波长220 nm。结果安立生坦与各杂质的分离度良好,杂质Z1、Z2、Z3、Z4、DP1的定量限分别为2.14、2.54、2.44、2.45、2.41 ng,平均回收率分别为102.9%、96.0%、93.1%、104.6%、115.2%,RSD值分别为2.1%、4.6%、2.9%、2.7%、4.9%(n=10)。结论该方法检测灵敏度高,精密度好,可以用于安立生坦原料药中有关物质的质量控制。%Objective To establish a method for determination of related substances in ambrisentan active pharmaceutical ingredients. Methods HPLC method was adopted. The determination was performed on Waters Atlantis T3 column (250 mm × 4.6 mm, 5μm) with mobile phase consisted of 0.02% trifluoroacetic acid - acetonitrile (containing 0.01% trifluoroacetic acid) with gradient elution. The temperature of column was set at 30℃. The flow rate was 1.0 mL/min with automatic injection volume of 5μL. The detective wavelength was set at 220 nm. Results Ambrisentan and its related substances could be separated completely. The LOQ of the related substances, such as Z1, Z2, Z3, Z4, and DP1 were 2.14, 2.54, 2.44, 2.45, and 2.41 ng, respectively. They all had good linearity. The average recovery were 102.9%, 96.0%, 93.1%, 104.6%, and 115.2%with RSD values of 2.1%, 4.6%, 2.9%, 2.7%, and 4.9%(n = 10), respectively. Conclusion The method is sensitive and accurate, and can be used for quality control of related substances in ambrisentan active pharmaceutical ingredients.

  10. Dynamics of active pharmaceutical ingredients loads in a Swiss university hospital wastewaters and prediction of the related environmental risk for the aquatic ecosystems.

    Science.gov (United States)

    Daouk, Silwan; Chèvre, Nathalie; Vernaz, Nathalie; Widmer, Christèle; Daali, Youssef; Fleury-Souverain, Sandrine

    2016-03-15

    The wastewater contamination of a Swiss university hospital by active pharmaceutical ingredient (API) residues was evaluated with a three months monitoring campaign at the outlet of the main building. Flow-proportional samples were collected with an automatic refrigerated sampler and analyzed for 15 API, including antibiotics, analgesics, antiepileptic and anti-inflammatory drugs, by using a validated LC-MS/MS method. The metals Gd and Pt were also analyzed using ICP-MS. Measured concentrations were compared to the predicted ones calculated after the drug average consumption data obtained from the hospital pharmacy. The hospital contribution to the total urban load was calculated according to the consumption data obtained from city pharmacies. Lastly, the environmental hazard and risk quotients (RQ) related to the hospital fraction and the total urban consumption were calculated. Median concentrations of the 15 selected compounds were ranging from 0.04 to 675 μg/L, with a mean detection frequency of 84%. The ratio between predicted and measured environmental concentrations (PEC/MEC) has shown a good accuracy for 5 out of 15 compounds, revealing over- and under-estimations of the PEC model. Mean daily loads were ranging between 0.01 and 14.2g/d, with the exception of paracetamol (109.7 g/d). The hospital contribution to the total urban loads varied from 2.1 to 100% according to the compound. While taking into account dilution and removal efficiencies in wastewater treatment plant, only the hospital fraction of the antibiotics ciprofloxacin and sulfamethoxazole showed, respectively, a high (RQ>1) and moderate (RQ>0.1) risk for the aquatic ecosystems. Nevertheless, when considering the total urban consumption, 7 compounds showed potential deleterious effects on aquatic organisms (RQ>1): gabapentin, sulfamethoxazole, ciprofloxacin, piperacillin, ibuprofen, diclofenac and mefenamic acid. In order to reduce inputs of API residues originating from hospitals various

  11. Dynamics of active pharmaceutical ingredients loads in a Swiss university hospital wastewaters and prediction of the related environmental risk for the aquatic ecosystems.

    Science.gov (United States)

    Daouk, Silwan; Chèvre, Nathalie; Vernaz, Nathalie; Widmer, Christèle; Daali, Youssef; Fleury-Souverain, Sandrine

    2016-03-15

    The wastewater contamination of a Swiss university hospital by active pharmaceutical ingredient (API) residues was evaluated with a three months monitoring campaign at the outlet of the main building. Flow-proportional samples were collected with an automatic refrigerated sampler and analyzed for 15 API, including antibiotics, analgesics, antiepileptic and anti-inflammatory drugs, by using a validated LC-MS/MS method. The metals Gd and Pt were also analyzed using ICP-MS. Measured concentrations were compared to the predicted ones calculated after the drug average consumption data obtained from the hospital pharmacy. The hospital contribution to the total urban load was calculated according to the consumption data obtained from city pharmacies. Lastly, the environmental hazard and risk quotients (RQ) related to the hospital fraction and the total urban consumption were calculated. Median concentrations of the 15 selected compounds were ranging from 0.04 to 675 μg/L, with a mean detection frequency of 84%. The ratio between predicted and measured environmental concentrations (PEC/MEC) has shown a good accuracy for 5 out of 15 compounds, revealing over- and under-estimations of the PEC model. Mean daily loads were ranging between 0.01 and 14.2g/d, with the exception of paracetamol (109.7 g/d). The hospital contribution to the total urban loads varied from 2.1 to 100% according to the compound. While taking into account dilution and removal efficiencies in wastewater treatment plant, only the hospital fraction of the antibiotics ciprofloxacin and sulfamethoxazole showed, respectively, a high (RQ>1) and moderate (RQ>0.1) risk for the aquatic ecosystems. Nevertheless, when considering the total urban consumption, 7 compounds showed potential deleterious effects on aquatic organisms (RQ>1): gabapentin, sulfamethoxazole, ciprofloxacin, piperacillin, ibuprofen, diclofenac and mefenamic acid. In order to reduce inputs of API residues originating from hospitals various

  12. Content of Active Pharmaceutical Ingredient with Somatostatin by UPLC Method%UPLC法测定生长抑素原料药的含量

    Institute of Scientific and Technical Information of China (English)

    张承军; 王秀梅; 王建良; 贾长久; 李兰兰

    2012-01-01

    目的:建立快速、准确、灵敏的测定生长抑素原料药的方法.方法:采用沃特世ACQUITY超高液相色谱系统(UPLC),以磷酸(取磷酸11 mL,加水900 mL,用三乙胺调pH至2.3,用水稀释至刻度1 000 mL处)为流动相,(A)-乙腈 (B)梯度洗脱,流速:0.3 mL/min;检测波长为215 nm;柱温45℃;进样体积2μL.结果:生长抑素在0.005 149 2~0.128 73 mg / mL范围内有良好的线性关系(R2= 0.999 3),平均回收率(n=9)为99.1%.结论:UPLC法检测快速、准确、灵敏度高、重复性好,为生长抑素原料药的质量控制提供了一种快速准确的方法.%Objective: To establish a rapid, accurate and sensitive method to determine active pharmaceutical ingredient (API) with somatostatin. Method: Waters ACQUITY UPLC was adopted. Phosphoric acid-triethylamine buffer solution was as mobile phase A and acetonitrile as B, gradient elution was used with flow rate of 0.3 mL/min; detection wave length was 215 nm; column temperature was 45 ℃; injection volume was 2μL. Result: Somatostatin has a great linearity (R2 = 0.999 3) from 0.005 149 2 mg/mL to 0.128 73 mg/mL. Average recovery rate (n= 9) is 99.1%. Conclusion: UPLC method, which is rapid, accurate, sensitive and with good repeatability, could service for quality control of somatostatin (API).

  13. Identification, synthesis and characterization of an unknown process related impurity in eslicarbazepine acetate active pharmaceutical ingredient by LC/ESI-IT/MS, 1H, 13C and 1H-1H COSY NMR

    Institute of Scientific and Technical Information of China (English)

    Saji Thomas; Saroj Kumar Paul; Subhash Chandra Joshi; Vineet Kumar; Ashutosh Agarwal; Dharam Vir

    2014-01-01

    A new impurity was detected during high performance liquid chromatographic (HPLC) analysis of eslicarbazepine acetate active pharmaceutical ingredient. The structure of unknown impurity was postulated based on liquid chromatography mass spectrometry using electrospray ionization and ion trap analyzer (LC/ESI-IT/MS) analysis. Proposed structure of impurity was unambiguously confirmed by synthesis followed by characterization using 1H, 13C nuclear magnetic resonance spectrometry (NMR), 1H-1H correlation spectro-scopy (COSY) and infrared spectroscopy (IR). Based on the spectroscopic and spectrometric data, unknown impurity was characterized as 5-carbamoyl-10,11-dihydro-5H-dibenzo[b,f]azepin-10-yl propionate.

  14. Identification, synthesis and characterization of an unknown process related impurity in eslicarbazepine acetate active pharmaceutical ingredient by LC/ESI–IT/MS, 1H, 13C and 1H–1H COSY NMR

    Directory of Open Access Journals (Sweden)

    Saji Thomas

    2014-10-01

    Full Text Available A new impurity was detected during high performance liquid chromatographic (HPLC analysis of eslicarbazepine acetate active pharmaceutical ingredient. The structure of unknown impurity was postulated based on liquid chromatography mass spectrometry using electrospray ionization and ion trap analyzer (LC/ESI–IT/MS analysis. Proposed structure of impurity was unambiguously confirmed by synthesis followed by characterization using 1H, 13C nuclear magnetic resonance spectrometry (NMR, 1H–1H correlation spectroscopy (COSY and infrared spectroscopy (IR. Based on the spectroscopic and spectrometric data, unknown impurity was characterized as 5-carbamoyl-10,11-dihydro-5H-dibenzo[b,f]azepin-10-yl propionate.

  15. The validation of the analytical method (HPLC, use for identification and assay of the pharmaceutical active ingredient, colistine sulphate and the finished product Colidem 50 – hydrosoluble powder, in SC DELOS impex ‘96 SRL

    Directory of Open Access Journals (Sweden)

    Maria Neagu,

    2011-06-01

    Full Text Available In SC DELOS IMPEX ’96 SRL the quality of the active pharmaceutical ingredient (API for the finished product Colidem 50 - hydrosoluble powder is make according to European Pharmacopoeia, curent edition. The method for analysis use in this purpose is the compendial method „Colistine sulphate” in E.P. in current edition and represent a optimized variant, developed and validated „in house”.The parameters which was included in the methodology validation for chromatographic method are the follow: Selectivity/Specificity, Linearity, Range of Linearity, Limit of Detection and Limit of Quantification, Precision (Repeatability - intra day, inter-Day Reproducibility, Accuracy, Robustness, Stability Solutions and System Suitability.

  16. Environmental Impact Assessment and Management for Active Pharmaceutical Ingredients from Pharmaceutical Wastewater%制药废水药物活性成分的环境影响评价与管理初探

    Institute of Scientific and Technical Information of China (English)

    孟妮; 王峰; 周振

    2011-01-01

    The influence of active pharmaceutical ingredients(API) on the aquatic environment has been increasingly concerned in recent years.The main pathways of API into the environment are through waste discharge from pharmaceutical enterprises,excretion from the body and irrational disposal of unused or expired pharmaceuticals.The ratio between predicted environmental concentration(PEC) and predicted no effect concentration(PNEC) was introduced to evaluate the environmental risk of API in an API management practice,and the environmental risk includes both the effect of API on the aquatic environment and its disturbance to the biological wastewater treatment plant.The method can be applies to the environment management of API for both pharmaceutical enterprises and governmental authorities.%药物活性成分(API)对水环境的影响近年来日益引起关注。API可通过制药企业的废弃物排放、未完全被吸收利用的API排泄以及过期药物的不合理处置三种途径进入水体。通过具体案例分析介绍了制药企业采用预测环境浓度(PEC)和预测无效应浓度(PNEC)的比值对API的环境风险进行评估的方法,API的环境风险包括对自然水体的影响和对污水生物处理系统的干扰。该方法可作为API环境影响分析评价的有效工具用于制药企业的环境管理或者政府部门的监管工作中。

  17. Determination of palladium, platinum and rhodium in used automobile catalysts and active pharmaceutical ingredients using high-resolution continuum source graphite furnace atomic absorption spectrometry and direct solid sample analysis

    International Nuclear Information System (INIS)

    This work investigates the potential of high-resolution continuum source graphite furnace atomic absorption spectrometry for the direct determination of Pd, Pt and Rh in two samples of very different nature. While analysis of active pharmaceutical ingredients is straightforward and it is feasible to minimize matrix effects, to the point that calibration can be carried out against aqueous standard solutions, the analysis of used automobile catalysts is more challenging requiring the addition of a chemical modifier (NH4F·HF) to help in releasing the analytes, a more vigorous temperature program and the use of a solid standard (CRM ERM®-EB504) for calibration. However, in both cases it was possible to obtain accurate results and precision values typically better than 10% RSD in a fast and simple way, while only two determinations are needed for the three analytes, since Pt and Rh can be simultaneously monitored in both types of samples. Overall, the methods proposed seem suited for the determination of these analytes in such types of samples, offering a greener and faster alternative that circumvents the traditional problems associated with sample digestion, requiring a small amount of sample only (0.05 mg per replicate for catalysts, and a few milligrams for the pharmaceuticals) and providing sufficient sensitivity to easily comply with regulations. The LODs achieved were 6.5 μg g−1 (Pd), 8.3 μg g−1 (Pt) and 9.3 μg g−1 (Rh) for catalysts, which decreased to 0.08 μg g−1 (Pd), 0.15 μg g−1 (Pt) and 0.10 μg g−1 (Rh) for pharmaceuticals. - Highlights: • Solid sampling HR CS GFAAS permits the fast and direct determination of Pd, Pt and Rh. • 2 determinations suffice for the 3 elements (2 of them can be measured simultaneously). • Samples as different as car catalysts and pharmaceuticals can be accurately analyzed. • Aqueous standards (pharmaceuticals) or a solid CRM (catalysts) is used for calibration. • 6–9 μg g−1 (catalysts) and 0.1–0

  18. Determination of palladium, platinum and rhodium in used automobile catalysts and active pharmaceutical ingredients using high-resolution continuum source graphite furnace atomic absorption spectrometry and direct solid sample analysis

    Energy Technology Data Exchange (ETDEWEB)

    Resano, Martín, E-mail: mresano@unizar.es [Department of Analytical Chemistry, Aragón Institute of Engineering Research (I3A), University of Zaragoza, Pedro Cerbuna 12, 50009 Zaragoza (Spain); Flórez, María del Rosario [Department of Analytical Chemistry, Aragón Institute of Engineering Research (I3A), University of Zaragoza, Pedro Cerbuna 12, 50009 Zaragoza (Spain); Queralt, Ignasi [Institute of Earth Sciences Jaume Almera ICTJA-CSIC, Sole Sabarís s/n, 08028 Barcelona (Spain); Marguí, Eva [Department of Chemistry, Faculty of Sciences, Universitat de Girona, Campus Montilivi s/n, 17071 Girona (Spain)

    2015-03-01

    This work investigates the potential of high-resolution continuum source graphite furnace atomic absorption spectrometry for the direct determination of Pd, Pt and Rh in two samples of very different nature. While analysis of active pharmaceutical ingredients is straightforward and it is feasible to minimize matrix effects, to the point that calibration can be carried out against aqueous standard solutions, the analysis of used automobile catalysts is more challenging requiring the addition of a chemical modifier (NH{sub 4}F·HF) to help in releasing the analytes, a more vigorous temperature program and the use of a solid standard (CRM ERM®-EB504) for calibration. However, in both cases it was possible to obtain accurate results and precision values typically better than 10% RSD in a fast and simple way, while only two determinations are needed for the three analytes, since Pt and Rh can be simultaneously monitored in both types of samples. Overall, the methods proposed seem suited for the determination of these analytes in such types of samples, offering a greener and faster alternative that circumvents the traditional problems associated with sample digestion, requiring a small amount of sample only (0.05 mg per replicate for catalysts, and a few milligrams for the pharmaceuticals) and providing sufficient sensitivity to easily comply with regulations. The LODs achieved were 6.5 μg g{sup −1} (Pd), 8.3 μg g{sup −1} (Pt) and 9.3 μg g{sup −1} (Rh) for catalysts, which decreased to 0.08 μg g{sup −1} (Pd), 0.15 μg g{sup −1} (Pt) and 0.10 μg g{sup −1} (Rh) for pharmaceuticals. - Highlights: • Solid sampling HR CS GFAAS permits the fast and direct determination of Pd, Pt and Rh. • 2 determinations suffice for the 3 elements (2 of them can be measured simultaneously). • Samples as different as car catalysts and pharmaceuticals can be accurately analyzed. • Aqueous standards (pharmaceuticals) or a solid CRM (catalysts) is used for calibration.

  19. Rapid Detection of Active Pharmaceutical Ingredients in Weak Active Pharmaceutical Ingredient Signal Drugs by Paper Substrate-Surface Enhanced Raman Scattering Spectrometry%纸基-表面增强拉曼光谱法快速检测弱主药信号药品中的主药成分

    Institute of Scientific and Technical Information of China (English)

    李晓; 陈梦云; 王磊; 张倩倩; 方芳; 苗丽; 陆峰

    2015-01-01

    A rapid detection method of active pharmaceutical ingredients( API) in weak API signal drugs by surface enhanced Raman scattering ( SERS) technology combined with paper substrate was established in this work. By soaking the filter paper in silver nanoparticles solution ( Ag NPs) to synthesize Ag NPs-paper as the substrate, and then the sample solution was dropping on the substrate with SERS detection. On the basis of strengthen ability of Ag NPs-paper, result of SERS detection and optimal preparation conditions, the fast identification method of weak API signal drugs was established. In this case, the SERS spectra of weak API signal drugs and their standards SERS spectra were obtained, where the correlation coefficient of weak API signal drug SERS spectra and its standard was more than 0. 9. The result showed that by this method, the low content API in weak API signal drugs could be well investigated, and the deficiencies of the normal Raman spectroscopy efficiently was also overcome. In conclusion, the synthesize method of Ag NPs-paper was simple, and the strengthen effect of this Ag NPs-paper on the intensity was obviously observed. Paper substrate-SERS method was simple, rapid and sensitive, and could be used to detect weak API signal drugs, presenting broad application prospects in the rapid detection of weak API signal drugs.%建立了弱主药信号药品中主药成分的纸基-表面增强拉曼光谱( SERS)快速检测方法。采用浸泡法制备纳米银溶胶滤纸SERS基底(简称银胶纸),将待检样品滴加于银胶纸上进行SERS检测。通过考察银胶纸制备条件、银胶纸增强能力、SERS检测结果,建立用于弱主药信号药品中主药成分的快速检测方法。通过本方法获得弱主药信号药品中主药成分的SERS图谱,与其对应标准品图谱的相关系数大于0.9,较好地检测出弱主药信号药品中的主药成分,有效克服了常规拉曼光谱分析的不足之处。新型银胶纸制备简

  20. Determination of palladium, platinum and rhodium in used automobile catalysts and active pharmaceutical ingredients using high-resolution continuum source graphite furnace atomic absorption spectrometry and direct solid sample analysis

    Science.gov (United States)

    Resano, Martín; Flórez, María del Rosario; Queralt, Ignasi; Marguí, Eva

    2015-03-01

    This work investigates the potential of high-resolution continuum source graphite furnace atomic absorption spectrometry for the direct determination of Pd, Pt and Rh in two samples of very different nature. While analysis of active pharmaceutical ingredients is straightforward and it is feasible to minimize matrix effects, to the point that calibration can be carried out against aqueous standard solutions, the analysis of used automobile catalysts is more challenging requiring the addition of a chemical modifier (NH4F·HF) to help in releasing the analytes, a more vigorous temperature program and the use of a solid standard (CRM ERM®-EB504) for calibration. However, in both cases it was possible to obtain accurate results and precision values typically better than 10% RSD in a fast and simple way, while only two determinations are needed for the three analytes, since Pt and Rh can be simultaneously monitored in both types of samples. Overall, the methods proposed seem suited for the determination of these analytes in such types of samples, offering a greener and faster alternative that circumvents the traditional problems associated with sample digestion, requiring a small amount of sample only (0.05 mg per replicate for catalysts, and a few milligrams for the pharmaceuticals) and providing sufficient sensitivity to easily comply with regulations. The LODs achieved were 6.5 μg g- 1 (Pd), 8.3 μg g- 1 (Pt) and 9.3 μg g- 1 (Rh) for catalysts, which decreased to 0.08 μg g- 1 (Pd), 0.15 μg g- 1 (Pt) and 0.10 μg g- 1 (Rh) for pharmaceuticals.

  1. 阿莫西林原料药中有关物质的UPLC-TOF-MS/MS鉴定%Identification of related substances in amoxicillin active pharmaceutical ingredients by UPLC-TOF-MS/MS

    Institute of Scientific and Technical Information of China (English)

    雷勇胜; 宋丽明; 郝英魁; 王云; 李瑜; 蒋庆峰

    2015-01-01

    目的:快速鉴定阿莫西林原料药中的有关物质。方法采用UPLC-TOF-MS/MS法测定。Waters Acquity UPLCTM BEH色谱柱(100 mm×2.1 mm,1.7μm);流动相为乙酸铵体系;体积流量0.5 mL/min;检测波长254 nm;柱温30℃;进样量10μL。电喷雾电离源;正离子检测;毛细管电压3.0 kV;离子源温度120℃;雾化气温度500℃;雾化气体积流量700 L/h;锥孔气体积流量50 L/h。结果推测了阿莫西林原料药中6个杂质的化学结构及其裂解规律,同时与欧洲药典中的杂质进行了比对归属。结论建立的UPLC-TOF-MS/MS的方法和实验数据可为阿莫西林原料药的质量控制提供了重要依据。%Objective To establish a rapid identification method for related substances in amoxicillin active pharmaceutical ingredients. Methods UPLC-TOF-MS/MS method was used. HPLC was carried out on Waters Acquity UPLCTM BEH column (100 mm × 2.1 mm, 1.7μm) with ammonium acetate solution as mobile phase. The detection wavelength was 254 nm and injection volume was 10μL at the flow rate of 0.5 mL/min. The column temperature was set for 30℃. MS conditions were that a mass spectrometry equipped with electrospray ionization (ESI) (+) source for detection. Capillary voltage was 3.0 kV, and source temperature was 120℃. The desolvation temperature and flow rate of desolvation gas were 500℃ and 700 L/h. The flow rate of cone gas was 50 L/h. Results The structures and fragmentation regularities of six related substances in amoxicillin were elucidated according to their MS characteristics. At the same time, related substances were compared to the impurities from European Pharmacopoeia. Conclusion UPLC-TOF-MS/MS method and results can establish a basis for quality control and stability study of amoxicillin active pharmaceutical ingredients.

  2. Sterilization of pharmaceutical ingredients, adjuvants and packaging materials by gamma radiation

    International Nuclear Information System (INIS)

    Different antibiotics, pharmaceutical ingredients, adjuvants and packaging materials were treated with gamma radiation of 0.5-2.8x106 rad using 60Co source. The effect of 2.5-2.8x106 rad on antibiotics, carbohydrates, citiric acid is a discoloration in some degree. The change of colour was accompanied by a decrease of activity of oxytetracycline hydrochloride and tobramycin sulphate, a decrease of viscosity of starch, and an increase of the reducing rate of saccharose and lactose. The sterility of substances contaminated by 103 organisms per gram was obtained by a dose of 0.5x106 rad. There was no discoloration and no changes were observed in the examined parameter of these materials. The examined aluminium, rubber and plastic packaging materials suffered no changes. (author)

  3. PTSD: A Search for "Active Ingredients."

    Science.gov (United States)

    Huber, Charles H.

    1997-01-01

    Family counselors working with individuals suffering the effects of trauma are encouraged to consider the "active ingredients" found by Charles Figley and Joyce Carbonell at Florida State University and reported in the two articles reviewed. (Author/MKA)

  4. STABILITY TESTING OF ACTIVE PHARMACEUTICAL INGREDIENT [API

    Directory of Open Access Journals (Sweden)

    Agarwal Vipul

    2012-04-01

    Full Text Available Stability plays an important role in drug development process. It explains several factors that affect the quality of a drug substance or drug products varies with time under the influence of environmental factors such as temperature, humidity and light. Stability studies play a vital role to decide the re-test period and shelf life for the drug substance and recommended storage conditions of API. ICH and EMEA guidelines define stability data package for new drug substance or drug product that is sufficient for a registration application within the three regions of the EC, Japan and United States.

  5. 21 CFR 341.12 - Antihistamine active ingredients.

    Science.gov (United States)

    2010-04-01

    ... 21 Food and Drugs 5 2010-04-01 2010-04-01 false Antihistamine active ingredients. 341.12 Section 341.12 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED...-COUNTER HUMAN USE Active Ingredients § 341.12 Antihistamine active ingredients. The active ingredient...

  6. Improved metabolites of pharmaceutical ingredient grade Ginkgo biloba and the correlated proteomics analysis.

    Science.gov (United States)

    Zheng, Wen; Li, Ximin; Zhang, Lin; Zhang, Yanzhen; Lu, Xiaoping; Tian, Jingkui

    2015-06-01

    Ginkgo biloba is an attractive and traditional medicinal plant, and has been widely used as a phytomedicine in the prevention and treatment of cardiovascular and cerebrovascular diseases. Flavonoids and terpene lactones are the major bioactive components of Ginkgo, whereas the ginkgolic acids (GAs) with strong allergenic properties are strictly controlled. In this study, we tested the content of flavonoids and GAs under ultraviolet-B (UV-B) treatment and performed comparative proteomic analyses to determine the differential proteins that occur upon UV-B radiation. That might play a crucial role in producing flavonoids and GAs. Our phytochemical analyses demonstrated that UV-B irradiation significantly increased the content of active flavonoids, and decreased the content of toxic GAs. We conducted comparative proteomic analysis of both whole leaf and chloroplasts proteins. In total, 27 differential proteins in the whole leaf and 43 differential proteins in the chloroplast were positively identified and functionally annotated. The proteomic data suggested that enhanced UV-B radiation exposure activated antioxidants and stress-responsive proteins as well as reduced the rate of photosynthesis. We demonstrate that UV-B irradiation pharmaceutically improved the metabolic ingredients of Ginkgo, particularly in terms of reducing GAs. With high UV absorption properties, and antioxidant activities, the flavonoids were likely highly induced as protective molecules following UV-B irradiation.

  7. The search for compounds that stimulate thermogenesis in obesity management: from pharmaceuticals to functional food ingredients

    OpenAIRE

    Dulloo, Abdull G.

    2012-01-01

    The concept of managing obesity through the stimulation of thermogenesis is currently a focus of considerable attention by the pharmaceutical, nutraceutical and functional food industries. This paper first reviews the landmark discoveries that have fuelled the search for thermogenic anti-obesity products that range from single-target drugs to multi-target functional foods. It subsequently analyses the thermogenic and fat-oxidizing potentials of a wide array of bioactive food ingredients which...

  8. Bioequivalence of Eslicarbazepine Acetate from Two Different Sources of its Active Product Ingredient in Healthy Subjects

    OpenAIRE

    Falcão, Amílcar; Lima, Ricardo; Sousa, Rui; Nunes, Teresa; Soares-da-Silva, Patrício

    2013-01-01

    Purpose To compare the bioavailability (BA) and pharmacokinetic (PK) properties and to demonstrate the bioequivalence (BE) between two active product ingredient (API) sources of eslicarbazepine acetate (ESL) in healthy volunteers. Design, subjects and methods Forty healthy male and female subjects aged 18–40 years were randomized to treatment with 400 or 800 mg ESL marketed (MF) formulation [current active pharmaceutical ingredient (API) source] and 400 or 800 mg ESL to-be-marketed (TBM) form...

  9. Radiation sensitivity of fungal microflora isolated from some pharmaceutical ingredients

    International Nuclear Information System (INIS)

    The total number of fungal microflora of D-glucose, NaCl, KCl and their solutions was determined. The fungal isolates were identified as Aspergillus fumigatus. Aspergillus niger; Spicaria divaricate and Spicaria silvatica and their response to γ-radiation was determined, the most predominant isolate Asp. fumigatus was also the most irradiation resistant. The Dio and the lethal dose were determined for each isolate in a pure spore suspension as well as in the presence of the other isolates. The higher lethal dose values obtained for pure spore suspension as compared to that obtained for the natural fungal flora a D-glucose are discussed in terms of spore clumping. The activity of amylase, protease and L-asparaginase of Asp. fumigatus was examined prior to and after exposure to different doses of γ-radiation. Though all were inhibited at high doses, the effect was not as drastic as it was on cell viability

  10. 21 CFR 347.20 - Permitted combinations of active ingredients.

    Science.gov (United States)

    2010-04-01

    ... antiseptic active ingredients. Any one (two when required to be in combination) or more of the active... generally recognized as safe and effective single first aid antiseptic active ingredient, or any...

  11. Identification of uniformity in Pravastatin Sodium Tablets and crystallographic form in their active pharmaceutical ingredient by NIRS method%近红外光谱法鉴别普伐他汀钠片及其原料药晶型的一致性研究

    Institute of Scientific and Technical Information of China (English)

    耿颖; 程奇蕾; 何兰

    2014-01-01

    目的:建立全覆盖抽样的普伐他汀钠片的近红外光谱法一致性检验模型,考察制剂工艺的差别和原料药晶型的差异,通过稳健、准确、代表性强的近红外光谱一致性模型实现普伐他汀钠片的快速检验和筛查。方法对评价性抽验抽取的5个企业中的4个共65批样品建立普伐他汀钠片近红外一致性检验模型,并对4个厂家的原料药的近红外光谱图进行比较。结果建立了4个厂家普伐他汀钠片剂的近红外一致性模型,预测成功率均为100%;4种原料药和1种无定型粉末的近红外光谱图显示不同晶型光谱图具有差异。结论近红外光谱法能够用于快速鉴别质量工艺稳定的普伐他汀钠片产品,对制剂工艺进行考察,并能够区分不同晶型的原料药。%Objective To develop near-infrared spectroscopy (NIRS) uniformity models for sampling of Pravastatin Sodium Tablets from overall manufactures in Chinese market, to evaluate the uniformity of Pravastatin Sodium Tablets and their active pharmaceutical ingredients, and provide robust, accurate, and representative uniformity models. Methods NIRS models for 65 batches of tablets were built for four individual manufactures from five manufactures. The active pharmaceutical ingredients form the four manufactures and an amorphous powder were investigated by comparing NIR spectrum. Results Uniformity Models for the four different manufactures were built with prediction rate 100%, respectively. The spectra of four active pharmaceutical ingredients and an amorphous powder showed differences in various crystallographic forms of NIRS. Conclusion It demonstrates the potential of NIRS being a rapid and highly effective method for the identification of Pravastatin Sodium Tablats, the investigation of their preparation process, and the discrimination of the active pharmaceutical ingredients from their various crystallographic forms.

  12. Expanding the analytical toolbox for identity testing of pharmaceutical ingredients: Spectroscopic screening of dextrose using portable Raman and near infrared spectrometers.

    Science.gov (United States)

    Srivastava, Hirsch K; Wolfgang, Steven; Rodriguez, Jason D

    2016-03-31

    In the pharmaceutical industry, dextrose is used as an active ingredient in parenteral solutions and as an inactive ingredient (excipient) in tablets and capsules. In order to address the need for more sophisticated analytical techniques, we report our efforts to develop enhanced identification methods to screen pharmaceutical ingredients at risk for adulteration or substitution using field-deployable spectroscopic screening. In this paper, we report our results for a study designed to evaluate the performance of field-deployable Raman and near infrared (NIR) methods to identify dextrose samples. We report a comparison of the sensitivity of the spectroscopic screening methods against current compendial identification tests that rely largely on a colorimetric assay. Our findings indicate that NIR and Raman spectroscopy are both able to distinguish dextrose by hydration state and from other sugar substitutes with 100% accuracy for all methods tested including spectral correlation based library methods, principal component analysis and classification methods. PMID:26965331

  13. 21 CFR 333.210 - Antifungal active ingredients.

    Science.gov (United States)

    2010-04-01

    ... 21 Food and Drugs 5 2010-04-01 2010-04-01 false Antifungal active ingredients. 333.210 Section 333.210 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED... Antifungal Drug Products § 333.210 Antifungal active ingredients. The active ingredient of the...

  14. 21 CFR 344.12 - Ear drying aid active ingredient.

    Science.gov (United States)

    2010-04-01

    ... 21 Food and Drugs 5 2010-04-01 2010-04-01 false Ear drying aid active ingredient. 344.12 Section 344.12 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED....12 Ear drying aid active ingredient. The active ingredient of the product consists of...

  15. Simple and direct determination of active ingredients in drugs by neutron activation analysis

    International Nuclear Information System (INIS)

    The increasing number of drugs in the market and the need for their control requires new, simple, fast and accurate analytical methods. Iodine, iron, manganese, silver and sodium were determined by INAA in various pharmaceutical formulations, representing capsules, injectables, powders for injection, solutions and tablets. From the results it appears that NAA could be used as an official method for the determination of iron, manganese and silver in pharmaceutical products, in which these elements are present as active ingredients, as well as for the control of the concentration limits for iodine and sodium. (author)

  16. Polyphenols as active ingredients for cosmetic products.

    Science.gov (United States)

    Zillich, O V; Schweiggert-Weisz, U; Eisner, P; Kerscher, M

    2015-10-01

    Polyphenols are secondary plant metabolites with antioxidant, anti-inflammatory and anti-microbial activity. They are ubiquitously distributed in the plant kingdom; high amounts contain, for example, green tea and grape seeds. Polyphenolic extracts are attractive ingredients for cosmetics and pharmacy due to their beneficial biological properties. This review summarizes the effects of polyphenols in the context of anti-ageing activity. We have explored in vitro studies, which investigate antioxidant activity, inhibition of dermal proteases and photoprotective activity, mostly studied using dermal fibroblasts or epidermal keratinocytes cell lines. Possible negative effects of polyphenols were also discussed. Further, some physicochemical aspects, namely the possible interactions with emulsifiers and the influence of the cosmetic formulation on the skin delivery, were reported. Finally, few clinical studies, which cover the anti-ageing action of polyphenols on the skin after topical application, were reviewed. PMID:25712493

  17. Plant Cell Cultures as Source of Cosmetic Active Ingredients

    Directory of Open Access Journals (Sweden)

    Ani Barbulova

    2014-04-01

    Full Text Available The last decades witnessed a great demand of natural remedies. As a result, medicinal plants have been increasingly cultivated on a commercial scale, but the yield, the productive quality and the safety have not always been satisfactory. Plant cell cultures provide useful alternatives for the production of active ingredients for biomedical and cosmetic uses, since they represent standardized, contaminant-free and biosustainable systems, which allow the production of desired compounds on an industrial scale. Moreover, thanks to their totipotency, plant cells grown as liquid suspension cultures can be used as “biofactories” for the production of commercially interesting secondary metabolites, which are in many cases synthesized in low amounts in plant tissues and differentially distributed in the plant organs, such as roots, leaves, flowers or fruits. Although it is very widespread in the pharmaceutical industry, plant cell culture technology is not yet very common in the cosmetic field. The aim of the present review is to focus on the successful research accomplishments in the development of plant cell cultures for the production of active ingredients for cosmetic applications.

  18. Tests Comparing of Benzylpenicillin Potassium Industry Salt and Benzylpenicillin Potassium Active Pharmaceutical Ingredient by Methods in Chinese Veterinary Pharmacopoeia%利用兽药典方法对青霉素钾工业盐和原料药的检测比较

    Institute of Scientific and Technical Information of China (English)

    徐嫄; 于丽娜; 韩宁宁; 龚旭昊; 王静文; 郝利华; 赵晖

    2016-01-01

    In order to distinguish between benzylpenicillin potassium industry salt and benzylpenicillin potassium active pharmaceutical ingredient,4 bathes of industry salt samples and 4 bathes of active pharmaceutical ingredient samples offered by 4 different veterinary drug manufacturers respectively were identified according to quality standards in Chinese Veterinary Pharmacopoeia 2010 version.Results of those 8 batches of samples were all in compliance with the standards,however,finding no distinguish differences between industry salt and active pharmaceutical ingredient,which might indicate that quality standard of benzylpenicillin potassium need to be improved in order to enhance quality control of the finished drug -benzylpeninicillin potassium for injection.%为了辨别青霉素钾工业盐和青霉素钾原料药,依据《中国兽药典》中青霉素钾的质量标准,对四家青霉素原料药生产企业提供的4批青霉素钾工业盐和4批青霉素钾原料药进行了检测,项目包括性状、鉴别、吸光度、结晶性、溶液澄清度与颜色、青霉素聚合物、干燥失重、不溶性微粒、酸碱度、有关物质、细菌内毒素、可见异物、无菌和含量测定。结果表明,8批样品均符合现行兽药典青霉素钾标准中各项规定,但结果无法用以区分青霉素钾工业盐和青霉素钾原料药,提示青霉素钾的质量标准需进一步完善,以提高对成品药———注射用青霉素钾的质量控制。

  19. 21 CFR 331.11 - Listing of specific active ingredients.

    Science.gov (United States)

    2010-04-01

    .... (5) Dihydroxyaluminum sodium carbonate. (b) Bicarbonate-containing active ingredients: Bicarbonate...., 8 grams calcium carbonate). (e) Citrate-containing active ingredients: Citrate ion, as citric acid... old and 100 mEq. of bicarbonate ion for persons 60 years or older. (2) Sodium potassium tartrate....

  20. Choleretic Activity of Turmeric and its Active Ingredients.

    Science.gov (United States)

    Wang, Yonglu; Wang, Liyao; Zhu, Xinyi; Wang, Dong; Li, Xueming

    2016-07-01

    Turmeric, a rhizome of Curcumin longa L. is widely used as both a spice and an herbal medicine. The traditional use of turmeric in gastroenterology is mainly based on its choleretic activity. The aim of this study is to determine the effects of turmeric on bile flow (BF) and total bile acids (TBAs) excretion in a bile fistula rat model after acute duodenal administration. A significant dose-dependent enhancement in both BF and TBAs was detected after treatment with the turmeric decoctions which suggested the choleretic activity was bile acid-dependent secretion. In order to direct the active group of compounds, aqueous (AE), ethyl acetate (EtOAc), and petroleum ether (PE) extracts were investigated. The EtOAc and PE extracts showing high effects were purified to locate the active ingredients. Three curcuminoids (curcumin, demethoxycurcumin, and bisdemethoxycurcumin) and 2 sesquiterpenes (bisacurone B and ar-turmerone) were isolated. It was found Bisacurone B was the most potent choleretic ingredient followed by ar-turmerone, bisdemethoxycurcumin demethoxycurcumin, and then curcumin. The amounts of the active ingredients were quantitatively analyzed by high-performance liquid chromatography. The EtOAc and PE extracts had high sesquiterpenes and curcuminoids content, while the AE extract had poor content of sesquiterpenes and curcuminoids which affected neither BF nor TBAs. Based on the results of multiple linear regression analysis, the content of BIS and TUR were dominant factors (P < 0.01) of controlling BL and TBAs in EtOAC and PE extracts.

  1. 21 CFR 338.10 - Nighttime sleep-aid active ingredients.

    Science.gov (United States)

    2010-04-01

    ... 21 Food and Drugs 5 2010-04-01 2010-04-01 false Nighttime sleep-aid active ingredients. 338.10... (CONTINUED) DRUGS FOR HUMAN USE NIGHTTIME SLEEP-AID DRUG PRODUCTS FOR OVER-THE-COUNTER HUMAN USE Active Ingredients § 338.10 Nighttime sleep-aid active ingredients. The active ingredient of the product consists...

  2. 77 FR 60124 - Draft Guidance for Industry on Initial Completeness Assessments for Type II Active Pharmaceutical...

    Science.gov (United States)

    2012-10-02

    ... HUMAN SERVICES Food and Drug Administration Draft Guidance for Industry on Initial Completeness Assessments for Type II Active Pharmaceutical Ingredient Drug Master Files Under the Generic Drug User Fee Amendments of 2012 AGENCY: Food and Drug Administration, HHS. ACTION: Notice. SUMMARY: The Food and...

  3. Studies of Active Ingredients in Cough Syrup by Capillary Zone Electrophoresis with Amperometric Detection

    Institute of Scientific and Technical Information of China (English)

    ZHOU Tian-shu; WANG Ai-fang; WU Fang; SHI Guo-yue; FANG Yu-zhi

    2003-01-01

    The present paper covers a simple, reliable and reproducible method, based on capillary zone electrophoresis(CZE) with amperometric detection(AD), for the separation and the determination of ephedrine hydrochloride, promethazine hydrochloride and codeine phosphate. Under the optimal conditions, the three analytes were base-line separated completely within 16 min. Good linear relationships between the peak heights and the concentrations of the three analytes were obtained with the correlation coefficients better than 0.9993. The method was directly applied to the determination of the active ingredients in pharmaceutical preparations and the assay results were satisfactory.

  4. Metabolically active functional food ingredients for weight control.

    Science.gov (United States)

    Kovacs, E M R; Mela, D J

    2006-02-01

    The scale of the obesity epidemic creates a pressing consumer need as well as an enormous business opportunity for successful development and marketing of food products with added benefits for weight control. A number of proposed functional food ingredients have been shown to act post-absorptively to influence substrate utilization or thermogenesis. Characteristics and supporting data on conjugated linoleic acid, diglycerides, medium-chain triglycerides, green tea, ephedrine, caffeine, capsaicin and calcium, are reviewed here, giving examples of how these could act to alter energy expenditure or appetite control. Consideration is also given to other factors, in addition to efficacy, which must be satisfied to get such ingredients into foods. We conclude that, for each of the safe, putatively metabolically active agents, there remain gaps in clinical evidence or knowledge of mechanisms, which need to be addressed in order to specify the dietary conditions and food product compositions where these ingredients could be of most benefit for weight control. PMID:16436103

  5. 21 CFR 343.13 - Rheumatologic active ingredients.

    Science.gov (United States)

    2010-04-01

    ... 21 Food and Drugs 5 2010-04-01 2010-04-01 false Rheumatologic active ingredients. 343.13 Section 343.13 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) DRUGS FOR HUMAN USE INTERNAL ANALGESIC, ANTIPYRETIC, AND ANTIRHEUMATIC DRUG PRODUCTS FOR...

  6. 21 CFR 343.12 - Cardiovascular active ingredients.

    Science.gov (United States)

    2010-04-01

    ... 21 Food and Drugs 5 2010-04-01 2010-04-01 false Cardiovascular active ingredients. 343.12 Section 343.12 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) DRUGS FOR HUMAN USE INTERNAL ANALGESIC, ANTIPYRETIC, AND ANTIRHEUMATIC DRUG PRODUCTS FOR...

  7. Synthesis of cinacalcet: an enantiopure active pharmaceutical ingredient (API)

    OpenAIRE

    Barniol-Xicota, Marta; Leiva Martínez, Rosana; Escolano Mirón, Carmen; Vázquez Cruz, Santiago

    2016-01-01

    Cinacalcet hydrochloride is the only approved drug acting as calcimimetic, a new class of compds. used in the therapy of secondary hyperparathyroidism and parathyroid carcinoma. Several generic drug manufacturers and research groups from academia have reported alternative approaches to this mol., mainly from (R)​-​(+)​-​1-​(1-​naphthyl)​ethylamine. There are mainly three strategies that have been used to couple this readily accessible enantiopure amine to the other part of the mol.: amide for...

  8. Solubility Prediction of Active Pharmaceutical Compounds with the UNIFAC Model

    Science.gov (United States)

    Nouar, Abderrahim; Benmessaoud, Ibtissem; Koutchoukali, Ouahiba; Koutchoukali, Mohamed Salah

    2016-03-01

    The crystallization from solution of an active pharmaceutical ingredient requires the knowledge of the solubility in the entire temperature range investigated during the process. However, during the development of a new active ingredient, these data are missing. Its experimental determination is possible, but tedious. UNIFAC Group contribution method Fredenslund et al. (Vapor-liquid equilibria using UNIFAC: a group contribution method, 1977; AIChE J 21:1086, 1975) can be used to predict this physical property. Several modifications on this model have been proposed since its development in 1977, modified UNIFAC of Dortmund Weidlich et al. (Ind Eng Chem Res 26:1372, 1987), Gmehling et al. (Ind Eng Chem Res 32:178, 1993), Pharma-modified UNIFAC Diedrichs et al. (Evaluation und Erweiterung thermodynamischer Modelle zur Vorhersage von Wirkstofflöslichkeiten, PhD Thesis, 2010), KT-UNIFAC Kang et al. (Ind Eng Chem Res 41:3260, 2002), ldots In this study, we used UNIFAC model by considering the linear temperature dependence of interaction parameters as in Pharma-modified UNIFAC and structural groups as defined by KT-UNIFAC first-order model. More than 100 binary datasets were involved in the estimation of interaction parameters. These new parameters were then used to calculate activity coefficient and solubility of some molecules in various solvents at different temperatures. The model gives better results than those from the original UNIFAC and shows good agreement between the experimental solubility and the calculated one.

  9. 78 FR 70043 - Pesticide Product Registration; Receipt of an Application for a New Active Ingredient

    Science.gov (United States)

    2013-11-22

    ... AGENCY Pesticide Product Registration; Receipt of an Application for a New Active Ingredient AGENCY... pesticide product containing an active ingredient not included in any previously registered pesticide product. Pursuant to the Federal Insecticide, Fungicide, and Rodenticide Act (FIFRA), EPA is...

  10. 75 FR 6386 - Pesticide Products; Registration Applications for a New Active Ingredient Chemical; Demiditraz

    Science.gov (United States)

    2010-02-09

    ... register pesticide products containing active ingredients not included in any previously registered pesticide products. Pursuant to the provisions of section 3(c)(4) of the Federal Insecticide, Fungicide, and... AGENCY Pesticide Products; Registration Applications for a New Active Ingredient Chemical;...

  11. 78 FR 32246 - Pesticide Products; Registration Applications for New Active Ingredients

    Science.gov (United States)

    2013-05-29

    ... 12014, Research Triangle Park, NC 27709. Active ingredient: Flupyradifurone. Product Type: Insecticide..., Stewartsville, NJ 08886. Active ingredient: Ethyl Formate. Product Type: Insecticide. Proposed Use: Fumigant on.... Pursuant to the Federal Insecticide, Fungicide, and Rodenticide Act (FIFRA), EPA is hereby providing...

  12. Evaluation of P-Listed Pharmaceutical Residues in Empty Pharmaceutical Containers

    Science.gov (United States)

    Under the Resource Conservation and Recovery Act (RCRA), some pharmaceuticals are considered acute hazardous wastes because their sole active pharmaceutical ingredients are P-listed commercial chemical products (40 CFR 261.33). Hospitals and other healthcare facilities have stru...

  13. Development and validation of stability indicating UPLC assay method for ziprasidone active pharma ingredient

    Directory of Open Access Journals (Sweden)

    Sonam Mittal

    2012-01-01

    Full Text Available Background: Ziprasidone, a novel antipsychotic, exhibits a potent highly selective antagonistic activity on D2 and 5HT2A receptors. Literature survey for ziprasidone revealed several analytical methods based on different techniques but no UPLC method has been reported so far. Aim: Aim of this research paper is to present a simple and rapid stability indicating isocratic, ultra performance liquid chromatographic (UPLC method which was developed and validated for the determination of ziprasidone active pharmaceutical ingredient. Forced degradation studies of ziprasidone were studied under acid, base, oxidative hydrolysis, thermal stress and photo stress conditions. Materials and Methods: The quantitative determination of ziprasidone drug was performed on a Supelco analytical column (100×2.1 mm i.d., 2.7 ΅m with 10 mM ammonium acetate buffer (pH: 6.7 and acetonitrile (ACN as mobile phase with the ratio (55:45-Buffer:ACN at a flow rate of 0.35 ml/ min. For UPLC method, UV detection was made at 318 nm and the run time was 3 min. Developed UPLC method was validated as per ICH guidelines. Results and Conclusion: Mild degradation of the drug substance was observed during oxidative hydrolysis and considerable degradation observed during basic hydrolysis. During method validation, parameters such as precision, linearity, ruggedness, stability, robustness, and specificity were evaluated, which remained within acceptable limits. Developed UPLC method was successfully applied for evaluating assay of Ziprasidone active Pharma ingredient.

  14. Wisdom Pharmaceutical Co., Ltd.

    Institute of Scientific and Technical Information of China (English)

    2003-01-01

    @@ Wisdom Pharmaceutical Co., Ltd. (Wisdom) headquartered in Haimen, Nantong, Jiangsu Province, China, is specialized in providing highly efficient production processes of active pharmaceutical ingredients (API) and intermediates. Currently, Wisdom is in the process of expanding GMP (Good Manufacturing Practice) capabilities, which is expected to be approved by the authorities before the end of September 2003.

  15. Validation of an assessment tool for evaluating the implementation of WHO GMP standards by Chinese manufacturers of active pharmaceutical ingredients (APIs)%我国原料药生产企业执行WHO GMP的评估工具验证

    Institute of Scientific and Technical Information of China (English)

    黄宝斌; 孙新生; 许明哲; 白东亭; 武志昂; 吴春福

    2015-01-01

    目的:为客观评估我国活性原料药(active pharmaceutical ingredients,APIs)生产企业执行WHO GMP中的能力和现状,对评估工具进行验证,考察工具的信度(可靠性)和效度(准确性).方法:根据设定标准,筛选国内3家APIs生产企业和9名GMP专家参与验证.对于每家企业,先后应用评估工具进行自我评价和GMP专家独立评估,比较3种(严重、主要和次要)缺陷差异,考察信度.对参与评估的GMP专家进行问卷调查和访谈,评价工具对WHO GMP标准覆盖的全面性和代表性,考察效度.收集和整理企业和专家对于评估工具改进建议.结果:企业自评和专家独立评估结果均显示,3家企业均无“严重”缺陷项.在自评中,企业A,B,C的“主要”和“次要”缺陷项数量分别是(2;9),(22;36),(3;8);在独立评估中,企业A,B,C的“主要”和“次要”缺陷分别是(3;12),(26;41),(4;9).经统计学分析,企业自评和专家独立评估结果之间没有显著差异.专家访谈显示,9名专家均认为评估工具覆盖性良好,除4名专家认为4个评估指标有重复外,其余5名专家均认为代表性良好.企业和专家提出建议,对于指标重复、规定过细、缺乏操作性的情况进行改进.结论:经适宜企业和专家参与验证,认为该评估工具具有良好的信度和效度,能够测评我国APIs企业执行WHO GMP标准的差距和进度,在进行适当调整和完善后,可以在国内推广使用.

  16. Aloe vera: a valuable ingredient for the food, pharmaceutical and cosmetic industries--a review.

    Science.gov (United States)

    Eshun, Kojo; He, Qian

    2004-01-01

    Scientific investigations on Aloe vera have gained more attention over the last several decades due to its reputable medicinal properties. Some publications have appeared in reputable Scientific Journals that have made appreciable contributions to the discovery of the functions and utilizations of Aloe--"nature's gift." Chemical analysis reveals that Aloe vera contains various carbohydrate polymers, notably glucomannans, along with a range of other organic and inorganic components. Although many physiological properties of Aloe vera have been described, it still remains uncertain as to which of the component(s) is responsible for these physiological properties. Further research needs to be done to unravel the myth surrounding the biological activities and the functional properties of A. vera. Appropriate processing techniques should be employed during the stabilization of the gel in order to affect and extend its field of utilization. PMID:15116756

  17. Suspended biofilm carrier and activated sludge removal of acidic pharmaceuticals

    DEFF Research Database (Denmark)

    Falås, Per; Baillon-Dhumez, Aude; Andersen, Henrik Rasmus;

    2012-01-01

    Removal of seven active pharmaceutical substances (ibuprofen, ketoprofen, naproxen, diclofenac, clofibric acid, mefenamic acid, and gemfibrozil) was assessed by batch experiments, with suspended biofilm carriers and activated sludge from several full-scale wastewater treatment plants. A distinct ...... bacteria to degrade or transform the target pharmaceuticals was further demonstrated by the limited pharmaceutical removal in an experiment with continuous nitritation and biofilm carriers from a partial nitritation/anammox sludge liquor treatment process....

  18. 21 CFR 358.110 - Wart remover active ingredients.

    Science.gov (United States)

    2010-04-01

    ... ingredient. (a) Salicylic acid 12 to 40 percent in a plaster vehicle. (b) Salicylic acid 5 to 17 percent in a collodion-like vehicle. (c) Salicylic acid 15 percent in a karaya gum, glycol plaster vehicle....

  19. 75 FR 53691 - Pesticide Products; Registration Applications for a New Active Ingredient Chemical Sedaxane

    Science.gov (United States)

    2010-09-01

    ... AGENCY Pesticide Products; Registration Applications for a New Active Ingredient Chemical Sedaxane AGENCY... pesticide products containing an active ingredient not included in any previously registered pesticide products. Pursuant to the provisions of section 3(c)(4) of the Federal Insecticide, Fungicide,...

  20. Selecting an optimal instrument to identify active ingredients of the motivational interviewing-process

    NARCIS (Netherlands)

    Dobber, Jos; Meijel, Berno van; Barkhof, Emile; Scholte op Reimer, Wilma; Latour, Corine; Peters, Ron; Linszen, Don

    2014-01-01

    Motivational Interviewing (MI) can effectively stimulate motivation for health behavior change, but the active ingredients of MI are not well known. To help clinicians further stimulate motivation, they need to know the active ingredients of MI. A psychometrically sound instrument is required to ide

  1. Internet as a Medium of Pharmaceutical Companies Promotional Activities

    OpenAIRE

    Darko Pantelic

    2009-01-01

    Pharmaceuticals market is highly regulated, and it can be stated that prescription (legal or ethical) drugs have a status of substances in controlled circulation. Promotional activities are also under strict legislation, further burdened with ethical consideration and public scrutiny. Internet as liberal and hard to control medium brings entirely new sets of solutions and/or problems to pharmaceuticals market(ers).

  2. 21 CFR 341.14 - Antitussive active ingredients.

    Science.gov (United States)

    2010-04-01

    ...) DRUGS FOR HUMAN USE COLD, COUGH, ALLERGY, BRONCHODILATOR, AND ANTIASTHMATIC DRUG PRODUCTS FOR OVER-THE... established for each ingredient in § 341.74(d): (a) Oral antitussives. (1) Chlophedianol hydrochloride. (2... and 21 CFR 1308.15(c). (i) Codeine. (ii) Codeine phosphate. (iii) Codeine sulfate....

  3. Studies on Insecticidal Activities and Active Ingredients of Stephania kwangsiensis Lo.

    Institute of Scientific and Technical Information of China (English)

    DENG Ye-cheng; XU Han-hong

    2005-01-01

    Insecticidal activities and active ingredients of Stephania kwangsiensis Lo. were studied for the first time. The results showed that all parts of S. kwangsiensis Lo. had contact activity against brown planthoppers, Nilaparvata lugens Stal,and the contact activity of methanol extract from root tubers was the highest, with a LD50 value being 1.5794 μg/female.l-roemerine was isolated from root tubers of S. kwangsiensis Lo. and identified, and it was the main active ingredient.l-roemerine had high contact toxicity to brown planthoppers, with a LD50 value being 0.0443 μg/female. Contact toxicity of l-roemerine to brown planthoppers was 7.48 times that of malathion, the convientional chemical insecticide used for controlling brown planthoppers.l-roemerine also had stomach poison activity against brown planthoppers.

  4. The Role of PharmEcovigilance in Reducing the Environmental Footprint of Pharmaceuticals

    Science.gov (United States)

    The prescribing and usage of medications have ramifications extending far beyond conventional medical care. The pharmaceutical and healthcare industries have an environmental footprint because the active pharmaceutical ingredients (APIs) can enter the environment as contaminants ...

  5. Equivalence studies for complex active ingredients and dosage forms

    OpenAIRE

    Bhattycharyya, Lokesh; Dabbah, Roger; Hauck, Walter; Sheinin, Eric; Yeoman, Lynn; Williams, Roger,

    2005-01-01

    This article examines the United States Pharmacopeia (USP) and its role in assessing the equivalence and inequivalence of biological and biotechnological drug substances and products—a role USP has played since its founding in 1820. A public monograph in theUnited States Pharmacopeia-National Formulary helps practitioners and other interested parties understand how an article’s strenght, quality, and purity should be controlled. Such a monograph is a standard to which all manufactured ingredi...

  6. 21 CFR 201.322 - Over-the-counter drug products containing internal analgesic/antipyretic active ingredients...

    Science.gov (United States)

    2010-04-01

    ... analgesic/antipyretic active ingredients; required alcohol warning. 201.322 Section 201.322 Food and Drugs... containing internal analgesic/antipyretic active ingredients; required alcohol warning. (a) People who... internal analgesic/antipyretic active ingredients may cause similar adverse effects. FDA concludes that...

  7. Health effects of Vaccinium myrtillus L.: evaluation of efficacy and technological strategies for preservation of active ingredients.

    Science.gov (United States)

    Smeriglio, Antonella; Monteleone, Domenico; Trombetta, Domenico

    2014-01-01

    Bilberries are a rich dietary source of various phytonutrients, including anthocyanins which contribute greatly to their antioxidant capacity and have demonstrated a broad spectrum of biomedical functions. These include protection against cardiovascular disorders, age-induced oxidative stress, inflammatory responses and several degenerative diseases. Berry anthocyanins also improve neuronal and cognitive brain functions, ocular health as well as protecting genomic DNA integrity. In recent years, sales of many dietary supplements/pharmaceutical products containing anthocyanins in various dosages and formulations have been made by advertising their wide range of beneficial effects. However, there is a heightened risk of distributing deteriorated formulations to consumers due to lax regulations, in particular those applicable to phytochemical characterization and extract standardization, and in terms of quality regarding the stability of anthocyanins. Anthocyanin pigments readily degrade during industrial processing and this can have a dramatic impact on color quality and may also affect nutritional/pharmaceutical properties. This review aims to summarize the main health effects of bilberry extract used in several food supplements/pharmaceutical formulations focusing on some important aspects of anthocyanin degradation during processing and storage. It will also describe the main technological strategies which can give active ingredients greater stability, solubility and dispersibility in order to enhance formulation quality which is of great interest to the consumer and industry due to its direct and indirect impact on consumer health.

  8. Opinions expressed by Italian National Advisory Toxicological Committee on some active ingredients of pesticides

    Energy Technology Data Exchange (ETDEWEB)

    Camoni, I. [Ist. Superiore di Sanita`, Rome (Italy). Lab. di Tossicologia Applicata

    1996-03-01

    The opinions expressed by the Italian National Advisory Toxicological Committee (CCTN) on some active ingredients of pesticides are presented. Carcinogenic and mutagenic effects of these substances have been examined and, on this basis, an evaluation and relative classification were expressed.

  9. Consensus Modeling for Prediction of Estrogenic Activity of Ingredients Commonly Used in Sunscreen Products

    Directory of Open Access Journals (Sweden)

    Huixiao Hong

    2016-09-01

    Full Text Available Sunscreen products are predominantly regulated as over-the-counter (OTC drugs by the US FDA. The “active” ingredients function as ultraviolet filters. Once a sunscreen product is generally recognized as safe and effective (GRASE via an OTC drug review process, new formulations using these ingredients do not require FDA review and approval, however, the majority of ingredients have never been tested to uncover any potential endocrine activity and their ability to interact with the estrogen receptor (ER is unknown, despite the fact that this is a very extensively studied target related to endocrine activity. Consequently, we have developed an in silico model to prioritize single ingredient estrogen receptor activity for use when actual animal data are inadequate, equivocal, or absent. It relies on consensus modeling to qualitatively and quantitatively predict ER binding activity. As proof of concept, the model was applied to ingredients commonly used in sunscreen products worldwide and a few reference chemicals. Of the 32 chemicals with unknown ER binding activity that were evaluated, seven were predicted to be active estrogenic compounds. Five of the seven were confirmed by the published data. Further experimental data is needed to confirm the other two predictions.

  10. Influence of environmental factors on the contents of active ingredients and radical scavenging property of potentilla fruticosa in the main production areas of China

    International Nuclear Information System (INIS)

    Extracts from Potentilla fruticosa have been applied in traditional medicine and exhibited antioxidant property, but little has been known about the diversity of phytochemicals and properties on this species from different growing environment. This study investigated the influence of environmental factors on the active ingredient contents and radical scavenging property of P. fruticosa from different production areas of China in order to discover a location could produce high-quality resources for pharmaceutical products. The contents of tannin, total flavonoids, and rutin were determined and varied within the range of 7.64 ± 0.43 ∼ 10.68 ± 0.67 percentage, 2.29 ± 0.34 ∼ 5.37 ± 0.36 percentage, and 0.19 ± 0.053 ∼ 0.79 ± 0.125 percentage, respectively. Radical scavenging property was quantified, with the IC /sub 50/ of 7.24 ± 0.423 to 17.23 ± 0.551 μ g mL-1. Principal component analysis, multiple linear stepwise regression analysis, and path analysis were conducted to further analysis the relationship between the variations of active ingredients and radical scavenging capacity and growth environment. The results showed dominant environmental factors for these variations were rapidly available nitrogen, rapidly available phosphorus, pH, July average temperature, and annual sunshine duration. Furthermore, a significant positive correlation was observed between pH, annual sunshine duration and active ingredients and radical scavenging property (p<0.05). Considering the high active ingredient contents and strong radical scavenging property, leaf extracts from P. fruticosa could become useful supplements for pharmaceutical products as a new antioxidant agent, and Huzhu Northern Mountain in Qinghai Province and E-mei Mountain in Sichuan Province were selected as favorable production locations. (author)

  11. Data-mining of potential antitubercular activities from molecular ingredients of traditional Chinese medicines

    Directory of Open Access Journals (Sweden)

    Salma Jamal

    2014-07-01

    Full Text Available Background. Traditional Chinese medicine encompasses a well established alternate system of medicine based on a broad range of herbal formulations and is practiced extensively in the region for the treatment of a wide variety of diseases. In recent years, several reports describe in depth studies of the molecular ingredients of traditional Chinese medicines on the biological activities including anti-bacterial activities. The availability of a well-curated dataset of molecular ingredients of traditional Chinese medicines and accurate in-silico cheminformatics models for data mining for antitubercular agents and computational filters to prioritize molecules has prompted us to search for potential hits from these datasets. Results. We used a consensus approach to predict molecules with potential antitubercular activities from a large dataset of molecular ingredients of traditional Chinese medicines available in the public domain. We further prioritized 160 molecules based on five computational filters (SMARTSfilter so as to avoid potentially undesirable molecules. We further examined the molecules for permeability across Mycobacterial cell wall and for potential activities against non-replicating and drug tolerant Mycobacteria. Additional in-depth literature surveys for the reported antitubercular activities of the molecular ingredients and their sources were considered for drawing support to prioritization. Conclusions. Our analysis suggests that datasets of molecular ingredients of traditional Chinese medicines offer a new opportunity to mine for potential biological activities. In this report, we suggest a proof-of-concept methodology to prioritize molecules for further experimental assays using a variety of computational tools. We also additionally suggest that a subset of prioritized molecules could be used for evaluation for tuberculosis due to their additional effect against non-replicating tuberculosis as well as the additional hepato

  12. Study on THz spectra of the active ingredients in the TCM

    Science.gov (United States)

    Ma, ShiHua; Wang, WenFeng; Liu, GuiFeng; Ge, Min; Zhu, ZhiYong

    2008-03-01

    Terahertz spectroscopy has tremendous potential for applications to evaluate the quality of the drugs including the TCM. In this paper, the Terahertz Time-Domain Spectroscopy investigated two active ingredients: Andrographolide and Dehydroandrographoline, isolated from Andrographis paniculata (Burm. f.) Nees. We also measured the mixtures of two active ingredients at the different ratio and the quantitative analysis is also applied to determine the contents of compound. The Terahertz spectroscopy is a potential and promising technique in identifying the components, evaluating the drugs sanitation and inspecting the quality of medicine including TCM.

  13. Encapsulation of cosmetic active ingredients for topical application--a review.

    Science.gov (United States)

    Casanova, Francisca; Santos, Lúcia

    2016-02-01

    Microencapsulation is finding increasing applications in cosmetics and personal care markets. This article provides an overall discussion on encapsulation of cosmetically active ingredients and encapsulation techniques for cosmetic and personal care products for topical applications. Some of the challenges are identified and critical aspects and future perspectives are addressed. Many cosmetics and personal care products contain biologically active substances that require encapsulation for increased stability of the active materials. The topical and transdermal delivery of active cosmetic ingredients requires effective, controlled and safe means of reaching the target site within the skin. Preservation of the active ingredients is also essential during formulation, storage and application of the final cosmetic product. Microencapsulation offers an ideal and unique carrier system for cosmetic active ingredients, as it has the potential to respond to all these requirements. The encapsulated agent can be released by several mechanisms, such as mechanical action, heat, diffusion, pH, biodegradation and dissolution. The selection of the encapsulation technique and shell material depends on the final application of the product, considering physical and chemical stability, concentration, required particle size, release mechanism and manufacturing costs. PMID:26612271

  14. INFLUENCE OF SELECTED PHARMACEUTICALS ON ACTIVATED SLUDGE DEHYDROGENASE ACTIVITY

    OpenAIRE

    Agnieszka Tomska

    2016-01-01

    Due to the increasing consumption of pharmaceuticals for the treatment of humans and animals as well as inadequate procedures for the disposal of pharmaceuticals into environmental, pollution caused by them is increasing. Generally these substances are introduced to the wastewater treatment plant with municipal wastewater. They are often resistant to biodegradation and can cause to the disruption in biological wastewater treatment processes. Traditional water treatment plants are not designed...

  15. Potential metal impurities in active pharmaceutical substances and finished medicinal products - A market surveillance study.

    Science.gov (United States)

    Wollein, Uwe; Bauer, Bettina; Habernegg, Renate; Schramek, Nicholas

    2015-09-18

    A market surveillance study has been established by using different atomic spectrometric methods for the determination of selected elemental impurities of particular interest, to gain an overview about the quality of presently marketed drug products and their bulk drug substances. The limit tests were carried out with respect to the existing EMA guideline on the specification limits for residuals of metal catalysts or metal reagents. Also attention was given to the future implementation of two new chapters of the United States Pharmacopoeia (USP) stating limit concentrations of elemental impurities. The methods used for determination of metal residues were inductively coupled plasma-mass spectrometry (ICP-MS), inductively coupled plasma-optical emission spectrometry (ICP-OES), and atomic absorption spectrometry technologies (GFAAS, CVAAS, HGAAS). This article presents the development and validation of the methods used for the determination of 21 selected metals in 113 samples from drug products and their active pharmaceutical ingredients. PMID:26036232

  16. Potential metal impurities in active pharmaceutical substances and finished medicinal products - A market surveillance study.

    Science.gov (United States)

    Wollein, Uwe; Bauer, Bettina; Habernegg, Renate; Schramek, Nicholas

    2015-09-18

    A market surveillance study has been established by using different atomic spectrometric methods for the determination of selected elemental impurities of particular interest, to gain an overview about the quality of presently marketed drug products and their bulk drug substances. The limit tests were carried out with respect to the existing EMA guideline on the specification limits for residuals of metal catalysts or metal reagents. Also attention was given to the future implementation of two new chapters of the United States Pharmacopoeia (USP) stating limit concentrations of elemental impurities. The methods used for determination of metal residues were inductively coupled plasma-mass spectrometry (ICP-MS), inductively coupled plasma-optical emission spectrometry (ICP-OES), and atomic absorption spectrometry technologies (GFAAS, CVAAS, HGAAS). This article presents the development and validation of the methods used for the determination of 21 selected metals in 113 samples from drug products and their active pharmaceutical ingredients.

  17. 77 FR 48519 - Registration Applications for Pesticide Products Containing New Active Ingredients

    Science.gov (United States)

    2012-08-14

    .... israelensis, Strain SUM-6218 at 100.0%. Product Type: microbial insecticide. Proposed Use: Manufacturing use..., Kalamazoo, MI 49008. Active Ingredient: GS-U-ACTX-Hv1a-SEQ2 at 30.00%. Product Type: Insecticide. Proposed...%. Product Type: Insecticide. Proposed Uses: For use on ornamental plants, turf, vegetables, fruits,...

  18. 21 CFR 343.22 - Permitted combinations of active ingredients for cardiovascular-rheumatologic use.

    Science.gov (United States)

    2010-04-01

    ... 21 Food and Drugs 5 2010-04-01 2010-04-01 false Permitted combinations of active ingredients for cardiovascular-rheumatologic use. 343.22 Section 343.22 Food and Drugs FOOD AND DRUG ADMINISTRATION, DEPARTMENT OF HEALTH AND HUMAN SERVICES (CONTINUED) DRUGS FOR HUMAN USE INTERNAL ANALGESIC, ANTIPYRETIC,...

  19. 78 FR 64937 - Pesticide Products; Registration Applications for New Active Ingredients

    Science.gov (United States)

    2013-10-30

    ... type: Fungicide. Proposed uses: Greenhouse, field use, and home and garden use on various fruits and vegetables, cotton, hops, tobacco, fruit and nut trees, turf, and ornamentals. (BPPD) List of Subjects..., Japan. Active ingredient: Momfluorothrin. Product type: Insecticide. Proposed uses: Non-food...

  20. 21 CFR 358.710 - Active ingredients for the control of dandruff, seborrheic dermatitis, or psoriasis.

    Science.gov (United States)

    2010-04-01

    ... to be applied and left on the skin or scalp. (4) Salicylic acid, 1.8 to 3 percent. (5) Selenium...) Salicylic acid, 1.8 to 3 percent. (5) Selenium sulfide, 1 percent. (c) Active ingredients for the control of... used and the concentration of the coal tar present in the final product. (2) Salicylic acid, 1.8 to...

  1. PharmEcovigilance and the Environmental Footprint of Pharmaceuticals

    Science.gov (United States)

    The prescribing and usage of medications have ramifications extending far beyond conventional medical care. The healthcare industry has an environmental footprint because the active ingredients from pharmaceuticals enter the environment as pollutants by a variety of routes, prima...

  2. A simple and fast method for the determination of active ingredient in antiperspirant cosmetics by neutron activation analysis

    International Nuclear Information System (INIS)

    Antiperspirant cosmetics are tested for their active ingredient (aluminium chlorohydroxide) by conventional analytical techniques. Aluminium has been determined by instrumental neutron activation analysis in all antiperspirant products and package forms available in the Greek market in order to develop a simple and fast method for quantization. The results show that neutron activation analysis could be established as an official method for the determination of active ingredient in antiperspirant cosmetics. The proposed method is compared with the existing official methods and an alternative sampling method for aerosol package is presented. (author)

  3. Theory-based active ingredients of effective treatments for substance use disorders.

    Science.gov (United States)

    Moos, Rudolf H

    2007-05-11

    This paper describes four related theories that specify common social processes that protect individuals from developing substance use disorders and may underlie effective psychosocial treatments for these disorders: social control theory, behavioral economics and behavioral choice theory, social learning theory, and stress and coping theory. It then provides an overview of the rationale and evidence for four effective psychosocial treatments for substance use disorders: motivational interviewing and motivational enhancement therapy, 12-step facilitation treatment, cognitive-behavioral treatment and behavioral family counseling, and contingency management and community reinforcement approaches. The presumed active ingredients of these treatments are described in terms of how they exemplify the social processes highlighted by the four theories. The identified common components of effective treatment include support, goal direction, and structure; an emphasis on rewards that compete with substance use, a focus on abstinence-oriented norms and models, and attempts to develop self-efficacy and coping skills. Several issues that need to be addressed to enhance our understanding of the active ingredients involved in effective treatment are discussed, including how to develop measures of these ingredients, how well the ingredients predict outcomes and influence conceptually comparable aspects of clients' life contexts, and how much their influence varies depending upon clients' demographic and personal characteristics. PMID:17129682

  4. Theory-based active ingredients of effective treatments for substance use disorders.

    Science.gov (United States)

    Moos, Rudolf H

    2007-05-11

    This paper describes four related theories that specify common social processes that protect individuals from developing substance use disorders and may underlie effective psychosocial treatments for these disorders: social control theory, behavioral economics and behavioral choice theory, social learning theory, and stress and coping theory. It then provides an overview of the rationale and evidence for four effective psychosocial treatments for substance use disorders: motivational interviewing and motivational enhancement therapy, 12-step facilitation treatment, cognitive-behavioral treatment and behavioral family counseling, and contingency management and community reinforcement approaches. The presumed active ingredients of these treatments are described in terms of how they exemplify the social processes highlighted by the four theories. The identified common components of effective treatment include support, goal direction, and structure; an emphasis on rewards that compete with substance use, a focus on abstinence-oriented norms and models, and attempts to develop self-efficacy and coping skills. Several issues that need to be addressed to enhance our understanding of the active ingredients involved in effective treatment are discussed, including how to develop measures of these ingredients, how well the ingredients predict outcomes and influence conceptually comparable aspects of clients' life contexts, and how much their influence varies depending upon clients' demographic and personal characteristics.

  5. ANTIMICROBIAL ACTIVITY OF WATER EXTRACTS OF TRIKATU CHURNA AND ITS INDIVIDUAL INGREDIENT

    Directory of Open Access Journals (Sweden)

    P.R. Malvankar* and M. M. Abhyankar

    2012-04-01

    Full Text Available Trikatu churna is one of the traditional poly herbal preparation, formed by mixing equal quantities of three important spicy materials such as Piper longum L. (Piperaceae, Piper nigrum L. (Piperaceae and Zingiber officinale Roscoe (Zingiberaceae. Trikatu is also known as “ Three Bitters”. The trikatu preparation was reported to contain alkaloids, phenols, tannins, flavanoids, steroids, lignin & saponins. The objective of study is to evaluate the antimicrobial activity of trikatu churna & its individual ingredients with their preliminary phytochemical study. The aqueous extracts of trikatu churna & its each ingredient were tested for antimicrobial activity against certain bacterial strains of Escherichia coli, Staphylococcus aureus by in vitro agar well diffusion method and the results are recorded as the zone of inhibition. Trikatu churna was found to possess higher extent of phytoconstituents with promising antimicrobial activity.

  6. A slow-release system of bacterial cellulose gel and nanoparticles for hydrophobic active ingredients.

    Science.gov (United States)

    Numata, Yukari; Mazzarino, Leticia; Borsali, Redouane

    2015-01-01

    A combination of bacterial cellulose (BC) gel and amphiphilic block copolymer nanoparticles was investigated as a drug delivery system (DDS) for hydrophobic active ingredients. Poly(ethylene oxide)-b-poly(caprolactone) (PEO-b-PCL) and retinol were used as the block copolymer and hydrophobic active ingredient, respectively. The BC gel was capable of incorporating copolymer nanoparticles and releasing them in an acetic acid-sodium acetate buffer solution (pH 5.2) at 37 °C. The percentage of released copolymer reached a maximum value of approximately 60% after 6h and remained constant after 24h. The percentage of retinol released from the copolymer-containing BC gel reached a maximum value at 4h. These results show that the combination of BC gel and nanoparticles is a slow-release system that may be useful in the cosmetic and biomedical fields for skin treatment and preparation. PMID:25840273

  7. An active ingredient of Cat's Claw water extracts identification and efficacy of quinic acid.

    Science.gov (United States)

    Sheng, Yezhou; Akesson, Christina; Holmgren, Kristin; Bryngelsson, Carl; Giamapa, Vincent; Pero, Ronald W

    2005-01-15

    Historic medicinal practice has defined Cat's Claw, also known as Una de Gato or Uncaria tomentosa, as an effective treatment for several health disorders including chronic inflammation, gastrointestinal dysfunction such as ulcers, tumors and infections. The efficacy of Cat's Claw was originally believed, as early as the 1960s, to be due to the presence of oxindole alkaloids. However, more recently water-soluble Cat's Claw extracts were shown not to contain significant amounts of alkaloids (<0.05%), and yet still were shown to be very efficacious. Here we characterize the active ingredients of a water-soluble Cat's Claw extract called C-Med-100 as inhibiting cell growth without cell death thus providing enhanced opportunities for DNA repair, and the consequences thereof, such as immune stimulation, anti-inflammation and cancer prevention. The active ingredients were chemically defined as quinic acid esters and could also be shown to be bioactive in vivo as quinic acid. PMID:15619581

  8. In vitro effects of buyang huanwu decoction and its ingredients on inhibiting the specific binding of 3H-platelet activating factor to its receptor in rabbits

    Institute of Scientific and Technical Information of China (English)

    2007-01-01

    BACKGROUND: Pharmacologic action of traditional Chinese medicine compound is the comprehensive effect of various ingredients, and the interactions of various ingredients are closely correlated with the final effect. In order to reveal the compatibility mechanism of buyang huanwu decoction (BHD)'s prescription in treating and preventing ischemic cerebrovascular disease, we need to explore the effect and relation of ingredients in prescription except for considering the effect of each ingredient on the whole prescription.OBJECTIVE: To study the effect of BHD and its ingredients in the prescription on the specific binding of 3H-platelet activating factor (PAF) to its receptor (PAFR)in rabbits in vitro, and to analyze the action of each ingredient in the prescription.DESIGN: A decomposed recipe study based on orthogonal test.SETTING: Guangzhou University of Traditional Chinese Medicine.MATERIALS: Five healthy adult New Zealand rabbits of either gender were provided by the Experimental Animal Center of Guangzhou University of Traditional Chinese medicine. The prescription herbal pieces were purchased from Foshan Kangpu Pharmaceuticals Company and Jianmin Pharmaceuticals Company, and were appraised by Professor Yanchen Xu from College of Traditional Chinese Medicine, Guangzhou University of Traditional Chinese Medicine. 3H-PAF was supplied by Amersham Co.,Ltd.(Specific activity:6.475 TBq/mmol;batch number:200402); PAF standard by Biomol Co., Ltd.(batch number: P1318V).METHODS: This experiment was carried out in the Laboratory of Nuclear Medicine, Guangzhou University of Traditional Chinese Medicine between September and December 2004. ① The seven influencing factors were selected: such as Shenghuangqi , Dangguiwei, Chishao, Dilong, Taoren, Honghua, Chuanxiong. Each factor was divided into two levels, selected or not selected. The tests were arranged according to L8 (27) orthogonal test table. ②The specific binding of 3H-PAF to its receptors in rabbits was measured by

  9. Validation of the quality control methods for active ingredients of Fungirex cream

    International Nuclear Information System (INIS)

    Fungirex cream is a two-drug product, that is, undecylenic acid and zinc undecylenate over a suitable basis. Since this is a product not documented in the official monographs of the pharmacopoeia, simple analytical methods were suggested for quantitation of analytes of interest in the cream, which are useful for release of newly prepared cream batches. To validate two volumetric methods for the quality control of active ingredients in Fungirex cream

  10. Arbuscular mycorrhizal symbiosis and active ingredients of medicinal plants: current research status and prospectives.

    Science.gov (United States)

    Zeng, Yan; Guo, Lan-Ping; Chen, Bao-Dong; Hao, Zhi-Peng; Wang, Ji-Yong; Huang, Lu-Qi; Yang, Guang; Cui, Xiu-Ming; Yang, Li; Wu, Zhao-Xiang; Chen, Mei-Lan; Zhang, Yan

    2013-05-01

    Medicinal plants have been used world-wide for thousands of years and are widely recognized as having high healing but minor toxic side effects. The scarcity and increasing demand for medicinal plants and their products have promoted the development of artificial cultivation of medicinal plants. Currently, one of the prominent issues in medicinal cultivation systems is the unstable quality of the products. Arbuscular mycorrhiza (AM) affects secondary metabolism and the production of active ingredients of medicinal plants and thus influence the quality of herbal medicines. In this review, we have assembled, analyzed, and summarized the effects of AM symbioses on secondary metabolites of medicinal plants. We conclude that symbiosis of AM is conducive to favorable characteristics of medicinal plants, by improving the production and accumulation of important active ingredients of medicinal plants such as terpenes, phenols, and alkaloids, optimizing the composition of different active ingredients in medicinal plants and ultimately improving the quality of herbal materials. We are convinced that the AM symbiosis will benefit the cultivation of medicinal plants and improve the total yield and quality of herbal materials. Through this review, we hope to draw attention to the status and prospects of, and arouse more interest in, the research field of medicinal plants and mycorrhiza.

  11. Release effect of the active ingredients using a radiation cross linking technology

    Energy Technology Data Exchange (ETDEWEB)

    Hwang, Seung Hyun; Ahn, Sung Jun; Park, Jong Seok; Jeong, Sung In; Gwon, Hui Jeong; Lim, Youn Mook [Research Division for Industry and Environment, Korea Atomic Energy Research Institute, Jeongeup (Korea, Republic of); Lee, Dong Yun [Dept. of Bioengineering, Division of Applied Chemical and Bio Engineering, Hanyang University, Seoul (Korea, Republic of)

    2015-12-15

    Typical radiation cross-linked hydrogels has the characteristic that high water content, but low emission efficiency of active ingredients. Therefore, the hydrogel was prepared by the addition to collagen, which is closely related to the formation of skin wrinkles in biocompatibility and highly water-soluble carboxymethyl cellulose sodium salt (CMC) in order to preparation of hydrogels has excellent emission efficiency of active ingredients. Hydrogels were prepared by dissolving CMC and collagen each of 0.5%, 10% concentration in deionized water. Then, prepared hydrogels are performed by gamma-radiation at 1, 3, 5 kGy irradiation dose. The results showed that the gel fraction of after irradiated 3 kGy hydrogel was higher than before irradiated gelation as long as the 55.3%. The swelling rate of irradiated 3 kGy hydrogel was lower than the non-irradiated sample. The compressive strength of 3 kGy irradiated hydrogel was the highest. The visco-elastic did not show any significant differences, even after irradiation. The CMC hydrogel in this study suggested a potential use as a material for the mask pack for improved emission efficiency of the active ingredient and anti-wrinkles.

  12. Comparison of Active Ingredient Content of Nanwuweizi and Beiwuweizi Collected in Different Seasons Detected by HPLC-DAD

    Institute of Scientific and Technical Information of China (English)

    YAO Feng; CHEN Da-shuai

    2015-01-01

    Objective:To compare the active ingredient content of Nanwuweizi (Kadsura longepedunculata) and Beiwuweizi (Fructus Schisandrae Chinensis) collected in different seasons. Methods:Microwave-assisted extraction was applied to extract the active ingredients in Nanwuweizi and Beiwuweizi, with methanol as the solvent. High performance liquid chromatography-diode array detection (HPLC-DAD) method was used to analyze the content of each ingredient, with chromatographic conditions as follows: Brava BDS C18 column (250 mm×4.6 mm, 5 μm); column temperature: 30℃; mobile phase: water (A) - acetonitrile (B); gradient elution: 0.8 mL/min; and detection wavelength: 225 nm. Results:All ingredients waiting for detection reached their peaks within 75 min, with excellent degree of separation and higher number of theoretical plates. Standard curves were drawn, and the mean value of phase relationship of each ingredient was >0.999. The content of active ingredients in lignans of Nanwuweizi and Beiwuweizi showed tendency of increase ifrst and then decreased. In addition, all ingredients in Beiwuweizi reached their peaks in September while those in Nanwuweizi in August. Conclusion:This method can be used to detect the content of multiple ingredients in Wuweizi (Schisandra chinensis) simultaneously because it is simple in operation, precise in results and excellent in repeatability.

  13. Comparison of Active Ingredient Content of Nanwuweizi and Beiwuweizi Collected in Different Seasons Detected by HPLC-DAD

    Directory of Open Access Journals (Sweden)

    Feng YAO

    2015-12-01

    Full Text Available Abstract Objective: To compare the active ingredient content of Nanwuweizi (Kadsura longepedunculata and Beiwuweizi (Fructus Schisandrae Chinensis collected in different seasons. Methods: Microwave-assisted extraction was applied to extract the active ingredients in Nanwuweizi and Beiwuweizi, with methanol as the solvent. High performance liquid chromatography-diode array detection ℃; mobile phase: water (A - acetonitrile (B; gradient elution: 0.8 mL/min; and detection wavelength: 225 nm. (HPLC-DAD method was used to analyze the content of each ingredient, with chromatographic conditions as follows: Brava BDS C18 column (250 mm×4.6 mm, 5 μm; column temperature: 30 Results: All ingredients waiting for detection reached their peaks within 75 min, with excellent degree of separation and higher number of theoretical plates. Standard curves were drawn, and the mean value of phase relationship of each ingredient was >0.999. The content of active ingredients in lignans of Nanwuweizi and Beiwuweizi showed tendency of increase first and then decreased. In addition, all ingredients in Beiwuweizi reached their peaks in September while those in Nanwuweizi in August. Conclusion: This method can be used to detect the content of multiple ingredients in Wuweizi (Schisandra chinensis simultaneously because it is simple in operation, precise in results and excellent in repeatability.

  14. New Trends in Cosmetics: By-Products of Plant Origin and Their Potential Use as Cosmetic Active Ingredients

    Directory of Open Access Journals (Sweden)

    Ani Barbulova

    2015-04-01

    Full Text Available In recent years, the amount of waste deriving from industrial processes has increased substantially. Many industries produce different types of disposable by-products, rich in valuable compounds. Their characterization and valorization could not only convert them into high value products with application in diverse biotechnological fields, such as Pharmaceutics, Food or Cosmetics, but would also reduce the waste environmental impact and the related treatment costs. There are many examples of cosmetic active ingredients deriving from fish, meat and dairy products, but in the present review we would like to focus on the potentialities and the current use of compounds and extracts deriving from agronomical disposable wastes in the cosmetic field. These types of products are effective, inexpensive and bio-sustainable, and thus represent a valid alternative to the regular plant derived extracts, more commonly adopted in cosmetic formulations. Moreover, if the waste products come from organic farming, they are certainly an even more valuable source of safe extracts for Cosmetics, since they lack any residual pesticide or potentially toxic chemical.

  15. Solubilization of active ingredients of different polarity in Pluronic® micellar solutions - Correlations between solubilizate polarity and solubilization site.

    Science.gov (United States)

    Nguyen-Kim, Viet; Prévost, Sylvain; Seidel, Karsten; Maier, Walter; Marguerre, Ann-Kathrin; Oetter, Günter; Tadros, Tharwat; Gradzielski, Michael

    2016-09-01

    The solubilization of two pharmaceutically active ingredients (AI) with significantly different water solubility, namely carbamazepine and fenofibrate (solubility of 150ppm and 10ppm, respectively), has been investigated using a series of Pluronics® (Poloxamers) containing different ethylene oxide and propylene oxide (EO/PO) units in the molecule. The results show largely enhanced solubilization of fenofibrate by Pluronic® micelles that increases with the PPO chain length provided the temperature is above the critical micelle temperature (cmt). In contrast the more water-soluble carbamazepine only shows a moderate increase in solubilization upon addition of Pluronics®. Small angle neutron scattering (SANS) and pulsed field gradient (PFG) NMR experiments show that the solubilization of fenofibrate occurs in the core of the micelles, whereas carbamazepine shows no direct association with the micelles. These clearly different solubilization mechanisms for the two AIs were confirmed by Nuclear Overhauser Enhancement Spectroscopy (NOESY) experiments, which show that fenofibrate interacts only with the PPO core of the micelle, whereas carbamazepine interacts with both PPO and PEO similarly. Accordingly, the large enhancement of the solubilization of fenofibrate is related to the fact that it is solubilized within the PPO core of the Pluronic® micelles, while the much more moderate increase of carbamazepine solubility is attributed to the change of solvent quality due to the presence of the amphiphilic copolymer and the interaction with the EO and PO units in solution. PMID:27244594

  16. Soil sorption and leaching of active ingredients of Lumax® under mineral or organic fertilization.

    Science.gov (United States)

    Pinna, Maria Vittoria; Roggero, Pier Paolo; Seddaiu, Giovanna; Pusino, Alba

    2014-09-01

    The study describes the soil sorption of the herbicide Lumax®, composed of S-metolachlor (MTC), terbuthylazine (TBZ), and mesotrione (MST), as influenced by mineral and organic fertilizers. The investigation was performed on a sandy soil of an agricultural area designated as a Nitrate Vulnerable Zone, where mineral and organic fertilizers were applied for many years. Two organic fertilizers, cattle manure and slurry, respectively, and a mineral fertilizer with a nitrification inhibitor, Entec®, were compared. According to the experiments, performed with a batch method, the sorption conformed to Freundlich model. The extent of sorption of Lumax® ingredients was closely related to their octanol-water partition coefficient Kow. The respective desorption was hysteretic. Leaching trials were carried out by using water or solutions of DOM or Entec® as the eluants. Only the elution with the mineral fertilizer promoted the leaching of Lumax® active ingredients.

  17. Oxidation of pharmaceutically active compounds by a ligninolytic fungal peroxidase.

    Science.gov (United States)

    Eibes, Gemma; Debernardi, Gianfranco; Feijoo, Gumersindo; Moreira, M Teresa; Lema, Juan M

    2011-06-01

    Pharmaceuticals are an important group of emerging pollutants with increasing interest due to their rising consumption and the evidence for ecotoxicological effects associated to trace amounts in aquatic environments. In this paper, we assessed the potential degradation of a series of pharmaceuticals: antibiotics (sulfamethoxazole), antidepressives (citalopram hydrobromide and fluoxetine hydrochloride), antiepileptics (carbamazepine), anti-inflammatory drugs (diclofenac and naproxen) and estrogen hormones (estrone, 17β-estradiol, 17α-ethinylestradiol) by means of a versatile peroxidase (VP) from the ligninolytic fungus Bjerkandera adusta. The effects of the reaction conditions: VP activity, organic acid concentration and H(2)O(2) addition rate, on the kinetics of the VP based oxidation system were evaluated. Diclofenac and estrogens were completely degraded after only 5-25 min even with a very low VP activity (10 U l(-1)). High degradation percentages (80%) were achieved for sulfamethoxazole and naproxen. Low or undetectable removal yields were observed for citalopram (up to 18%), fluoxetine (lower than 10%) and carbamazepine (not degraded). PMID:20972884

  18. Testing of the structure of macromolecular polymer films containing solid active pharmaceutical ingredient (API) particles

    Energy Technology Data Exchange (ETDEWEB)

    Boelcskei, E. [Department of Pharmaceutical Technology, University of Szeged, H-6720 Szeged, Eoetvoes u. 6 (Hungary); Suevegh, K. [Laboratory of Nuclear Chemistry, Eoetvoes Lorand University, H-1518 Budapest 112, P.O. Box 32 (Hungary); Marek, T. [Hungarian Academy of Sciences, Research Group for Nuclear Techniques in Structural Chemistry, Eoetvoes Lorand University, H-1518 Budapest 112, P.O. Box 32 (Hungary); Regdon, G. [Department of Pharmaceutical Technology, University of Szeged, H-6720 Szeged, Eoetvoes u. 6 (Hungary); Pintye-Hodi, K., E-mail: klara.hodi@pharm.u-szeged.h [Department of Pharmaceutical Technology, University of Szeged, H-6720 Szeged, Eoetvoes u. 6 (Hungary)

    2011-07-15

    The aim of the present study was to investigate the structure of free films of Eudragit{sup L} 30D-55 containing different concentrations (0%, 1% or 5%) of diclofenac sodium by positron annihilation spectroscopy. The data revealed that the size of the free-volume holes and the lifetimes of ortho-positronium atoms decreased with increase of the API concentration. Films containing 5% of the API exhibited a different behavior during storage (17 {sup o}C, 65% relative humidity (RH)) in consequence of the uptake of water from the air. -- Highlights: {yields} The aim of the present study was to investigate the structure of free films of Eudragit{sup L} 30D-55 containing different concentrations (0%, 1% or 5%) of diclofenac sodium by positron annihilation spectroscopy. {yields} The data revealed that the size of the free-volume holes and the lifetimes of ortho-positronium atoms decreased with increase of the API concentration (). {yields} The API distorts the original polymer structure, but as time goes by, the metastable structure relaxes and it is almost totally restored after 3 weeks of storage (17 {sup o}C, 65% RH).

  19. Testing of the structure of macromolecular polymer films containing solid active pharmaceutical ingredient (API) particles

    Science.gov (United States)

    Bölcskei, É.; Süvegh, K.; Marek, T.; Regdon, G.; Pintye-Hódi, K.

    2011-07-01

    The aim of the present study was to investigate the structure of free films of Eudragit ® L 30D-55 containing different concentrations (0%, 1% or 5%) of diclofenac sodium by positron annihilation spectroscopy. The data revealed that the size of the free-volume holes and the lifetimes of ortho-positronium atoms decreased with increase of the API concentration. Films containing 5% of the API exhibited a different behavior during storage (17 °C, 65% relative humidity (RH)) in consequence of the uptake of water from the air.

  20. Incorporation of acetaminophen as an active pharmaceutical ingredient into porous lactose.

    Science.gov (United States)

    Ebrahimi, Amirali; Saffari, Morteza; Dehghani, Fariba; Langrish, Timothy

    2016-02-29

    A new formulation method for solid dosage forms with drug loadings from 0.65 ± 0.03% to 39 ± 1% (w/w) of acetaminophen (APAP) as a model drug has been presented. The proposed method involves the production of highly-porous lactose with a BET surface area of 20 ± 1 m(2)/g as an excipient using a templating method and the incorporation of drug into the porous structure by adsorption from a solution of the drug in ethanol. Drug deposition inside the carrier particles, rather than being physically distributed between them, eliminated the potential drug/carrier segregation, which resulted in excellent blend uniformities with relative standard deviations of less than 3.5% for all drug formulations. The results of DSC and XRD tests have shown deposition of nanocrystals of APAP inside the nanopores of lactose due the nanoconfinement phenomenon. FTIR spectroscopy has revealed no interaction between the adsorbed drug and the surface of lactose. The final loaded lactose particles had large BET surface areas and high porosities, which significantly increased the crushing strengths of the produced tablets. In vitro release studies in phosphate buffer (pH 5.8) have shown an acceptable delivery performance of 85% APAP release within 7 minutes for loaded powders filled in gelatin capsules. PMID:26768724

  1. WHO Prequalification of Active Pharmaceutical Ingredients%WHO原料药预认证项目

    Institute of Scientific and Technical Information of China (English)

    吕修梅

    2014-01-01

    目的 帮助国内原料药厂家了解并通过WHO预认证项目.方法 全面论述WHO原料药预认证项目的背景、申请流程、文件要求和意义.结果与结论 通过加深对WHO原料药预认证项目的认识,可以提高生产厂家参与WHO原料药预认证的积极性,增强通过预认证的信心.

  2. Active pharmaceutical ingredient (api) from an estuarine fungus, Microdochium nivale (Fr.)

    Digital Repository Service at National Institute of Oceanography (India)

    Bhosale, S.H.; Patil, K.B.; Parameswaran, P.S.; Jagtap, T.G.

    . Its antifungal inhibition and MIC (Minimum inhibitory concentration) against Aspergillus strains (A. niger, A. japonicus, A. fresenii), yeasts and dermatophytes (Candida sp., Cryptococcus neoformans, Trichophyton mentagrophytes, T. tonsurans, T...

  3. Crystallization kinetics and molecular mobility of an amorphous active pharmaceutical ingredient: A case study with Biclotymol.

    Science.gov (United States)

    Schammé, Benjamin; Couvrat, Nicolas; Malpeli, Pascal; Delbreilh, Laurent; Dupray, Valérie; Dargent, Éric; Coquerel, Gérard

    2015-07-25

    The present case study focuses on the crystallization kinetics and molecular mobility of an amorphous mouth and throat drug namely Biclotymol, through differential scanning calorimetry (DSC), temperature resolved X-ray powder diffraction (TR-XRPD) and hot stage microscopy (HSM). Kinetics of crystallization above the glass transition through isothermal and non-isothermal cold crystallization were considered. Avrami model was used for isothermal crystallization process. Non-isothermal cold crystallization was investigated through Augis and Bennett model. Differences between crystallization processes have been ascribed to a site-saturated nucleation mechanism of the metastable form, confirmed by optical microscopy images. Regarding molecular mobility, a feature of molecular dynamics in glass-forming liquids as thermodynamic fragility index m was determined through calorimetric measurements. It turned out to be around m=100, describing Biclotymol as a fragile glass-former for Angell's classification. Relatively long-term stability of amorphous Biclotymol above Tg was analyzed indirectly by calorimetric monitoring to evaluate thermodynamic parameters and crystallization behavior of glassy Biclotymol. Within eight months of storage above Tg (T=Tg+2°C), amorphous Biclotymol does not show a strong inclination to crystallize and forms a relatively stable glass. This case study, involving a multidisciplinary approach, points out the importance of continuing looking for stability predictors. PMID:26003417

  4. Classification of parasite eggs used as an active pharmaceutical ingredient (API)

    DEFF Research Database (Denmark)

    Bruun, J. M.; Carstensen, Jens Michael; Thamsborg, S.;

    2012-01-01

    The aim of the project is to describe the developmental stages of parasite eggs using digital image analysis of multispectral imagery. The primary focus is to identify and count eggs of different developmental stages and distinguish them from unrelated particles. This information is used to asses...

  5. Crystallization kinetics and molecular mobility of an amorphous active pharmaceutical ingredient: A case study with Biclotymol.

    Science.gov (United States)

    Schammé, Benjamin; Couvrat, Nicolas; Malpeli, Pascal; Delbreilh, Laurent; Dupray, Valérie; Dargent, Éric; Coquerel, Gérard

    2015-07-25

    The present case study focuses on the crystallization kinetics and molecular mobility of an amorphous mouth and throat drug namely Biclotymol, through differential scanning calorimetry (DSC), temperature resolved X-ray powder diffraction (TR-XRPD) and hot stage microscopy (HSM). Kinetics of crystallization above the glass transition through isothermal and non-isothermal cold crystallization were considered. Avrami model was used for isothermal crystallization process. Non-isothermal cold crystallization was investigated through Augis and Bennett model. Differences between crystallization processes have been ascribed to a site-saturated nucleation mechanism of the metastable form, confirmed by optical microscopy images. Regarding molecular mobility, a feature of molecular dynamics in glass-forming liquids as thermodynamic fragility index m was determined through calorimetric measurements. It turned out to be around m=100, describing Biclotymol as a fragile glass-former for Angell's classification. Relatively long-term stability of amorphous Biclotymol above Tg was analyzed indirectly by calorimetric monitoring to evaluate thermodynamic parameters and crystallization behavior of glassy Biclotymol. Within eight months of storage above Tg (T=Tg+2°C), amorphous Biclotymol does not show a strong inclination to crystallize and forms a relatively stable glass. This case study, involving a multidisciplinary approach, points out the importance of continuing looking for stability predictors.

  6. Demand Forecasting In Pharmaceutical Industry Using Neuro-Fuzzy Approach

    OpenAIRE

    Taskin, M.Fatih; Candan, Gökçe; Yazgan, Harun Reşit

    2014-01-01

    Because of human healthcare, the pharmaceutical industry can be considered as one of the most significant industrial sector. For this reason, demand forecasting in pharmaceutical industry has more complex structure than other sectors. Human factors, seasonal and epidemic diseases, market shares of the competitive products and marketing conditions are considered as main external factors for forecasting pharmaceutical product. Additionally, active ingredients rate is also important factor for f...

  7. ANALYSIS OF PHARMACEUTICAL COMPANIES’ ACTIVITIES THAT ARE DIRECTED TO PHYSICIANS IN EGYPT

    Directory of Open Access Journals (Sweden)

    M. M. Bahlol

    2016-01-01

    Full Text Available Purpose. Pharmaceutical market is one of the largest world markets with its own conditions. In Middle East, Egypt is a major pharmaceutical emerging market and has geographical, historical and political effective leading role among Arab countries. This research aims to investigate pharmaceutical companies’ activities in Egypt directed to physicians.Methodology. Urveying through simple random probability sampling is the approach appropriate for broad and representative overview of situation in research. Therefore, a survey of 1068 physicians was conducted through interviews and establishing structured data collection questionnaire.Originality. This is the first empirical paper to investigate pharmaceutical companies’ activities directed to physicians in pharmaceutical market of Egypt. These activities include identifying pharmaceutical companies through visits of medical representatives, analysis of those visits, frequency of medical representatives’ visits, characteristics of information introduced by medical representatives to physicians, physicians’ trust in provided information, spending of pharmaceutical companies on physicians, promotional techniques applied by medical representatives. These findings are useful for managers in pharmaceutical industry. They can be also useful in other industries such as medical equipment.Findings. Pharmaceutical companies are employing medical representatives widely, as the most effective and widely-applied promotion tool in Egypt.Practical Implications. Coordinate marketing management vision with pharmaceutical market real context will lead to synergism effect in utilizing medical representatives’ activities.

  8. Determination of active ingredients of Rhododendron dauricum L. by capillary electrophoresis with electrochemical detection.

    Science.gov (United States)

    Cao, Yuhua; Lou, Changgang; Fang, Yuzhi; Ye, Jiannong

    2002-01-11

    High-performance capillary electrophoresis with electrochemical detection was employed to analyse active ingredients of Rhododendron dauricum L., an important crude herb frequently used in Chinese medicines. Farrerol, quercetin, syringic acid, vanillic acid, 4-hydroxybenzoic acid, protocatechuic acid are major important active ingredients. Operated in a wall-jet configuration, a 300-microm diameter carbon-disk electrode was used as the working electrode, which exhibits a good response at +950 mV (vs. saturated calomel electrodes) for six analytes. Under the optimum conditions, the analytes were baseline separated within 16 min in a borax buffer (pH 8.7). Notably, excellent linearity was obtained over two orders of magnitude with detection limits (S/N=3) ranged from 9 x 10(-7) to 3.0 x 10(-6) M for all analytes. This method was successfully used in the analysis of Rhododendron dauricum L. with relatively simple extraction procedures, and the assay results were satisfactory. PMID:11820277

  9. INFLUENCE OF A WAY OF CRUSHING ON ACTIVITY OF INGREDIENTS OF CONCRETE MIX

    Directory of Open Access Journals (Sweden)

    Burenina O. N.

    2015-09-01

    Full Text Available The article presents the results of the researches of the influence of a way of crushing on activity of ingredients of concrete mix. It is shown that sand crushing by method of free kick in a planetary mill of AGO-2 allows not only to raise its specific surface, to receive the demanded particle size distribution, but also to improve quality of a surface of particles by removal, destruction of superficial inactive films. On a new surface of sand excess energy concentrates, the active centers are formed and there is a fixing of germs of new growths of products of hydration of cement in a place of an exit of dislocations to surfaces of crystals of sand that leads to substantial increase of chemical activity and reactionary ability of sand

  10. INFLUENCE OF SELECTED PHARMACEUTICALS ON ACTIVATED SLUDGE DEHYDROGENASE ACTIVITY

    Directory of Open Access Journals (Sweden)

    Agnieszka Tomska

    2016-06-01

    The aim of this work was to evaluate the effect of selected antibiotics - sulfanilamide and erythromycin on activated sludge dehydrogenase activity with use of trifenyltetrazolinum chloride (TTC test. Dehydrogenases activity is an indicator of biochemical activity of microorganisms present in activated sludge or the ability to degrade organic compounds in waste water. TTC test is particularly useful for the regularity of the course of treatment, in which the presence of inhibitors of biochemical reactions and toxic compounds are present. It was observed that the dehydrogenase activity decreases with the increase of a antibiotics concentration. The lowest value of the dehydrogenase activity equal to 32.4 μmol TF / gMLSS obtained at sulfanilamide concentration 150mg / l. For this sample, an inhibition of dehydrogenase activity was 31%.

  11. Comparative analysis of ciprofloxacin in different pharmaceutical products by high performance liquid chromatograph

    International Nuclear Information System (INIS)

    Pharmaceutical products with different trade names having ciprofloxacin as an active ingredient were collected from the market. The products were assayed under similar conditions for active ingredient applying HPLC technique. Results obtained from quantification of ciprofloxacin contents of each product were compared with their label claims. Comparative analysis of these products was performed based on the quantity of ciprofloxacin. (author)

  12. Activity and stability studies of verbascoside, a novel antioxidant, in dermo-cosmetic and pharmaceutical topical formulations.

    Science.gov (United States)

    Vertuani, Silvia; Beghelli, Erika; Scalambra, Emanuela; Malisardi, Gemma; Copetti, Stefano; Dal Toso, Roberto; Baldisserotto, Anna; Manfredini, Stefano

    2011-08-18

    We here report the results of our investigations carried out on verbascoside, a phenylpropanoid glycoside known for its antioxidant, anti-inflammatory and photoprotective actions. Verbascoside was obtained from Buddleia davidii meristematic cells, obtained in turn using a sustainable biotechnology platform which employs an in vitro plant cell culture technology. Verbascoside was first investigated to assess the behaviour of the active ingredient in solution or in finished preparations, in view of its potential topical use, especially in skin protection. Stability studies were performed by HPLC, and a PCL assay was adopted to determine the radical scavenging activity toward superoxide anion. The high hydrophilic character of verbascoside, suggested in a somewhat limited range of possible applications, leading us to explore its derivatization to obtain the semi-synthetic derivative VPP, an acyl derivative of verbascoside, with an improved range of applications due to its lower hydrophilic profile. Alone, VPP revealed increased antioxidant activity, both as an active ingredient and in dermocosmetic preparations. Stability studies showed a greater stability of VPP in lipophilic vehicles, whereas the parent verbascoside proved more stable in an O/W emulsions. Verbascoside was also stable in suppositories, an interesting pharmaceutical form for possible applications in treatment of inflammation of the intestinal mucosa.

  13. Methodological Establishment of HPLC-DAD for Determination of 10 Active Ingredients in Wuweizi

    Directory of Open Access Journals (Sweden)

    Feng YAO

    2015-09-01

    Full Text Available Objective: To establish high performance liquid chromatography-diode array detection (HPLC-DAD method for the determination of active ingredients of multiple lignans in Nanwuweizi (Kadsura longepedunculata and Beiwuweizi (Fructus Schisandrae Chinensis so as to set up the standard for the quality control of Wuweizi (Schisandra chinensis. Methods: Brava BDS C18 column (250 mm×4.6 mm, 5 μm was applied, with detection condition as follows: column temperature: 30℃; mobile phase: water (A-acetonitrile (B; gradient elution: 0.8 mL/min and detection wavelength: 225 nm.Results: Ten ingredients in Beiwuweizi and 5 in Nanwuweizi were completely separately within 75 min. Peak area was in favorable linear relationship with concentration. In addition, the recovery rate was 96.87-103.29% and relative standard deviation (RSD was 0.68-2.09%.Conclusion: HPLC-DAD is simple and reliable with favorable repeatability, so it can be used for the determination of multiple lignans in Wuweizi.

  14. Methodological Establishment of HPLC-DAD for Determination of 10 Active Ingredients in Wuweizi

    Institute of Scientific and Technical Information of China (English)

    YAO Feng; CHEN Da-shuai

    2015-01-01

    Objective: To establish high performance liquid chromatography-diode array detection (HPLC-DAD) method for the determination of active ingredients of multiple lignans in Nanwuweizi (Kadsura longepedunculata) and Beiwuweizi (Fructus Schisandrae Chinensis) so as to set up the standard for the quality control of Wuweizi (Schisandra chinensis). Methods: Brava BDS C18 column (250 mm×4.6 mm, 5 μm) was applied, with detection condition as follows: column temperature: 30℃; mobile phase: water (A)-acetonitrile (B); gradient elution: 0.8 mL/min and detection wavelength: 225 nm. Results: Ten ingredients in Beiwuweizi and 5 in Nanwuweizi were completely separately within 75 min. Peak area was in favorable linear relationship with concentration. In addition, the recovery rate was 96.87%-103.29% and relative standard deviation (RSD) was 0.68%-2.09%. Conclusion: HPLC-DAD is simple and reliable with favorable repeatability, so it can be used for the determination of multiple lignans in Wuweizi.

  15. Synthesis, structure, antitumor activity of novel pharmaceutical co-crystals based on bispyridyl-substituted α, β-unsaturated ketones with gallic acid

    Science.gov (United States)

    Liu, Lian-Dong; Liu, Shu-Lian; Liu, Zhi-Xian; Hou, Gui-Ge

    2016-05-01

    Three novel pharmaceutical co-crystals, (A)·(gallic acid) (1), (B)·(gallic acid) (2), and (C)·(gallic acid) (3) were generated based on 2,6-bis((pyridin-4-yl)methylene)cyclohexanone (A), N-methyl-3,5-bis((pyridin-3-yl)methylene)-4-piperidone (B), N-methyl-3,5-bis((pyridin-4-yl)methylene)-4-piperidone (C) with gallic acid, respectively. They are characterized by elemental analysis, FTIR spectroscopy, 1H NMR and single-crystal X-ray diffraction. Structural analysis reveals that two pharmaceutical ingredients link each other into H-bonding-driven 3D network in 1, 2, or 2D plane in 3. In addition, their antitumor activities against human neoplastic cell lines A549, SGC-7901, MCF-7, OVCA-433, HePG2 and cytotoxicity for HUVEC cell lines by CCK-8 method were evaluated primarily. Compared with gallic acid and free A, B and C, their antitumor activities have improved distinctly, while cytotoxicities have reduced markedly, especially for co-crystal 1. This is mainly because of the synergistic effect between pharmaceutical ingredients A, B, and C and gallic acid.

  16. How active ingredient localisation in plant tissues determines the targeted pest spectrum of different chemistries

    DEFF Research Database (Denmark)

    Buchholz, Anke; Trapp, Stefan

    2016-01-01

    BACKGROUND: The efficacies of four commercial insecticides and of two research compounds were tested against aphids (Aphis craccivora and Myzus persicae), whiteflies (Bemisia tabaci) and red-spotted spider mites (Tetranychus urticae) in intrinsic (oral administration), curative (direct contact...... information sets revealed that the intracellular localisation of active ingredients determines the performance of test compounds against different target pests because of different feeding behaviours: mites feed on mesophyll, and aphids and whiteflies mostly in the vascular system. Polar compounds have a slow...... adsorption into leaf cells and thus a favourable distribution into apoplast and xylem sap. Slightly lipophilic bases get trapped in vacuoles, which is a less suited place to control hemipteran pests but appropriate to control mites. Non-favourable cellular localisation led to a strong reduction...

  17. 77 FR 15764 - Agency Information Collection Activities; Submission for Office of Management and Budget Review...

    Science.gov (United States)

    2012-03-16

    ... process if it can be shown that the active pharmaceutical ingredient(s) (API) is the same as the pioneer... applications over the past 10 years. In the Federal Register of October 24, 2011 (76 FR 65733), FDA published...

  18. Inter- and Intra-Manufacturer Variability in Pharmaceutical Grades and Lots of Xanthan Gum

    OpenAIRE

    Thacker, Ankur; Fu, Shao; Boni, Riccardo L.; Block, Lawrence H.

    2010-01-01

    A pharmaceutical formulation typically contains one or more excipients in addition to the active pharmaceutical ingredient(s). Though excipients have been considered inert components of a formulation, variability in their properties has been shown to affect the performance of drug dosage forms and delivery systems. This study investigates the inter- and intra-manufacturer variability among different NF grades and lots of xanthan gum made by two manufacturers. As many formulators rely on compe...

  19. Evaluation of teratogenic effects of crocin and safranal, active ingredients of saffron, in mice.

    Science.gov (United States)

    Moallem, Seyed Adel; Afshar, Mohammad; Etemad, Leila; Razavi, Bibi Marjan; Hosseinzadeh, Hossein

    2016-02-01

    Saffron (Crocus sativus) is a widely used food additive for its color and taste. Crocin and safranal are two main components of this plant. Numerous studies are underway to introduce saffron and its active ingredients as pharmacological agents. Safety assessments of these compounds are important parts of this endeavor. In this study, the effects of crocin and safranal administrations during embryogenesis have been investigated in mice. A total of 75 BALB/c pregnant mice were divided into six experimental and control groups. Four experimental groups received intraperitoneal injection of crocin (200 mg/kg or 600 mg/kg) daily or safranal (0.075 ml/kg or 0.225 ml/kg) on gestational days (GDs) 6 to 15. Control groups received normal saline or paraffin as solvents of crocin and safranal. Dams were dissected on GD18 and embryos were collected. Routine maternal and fetal parameters were recorded. Macroscopic observation of external malformations was also performed. Fetuses were then selected for double skeletal staining with alizarin red and alcian blue. All experimental groups caused significant decrease in length and weight of fetuses when compared with the control groups and revealed malformations such as minor skeletal malformations, mandible and calvaria malformations, and growth retardation. Minor skeletal malformations were the most commonly observed abnormality, which were statistically significant when compared with the control groups (p < 0.05). The severities of malformations were comparable in the crocin- and safranal-treated groups. This study suggests that crocin or safranal can induce embryonic malformations when administered in pregnant mice. Due to the wide use of saffron, further elaborate studies to understand the malformation mechanisms of these ingredients are recommended. PMID:24097366

  20. Acetylcholinesterase inhibitory activity of Thai traditional nootropic remedy and its herbal ingredients.

    Science.gov (United States)

    Tappayuthpijarn, Pimolvan; Itharat, Arunporn; Makchuchit, Sunita

    2011-12-01

    The incidence of Alzheimer disease (AD) is increasing every year in accordance with the increasing of elderly population and could pose significant health problems in the future. The use of medicinal plants as an alternative prevention or even for a possible treatment of the AD is, therefore, becoming an interesting research issue. Acetylcholinesterase (AChE) inhibitors are well-known drugs commonly used in the treatment of AD. The aim of the present study was to screen for AChE inhibitory activity of the Thai traditional nootropic recipe and its herbal ingredients. The results showed that ethanolic extracts of four out of twenty-five herbs i.e. Stephania pierrei Diels. Kaempfera parviflora Wall. ex Baker, Stephania venosa (Blume) Spreng, Piper nigrum L at 0.1 mg/mL showed % AChE inhibition of 89, 64, 59, 50; the IC50 were 6, 21, 29, 30 microg/mL respectively. The other herbs as well as combination of the whole recipe had no synergistic inhibitory effect on AChE activity. However some plants revealed antioxidant activity. More research should have be performed on this local wisdom remedy to verify the uses in scientific term. PMID:22619927

  1. Dampened neural activity and abolition of epileptic-like activity in cortical slices by active ingredients of spices.

    Science.gov (United States)

    Pezzoli, Maurizio; Elhamdani, Abdeladim; Camacho, Susana; Meystre, Julie; González, Stephanie Michlig; le Coutre, Johannes; Markram, Henry

    2014-10-31

    Active ingredients of spices (AIS) modulate neural response in the peripheral nervous system, mainly through interaction with TRP channel/receptors. The present study explores how different AIS modulate neural response in layer 5 pyramidal neurons of S1 neocortex. The AIS tested are agonists of TRPV1/3, TRPM8 or TRPA1. Our results demonstrate that capsaicin, eugenol, menthol, icilin and cinnamaldehyde, but not AITC dampen the generation of APs in a voltage- and time-dependent manner. This effect was further tested for the TRPM8 ligands in the presence of a TRPM8 blocker (BCTC) and on TRPM8 KO mice. The observable effect was still present. Finally, the influence of the selected AIS was tested on in vitro gabazine-induced seizures. Results coincide with the above observations: except for cinnamaldehyde, the same AIS were able to reduce the number, duration of the AP bursts and increase the concentration of gabazine needed to elicit them. In conclusion, our data suggests that some of these AIS can modulate glutamatergic neurons in the brain through a TRP-independent pathway, regardless of whether the neurons are stimulated intracellularly or by hyperactive microcircuitry.

  2. Effects of ginsenosides, the active ingredients of Panax ginseng, on development, growth, and life span of Caenorhabditis elegans

    Science.gov (United States)

    Ginsenosides, the active ingredients of Panax ginseng, are saponins derived from sterols. The free-living nematode Caenorhabditis elegans is a well-established model for biochemical and genetic studies in animals. Although cholesterol is an essential requirement for the growth and development of C. ...

  3. Collaborative Care for Patients With Severe Personality Disorders: Preliminary Results and Active Ingredients From a Pilot Study (Part I)

    NARCIS (Netherlands)

    Stringer, Barbara; Meijel, Berno van; Karman, Pieter; Koekkoek, Bauke; Hoogendoorn, Adriaan; Kerkhof, Ad; Beekman, Aartjan

    2014-01-01

    PURPOSE: To test if a collaborative care program (CCP) with nurses in a coordinating position is beneficial for patients with severe personality disorders. DESIGN AND METHODS: A pilot study with a comparative multiple case study design using mixed methods investigating active ingredients and prelimi

  4. Effects of rhubarb and the active ingredients of rhubarb on the cytoplasmic free calcium in INTMNC of rabbits

    Institute of Scientific and Technical Information of China (English)

    Xiu Zhen Lin; De Lu Ma; Zhi Qing Cui; Yi Kang

    2000-01-01

    @@INTRODUCTION The recent studies have shown that rhubarb has not only the effect of removing stasis by purgation, but also intestinal barrier effects[1,2]. In order to further clarify the intestinal barrier mechanism of rhubarb, we studied the effects of rhubarb decoction and the active ingredients of rhubarb on the cytoplasmic free calcium in isolated intestinal mononuclear cells (INT-MNC)

  5. The protective effect of the earthworm active ingredients on hepatocellular injury induced by endoplasmic reticulum stress.

    Science.gov (United States)

    Wang, Qi; Duan, Leng-Xin; Xu, Zheng-Shun; Wang, Jian-Gang; Xi, Shou-Min

    2016-08-01

    The earthworm is a widely used Chinese herbal medicine. There are more than 40 prescriptions including earthworms in the "Compendium of Materia Medica". TCM theory holds that earthworms exert antispasmodic and antipyretic effects through the liver meridian to calm the liver. However, the clinical effect of earthworms on liver injury has not been clearly demonstrated. We have previously established a method to extract the active ingredients from earthworms (hereinafter referred to as EWAs) [1]. In the present study, we observed protective effect of the EWAs on tunicamycin-induced ERS (endoplasmic reticulum stress) model in human hepatic L02 cells. The results showed that the EWAs promote proliferation and reduced apoptosis of ERS model in L02 cells (P<0.01). The up-regulation of ERS-related proteins, including PERK (protein kinase RNA-like endoplasmic reticulum kinase), eIF2a (eukaryotic translation initiation factor 2a), ATF4 (activating transcription factor 4) and CHOP (CCAAT/enhancer binding protein homologous protein), in L02 cell under ERS was inhibited by treatment of the EWAs (P<0.01). In summary, our data suggest the EWAs can significant attenuate ERS-induced hepatocyte injury via PERK-eIF2a-ATF4 pathway. PMID:27470367

  6. Quantifying Amphibian Pesticide Body Burdens for Active Ingredients Versus Formulations Through Dermal Exposure

    Science.gov (United States)

    Widespread pesticide applications throughout agricultural landscapes pose a risk to post-metamorphic amphibians leaving or moving between breeding ponds in terrestrial habitats. Recent studies indicate that the inactive ingredients in pesticide formulations may be equally or more...

  7. MICROSPONGE DELIVERY SYSTEM (MDS: A UNIQUE TECHNOLOGY FOR DELIVERY OF ACTIVE INGREDIENTS

    Directory of Open Access Journals (Sweden)

    Saurabh Kumar et al.

    2011-12-01

    Full Text Available In pharmaceutical industry, various controlled released dosage forms like solid formulation, semi solid formulation and topical preparation have more importance due to efficacy and patient compliance. Topical preparations have some disadvantages like unpleasant odour, greasiness and skin irritation and fail to reach the systemic circulation in sufficient amounts in few cases. This problem is overcome by microsponge delivery system. Microsponges are tiny sponge like spherical and highly porous micro-sized particles with a unique ability for entrapping actives. They offers programmable release active drug into the skin in order to reduce systemic exposure and minimize local cutaneous reactions to active. These MDS’s are closely related to microspheres, and used in the sun screens, creams, ointments, over- the-counter (OTC skin care preparations, recently used in oral drug as well as biopharmaceuticals (peptides, proteins and DNA-based therapeutics drug delivery. The present review introduces microsponge technology along with its synthesis, characterization, programmable parameters and release mechanism of MDS.

  8. Biodegradation of pharmaceuticals in hospital wastewater by a hybrid biofilm and activated sludge system (Hybas)

    DEFF Research Database (Denmark)

    Escola Casas, Monica; Chhetri, Ravi Kumar; Ooi, Gordon Tze Hoong;

    2015-01-01

    of one activated sludge reactor, two HybasTM reactors and one moving bed biofilm reactor (MBBR) has been operated for 10 months, where after batch and continuous flow tests were performed for the degradation of pharmaceuticals. Removal of organic matter and nitrification mainly occurred in the first...... reactor. Most pharmaceuticals were removed significantly. The removal of pharmaceuticals (including x-ray contrast media, ß-blockers, analgesics and antibiotics) were fitted to a single first-order kinetics degradation function, giving degradation rate constants from 0 to 1.49 h-1, from 0 to 7.78×10-1 h-1...... amount, the last reactor (biofilm only) appeared to have the most effective biomass in respect of removing pharmaceuticals. In the batch experiment, out of 26 compounds, 16 were assessed to degrade more than 20% of the respective pharmaceutical within the Hybas train. In the continuous flow experiment...

  9. Chitosonic® Acid as a Novel Cosmetic Ingredient: Evaluation of its Antimicrobial, Antioxidant and Hydration Activities

    Directory of Open Access Journals (Sweden)

    Yi-Shyan Chen

    2013-03-01

    Full Text Available Chitosonic® Acid, carboxymethyl hexanoyl chitosan, is a novel chitosan material that has recently been accepted by the Personal Care Products Council as a new cosmetic ingredient with the INCI (International Nomenclature of Cosmetic Ingredients name Carboxymethyl Caprooyl Chitosan. In this study, we analyze several important cosmetic characteristics of Chitosonic® Acid. Our results demonstrate that Chitosonic® Acid is a water-soluble chitosan derivative with a high HLB value. Chitosonic® Acid can form a nano-network structure when its concentration is higher than 0.5% and can self-assemble into a nanosphere structure when its concentration is lower than 0.2%. Chitosonic® Acid has potent antimicrobial activities against gram-positive bacteria, gram-negative bacteria and fungus. Chitosonic® Acid also has moderate DPPH radical scavenging activity. Additionally, Chitosonic® Acid exhibits good hydration activity for absorbing and retaining water molecules with its hydrophilic groups. From a safety point of view, Chitosonic® Acid has no cytotoxicity to L-929 cells if its concentration is less than 0.5%. Moreover, Chitosonic® Acid has good compatibilities with various normal cosmetic ingredients. Therefore, we propose that Chitosonic® Acid has the potential to be a widely used ingredient in various types of cosmetic products.

  10. Determination of sorption of seventy five pharmaceuticals in sewage sludge

    DEFF Research Database (Denmark)

    Hörsing, Maritha; Ledin, Anna; Grabic, Roman;

    2011-01-01

    Sorption of 75 active pharmaceutical ingredients (APIs) to three different types of sludge (primary sludge, secondary sludge with short and long sludge age respectively) were investigated. To obtain the sorption isotherms batch studies with the APIs mixture were performed in four nominal concentr......Sorption of 75 active pharmaceutical ingredients (APIs) to three different types of sludge (primary sludge, secondary sludge with short and long sludge age respectively) were investigated. To obtain the sorption isotherms batch studies with the APIs mixture were performed in four nominal...

  11. Determination of Four Active Ingredients in Vc Yinqiao Tablets by Capillary Zone Electrophoresis with Amperometric Detection

    Institute of Scientific and Technical Information of China (English)

    L(U),Jin; WANG,Qing-Jiang; CHENG,Xi; LIU,Hai-Yan; HE,Pin-Gang; FANG,Yu-Zhi

    2006-01-01

    A simple, reliable and reproducible method, based on capillary zone electrophoresis with amperometric detection (CZE-AD), has been developed for simultaneous determination of four active ingredients in Vc Yinqiao tablets including paracetamol, vitamin C, caffeic acid and chlorogenic acid. A carbon-disk electrode was used as working electrode and 0.95 V (versus SCE) was selected as detection potential. The optimal conditions of CZE experiment were 30 mmol·L-1 borate solution (pH 9.5) as running buffer, 14 kV as separation voltage and 8 s (14 kV) as electro-kinetic sampling time. Under the selected optimum conditions, paracetamol, vitamin C, caffeic acid and chlorogenic acid could be perfectly separated within 22 min, and their detection limits (S/N=3) ranged from 5 × 10-7 to 1×10-6 mol·L-1. This proposed method demonstrated good reproducibility with relative standard deviations of less than 3% for both migration time and peak current (n=7). The utility of this method was demonstrated by monitoring a kind of compound medicine named Vc Yinqiao tablets and the assay results were satisfactory.

  12. Pharmacokinetics of hederacoside C, an active ingredient in AG NPP709, in rats.

    Science.gov (United States)

    Kim, Ju Myung; Yoon, Ji Na; Jung, Ji Won; Choi, Hye Duck; Shin, Young June; Han, Chang Kyun; Lee, Hye Suk; Kang, Hee Eun

    2013-11-01

    1. Hederacoside C (HDC) is one of the active ingredients in Hedera helix leaf extract (Ivy Ex.) and AG NPP709, a new botanical drug to treat acute respiratory infection and chronic inflammatory bronchitis. However, information regarding its pharmacokinetic properties remains limited. 2. Here, we report the pharmacokinetics of HDC in rats after intravenous administration of HDC (3, 12.5, and 25 mg/kg) and after oral administration of HDC, Ivy Ex., and AG NPP709 (equivalent to 12.5, 25, and 50 mg/kg HDC). 3. Linear pharmacokinetics of HDC were identified upon its intravenous administration at doses of 3-25 mg/kg. Intravenous administration of HDC results in relatively slow clearance (1.46-2.08 mL/min/kg) and a small volume of distribution at steady state (138-222 mL/kg), while oral administration results in a low absolute oral bioavailability (F) of 0.118-0.250%. The extremely low F of HDC may be due to poor absorption of HDC from the gastrointestinal (GI) tract and/or its decomposition therein. 4. The oral pharmacokinetics of HDC did not differ significantly among pure HDC, Ivy Ex., and AG NPP709. PMID:23607546

  13. Study of Active Ingredients in Black Soybean Sprouts and Their Safety in Cosmetic Use

    Directory of Open Access Journals (Sweden)

    Yinmao Dong

    2012-10-01

    Full Text Available Active ingredients in different lengths of black soybean sprouts were extracted with water. Concentrations of the main proteins and polysaccharides were determined by the Forint phenol assay and phenol-sulfuric acid assay, respectively. Anti-oxidizing capacities of the extracts were measured in vitro using the DPPH scavenging test and whitening capacity was measured in vitro using the tyrosinase inhibition test. The effects of the bean sprout extracts on human skin fibroblasts damnified by H2O2 were studied using an MTT colorimetric assay. The safety of the extracts was determined using the red blood cell (RBC test, chick chorioallantoic membrane (CAM assay and human patch test. Results show that DPPH radical scavenging rates at different shoot lengths were all greater than 95%, while the tyrosinase inhibition capacity of the extracts reached 98%. Hemolysis rate in all extracts were lower than 10%, below the 20% regulatory limit for the RBC test. No signs of allergic reactions were observed in the human patch tests. The optimum extract was obtained from bean sprouts grown to 0.5 cm. Extracts of black bean sprouts are safe and can be used as additives in anti-aging and whitening cosmetic products.

  14. Inactive ingredient Search for Approved Drug Products

    Data.gov (United States)

    U.S. Department of Health & Human Services — According to 21 CFR 210.3(b)(8), an inactive ingredient is any component of a drug product other than the active ingredient. Only inactive ingredients in the final...

  15. Identification of aroma active compounds of cereal coffee brew and its roasted ingredients.

    Science.gov (United States)

    Majcher, Małgorzata A; Klensporf-Pawlik, Dorota; Dziadas, Mariusz; Jeleń, Henryk H

    2013-03-20

    Cereal coffee is a coffee substitute made mainly from roasted cereals such as barley and rye (60-70%), chicory (15-20%), and sugar beets (6-10%). It is perceived by consumers as a healthy, caffeine free, non-irritating beverage suitable for those who cannot drink regular coffee made from coffee beans. In presented studies, typical Polish cereal coffee brew has been subjected to the key odorants analysis with the application of gas chromatography-olfactometry (GC-O) and aroma extract dilution analysis (AEDA). In the analyzed cereal coffee extract, 30 aroma-active volatiles have been identified with FD factors ranging from 16 to 4096. This approach was also used for characterization of key odorants in ingredients used for the cereal coffee production. Comparing the main odors detected in GC-O analysis of roasted cereals brew to the odor notes of cereal coffee brew, it was evident that the aroma of cereal coffee brew is mainly influenced by roasted barley. Flavor compound identification and quantitation has been performed with application of comprehensive multidimentional gas chromatography and time-of-flight mass spectrometry (GCxGC-ToFMS). The results of the quantitative measurements followed by calculation of the odor activity values (OAV) revealed 17 aroma active compounds of the cereal coffee brew with OAV ranging from 12.5 and 2000. The most potent odorant was 2-furfurylthiol followed by the 3-mercapto-3-methylbutyl formate, 3-isobutyl-2-methoxypyrazine and 2-ethyl-3,5-dimethylpyrazine, 2-thenylthiol, 2,3-butanedione, 2-methoxy phenol and 2-methoxy-4-vinyl phenol, 3(sec-butyl)-2-methoxypyrazine, 2-acetyl-1-pyrroline, 3-(methylthio)-propanal, 2,3-pentanedione, 4-hydroxy-2,5-dimethyl-3-(2H)-furanone, (E,E)-2,4-decadienal, (Z)-4-heptenal, phenylacetaldehyde, and 1-octen-3-one. PMID:23414530

  16. Biodegradation of pharmaceuticals in hospital wastewater by a hybrid biofilm and activated sludge system (Hybas)

    DEFF Research Database (Denmark)

    Escola Casas, Monica; Chhetri, Ravi Kumar; Ooi, Gordon Tze Hoong;

    2015-01-01

    of one activated sludge reactor, two HybasTM reactors and one moving bed biofilm reactor (MBBR) has been operated for 10 months, where after batch and continuous flow tests were performed for the degradation of pharmaceuticals. Removal of organic matter and nitrification mainly occurred in the first...... amount, the last reactor (biofilm only) appeared to have the most effective biomass in respect of removing pharmaceuticals. In the batch experiment, out of 26 compounds, 16 were assessed to degrade more than 20% of the respective pharmaceutical within the Hybas train. In the continuous flow experiment......Hospital wastewater contributes a significant input of pharmaceuticals into municipal wastewater. The combination of suspended activated sludge and biofilm processes, as stand-alone or as hybrid process, has been suggested as a possible solution for hospital wastewater treatment. Hybas...

  17. The Contribution of Innovation Strategy Development and Implementation in Active Facilitation of Pharmaceutical Front End Innovation

    DEFF Research Database (Denmark)

    Aagaard, Annabeth

    2012-01-01

    ; Igartua, 2010) as a facilitator of innovation and may therefore also be targeted at FEI support. The pharmaceutical industry has experienced a worldwide decline in the number of applications for new molecular entities to regulatory agencies since 1997. Therefore high pressures are put on pharmaceutical...... research and FEI to produce more valid candidates and faster for drug development. This paper explores how pharmaceutical front end innovation can be actively supported through the development and implementation of an innovation strategy. The empirical field and applied methodology is an action......-oriented longitudinal case study of a Danish pharmaceutical company. The findings and key learnings from the study are presented as propositions of how innovation strategies can be applied to actively facilitate FEI and with measurable results....

  18. Acaricidal activity against Panonychus citri and active ingredient of the mangrove plant Cerbera manghas.

    Science.gov (United States)

    Deng, Yecheng; Yongmei Liao; Li, Jingjing; Yang, Linlin; Zhong, Hui; Zhou, Qiuyan; Qing, Zhen

    2014-09-01

    Cerbera manghas is a mangrove plant which possesses comprehensive biological activities. A great deal of research has been undertaken on the chemical constituents and medical functions of C. manghas; insecticidal and antifungal activities have also been reported, but the acaricidal activity has not been studied. In our study, the acaricidal activity and active substances of C. manghas were investigated using a spray method, which showed that the methanol extracts of the fruit, twigs and leaves exhibited contact activity against female adults of Panonychus citri, with LC50 values at 24 h of 3.39 g L(-1), 4.09 g L(-1) and 4.11 g L(-1), respectively. An acaricidal compound was isolated from C. manghas by an activity-guided isolation method, and identified as (-)-17β-neriifolin, which is a cardiac glycoside. (-)-17β-Neriifolin revealed high contact activity against female adults, nymphae, larvae and eggs of P. citri, with LC50 values at 24 h of 0.28 g L(-1), 0.29 g L(-1), 0.28 g L(-1) and 1.45 g L(-1), respectively. PMID:25918788

  19. Active ingredient-containing chitosan/polycaprolactone nonwoven mats: Characterizations and their functional assays

    Energy Technology Data Exchange (ETDEWEB)

    Bai, Meng-Yi, E-mail: mybai@mail.ntust.edu.tw [Graduate Institute of Biomedical Engineering, National Taiwan University of Science and Technology, Taipei 10607, Taiwan, ROC (China); Adjunct appointment to the Department of Biomedical Engineering, National Defense Medical Center, Taipei 114, Taiwan, ROC (China); Chou, Tz-Chong, E-mail: tcchou@ms5.hinet.net [Department of Biomedical Engineering, National Defense Medical Center, Taipei 114, Taiwan, ROC (China); Tsai, Jie-Chang; Yang, Hui-Ching [Graduate Institute of Biomedical Engineering, National Taiwan University of Science and Technology, Taipei 10607, Taiwan, ROC (China)

    2013-01-01

    This study demonstrates a facile method developed to generate a chitosan/polycaprolactone (CS/PCL) nonwoven mat. All nonwoven mats are composed of microfibers with an average diameter of 2.51 {+-} 0.69 {mu}m. The X-ray photoelectron spectroscopy data indicate that positively charged nitrogen was generated on the surface of the mats after undergoing CS coating. By using a non-contacting electrostatic voltmeter, we determined that the nonwoven mats exhibited a positive potential and the charge density of the CS/PCL nonwoven mat was in proportion to the thickness of the CS overlayer. Moreover, platelet aggregation and anti-bacterial ability were enhanced by the CS/PCL nonwoven mat as compared to that of PCL nonwoven mat alone. The enhancements of the CS/PCL nonwoven mat on platelet aggregation are further promoted by incorporating a 1 mM calcium ion in its CS overlayer. We also find that the addition of tea tree oil in the CS overlayer significantly inhibited LPS-induced nitrite formation in Raw 264.7 macrophages. In conclusion, our CS/PCL nonwoven mat possesses pharmacological effects including an increase of platelet aggregation, anti-bacterial, anti-adhesive, and anti-inflammatory activities. The performance of this CS/PCL nonwoven mat can be further promoted by incorporating active compounds to exert therapeutic effects in wound healing. Highlights: Black-Right-Pointing-Pointer We develop a facile method to generate active ingredient-containing CS/PCLNM. Black-Right-Pointing-Pointer Our CS/PCLNM possesses superior mechanical strength, compared to CS-blended PCL nanofibers. Black-Right-Pointing-Pointer We prove that our prepared CS/PCLNM possesses several pharmacological properties Black-Right-Pointing-Pointer The functional performances of CS/PCLNM are enhanced by incorporation of active compounds. Black-Right-Pointing-Pointer Incorporation of 1 mM of calcium ions or 100 {mu}L of TTO into the CS overlayer of CS/PCLNM is the optimum dose.

  20. Chitin-Hyaluronan Nanoparticles: A Multifunctional Carrier to Deliver Anti-Aging Active Ingredients through the Skin

    Directory of Open Access Journals (Sweden)

    Pierfrancesco Morganti

    2014-07-01

    Full Text Available The paper describes the process to produce Chitin Nanofibril-Hyaluronan nanoparticles (CN-HA, showing their ability to easily load active ingredients, facilitate penetration through the skin layers, and increase their effectiveness and safety as an anti-aging agent. Size and characterization of CN-HA nanoparticles were determined by Scanning Electron Microscopy (SEM and Zetasizer, while encapsulation efficiency and loading capacity of the entrapped ingredients were controlled by chromatographic and spectrophotometric methods. Safeness was evidenced on fibroblasts and keratinocytes culture viability by the MTT (Methylthiazol assay; anti-aging activity was evaluated in vitro measuring antioxidant capacity, anti-collagenase activity, and metalloproteinase and pro-inflammatory release; efficacy was shown in vivo by a double-blind vehicle-controlled study for 60 days on 60 women affected by photo-aging. In addition, the CN-HA nanoparticles have shown interesting possibility to be used as active ingredients, for designing and making advanced medication by the electrospinning technology, as well as to produce transparent films for food packaging, by the casting method, and can be used also in their dry form as tissues or films without adding preservatives. These unusual CN-HA nanoparticles obtained from the use of raw materials of waste origin may offer an unprecedented occasion for making innovative products, ameliorating the quality of life, reducing pollution and safeguarding the environment’s integrity.

  1. Biodegradation of pharmaceuticals in hospital wastewater by a hybrid biofilm and activated sludge system (Hybas).

    Science.gov (United States)

    Escolà Casas, Mònica; Chhetri, Ravi Kumar; Ooi, Gordon; Hansen, Kamilla M S; Litty, Klaus; Christensson, Magnus; Kragelund, Caroline; Andersen, Henrik R; Bester, Kai

    2015-10-15

    Hospital wastewater contributes a significant input of pharmaceuticals into municipal wastewater. The combination of suspended activated sludge and biofilm processes, as stand-alone or as hybrid process (hybrid biofilm and activated sludge system (Hybas™)) has been suggested as a possible solution for hospital wastewater treatment. To investigate the potential of such a hybrid system for the removal of pharmaceuticals in hospital wastewater a pilot plant consisting of a series of one activated sludge reactor, two Hybas™ reactors and one moving bed biofilm reactor (MBBR) has been established and adapted during 10 months of continuous operation. After this adaption phase batch and continuous experiments were performed for the determination of degradation of pharmaceuticals. Removal of organic matter and nitrification mainly occurred in the first reactor. Most pharmaceuticals were removed significantly. The removal of pharmaceuticals (including X-ray contrast media, β-blockers, analgesics and antibiotics) was fitted to a single first-order kinetics degradation function, giving degradation rate constants from 0 to 1.49 h(-1), from 0 to 7.78 × 10(-1)h(-1), from 0 to 7.86 × 10(-1)h(-1) and from 0 to 1.07 × 10(-1)h(-1) for first, second, third and fourth reactors respectively. Generally, the highest removal rate constants were found in the first and third reactors while the lowest were found in the second one. When the removal rate constants were normalized to biomass amount, the last reactor (biofilm only) appeared to have the most effective biomass in respect to removing pharmaceuticals. In the batch experiment, out of 26 compounds, 16 were assessed to degrade more than 20% of the respective pharmaceutical within the Hybas™ train. In the continuous flow experiments, the measured removals were similar to those estimated from the batch experiments, but the concentrations of a few pharmaceuticals appeared to increase during the first treatment step. Such increase

  2. 21 CFR 341.85 - Labeling of permitted combinations of active ingredients.

    Science.gov (United States)

    2010-04-01

    ... ingredients in part 356 of this chapter should be used. (5) For permitted combinations containing camphor... camphor, menthol, and eucalyptus oil identified in § 341.40(u). The labeling states the warnings for... containing camphor, menthol, and eucalyptus oil identified in § 341.40(u). The labeling states the...

  3. Antifeedant Activity and Active Ingredients Against Plutella xylostella from Momordica charantia Leaves

    Institute of Scientific and Technical Information of China (English)

    2008-01-01

    With the bioguided fractionation of the ethanol extracts from the leaves of Momordica charantia, we obtained two most active compounds against the feeding of the diamondback moth, Plutella xylostella larvae. The antifeedant activity of momordicine Ⅰ and momordicine Ⅱ against the second and the third instar larvae of Plutella xylostella were tested using leaf discs of cabbage in the laboratory. The results showed that momordicin Ⅰ and momordiein Ⅱ had significant antifeedant activity on the larvae of P. Xylostella, and momordicin Ⅱ was more active than momordicin Ⅰ. The concentrations for 50% antifeedant effects (AFC50) of momordicin Ⅱ against the second and the third instar larvae of P. Xylostella were 76.69 and 116.24 μg mL-1, whereas that of momordicin Ⅰ was 144.08 and 168.42 μg mL-1, respectively. In addition, momordicin Ⅰ and momordicin Ⅱ had significant inhibitive effect on the rate of weight gain and survival of P. Xylostella larvae.

  4. Content of Selected Minerals and Active Ingredients in Teas Containing Yerba Mate and Rooibos.

    Science.gov (United States)

    Rusinek-Prystupa, Elżbieta; Marzec, Zbigniew; Sembratowicz, Iwona; Samolińska, Wioletta; Kiczorowska, Bożena; Kwiecień, Małgorzata

    2016-07-01

    The study aimed to determine the content of selected elements: sodium, potassium, copper, zinc, iron, manganese and active ingredients such as phenolic acids and tannins in teas containing Yerba Mate and Rooibos cultivated in various areas. The study material comprised six samples of Yerba Mate teas and of Rooibos teas, both tea bags and leaves, purchased in Puławy and online via Allegro. In total, 24 samples were tested. Yerba Mate was particularly abundant in Mn and Fe. The richest source of these elements was Yerba Mate Yer-Vita (2261.3 mg · kg(-1) d.m.) and (691.6 mg · kg(-1) d.m.). The highest content of zinc was determined in Yerba Mate Amanda with lime (106.0 mg · kg(-1) d.m.), while copper was most abundant in Yerba Mate Big-Active cocoa and vanilla (14.05 mg · kg(-1) d.m.). In Rooibos, the content of sodium was several times higher than in Yerba Mate. A clear difference was observed in the content of minerals in dry weight of the examined products, which could be a result of both the taxonomic distinctness and the origin of the raw material. Leaf teas turned out to be a better source of tannins; on the other hand, tea bags contained substantially more phenolic acids. The richest source of phenolic acids was Yer-Vita in bags (1.8 %), and the highest amount of tannins was recorded in the leaf tea Green Goucho caramel and dark chocolate (9.04 g · 100 g(-1) d.m.). In Rooibos products, the highest content of phenolic acids was recorded in tea bags (Savannah with honey and vanilla 0.96 %), and tannins in (Lord Nelson with strawberry and cream 7.99 g · 100 g (-1) d.m.). PMID:26686675

  5. Biodegradation of pharmaceuticals in hospital wastewater by a hybrid biofilm and activated sludge system (Hybas)

    Energy Technology Data Exchange (ETDEWEB)

    Escolà Casas, Mònica [Environmental Science, Aarhus University, Frederiksborgsvej 399, 4000 Roskilde (Denmark); Chhetri, Ravi Kumar [Department of Environmental Engineering, Technical University of Denmark, Miljøvej 113, 2800 Kgs. Lyngby (Denmark); Ooi, Gordon [Environmental Science, Aarhus University, Frederiksborgsvej 399, 4000 Roskilde (Denmark); Hansen, Kamilla M.S. [Department of Environmental Engineering, Technical University of Denmark, Miljøvej 113, 2800 Kgs. Lyngby (Denmark); Litty, Klaus [Department of Chemistry and Biotechnology, Danish Technological Institute, Kongsvang Allé 29, 8000 Aarhus C (Denmark); Christensson, Magnus [AnoxKaldnes, Klosterängsvägen 11A, 226 47 Lund (Sweden); Kragelund, Caroline [Department of Chemistry and Biotechnology, Danish Technological Institute, Kongsvang Allé 29, 8000 Aarhus C (Denmark); Andersen, Henrik R. [Department of Environmental Engineering, Technical University of Denmark, Miljøvej 113, 2800 Kgs. Lyngby (Denmark); Bester, Kai, E-mail: kb@envs.au.dk [Environmental Science, Aarhus University, Frederiksborgsvej 399, 4000 Roskilde (Denmark)

    2015-10-15

    Hospital wastewater contributes a significant input of pharmaceuticals into municipal wastewater. The combination of suspended activated sludge and biofilm processes, as stand-alone or as hybrid process (hybrid biofilm and activated sludge system (Hybas™)) has been suggested as a possible solution for hospital wastewater treatment. To investigate the potential of such a hybrid system for the removal of pharmaceuticals in hospital wastewater a pilot plant consisting of a series of one activated sludge reactor, two Hybas™ reactors and one moving bed biofilm reactor (MBBR) has been established and adapted during 10 months of continuous operation. After this adaption phase batch and continuous experiments were performed for the determination of degradation of pharmaceuticals. Removal of organic matter and nitrification mainly occurred in the first reactor. Most pharmaceuticals were removed significantly. The removal of pharmaceuticals (including X-ray contrast media, β-blockers, analgesics and antibiotics) was fitted to a single first-order kinetics degradation function, giving degradation rate constants from 0 to 1.49 h{sup −1}, from 0 to 7.78 × 10{sup −1} h{sup −1}, from 0 to 7.86 × 10{sup −1} h{sup −1} and from 0 to 1.07 × 10{sup −1} h{sup −1} for first, second, third and fourth reactors respectively. Generally, the highest removal rate constants were found in the first and third reactors while the lowest were found in the second one. When the removal rate constants were normalized to biomass amount, the last reactor (biofilm only) appeared to have the most effective biomass in respect to removing pharmaceuticals. In the batch experiment, out of 26 compounds, 16 were assessed to degrade more than 20% of the respective pharmaceutical within the Hybas™ train. In the continuous flow experiments, the measured removals were similar to those estimated from the batch experiments, but the concentrations of a few pharmaceuticals appeared to increase

  6. Biodegradation of pharmaceuticals in hospital wastewater by a hybrid biofilm and activated sludge system (Hybas)

    International Nuclear Information System (INIS)

    Hospital wastewater contributes a significant input of pharmaceuticals into municipal wastewater. The combination of suspended activated sludge and biofilm processes, as stand-alone or as hybrid process (hybrid biofilm and activated sludge system (Hybas™)) has been suggested as a possible solution for hospital wastewater treatment. To investigate the potential of such a hybrid system for the removal of pharmaceuticals in hospital wastewater a pilot plant consisting of a series of one activated sludge reactor, two Hybas™ reactors and one moving bed biofilm reactor (MBBR) has been established and adapted during 10 months of continuous operation. After this adaption phase batch and continuous experiments were performed for the determination of degradation of pharmaceuticals. Removal of organic matter and nitrification mainly occurred in the first reactor. Most pharmaceuticals were removed significantly. The removal of pharmaceuticals (including X-ray contrast media, β-blockers, analgesics and antibiotics) was fitted to a single first-order kinetics degradation function, giving degradation rate constants from 0 to 1.49 h−1, from 0 to 7.78 × 10−1 h−1, from 0 to 7.86 × 10−1 h−1 and from 0 to 1.07 × 10−1 h−1 for first, second, third and fourth reactors respectively. Generally, the highest removal rate constants were found in the first and third reactors while the lowest were found in the second one. When the removal rate constants were normalized to biomass amount, the last reactor (biofilm only) appeared to have the most effective biomass in respect to removing pharmaceuticals. In the batch experiment, out of 26 compounds, 16 were assessed to degrade more than 20% of the respective pharmaceutical within the Hybas™ train. In the continuous flow experiments, the measured removals were similar to those estimated from the batch experiments, but the concentrations of a few pharmaceuticals appeared to increase during the first treatment step. Such

  7. The effect of different formulations of equivalent active ingredients on the performance of two topical wound treatment products.

    Science.gov (United States)

    Gray, Mikel; Jones, David P

    2004-03-01

    Product selection for the management of pressure ulcers or perineal dermatitis is typically based on consideration of active ingredients, but a growing body of evidence suggests that delivery vehicles also may influence product safety and efficacy. A 10-day, randomized, controlled experimental study was conducted to compare the safety and efficacy of two prescription products used for the treatment of pressure ulcers and perineal dermatitis. Both products contain equivalent active ingredients (balsam of Peru, castor oil, and trypsin), but one product delivers these ingredients in an ointment base while the other uses an aerosol spray. Sixty healthy volunteers (> 65 years of age) underwent intentional creation of two equivalent skin wounds (approximately 6 mm in diameter) using an Erbium-YAG laser. Volunteers served as their own control. Wounds were randomized to treatment with one of the balsam of Peru products or saline. Wounds were evaluated every other day. Significant differences between treatments were observed for most outcome variables (edema, scabbing, erythema, epithelialization). Wounds managed with the ointment-based product had lower edema, scabbing, and erythema scores and higher epithelialization scores than the spray or saline managed wounds. The results of this study confirm that formulation of the vehicle base can have a significant effect on product safety and effectiveness.

  8. Special active ingredients and beauty-food%特种活性物及营养美容

    Institute of Scientific and Technical Information of China (English)

    韩建英

    2012-01-01

    介绍了特种活性物及营养美容的理念。消费者目前对营养美容理念的兴趣越来越浓厚,使得营养美容产品逐渐成为市场营销的热点。配方师也热衷于将营养品与美容相结合,开发出营养美容产品,并将营养美容对身体的益处都囊括在产品配方中。介绍了几种最具潜力的营养美容成分以及特种活性物成分,并对其前景进行了展望。%The idea of special active ingredients and beauty-food are introduced briefly. Nowadays, the consumers become more and more interested in the concept of beauty-food, and the beauty-food product category has gradually become the hot topic of marketing. Formulators are eager to combine the benefits of nutrition with beauty in the formulations, and develop the beauty-food products. Some diet beauty ingredients with the greatest potential are introduced, and the future of the special active ingredients and the beauty-food are prospected here.

  9. Anti-inflammaging and antiglycation activity of a novel botanical ingredient from African biodiversity (Centevita™

    Directory of Open Access Journals (Sweden)

    Maramaldi G

    2013-12-01

    Full Text Available Giada Maramaldi,1 Stefano Togni,1 Federico Franceschi,1 Elian Lati21Indena SpA, Milan, Italy; 2Laboratoire BIO-EC, Longjumeau, FrancePurpose: The aim of this study was to investigate the topical efficacy of a new purified extract from Madagascar, Gotu Kola (Centella asiatica [L.] Urban, both on human explants and on human volunteers, in relation to skin wrinkling and skin protection against ultraviolet light exposure. The extract, with a peculiar content of biologically active molecules, was investigated as a novel anti-inflammaging and antiglycation agent. Its typical terpenes, known as collagen synthesis promoters, represent at least 45% of the extract. It also contains a polyphenolic fraction cooperating to the observed properties.Methods: C. asiatica purified extract was assayed on human skin explants maintained alive, and several parameters were evaluated. Among the most relevant, the thymine dimerization was evaluated by immunostaining. Malondialdehyde formation was evaluated as free-radical scavenging marker by enzyme-linked immunosorbent assay. The expression of interleukin-1a was observed by enzyme-linked immunosorbent assay as well. The product was further evaluated as an antiglycation agent, being glycation quantified by the advanced glycation product carboxymethyl lysine. C. asiatica purified extract was also evaluated as an antiwrinkling agent in a single-blind, placebo-controlled study. Formulated in a simple oil-in-water emulsion, the extent of wrinkling was assessed by skin replicas, skin firmness, skin elasticity, and collagen density measurements.Results: C. asiatica purified extract could protect DNA from ultraviolet light-induced damage, decreasing the thymine photodimerization by over 28% (P<0.05. A reduced (26%, P<0.01 expression of interleukin-1α was also observed, supporting its anti-inflammatory potential. C. asiatica purified extract showed in vitro a total inhibition of carboxymethyl lysine formation induced by the

  10. Bioactive Ingredients and Antioxidant Activity of Austrian Wine and Grape Juice

    OpenAIRE

    Pérez Navarro, Roser

    2008-01-01

    Wine has already been investigated for its potential nutritional quality, such as high amount of phenolic compounds. Phenolic compounds, well-known as natural antioxidants, are reported due their radical scavenging capacity. In the present work, the bioactive ingredients of nine Austrian wines (four red wines: Zweigelt, Blaufränkisch, Syrah and Cuvée; two white wines: Pinot Blanc and Chardonnay; one rosé Blaufränkisch; and two grape juice: red and white) have been quantified an...

  11. The interaction of a model active pharmaceutical with cationic surfactant and the subsequent design of drug based ionic liquid surfactants.

    Science.gov (United States)

    Qamar, Sara; Brown, Paul; Ferguson, Steven; Khan, Rafaqat Ali; Ismail, Bushra; Khan, Abdur Rahman; Sayed, Murtaza; Khan, Asad Muhammad

    2016-11-01

    Interactions of active pharmaceutical ingredients (API) with surfactants remain an important research area due to the need to improve drug delivery systems. In this study, UV-Visible spectrophotometry was used to investigate the interactions between a model low molecular weight hydrophilic drug sodium valproate (SV) and cationic surfactant cetyltrimethylammonium bromide (CTAB). Changes in the spectra of SV were observed in pre- and post-micellar concentrations of CTAB. The binding constant (Kb) values and the number of drug molecules encapsulated per micelle were calculated, which posed the possibility of mixed micelle formation and strong complexation between SV and CTAB. These results were compared to those of a novel room temperature surface active ionic liquid, which was synthesized by the removal of inorganic counterions from a 1:1 mixture of CTAB and SV. In this new compound the drug now constitutes a building block of the carrier and, as such, has considerably different surfactant properties to its building blocks. In addition, enhanced solubility in a range of solvents, including simulated gastric fluid, was observed. The study provides valuable experimental evidence concerning the performance of drug based surfactant ionic liquids and how their chemical manipulation, without altering the architecture of the API, leads to control of surfactant behavior and physicochemical properties. In turn, this should feed through to improved and controlled drug release rates and delivery mechanisms, and the prevention of precipitation or formation of polymorphs typical of crystalline form APIs. PMID:27472069

  12. Required ozone doses for removing pharmaceuticals from wastewater effluents

    DEFF Research Database (Denmark)

    Antoniou, Maria; Hey, Gerly; Rodríguez Vega, Sergio;

    2013-01-01

    The aim of the this study was to investigate the ozone dosage required to remove active pharmaceutical ingredients (APIs) from biologically treated wastewater of varying quality, originated from different raw wastewater and wastewater treatment processes.Secondary effluents from six Swedish...

  13. An Integrated Approach to Thermal Analysis of Pharmaceutical Solids

    Science.gov (United States)

    Riley, Shelley R. Rabel

    2015-01-01

    A three-tiered experiment for undergraduate Instrumental Analysis students is presented in which students characterize the solid-state thermal behavior of an active pharmaceutical ingredient (acetaminophen) and excipient (a-lactose hydrate) using differential scanning calorimetry, thermogravimetric analysis, and thermal microscopy. Students are…

  14. Examining pharmaceuticals using terahertz spectroscopy

    Science.gov (United States)

    Sulovská, Kateřina; Křesálek, Vojtěch

    2015-10-01

    Pharmaceutical trafficking is common issue in countries where they are under stricter dispensing regime with monitoring of users. Most commonly smuggled pharmaceuticals include trade names Paralen Plus, Modafen, Clarinase repetabs, Aspirin complex, etc. These are transported mainly from Eastern Europe (e.g. Poland, Ukraine, Russia) to countries like Czech Republic, which is said to have one of the highest number of methamphetamine producers in Europe. The aim of this paper is to describe the possibility of terahertz spectroscopy utilization as an examining tool to distinguish between pharmaceuticals containing pseudoephedrine compounds and those without it. Selected medicaments for experimental part contain as an active ingredient pseudoephedrine hydrochloride or pseudoephedrine sulphate. Results show a possibility to find a pseudoephedrine compound spectra in samples according to previously computed and experimentally found ones, and point out that spectra of same brand names pills may vary according to their expiration date, batch, and amount of absorbed water vapours from ambience. Mislead spectrum also occurs during experimental work in a sample without chosen active ingredient, which shows persistent minor inconveniences of terahertz spectroscopy. All measurement were done on the TPS Spectra 3000 instrument.

  15. BULK AND SURFACE PROPERTIES OF TIN BASED HERBAL DRUG DURING ITS PREPARATION: FINGERPRINTING OF THE ACTIVE PHARMACEUTICAL CONSTITUENT

    Directory of Open Access Journals (Sweden)

    Asit Baran Mandal et al.

    2012-04-01

    Full Text Available The Tin based herbal drug (Vangaparpam - a Siddha system of Medicine has been widely used for the treatment of urinogenital infection and Arthritis. It was prepared by ten sequential stages of calcinations of the medicinally purified tin along with Aloe vera extract. In this study we analysed samples from various stages of preparation using analytical techniques viz., Fourier Transformed Infrared spectroscopy, Powder X ray Diffraction, X ray Photoelectron Spectroscopy, Energy Dispersive X- ray spectroscopy , Scanning Electron Microscopy, to create fingerprints required for the optimisation of the process parameters, detection of toxic impurities and crystal morphology of the Active Pharmaceutical ingredient during the formulation of drug for which reports are not available. Upon analysis of the samples of various stages of calcinations, we found that there was a programmed heating the medicinally purified tin metal was converted to crystalline tin oxide in the tetragonal phase at the first stage of calcinations itself along with a small percentage of therapeutically important elements of Calcium, Iron, and Potassium. Further calcinations steps brought interplay of nano and sub-micro sized particles for optimum bioavailability of the drug.

  16. [Efficiency in the prescription of drugs. Impact of a health policy: automatic change to prescription by active ingredient].

    Science.gov (United States)

    López de Landache, Isabel Elizondo; Braceras Izaguirre, Leire; Echeto García, Ainara; Gardeazabal Romillo, Maria José; Acevedo Heranz, Paloma

    2013-11-01

    In the Basque Country in June 2010 were changed in the electronic prescription system the treatments prescribed by a brand by active ingredients, all the patients who had prescribed these molecules: atorvastatin, clopidogrel, weekly risedronate and losartan-hydrochlorothiazide. The aim of this study was to evaluate the economic impact of this change automated done in June 2010. Retrospective study of the prescriptions made in the Basque Country of the selected active ingredients. The use of generics of these molecules from May to December 2010 increased from 64 points to 87. Particularly clopidogrel increased from 6.25% in generic prescriptions to 93.76%, losartan + hydrochlorothiazide from 17.94% to 93.83%, 18.92% for atorvastatin acid and 96.03% risedronic 1.76% to 65.97%. If we make the estimation of the amount of active ingredient in generic containers that have been dispensed from June to December 2010. If they had dispensed brand drugs you get this quantity of total savings: 8 104 762.22 euros. This work suggests that a program to promote use of generics increased efficiency in the use of drugs. To promote the use of generic drugs is an efficiency measure implemented in the NHS and in the neighboring countries, in recent figures are reached 40% in securities of U.S.A packaging and around 65% in the Basque Country the consume in early 2010 was much lower than these figures stand at 20% and at the end of the year stood at 27% thanks to the measures taken. PMID:24404717

  17. Preventive effects of Flos Perariae (Gehua water extract and its active ingredient puerarin in rodent alcoholism models

    Directory of Open Access Journals (Sweden)

    Wang Yuqiang

    2010-10-01

    Full Text Available Abstract Background Radix Puerariae is used in Chinese medicine to treat alcohol addiction and intoxication. The present study investigates the effects of Flos puerariae lobatae water extract (FPE and its active ingredient puerarin on alcoholism using rodent models. Methods Alcoholic animals were given FPE or puerarin by oral intubation prior or after alcohol treatment. The loss of righting reflex (LORR assay was used to evaluate sedative/hypnotic effects. Changes of gama-aminobutyric acid type A receptor (GABAAR subunits induced by alcohol treatment in hippocampus were measured with western blot. In alcoholic mice, body weight gain was monitored throughout the experiments. Alcohol dehydrogenase (ADH levels in liver were measured. Results FPE and puerarin pretreatment significantly prolonged the time of LORR induced by diazepam in acute alcoholic rat. Puerarin increased expression of gama-aminobutyric acid type A receptor alpha1 subunit and decreased expression of alpha4 subunit. In chronic alcoholic mice, puerarin pretreatment significantly increased body weight and liver ADH activity in a dose-dependent manner. Puerarin pretreatment, but not post-treatment, can reverse the changes of gama-aminobutyric acid type A receptor subunit expression and increase ADH activity in alcoholism models. Conclusion The present study demonstrates that FPE and its active ingredient puerarin have preventive effects on alcoholism related disorders.

  18. 21 CFR 310.545 - Drug products containing certain active ingredients offered over-the-counter (OTC) for certain uses.

    Science.gov (United States)

    2010-04-01

    ... (as single ingredient) Resorcinol monoacetate (as single ingredient) Salicylic acid (over 2 up to 5...-vinylacetate copolymers Pyrilamine maleate Salicylamide Salicylic acid Simethicone Sulfur Tannic acid Thymol... dihydrogen citrate Povidone-vinylacetate copolymers Salicylic acid Simethicone Tannic acid Topical...

  19. Analysis of Three Penicillin Antibiotics (Ampicillin, Amoxicillin and Cloxacillin) of Several Iranian Pharmaceutical Companies by HPLC

    OpenAIRE

    A. Ashnagar; N. Gharib Naseri

    2007-01-01

    Penicillin has been the most widely used antibiotic for many gram-positive bacterial infections. In this research the purity of the standard active ingredients of the various dosage forms of three penicillins (Amoxicillin, Cloxacillin and Ampicillin) imported and the purity percentage of the active ingredients in each of the various dosage forms of these drugs manufactured by several pharmaceutical companies of Iran (Kosar, Farabi and Jaber Ibn Hayan) were investigated and determined by HPLC ...

  20. Lubricants in Pharmaceutical Solid Dosage Forms

    Directory of Open Access Journals (Sweden)

    Jinjiang Li

    2014-02-01

    Full Text Available Lubrication plays a key role in successful manufacturing of pharmaceutical solid dosage forms; lubricants are essential ingredients in robust formulations to achieve this. Although many failures in pharmaceutical manufacturing operations are caused by issues related to lubrication, in general, lubricants do not gain adequate attention in the development of pharmaceutical formulations. In this paper, the fundamental background on lubrication is introduced, in which the relationships between lubrication and friction/adhesion forces are discussed. Then, the application of lubrication in the development of pharmaceutical products and manufacturing processes is discussed with an emphasis on magnesium stearate. In particular, the effect of its hydration state (anhydrate, monohydrate, dihydrate, and trihydrate and its powder characteristics on lubrication efficiency, as well as product and process performance is summarized. In addition, the impact of lubrication on the dynamics of compaction/compression processes and on the mechanical properties of compacts/tablets is presented. Furthermore, the online monitoring of magnesium stearate in a blending process is briefly mentioned. Finally, the chemical compatibility of active pharmaceutical ingredient (API with magnesium stearate and its reactive impurities is reviewed with examples from the literature illustrating the various reaction mechanisms involved.

  1. Validation of a method by gas chromatography for the determination of fatty acids that comprise the active ingredient D-004

    International Nuclear Information System (INIS)

    D-004 is a new active ingredient obtained from the Cuban royal palm (Roystonea regia) fruits. This substance is mainly composed by a mixture of saturated and unsaturated free fatty acids, from 8 to 18 carbon atoms, and has shown to be effective in experimental model of prostate hyperplasia. A capillary gas chromatographic method for the determination of the fatty acids in D-004 was developed and validated. The acids were analyzed as methyl ester derivatives, which were obtained by reaction with 10 % acetyl chloride in methanol and separated in a BPX-5 wide-bore column using tridecanoic acid as internal standard. The specificity study showed no interferences regarding the determination of this mixture, once the samples were submitted to stress conditions. Determination of the total fatty acid content was linear (r > 0.999; CVs of the response factors and of the slopes lower than 5 and 2 %, respectively) and without bias in the studied concentration range, from 50 to 150 % of the nominal mass. In the accuracy study, over the range 80 to 120 % of the nominal fatty acid concentration, high recoveries (100.4 to 100.8 %) were reached. Good results were obtained in the repeatability and intermediate precision studies (CV < 2%), proving that the method is precise. These results support that this method is properly validated, being appropriate for the quality control and stability studies of this active ingredient

  2. Pharmaceutical gel analysis by NIR spectroscopy. Determination of the active principle and low concentration of preservatives.

    Science.gov (United States)

    Blanco, M; Alcalá, M; Bautista, M

    2008-04-23

    Near infrared spectroscopy has proved highly suitable for the analysis of pharmaceutical formulations. However, its limited sensitivity can severely restrict its scope of application. In this work, we determine the active principle and two preservatives in a pharmaceutical preparation available as a hydrogel. The matrix of the pharmaceutical preparation exhibits strong absorption in the NIR spectral region; also, the two preservatives (parabens) are very similar in chemical and spectral terms, and present at low concentrations in the pharmaceutical. These complications make it rather difficult to accurately quantify the active principle and the preservatives, which can only be accomplished by using an effective design in order to prepare the samples to be included in the calibration set and select the optimum spectral range for measuring each analyte. The evaporation of solvents during the measurement process produces increasing errors related with sample's air exposition; the introductions of new samples with a wider range of the volatile components correct this effect. An ANOVA of the predictions obtained with the new models shows that correct the error due to evaporation. The proposed method was validated for the analytical control of the studied preparation.

  3. Behavior of selected pharmaceuticals in topsoil of Greyic Phaeozem

    Science.gov (United States)

    Kodesova, Radka; Klement, Ales; Kocarek, Martin; Fer, Miroslav; Golovko, Oksana; Grabic, Roman; Jaksik, Ondrej

    2014-05-01

    It has been documented in several studies that soil may be contaminated by human or veterinary pharmaceuticals. Some of pharmaceutical ingredient may be retained in soils. The rest can be transported to the surface and groundwater through surface runoff and infiltration. Mobility of contaminants in soils is dependent on many soil and pharmaceutical properties (e.g. pharmaceutical adsorption on soil particles and pharmaceutical degradation). The goals of this study were: (1) to measure adsorption isotherms of selected pharmaceuticals in one soil; (2) to evaluate degradation of selected pharmaceuticals in this soil, and (3) to evaluate impact of applied pharmaceuticals on biological activity in soil, which influences pharmaceutical decomposition. Batch sorption tests were performed for 7 selected pharmaceuticals (beta blockers Atenolol and Metoprolol, anticonvulsant Carbamazepin, and antibiotics Clarithromycin, Clindamycin, Trimetoprim and Sulfamethoxazol) and one soil (topsoil of Greyic Phaeozem from Čáslav). The same concentrations (0.5, 1, 2.5, 5 and 10 mg/l) were used for almost all pharmaceuticals except Clarithromycin (0.033, 0.08, 0.165, 0.25, 0.33 mg/l). The Freundlich equations were used to describe adsorption isotherms. Degradation of all 7 pharmaceuticals was also studied. Solutes of different pharmaceuticals (concentration of 8.3 mg/l) were added into the plastic bottles (one pharmaceutical per bottle) with soil. Concentrations of pharmaceuticals remaining in soil 1, 2, 5, 12, 23, 40 and 61 days after the pharmaceutical application were analyzed. Colony forming unites were evaluated to describe microbial activity in time affected by different pharmaceuticals. Adsorption of studied pharmaceuticals on soil particles decreasing as follows: Clarithromycin, Trimetoprim, Metoprolol, Clindamycin, Atenolol, Carbamazepin, Sulfamethoxazol. Degradation rates in some degree reflected adsorption of studied pharmaceuticals on soil particles and increased with

  4. Severe anaphylaxis: the secret ingredient.

    Science.gov (United States)

    Buergi, Andreas; Jung, Barbara; Padevit, Christian; John, Hubert; Ganter, Michael T

    2014-02-01

    In this case report, we describe a healthy urological patient who suffered severe intraoperative anaphylaxis to chlorhexidine, an ingredient contained in frequently used lubricants (Instillagel, Endosgel). Chlorhexidine is a well-known skin disinfectant and antiseptic component in mouthwash or other over the counter antiseptic pharmaceuticals. There is little awareness that commonly used lubricants may contain hidden chlorhexidine. After severe intraoperative anaphylaxis, it is important to investigate all potential (including hidden) agents that might have caused this life-threatening reaction. PMID:25611155

  5. 原料药清洁验证的程序%Cleaning Validation Procedure for Active Pharmaceutical Ingredient

    Institute of Scientific and Technical Information of China (English)

    刘锋; 代兴华; 刘欢欢

    2015-01-01

    新版GMP实施后,为最大限度地降低药品生产过程中污染、交叉污染等风险,必须进行清洁验证。而在实际操作中,有一些人特别是新参加工作的人不清楚清洁验证将按照什么程序来进行。笔者在此根据本人工作经验和相关法规要求,对清洁验证的程序按照时间先后顺序一一列出,并对每一步应完成的工作进行总结。%After the implementation of new edition of GMP, to minimize the risk of contamination, cross-contamination etc. in the drug manufacturing course, conducting cleaning validation is necessary. But in actual operating practices, some people, especially new employee are not sure how to carry out cleaning validation. According to author’s experience and requirements of relevant regulations, this text lists cleaning validation procedure step by step, and provides details on how to complete each step.

  6. Analysis of China's active pharmaceutical ingredient export situation%中国原料药出口态势分析

    Institute of Scientific and Technical Information of China (English)

    曹钢; 柳燕

    2014-01-01

    原料药是中国的传统优势产业,近年来政府的助力推动、竞争环境的变化和国际医药产业分工的调整,推动了中国原料药产业的转型升级.中国在全球医药供应体系中扮演着越来越重要的角色,特色原料药的品种越来越丰富,产业链不断向高端延伸.对中国原料药出口态势进行了分析.

  7. Transformation of an active pharmaceutical ingredient upon high-energy milling: A process-induced disorder in Biclotymol.

    Science.gov (United States)

    Schammé, Benjamin; Couvrat, Nicolas; Malpeli, Pascal; Dudognon, Emeline; Delbreilh, Laurent; Dupray, Valérie; Dargent, Éric; Coquerel, Gérard

    2016-02-29

    This study investigates for the first time the thermodynamic changes of Biclotymol upon high-energy milling at various levels of temperature above and below its glass transition temperature (Tg). Investigations have been carried out by temperature modulated differential scanning calorimetry (TM-DSC) and X-ray powder diffraction (XRPD). Results indicate that Biclotymol undergoes a solid-state amorphization upon milling at Tg-45 °C. It is shown that recrystallization of amorphous milled Biclotymol occurs below the glass transition temperature of Biclotymol (Tg=20 °C). This displays molecular mobility differences between milled Biclotymol and quenched liquid. A systematic study at several milling temperatures is performed and the implication of Tg in the solid-state transformations generally observed upon milling is discussed. Influence of analysis temperature with respect to interpretation of results was investigated. Finally, it is shown that co-milling Biclotymol with only 20 wt% of amorphous PVP allows a stable amorphous dispersion during at least 5 months of storage. PMID:26707413

  8. Chemical constituents of active pharmaceutical ingredients of elemene%榄香烯原料药的化学成分

    Institute of Scientific and Technical Information of China (English)

    孙敏鸽; 李淑斌; 周莉; 张青

    2009-01-01

    目的 对榄香烯原料药化学成分进行系统研究.方法 采用氧化铝柱色谱、硅胶柱色谱和制备型HPLC等分离方法从榄香烯原料药中分离化合物,采用NMR等光谱学手段对它们进行结构鉴定.结果 共分离得到4个化合物,分别鉴定为β -榄香烯(1)、γ -榄香烯(2)、β -石竹烯(3)和δ -榄香烯(4).结论 不仅对榄香烯原料药的3个主要活性成分进行了结构确证,而且对原料药中的1个主要杂质成分β -石竹烯进行了结构确证,并首次对文献中β -石竹烯碳谱数据中有误的归属进行了纠正.为榄香烯原料药质量控制和临床试验的研究提供了明确的物质基础.

  9. Self-assembled sorbitol-derived supramolecular hydrogels for the controlled encapsulation and release of active pharmaceutical ingredients.

    Science.gov (United States)

    Howe, Edward J; Okesola, Babatunde O; Smith, David K

    2015-05-01

    A simple supramolecular hydrogel based on 1,3:2,4-di(4-acylhydrazide)benzylidene sorbitol (DBS-CONHNH2), is able to extract acid-functionalised anti-inflammatory drugs via directed interactions with the self-assembled gel nanofibres. Two-component hydrogel-drug hybrid materials can be easily formed by mixing and exhibit pH-controlled drug release.

  10. Transformation of an active pharmaceutical ingredient upon high-energy milling: A process-induced disorder in Biclotymol.

    Science.gov (United States)

    Schammé, Benjamin; Couvrat, Nicolas; Malpeli, Pascal; Dudognon, Emeline; Delbreilh, Laurent; Dupray, Valérie; Dargent, Éric; Coquerel, Gérard

    2016-02-29

    This study investigates for the first time the thermodynamic changes of Biclotymol upon high-energy milling at various levels of temperature above and below its glass transition temperature (Tg). Investigations have been carried out by temperature modulated differential scanning calorimetry (TM-DSC) and X-ray powder diffraction (XRPD). Results indicate that Biclotymol undergoes a solid-state amorphization upon milling at Tg-45 °C. It is shown that recrystallization of amorphous milled Biclotymol occurs below the glass transition temperature of Biclotymol (Tg=20 °C). This displays molecular mobility differences between milled Biclotymol and quenched liquid. A systematic study at several milling temperatures is performed and the implication of Tg in the solid-state transformations generally observed upon milling is discussed. Influence of analysis temperature with respect to interpretation of results was investigated. Finally, it is shown that co-milling Biclotymol with only 20 wt% of amorphous PVP allows a stable amorphous dispersion during at least 5 months of storage.

  11. An investigation into the crystallization tendency/kinetics of amorphous active pharmaceutical ingredients: A case study with dipyridamole and cinnarizine.

    Science.gov (United States)

    Baghel, Shrawan; Cathcart, Helen; Redington, Wynette; O'Reilly, Niall J

    2016-07-01

    Amorphous drug formulations have great potential to enhance solubility and thus bioavailability of BCS class II drugs. However, the higher free energy and molecular mobility of the amorphous form drive them towards the crystalline state which makes them unstable. Accurate determination of the crystallization tendency/kinetics is the key to the successful design and development of such systems. In this study, dipyridamole (DPM) and cinnarizine (CNZ) have been selected as model compounds. Thermodynamic fragility (mT) was measured from the heat capacity change at the glass transition temperature (Tg) whereas dynamic fragility (mD) was evaluated using methods based on extrapolation of configurational entropy to zero [Formula: see text] , and heating rate dependence of Tg [Formula: see text] . The mean relaxation time of amorphous drugs was calculated from the Vogel-Tammann-Fulcher (VTF) equation. Furthermore, the correlation between fragility and glass forming ability (GFA) of the model drugs has been established and the relevance of these parameters to crystallization of amorphous drugs is also assessed. Moreover, the crystallization kinetics of model drugs under isothermal conditions has been studied using Johnson-Mehl-Avrami (JMA) approach to determine the Avrami constant 'n' which provides an insight into the mechanism of crystallization. To further probe into the crystallization mechanism, the non-isothermal crystallization kinetics of model systems were also analysed by statistically fitting the crystallization data to 15 different kinetic models and the relevance of model-free kinetic approach has been established. The crystallization mechanism for DPM and CNZ at each extent of transformation has been predicted. The calculated fragility, glass forming ability (GFA) and crystallization kinetics are found to be in good correlation with the stability prediction of amorphous solid dispersions. Thus, this research work involves a multidisciplinary approach to establish fragility, GFA and crystallization kinetics as stability predictors for amorphous drug formulations. PMID:27108783

  12. Impact of solid retention time and nitrification capacity on the ability of activated sludge to remove pharmaceuticals

    DEFF Research Database (Denmark)

    Falås, Per; Andersen, Henrik Rasmus; Ledin, Anna;

    2012-01-01

    Removal of five acidic pharmaceuticals (ibuprofen, ketoprofen, naproxen, diclofenac and clofibric acid) by activated sludge from five municipal activated sludge treatment processes, with various sludge ages and nitrification capacities, was assessed through batch experiments. The increase in aero...

  13. The use of green tea extract in cosmetic formulations: not only an antioxidant active ingredient.

    Science.gov (United States)

    Gianeti, Mirela D; Mercurio, Daiane G; Campos, Patricia M B G Maia

    2013-01-01

    Green tea (GT) extracts contain polyphenols, known to be effective free radical scavengers, and other ingredients that could also provide benefits to the skin. This is a report on clinical studies using objective, noninvasive methods to evaluate the effects of cosmetic formulations containing GT. Experimental formulations were supplemented or not (vehicle) with 6% Camellia sinensis glycolic leaf extracts (GT). These formulations were applied to the forearm skin of 24 volunteers, and their effects were evaluated before and after 2 hours, 15 and 30 days according to the following parameters: stratum corneum water content, transepidermal water loss, skin viscoelastic-to-elastic ratio (Uv/Ue), and microrelief. The volunteers were instructed not to apply any formulation in an area of the forearm (control area). Experimental formulations (GT) increased skin moisture in the long-term study, indicating that GT has a prolonged moisturizing effect. The Uv/Ue was significantly enhanced after 30 days of topical application of the experimental formulation when compared with vehicle and control. After 15-30 days, skin microrelief was significantly improved due to a reduction in skin roughness. The results suggest that GT-containing cosmetic formulations have pronounced moisturizing effects and improve skin microrelief.

  14. The use of green tea extract in cosmetic formulations: not only an antioxidant active ingredient.

    Science.gov (United States)

    Gianeti, Mirela D; Mercurio, Daiane G; Campos, Patricia M B G Maia

    2013-01-01

    Green tea (GT) extracts contain polyphenols, known to be effective free radical scavengers, and other ingredients that could also provide benefits to the skin. This is a report on clinical studies using objective, noninvasive methods to evaluate the effects of cosmetic formulations containing GT. Experimental formulations were supplemented or not (vehicle) with 6% Camellia sinensis glycolic leaf extracts (GT). These formulations were applied to the forearm skin of 24 volunteers, and their effects were evaluated before and after 2 hours, 15 and 30 days according to the following parameters: stratum corneum water content, transepidermal water loss, skin viscoelastic-to-elastic ratio (Uv/Ue), and microrelief. The volunteers were instructed not to apply any formulation in an area of the forearm (control area). Experimental formulations (GT) increased skin moisture in the long-term study, indicating that GT has a prolonged moisturizing effect. The Uv/Ue was significantly enhanced after 30 days of topical application of the experimental formulation when compared with vehicle and control. After 15-30 days, skin microrelief was significantly improved due to a reduction in skin roughness. The results suggest that GT-containing cosmetic formulations have pronounced moisturizing effects and improve skin microrelief. PMID:23742288

  15. Investigation of pharmaceutical drugs and caffeine-containing foods using Fourier and terahertz time-domain spectroscopy

    Science.gov (United States)

    KaraliÅ«nas, Mindaugas; Venckevičius, Rimvydas; Kašalynas, Irmantas; Puc, Uroš; Abina, Andreja; Jeglič, Anton; Zidanšek, Aleksander; Valušis, Gintaras

    2015-08-01

    Several pharmaceutical drugs, such as alprazolam, ibuprofen, acetaminophen, activated carbon and others, and caffeine-containing foods were tested using terahertz (THz) time domain spectroscopy in the range from 0.3 to 2 THz. The dry powder of pharmaceutical drugs was mixed with HDPE and pressed into the pellets using hydraulic press. The coffee grounds were also pressed into the pellets after ball-milling and mixing with HDPE. The caffeine containing liquid foods were dried out on the paper strips of various stacking. Experiments allow one to determine characteristic spectral signatures of the investigated substances within THz range caused by active pharmaceutical ingredients, like in the case of caffeine, as well as supporting pharmaceutical ingredients. Spectroscopic THz imaging approach is considered as a possible option to identify packaged pharmaceutical drugs. The caffeine spectral features in the tested caffeine containing foods are difficult to observed due to the low caffeine concentration and complex caffeine chemical surrounding.

  16. Perceptions and Attitudes of Egyptian Health Professionals and Policy-Makers towards Pharmaceutical Sales Representatives and Other Promotional Activities.

    Directory of Open Access Journals (Sweden)

    Susan Kamal

    Full Text Available Pharmaceutical promotion activities in low and middle-income countries are often neither regulated nor monitored. While Egypt has the highest population and per capita use of medicines in the Arab world, we know very little about pharmaceutical companies promotional activities in the country.To explore and analyze the perceptions of physicians towards promotional and marketing activities of pharmaceutical companies among physicians and pharmacists in Egypt.Perspectives of different healthcare system stakeholders were explored through semi-structured, in-depth interviews conducted in 2014 in Cairo, Egypt. Interviewees were chosen via purposive sampling and snowball technique. Each interview was recorded and transcribed. Then qualitative, thematic analysis was conducted with the help of NVIVO software.The majority of physicians and pharmacists acknowledged exposure to pharmaceutical promotion. It was commonly believed that interaction with the pharmaceutical industry is necessary and both associated risks and benefits were acknowledged. The interviewed physicians considered themselves competent enough to minimize risks and maximize benefits to their prescribing habits. Views diverged on the extent and magnitude of the risks and benefits of pharmaceutical promotion, especially in regard to the influence on patients' health.Pharmaceutical promotion in Egypt is intensely directed at prescribers and dispensers. Physicians, pharmacists and policymakers expressed little skepticism to the influence of promotion towards their individual prescribing. Raising awareness of the pitfalls of pharmaceutical promotion is necessary, especially among the less experienced physicians.

  17. Water and stability of pharmaceutical solids

    Science.gov (United States)

    Shalaev, Evgenyi

    2007-03-01

    Solid pharmaceuticals are multi-component systems consisting of an active pharmaceutical ingredient (API) and inactive ingredients (excipients). Excipients may include inorganic salts (e.g., NaCl), carbohydrates (e.g., lactose), and polymers, to name a few, whereas APIs range from relatively simple molecules (e.g., aspirin) to proteins and olygonucleotides. Pharmaceutical solids could exist either as single-phase or heterophase systems. They also may have different extent of order, such as highly ordered crystalline phases, amorphous solids that are thermodynamically unstable but might be kinetically stable under the time frame of observation, and crystalline mesophases including liquid crystals. With all this diversity, there are common features for such systems, and two of them will be discussed in the presentation. (i) Requirements for chemical stability of pharmaceuticals are very strict. A very limited (e.g., less than 0.1%) extent of conversion is allowed in these materials over the shelf life, i.e., during several years of storage at ambient and (sometimes) not fully controlled (e.g., a medicine cabinet in one's bathroom) conditions. (ii) All pharmaceutical solids contain some water, although its amount and physical state are highly variable and may change during manufacturing and shelf life. There are many challenging questions and issues associated with the ``Water and stability of pharmaceutical solids'' subject; some of them will be considered in the presentation: (i) What are the features of chemical reactivity of crystalline vs disordered systems? (ii) What is the role of water in solid state chemical reactivity of amorphous solids, e.g., water as plasticizer vs reactant vs reaction media? (iii) How homogeneous are pharmaceutical amorphous solid solutions, e.g., carbohydrate-water systems? (iv) What is the optimal water content? With water being the most common destabilizing factor, is ``the drier - the better'' always the case?

  18. In silico dissolution rates of pharmaceutical ingredients

    Science.gov (United States)

    Dogan, Berna; Schneider, Julian; Reuter, Karsten

    2016-10-01

    The correlation between in vitro dissolution rates and the efficiency of drug formulations establishes an opportunity for accelerated drug development. Using in silico methods to predict the dissolution rates bears the prospect of further efficiency gains by avoiding the actual synthesis of candidate formulations. Here, we present a computational protocol that achieves such prediction for molecular crystals at low undersaturation. The protocol exploits the classic spiral dissolution model to minimize the number of material parameters that require explicit molecular simulations. Comparison to available data for acetylsalicylic acid and alpha lactose monohydrate indicates a tunable accuracy within one order of magnitude.

  19. Activated carbon for the removal of pharmaceutical residues from treated wastewater.

    Science.gov (United States)

    Ek, Mats; Baresel, Christian; Magnér, Jörgen; Bergström, Rune; Harding, Mila

    2014-01-01

    Pharmaceutical residues, which pass naturally through the human body into sewage, are in many cases virtually unaffected by conventional wastewater treatment. Accumulated in the environment, however, they can significantly impact aquatic life. The present study indicates that many pharmaceutical residues found in wastewater can be removed with activated carbon in a cost-efficient system that delivers higher resource utilisation and security than other carbon systems. The experiment revealed a substantial separation of the analysed compounds, notwithstanding their relatively high solubility in water and dissimilar chemical structures. This implies that beds of activated carbon may be a competitive alternative to treatment with ozone. The effluent water used for the tests, performed over 20 months, originated from Stockholm's largest sewage treatment plant. Passing through a number of different filters with activated carbon removed 90-98% of the pharmaceutical residues from the water. This paper describes pilot-scale tests performed by IVL and the implications for an actual treatment plant that has to treat up to several thousand litres of wastewater per second. In addition, the advantages, disadvantages and costs of the method are discussed. This includes, for example, the clogging of carbon filters and the associated hydraulic capacity limits of the activated carbon.

  20. Simultaneous determination of active ingredients in Erigeron breviscapus (Vant.) Hand-Mazz. by capillary electrophoresis with electrochemical detection.

    Science.gov (United States)

    Chu, Qingcui; Wu, Ting; Fu, Liang; Ye, Jiannong

    2005-03-01

    A high-performance capillary electrophoresis (CE) with electrochemical detection (ED) method was developed for the determination of the pharmacologically active ingredients in Erigeron breviscapus (Vant.) Hand-Mazz. and its extract phytopharmaceuticals in this work. Under the optimum conditions, nine analytes, baicalein, naringenin, scopoletin, kaempferol, apigenin, scutellarin, luteolin, caffeic acid and protocatechuic acid were separated within 24 min in a borax buffer (pH 8.7). Notably, excellent linearity was obtained over two orders of magnitude with detection limits (S/N=3) ranged from 1.0 x 10(-7) g/mL to 5.6 x 10(-7) g/mL for all nine analytes. This method was successfully used in the analysis of E. breviscapus (Vant.) Hand-Mazz. and its phytopharmaceuticals with a relatively simple extraction procedure, and the assay results were satisfactory. PMID:15740914

  1. [Chemical diversity of the biological active ingredients of salvia officinalis and some closely related species].

    Science.gov (United States)

    Máthé, Imre; Hohmann, Judit; Janicsák, Gábor; Nagy, Gábor; Dora, Rédei

    2007-01-01

    Comparative studies on the volatile and non-volatile fractions of 6 species. i.e. Salvia officinalis, S. tomentosa, S. fruticosa, S. candelabrum, S. ringens, S. lavandulifolia of the Section Salvia (Lamiaceae) have been carried out. Both fractions provide the chemical pattern matches to the chemotaxonomic character of Subfamily Nepetoideae in Erdtmanr two subfamiliar system. S. lavandulifolia had the highest essential oil content, followed by S. fruticosa, S. tomentosa, S. officinalis and S. candelabrum. S. ringens contains volatile oil only in traces. The neurotoxin thujone content was the highest in the S. officinalis oils and in that of S. fruticosa. No thujone was detected in S. lavandulifolia. The other species, e.g.: S. tomentosa contain this compound only in moderate concentrations (less than 10%). Among the non-volatile fractions of the plant ingredients the triterpene ursolic and oleanolic acids had the highest concentration in the leaves. Despite some rare cases, ursolic acid dominates the tritepene fraction. Rosmarinic and caffeic acids were measured in similar concentrations, in all species. As the case of S. officinalis shows, these compounds vary significantly in all organs during the vegetation period. Caffeic acid is also ubiquitous in the genus Salvia but as our data suggest it occurs in an order of magnitude lower concentration than rosmarinic acid. The isolation of phenylethanolid martynoside, though obtained in a rather small concentration, is of great chemotaxonomic significance, as this is the first phenylethanolid type glycoside isolated not only from the Salvia genus but also from the entire Subfamily Nepetoideae. As pheylethanolids are rather common and accumulate in significant concentrations in plants of the Subfamily Lamioideae, our opinion that the chemical differences between the two subfamilies are less qualititative than quantitative, is confirmed. This holds true of other chemical markers like monoterpenes, ursolic and oleanolic

  2. Comparative activity of some veterinary pharmaceutical products in swine dysentery

    Directory of Open Access Journals (Sweden)

    Cristina, T. Romeo

    2010-12-01

    after the treatment, no longer signs of illness being observed, all animals became normothermic. Weight gain recorded on our observation period was 29.3 kg/ lot which correspond to average daily gain of 162.7 g/day/animal.Group III, considered as control group, was at the beginning of the observation period, established with the average weight per lot, of 7.88 kg/head. In this series evolved enteritis with clear clinical manifestations (acute and subacute forms and during the experiment did not receive any treatment. Within this lot, in the studied period have died five piglets which represent 33.33% of the group. Consequently, to avoid the unnecessary losses, in the 21 day of experiment, the 10 remaining piglets were orally treated with tiamulin (60 mg/litre drinking water. Subsequent observations have shown gradual improvement and clinical remission to the remaining piglets. In the control group, practically can’t talk about a weight gain. After the 21 day average daily gain for animals remaining batch was 45.1 g/day/animal.Experiment IIThe groups were selected from age group 35-45 days, which are each, composed of 12 heads per group.Group I was treated with soluble granules tiamulin concentration of 45 mg of active substance per litre of drinking water. Treatment was performed over a period of 5 days. During the experiment, within this group there was one death case representing 8.33%. The remaining 12 piglets were cured within two weeks. Initial weight was of 92.9 kg/ group, and after 21 days of experiment, it reached at 98.9 kg, corresponding to an average daily gain of 101.5 g/head/day. Although, there was loss of a pig, average daily gain of piglets remaining was considered positive, the group recorded an increase of 6 kg in the 21 days of study.Group II received in drinking water, soluble tiamulin at concentration of 60 mg / litre for 5 consecutive days. In this group there was no mortality, all 12 piglets to heal within 10 days (cure rate 100%. The final

  3. [Effect of exogenous sucrose on growth and active ingredient content of licorice seedlings under salt stress conditions].

    Science.gov (United States)

    Liu, Fu-zhi; Yang, Jun

    2015-11-01

    Licorice seedlings were taken as experimental materials, an experiment was conducted to study the effects of exogenous sucrose on growth and active ingredient content of licorice seedlings under NaCl stress conditions. The results of this study showed that under salt stress conditions, after adding a certain concentration of exogenous sucrose, the licorice seedlings day of relative growth rate was increasing, and this stress can be a significant weakening effect, indicating that exogenous sucrose salt stress-relieving effect. The total flavonoids and phenylalanine ammonia lyase (PAL) activity were significantly increased, the exogenous sucrose can mitigated the seedling roots under salt stress, the licorice flavonoid content in the enhanced growth was largely due to the activity of PAL an increased, when the concentration of exogenous sucrose wae 10 mmol x L(-1), PAL activity reaching a maximum, when the concentration of exogenous sucrose was 15 mmol x L(-1), PAL activity turned into a downward trend, the results indicating that this mitigation has concentration effect. After applying different concentrations of exogenous sugar, the contents of liquiritin changes with the change of flavonoids content was similar. After applying different concentrations of exogenous sucrose, the content of licorice acid under salt stress was higher than the levels were not reached during salt stress, the impact of exogenous sucrose concentration gradient of licorice acid accumulation was not obvious.

  4. Application of chemical oxidation processes for the removal of pharmaceuticals in biologically treated wastewater

    OpenAIRE

    Hey, Gerly

    2013-01-01

    The discharge of effluents from wastewater treatment plants (WWTPs) is considered to be the major source of residual pharmaceuticals frequently found in aquatic environments. The complex nature of such compounds tends to make conventional biological treatments aimed at their removal ineffective. The present thesis concerns the removal of 62 different active pharmaceutical ingredients commonly detected in Swedish wastewater effluents by means of chemical oxidation techniques. Techniques wit...

  5. Studies on free-radical scavenging activity and identification of active ingredients of different plant crude extracts of Mentha piperita collected from Sur, Sultanate of Oman

    Institute of Scientific and Technical Information of China (English)

    Mohammad Amzad Hossain; Aqeela Said Hamed AL Orimi; Afaf Mohammed Weli; Qasim Al-Riyami; Jamal Nasser Al-Sabahi

    2014-01-01

    Objective: To determine free radical scavenging activity and active chemical ingredients of different plant crude extracts of Mentha piperita (M. piperita). Methods: The dried powder leaves of M. piperita were extracted with polar organic solvent by Soxhlet extractor. The crude extract and its fractions of hexane, chloroform, ethyl acetate and butanol crude extracts were prepared. The antioxidant activity of different crude extracts from M. piperita was carried out by DPPH method with minor modification, and the active chemical ingredients of different plant crude extracts of M. piperita were analyzed by gas chromatography-mass spectrometry (GC-MS). Results: Qualitative analysis of different polarities crude extracts by GC-MS found different types of active organic compounds. The antioxidant activity of different crude extracts were found to be in the order of chloroform extract> butanol extract> ethyl acetate extract> hexane extract>methanol extract. Majority identified compounds in the plant crude extracts by GC-MS were biologically active. Conclusions: Therefore, the isolation, purification, identification and characterization of bioactive compounds from various crude extracts of M. piperita might have ecological significance.

  6. Studies on free-radical scavenging activity and identification of active ingredients of different plant crude extracts of Mentha piperita collected from Sur, Sultanate of Oman

    Directory of Open Access Journals (Sweden)

    Mohammad Amzad Hossain

    2014-10-01

    Full Text Available Objective: To determine free radical scavenging activity and active chemical ingredients of different plant crude extracts of Mentha piperita (M. piperita. Methods: The dried powder leaves of M. piperita were extracted with polar organic solvent by Soxhlet extractor. The crude extract and its fractions of hexane, chloroform, ethyl acetate and butanol crude extracts were prepared. The antioxidant activity of different crude extracts from M. piperita was carried out by DPPH method with minor modification, and the active chemical ingredients of different plant crude extracts of M. piperita were analyzed by gas chromatographymass spectrometry (GC-MS. Results: Qualitative analysis of different polarities crude extracts by GC-MS found different types of active organic compounds. The antioxidant activity of different crude extracts were found to be in the order of chloroform extract> butanol extract> ethyl acetate extract> hexane extract> methanol extract. Majority identified compounds in the plant crude extracts by GC-MS were biologically active. Conclusions: Therefore, the isolation, purification, identification and characterization of bioactive compounds from various crude extracts of M. piperita might have ecological significance.

  7. Effects of Pharmaceuticals Used for Breast Cancer Treatment on Reproduction and Aromatase Activity in a Marine Fish

    Science.gov (United States)

    Laboratory experiments were conducted with the marine fish cunner (Tautogolabrus adspersus) to evaluate whether four pharmaceuticals used in breast cancer treatment have an impact on reproduction or aromatase activity. Tamoxifen binds to estrogen receptors, while anastrozole, let...

  8. Effects of Two Endocrine-active Pharmaceuticals, Tamoxifen and Anastrozole, on Reproduction in a Marine Fish, Tautogolabrus adspersus

    Science.gov (United States)

    Endocrine-active pharmaceuticals entering the aquatic environment through sewage effluent may have unintended, adverse impacts on the reproduction of aquatic organisms, which in turn may affect the sustainability of exposed populations. Laboratory experiments were conducted with ...

  9. 21 CFR 347.60 - Labeling of permitted combinations of active ingredients.

    Science.gov (United States)

    2010-04-01

    ... labeled for concurrent symptoms. (2) Combinations of skin protectant and first aid antiseptic active... § 347.50(b)(1), the required indications for first aid antiseptic drug products should be used....

  10. Risks of hormonally active pharmaceuticals to amphibians: a growing concern regarding progestagens.

    Science.gov (United States)

    Säfholm, Moa; Ribbenstedt, Anton; Fick, Jerker; Berg, Cecilia

    2014-11-19

    Most amphibians breed in water, including the terrestrial species, and may therefore be exposed to water-borne pharmaceuticals during critical phases of the reproductive cycle, i.e. sex differentiation and gamete maturation. The objectives of this paper were to (i) review available literature regarding adverse effects of hormonally active pharmaceuticals on amphibians, with special reference to environmentally relevant exposure levels and (ii) expand the knowledge on toxicity of progestagens in amphibians by determining effects of norethindrone (NET) and progesterone (P) exposure to 0, 1, 10 or 100 ng l(-1) (nominal) on oogenesis in the test species Xenopus tropicalis. Very little information was found on toxicity of environmentally relevant concentrations of pharmaceuticals on amphibians. Research has shown that environmental concentrations (1.8 ng l(-1)) of the pharmaceutical oestrogen ethinylestradiol (EE2) cause developmental reproductive toxicity involving impaired spermatogenesis in frogs. Recently, it was found that the progestagen levonorgestrel (LNG) inhibited oogenesis in frogs by interrupting the formation of vitellogenic oocytes at an environmentally relevant concentration (1.3 ng l(-1)). Results from the present study revealed that 1 ng NET l(-1) and 10 ng P l(-1) caused reduced proportions of vitellogenic oocytes and increased proportions of previtellogenic oocytes compared with the controls, thereby indicating inhibited vitellogenesis. Hence, the available literature shows that the oestrogen EE2 and the progestagens LNG, NET and P impair reproductive functions in amphibians at environmentally relevant exposure concentrations. The progestagens are of particular concern given their prevalence, the range of compounds and that several of them (LNG, NET and P) share the same target (oogenesis) at environmental exposure concentrations, indicating a risk for adverse effects on fertility in exposed wild amphibians.

  11. Active ingredients fatty acids as antibacterial agent from the brown algae Padina pavonica and Hormophysa triquetra

    Directory of Open Access Journals (Sweden)

    Gihan Ahmed El Shoubaky

    2014-07-01

    Full Text Available Objective: To estimate the fatty acids content in the brown algae Padina pavonica (P. pavonica and Hormophysa triquetra (H. triquetra and evaluate their potential antimicrobial activity as bioactive compounds. Methods: The fatty acid compositions of the examined species were analyzed using gas chromatography-mass spectrometry. The antimicrobial activity of crude and fatty acids was assessed using the agar plug technique. Results: The fatty acids profile ranged from C8:0 to C20:4. Concentration of saturated fatty acids in P. pavonica was in the order palmitic>myristic>stearic whereas concentration of the unsaturated fatty acids was oleic acid>palmitoleic>9-cis-hexadecenoic>linoleic acid>α- linolenic>arachidonic> elaidic acid. H. triquetra contained high concentration of saturated fatty acids than those of P. pavonica which was in the order as follows: palmitic>margaric>myristic> nonadecyclic>stearic>caprylic>tridecylic>pentadecylic>lauric while the unsaturated fatty acids consisted of oleic>nonadecenoic>non adecadienoate>margaroleic. The crude and fatty acid extracts of H. triquetra and P. pavonica were biologically active on the tested pathogens. H. triquetra exhibited a larger inhibitory zone than P. pavonica. Conclusions: The brown algae P. pavonica and H. triquetra have high efficient amount of fatty acids and showed strong antibacterial activity, especially H. triquetra.

  12. Active ingredients fatty acids as antibacterial agent from the brown algae Padina pavonica and Hormophysa triquetra

    Institute of Scientific and Technical Information of China (English)

    Gihan Ahmed El Shoubaky; Essam Abd El Rahman Salem

    2014-01-01

    Objective: To estimate the fatty acids content in the brown algae Padina pavonica (P. pavonica) and Hormophysa triquetra (H. triquetra) and evaluate their potential antimicrobial activity as bioactive compounds.Methods:The fatty acid compositions of the examined species were analyzed using gas chromatography-mass spectrometry. The antimicrobial activity of crude and fatty acids was assessed using the agar plug technique.Results:The fatty acids profile ranged from C8:0 to C20:4. Concentration of saturated fatty acids in P. pavonica was in the order palmitic>myristic>stearic whereas concentration of the unsaturated fatty acids was oleic acid>palmitoleic>9-cis-hexadecenoic>linoleic acid>α-linolenic>arachidonic> elaidic acid. H. triquetra contained high concentration of saturated fatty acids than those of P. pavonica which was in the order as follows: palmitic>margaric>myristic>nonadecyclic>stearic>caprylic>tridecylic>pentadecylic>lauric while the unsaturated fatty acids consisted of oleic>nonadecenoic>non adecadienoate>margaroleic. The crude and fatty acid extracts of H. triquetra and P. pavonica were biologically active on the tested pathogens. H.triquetra exhibited a larger inhibitory zone than P. pavonica. Conclusions: The brown algae P. pavonica and H. triquetra have high efficient amount of fatty acids and showed strong antibacterial activity, especially H. triquetra.

  13. Intrinsic Motivation and Engagement as "Active Ingredients" in Garden-Based Education: Examining Models and Measures Derived from Self-Determination Theory

    Science.gov (United States)

    Skinner, Ellen A.; Chi, Una

    2012-01-01

    Building on self-determination theory, this study presents a model of intrinsic motivation and engagement as "active ingredients" in garden-based education. The model was used to create reliable and valid measures of key constructs, and to guide the empirical exploration of motivational processes in garden-based learning. Teacher- and…

  14. Genotoxic Potential of Two Herbicides and their Active Ingredients Assessed with Comet Assay on a Fish Cell Line, Epithelioma Papillosum Cyprini (EPC)

    DEFF Research Database (Denmark)

    Syberg, Kristian; Rank, Jette; Jensen, Klara;

    2013-01-01

    that avoiding trypsin to detach cells led to lower level of DNA damage in the negative control. Further, two commonly used herbicides (Dezormon and Optica trio) and their four active ingredients (4-chloro-o-tolyloxyacetic acid, 2,4-dichlorophenoxyacetic acid, 2-(4-chloro-2-methylphenoxy)propionic acid, 2...

  15. Attractive toxic sugar baits: Control of mosquitoes with the low risk active ingredient dinotefuran and potential impacts on non-target organisms in Morocco

    Science.gov (United States)

    We evaluated the efficacy of ATSB in the laboratory and the field with the low risk active ingredient dinotefuran against mosquito populations. Assays indicated that dinotefuran in solution with the sugar baits was ingested and resulted in high mortality of female Culex quinquefasciatus and Aedes a...

  16. Understanding the Active Ingredients in an Effective Preschool Vocabulary Intervention: An Exploratory Study of Teacher and Child Talk during Book Reading

    Science.gov (United States)

    Wasik, Barbara A.; Hindman, Annemarie H.

    2014-01-01

    Research Findings: In order to identify the active ingredients in an effective professional development intervention focused on enhancing preschool vocabulary instruction, this study examines the frequency with which teachers and children discussed theme-related vocabulary words during shared book reading. Head Start teachers received 1 year of…

  17. Efficacy of attractive toxic sugar baits (ATSB) against Aedes albopictus with garlic oil encapsulated in beta-Cyclodextrin as the active ingredient

    Science.gov (United States)

    We tested the efficacy of attractive toxic sugar bait (ATSB) with garlic oil microencapsulated in beta-cyclodextrin as active ingredient against Aedes albopictus in suburban Haifa, Israel. Two three-acre gardens with high numbers of Ae. albopictus were chosen for perimeter spray treatment with ATSB ...

  18. The possibilities of using essential oils as an active ingredients or preservatives in cosmetic products

    OpenAIRE

    Adaszy?ska, Michalina; Swarcewicz, Maria

    2011-01-01

    An important trend in the development of the cosmetics industry is searching for new biologically active, natural compounds and preservative systems, which will find application in the natural cosmetics production. Natural cosmetics are of considerable interest nowadays and essential oils could be employed in theirs production. The huge potential of essential oils indicates the possibility of applying them in practice because of theirs antibacterial, antiseptic, antifungal, and antioxidant...

  19. Widespread occurrence of neuro-active pharmaceuticals and metabolites in 24 Minnesota rivers and wastewaters

    Science.gov (United States)

    Writer, Jeffrey; Ferrer, Imma; Barber, Larry B.; Thurman, E. Michael

    2013-01-01

    Concentrations of 17 neuro-active pharmaceuticals and their major metabolites (bupropion, hydroxy-bupropion, erythro-hydrobupropion, threo-hydrobupropion, carbamazepine, 10,11,-dihydro-10,11,-dihydroxycarbamazepine, 10-hydroxy-carbamazepine, citalopram, N-desmethyl-citalopram, fluoxetine, norfluoxetine, gabapentin, lamotrigine, 2-N-glucuronide-lamotrigine, oxcarbazepine, venlafaxine and O-desmethyl-venlafaxine), were measured in treated wastewater and receiving surface waters from 24 locations across Minnesota, USA. The analysis of upstream and downstream sampling sites indicated that the wastewater treatment plants were the major source of the neuro-active pharmaceuticals and associated metabolites in surface waters of Minnesota. Concentrations of parent compound and the associated metabolite varied substantially between treatment plants (concentrations ± standard deviation of the parent compound relative to its major metabolite) as illustrated by the following examples; bupropion and hydrobupropion 700 ± 1000 ng L−1, 2100 ± 1700 ng L−1, carbamazepine and 10-hydroxy-carbamazepine 480 ± 380 ng L−1, 360 ± 400 ng L−1, venlafaxine and O-desmethyl-venlafaxine 1400 ± 1300 ng L−1, 1800 ± 2300 ng L−1. Metabolites of the neuro-active compounds were commonly found at higher or comparable concentrations to the parent compounds in wastewater effluent and the receiving surface water. Neuro-active pharmaceuticals and associated metabolites were detected only sporadically in samples upstream from the effluent outfall. Metabolite to parent ratios were used to evaluate transformation, and we determined that ratios in wastewater were much lower than those reported in urine, indicating that the metabolites are relatively more labile than the parent compounds in the treatment plants and in receiving waters. The widespread occurrence of neuro-active pharmaceuticals and metabolites in Minnesota effluents and surface waters indicate that

  20. Diffusion of active ingredients in textiles: a three step multiscale model

    OpenAIRE

    Goessens, Tineke; Malengier, Benny; Li, Pei; De Staelen, Rob H.

    2013-01-01

    Most practical textile models are based on a two scale approach: a one-dimensional fiber model and a fabric model. No meso-level is used in between, i.e. the yarn scale is neglected in this setup. For dense textile substrates this seems appropriate as the yarns connect everywhere, but for loose fabrics or scrims this approach cannot be kept. Specifically when one is interested in tracking an active component released by the fibers, the yarn level plays an important role. This is because the satu...

  1. Identification of Major Active Ingredients Responsible for Burn Wound Healing of Centella asiatica Herbs

    Directory of Open Access Journals (Sweden)

    Fang Wu

    2012-01-01

    Full Text Available Centella asiatica herbs have been prescribed as a traditional medicine for wound healing in China and Southeast Asia for a long time. They contain many kinds of triterpenoid compounds, mainly including glycosides (asiaticoside and madecassoside and corresponding aglycones (asiatic acid and madecassic acid. To identify which is the major active constituent, a comprehensive and comparative study of these compounds was performed. In vitro, primary human skin fibroblasts, originating from healthy human foreskin samples, were treated with various concentrations of asiaticoside, madecassoside, asiatic acid, and madecassic acid, respectively. Cell proliferation, collagen synthesis, MMP-1/TIMP-1 balance, and TGF-β/Smad signaling pathway were investigated. In vivo, mice were orally administered with the four compounds mentioned above for two weeks after burn injury. The speed and quality of wound healing, as well as TGF-β1 levels in skin tissues, were examined. Interestingly, in contrast to prevalent postulations, asiaticoside and madecassoside themselves, rather than their corresponding metabolites asiatic acid and madecassic acid, are recognized as the main active constituents of C. asiatica herbs responsible for burn wound healing. Furthermore, madecassoside is more effective than asiaticoside (P=0.0446 for procollagen type III synthesis in vitro, P=0.0057 for wound healing speed, and P=0.0491 for wound healing pattern in vivo, correspondingly.

  2. Piperine, an active ingredient of black pepper attenuates acetaminophen-induced hepatotoxicity in mice

    Institute of Scientific and Technical Information of China (English)

    Evan Prince Sabina; Annie Deborah Harris Souriyan; Deborah Jackline; Mahaboob Khan Rasool

    2010-01-01

    Objective: To explore the hepatoprotective and antioxidant effects of piperine against acetaminophen-induced hepatotoxicity in mice. Methods: In mice, hepatotoxicity was induced by a single dose of acetaminophen (900 mg/kg b.w. i.p.). Piperine (25 mg/kg b.w. i.p.) and standard drug silymarin (25 mg/kg b.w. i.p.) were given to mice, 30 min after the single injection of acetaminophen. After 4 h, the mice were decapitated. Activities of liver marker enzymes [(aspartate transaminase (AST), alanine transaminase (ALT), and alkaline phosphatase (ALP)] and inflammatory mediator tumour necrosis factor-alpha (TNF-α) were estimated in serum, while lipid peroxidation and antioxidant status (superoxide dismutase, catalase, glutathione peroxidase, glutathione reductase, glutathione-s-transferase and glutathione) were determined in liver homogenate of control and experimental mice. Results: Acetaminophen induction (900 mg/kg b.w. i.p.) significantly increased the levels of liver marker enzymes, TNF-α, and lipid peroxidation, and caused the depletion of antioxidant status. Piperine and silymarin treatment to acetaminophen challenged mice resulted in decreased liver marker enzymes activity, TNF-α and lipid peroxidation levels with increase in antioxidant status. Conclusions: The results clearly demonstrate that piperine shows promising hepatoprotective effect as comparable to standard drug silymarin.

  3. Determination of antioxidant activity in herbal ingredients for foods using new methods of chemical analysis

    Directory of Open Access Journals (Sweden)

    Katalina Muñoz

    2012-06-01

    Full Text Available A new procedure has been used to separate and quantify the free radical-scavenging activity of individual compounds 18 samples of Thymus vulgaris and 12 samples of Rosmarinus officinalis (both used as natural food preservatives, based on the combination of HPTLC (High Performance Thin Layer Chromatography and postchromatographic DPPH● radical derivatization. The compounds thymol and rosmarinic acid in T. vulgaris and R. officinalis, respectively, were identified by comparisons of their Rf values and UV spectra to standards analyzed under identical analytical conditions, while the quantitative data were calculated from their calibration curves. We found that not only that the biomass yield but also the metabolite content in herbs, depend on the ecotype (genetics and on the agro ecological conditions. The effect of the ambient on the metabolite content is extremely significant and also on their antioxidant activity (One-way ANOVA with Newman-Keuls Multiple Comparison post test was performed using GraphPad Prism version 4.00 for Windows, GraphPad Software. This work pretends to demonstrate the great importance of using new technologies for the selection of the best materials used as natural food preservatives.

  4. Ibuprofen-in-cyclodextrin-in-W/O/W emulsion - Improving the initial and long-term encapsulation efficiency of a model active ingredient.

    Science.gov (United States)

    Hattrem, Magnus N; Kristiansen, Kåre A; Aachmann, Finn L; Dille, Morten J; Draget, Kurt I

    2015-06-20

    A challenge in formulating water-in-oil-in-water (W/O/W) emulsions is the uncontrolled release of the encapsulated compound prior to application. Pharmaceuticals and nutraceuticals usually have amphipathic nature, which may contribute to leakage of the active ingredient. In the present study, cyclodextrins (CyDs) were used to impart a change in the relative polarity and size of a model compound (ibuprofen) by the formation of inclusion complexes. Various inclusion complexes (2-hydroxypropyl (HP)-β-CyD-, α-CyD- and γ-CyD-ibuprofen) were prepared and presented within W/O/W emulsions, and the initial and long-term encapsulation efficiency was investigated. HP-β-CyD-ibuprofen provided the highest encapsulation of ibuprofen in comparison to a W/O/W emulsion with unassociated ibuprofen confined within the inner water phase, with a four-fold increase in the encapsulation efficiency. An improved, although lower, encapsulation efficiency was obtained for the inclusion complex γ-CyD-ibuprofen in comparison to HP-β-CyD-ibuprofen, whereas α-CyD-ibuprofen had a similar encapsulation efficiency to that of unassociated ibuprofen. The lower encapsulation efficiency of ibuprofen in combination with α-CyD and γ-CyD was attributed to a lower association constant for the γ-CyD-ibuprofen inclusion complex and the ability of α-CyD to form inclusion complexes with fatty acids. For the W/O/W emulsion prepared with HP-β-CyD-ibuprofen, the highest encapsulation of ibuprofen was obtained at hyper- and iso-osmotic conditions and by using an excess molar ratio of CyD to ibuprofen. In the last part of the study, it was suggested that the chemical modification of the HP-β-CyD molecule did not influence the encapsulation of ibuprofen, as a similar encapsulation efficiency was obtained for an inclusion complex prepared with mono-1-glucose-β-CyD.

  5. Evaluation of Fenton's Reagent and Activated Persulfate for Treatment of a Pharmaceutical Waste Mixture in Groundwater

    DEFF Research Database (Denmark)

    Bennedsen, Lars Rønn; Søgaard, Erik Gydesen; Kakarla, Prasad;

    Groundwater beneath the Kærgård Plantage megasite in Denmark are contaminated with a complex mixtu of pharmaceutical wastes, including sulfonamides, barbiturates, aniline, pyridine chlorinated solvents, mercury, and cyanide.  Regulatory agencies in Denmark are now in the process of evaluating...... is to identify the fate of mercury and cyanide consequent to the application of Fenton's reagent and activated persulfate.  Batch and continuous-flow column reactors will be used to measure mobilization of the mercury, cyanide and other metals both within the aqueous and vapor phases.   The collective chemical...

  6. 槟榔十三味丸(高尤-13)对慢性应激抑郁大鼠行为学及海马神经元凋亡的影响%Effects of Mongolian Pharmaceutical Betel Shisanwei Ingredients Pill on Behavior and APoPtosis of HiPPocamPal Cells in DePressive Rats

    Institute of Scientific and Technical Information of China (English)

    乌吉斯古冷; 佟海英; 斯日古楞; 白亮凤; 包伍叶; 胡日乐巴根; 李婧; 张月

    2014-01-01

    Objective:To study the effect of Mongolian Pharmaceutical Betel Shisanwei Ingredients Pill on behavior and apoptosis of hipp-ocampal cells in depressive rats and from the cell level to discuss antidepressant mechanism. Methods:48 male Wistar rats were random-ly divided into six groups according to the sugar consumption test and body weight(8 rats in each group):normal control group,model group,Fluoxetine group(3. 3 mg·kg - 1 )and high,medium and low dose group(0. 25,0. 5,1. 0 g·kg - 1 )of Betel Shisanwei ingredi-ents Pill. Except the normal control,the other groups were treated with the chronic unpredictable mild stress stimulation combined with lonely raising. Intragastric administration,once daily,continuously for 28 days. Behavior changes of rats were detected through open?field test,and sugar consumption test were also measured by AnnexinV - FITC/ PI double labeling. Flow Cytometer was used to detect the apoptotic rats in the hippocampus. Results:Compared with normal control group,the scores of horizontal activity and vertical activi-ty,weight and sugar consumption group decreased significantly(P < 0. 01);Compared with model group,Fluoxetine group and Betel Shisanwei Ingredients Pill medium,high dose group got significantly higher scores of horizontal activity and vertical activity,weight and sugar consumption(P < 0. 05). Flow Cytometer results show that compared with normal control group,model group rats hippocampal ap-optosis rate was significantly higher(P < 0. 05);Compared with model group,fluoxetine group,Betel Shisanwei ingredients pills medi-um,high dose group of rat hippocampal apoptosis rate is reduced,with decreased significantly(P < 0. 01). Conclusion:Chronic stress depression model rats exists abnormal behavior and hippocampus apoptosis phenomenon,Betel Shisanwei Ingredients pill can improve depression model rats abnormal behavior and inhibit apoptosis of rat hippocampal caused by chronic stress and play a role of antidepres-sant.%目的:观

  7. Ginkgo biloba extracts: a review of the pharmacokinetics of the active ingredients.

    Science.gov (United States)

    Ude, Christian; Schubert-Zsilavecz, Manfred; Wurglics, Mario

    2013-09-01

    Ginkgo biloba is among the most favourite and best explored herbal drugs. Standardized extracts of Ginkgo biloba represent the only herbal alternative to synthetic antidementia drugs in the therapy of cognitive decline and Alzheimer's diseases. The clinical efficiency of such standardized Ginkgo biloba extracts (GBE) is still controversial, but authors of numerous international clinical studies recommended the use of GBE in the described therapies.Extracts of Ginkgo biloba are a mixture of substances with a wide variety of physical and chemical properties and activities. Numerous pharmacological investigations lead to the conclusion that the terpene trilactones (TTL) and the flavonoids of GBE are responsible for the main pharmacological effects of the extract in the therapy of cognitive decline. Therefore, the quality of GBE products must be oriented on a defined quantity of TTL and flavonoids. Furthermore, because of their toxic potential the amount of ginkgolic acid should be less than 5 ppm.However, data on pharmacokinetics and bioavailability, especially related to the central nervous system (CNS), which is the target tissue, are relatively rare. A few investigations characterize the TTL and flavonoids of Ginkgo biloba pharmacokinetically in plasma and in the brain. Recent investigations show that significant levels of TTL and Ginkgo biloba flavonoids cross the blood-brain barrier and enter the CNS of rats after oral application of GBE. Knowledge about the pharmacokinetic behaviour of these substances is necessary to discuss the pharmacological results on a more realistic basis.

  8. Application of the KeratinoSens™ assay for assessing the skin sensitization potential of agrochemical active ingredients and formulations.

    Science.gov (United States)

    Settivari, Raja S; Gehen, Sean C; Amado, Ricardo Acosta; Visconti, Nicolo R; Boverhof, Darrell R; Carney, Edward W

    2015-07-01

    Assessment of skin sensitization potential is an important component of the safety evaluation process for agrochemical products. Recently, non-animal approaches including the KeratinoSens™ assay have been developed for predicting skin sensitization potential. Assessing the utility of the KeratinoSens™ assay for use with multi-component mixtures such as agrochemical formulations has not been previously evaluated and is a significant need. This study was undertaken to evaluate the KeratinoSens™ assay prediction potential for agrochemical formulations. The assay was conducted for 8 agrochemical active ingredients (AIs) including 3 sensitizers (acetochlor, meptyldinocap, triclopyr), 5 non-sensitizers (aminopyralid, clopyralid, florasulam, methoxyfenozide, oxyfluorfen) and 10 formulations for which in vivo sensitization data were available. The KeratinoSens™ correctly predicted the sensitization potential of all the AIs. For agrochemical formulations it was necessary to modify the standard assay procedure whereby the formulation was assumed to have a common molecular weight. The resultant approach correctly predicted the sensitization potential for 3 of 4 sensitizing formulations and all 6 non-sensitizing formulations when compared to in vivo data. Only the meptyldinocap-containing formulation was misclassified, as a result of high cytotoxicity. These results demonstrate the promising utility of the KeratinoSens™ assay for evaluating the skin sensitization potential of agrochemical AIs and formulations. PMID:25981449

  9. Pharmaceutically active compounds in sludge stabilization treatments: anaerobic and aerobic digestion, wastewater stabilization ponds and composting.

    Science.gov (United States)

    Martín, Julia; Santos, Juan Luis; Aparicio, Irene; Alonso, Esteban

    2015-01-15

    Sewage sludge disposal onto lands has been stabilized previously but still many pollutants are not efficiently removed. Special interest has been focused on pharmaceutical compounds due to their potential ecotoxicological effects. Nowadays, there is scarce information about their occurrence in different sludge stabilization treatments. In this work, the occurrence of twenty-two pharmaceutically active compounds has been studied in sludge from four sludge stabilization treatments: anaerobic digestion, aerobic digestion, composting and lagooning. The types of sludge evaluated were primary, secondary, anaerobically-digested and dehydrated, composted, mixed, aerobically-digested and dehydrated and lagoon sludge. Nineteen of the twenty-two pharmaceutically active compounds monitored were detected in sewage sludge. The most contaminated samples were primary sludge, secondary sludge and mixed sludge (the average concentrations of studied compounds in these sludges were 179, 310 and 142 μg/kg dm, respectively) while the mean concentrations found in the other types of sewage sludge were 70 μg/kg dm (aerobically-digested sludge), 63 μg/kg dm (lagoon sludge), 12 μg/kg dm (composted sludge) and 8 μg/kg dm (anaerobically-digested sludge). The antibiotics ciprofloxacin and norfloxacin were found at the highest concentration levels in most of the analyzed sludge samples (up to 2660 and 4328 μg/kg dm, respectively). Anaerobic-digestion treatment reduced more considerably the concentration of most of the studied compounds than aerobic-digestion (especially in the case of bezafibrate and fluoroquinolones) and more than anaerobic stabilization ponds (in the case of acetaminophen, atenolol, bezafibrate, carbamazepine, 17α-ethinylestradiol, naproxen and salicylic acid). Ecotoxicological risk assessment, of sludge application onto soils, has also been evaluated. Risk quotients, expressed as the ratio between the predicted environmental concentration and the predicted non

  10. Elemental characterization of marijuana (cannabis sativa) as a stride in the isolation of its active ingredients

    International Nuclear Information System (INIS)

    Seed, stem and leaves samples of Marijuana (Cannabis sativa) popularly called Indian Hemp available in northern Nigeria were analyzed for trace amounts of Mg, Al, Ca, Ti, Mn, Na, Br, La, Yb, Cr, Fe, Zn, and Ba using Instrumental Neutron Activation Analysis. Sample sizes of roughly 300mg irradiated for five minutes (short irradiation) and six hours (long irradiation), with decay times of 7 minutes, 10,000 minutes and 26,000 minutes for short, medium and long-lived nuclides respectively. Counting times for ten minutes (short-lived nuclides), 1,800 minutes (medium-lived nuclides) and 36,000 minutes (long-lived nuclides) yielded detection limits between 0.05 - 0.09μg/g. For comparative study, refined tobacco produced by a tobacco company operating in northern Nigeria were characterized together with the marijuana-which is usually smoked raw with leaves stem and seed packed together. The results obtained shows that both the refined tobacco and the raw marijuana have high c oncentration of Ca, Mg, Al and Mn and low values of Na, Br and La. However, marijuana was found to have heavy elements in abundance compared to the refined tobacco, with Zn = 20.5 μg/g and Cr = 14.3μg/g recording the highest values among the heavy elements detected. This is a sharp difference between the two since the values of heavy elements obtained for the refined tobacco are even below detection limits. Quality Control and Quality Assurance was tested using certified reference material obtained from NIST (Tomato Leaves).

  11. Khaya grandifoliola C.DC: a potential source of active ingredients against hepatitis C virus in vitro.

    Science.gov (United States)

    Galani, Borris Rosnay Tietcheu; Sahuc, Marie-Emmanuelle; Sass, Gabriele; Njayou, Frédéric Nico; Loscher, Christine; Mkounga, Pierre; Deloison, Gaspard; Brodin, Priscille; Rouillé, Yves; Tiegs, Gisa; Séron, Karin; Moundipa, Paul Fewou

    2016-05-01

    In this study, we examined the antiviral properties of Khaya grandifoliola C.DC (Meliaceae) on the hepatitis C virus (HCV) life cycle in vitro and identified some of the chemical constituents contained in the fraction with the most antiviral activity. Dried bark powder was extracted by maceration in a methylene chloride/methanol (MCM) system (50:50; v/v) and separated on silica gel by flash chromatography. Infection and replication rates in Huh-7 cells were investigated by luciferase reporter assay and indirect immunofluorescence assay using subgenomic replicons, HCV pseudotyped particles, and cell-culture-derived HCV (HCVcc), respectively. Cell viability was assessed by MTT assay, and cellular gene expression was analysed by qRT-PCR. The chemical composition of the fraction with the most antiviral activity was analysed by coupled gas chromatography and mass spectrometry (GC-MS). Five fractions of different polarities (F0-F100) were obtained from the MCM extract. One fraction (KgF25) showed the strongest antiviral effect on LucUbiNeoET replicons at nontoxic concentrations. Tested at 100 µg/mL, KgF25 had a high inhibitory effect on HCV replication, comparable to that of 0.01 µM daclatasvir or 1 µM telaprevir. This fraction also inhibited HCVcc infection by mostly targeting the entry step. KgF25 inhibited HCV entry in a pan-genotypic manner by directly inactivating free viral particles. Its antiviral effects were mediated by the transcriptional upregulation of the haem oxygenase-1 gene and interferon antiviral response. Three constituents, namely, benzene, 1,1'-(oxydiethylidene)bis (1), carbamic acid, (4-methylphenyl)-, 1-phenyl (2), and 6-phenyl, 4-(1'-oxyethylphenyl) hexene (3), were identified from the active fraction KgF25 by GC-MS. Khaya grandifoliola contains ingredients capable of acting on different steps of the HCV life cycle. PMID:26843184

  12. Importance and globalization status of good manufacturing practice (GMP) requirements for pharmaceutical excipients.

    Science.gov (United States)

    Abdellah, Abubaker; Noordin, Mohamed Ibrahim; Wan Ismail, Wan Azman

    2015-01-01

    Pharmaceutical excipients are no longer inert materials but it is effective and able to improve the characteristics of the products' quality, stability, functionality, safety, solubility and acceptance of patients. It can interact with the active ingredients and alter the medicament characteristics. The globalization of medicines' supply enhances the importance of globalized good manufacturing practice (GMP) requirements for pharmaceutical excipients. This review was intended to assess the globalization status of good manufacturing practice (GMP) requirements for pharmaceutical excipients. The review outcomes demonstrate that there is a lack of accurately defined methods to evaluate and measure excipients' safety. Furthermore good manufacturing practice requirements for excipients are not effectively globalized.

  13. 蒿属植物的农药活性及其有效成分%Pesticidal Activities and Active Ingredients of Artemisia

    Institute of Scientific and Technical Information of China (English)

    周利娟; 桑晓清; 孙永艳; 杨文杰

    2012-01-01

    Recent studies on pesticidal activities and the corresponding active ingredients of Artemisia are presented. Artemisia annua, Artemisia lavandulaefolia, Artemisia absinthium, Artemisia selengensis, Artemisia vestita, Artemisia parvijlora, Artemisia sieversiana, Artemisia scoparia, Artemisia capillarie, Artemisia mongoli-ca, Artemisia borealis, Artemisia nilagirica, Artemisia monosperma and Artemisia judaica possess insecticidal activities and the main active ingredients are cineole, borneol, camphor, caryophyllene, isoaryophyllene and farnesene. Artemisia annua, Artemisia ludoviciana, Artemisia tournefortiana, Artemisia absinthium, Artemisia herba alba, Artemisia taurica, Artemisia judaica, Artemisia borealis, Artemisia molinieri, Artemisia stolonifera show fungicidal activities and the main active ingredients are camphor, cineole, borneol, flavonoids, olefins, terpene hydrocarbons, alkanes and organic acids. Artemisia caerulescens subsp. gallica, Artemisia ordosica, Artemisia roxburghiana,Artenisia annua, Artemisia tridentate, Artemisia scoparia and Artemisia taurica exhibit herbicide activities and the main active ingredients are cineole, camphor, arteether, monoterpenes and ses-quiterpenes. Artemisia absinthium shows nematicidal activity. Artemisia absinthium and Artemisia dracunculus have mollusicidal activities. In all, Artemisia annua, Artemisia absinthium, Artemisia borealis and Artemisia judaica show multiple activities and may be used as botanical pesticides.%综述了蒿属植物的杀虫、杀螨、杀菌、除草、杀线虫和杀软体动物活性及相应的有效成分.该属中具有杀虫杀螨活性的主要有黄花蒿、野艾蒿、苦艾、蒌蒿、毛莲蒿、西南牡蒿、大籽蒿、猪毛蒿、茵陈蒿、蒙古蒿、巴儿古津蒿、南亚蒿、犹地蒿和Artemisia monsperma等,其主要有效成分是桉树脑、龙脑、樟脑、石竹烯、异石竹烯和β-法呢烯等.该属中具有杀菌活性的主要有黄花蒿、银叶艾蒿

  14. Alkaloids in the pharmaceutical industry: Structure, isolation and application

    OpenAIRE

    Nikolić Milan; Đorđević Siniša M.

    2003-01-01

    By the end of the 18th and the beginning of the 19th century a new era began in medicine, pharmaceutics and chemistry that was strongly connected with alkaloids and alkaloid drugs. Even before that it was known that certain drugs administered in limited doses were medicines, and toxic if taken in larger doses (opium, coke leaves, belladonna roots, monkshood tubers crocus or hemlock seeds). However, the identification, isolation and structural characterization of the active ingredients of the ...

  15. Pharmaceutical aerosols. Study of their gamma radiation sterilization

    International Nuclear Information System (INIS)

    The gamma radiation sterilization of pharmaceutical aerosols was studied. The following topics were investigated: radiosterilization of nitrogen protoxide used as a propellant; radiosterilization of packaging materials (aluminium containers, plastics valves); radio-sterilization of excipients and active ingredients. Most of the investigated materials proved to be stable to irradiation (2,5 Mrads) from pharmacopoeial aspect. Stability tests of the preparations packaged showed no change in the parameters investigated

  16. THE EFFECT OF DIFFERENT DOSES OF NITROGEN (N) APPLICATION ON THE ANTIOXIDANT ACTIVITY AND PHENOLIC MATERIAL INGREDIENT OF SORREL (RUMEX ACETOSA L.)

    OpenAIRE

    Adiloğlu, Sevinç; Açıkgöz, Funda Eryılmaz; Dağlıoğlu, Figen; Barut Gök, Sıla; Altan, Deniz Damla

    2015-01-01

    In this study, The effect of different doses of nitrogen (N) application on the antioxidant activity and phenolic material ingredient of sorrel (Rumex acetosa L.) are investigated. In the test, four various doses of nitrogen NH4NO3 fertilizer have been applied to the plants. As a result, it has been determined that the antioxidant activity and phenolic compounds of Sorrel (Rumex acetosa L.) have parallels with the increase in the application of nitrogen.

  17. Rosmarinus officinalis L. extract and some of its active ingredients as potential emulsion stabilizers: a new approach to the formation of multiple (W/O/W) emulsion.

    Science.gov (United States)

    Cizauskaite, Ugne; Ivanauskas, Liudas; Jakštas, Valdas; Marksiene, Ruta; Jonaitiene, Laimute; Bernatoniene, Jurga

    2016-09-01

    Nowadays, novel topical formulations loaded with natural functional actives are under intense investigations. Therefore, the aim of our study was to evaluate how the rosemary extract and some of its active ingredients [rosmarinic acid (RA), ursolic acid (UA) and oleanolic acid (OA)] affect technological characteristics of multiple emulsion. Formulation has been prepared by adding investigated solutions (10%) in water/oil/water (W/O/W) multiple emulsion consisting of different lipophilic phases: olive oil and liquid paraffin, with 0.5% emulsifying agent (complex of sodium polyacrylate and polysorbate 20) under constant stirring with mechanical stirrer at room temperature. The emulsion parameters were evaluated using centrifugation test, freeze-thaw cycle test, microscopical and texture analyses. Rosemary's triterpenic saponins UA and OA showed the highest emulsion stabilizing properties: they decreased CI from 3.26% to 10.23% (p rosemary active ingredients is not surfactant-like. Even though emulsifier itself at low concentration intends to form directly the multiple emulsion, the obtained results indicate that rosemary extract containing active ingredients does not only serve as functional cosmetic agent due to a number of biological activities, but also offer potential advantages as a stabilizer and an enhancer of W/O/W emulsions formation for dermopharmaceutical and cosmetic preparations. PMID:26000558

  18. Fusion production of solid dispersions containing a heat-sensitive active ingredient by hot melt extrusion and Kinetisol dispersing.

    Science.gov (United States)

    Dinunzio, James C; Brough, Chris; Hughey, Justin R; Miller, Dave A; Williams, Robert O; McGinity, James W

    2010-02-01

    Many techniques for the production of solid dispersions rely on elevated temperatures and prolonged material residence times, which can result in decomposition of temperature-sensitive components. In this study, hydrocortisone was used as a model temperature-sensitive active ingredient to study the effect of formulation and processing techniques as well as to characterize the benefits of KinetiSol Dispersing for the production of solid dispersions. Preformulation studies were conducted using differential scanning calorimetry and hot stage microscopy to identify optimum carriers for the production of amorphous solid dispersions. After identification, solid dispersions were prepared by hot melt extrusion and KinetiSol Dispersing, with material characterized by X-ray diffraction, dissolution and potency testing to evaluate physicochemical properties. Results from the preformulation studies showed that vinylacetate:vinylpyrrolidone (PVPVA) copolymer allowed for hydrocortisone dissolution within the carrier at temperatures as low as 160 degrees C, while hydroxypropyl methylcellulose required temperatures upward of 180 degrees C to facilitate solubilization. Low substituted hydroxypropyl cellulose, a high glass transition temperature control, showed that the material was unable to solubilize hydrocortisone. Manufacturing process control studies using hot melt extruded compositions of hydrocortisone and PVPVA showed that increased temperatures and residence times negatively impacted product potency due to decomposition. Using KinetiSol Dispersing to reduce residence time and to facilitate lower temperature processing, it was possible to produce solid dispersions with improved product potency. This study clearly demonstrated the importance of carrier selection to facilitate lower temperature processing, as well as the effect of residence time on product potency. Furthermore, KinetiSol Dispersing provided significant advantages over hot melt extrusion due to the reduced

  19. A target analogue imprinted polymer for the recognition of antiplatelet active ingredients in Radix Salviae Miltiorrhizae by LC/MS/MS.

    Science.gov (United States)

    Huang, Meixia; Pang, Wensheng; Zhang, Jing; Lin, Siding; Hu, Juan

    2012-01-25

    The purpose of this study was to prepare a propyl gallate (PrG) molecular imprinted polymer as a cartridge stuffing material to isolate antiplatelet active ingredients. A macroporous polymer was synthesized utilizing ethylene glycol dimethacrylate (EDMA) as the crosslinking agent, PrG as the template molecule and 4-vinylpyridine (4-Vpy) as the functional monomer. Subsequently, PrG was removed by washing with methanol-glacial acetic acid (9:1, v/v). The molecular imprinted polymer recognized an active ingredient, protocatechuic acid, from a crude extract of the Chinese herbal medicine, Radix Salviae Miltiorrhizae (Danshen), using an on-line column switching solid phase extraction process. Pharmacological experiments showed that protocatechuic acid inhibits arachidonic acid (10 mg/kg) induced aggregation of rat platelets in vivo. This study provides an example of an application of separation-analysis technique for screening potentially bioactive compounds. PMID:21978827

  20. 21 CFR 310.540 - Drug products containing active ingredients offered over-the-counter (OTC) for use as stomach...

    Science.gov (United States)

    2010-04-01

    ... offered over-the-counter (OTC) for use as stomach acidifiers. 310.540 Section 310.540 Food and Drugs FOOD... ingredients offered over-the-counter (OTC) for use as stomach acidifiers. (a) Betaine hydrochloride, glutamic...-counter (OTC) drug products for use as stomach acidifiers. Because of the lack of adequate data...

  1. Assessing the diurnal variability of pharmaceutical and personal care products in a full-scale activated sludge plant

    Energy Technology Data Exchange (ETDEWEB)

    Salgado, R. [REQUIMTE/CQFB, Chemistry Department, FCT, Universidade Nova de Lisboa, 2829-516 Caparica (Portugal); ESTS-IPS, Escola Superior de Tecnologia de Setubal do Instituto Politecnico de Setubal, Rua Vale de Chaves, Campus do IPS, Estefanilha, 2910-761 Setubal (Portugal); Marques, R. [REQUIMTE/CQFB, Chemistry Department, FCT, Universidade Nova de Lisboa, 2829-516 Caparica (Portugal); Instituto de Biologia Experimental e Tecnologica (IBET), Av. da Republica (EAN), 2784-505 Oeiras (Portugal); Noronha, J.P. [REQUIMTE/CQFB, Chemistry Department, FCT, Universidade Nova de Lisboa, 2829-516 Caparica (Portugal); Mexia, J.T. [Center of Mathematic Applications, Mathematics Department, FCT, Universidade Nova de Lisboa, 2829-516 Caparica (Portugal); Carvalho, G. [REQUIMTE/CQFB, Chemistry Department, FCT, Universidade Nova de Lisboa, 2829-516 Caparica (Portugal); Instituto de Biologia Experimental e Tecnologica (IBET), Av. da Republica (EAN), 2784-505 Oeiras (Portugal); Oehmen, A., E-mail: adriano@dq.fct.unl.pt [REQUIMTE/CQFB, Chemistry Department, FCT, Universidade Nova de Lisboa, 2829-516 Caparica (Portugal); Reis, M.A.M. [REQUIMTE/CQFB, Chemistry Department, FCT, Universidade Nova de Lisboa, 2829-516 Caparica (Portugal)

    2011-10-15

    An intensive sampling campaign has been carried out in a municipal wastewater treatment plant (WWTP) to assess the dynamics of the influent pharmaceutical active compounds (PhAC) and musks. The mass loadings of these compounds in wastewater influents displayed contrasting diurnal variations depending on the compound. The musks and some groups of PhACs tended to follow a similar diurnal trend as compared to macropollutants, while the majority of PhACs followed either the opposite trend or no repeatable trend. The total musk loading to the WWTP was 0.74 {+-} 0.25 g d{sup -1}, whereas the total PhAC mass loading was 84.7 {+-} 63.8 g d{sup -1}. Unlike the PhACs, the musks displayed a high repeatability from one sampling day to the next. The range of PhAC loadings in the influent to WWTPs can vary several orders of magnitude from one day or week to the next, representing a challenge in obtaining data for steady-state modelling purposes. - Highlights: > Investigated the variations in influent wastewater pharmaceutical and musk loadings. > A high number of different pharmaceutical and musk compounds was analysed. > Many pharmaceutical groups displayed different characteristic patterns. > A representative steady-state pattern was observable for musks, not pharmaceuticals. > The results are relevant to the design of sampling campaigns for modelling purposes. - The diurnal variations of pharmaceuticals and musks were studied in an activated sludge plant, where the loadings of the musks were more repeatable than the pharmaceuticals.

  2. Altered Gene Expression in the Schistosome-Transmitting Snail Biomphalaria glabrata following Exposure to Niclosamide, the Active Ingredient in the Widely Used Molluscicide Bayluscide

    OpenAIRE

    Zhang, Si-Ming; Buddenborg, Sarah K; Adema, Coen M.; Sullivan, John T.; Loker, Eric S

    2015-01-01

    In view of the call by the World Health Organization (WHO) for elimination of schistosomiasis as a public health problem by 2025, use of molluscicides in snail control to supplement chemotherapy–based control efforts is likely to increase in the coming years. The mechanisms of action of niclosamide, the active ingredient in the most widely used molluscicides, remain largely unknown. A better understanding of its toxicology at the molecular level will both improve our knowledge of snail biolog...

  3. On the Correlation of Effective Terahertz Refractive Index and Average Surface Roughness of Pharmaceutical Tablets

    Science.gov (United States)

    Chakraborty, Mousumi; Bawuah, Prince; Tan, Nicholas; Ervasti, Tuomas; Pääkkönen, Pertti; Zeitler, J. Axel; Ketolainen, Jarkko; Peiponen, Kai-Erik

    2016-08-01

    In this paper, we have studied terahertz (THz) pulse time delay of porous pharmaceutical microcrystalline compacts and also pharmaceutical tablets that contain indomethacin (painkiller) as an active pharmaceutical ingredient (API) and microcrystalline cellulose as the matrix of the tablet. The porosity of a pharmaceutical tablet is important because it affects the release of drug substance. In addition, surface roughness of the tablet has much importance regarding dissolution of the tablet and hence the rate of drug release. Here, we show, using a training set of tablets containing API and with a priori known tablet's quality parameters, that the effective refractive index (obtained from THz time delay data) of such porous tablets correlates with the average surface roughness of a tablet. Hence, THz pulse time delay measurement in the transmission mode provides information on both porosity and the average surface roughness of a compact. This is demonstrated for two different sets of pharmaceutical tablets having different porosity and average surface roughness values.

  4. The simultaneous determination of active ingredients in cough-cold mixtures by isocratic reversed-phase ion-pair high-performance liquid chromatography.

    Science.gov (United States)

    Lau, O W; Chan, K; Lau, Y K; Wong, W C

    1989-01-01

    A simple, rapid and accurate method for the simultaneous determination of active ingredients in cough-cold mixtures using isocratic reversed-phase ion-pair high-performance liquid chromatography has been developed. It involves the use of an octadecylsilane column as the stationary phase with methanol, water, tetrahydrofuran, phosphoric acid mixtures as mobile phase including sodium dioctylsulphosuccinate as the ion-pair agent. The pH of the mobile phase was adjusted to 4.6 by means of phosphoric acid and ammonium hydroxide solutions. The proposed method involves the simple dilution of the samples with the mobile phase and the addition of metoclopramide hydrochloride as the internal standard. The active ingredients under investigation were chlorpheniramine, codeine, diphenhydramine, ephedrine, ethylmorphine, phenylephrine, phenylpropanolamine and pholcodine, which exist as various combinations in cough-cold mixtures. The optimum composition of the mobile phase and the optimum flow rate were determined and are reported. The method was applied to the determination of active ingredients in seven commercially available cough-cold mixtures.

  5. The simultaneous determination of active ingredients in cough-cold mixtures by isocratic reversed-phase ion-pair high-performance liquid chromatography.

    Science.gov (United States)

    Lau, O W; Chan, K; Lau, Y K; Wong, W C

    1989-01-01

    A simple, rapid and accurate method for the simultaneous determination of active ingredients in cough-cold mixtures using isocratic reversed-phase ion-pair high-performance liquid chromatography has been developed. It involves the use of an octadecylsilane column as the stationary phase with methanol, water, tetrahydrofuran, phosphoric acid mixtures as mobile phase including sodium dioctylsulphosuccinate as the ion-pair agent. The pH of the mobile phase was adjusted to 4.6 by means of phosphoric acid and ammonium hydroxide solutions. The proposed method involves the simple dilution of the samples with the mobile phase and the addition of metoclopramide hydrochloride as the internal standard. The active ingredients under investigation were chlorpheniramine, codeine, diphenhydramine, ephedrine, ethylmorphine, phenylephrine, phenylpropanolamine and pholcodine, which exist as various combinations in cough-cold mixtures. The optimum composition of the mobile phase and the optimum flow rate were determined and are reported. The method was applied to the determination of active ingredients in seven commercially available cough-cold mixtures. PMID:2577452

  6. Non-Hodgkin Lymphoma and Occupational Exposure to Agricultural Pesticide Chemical Groups and Active Ingredients: A Systematic Review and Meta-Analysis

    Directory of Open Access Journals (Sweden)

    Leah Schinasi

    2014-04-01

    Full Text Available This paper describes results from a systematic review and a series of meta-analyses of nearly three decades worth of epidemiologic research on the relationship between non-Hodgkin lymphoma (NHL and occupational exposure to agricultural pesticide active ingredients and chemical groups. Estimates of associations of NHL with 21 pesticide chemical groups and 80 active ingredients were extracted from 44 papers, all of which reported results from analyses of studies conducted in high-income countries. Random effects meta-analyses showed that phenoxy herbicides, carbamate insecticides, organophosphorus insecticides and the active ingredient lindane, an organochlorine insecticide, were positively associated with NHL. In a handful of papers, associations between pesticides and NHL subtypes were reported; B cell lymphoma was positively associated with phenoxy herbicides and the organophosphorus herbicide glyphosate. Diffuse large B-cell lymphoma was positively associated with phenoxy herbicide exposure. Despite compelling evidence that NHL is associated with certain chemicals, this review indicates the need for investigations of a larger variety of pesticides in more geographic areas, especially in low- and middle-income countries, which, despite producing a large portion of the world’s agriculture, were missing in the literature that were reviewed.

  7. Effect of Pharmaceutically Active Compound Nitroxoline on the Corrosion of Mild Steel in an Acidic Environment

    Directory of Open Access Journals (Sweden)

    R. Ganapathi Sundaram

    2016-01-01

    Full Text Available The effect of Nitroxoline, antibiotic drug, was tested as a corrosion inhibitor for mild steel (MS in an acidic environment by chemical method (mass loss measurement and electrochemical methods such as electrochemical impedance spectroscopy and potentiodynamic polarization. The surface morphology of mild steel was investigated by scanning electron microscopy, energy dispersive X-ray spectroscopy, and atomic force microscopy techniques. From the chemical and electrochemical methods, the resistance of corrosion was increased with the addition of Nitroxoline concentration. Tafel curves indicate that the pharmaceutically active compound is a cathodic type inhibitor. An adsorption of Nitroxoline on the surface of mild steel was obeyed by Langmuir isotherm. SEM, EDX, and AFM techniques prove the adsorption process. All the obtained results confirmed that the investigated compound Nitroxoline acts as a good inhibitor for the corrosion of mild steel in an acidic environment.

  8. Validation of quantitative 1H NMR method for the analysis of pharmaceutical formulations

    International Nuclear Information System (INIS)

    The need for effective and reliable quality control in products from pharmaceutical industries renders the analyses of their active ingredients and constituents of great importance. This study presents the theoretical basis of ¹H NMR for quantitative analyses and an example of the method validation according to Resolution RE N. 899 by the Brazilian National Health Surveillance Agency (ANVISA), in which the compound paracetamol was the active ingredient. All evaluated parameters (selectivity, linearity, accuracy, repeatability and robustness) showed satisfactory results. It was concluded that a single NMR measurement provides structural and quantitative information of active components and excipients in the sample. (author)

  9. Pharmaceutical cocrystals: walking the talk.

    Science.gov (United States)

    Bolla, Geetha; Nangia, Ashwini

    2016-06-28

    Pharmaceutical cocrystals belong to a sub-class of cocrystals wherein one of the components is a drug molecule (or an active pharmaceutical ingredient, API) and the second is a benign food or drug grade additive (generally regarded as safe, GRAS). The two components are hydrogen-bonded in a fixed stoichiometric ratio in the crystal lattice. In the past decade, pharmaceutical cocrystals have demonstrated significant promise in their ability to modify the physicochemical and pharmacokinetic properties of drug substances, such as the solubility and dissolution rate, bioavailability, particle morphology and size, tableting and compaction, melting point, physical form, biochemical and hydration stability, and permeability. In this feature review, we highlight some prominent examples of drug cocrystals which exhibit variable hardness/softness and elasticity/plasticity depending on coformer selection, improvement of solubility and permeability in the same cocrystal, increase of the melting point for solid formulation, enhanced color performance, photostability and hydration stability, and a longer half-life. Cocrystals of flavanoids and polyphenols can make improved pharmaceuticals and also extend to the larger class of nutraceuticals. The application of crystal engineering to assemble ternary cocrystals expands this field to drug-drug cocrystals which may be useful in multi-drug resistance, mitigating side effects of drugs, or attenuating/enhancing drug action synergistically by rational selection. The advent of new techniques for structural characterization beyond the standard X-ray diffraction will provide a better understanding of drug phases which are at the borderline of crystalline-amorphous nature and even newer opportunities in the future. PMID:27278109

  10. 77 FR 63290 - Foreign-Trade Zone 121-Albany, NY; Notification of Proposed Production Activity; Albany Molecular...

    Science.gov (United States)

    2012-10-16

    ... Rensselaer, New York, (Board Order 698, 7/20/1994, 59 FR 18318, 7/28/1994). AMRI is now requesting to produce an active pharmaceutical ingredient, dexpramipexole dihydrochloride monohydrate, under...

  11. Inkjet printing for pharmaceutics - A review of research and manufacturing.

    Science.gov (United States)

    Daly, Ronan; Harrington, Tomás S; Martin, Graham D; Hutchings, Ian M

    2015-10-30

    Global regulatory, manufacturing and consumer trends are driving a need for change in current pharmaceutical sector business models, with a specific focus on the inherently expensive research costs, high-risk capital-intensive scale-up and the traditional centralised batch manufacturing paradigm. New technologies, such as inkjet printing, are being explored to radically transform pharmaceutical production processing and the end-to-end supply chain. This review provides a brief summary of inkjet printing technologies and their current applications in manufacturing before examining the business context driving the exploration of inkjet printing in the pharmaceutical sector. We then examine the trends reported in the literature for pharmaceutical printing, followed by the scientific considerations and challenges facing the adoption of this technology. We demonstrate that research activities are highly diverse, targeting a broad range of pharmaceutical types and printing systems. To mitigate this complexity we show that by categorising findings in terms of targeted business models and Active Pharmaceutical Ingredient (API) chemistry we have a more coherent approach to comparing research findings and can drive efficient translation of a chosen drug to inkjet manufacturing. PMID:25772419

  12. Inkjet printing for pharmaceutics - A review of research and manufacturing.

    Science.gov (United States)

    Daly, Ronan; Harrington, Tomás S; Martin, Graham D; Hutchings, Ian M

    2015-10-30

    Global regulatory, manufacturing and consumer trends are driving a need for change in current pharmaceutical sector business models, with a specific focus on the inherently expensive research costs, high-risk capital-intensive scale-up and the traditional centralised batch manufacturing paradigm. New technologies, such as inkjet printing, are being explored to radically transform pharmaceutical production processing and the end-to-end supply chain. This review provides a brief summary of inkjet printing technologies and their current applications in manufacturing before examining the business context driving the exploration of inkjet printing in the pharmaceutical sector. We then examine the trends reported in the literature for pharmaceutical printing, followed by the scientific considerations and challenges facing the adoption of this technology. We demonstrate that research activities are highly diverse, targeting a broad range of pharmaceutical types and printing systems. To mitigate this complexity we show that by categorising findings in terms of targeted business models and Active Pharmaceutical Ingredient (API) chemistry we have a more coherent approach to comparing research findings and can drive efficient translation of a chosen drug to inkjet manufacturing.

  13. How Chinese Pharmaceutical Companies to Become Successful API/Key Intermediate Outsourcing Suppliers from the Regulatory Perspective

    Institute of Scientific and Technical Information of China (English)

    MinLi,Ph.D.

    2003-01-01

    With a record number of blockbuster drugs losing patent protection in recent years, major U.S. based multinational drug makers are finding ways to cut cost in order to keep their profit margin in the face of fierce generic competition. On the other hand, generic drug makers are looking for quality, yet inexpensive API/intermediate outsourcing suppliers in order to be profitable in a highly competitive industry. This has created an excellent opportunity for Chinese pharmaceutical companies to become active-pharmaceutical-ingredient (API, or drug substance) and/or pharmaceutical intermediate suppliers for the lucrative U.S.

  14. Pharmaceutical virtue.

    Science.gov (United States)

    Martin, Emily

    2006-06-01

    In the early history of psychopharmacology, the prospect of developing technologically sophisticated drugs to alleviate human ills was surrounded with a fervor that could be described as religious. This paper explores the subsequent history of the development of psychopharmacological agents, focusing on the ambivalent position of both the industry and its employees. Based on interviews with retired pharmaceutical employees who were active in the industry in the 1950s and 1960s when the major breakthroughs were made in the development of MAOIs and SSRIs, the paper explores the initial development of educational materials for use in sales campaigns. In addition, based on interviews with current employees in pharmaceutical sales and marketing, the paper describes the complex perspective of contemporary pharmaceutical employees who must live surrounded by the growing public vilification of the industry as rapacious and profit hungry and yet find ways to make their jobs meaningful and dignified. The paper will contribute to the understudied problem of how individuals function in positions that require them to be part of processes that on one description constitute a social evil, but on another, constitute a social good.

  15. "Natural" ingredients in cosmetic dermatology.

    Science.gov (United States)

    Baumann, Leslie; Woolery-Lloyd, Heather; Friedman, Adam

    2009-06-01

    Recently, both clinical and bench research has begun to provide scientific validation for the use of certain botanical ingredients. Related findings regarding proposed biological mechanisms of action have translated into clinical practice. Botanical compounds for which dermatologic and cosmetic applications have emerged include: olive oil, chamomile, colloidal oatmeal, oat kernal extract, feverfew, acai berry, coffee berry, curcumin, green tea, pomegranate, licorice, paper mulberry, arbutin, and soy. Many of these botanical sources offer biologically active components that require further in vitro and in vivo investigation in order for us to properly educate ourselves, and our patients, regarding over-the-counter products based on these ingredients. PMID:19562883

  16. Nitrification activity and community structure of nitrite-oxidizing bacteria in the bioreactors operated with addition of pharmaceuticals

    Energy Technology Data Exchange (ETDEWEB)

    Kraigher, Barbara, E-mail: barbara.kraigher@bf.uni-lj.si [University of Ljubljana, Biotechnical Faculty, Department of Food Science and Technology, Chair of Microbiology, Vecna pot 111, 1000 Ljubljana (Slovenia); Mandic-Mulec, Ines [University of Ljubljana, Biotechnical Faculty, Department of Food Science and Technology, Chair of Microbiology, Vecna pot 111, 1000 Ljubljana (Slovenia)

    2011-04-15

    Pharmaceuticals represent a group of the new emerging contaminants, which might influence microbial communities in the activated sludge. Nitrification activity and Nitrospira community structure in the small-scale reactors supplied with different concentrations (0, 50, 200, 500 {mu}g L{sup -1}) of the selected pharmaceuticals (ibuprofen, naproxen, ketoprofen, diclofenac and clofibric acid) were evaluated. Ammonia removal was not influenced by selected pharmaceuticals. However, in the two reactors operated with 50 {mu}g L{sup -1} of pharmaceuticals (R50 and R50P), the effluent concentration of N-(NO{sub 2}{sup -} + NO{sub 3}{sup -}) was significantly higher than in the other reactors. Nitrospira community structure was assessed by terminal restriction fragment length polymorphism (T-RFLP) and by cloning and sequencing of the partial genes for 16S rRNA. Nitrospira spp. were detected in all reactors. The two dominant T-RFs represented the sublineages I and II of the genus Nitrospira. Main shifts were observed in the reactors R50 and R50P, where the T-RF representing sublineage II was much higher as compared to the other reactors. Consistent with this, the Nitrospira sublineage II was detected only in the clone libraries from the reactors R50 and R50P. Our results suggest that the relative abundance of Nitrospira sublineage II could be related to the effluent N-(NO{sub 2}{sup -} + NO{sub 3}{sup -}) concentration.

  17. Analysis of the pharmaceutical care activities practiced by private homeopathic pharmacies located in Rio de Janeiro North Zone

    Directory of Open Access Journals (Sweden)

    Tereza Aguiar

    2011-09-01

    Full Text Available The complexity of homeopathic treatment delegates to the Pharmacist the need and the responsibility of pharmaceutical care. This paper had the objective of verifying the practices of pharmaceutical care in homeopathy. The study was conducted in homeopathic pharmacies situated in Rio de Janeiro North Zone, during March and April, 2011, where 15 pharmacists were interviewed, with the help of a semi-open questionary self-administered. For the survey were investigated variables related to pharmaceutical: sex, age, nature of the institution where he graduated, having completed post-graduate and working ties. Information professionals for the pharmaceutical care were collected in 14 questions grouped into three areas: attitudes, perceptions and satisfaction. Attending the ethical aspects, the study was submitted to and approved by the Ethics Committee of University Estácio de Sá. The results demonstrated that 33% of the pharmacists have less than 5 years of professional practice, and 53% are specialists graduated by the Hahnemann’s Institutite of Brasil. All Pharmacists claim to orient patients, mostly during dispensation and through phone contacts. Most pharmacists oriented patients passively and actively. The elderly were pointed as the ones, who most often sought orientation. During dispensation of homeopathic drugs, all patients elicit some orientation. 67% of the pharmacies keep material for pharmaceutical guidance to the patients, usually leaflets. The verbal and written orientation was predominanted on homeopathic pharmacist. Posology and instructions of use for the pharmaceutical form dispensed were described as the most common doubts of the patients. Of all pharmacists interviewed, 67% pointed to self-medication practices in the pharmacy. The questions which measure the position and perception of the pharmacists related to pharmaceutical assistance scored over 3. The question which scored higher was related to

  18. Evaluation of Fenton's Reagent and Activated Persulfate for Treatment of a Pharmaceutical Waste Mixture in Groundwater

    DEFF Research Database (Denmark)

    Bennedsen, Lars Rønn; Søgaard, Erik Gydesen; Kakarla, Prasad;

    2010-01-01

    Soil and groundwater beneath the Kærgård Plantage megasite in Denmark are contaminated with a complex mixture of pharmaceutical wastes, including sulfonamides, barbiturates, aniline, pyridine chlorinated solvents (DNAPL), benzene, toluene, mercury, and cyanide. Regulatory agencies in Denmark...

  19. Active Ingredient Analysis of Tibet Cultivated Ganoderma Lucidum%西藏人工栽培灵芝活性成分分析

    Institute of Scientific and Technical Information of China (English)

    饶恩铭; 刘涛; 次仁德吉; 宋博文

    2015-01-01

    In order to understand the main active ingredient in Tibet cultivated Ganoderma Lucidum, this article collected the local cultivated Ganoderma Lucidum as the raw materials, used anthrone-sulfuric acid spectroscopy, spectrophotometry, pre-column derivatization RP-HPLC method to analyze the main active ingredient. The results showed that the contents of Ganoderma lucidum polysaccharides, triterpenoids, amino acids in Tibet cultivated Ganoderma Lucidum were:1.199g/100g, 1.63%, 8.898g/100g. Compared with national coverage, the active ingredient of cultivated Ganoderma Lucidum is richer, and the acid and triterpenoids content is higher than that in other regions.%为了解西藏人工栽培灵芝的主要活性成分,采集当地栽培的灵芝为原材料,分别采用蒽酮-硫酸分光法、紫外分光光度法、柱前衍生化RP-HPLC方法,分析其主要活性成分。结果表明,西藏人工栽培的灵芝中灵芝多糖、三萜类、氨基酸含量依次为:1.199g/100g、1.63%、8.898g/100g,经与国内报道相比较,西藏人工灵芝活性成分比较丰富,氨基酸和三萜类含量高于其他区域。

  20. Genotoxicity evaluation of the herbicide Garlon(®) and its active ingredient (triclopyr) in fish (Anguilla anguilla L.) using the comet assay.

    Science.gov (United States)

    Guilherme, Sofia; Santos, Maria A; Gaivão, Isabel; Pacheco, Mário

    2015-09-01

    Triclopyr-based herbicides are broadly used worldwide for site preparation and forest vegetation management. Thus, following application, these agrochemicals can inadvertently reach the aquatic ecosystems. Garlon(®) is one of the most popular commercial denominations of this group of herbicides, considered as highly toxic to fish, even by its manufacturer. Although DNA is frequently regarded as a target of pesticide toxicity, the genotoxic potential of Garlon(®) to fish remains completely unknown. Hence, the main goal of this study was to evaluate the genotoxicity of Garlon(®) and its active ingredient (triclopyr), clarifying the underlying mechanisms. Therefore, the comet assay, implemented as the standard procedure, with an extra step involving DNA lesion-specific repair enzymes (formamidopyrimidine DNA glycosylase and endonuclease III), was used to identify DNA damage in blood cells of Anguilla anguilla L. Short-term exposures (1 and 3 days) to Garlon(®) and triclopyr were carried out, adopting environmentally realistic concentrations (67.6 and 270.5 µg L(-1) Garlon(®) and 30 and 120 µg L(-1) triclopyr). The results concerning the nonspecific DNA damage proved the risk of the herbicide Garlon(®) and its active ingredient triclopyr in both tested concentrations and exposure lengths. In addition, the higher genotoxic potential of the formulation, in comparison with the active ingredient, was demonstrated. When the additional breaks corresponding to net enzyme-sensitive sites were considered, none of the conditions revealed significant levels of oxidative damage. This identification of the genotoxic properties of triclopyr-based herbicides to fish highlights the need to develop less hazardous formulations, as well as the adoption of mitigation measures related to the application of these agrochemicals in the framework of forestry and agriculture sustainable management. PMID:24623388

  1. Effects of Mongolian Pharmaceutical Betel Shisanwei Ingredients Pill on hypothalamic-pituitary-adrenal axis negative feedback function in rat models of chronic stress-induced depression%慢性应激抑郁模型大鼠下丘脑-垂体-肾上腺轴负反馈功能与蒙药槟榔十三味丸的干预

    Institute of Scientific and Technical Information of China (English)

    包伍叶; 范盎然; 白亮凤; 佟海英; 于雪; 乌吉斯古冷; 李婧; 胡日乐巴根; 张月

    2014-01-01

    BACKGROUND:Mongolian Pharmaceutical Betel Shisanwei Ingredients Pil has achieved good clinical efficacy, but the underlying mechanism remains unclear. OBJECTIVE: To study the effects of Mongolian Pharmaceutical Betel Shisanwei Ingredients Pil on the hypothalamic-pituitary-adrenal axis negative feedback function in the chronic depressed rats, and to explore anti-depression mechanisms of Mongolian Pharmaceutical Betel Shisanwei ingredients pil. METHODS: Eighty male Wistar rats were randomly divided into ten groups according to the sugar consumption test (with eight rats in each group): normal control group, model group, fluoxetine group, high-, medium- and low-dose Betel Shisanwei Ingredients Pil groups, RU486 group, high-, medium- and low-dose Betel Shisanwei Ingredients Pil plus RU486 groups. Except normal control group, the other groups were treated with the chronic unpredictable mild stress stimulation combined with lonely rising, to establish depression models. In the meantime, rats of the high-, medium- and low-dose Betel Shisanwei Ingredients Pil groups were given oral gavage of Betel Shisanwei Ingredients Pil (0.2, 0.4, 0.8 g/kg) for 28 days; rats of the normal control group and model group were intragstricaly administered with sodium carboxymethyl celulose; rats of RU486 group were given abdominal subcutaneous injection of RU486 from day 21 after modeling; rats of the high-, medium- and low-dose Betel Shisanwei Ingredients Pil plus RU486 groups were intragstricaly administered with Betel Shisanwei Ingredients Pil (0.2, 0.4, 0.8 g/kg) and subcutaneous injection of RU486 from day 21. RESULTS AND CONCLUSION:Compared with normal control group, cortisone content increased significantly (P < 0.05), the expression of glucocorticoid receptor mRNA in hippocampus, hypothalamus and pituitary gland decreased significantly, and hypothalamic corticotrophin releasing hormone mRNA expression increased significantly in the model group and RU486 group. Compared with model

  2. Robust Market Launch Planning for a Multi- Echelon Pharmaceutical Supply Chain

    DEFF Research Database (Denmark)

    Hansen, Klaus Reinholdt Nyhuus; Grunow, Martin; Gani, Rafiqul

    2011-01-01

    It is well known, that the pharmaceutical industry is struggling with increasing cost and length of R&D projects. Earnings of a drug drop drastically after patent expiration. Thus, the industry spends much effort on reducing Time-to-Market. In the literature, little attention is given to drug...... launching activities after the drug has been approved. In this paper, we present a recourse-based stochastic model, which allows for time phasing the market entries to balance the fluctuating demand with the fixed and periodic production of the active pharmaceutical ingredient. The two major risk elements...

  3. TASTE MASKING TECHNOLOGIES: A NOVEL APPROACH FOR THE IMPROVEMENT OF ORGANOLEPTIC PROPERTY OF PHARMACEUTICAL ACTIVE SUBSTANCE

    Directory of Open Access Journals (Sweden)

    Sharma Deepak

    2012-04-01

    Full Text Available Acceptability of any dosage form are mainly depends over its taste i.e. mouth feel. Drug molecule interacts with taste receptor on the tongue to give bitter, sweet or salty taste sensation, when they dissolve in saliva. This sensation of the taste is the result of signal transduction from the receptor organs for taste, commonly known as taste buds. In market, there are numbers of pharmaceutical preparations available in which actives are bitter in taste. The improved palatability in these products has prompted the development of numerous formulations, which improved performance and acceptability. The bitterness of preparation also leads to patient incompliance. So masking of bitterness becomes essential. To overcome this problem, many techniques have been developed to mask the bitter taste of drugs. These techniques are not only mask the bitter taste of drug but also enhance the bioavailability and performance of drug dosage form. It includes adding sugars, flavors, sweeteners, use of lipoproteins, numbing taste buds, granulation, use of adsorbates ,coating drug, microencapsulation, multiple emulsion, viscosity modifier, vesicles and liposomes, prodrug and salt formation, inclusion and molecular complexes, solid dispersion and Ion Exchange Resins (IERs which have been tried by the formulators to mask the unpleasant taste of the bitter drugs. The present review article highlights different technologies of taste masking with respect to dosage form and novel methods of evaluation of taste masking effect.

  4. Photo-transformation of pharmaceutically active compounds in the aqueous environment: a review.

    Science.gov (United States)

    Yan, Shuwen; Song, Weihua

    2014-04-01

    In the past few years, the fate and transportation of pharmaceutically active compounds (PhACs) in aqueous environments have raised significant concerns among the public, scientists and regulatory groups. Photodegradation is an important removal process in surface waters. This review summarizes the last 10 years (2003-2013) of studies on the solar or solar-simulated photodegradation of PhACs in aqueous environments. The PhACs covered include: beta-blockers, antibiotics, non-steroidal anti-inflammatory drugs (NSAIDs), histamine H₂-receptor antagonists, lipid regulators, carbamazepine, steroid hormones, and X-ray contrast media compounds. Kinetic studies, degradation mechanisms and toxicity removal are the three major topics involved in this review. The quantum yield for the direct photolysis of PhACs and the bimolecular reaction rate constants of PhACs with reactive oxygen species (ROS), such as the ˙OH radical and singlet oxygen, are also summarized. This information is not only important to predict the PhAC photodegradation fate, but also is very useful for advanced treatment technologies, such as ozone or advanced oxidation processes.

  5. Development of RP-HPLC method for Qualitative Analysis of Active Ingredient (Gallic acid) from Stem Bark of Dendrophthoe falcate Linn.

    OpenAIRE

    Hafsa Deshmukh; Pradnya J. Prabhu

    2011-01-01

    A simple, precise and sensitive, RP-HPLC method with UV detection at 271nm was developed and validated for qualitative determination of active ingredient Gallic acid from stem bark of Dendrophthoe falcate Linn. Separation was performed on a ThermoMOS 2 HYPERSIL C18 column (250 cm × 4.6 mm, 5µm ODS 3) using mobile phase comprising of 0.1% Orthophosphoric acid : Acetonitrile (400 cm3 : 600 cm3) with a flow rate of 1 ml/minute with a short run time of 13 minute. The method was validated accordi...

  6. Adsorption of selected endocrine disrupting compounds and pharmaceuticals on activated biochars.

    Science.gov (United States)

    Jung, Chanil; Park, Junyeong; Lim, Kwang Hun; Park, Sunkyu; Heo, Jiyong; Her, Namguk; Oh, Jeill; Yun, Soyoung; Yoon, Yeomin

    2013-12-15

    Chemically activated biochar produced under oxygenated (O-biochar) and oxygen-free (N-biochar) conditions were characterized and the adsorption of endocrine disrupting compounds (EDCs): bisphenol A (BPA), atrazine (ATR), 17 α-ethinylestradiol (EE2), and pharmaceutical active compounds (PhACs); sulfamethoxazole (SMX), carbamazepine (CBM), diclofenac (DCF), ibuprofen (IBP) on both biochars and commercialized powdered activated carbon (PAC) were investigated. Characteristic analysis of adsorbents by solid-state nuclear magnetic resonance (NMR) was conducted to determine better understanding about the EDCs/PhACs adsorption. N-biochar consisted of higher polarity moieties with more alkyl (0-45 ppm), methoxyl (45-63 ppm), O-alkyl (63-108 ppm), and carboxyl carbon (165-187 ppm) content than other adsorbents, while aromaticity of O-biochar was higher than that of N-biochar. O-biochar was composed mostly of aromatic moieties, with low H/C and O/C ratios compared to the highly polarized N-biochar that contained diverse polar functional groups. The higher surface area and pore volume of N-biochar resulted in higher adsorption capacity toward EDCs/PhACs along with atomic-level molecular structural property than O-biochar and PAC. N-biochar had a highest adsorption capacity of all chemicals, suggesting that N-biochar derived from loblolly pine chip is a promising sorbent for agricultural and environmental applications. The adsorption of pH-sensitive dissociable SMX, DCF, IBP, and BPA varied and the order of adsorption capacity was correlated with the hydrophobicity (Kow) of adsorbates throughout the all adsorbents, whereas adsorption of non-ionizable CBM, ATR, and EE2 in varied pH allowed adsorbents to interact with hydrophobic property of adsorbates steadily throughout the study. PMID:24231319

  7. Quality control of tuirejieduling granules using high-performance liquid chromatography fingerprint method and simultaneous determination of four main active ingredients

    Directory of Open Access Journals (Sweden)

    Aixia Yang

    2013-01-01

    Full Text Available Background: The Tuirejieduling granule is a compound preparation made from four kinds of Chinese medicines. It is effective for anti-inflammation, antivirus, defervescence and anti-bacterium; however, its quality control standards have remained unknown. Objective: To establish a simple and accurate fingerprint method for quality control of the Tuirejieduling granule. Materials and Methods: The methanol extract of the Tuirejieduling granule was used for the fingerprint analysis and the four selected active ingredients (epigoitrin, phillyrin, saikosaponin A and glycyrrhetinic acid in the extract were determined. The fingerprint method was performed on an Amethyst C18-P chromatography column by gradient elution with acetonitrile and aqueous phase (containing 0.5% H 3 PO 4 (v/v, pH 3.0. Results: Under the optimal chromatographic condition, twenty peaks were chosen as fingerprint peaks of the Tuirejieduling granules extractions. The similarities of 10 batches of Tuirejieduling granule was more than 0.99. This indicates that the different batches of Tuirejieduling granules were under the consistent quality control. Good linear behaviors over the investigated concentration ranges were obtained with the values of R2 higher than 0.99 for four studied active ingredients. The recoveries for spiked samples were in the range of 96.2-105.5%. The developed method was successfully applied to determine the contents of active constituents in different batches of Tuirejieduling granule. Conclusion: The HPLC fingerprint was proved to be a reliable method for the quality control of Tuirejieduling granule.

  8. Effects of the glyphosate active ingredient and a formulation on Lemna gibba L. at different exposure levels and assessment end-points.

    Science.gov (United States)

    Sobrero, M C; Rimoldi, F; Ronco, A E

    2007-11-01

    The use of formulations of the herbicide glyphosate in transgenic crops of the Pampa's plains of Argentina has extensively increased, though there is scarce information of its impact on non-target vascular plants from agro-ecosystem related surface waters. The sensitivity of a local clone of the macrophyte Lemna gibba L. to glyphosate active principle and Roundup Max formulation was studied in standardized laboratory conditions. Phytotoxic effects, considering the aquatic route, at a concentration range of glyphosate between 0.5 and 80 mg L(-1) as active ingredient during 10 days of exposure were assessed on plant population growth, frond growth, shape and number, total chlorophyll content and colony architecture. Exposure to 1 mg L(-1) of glyphosate (an expected environmental concentration) affects all the studied assessment endpoints, except for population growth and chlorophyll content. Equivalent concentrations of this herbicide as the active ingredient or RoundupMax indicate higher phytotocity of the formulation. Exposed plants at concentrations of herbicide between 1 and 7.5 mg L(-1) exhibit after two days a recovery of the multiplication rate. Frond aggregation and longer stipe was detected between 1 and 15 mg L(-1) of glyphosate, determining more open colony architecture. At higher concentrations of the herbicide fronds break-up. Comparisons with literature data indicate a higher sensitivity of the L. gibba local clone with respect to L. minor and algal species, and also a similar response to the herbicide in field experiments with the same species. PMID:17940715

  9. Expanding the Therapeutic Spectrum of Artemisinin: Activity Against Infectious Diseases Beyond Malaria and Novel Pharmaceutical Developments

    Directory of Open Access Journals (Sweden)

    Thomas Efferth

    2016-08-01

    Full Text Available The interest of Western medicine in Traditional Chinese Medicine (TCM as a source of drug leads/new drugs to treat diseases without available efficient therapies has been dramatically augmented in the last decades by the extensive work and the outstanding findings achieved within this kind of medicine. The practice of TCM over thousands of years has equipped scientists with substantial experience with hundreds of plants that led to the discovery of artemisinin (qinghaosu, which is extracted from the medicinal plant Artemisia annua L. (qinghao. The unexpected success of artemisinin in combating malaria has drawn strong attention from the scientific community towards TCM. Artemisinin was discovered by Youyou Tu in 1972. Since then, several novel pharmacological activities based on the well-known properties of the sesquiterpene lactone structure with the oxepane ring and an endoperoxide bridge have been unravelled. Beyond malaria, artemisinin and its derivatives (artemisinins exert profound activities towards other protozoans (Leishmania, Trypanosoma, amoebas, Neospora caninum, and Eimeria tenella, trematodes (Schistosoma, liver flukes, and viruses (human cytomegalovirus, hepatitis B and C viruses. Less clear is the effect against bacteria and fungi. Based on the promising results of artemisinin and the first generation derivatives (artesunate, artemether, arteether, novel drug development strategies have been pursued. These included the synthesis of acetal- and non-acetal-type artemisinin dimeric molecules as well as developing nanotechnological approaches, e.g. artemisinin-based liposomes, niosomes, micelles, solid lipid nanocarriers, nanostructured lipid carriers, nanoparticles, fullerenes and nanotubes. The current review presents an overview on different aspects of artemisinins, including sources, chemistry, biological/pharmacological properties, types of infectious pathogens that are susceptible to artemisinins in vitro and in vivo, in

  10. Occurrence and removal of pharmaceutically active compounds in sewage treatment plants with different technologies.

    Science.gov (United States)

    Ying, Guang-Guo; Kookana, Rai S; Kolpin, Dana W

    2009-08-01

    Occurrence of eight selected pharmaceutically active compounds (PhACs; caffeine, carbamazepine, triclosan, gemfibrozil, diclofenac, ibuprofen, ketoprofen and naproxen) were investigated in effluents from fifteen sewage treatment plants (STPs) across South Australia. In addition, a detailed investigation into the removal of these compounds was also carried out in four STPs with different technologies (Plant A: conventional activated sludge; plant B: two oxidation ditches; plant C: three bioreactors; and plant D: ten lagoons in series). The concentrations of these compounds in the effluents from the fifteen STPs showed substantial variations among the STPs, with their median concentrations ranging from 26 ng/L for caffeine to 710 ng/L for carbamazepine. Risk assessment based on the "worst case scenario" of the monitoring data from the present study suggested potential toxic risks to aquatic organisms posed by carbamazepine, triclosan and diclofenac associated with such effluent discharge. With the exception of carbamazepine and gemfibrozil, significant concentration decreases between influent and effluent were observed in the four STPs studied in more detail. Biodegradation was found to be the main mechanism for removing concentrations from the liquid waste stream for the PhACs within the four STPs, while adsorption onto sludge appeared to be a minor process for all target PhACs except for triclosan. Some compounds (e.g. gemfibrozil) exhibited variable removal efficiencies within the four STPs. Plant D (10 lagoons in series) was least efficient in the removal of the target PhACs; significant biodegradation of these compounds only occurred from the sixth or seventh lagoon. PMID:19657534

  11. Occurrence and removal of pharmaceutically active compounds in sewage treatment plants with different technologies

    Science.gov (United States)

    Ying, Guang-Guo; Kookana, Rai S.; Kolpin, Dana W.

    2009-01-01

    Occurrence of eight selected pharmaceutically active compounds (PhACs; caffeine, carbamazepine, triclosan, gemfibrozil, diclofenac, ibuprofen, ketoprofen and naproxen) were investigated in effluents from fifteen sewage treatment plants (STPs) across South Australia. In addition, a detailed investigation into the removal of these compounds was also carried out in four STPs with different technologies (Plant A: conventional activated sludge; plant B: two oxidation ditches; plant C: three bioreactors; and plant D: ten lagoons in series). The concentrations of these compounds in the effluents from the fifteen STPs showed substantial variations among the STPs, with their median concentrations ranging from 26 ng/L for caffeine to 710 ng/L for carbamazepine. Risk assessment based on the "worst case scenario" of the monitoring data from the present study suggested potential toxic risks to aquatic organisms posed by carbamazepine, triclosan and diclofenac associated with such effluent discharge. With the exception of carbamazepine and gemfibrozil, significant concentration decreases between influent and effluent were observed in the four STPs studied in more detail. Biodegradation was found to be the main mechanism for removing concentrations from the liquid waste stream for the PhACs within the four STPs, while adsorption onto sludge appeared to be a minor process for all target PhACs except for triclosan. Some compounds (e.g. gemfibrozil) exhibited variable removal efficiencies within the four STPs. Plant D (10 lagoons in series) was least efficient in the removal of the target PhACs; significant biodegradation of these compounds only occurred from the sixth or seventh lagoon.

  12. Study of split-ring resonators for use on a pharmaceutical drug capsule for microwave activated drug release

    DEFF Research Database (Denmark)

    Jónasson, Sævar Þór; Jensen, Brian Sveistrup; Johansen, Tom Keinicke

    2012-01-01

    the gap simultaneously with the magnetic field component normal to the SRRs. Furthermore, an analysis of the optimal conductivity and relative permittivity for enhanced temperature rise in the lid is performed. Conductivity of 0.09 S/m and relative permittivity of 12 shows the highest temperature rise.......In this paper, a novel method for externally activating a pharmaceutical drug capsule by use of split-ring resonators (SRR) is introduced. To this end, the effect of the orientation of the SRRs on the ability to activate the capsules is examined. A coplanar waveguide is used to excite an identical...... pair of SRRs fabricated on a substrate, representing an enlarged lid for a pharmaceutical drug capsule. Orientations where the electric field component of a quasi-TEM wave lies across the gap of the SRRs provides the largest response. The optimal case is when the electric field component lies across...

  13. Adsorption of pharmaceuticals onto activated carbon fiber cloths - Modeling and extrapolation of adsorption isotherms at very low concentrations

    OpenAIRE

    Fallou, Hélène; Cimetiere, Nicolas; Giraudet, Sylvain; Wolbert, Dominique; Le Cloirec, Pierre

    2016-01-01

    International audience Activated carbon fiber cloths (ACFC) have shown promising results when applied to water treatment, especially for removing organic micropollutants such as pharmaceutical compounds. Nevertheless, further investigations are required, especially considering trace concentrations, which are found in current water treatment. Until now, most studies have been carried out at relatively high concentrations (mg L(-1)), since the experimental and analytical methodologies are mo...

  14. Changes in FDA enforcement activities following changes in federal administration: the case of regulatory letters released to pharmaceutical companies

    OpenAIRE

    Nguyen Diane; Seoane-Vazquez Enrique; Rodriguez-Monguio Rosa; Montagne Michael

    2013-01-01

    Abstract Background The United States (US) Food and Drug Administration (FDA) is responsible for the protection of the public health by assuring the safety, effectiveness and security of human drugs and biological products through the enforcement of the Federal Food, Drug and Cosmetic Act (FDCA) and related regulations. These enforcement activities include regulatory letters (i.e. warning letters and notice of violation) to pharmaceutical companies. A regulatory letter represents the FDA’s fi...

  15. Hovenia dulcis Thunb extract and its ingredient methyl vanillate activate Wnt/β-catenin pathway and increase bone mass in growing or ovariectomized mice.

    Directory of Open Access Journals (Sweden)

    Pu-Hyeon Cha

    Full Text Available The Wnt/β-catenin pathway is a potential target for development of anabolic agents to treat osteoporosis because of its role in osteoblast differentiation and bone formation. However, there is no clinically available anti-osteoporosis drug that targets this Wnt/β-catenin pathway. In this study, we screened a library of aqueous extracts of 350 plants and identified Hovenia dulcis Thunb (HDT extract as a Wnt/β-catenin pathway activator. HDT extract induced osteogenic differentiation of calvarial osteoblasts without cytotoxicity. In addition, HDT extract increased femoral bone mass without inducing significant weight changes in normal mice. In addition, thickness and area of femoral cortical bone were also significantly increased by the HDT extract. Methyl vanillate (MV, one of the ingredients in HDT, also activated the Wnt/β-catenin pathway and induced osteoblast differentiation in vitro. MV rescued trabecular or cortical femoral bone loss in the ovariectomized mice without inducing any significant weight changes or abnormality in liver tissue when administrated orally. Thus, natural HDT extract and its ingredient MV are potential anabolic agents for treating osteoporosis.

  16. Computer-aided tool for solvent selection in pharmaceutical processes: Solvent swap

    DEFF Research Database (Denmark)

    Papadakis, Emmanouil; K. Tula, Anjan; Gernaey, Krist V.;

    swap solvents is developed and is used to retrieve information for the most commonly used solvent candidates typically found in the pharmaceutical industry. The selection is verified by simulation. The framework for the solvent selection and solvent swap is part of an integrated computer......-aided framework with the objective to assist the pharmaceutical industry in gaining better process understanding. A software interface to improve the usability of the tool has been created also.......In the pharmaceutical processes, solvents have a multipurpose role since different solvents can be used in different stages (such as chemical reactions, separations and purification) in the multistage active pharmaceutical ingredients (APIs) production process. The solvent swap and selection tasks...

  17. Supercritical fluid chromatography for GMP analysis in support of pharmaceutical development and manufacturing activities.

    Science.gov (United States)

    Hicks, Michael B; Regalado, Erik L; Tan, Feng; Gong, Xiaoyi; Welch, Christopher J

    2016-01-01

    Supercritical fluid chromatography (SFC) has long been a preferred method for enantiopurity analysis in support of pharmaceutical discovery and development, but implementation of the technique in regulated GMP laboratories has been somewhat slow, owing to limitations in instrument sensitivity, reproducibility, accuracy and robustness. In recent years, commercialization of next generation analytical SFC instrumentation has addressed previous shortcomings, making the technique better suited for GMP analysis. In this study we investigate the use of modern SFC for enantiopurity analysis of several pharmaceutical intermediates and compare the results with the conventional HPLC approaches historically used for analysis in a GMP setting. The findings clearly illustrate that modern SFC now exhibits improved precision, reproducibility, accuracy and robustness; also providing superior resolution and peak capacity compared to HPLC. Based on these findings, the use of modern chiral SFC is recommended for GMP studies of stereochemistry in pharmaceutical development and manufacturing.

  18. Analysis of pharmaceutical pellets: An approach using near-infrared chemical imaging

    Energy Technology Data Exchange (ETDEWEB)

    Sabin, Guilherme P.; Breitkreitz, Marcia C.; Souza, Andre M. de [Institute of Chemistry, University of Campinas, P.O. Box 6154, 13084-971 Campinas, SP (Brazil); Fonseca, Patricia da; Calefe, Lupercio; Moffa, Mario [Zelus Servicos para Industria Farmaceutica Ltda., Av. Professor Lineu Prestes n. 2242, Sao Paulo, SP (Brazil); Poppi, Ronei J., E-mail: ronei@iqm.unicamp.br [Institute of Chemistry, University of Campinas, P.O. Box 6154, 13084-971 Campinas, SP (Brazil)

    2011-11-07

    Highlights: {yields} Near-Infrared Chemical Imaging was used for pellets analysis. {yields} Distribution of the components throughout the coatings layers and core of the pellets was estimated. {yields} Classical Least Squares (CLS) was used for calculation of the concentration maps. - Abstract: Pharmaceutical pellets are spherical or nearly spherical multi-unit dosage forms designed to optimize pharmacokinetics and pharmacodynamics features of drug release. The distribution of the pharmaceutical ingredients in the layers and core is a very important parameter for appropriate drug release, especially for pellets manufactured by the process of layer gain. Physical aspects of the sample are normally evaluated by Scanning Electron Microscopy (SEM), but it is in many cases unsuitable to provide conclusive chemical information about the distribution of the pharmaceutical ingredients in both layers and core. On the other hand, methods based on spectroscopic imaging can be very promising for this purpose. In this work, a Near-Infrared Chemical Imaging (NIR-CI) method was developed and applied to the analysis of diclophenac sodium pellets. Since all the compounds present in the sample were known in advance, Classical Least Squares (CLS) was used for calculations. The results have shown that the method was capable of providing chemical information about the distribution of the active ingredient and excipients in the core and coating layers and therefore can be complementary to SEM for the pharmaceutical development of pellets.

  19. Adsorption of selected endocrine disrupting compounds and pharmaceuticals on activated biochars

    Energy Technology Data Exchange (ETDEWEB)

    Jung, Chanil [Department of Civil and Environmental Engineering, University of South Carolina, Columbia, SC 29208 (United States); Park, Junyeong [Department of Forest Biomaterials, North Carolina State University, Raleigh, NC 27695 (United States); Lim, Kwang Hun [Department of Chemistry, East Carolina University, Greenville, NC 27858 (United States); Park, Sunkyu [Department of Forest Biomaterials, North Carolina State University, Raleigh, NC 27695 (United States); Heo, Jiyong [Department of Civil and Environmental Engineering, Korea Army Academy at Young-Cheon, PO Box 135-1, Changhari, Gogyeongmeon, Young-cheon 770-849, Gyeongbuk (Korea, Republic of); Her, Namguk [Department of Chemistry and Environmental Sciences, Korea Army Academy at Young-Cheon, PO Box 135-1, Changhari, Gogyeongmeon, Young-cheon 770-849, Gyeongbuk (Korea, Republic of); Oh, Jeill; Yun, Soyoung [Department of Civil and Environmental Engineering, Chung-Ang University, Dongjak-Ku, Seoul 156-756 (Korea, Republic of); Yoon, Yeomin, E-mail: yoony@cec.sc.edu [Department of Civil and Environmental Engineering, University of South Carolina, Columbia, SC 29208 (United States)

    2013-12-15

    Highlights: • Biochars were prepared at different gas environments. • The competitive adsorption among EDCs/PhACs were investigated. • Aromaticity of adsorbent plays a significant role for EDCs/PhACs adsorption. -- Abstract: Chemically activated biochar produced under oxygenated (O-biochar) and oxygen-free (N-biochar) conditions were characterized and the adsorption of endocrine disrupting compounds (EDCs): bisphenol A (BPA), atrazine (ATR), 17 α-ethinylestradiol (EE2), and pharmaceutical active compounds (PhACs); sulfamethoxazole (SMX), carbamazepine (CBM), diclofenac (DCF), ibuprofen (IBP) on both biochars and commercialized powdered activated carbon (PAC) were investigated. Characteristic analysis of adsorbents by solid-state nuclear magnetic resonance (NMR) was conducted to determine better understanding about the EDCs/PhACs adsorption. N-biochar consisted of higher polarity moieties with more alkyl (0–45 ppm), methoxyl (45–63 ppm), O-alkyl (63–108 ppm), and carboxyl carbon (165–187 ppm) content than other adsorbents, while aromaticity of O-biochar was higher than that of N-biochar. O-biochar was composed mostly of aromatic moieties, with low H/C and O/C ratios compared to the highly polarized N-biochar that contained diverse polar functional groups. The higher surface area and pore volume of N-biochar resulted in higher adsorption capacity toward EDCs/PhACs along with atomic-level molecular structural property than O-biochar and PAC. N-biochar had a highest adsorption capacity of all chemicals, suggesting that N-biochar derived from loblolly pine chip is a promising sorbent for agricultural and environmental applications. The adsorption of pH-sensitive dissociable SMX, DCF, IBP, and BPA varied and the order of adsorption capacity was correlated with the hydrophobicity (K{sub ow}) of adsorbates throughout the all adsorbents, whereas adsorption of non-ionizable CBM, ATR, and EE2 in varied pH allowed adsorbents to interact with hydrophobic property

  20. An Overview of Pharmaceutical Excipients: Safe or Not Safe?

    Science.gov (United States)

    Abrantes, Cátia G; Duarte, Dinah; Reis, Catarina P

    2016-07-01

    A medicine consists of 2 fundamental parts: the active pharmaceutical ingredient and the excipient. Most, if not all, medicines could not be made without the use of excipients. In the early times, the safety of excipients was overlooked and no specific safety tests were generally conducted. This fact has been changed over times and is currently being recognized that the excipient's toxicity is not negligible, because its direct interaction with the active pharmaceutical ingredient or between other excipients may occur, leading to a potential change in the relationship between effectiveness and toxicity. This review is intended to address the general status of the pharmaceutical excipients and to describe the safety assessment. As a summary, this review suggests the interest of simplifying the formulations as much as possible and the interest of reducing the number of excipients necessary to strictly meet the required functions. The risk/benefit ratio of an excipient should be always evaluated on the basis of not only its production and quality but also of its safety. Further research according to Good Manufacturing Practices, Guiding Principles in Toxicology Assessment, Good Laboratory Practices, and Good Distribution Practices requirements are needed and are fundamental for health safety, contributing to a comprehensive picture of this matter. PMID:27262205

  1. Using a Mass Balance to Determine the Potency Loss during the Production of a Pharmaceutical Blend

    OpenAIRE

    Mackaplow, Michael B.

    2010-01-01

    The manufacture of a blend containing the active pharmaceutical ingredient (API) and inert excipients is a precursor for the production of most pharmaceutical capsules and tablets. However, if there is a net water gain or preferential loss of API during production, the potency of the final drug product may be less than the target value. We use a mass balance to predict the mean potency loss during the production of a blend via wet granulation and fluidized bed drying. The result is an explici...

  2. Epithermal neutron activation analysis of blue-green algae Spirulina Platensis as a matrix for selenium-containing pharmaceuticals

    International Nuclear Information System (INIS)

    To evaluate the potentiality of the blue-green algae Spirulina Platensis as a matrix for the production of Se-containing pharmaceuticals, the background levels of 31 major, minor and trace elements (Na, Mg, Al, Cl, K, Ca, Sc, V, Cr, Mn, Fe, Co, Ni (using (n,p)-reaction), As, Br, Zn, Rb, Mo, Ag, Sb, I, Ba, Sm, Tb, Tm, Hf, Ta, W, Au, Hg, Th) in Spirulina Platensis biomass were determined by means of epithermal neutron activation analysis. The possibility of the purpose-oriented incorporation of Se into Spirulina Platensis biomass was demonstrated. The polynomial dependence of the Se accumulation on nutritional medium loading was revealed. The employed analytical technique allows one to reliably control the amount of toxic elements in algae Spirulina Platensis. Based on this study, a conclusion of the possibility to use Spirulina Platensis as a matrix for the production of Se-containing pharmaceuticals was drawn

  3. Epithermal neutron activation analysis of blue-green algae Spirulina platensis as a matrix for selenium-containing pharmaceuticals

    International Nuclear Information System (INIS)

    To evaluate the potentiality of the blue-green algae Spirulina platensis as a matrix for the production of Se-containing pharmaceuticals, the background levels of 31 major, minor and trace elements (Na, Mg, Al, Cl, K, Ca, Sc, V, Cr, Mn, Fe, Co, Ni using (n,p) reaction), As, Br, Zn, Rb, Mo, Ag, Sb, I, Ba, Sm, Tb, Tm, Hf, Ta, W, Au, Hg, Th were determined in Spirulina platensis biomass by means of epithermal neutron activation analysis. The possibility of the purpose-oriented incorporation of Se into Spirulina platensis biomass was demonstrated. The polynomial dependence of the Se accumulation on nutritional medium loading was revealed. The analytical technique used allows to control the amount of toxic elements in algae Spirulina platensis. Conclusion of the possibility to use Spirulina platensis as a matrix for the production of Se-containing pharmaceutical was drawn. (author)

  4. 圆孢蘑菇有效成分的定性分析%Qualitative Analysis of Active Ingredients of Agaricus gennadii

    Institute of Scientific and Technical Information of China (English)

    白世俊; 包锦渊

    2012-01-01

    [Objective] The aim was to confirm the active ingredients of Agaricus gennadii. [Method] The water extraction method, alcohol extraction method and petroleum ether extraction method were used to extracted the chemical ingredients of Agaricus gennadii, and analyzed them. [Result]The results show that Agaricus gennadii contains protein,carbohydrates,organic acids,coumarin and lactones,etc. ,may also contains saponins and steroidal triterpenes,but does not contain alkaloids,cardiac glycosides,volatile oils,phenols and tannins,etc. [Conclusion] The study makes people to fully know Agaricus gennadii.%[目的]确定圆孢蘑菇(Agaricus gennadii)的有效成分.[方法]采用水提法、醇提法和石油醚提取法对圆孢蘑菇的有效成分进行定性提取和分析.[结果]圆孢蘑菇中含有蛋白质、糖类、有机酸、香豆素与内酯等物质,可能含有皂苷和甾体三萜类,不含生物碱、强心苷、挥发油、酚类和鞣质等.[结论]该研究可使人们更加清楚地了解圆孢蘑菇.

  5. Evaluation of Bioactive Compounds, Pharmaceutical Quality, and Anticancer Activity of Curry Leaf (Murraya koenigii L.

    Directory of Open Access Journals (Sweden)

    Ali Ghasemzadeh

    2014-01-01

    Full Text Available In this study, we investigated some bioactive compounds and pharmaceutical qualities of curry leaf (Murraya koenigii L. extracts from three different locations in Malaysia. The highest TF and total phenolic (TP contents were observed in the extracts from Kelantan (3.771 and 14.371 mg/g DW, followed by Selangor (3.146 and 12.272 mg/g DW and Johor (2.801 and 12.02 mg/g DW, respectively. High quercetin (0.350 mg/g DW, catechin (0.325 mg/g DW, epicatechin (0.678 mg/g DW, naringin (0.203 mg/g DW, and myricetin (0.703 mg/g DW levels were observed in the extracts from Kelantan, while the highest rutin content (0.082 mg/g DW was detected in the leaves from Selangor. The curry leaf extract from Kelantan exhibited higher concentration of gallic acid (0.933 mg/g DW than that from Selangor (0.904 mg/g DW and Johor (0.813 mg/g DW. Among the studied samples, the ones from Kelantan exhibited the highest radical scavenging activity (DPPH, 66.41% and ferric reduction activity potential (FRAP, 644.25 μm of Fe(II/g followed by those from Selangor (60.237% and 598.37 μm of Fe(II/g and Johor (50.76% and 563.42 μm of Fe(II/g, respectively. A preliminary screening showed that the curry leaf extracts from all the locations exhibited significant anticarcinogenic effects inhibiting the growth of breast cancer cell line (MDA-MB-231 and maximum inhibition of MDA-MB-231 cell was observed with the curry leaf extract from Kelantan. Based on these results, it is concluded that Malaysian curry leaf collected from the North (Kelantan might be potential source of potent natural antioxidant and beneficial chemopreventive agents.

  6. Changes in FDA enforcement activities following changes in federal administration: the case of regulatory letters released to pharmaceutical companies

    Directory of Open Access Journals (Sweden)

    Nguyen Diane

    2013-01-01

    Full Text Available Abstract Background The United States (US Food and Drug Administration (FDA is responsible for the protection of the public health by assuring the safety, effectiveness and security of human drugs and biological products through the enforcement of the Federal Food, Drug and Cosmetic Act (FDCA and related regulations. These enforcement activities include regulatory letters (i.e. warning letters and notice of violation to pharmaceutical companies. A regulatory letter represents the FDA’s first official notification to a pharmaceutical company that the FDA has discovered a product or activity in violation of the FDCA. This study analyzed trends in the pharmaceutical-related regulatory letters released by the FDA during the period 1997–2011 and assessed differences in the average number and type of regulatory letters released during the last four federal administrations. Methods Data derived from the FDA webpage. Information about the FDA office releasing the letter, date, company, and drug-related violation was collected. Regulatory letters were classified by federal administration. Descriptive statistics were performed for the analysis. Results Between 1997 and 2011 the FDA released 2,467 regulatory letters related to pharmaceuticals. FDA headquarters offices released 50.6% and district offices 49.4% of the regulatory letters. The Office of Prescription Drug Promotion released the largest number of regulatory letters (850; 34.5% of the total, followed by the Office of Scientific Investigations (131; 5.3%, and the Office of Compliance (105; 4.3%. During the 2nd Clinton Administration (1997–2000 the average number of regulatory letters per year was 242.8 ± 45.6, during the Bush Administration (2001–2008 it was 120.4 ± 33.7, and during the first three years of the Obama administration (2009–2011 it was 177.7.0 ± 17.0. The average number of regulatory letters released by the Office of Prescription Drug Promotion also varied by

  7. Effects of Mongolian Pharmaceutical Betel Shisanwei Ingredient Pills on the Behavior and Different Cerebral Region Monoamine Neurotransmitters in the Rat Models with Depressive Chronic Stress%蒙药槟榔十三味丸(高尤-13)对抑郁模型大鼠行为学及不同脑区单胺类神经递质的影响

    Institute of Scientific and Technical Information of China (English)

    佟海英; 王旭; 乌吉斯古冷; 白亮凤; 包伍叶; 胡日乐巴根; 李婧; 张月

    2014-01-01

    ingredient pills .Methods:Sixty male Wistar rats were randomly divided into six groups according to the sugar consumption test and body weight (10 rats in each group):Normal control group,Model group, Fluoxetine group and High dose,medium dose and low dose groups of Betel Shisanwei ingredient pills .Except the normal control group,other groups were treated with the chronic unpredictable mild stress stimulation combined with lonely rai -sing for 21days.10mL/kg drugs were given to the rats,once daily,continuously for 21 days.After 21 days,behavior chan-ges of rats were detected through Open -field test,and sugar consumption test and body weight were also measured . HPLC -ECD techniques were used to analyze the levels of prefrontal cortex and hippocampus NE and 5 -HT and DA and their metabolites.Results:Compared with normal control group ,the scores of horizontal activity and vertical activity , sugar consumption decreased significantly in the model group (P <0.01 or P <0.05);Compared with model group,Flu-oxetine group and Betel Shisanwei ingredient pills group got significantly higher scores of horizontal activity ,vertical ac-tivity and sugar consumption (P <0.05 or P <0.01).HPLC -ECD techniques showed that the model rats prefrontal cortex NE,5 -HT,DA,DOPAC,hippocampus 5 -HT,5HIAA,DA content decreased more significantly than those in normal control group(P <0.05 or P <0.01).Betel Shisanwei ingredient pills could increase model rat 's prefrontal cortex NE,5 -HT,DA,DOPAC and hippocampus 5 -HT,5HIAA,DA content, especially the medium and high dose groups were significant(P <0.05 or P <0.01).Conclusion: Betel Shisanwei ingredient pills can improve abnormal behavior of depressive model rats, improve the neurotransmitter NE, 5 -HT, DA and its metabolic product content in rats brain, and it could be one of the important antidepressant effect mechanisms of Betel Shisanwei ingredient pills .

  8. RECENT POTENTIAL USAGE OF SURFACTANT FROM MICROBIAL ORIGIN IN PHARMACEUTICAL AND BIOMEDICAL ARENA: A PERSPECTIVE

    OpenAIRE

    Rath Kalyani; Mishra Bishwambhar; Vuppu Suneetha

    2011-01-01

    The use and potential commercial application of biosurfactant has increased during the past decade which can be used as emulsifiers, de-emulsifiers, wetting and foaming agents, functional food ingredients and as detergents in petroleum, petrochemicals, environmental management, agrochemicals, foods and beverages, cosmetics and pharmaceuticals and in the mining and metallurgical industries. Their antibacterial, antifungal and antiviral activities make them relevant molecules for applications i...

  9. Application of chemical oxidation for removal of pharmaceuticals in wastewater effluents

    OpenAIRE

    Hey, G.; Ledin, A.; la Cour Jansen, J; Hörsing, M.; Antoniou, Maria; Spiliotopoulou, Aikaterini; Andersen, Henrik Rasmus

    2012-01-01

    This study was conducted to evaluate the potential of the chemical oxidation processes chlorine dioxide (ClO2) and ozone (O3) as tertiary steps in wastewater to remove traces of active pharmaceutical ingredients (APIs). Wastewater effluents of varying organic content (COD ~ 30-90 mg/L) were collected from different wastewater treatment plants in Sweden to represent different types of biological treatment. Laboratory-scale batch experiments were carried out employing different doses of ClO2 (0...

  10. Effect of resonant acoustic mixing on pharmaceutical powder blends and tablets

    OpenAIRE

    Osorio, Juan; Sowrirajan, Koushik; Muzzio, Fernando

    2014-01-01

    The blending performance in a resonant acoustic mixer (RAM) was characterized. The system showed to be highly effective in blending low concentrations of cohesive active pharmaceutical ingredients (APIs) and lubricants. A summary of these results will be described and changes in material properties were observed. Those changes, and their effects on tablet characteristics, were also studied. Changes in particle size, powder flow properties, and hydrophobicity of the blend were investigated. Ta...

  11. COMPRESSION PHYSICS OF PHARMACEUTICAL POWDERS: A REVIEW

    Directory of Open Access Journals (Sweden)

    Shailender Mohan

    2012-06-01

    Full Text Available Due to various advantages such as high-precision dosing, manufacturing efficiency and patient compliance helped making tablets the most popular dosage forms among all available dosages forms. Compaction, which is an essential manufacturing step in the manufacture of tablets, mainly includes compression (i.e. reduction of volume of the powder under consideration and particle rearrangement and consolidation (i.e., formation of interparticulate bond to facilitate stable compaction. The success of the compaction process depends not only on the physico-technical properties of drugs and excipients, but also on the instrument settings with respect to rate and magnitude of force transfer. Tablet manufacturing speed and pre/main compression force profile also have an influence on the quality of the final tablet. Mechanical aspects of tablet formation can be studied using, instrumented punches/dies, instrumented tablet punching machines, and compaction simulators. These have potential application in pharmaceutical research and development, such as studying basic compaction mechanism, various process variables, scale-up parameters, trouble shooting problems, creating compaction data library, and fingerprinting of new active pharmaceutical ingredients (APIs or excipients. Mathematical models, force-time, force-distance, and die-wall force parameters of tablet manufacturing are used to describe work of compaction, elasticity/plasticity, and time dependent deformation behavior of pharmaceuticals powder under consideration.

  12. Organic Pesticide Ingredients

    Science.gov (United States)

    ... Control a pest Integrated Pest Management What are pesticides? Herbicides Disinfectants Fungicides Insecticides Natural and Biological Pesticides ... Other types of pesticides Disponible en español Organic Pesticide Ingredients Organic foods are not necessarily pesticide-free. ...

  13. 抗心律失常天然活性成分的研究进展%Research progress of antiarrhythmic natural active ingredients

    Institute of Scientific and Technical Information of China (English)

    方永煌; 岑柏宏; 陈瑞晗; 曹静桦; 黄国杰; 梁燕玲; 董艳芬

    2015-01-01

    Arrhythmias are common in the field of cardiovascular disease. In March 2013, World Health Organization reported that, in 2008 the population who died of cardiovascular disease has been as high as 17.3 million, and by 2030 will increase to 23.3 million. Sudden cardiac death accounts for about 40%-50%, while the majority of sudden cardiac death caused by arrhythmia, so the development of new drugs antiarrhythmic is urgent. In recent years, the development of chemical antiarrhythmic drugs getting into the bottleneck, the value of natural antiarrhythmic drug has gotten the world's attention again. At present, the active ingredient of natural antiarrhythmic drugs mainly are alkaloids, flavonoids, saponins. By a comprehensive analysis of the reported literature, the article generalizes the research progress which is about the active ingredient of natural antiarrhythmic drug in nearly a decade, in order to provide certain basis for further study on the active ingredient of natural drugs.%心律失常是心血管领域的常见病、多发病。2013年3月世界卫生组织报道,2008年死于心脑血管疾病者高达1730万,而到2030年将增至2330万。其中心脏性猝死占40%~50%,而大多数心脏性猝死由心律失常所引发,故抗心律失常新药的研发刻不容缓。近几年化学抗心律药物的研发渐入瓶颈,天然药物抗心律失常的价值重新得到世界的关注。目前天然药物抗心律失常活性成分多为生物碱类、黄酮类、皂苷类。本研究通过综合分析已报道的相关文献,概括近几年抗心律失常的天然药物活性成分研究进展,为天然药物活性成分的进一步研究提供依据。

  14. Cell-based screening identifies the active ingredients from Traditional Chinese Medicine formula Shixiao San as the inhibitors of atherosclerotic endothelial dysfunction.

    Directory of Open Access Journals (Sweden)

    Xiaofan Wang

    Full Text Available In this study, we performed a phenotypic screening in human endothelial cells exposed to oxidized low density lipoprotein (an in vitro model of atherosclerotic endothelial dysfunction to identify the effective compounds in Shixiao San. After investigating the suitability and reliability of the cell-based screening method using atorvastatin as the positive control drug, this method was applied in screening Shixiao San and its extracts. The treatment of n-butanol fraction on endothelial cells exhibited stronger healing effects against oxidized low density lipoprotein-induced insult when compared with other fractions. Cell viability, the level of nitric oxide, endothelial nitric oxide synthase and endothelin-1 were measured, respectively. The assays revealed n-butanol fraction significantly elevated the survival ratio of impaired cells in culture. In parallel, n-butanol fraction exhibited the highest inhibition of inflammation. The generation of prostaglandin-2 and adhesion molecule (soluble intercellular adhesion molecule-1 was obviously declined. Furthermore, n-butanol fraction suppressed the production of reactive oxygen species and malondialdehyde, and restored the activity of superoxide dismutase. Compounds identification of the n-butanol fraction was carried out by ultra high liquid chromatography coupled to quadrupole time-of-flight tandem mass spectrometry. The active ingredients including quercetin-3-O-(2G-α-l-rhamnosyl-rutinoside, quercetin-3-O-neohesperidoside, isorhamnetin-3-O-neohesperidoside and isorhamnetin-3-O-rutinoside revealed the ability of anti-atherosclerosis after exposing on endothelial cells. The current work illustrated the pharmacology effect of Shixiao San and clearly indicated the major active components in Shixiao San. More importantly, the proposed cell-based screening method might be particularly suitable for fast evaluating the anti-atherosclerosis efficacy of Traditional Chinese Medicines and screening out the

  15. Research Progress in the Active Ingredients of Rose & Rose Wine%玫瑰花有效成分及玫瑰花酒的研究进展

    Institute of Scientific and Technical Information of China (English)

    胡晓燕; 沈才洪; 敖宗华; 杨学琴; 黄张君; 钟霞

    2014-01-01

    玫瑰花具有令人愉悦的香气,是一种适合开发保健酒的良好原料。主要对玫瑰花的有效成分、有效成分的提取方法、有效成分应用功能、玫瑰花酒生产等的研究进展作了简要的综述。%Rose has pleasant aroma and is suitable for the development of healthcare wine. In this paper, the research progress in the active ingre-dients of rose and their extraction and application, and the production of rose wine was reviewed.

  16. Review on active ingredients from Cannabis sativa leaves and its pharmacological characteristics%汉麻叶活性成分及其药理特性的研究概况

    Institute of Scientific and Technical Information of China (English)

    杜军强; 何锦风; 何聪芬; 蒲彪; 李靖宇; 蒋勇

    2011-01-01

    Cannabis saliva leaves contains a variety of active ingredients, including cannabinoid and non -cannabinoid. Active ingredients from Cannahis saliva leaves have a high application value in the pharmacy and other fields. In this paper, the pharmacological characteristics of cannabinoid, non-cannabinoid and unknown active ingredients was summarized.%汉麻叶含有多种活性成分,包括大麻酚类化合物和非大麻酚类化合物.汉麻叶的活性成分在医药等领域有极高的应用价值.本文就大麻酚类化合物,非大麻酚类化合物和未知活性成分的药理特性展开综述.

  17. Efficacy of attractive toxic sugar baits (ATSB) against Aedes albopictus with garlic oil encapsulated in beta-cyclodextrin as the active ingredient.

    Science.gov (United States)

    Junnila, Amy; Revay, Edita E; Müller, Gunter C; Kravchenko, Vasiliy; Qualls, Whitney A; Xue, Rui-de; Allen, Sandra A; Beier, John C; Schlein, Yosef

    2015-12-01

    We tested the efficacy of attractive toxic sugar bait (ATSB) with garlic oil microencapsulated in beta-cyclodextrin as active ingredient against Aedes albopictus in suburban Haifa, Israel. Two three-acre gardens with high numbers of Ae. albopictus were selected for perimeter spray treatment with ATSB and ASB (bait containing no active ingredient). Baits were colored with food dye to verify feeding of the mosquitoes. The mosquito population was monitored by human landing catches and sweep net catches in the surrounding vegetation. Experiments lasted for 44 days. Treatment occurred on day 13. The mosquito population collapsed about 4 days after treatment and continued to drop steadily for 27 days until the end of the study. At the experimental site the average pre-treatment landing rate was 17.2 per 5mins. Two days post-treatment, the landing rate dropped to 11.4, and continued to drop to an average of 2.6 during the following 26 days. During the same period, the control population was stable. Few sugar fed females (8-10%) approached a human bait and anthrone tests showed relatively small amounts of sugar within their crop/gut. Around 60-70 % of males caught near our human bait were sugar positive which may indicate that the males were feeding on sugar for mating related behavior. From the vegetation treated with the toxic bait, we recovered significantly fewer (about 10-14%) males and females stained by ATSB than at the ASB-treated control. This may indicate that the toxic baits alter the resting behavior of the poisoned mosquitoes within the vegetation. Almost no Ae. albopictus females (5.2±1.4) approached human bait after treatment with ATSB. It therefore appears that microencapsulated garlic oil is an effective pesticide against Ae. albopictus when used in an ATSB system.

  18. Characterization of pharmaceutically active compounds in Dongting Lake, China: Occurrence, chiral profiling and environmental risk.

    Science.gov (United States)

    Ma, Ruixue; Wang, Bin; Lu, Shaoyong; Zhang, Yizhe; Yin, Lina; Huang, Jun; Deng, Shubo; Wang, Yujue; Yu, Gang

    2016-07-01

    Twenty commonly used pharmaceuticals including eight chiral drugs were investigated in Dongting Lake, China. The contamination level was relatively low on a global scale. Twelve pharmaceuticals were identified. The most abundant compound was caffeine followed by diclofenac, DEET, mefenamic acid, fluoxetine, ibuprofen and carbamazepine with mean concentrations from 2.0 to 80.8ngL(-1). Concentrations between East and West Dongting Lake showed spatial difference, with the West Dongting Lake less polluted. The relatively high ratio of caffeine versus carbamazepine (over 50) may indicate there was possible direct discharge of domestic wastewater into the lake. This is the first study presenting a survey allowing for comprehensive analysis of multiclass achiral and chiral pharmaceuticals including beta-blockers, antidepressants and anti-inflammatory drugs in freshwater lake. The enantiomeric compositions presented racemic to weakly enantioselective, with the highest enantiomeric fraction (EF) of 0.63 for fluoxetine. Meanwhile, venlafaxine was identified and evaluated the environment risk in surface water in China for the first time. The results of risk assessment suggested that fluoxetine, venlafaxine and diclofenac acid might pose a significant risk to aquatic organisms in Dongting Lake. The resulting data will be useful to enrich the research of emerging pollutants in freshwater lake and stereochemistry for environment investigations. PMID:27016674

  19. The on-line analysis of aerosol-delivered pharmaceuticals via single particle aerosol mass spectrometry.

    Science.gov (United States)

    Morrical, Bradley D; Balaxi, Maria; Fergenson, David

    2015-07-15

    The use of single particle aerosol mass spectrometry (SPAMS) was evaluated for the analysis of inhaled pharmaceuticals to determine the mass distribution of the individual active pharmaceutical ingredients (API) in both single ingredient and combination drug products. SPAMS is an analytical technique where the individual aerodynamic diameters and chemical compositions of many aerosol particles are determined in real-time. The analysis was performed using a Livermore Instruments SPAMS 3.0, which allowed the efficient analysis of aerosol particles with broad size distributions and can acquire data even under a very large particle load. Data similar to what would normally require roughly three days of experimentation and analysis was collected in a five minute period and analyzed automatically. The results were computed to be comparable to those returned by a typical Next Generation Impactor (NGI) particle size distribution experiment.

  20. Oxidation of pharmaceuticals by chlorine dioxide in biologically treated wastewater

    OpenAIRE

    Hey, G.; Grabic, R.; Ledin, A.; la Cour Jansen, J; Andersen, H R

    2012-01-01

    Biologically treated wastewater spiked with a mixture of 56 active pharmaceutical ingredients (APIs) was treated with 0–20mg/L chlorine dioxide (ClO2) solution in laboratory-scale experiments. Wastewater effluents were collected from two wastewater treatment plants in Sweden, one with extended nitrogen removal (low COD) and one without (high COD). About one third of the tested APIs resisted degradation even at the highest ClO2 dose (20mg/L), while others were reduced by more than 90% at the l...

  1. PBT assessment and prioritization of contaminants of emerging concern: Pharmaceuticals.

    Science.gov (United States)

    Sangion, Alessandro; Gramatica, Paola

    2016-05-01

    The strong and widespread use of pharmaceuticals, together with incorrect disposal procedures, has recently made these products contaminants of emerging concern (CEC). Unfortunately, little is known about pharmaceuticals' environmental behaviour and ecotoxicity, so that EMEA (European Medicines Agency) released guidelines for the pharmaceuticals' environmental risk assessment. In particular, there is a severe lack of information about persistence, bioaccumulation and toxicity (PBT) of the majority of the thousands of substances on the market. Computational tools, like QSAR (Quantitative Structure Activity Relationship) models, are the only way to screen large sets of chemicals in short time, with the aim of ranking, highlighting and prioritizing the most environmentally hazardous for focusing further experimental studies. In this work we propose a screening method to assess the potential persistence, bioaccumulation and toxicity of more than 1200 pharmaceutical ingredients, based on the application of two different QSAR models. We applied the Insubria-PBT Index, a MLR (Multiple Linear Regression) QSAR model based on four simple molecular descriptors, implemented in QSARINS software, and able to synthesize the PBT potential in a unique cumulative value and the US-EPA PBT Profiler that assesses the PBT behaviour evaluating separately P, B and T. Particular attention was given to the study of Applicability Domain in order to provide reliable predictions. An agreement of 86% was found between the two models and a priority list of 35 pharmaceuticals, highlighted as potential PBTs by consensus, was proposed for further experimental validation. Moreover, the results of this computational screening are in agreement with preliminary experimental data in the literature. This study shows how in silico models can be applied in the hazard assessment to perform preliminary screening and prioritization of chemicals, and how the identification of the structural features, mainly

  2. Aryl Hydrocarbon Receptor (AHR)-Active Pharmaceuticals Are Selective AHR Modulators in MDA-MB-468 and BT474 Breast Cancer Cells

    OpenAIRE

    Jin, Un-Ho; Lee, Syng-Ook; Safe, Stephen

    2012-01-01

    Leflunomide, flutamide, nimodipine, mexiletine, sulindac, tranilast, 4-hydroxytamoxifen, and omeprazole are pharmaceuticals previously characterized as aryl hydrocarbon receptor (AHR) agonists in various cell lines and animal models. In this study, the eight AHR-active pharmaceuticals were investigated in highly aggressive aryl hydrocarbon (Ah)-responsive BT474 and MDA-MB-468 breast cancer cell lines, and their effects on AHR protein, CYP1A1 (protein and mRNA), CYP1B1 (mRNA), and cell migrati...

  3. Pharmaceutical Economics

    OpenAIRE

    2008-01-01

    Pharmaceutical Economics begins with an investigation of the structure of the industry and its three main components: the research firms which produce innovative products; the generic drug industry and its expanding role; and the biotech industry, which is regarded as the future for pharmaceuticals. Further sections discuss topics including demand and incentives, pricing and regulation.

  4. Suggestions on Improving Supervision of Active Pharmaceutical Ingredients in China%提高我国原料药监管水平的几点设想

    Institute of Scientific and Technical Information of China (English)

    马云鹏; 叶桦

    2012-01-01

    目的 为加强原料药监管提出建议.方法 分析原料药产业监管现状和存在的问题.结果与结论 应结合中国的国情,完善监管法规与制度,建立以原料药目录为依据的管理模式,强化GMP对原料药的规范内容,加强流通与出口管理,积极参与国际联合监管.

  5. 山茱萸炮制前后药效成分含量的变化%Content Changes of Activated Pharmaceutical Ingredients from Cornus Officinalis during Processing

    Institute of Scientific and Technical Information of China (English)

    赵玉丛; 杨卫华; 刘国际

    2007-01-01

    目的 对山茱萸炮制前后药效成分的含量进行比较研究.方法 分别采用高效液相色谱法和比色法对山茱萸生品和炮制品中的熊果酸和总皂苷的含量进行测定.结果 山茱萸酒蒸品与生品相比,熊果酸的含量增加,而总皂苷的含量却有所下降.结论 山茱萸的加工炮制对其有效成分含量的影响有所不同,临床入药应区别对待.

  6. 炮制对山茱萸中药效成分的影响%Effects of Processing on the Activated Pharmaceutical Ingredients from Cornus officinalis

    Institute of Scientific and Technical Information of China (English)

    赵玉丛; 李存法; 刘国际

    2008-01-01

    [目的]系统考察了炮制对中药山茱萸药效成分的影响,并初步探讨了山茱萸炮制前后其药理作用发生变化的相关物质基础.[方法]结合试验研究与文献综述,分别对山茱萸生品、酒蒸品中各类药效成分的含量进行考察.[结果]山茱萸酒蒸后苷类成分的含量均有所下降,而有机酸类成分、多糖类成分、与肝肾有关的药用氨基酸及微量元素的含量均有所增加.[结论]山茱萸炮制前后药理作用的差异与其物质基础密切相关.山茱萸临床入药是否进行加工炮制应取决于其具体临床应用.

  7. 浅谈国外客户对原料药的质量审计%Quality Audit of Active Pharmaceutical Ingredients by Foreign Clients

    Institute of Scientific and Technical Information of China (English)

    温耀明

    2012-01-01

    目的 浅析国外客户对原料药的质量审计.方法 介绍了质量审计的目的和特点,并针对客户审计的重点,按审计过程进行详细论述和分析.结果与结论 在准备和接受国外客户质量审计的活动中,完善了自身的质量管理体系,提高了企业的产品质量水平和国际市场竞争力.

  8. Analysis of FDA Inspection on GMP Conformance for the Manufacturing of Active Pharmaceutical Ingredients%谈谈FDA对原料药的GMP现场检查

    Institute of Scientific and Technical Information of China (English)

    吕冬梅; 史玮

    2010-01-01

    目的浅析FDA对原料药的GMP现场检查.方法针对FDA关于原料药GMP现场检查的重点进行详细论述和分析.结果与结论 企业如果建立了有效的GMP制度,那么企业完全能够通过FDA的认证.

  9. 急需开发的原料药--头孢克肟%Cefixime:An Active Pharmaceutical Ingredient to be Development Urgently

    Institute of Scientific and Technical Information of China (English)

    张诗海; 赵美法

    2003-01-01

    头孢克肟抗菌谱广、半衰期长、交叉耐药性小、用药剂量小、适应症广泛.该药专利已于2001年7月到期,是我国重点开发的第三代口服头孢菌素之一.头孢克肟的合成路线有两条:7-ACA工艺和脱乙酰头孢菌素C工艺.该药目前在欧洲的年销售额约2亿美元.

  10. Sterilization Process Validation of Aseptic Active Pharmaceutical Ingredient%无菌原料药生产的无菌工艺验证

    Institute of Scientific and Technical Information of China (English)

    翟铁伟; 韩志伟

    2004-01-01

    介绍了无菌原料药无菌工艺验证的一般过程和注意事项,包括验证前准备、验证实施、最终报告和再验证,以及人员培训、操作时限、模拟介质的选择和灭菌、环境监测、取样和样品培养等.

  11. Developments of China's Active Pharmaceutical Ingredients Industry%国内原料药产业动态及发展建议

    Institute of Scientific and Technical Information of China (English)

    汤方毅; 吴泉

    2003-01-01

    我国原料药年产量达56万t,是世界第二大原料药生产国.出口量占总产量的30%~40%,2001年出口额为19.2亿美元.产量大、劳动力成本低、技术水平不断提高成为我国原料药制造业的优势.在世界原料药生产中心向发展中国家转移的过程中,印度将成为我国的主要竞争对手,我国企业应通过技术创新来加强竞争力.

  12. 药品中遗传毒性杂质的评估和控制%Evaluation and Control of Genotoxic Impurities in Active Pharmaceutical Ingredients

    Institute of Scientific and Technical Information of China (English)

    张慧敏; 林建群; 冯康彪; 杜有功; 王红; 孙渊

    2014-01-01

    目的 综述药品遗传毒性杂质控制相关指南和法规,为制药企业执行国际标准和准则提供一些建议和思路.方法 通过查找数据库如Pubmed、Medline及欧洲药品管理局(European Medicines Agency,EMA)、美国食品药品监督管理局(USFood and Drug Administratio,U.S.FDA)、人用药品注册技术要求国际协调会议(ICH)等网站,比较各指南法规关于遗传毒性控制限度和控制措施的异同点,为遗传毒性杂质的控制提供一个可行性步骤.结果 通过比较发现,EMA、U.S.FDA和即将出版的ICH M7指南在关键原则的应用方面如毒理学关注阈值(threshold of toxicological concern,TTC)、风险评估步骤、杂质5分类法等基本相同,但现行EMA和U.S.FDA法规存在分歧,不利于其有效执行,而ICH M7将为遗传毒性杂质的控制提供一个可行框架.结论 目前还缺乏完善有效的遗传毒性控制指南,ICH M7将解决U.S.FDA和EMA指南间分歧,更好地指导制药企业遗传毒性杂质的控制.

  13. 药用化工原料监管政策的研究%Discussion on Regulatory Policy for Active Pharmaceutical Ingredient

    Institute of Scientific and Technical Information of China (English)

    王岩; 张启明; 孙磊

    2011-01-01

    目的 探讨药用化工原料的监管政策.方法 对比研究国内外原料药监管政策以及分析我国原料药的生产现状.结果与结论 应通过法律法规的完善、国际间的政府合作、提高技术准入标准等手段,加强对药用化工原料的监管.

  14. Whole-bowel irrigation versus activated charcoal in sorbitol for the ingestion of modified-release pharmaceuticals.

    Science.gov (United States)

    Kirshenbaum, L A; Mathews, S C; Sitar, D S; Tenenbein, M

    1989-09-01

    Overdose with modified-release pharmaceuticals is an increasing phenomenon. This study examines whole-bowel irrigation as a potential decontamination strategy after overdose with enteric-coated acetylsalicylic acid and compares it with administration of activated charcoal in sorbitol, which is currently the recommended intervention. A three-phase randomized crossover protocol was used in 10 adult volunteers. Each volunteer ingested nine 325 mg doses of enteric-coated acetylsalicylic acid on three occasions, with at least 1 week between each administration period. Serum samples were analyzed for salicylic acid concentration by HPLC. Both interventions decreased peak salicylic acid concentration, time-to-zero salicylic acid concentration, and AUC when compared with control (p less than 0.01). Whole-bowel irrigation was superior to activated charcoal in sorbitol by all three criteria (p less than 0.05). Adverse effects were qualitatively and quantitatively greater during activated charcoal in sorbitol, and the volunteers preferred whole-bowel irrigation over charcoal in sorbitol. Our data suggest that whole-bowel irrigation should be considered for overdose of other modified-release pharmaceuticals. PMID:2673619

  15. Pharmaceutically active compounds and endocrine disrupting chemicals in water, sediments and mollusks in mangrove ecosystems from Singapore.

    Science.gov (United States)

    Bayen, Stéphane; Estrada, Elvagris Segovia; Juhel, Guillaume; Kit, Lee Wei; Kelly, Barry C

    2016-08-30

    This study investigated the occurrence of bisphenol A (BPA), atrazine and selected pharmaceutically active compounds (PhACs) in mangrove habitats in Singapore in 2012-2013, using multiple tools (sediment sampling, POCIS and filter feeder molluscs). Using POCIS, the same suite of contaminants (atrazine, BPA and eleven PhACs) was detected in mangrove waters in 28-days deployments in both 2012 and 2013. POCIS concentrations ranged from pg/L to μg/L. Caffeine, BPA, carbamazepine, E1, triclosan, sulfamerazine, sulfamethazine, and lincomycin were also detected in mangrove sediments from the low pg/g dw (e.g. carbamazepine) to ng/g dw (e.g. BPA). The detection of caffeine, carbamazepine, BPA, sulfamethoxazole or lincomycin in bivalve tissues also showed that these chemicals are bioavailable in the mangrove habitat. Since there are some indications that some pharmaceutically active substances may be biologically active in the low ppb range in marine species, further assessment should be completed based on ecotoxicological data specific to mangrove species. PMID:27393211

  16. Field-scale monitoring of pharmaceutical compounds applied to active golf courses by recycled water.

    Science.gov (United States)

    Young, M H; Green, R L; Conkle, J L; McCullough, M; Devitt, D A; Wright, L; Vanderford, B J; Snyder, S A

    2014-03-01

    The scarcity of potable water in arid and semiarid environments has led to the wider use of recycled water for irrigating agricultural fields, parks, golf courses, and other areas. One concern using recycled water as a source of irrigation has been the presence, fate, and transport of pharmaceutical compounds in water that percolates below the root zone of plants; however, very few multiyear field studies have been reported in the peer-reviewed literature. Here, we assessed compound mass flux of 13 pharmaceuticals in the fairways of four golf courses in the southwestern United States during a 2-yr field study. The sites varied by climate and soil type but were similar regarding turfgrass management. The results showed the presence of at least one pharmaceutical compound in nearly all samples collected, although concentrations were substantially lower after transport through the soil. Percent reduction in compound mass fluxes in drainage water was effectively 100% in 22 of 52 cases, 98 to 100% in 27 of 52 cases, and 73 to 94% in 3 of 52 cases (a case is defined as a specific compound measured at a specific site). Mass fluxes migrating below the root zone were calculated as 100 × 10 g ha in only two cases. For cases where the majority of the analyses were reportable, all fluxes were <8.80 × 10 g ha. Carbamazepine, meprobamate, and sulfamethoxazole were most commonly found in drainage water, representing nearly 80% of all reportable detections. This research demonstrates the potential of turfgrass/soil systems to reduce contaminant loading below the root zone and potentially toward groundwater. PMID:25602667

  17. Pharmaceutical cocrystals of diflunisal and diclofenac with theophylline.

    Science.gov (United States)

    Surov, Artem O; Voronin, Alexander P; Manin, Alex N; Manin, Nikolay G; Kuzmina, Lyudmila G; Churakov, Andrei V; Perlovich, German L

    2014-10-01

    Pharmaceutical cocrystals of nonsteroidal anti-inflammatory drugs diflunisal (DIF) and diclofenac (DIC) with theophylline (THP) were obtained, and their crystal structures were determined. In both of the crystal structures, molecules form a hydrogen bonded supramolecular unit consisting of a centrosymmetric dimer of THP and two molecules of active pharmaceutical ingredient (API). Crystal lattice energy calculations showed that the packing energy gain of the [DIC + THP] cocrystal is derived mainly from the dispersion energy, which dominates the structures of the cocrystals. The enthalpies of cocrystal formation were estimated by solution calorimetry, and their thermal stability was studied by differential scanning calorimetry. The cocrystals showed an enhancement of apparent solubility compared to the corresponding pure APIs, while the intrinsic dissolution rates are comparable. Both cocrystals demonstrated physical stability upon storing at different relative humidity.

  18. Compatibility and stability of valsartan in a solid pharmaceutical formulation

    Directory of Open Access Journals (Sweden)

    Tamíris Amanda Júlio

    2013-12-01

    Full Text Available Valsartan (VAL is a highly selective blocker of the angiotensin II receptor that has been widely used in the treatment of hypertension. Active pharmaceutical ingredient compatibility with excipients (crospovidone, hypromellose, magnesium stearate, microcrystalline cellulose and titanium dioxide is usually evaluated in solid pharmaceutical development. Compatibility and stability can be evaluated by liquid chromatography. Studies were performed using binary mixtures of 1:1 (w/w VAL/excipient; samples were stored under accelerated stability test conditions (40 ºC at 75% relative humidity. The results indicate that VAL is incompatible with crospovidone and hypromellose, which reduced the VAL content and gave rise to new peaks in the chromatogram due to degradation products.

  19. Structural characterization of pharmaceutical heparins prepared from different animal tissues.

    Science.gov (United States)

    Fu, Li; Li, Guoyun; Yang, Bo; Onishi, Akihiro; Li, Lingyun; Sun, Peilong; Zhang, Fuming; Linhardt, Robert J

    2013-05-01

    Although most pharmaceutical heparin used today is obtained from porcine intestine, heparin has historically been prepared from bovine lung and ovine intestine. There is some regulatory concern about establishing the species origin of heparin. This concern began with the outbreak of mad cow disease in the 1990s and was exacerbated during the heparin shortage in the 2000s and the heparin contamination crisis of 2007-2008. Three heparins from porcine, ovine, and bovine were characterized through state-of-the-art carbohydrate analysis methods with a view profiling their physicochemical properties. Differences in molecular weight, monosaccharide and disaccharide composition, oligosaccharide sequence, and antithrombin III-binding affinity were observed. These data provide some insight into the variability of heparins obtained from these three species and suggest some analytical approaches that may be useful in confirming the species origin of a heparin active pharmaceutical ingredient. PMID:23526651

  20. Characterizing dense suspensions: two case studies from the pharmaceutical industry

    Science.gov (United States)

    Goldfarb, David J.; Khawaja, Nazia; Kazakevich, Irina; Bhattacharjee, Himanshu; Heslinga, Michael; Dalton, Chad

    2015-11-01

    Liquid suspensions of Active Pharmaceutical Ingredient powders are present as pharmaceutical dosage forms in the form of oral suspensions and injectables. We present two case studies, both dense (~ 30-40%) suspensions, in which the physical characterization of the product, specifically, particle size & shape and rheology were key to understanding the key product attributes as pertaining to the manufacturing process and to patient administration. For the one case study, an oral suspension, identifying variations in particle morphology during the wet milling of the product was key to the product understanding necessary to modify the milling process. Rheological measurements were applied as well. For the second case study, an injectable, results from different particle size measurement techniques and rheological measurements indicated the possibility of flocculation in a formulation. Additionally, measurements were obtained to assess the ``injectability'' of the product via rheometer and texture analyzer measurements and Poiseuille flow modeling. As a result, the relevant shear rate regime for this drug product administration was identified.

  1. Preparation of ultrafine magnetic biochar and activated carbon for pharmaceutical adsorption and subsequent degradation by ball milling.

    Science.gov (United States)

    Shan, Danna; Deng, Shubo; Zhao, Tianning; Wang, Bin; Wang, Yujue; Huang, Jun; Yu, Gang; Winglee, Judy; Wiesner, Mark R

    2016-03-15

    Ball milling was used to prepare two ultrafine magnetic biochar/Fe3O4 and activated carbon (AC)/Fe3O4 hybrid materials targeted for use in pharmaceutical removal by adsorption and mechanochemical degradation of pharmaceutical compounds. Both hybrid adsorbents prepared after 2h milling exhibited high removal of carbamazepine (CBZ), and were easily separated magnetically. These adsorbents exhibited fast adsorption of CBZ and tetracycline (TC) in the initial 1h. The biochar/Fe3O4 had a maximum adsorption capacity of 62.7mg/g for CBZ and 94.2mg/g for TC, while values obtained for AC/Fe3O4 were 135.1mg/g for CBZ and 45.3mg/g for TC respectively when data were fitted using the Langmuir expression. Solution pH values slightly affected the sorption of TC on the adsorbents, while CBZ sorption was almost pH-independent. The spent adsorbents with adsorbed CBZ and TC were milled to degrade the adsorbed pollutants. The adsorbed TC itself was over 97% degraded after 3h of milling, while about half of adsorbed CBZ were remained. The addition of quartz sand was found to improve the mechanochemical degradation of CBZ on biochar/Fe3O4, and its degradation percent was up to 98.4% at the dose of 0.3g quarts sand/g adsorbent. This research provided an easy method to prepare ultrafine magnetic adsorbents for the effective removal of typical pharmaceuticals from water or wastewater and degrade them using ball milling.

  2. Preparation of ultrafine magnetic biochar and activated carbon for pharmaceutical adsorption and subsequent degradation by ball milling.

    Science.gov (United States)

    Shan, Danna; Deng, Shubo; Zhao, Tianning; Wang, Bin; Wang, Yujue; Huang, Jun; Yu, Gang; Winglee, Judy; Wiesner, Mark R

    2016-03-15

    Ball milling was used to prepare two ultrafine magnetic biochar/Fe3O4 and activated carbon (AC)/Fe3O4 hybrid materials targeted for use in pharmaceutical removal by adsorption and mechanochemical degradation of pharmaceutical compounds. Both hybrid adsorbents prepared after 2h milling exhibited high removal of carbamazepine (CBZ), and were easily separated magnetically. These adsorbents exhibited fast adsorption of CBZ and tetracycline (TC) in the initial 1h. The biochar/Fe3O4 had a maximum adsorption capacity of 62.7mg/g for CBZ and 94.2mg/g for TC, while values obtained for AC/Fe3O4 were 135.1mg/g for CBZ and 45.3mg/g for TC respectively when data were fitted using the Langmuir expression. Solution pH values slightly affected the sorption of TC on the adsorbents, while CBZ sorption was almost pH-independent. The spent adsorbents with adsorbed CBZ and TC were milled to degrade the adsorbed pollutants. The adsorbed TC itself was over 97% degraded after 3h of milling, while about half of adsorbed CBZ were remained. The addition of quartz sand was found to improve the mechanochemical degradation of CBZ on biochar/Fe3O4, and its degradation percent was up to 98.4% at the dose of 0.3g quarts sand/g adsorbent. This research provided an easy method to prepare ultrafine magnetic adsorbents for the effective removal of typical pharmaceuticals from water or wastewater and degrade them using ball milling. PMID:26685062

  3. Aryl hydrocarbon receptor (AHR)-active pharmaceuticals are selective AHR modulators in MDA-MB-468 and BT474 breast cancer cells.

    Science.gov (United States)

    Jin, Un-Ho; Lee, Syng-ook; Safe, Stephen

    2012-11-01

    Leflunomide, flutamide, nimodipine, mexiletine, sulindac, tranilast, 4-hydroxytamoxifen, and omeprazole are pharmaceuticals previously characterized as aryl hydrocarbon receptor (AHR) agonists in various cell lines and animal models. In this study, the eight AHR-active pharmaceuticals were investigated in highly aggressive aryl hydrocarbon (Ah)-responsive BT474 and MDA-MB-468 breast cancer cell lines, and their effects on AHR protein, CYP1A1 (protein and mRNA), CYP1B1 (mRNA), and cell migration were determined. 2,3,7,8-Tetrachlorodibenzo-p-dioxin (TCDD) was used as a positive control. The AHR agonist activities of the pharmaceuticals depended on structure, response, and cell context. Most compounds induced one or more AHR-mediated responses in BT474 cells, whereas in Ah-responsive MDA-MB-468 cells effects of the AHR-active pharmaceuticals were highly variable. 4-Hydroxytamoxifen, mexiletine, and tranilast did not induce CYP1A1 in MDA-MB-468 cells; moreover, in combination with TCDD, mexiletine was a potent AHR antagonist, tranilast was a partial antagonist, and 4-hydroxytamoxifen also exhibited some AHR antagonist activity. Omeprazole and, to a lesser extent, sulindac and leflunomide were full and partial AHR agonists, respectively, in both breast cancer cell lines. These data indicate that the AHR-active pharmaceuticals are selective AHR modulators, and applications of these drugs for targeting the AHR must be confirmed by studies using the most relevant cell context. PMID:22879383

  4. Functional ingredients from microalgae

    NARCIS (Netherlands)

    Buono, S.; Langellotti, A.L.; Martello, A.; Rinna, F.; Fogliano, V.

    2014-01-01

    A wide variety of natural sources are under investigation to evaluate their possible use for new functional ingredient formulation. Some records attested the traditional and ancient use of wild harvested microalgae as human food but their cultivation for different purposes started about 40 years ago

  5. Rapid isolation and identification of active antioxidant ingredients from Gongju using HPLC-DAD-ESI-MS(n) and postcolumn derivatization.

    Science.gov (United States)

    Cui, Gang; Niu, Yaru; Wang, Hong; Dong, Jing; Yuki, Hashi; Chen, Shizhong

    2012-05-30

    Flos Chrysanthemi (Gongju, GJ) is used to prepare a herbal tea that is commonly consumed as a health beverage in Asia and is believed to contain abundant beneficial antioxidants. To rapidly identify the chemical constituents and to obtain the profile related to antioxidant activity, an online analytical method combining high-performance liquid chromatography-diode-array detector-electrospray ionization-ion-trap time-of-flight mass spectrometry (HPLC-DAD-ESI-IT-TOF-MS(n)) and postcolumn derivatization (PCD) has been applied for a precise and thorough identification of the chemical constituents. Meanwhile, the antioxidant profile has also been characterized by directly measuring the scavenging activity of each compound for the free radical produced by DPPH. As a result, 13 compounds have been identified in GJ, 7 of which account for its antioxidant activity. The established LC-MS(n)-PCD system has proved to offer a useful strategy for correlating the chemical profile with the bioactivities of the components without their isolation and purification, and may be used for multicomponent analysis of active substances in other foods and herbs. PMID:22540938

  6. Bioassay-tracked temperature-stress-induced chemical degradation of bio-active wound healing antibacterial extract of Dissotis theifolia stem dispersed in a pharmaceutical cream and ointment

    Directory of Open Access Journals (Sweden)

    D C Odimegwu

    2011-03-01

    Full Text Available Summary: Owing to the present upsurge in the utilization of medicinal herbal preparations, routine quality control assessment for their continued efficacy and safety is essential if the products are to continue to maintain their pharmacological usefulness under harsh use and storage temperature normally experienced, particularly in the tropics. As herbal medicinal products are complex mixtures which originate from biological sources and are therefore very variable and difficult to characterize, great efforts are necessary to guarantee a constant and adequate quality of potency and safety through selection of an appropriate analytical method for the monitoring of the active ingredient content of such products. Dissotis theifolia is a commonly used plant in traditional herbal medicine for the treatment of several medical ailments, including topical bacterial infections, among several communities in Nigeria. In this present study, the quality control monitoring of the content of active ingredient of pharmaceutical cream and ointment containing the methanol extract of the stem exposed to variegated temperatures was established using a specific microbiological assay method. Results showed reduction of potency of the formulated extracts due to chemical degradation through the first order reaction pathway. The ointment formulation demonstrated a longer half-life and shelf-life being more stable than the cream.   Industrial relevance: Herbal medicine, a form of complimentary and alternative medicine, is becoming increasingly popular in both developing and developed countries. However, there appear to be limited data on their temperature-induce chemical stability/instability profile which correspondingly impinges on their efficacy and safety. In view of this study involving stem extract of D. theifolia formulated as cream and ointment, appropriate bioassay-based techniques can be employed in monitoring the potency of herbal preparations and can serve as

  7. Pharmaceutical Frenzy

    Institute of Scientific and Technical Information of China (English)

    LAN XINZHEN

    2010-01-01

    @@ When shares of Shanghai Pharmaceutical(Group)Co.Ltd.(Shanghai Pharma)resumed normal transactions on March9,2010,the biggest listed pharmaceutical company on China's stock market was born.By the time the closing bell rang at the end of the trading day,the market value of Shanghai Pharma had reached 32.28 billion yuan($4.73 billion).

  8. Antimicrobial activity of a traditionally used complex essential oil distillate (Olbas(®) Tropfen) in comparison to its individual essential oil ingredients.

    Science.gov (United States)

    Hamoud, Razan; Sporer, Frank; Reichling, Jürgen; Wink, Michael

    2012-08-15

    Plant extracts and essential oils have been widely studied and used as antimicrobial agents in the last decades. In our study we investigated the antimicrobial activities of Olbas(®) Tropfen (in the following named Olbas), a traditionally used complex essential oil distillate, in comparison to its individual essential oil ingredients. Olbas (10 g) consists of three major components such as peppermint oil (5.3 g), eucalyptus oil (2.1 g), and cajuput oil (2.1 g) and of two minor constituents like juniper berry oil (0.3 g) and wintergreen oil (0.2 g). The composition of Olbas and the five individual essential oils were characterized by GLC-MS. According to GLC-MS analysis 1,8-cineol is the main component of the complex essential oil distillate followed by menthol and menthone. The minimum inhibitory and minimum microbicidal concentrations of Olbas and each of the single essential oils were evaluated in 17 species/strains of bacteria and fungi. Time-kill assay was performed to compare the microbicidal activity of Olbas and peppermint oil during several time intervals. Olbas displayed a high antimicrobial activity against all test strains used in this study, among them antibiotic resistant MRSA (methicillin-resistant Staphylococcus aureus) and VRE (vancomycin-resistant Enterococcus). Its antimicrobial activity was comparable to that of peppermint oil which was the most potent one of all individual essential oils tested. In the time kill assay Olbas as well as peppermint oil demonstrated similar microbicidal activities. Based on its wide antimicrobial properties Olbas can be a useful agent for the treatment of uncomplicated infections of skin and respiratory tract. PMID:22739414

  9. SIMULTANEOUS ESTIMATION OF SAXAGLIPTIN HYDROCHLORIDE AND METFORMIN HYDROCHLORIDE IN ACTIVE PHARMACEUTICAL INGRIDENT BY RP-HPLC

    Directory of Open Access Journals (Sweden)

    NYOLA NARENDRA, GOVINDASAMY JEYABALAN

    2013-09-01

    Full Text Available A new simple, accurate, precise and reproducible RP-HPLC method has been developed for the simultaneousestimation of Saxagliptin and Metformin in bulk drug form using C18 column (Phenomenex, 250 x 4.6 mm, 5 μm inisocratic mode. The mobile phase consisted of 0.02M Potassium dihydrogen phosphate (KH2PO4, Acetonitrile,Methanol in the ratio of 50:25:25 (v/v/v at pH 4.3. The detection wavelength was carried out at 240 nm. Themethod was linear over the concentration range for Saxagliptin 10-50μg/ml and for Metformin 5-25 μg/ml. Therecoveries of Saxagliptin and Metformin were found to be 100.48and 101.1% respectively. The validation of methodwas carried out utilizing ICH-guidelines. The described HPLC method was successfully employed for the analysisof pharmaceutical formulations containing combined dosage form.

  10. Extraction and Separation of Active Ingredients in Schisandra chinensis (Turcz. Baill and the Study of their Antifungal Effects.

    Directory of Open Access Journals (Sweden)

    Haijing Yi

    Full Text Available Schisandra chinensis extracts (SEs have traditionally been used as an oriental medicine for the treatment of various human diseases, however, their further application in the biocontrol of plant disease remains poorly understood. This study was conducted to develop eco-friendly botanical pesticides from extracts of S. chinensis and assess whether they could play a key role in plant disease defense. Concentrated active fractions (SE-I, SE-II, and SE-III were obtained from S. chinensis via specific extraction and separation. Then, lignan-like substances, such as Schisanhenol B, were detected via High-Performance Liquid Chromatography-ElectroSpray Ionization-Mass Spectrometry (HPLC-ESI-MS analyses of the active fractions. Moreover, the results from biological tests on colony growth inhibition and spore germination indicated that SE-I, SE-II, and SE-III could inhibit hyphal growth and spore generation of three important plant pathogenic fungi (Monilinia fructicola, Fusarium oxysporum, and Botryosphaeria dothidea. The study of the mechanisms of resistant fungi revealed that the oxidation resistance system, including reactive oxygen species (ROS, malondialdehyde (MDA, catalase (CAT, and superoxide dismutase (SOD, was activated. The expression of genes related to defense, such as pathogenesis-related protein (PR4, α-farnesene synthase (AFS, polyphenol oxidase (PPO, and phenylalanine ammonia lyase (PAL were shown to be up-regulated after treatment with SEs, which suggested an increase in apple immunity and that fruits were induced to effectively defend against the infection of pathogenic fungi (B. dothidea. This study revealed that SEs and their lignans represent promising resources for the development of safe, effective, and multi-targeted agents against pathogenic fungi.

  11. Extraction and Separation of Active Ingredients in Schisandra chinensis (Turcz.) Baill and the Study of their Antifungal Effects

    Science.gov (United States)

    Liu, Jun; Zhang, Jie; Guo, Wei; Xiao, Weilie; Yao, Yuncong

    2016-01-01

    Schisandra chinensis extracts (SEs) have traditionally been used as an oriental medicine for the treatment of various human diseases, however, their further application in the biocontrol of plant disease remains poorly understood. This study was conducted to develop eco-friendly botanical pesticides from extracts of S. chinensis and assess whether they could play a key role in plant disease defense. Concentrated active fractions (SE-I, SE-II, and SE-III) were obtained from S. chinensis via specific extraction and separation. Then, lignan-like substances, such as Schisanhenol B, were detected via High-Performance Liquid Chromatography-ElectroSpray Ionization-Mass Spectrometry (HPLC-ESI-MS) analyses of the active fractions. Moreover, the results from biological tests on colony growth inhibition and spore germination indicated that SE-I, SE-II, and SE-III could inhibit hyphal growth and spore generation of three important plant pathogenic fungi (Monilinia fructicola, Fusarium oxysporum, and Botryosphaeria dothidea). The study of the mechanisms of resistant fungi revealed that the oxidation resistance system, including reactive oxygen species (ROS), malondialdehyde (MDA), catalase (CAT), and superoxide dismutase (SOD), was activated. The expression of genes related to defense, such as pathogenesis-related protein (PR4), α-farnesene synthase (AFS), polyphenol oxidase (PPO), and phenylalanine ammonia lyase (PAL) were shown to be up-regulated after treatment with SEs, which suggested an increase in apple immunity and that fruits were induced to effectively defend against the infection of pathogenic fungi (B. dothidea). This study revealed that SEs and their lignans represent promising resources for the development of safe, effective, and multi-targeted agents against pathogenic fungi. PMID:27152614

  12. Removal of Trace Pharmaceuticals from Water using coagulation and powdered activated carbon as pretreatment to ultrafiltration membrane system.

    Science.gov (United States)

    Sheng, Chenguang; Nnanna, A G Agwu; Liu, Yanghe; Vargo, John D

    2016-04-15

    In this study, the efficacy of water treatment technologies: ultra-filtration (UF), powdered activated carbon (PAC), coagulation (COA) and a combination of these technologies (PAC/UF and COA/UF) to remove target pharmaceuticals (Acetaminophen, Bezafibrate, Caffeine, Carbamazepine, Cotinine, Diclofenac, Gemfibrozil, Ibuprofen, Metoprolol, Naproxen, Sulfadimethoxine, Sulfamethazine, Sulfamethoxazole, Sulfathiazole, Triclosan and Trimethoprim) was investigated. Samples of wastewater from municipal WWTPs were analyzed using direct aqueous injection High Performance Liquid Chromatography with Tandem Quadrupole Mass Spectrometric (LC/MS/MS) detection. On concentration basis, results showed an average removal efficiency of 29%, 50%, and 7%, respectively, for the UF, PAC dosage of 50ppm, and COA dosage of 10ppm. When PAC dosage of 100ppm was used as pretreatment to the combined PAC and UF in-line membrane system, a 90.3% removal efficiency was achieved. The removal efficiency of UF in tandem with COA was 33%, an increase of 4% compared with the single UF treatment. The adsorption effect of PAC combined with the physical separation process of UF revealed the best treatment strategy for removing pharmaceutical contaminant from water. PMID:26867086

  13. Sorption and toxicity reduction of pharmaceutically active compounds and endocrine disrupting chemicals in the presence of colloidal humic acid.

    Science.gov (United States)

    Kim, Injeong; Kim, Hyo-Dong; Jeong, Tae-Yong; Kim, Sang Don

    2016-01-01

    This study investigated the toxicity changes and sorption of pharmaceuticals and endocrine disrupters in the presence of humic acid (HA). For the sorption experiment, a dead end filtration (DEF) system was used to separate bound and free-form target compounds. An algae growth inhibition test and E-screen assay were conducted to estimate the toxic effect of pharmaceutically active compounds (PhACs) and endocrine disrupting chemicals (EDCs), respectively. The permeate concentration was confirmed using liquid chromatography-mass spectrometry. In the sorption test, we observed significant sorption of PhACs and EDCs on colloidal HA, except for sulfamethoxazole (SMX). The values of log KCOC derived from DEF determinations ranged from 4.40 to 5.03. The removal efficiency varied with the HA concentration and the target chemical properties. Tetracycline and 4-octylphenol showed the highest sorption or removal efficiency (≈50%), even at 5 mg C/L HA. The algal growth inhibition of PhACs and the estrogenic effects of EDCs were significantly decreased in proportion to HA concentrations, except for SMX. In addition, the chemical analysis results showed a positive relationship with the bioassay results. Consequently, the sorption of PhACs and EDCs onto colloidal HA should be emphasized in natural environments because it significantly reduces bioavailable concentrations and toxicity to aquatic organisms. PMID:27533865

  14. Automated evaluation of pharmaceutically active ionic liquids’ (eco)toxicity through the inhibition of human carboxylesterase and Vibrio fischeri

    Energy Technology Data Exchange (ETDEWEB)

    Costa, Susana P.F.; Justina, Vanessa D. [REQUIMTE, Departamento de Ciências Químicas, Faculdade de Farmácia, Universidade do Porto, Rua Jorge Viterbo Ferreira, n° 228, 4050-313 Porto (Portugal); Bica, Katharina; Vasiloiu, Maria [Vienna University of Technology, Institute of Applied and Synthetic Chemistry, A-1060 Vienna (Austria); Pinto, Paula C.A.G., E-mail: ppinto@ff.up.pt [REQUIMTE, Departamento de Ciências Químicas, Faculdade de Farmácia, Universidade do Porto, Rua Jorge Viterbo Ferreira, n° 228, 4050-313 Porto (Portugal); Saraiva, M. Lúcia M.F.S., E-mail: lsaraiva@ff.up.pt [REQUIMTE, Departamento de Ciências Químicas, Faculdade de Farmácia, Universidade do Porto, Rua Jorge Viterbo Ferreira, n° 228, 4050-313 Porto (Portugal)

    2014-01-30

    Highlights: • IL-APIs toxicity on humans and aquatic environment was evaluated by inhibition assays. • The inhibition assays were implemented through automated screening bioassays. • Automation of bioassays enabled a rigorous control of the reaction conditions. • EC{sub 50} obtained provide vital information on IL-APIs safety and potential use as drugs. -- Abstract: The toxicity of 16 pharmaceutical active ionic liquids (IL-APIs) was evaluated by automated approaches based on sequential injection analysis (SIA). The implemented bioassays were centered on the inhibition of human carboxylesterase 2 and Vibrio fischeri, in the presence of the tested compounds. The inhibitory effects were quantified by calculating the inhibitor concentration required to cause 50% of inhibition (EC{sub 50}). The EC{sub 50} values demonstrated that the cetylpyridinium group was one of the most toxic cations and that the imidazolium group was the less toxic. The obtained results provide important information about the safety of the studied IL-APIs and their possible use as pharmaceutical drugs. The developed automated SIA methodologies are robust screening bioassays, and can be used as a generic tools to identify the (eco)toxicity of the structural elements of ILs, contributing to a sustainable development of drugs.

  15. Recent trends in the impurity profile of pharmaceuticals

    Directory of Open Access Journals (Sweden)

    Kavita Pilaniya

    2010-01-01

    Full Text Available Various regulatory authorities such as the International Conference on Harmonization (ICH, the United States Food and Drug administration (FDA, and the Canadian Drug and Health Agency (CDHA are emphasizing on the purity requirements and the identification of impurities in Active Pharmaceutical Ingredients (APIs. The various sources of impurity in pharmaceutical products are - reagents, heavy metals, ligands, catalysts, other materials like filter aids, charcoal, and the like, degraded end products obtained during \\ after manufacturing of bulk drugs from hydrolysis, photolytic cleavage, oxidative degradation, decarboxylation, enantiomeric impurity, and so on. The different pharmacopoeias such as the British Pharmacopoeia, United State Pharmacopoeia, and Indian Pharmacopoeia are slowly incorporating limits to allowable levels of impurities present in APIs or formulations. Various methods are used to isolate and characterize impurities in pharmaceuticals, such as, capillary electrophoresis, electron paramagnetic resonance, gas-liquid chromatography, gravimetric analysis, high performance liquid chromatography, solid-phase extraction methods, liquid-liquid extraction method, Ultraviolet Spectrometry, infrared spectroscopy, supercritical fluid extraction column chromatography, mass spectrometry, Nuclear magnetic resonance (NMR spectroscopy, and RAMAN spectroscopy. Among all hyphenated techniques, the most exploited techniques for impurity profiling of drugs are Liquid Chromatography (LC-Mass Spectroscopy (MS, LC-NMR, LC-NMR-MS, GC-MS, and LC-MS. This reveals the need and scope of impurity profiling of drugs in pharmaceutical research.

  16. Component morphology, size, and compositional impact on pharmaceutical powder blend flowability

    Science.gov (United States)

    Goldfarb, David; Nakagawa, Hirotaka; Conway, Stephen

    2014-11-01

    Through analysis of particle morphology, particle size, and compositional influences, we present experimental case studies revealing unexpected transitions in flowability and cohesion of pharmaceutical powder blends. We explore interactions between the needle-like API (Active Pharmaceutical Ingredient) and the more spherical remaining components (excipients) in the blend to explain these transitions, and optimal concentrations are identified. A range of particle sizes, aspect ratios (for API), and compositions were examined. Surprisingly, under certain conditions, a blend with a low API concentration exhibits less cohesive flowability properties than a placebo blend containing no API. Effective volume and coordination number models are tested by investigation of particle geometry, particle contact, and Van der Waals force factors. These results should translate both to the improved understanding of mixed component morphology systems and to a novel approach towards pharmaceutical product formulation optimization.

  17. ICP-OES法快速检测药品中催化剂残留的14种重金属元素%Rapid Determination of 14 Heavy Metal Elements of Catalysts Residues in Pharmaceutical Ingredients by ICP- OES Method

    Institute of Scientific and Technical Information of China (English)

    张玲帆; 王艳萍; 刘鑫; 陶卫; 张磊; 张文清

    2012-01-01

    采用有机溶剂二甲基亚砜和水(4∶1)的混合溶剂溶解药物样品,建立了电感耦合等离子体发射光谱法(ICP - OES)直接检测药物产品中金属催化剂残留的方法.在优化实验条件下,该法能快速检测欧洲药物评审委员会(EMEA)颁布指南中的14种重金属元素;方法检出限均小于0.30 mg/kg,加标回收率在90%~115%之间;对不同前处理方法的数据结果进行了对比.实验结果表明,该法操作简单、快速、准确度高,适合大批量药物产品中多元素的快速检测.%An inductively coupled plasma optical emission spectrometric (ICP - OES) method was developed for the determination of metallic impurities in pharmaceutical ingredients. The samples were directly dissolved with organic mixed solvent (DMSO : H2O =4 : 1). The conditions of instrument were optimized, and the 14 metal elements listed in EMEA guidance could be rapidly analyzed by the method. The detection limits were less than 0. 30 mg/kg, and the recoveries of the 14 metal elements ranged from 90% to 115% . The data was compared with those obtained from the different treatment methods. The results showed that the method, with the advantages of simplicity, easy operation and high accuracy, was suitable for the quick determination of multi-elements in large quantities of samples.

  18. 黄芪的有效成分提取与纳滤提取应用分析%Active Ingredients Extracted and Nanofiltration Application in Astragalus Extract

    Institute of Scientific and Technical Information of China (English)

    郭立忠; 吴镝

    2015-01-01

    Objective To analyze the active ingredients of astragalus diarrhea extraction and nanofiltration extracted application,astragalus traditional extraction process improvements. Methods APS,saponins as subjects,the use of orthogonal experimental design and analysis of numerical range analysis by comparing the effects of different extraction temperature,time and number of ingredients,and the extraction process in boiling alcohol shen added effect of cel ulase,nanofiltration comparison,the evaporation method. Results The experimental results showed that the temperature < 80 ℃, extracting 2 times,and each time 60 min nanofiltration concentrated extract was the optimum water extraction of astragalus. Conclusion Compared to traditional boiling alcohol precipitation extraction,astragalus of nanofiltration extraction process in the economic,technical y strong advantages,it has some promotional value in guiding the preparation of manufacturing,clinical applications.%目的:分析黄芪的有效成分提取和纳滤提取的应用,对传统的黄芪提取工艺进行改进。方法将黄芪多糖、总皂甙作为实验对象,使用正交实验设计并用极差分析法分析数值,对比不同提取温度、时间和次数对成分含量的影响,并在水煮醇沉提取工艺中加入了纤维素酶,比较纳滤、蒸发方法的效果。结果实验表明温度<80℃、提取2次且每次60 min的纳滤浓缩提取是黄芪水提的最佳工艺。结论相比较传统水煮醇沉提取法,黄芪的纳滤浓缩提取工艺在经济、技术上有很强的优越性,在指导制剂生产、临床应用中具有一定的推广价值。

  19. Active Ingredients Extracted and Nanofiltration Application in Astragalus Extract%黄芪的有效成分提取与纳滤提取应用分析

    Institute of Scientific and Technical Information of China (English)

    郭立忠; 吴镝

    2015-01-01

    目的:分析黄芪的有效成分提取和纳滤提取的应用,对传统的黄芪提取工艺进行改进。方法将黄芪多糖、总皂甙作为实验对象,使用正交实验设计并用极差分析法分析数值,对比不同提取温度、时间和次数对成分含量的影响,并在水煮醇沉提取工艺中加入了纤维素酶,比较纳滤、蒸发方法的效果。结果实验表明温度<80℃、提取2次且每次60 min的纳滤浓缩提取是黄芪水提的最佳工艺。结论相比较传统水煮醇沉提取法,黄芪的纳滤浓缩提取工艺在经济、技术上有很强的优越性,在指导制剂生产、临床应用中具有一定的推广价值。%Objective To analyze the active ingredients of astragalus diarrhea extraction and nanofiltration extracted application,astragalus traditional extraction process improvements. Methods APS,saponins as subjects,the use of orthogonal experimental design and analysis of numerical range analysis by comparing the effects of different extraction temperature,time and number of ingredients,and the extraction process in boiling alcohol shen added effect of cel ulase,nanofiltration comparison,the evaporation method. Results The experimental results showed that the temperature < 80 ℃, extracting 2 times,and each time 60 min nanofiltration concentrated extract was the optimum water extraction of astragalus. Conclusion Compared to traditional boiling alcohol precipitation extraction,astragalus of nanofiltration extraction process in the economic,technical y strong advantages,it has some promotional value in guiding the preparation of manufacturing,clinical applications.

  20. Development of RP-HPLC method for Qualitative Analysis of Active Ingredient (Gallic acid from Stem Bark of Dendrophthoe falcate Linn.

    Directory of Open Access Journals (Sweden)

    Hafsa Deshmukh

    2011-04-01

    Full Text Available A simple, precise and sensitive, RP-HPLC method with UV detection at 271nm was developed and validated for qualitative determination of active ingredient Gallic acid from stem bark of Dendrophthoe falcate Linn. Separation was performed on a ThermoMOS 2 HYPERSIL C18 column (250 cm × 4.6 mm, 5µm ODS 3 using mobile phase comprising of 0.1% Orthophosphoric acid : Acetonitrile (400 cm3 : 600 cm3 with a flow rate of 1 ml/minute with a short run time of 13 minute. The method was validated according to the regulatory guidelines with respect to linearity, system suitability, precision, solution stability, accuracy, robustness, assay and recovery. Detector response was linear for HPLC in the range of 0.04 to 0.16 mg/cm3. The system suitability, precision, solution stability, accuracy, robustness, assay and recovery was assessed by calculating % COV for all these parameters which is less than two as expected. The recovery of the method for Gallic acid was found 98.94% which shows that method is accurate. The described method has the advantage of being rapid and easy hence it can be applied for routine quality control analysis of Gallic acid from Dendrophthoe falcate Linn.

  1. Simultaneous determination of active ingredients in ethnomedicine Gaultheria leucocarpa var. yunnanensis and its medicinal preparation by capillary electrophoresis with electrochemical detection.

    Science.gov (United States)

    Zeng, Yikun; Tang, Zhuxing; Wang, Qingjiang; He, Pingang; Fang, Yuzhi

    2007-10-01

    A simple and rapid capillary electrophoresis (CE) with electrcochemical detection (ED) method has been established for the simultaneous determination of seven active ingredients in the stems and roots of Gaultheria leucocarpa var. yunnanensis and its medicinal preparation, including (+)-catechin, rutin, gentisic acid, vallinic acid, salicylic acid, quercetin, and protocatechuic acid. The effects of working potential, pH, and concentration of running buffer, separation voltage, and injection time on CE-ED are systematically investigated. Under the optimum conditions, the seven analytes could be completely separated within 23 min in a borax running buffer (pH 8.7). A good linear relationship is obtained over three orders of magnitude with detection limits (signal-to-noise ratio=3) ranging from 5x10(-8) g/mL to 3x10(-7) g/mL for the analytes. The proposed method is successfully used in the analysis of real samples after a relatively simple extraction procedure, and the assay results are satisfactory. PMID:17988450

  2. Study on cinnamon hypoglycemic active ingredient extraction method%肉桂降糖活性成分提取方法的研究

    Institute of Scientific and Technical Information of China (English)

    卢春连; 陆志科

    2014-01-01

    用乙醇回流提取法、超声波提取法、新装置提取法提取肉桂降糖活性成分。结果表明,新装置提取法比回流提取法、超声波提取法提取效率高,且快速简便。新装置提取法提取肉桂降糖活性成分的最佳条件为:多功能提取器装置,提取溶剂为95%乙醇,提取时间2 h,产品粗提率达21.0%。%Three methods were compared of preparing cinnamon hypoglycemic active ingredients:the etha-nol refluxing extraction,ultrasonic extraction and the new device extraction. The results showed that the new device extraction was superior to ethanol refluxing extraction and ultrasonic extraction,and the meth-od was fast and simple. The best conditions of the method were:multi-extractor device,solvent of 95%ethanol,and the time of extraction was 2 h,the coarse product rate was 21. 0% .

  3. Electrochemical biosensors in pharmaceutical analysis

    OpenAIRE

    Eric de Souza Gil; Giselle Rodrigues de Melo

    2010-01-01

    Given the increasing demand for practical and low-cost analytical techniques, biosensors have attracted attention for use in the quality analysis of drugs, medicines, and other analytes of interest in the pharmaceutical area. Biosensors allow quantification not only of the active component in pharmaceutical formulations, but also the analysis of degradation products and metabolites in biological fluids. Thus, this article presents a brief review of biosensor use in pharmaceutical analysis, fo...

  4. Ingredients of Huangqi decoction slow biliary fibrosis progression by inhibiting the activation of the transforming growth factor-beta signaling pathway

    Directory of Open Access Journals (Sweden)

    Du Jin-Xing

    2012-04-01

    Full Text Available Abstract Background Huangqi decoction was first described in Prescriptions of the Bureau of Taiping People's Welfare Pharmacy in Song Dynasty (AD 1078, and it is an effective recipe that is usually used to treat consumptive disease, anorexia, and chronic liver diseases. Transforming growth factor beta 1 (TGFβ1 plays a key role in the progression of liver fibrosis, and Huangqi decoction and its ingredients (IHQD markedly ameliorated hepatic fibrotic lesions induced by ligation of the common bile duct (BDL. However, the mechanism of IHQD on hepatic fibrotic lesions is not yet clear. The purpose of the present study is to elucidate the roles of TGFβ1 activation, Smad-signaling pathway, and extracellular signal-regulated kinase (ERK in the pathogenesis of biliary fibrosis progression and the antifibrotic mechanism of IHQD. Methods A liver fibrosis model was induced by ligation of the common bile duct (BDL in rats. Sham-operation was performed in control rats. The BDL rats were randomly divided into two groups: the BDL group and the IHQD group. IHQD was administrated intragastrically for 4 weeks. At the end of the fifth week after BDL, animals were sacrificed for sampling of blood serum and liver tissue. The effect of IHQD on the TGFβ1 signaling pathway was evaluated by western blotting and laser confocal microscopy. Results Decreased content of hepatic hydroxyproline and improved liver function and histopathology were observed in IHQD rats. Hepatocytes, cholangiocytes, and myofibroblasts in the cholestatic liver injury released TGFβ1, and activated TGFβ1 receptors can accelerate liver fibrosis. IHQD markedly inhibited the protein expression of TGFβ1, TGFβ1 receptors, Smad3, and p-ERK1/2 expression with no change of Smad7 expression. Conclusion IHQD exert significant therapeutic effects on BDL-induced fibrosis in rats through inhibition of the activation of TGFβ1-Smad3 and TGFβ1-ERK1/2 signaling pathways.

  5. The cinnamon-oil ingredient trans-cinnamaldehyde fails to target Campylobacter jejuni strain KC 40 in the broiler chicken cecum despite marked in vitro activity.

    Science.gov (United States)

    Hermans, David; Martel, An; van Deun, Kim; van Immerseel, Filip; Heyndrickx, Marc; Haesebrouck, Freddy; Pasmans, Frank

    2011-10-01

    Campylobacter jejuni is the most common bacterial cause of diarrheal disease in humans worldwide, with poultry products being a major source. Therefore, strategies to decrease Campylobacter colonization during primary production might aid in reducing the number of human campylobacteriosis cases. Several plant-derived compounds have been reported to possess anti-Campylobacter properties in vitro, so they could be promising candidates to reduce Campylobacter colonization in broiler chickens. To test this hypothesis, selected plant-derived antimicrobials (caffeic, gallic, protocatechuic, and vanillic acids, epigallocatechin gallate, trans-cinnamaldehyde, and thymol) were screened for anti-Campylobacter activity by determining MICs and setting up time-kill curves for C. jejuni strain KC 40. These experiments revealed marked antibacterial activity, especially for the cinnamon oil ingredient trans-cinnamaldehyde (CIN). This compound was tested in a broiler chick seeder model; it was added to the feed in coated form at an effective concentration of 0.3 % from day-of-hatch for the entire 22-day duration of the experiment. At 14 days of age, one-third of the birds were inoculated with C. jejuni strain KC 40 and served as seeders. CIN was not able to reduce cecal Campylobacter colonization in this model, which was confirmed in a cecal loop experiment. Despite CIN concentrations much higher than the MIC, C. jejuni numbers were not reduced compared with those in nontreated ceca at 2 and 24 h after injection. In conclusion, this study shows a marked discrepancy between in vitro and in vivo activity of CIN against C. jejuni strain KC 40. PMID:22004822

  6. Nanoscale Concentration Quantification of Pharmaceutical Actives in Amorphous Polymer Matrices by Electron Energy-Loss Spectroscopy.

    Science.gov (United States)

    Ricarte, Ralm G; Lodge, Timothy P; Hillmyer, Marc A

    2016-07-26

    We demonstrated the use of electron energy-loss spectroscopy (EELS) to evaluate the composition of phenytoin:hydroxypropyl methylcellulose acetate succinate (HPMCAS) spin-coated solid dispersions (SDs). To overcome the inability of bright-field and high-angle annular dark-field TEM imaging to distinguish between glassy drug and polymer, we used the π-π* transition peak in the EELS spectrum to detect phenytoin within the HPMCAS matrix of the SD. The concentration of phenytoin within SDs of 10, 25, and 50 wt % drug loading was quantified by a multiple least-squares analysis. Evaluating the concentration of 50 different regions in each SD, we determined that phenytoin and HPMCAS are intimately mixed at a length scale of 200 nm, even for drug loadings up to 50 wt %. At length scales below 100 nm, the variance of the measured phenytoin concentration increases; we speculate that this increase is due to statistical fluctuations in local concentration and chemical changes induced by electron irradiation. We also performed EELS analysis of an annealed 25 wt % phenytoin SD and showed that the technique can resolve concentration differences between regions that are less than 50 nm apart. Our findings indicate that EELS is a useful tool for quantifying, with high accuracy and sub-100 nm spatial resolution, the composition of many pharmaceutical and soft matter systems. PMID:27419264

  7. The Consultancy Activity on In Silico Models for Genotoxic Prediction of Pharmaceutical Impurities.

    Science.gov (United States)

    Pavan, Manuela; Kovarich, Simona; Bassan, Arianna; Broccardo, Lorenza; Yang, Chihae; Fioravanzo, Elena

    2016-01-01

    The toxicological assessment of DNA-reactive/mutagenic or clastogenic impurities plays an important role in the regulatory process for pharmaceuticals; in this context, in silico structure-based approaches are applied as primary tools for the evaluation of the mutagenic potential of the drug impurities. The general recommendations regarding such use of in silico methods are provided in the recent ICH M7 guideline stating that computational (in silico) toxicology assessment should be performed using two (Q)SAR prediction methodologies complementing each other: a statistical-based method and an expert rule-based method.Based on our consultant experience, we describe here a framework for in silico assessment of mutagenic potential of drug impurities. Two main applications of in silico methods are presented: (1) support and optimization of drug synthesis processes by providing early indication of potential genotoxic impurities and (2) regulatory evaluation of genotoxic potential of impurities in compliance with the ICH M7 guideline. Some critical case studies are also discussed.

  8. Effect of pharmaceutical potential endocrine disruptor compounds on protein disulfide isomerase reductase activity using di-eosin-oxidized-glutathione.

    Directory of Open Access Journals (Sweden)

    Danièle Klett

    Full Text Available BACKGROUND: Protein Disulfide Isomerase (PDI in the endoplasmic reticulum of all cells catalyzes the rearrangement of disulfide bridges during folding of membrane and secreted proteins. As PDI is also known to bind various molecules including hormones such as estradiol and thyroxin, we considered the hypothesis that adverse effects of endocrine-disrupter compounds (EDC could be mediated through their interaction with PDI leading to defects in membrane or secreted proteins. METHODOLOGY/PRINCIPAL FINDINGS: Taking advantage of the recent description of the fluorescence self quenched substrate di-eosin-oxidized-glutathione (DiE-GSSG, we determined kinetically the effects of various potential pharmaceutical EDCs on the in-vitro reductase activity of bovine liver PDI by measuring the fluorescence of the reaction product (E-GSH. Our data show that estrogens (ethynylestradiol and bisphenol-A as well as indomethacin exert an inhibition whereas medroxyprogesteroneacetate and nortestosterone exert a potentiation of bovine PDI reductase activity. CONCLUSIONS: The present data indicate that the tested EDCs could not only affect endocrine target cells through nuclear receptors as previously shown, but could also affect these and all other cells by positively or negatively affecting PDI activity. The substrate DiE-GSSG has been demonstrated to be a convenient substrate to measure PDI reductase activity in the presence of various potential EDCs. It will certainly be usefull for the screening of potential effect of all kinds of chemicals on PDI reductase activity.

  9. Altered Gene Expression in the Schistosome-Transmitting Snail Biomphalaria glabrata following Exposure to Niclosamide, the Active Ingredient in the Widely Used Molluscicide Bayluscide.

    Science.gov (United States)

    Zhang, Si-Ming; Buddenborg, Sarah K; Adema, Coen M; Sullivan, John T; Loker, Eric S

    2015-01-01

    In view of the call by the World Health Organization (WHO) for elimination of schistosomiasis as a public health problem by 2025, use of molluscicides in snail control to supplement chemotherapy-based control efforts is likely to increase in the coming years. The mechanisms of action of niclosamide, the active ingredient in the most widely used molluscicides, remain largely unknown. A better understanding of its toxicology at the molecular level will both improve our knowledge of snail biology and may offer valuable insights into the development of better chemical control methods for snails. We used a recently developed Biomphalaria glabrata oligonucleotide microarray (31K features) to investigate the effect of sublethal exposure to niclosamide on the transcriptional responses of the snail B. glabrata relative to untreated snails. Most of the genes highly upregulated following exposure of snails to niclosamide are involved in biotransformation of xenobiotics, including genes encoding cytochrome P450s (CYP), glutathione S-transferases (GST), and drug transporters, notably multi-drug resistance protein (efflux transporter) and solute linked carrier (influx transporter). Niclosamide also induced stress responses. Specifically, six heat shock protein (HSP) genes from three super-families (HSP20, HSP40 and HSP70) were upregulated. Genes encoding ADP-ribosylation factor (ARF), cAMP response element-binding protein (CREB) and coatomer, all of which are involved in vesicle trafficking in the Golgi of mammalian cells, were also upregulated. Lastly, a hemoglobin gene was downregulated, suggesting niclosamide may affect oxygen transport. Our results show that snails mount substantial responses to sublethal concentrations of niclosamide, at least some of which appear to be protective. The topic of how niclosamide's lethality at higher concentrations is determined requires further study. Given that niclosamide has also been used as an anthelmintic drug for decades and has been

  10. Altered Gene Expression in the Schistosome-Transmitting Snail Biomphalaria glabrata following Exposure to Niclosamide, the Active Ingredient in the Widely Used Molluscicide Bayluscide.

    Directory of Open Access Journals (Sweden)

    Si-Ming Zhang

    Full Text Available In view of the call by the World Health Organization (WHO for elimination of schistosomiasis as a public health problem by 2025, use of molluscicides in snail control to supplement chemotherapy-based control efforts is likely to increase in the coming years. The mechanisms of action of niclosamide, the active ingredient in the most widely used molluscicides, remain largely unknown. A better understanding of its toxicology at the molecular level will both improve our knowledge of snail biology and may offer valuable insights into the development of better chemical control methods for snails. We used a recently developed Biomphalaria glabrata oligonucleotide microarray (31K features to investigate the effect of sublethal exposure to niclosamide on the transcriptional responses of the snail B. glabrata relative to untreated snails. Most of the genes highly upregulated following exposure of snails to niclosamide are involved in biotransformation of xenobiotics, including genes encoding cytochrome P450s (CYP, glutathione S-transferases (GST, and drug transporters, notably multi-drug resistance protein (efflux transporter and solute linked carrier (influx transporter. Niclosamide also induced stress responses. Specifically, six heat shock protein (HSP genes from three super-families (HSP20, HSP40 and HSP70 were upregulated. Genes encoding ADP-ribosylation factor (ARF, cAMP response element-binding protein (CREB and coatomer, all of which are involved in vesicle trafficking in the Golgi of mammalian cells, were also upregulated. Lastly, a hemoglobin gene was downregulated, suggesting niclosamide may affect oxygen transport. Our results show that snails mount substantial responses to sublethal concentrations of niclosamide, at least some of which appear to be protective. The topic of how niclosamide's lethality at higher concentrations is determined requires further study. Given that niclosamide has also been used as an anthelmintic drug for decades and

  11. Analysis on the active ingredients of lavender honey from Xinjiang province%新疆薰衣草蜜活性成分的分析

    Institute of Scientific and Technical Information of China (English)

    潘柳; 张琦; 毛秀丽; 黄俊逸

    2012-01-01

    The reduced sugar, amylase value, total protein, total phenolic acid and anti-oxidative activities (DPPH radical scavenging activity test) of lavender honey, black locust honey and linden honey were determined and compared. The results showed that the content of amylase value, total phenolic acid and total protein in lavender honey are 14.8 mL/g.h, (200.8+6.9) IJg/g and (25.35+2.74) mg/100 g, respectively, all of which are higher than that of the other two kinds of honey, but the content of reduced sugar is lower, which is 74%. Three kinds of bee honeys have anti-oxidative activity. The scavenging capacities of lavender honey and linden honey don't exhibit an obvious difference, which are stronger than that of black locust honey. In addition, total phenolic acid content have no obvious correlation with anti-oxidative activities. It suggests that there are other active ingredients contributing to the anti-oxidative activities in honey.%以薰衣草蜜、洋槐蜜和椴树蜜3种蜂蜜为材料,对蜂蜜中的还原糖含量、淀粉酶值、蛋白质含量、总酚酸含量和它们清除DPPH自由基的能力进行分析。结果表明:薰衣草蜜中的淀粉酶值、总酚酸含量、蛋白质的含量分别为14.8mL/g·h、(200.8±6.9)μg/g和(25.35±2.74)mg/100g,均高于其他2种蜜,但还原糖含量比其他2种蜂蜜略低,为74%。3种蜂蜜均具有抗氧化的作用,薰衣草蜜与椴树蜜对DPPH自由基的清除能力相当,均高于洋槐蜜。总酚酸含量与抗氧化能力之间无明显相关性,说明蜂蜜中还含有其他的抗氧化活性成分。

  12. Occurrence and fate of bulk organic matter and pharmaceutically active compounds in managed aquifer recharge: A review

    KAUST Repository

    Maeng, Sungkyu

    2011-05-01

    Managed aquifer recharge (MAR) is a natural water treatment process that induces surface water to flow in response to a hydraulic gradient through soil/sediment and into a vertical or horizontal well. It is a relatively cost-effective, robust and sustainable technology. Detailed characteristics of bulk organic matter and the occurrence and fate of pharmaceutically active compounds (PhACs) during MAR processes such as bank filtration (BF) and artificial recharge (AR) were reviewed. Understanding the fate of bulk organic matter during BF and AR is an essential step in determining pre- and/or post-treatment requirements. Analysis of organic matter characteristics using a suite of analytical tools suggests that there is a preferential removal of non-humic substances during MAR. Different classes of PhACs were found to behave differently during BF and AR. Antibiotics, non-steroidal anti-inflammatory drugs (NSAIDs), beta blockers, and steroid hormones generally exhibited good removal efficiencies, especially for compounds having hydrophobic-neutral characteristics. However, anticonvulsants showed a persistent behavior during soil passage. There were also some redox-dependent PhACs. For example, X-ray contrast agents measured, as adsorbable organic iodine (AOI), and sulfamethoxazole (an antibiotic) degraded more favorably under anoxic conditions compared to oxic conditions. Phenazone-type pharmaceuticals (NSAIDs) exhibited better removal under oxic conditions. The redox transition from oxic to anoxic conditions during soil passage can enhance the removal of PhACs that are sensitive to redox conditions. In general, BF and AR can be included in a multi-barrier treatment system for the removal of PhACs. © 2011.

  13. Occurrence and fate of bulk organic matter and pharmaceutically active compounds in managed aquifer recharge: a review.

    Science.gov (United States)

    Maeng, Sung Kyu; Sharma, Saroj K; Lekkerkerker-Teunissen, Karin; Amy, Gary L

    2011-05-01

    Managed aquifer recharge (MAR) is a natural water treatment process that induces surface water to flow in response to a hydraulic gradient through soil/sediment and into a vertical or horizontal well. It is a relatively cost-effective, robust and sustainable technology. Detailed characteristics of bulk organic matter and the occurrence and fate of pharmaceutically active compounds (PhACs) during MAR processes such as bank filtration (BF) and artificial recharge (AR) were reviewed. Understanding the fate of bulk organic matter during BF and AR is an essential step in determining pre- and/or post-treatment requirements. Analysis of organic matter characteristics using a suite of analytical tools suggests that there is a preferential removal of non-humic substances during MAR. Different classes of PhACs were found to behave differently during BF and AR. Antibiotics, non-steroidal anti-inflammatory drugs (NSAIDs), beta blockers, and steroid hormones generally exhibited good removal efficiencies, especially for compounds having hydrophobic-neutral characteristics. However, anticonvulsants showed a persistent behavior during soil passage. There were also some redox-dependent PhACs. For example, X-ray contrast agents measured, as adsorbable organic iodine (AOI), and sulfamethoxazole (an antibiotic) degraded more favorably under anoxic conditions compared to oxic conditions. Phenazone-type pharmaceuticals (NSAIDs) exhibited better removal under oxic conditions. The redox transition from oxic to anoxic conditions during soil passage can enhance the removal of PhACs that are sensitive to redox conditions. In general, BF and AR can be included in a multi-barrier treatment system for the removal of PhACs. PMID:21489592

  14. Reversible anti-settlement activity against Amphibalanus (= Balanus ) amphitrite, Bugula neritina , and Hydroides elegans by a nontoxic pharmaceutical compound, mizolastine

    KAUST Repository

    Zhou, Xiaojian

    2009-11-01

    Mizolastine, an antihistamine pharmaceutical, was found to significantly inhibit larval settlement of the barnacle Amphibalanus (=Balanus) amphitrite, the bryozoan Bugula neritina, and the polychaete Hydroides elegans with EC50 values of 4.2, 11.2, and 4.1 mg ml-1, respectively. No toxicity against the larvae of these three species was observed at the concentration range tested during incubations with mizolastine. To determine whether the anti-settlement activity of mizolastine is reversible, recovery bioassays using these three species were conducted. More than 70% of the larvae that had been exposed for 4 h to mizolastine at concentrations four-fold greater than their respective EC50 values completed normal metamorphosis. The results of the recovery bioassay provide evidence that the antisettlement effect of mizolastine is reversible in addition to being nontoxic. The anti-settlement activities of several intermediates of the synthesis process of mizolastine were also examined. One of the intermediates, 2-chloro-1-(4- fluorobenzyl)-1H-benzo[d]imidazole, inhibited larval settlement and metamorphosis with low toxicity. These results may improve the understanding of the key functional group responsible for the anti-settlement activity of mizolastine. © 2009 Taylor & Francis.

  15. Validation of quantitative {sup 1}H NMR method for the analysis of pharmaceutical formulations; Validacao de metodo quantitativo por RMN de {sup 1}H para analises de formulacoes farmaceuticas

    Energy Technology Data Exchange (ETDEWEB)

    Santos, Maiara da S. [Universidade de Sao Paulo (USP), Sao Carlos, SP (Brazil). Instituto de Quimica; Colnago, Luiz Alberto, E-mail: luiz.colnago@embrapa.br [Embrapa Instrumentacao, Sao Carlos, SP (Brazil)

    2013-09-01

    The need for effective and reliable quality control in products from pharmaceutical industries renders the analyses of their active ingredients and constituents of great importance. This study presents the theoretical basis of Superscript-One H NMR for quantitative analyses and an example of the method validation according to Resolution RE N. 899 by the Brazilian National Health Surveillance Agency (ANVISA), in which the compound paracetamol was the active ingredient. All evaluated parameters (selectivity, linearity, accuracy, repeatability and robustness) showed satisfactory results. It was concluded that a single NMR measurement provides structural and quantitative information of active components and excipients in the sample. (author)

  16. 21 CFR 310.544 - Drug products containing active ingredients offered over-the-counter (OTC) for use as a smoking...

    Science.gov (United States)

    2010-04-01

    ... offered over-the-counter (OTC) for use as a smoking deterrent. 310.544 Section 310.544 Food and Drugs FOOD... ingredients offered over-the-counter (OTC) for use as a smoking deterrent. (a) Any product that bears labeling... or reduce smoking,” or similar claims is a smoking deterrent drug product. Cloves,...

  17. 超分子化学在药物共晶中的应用%Application of Supramolecular Chemistry on Pharmaceutical Cocrystals

    Institute of Scientific and Technical Information of China (English)

    陈嘉媚; 吴传斌; 鲁统部

    2011-01-01

    药物共晶是一种新兴的药物晶型,一个给定的活性药物分子通过形成共晶,一方面可以大大丰富其结晶形式,另一方面可以改善其物化性质及临床疗效.本文从超分子化学的角度对药物共晶进行了综述,列举了一系列通过氢键超分子合成子进行药物共晶设计和制备的研究实例,旨在促进超分子化学和药学的交叉融合.%Pharmaceutical cocrystal is a new type of pharmaceutical crystalline state. It is attractive to pharmaceutical scientists because it can provide a number of crystalline states for a given active pharmaceutical ingredient ( API) , in which the physical and chemical properties of the API can be adjusted by pharmaceutical cocrystal. In this review, we address pharmaceutical cocrystals from the perspective of supramolecular chemistry , and present a series of structures of pharmaceutical cocrystals constructed through hydrogen bonding supramolecular synthons, in which the physical and chemical properties(solubility, dissolution, bioavailability, melting point, stability, etc. ) of APIs can be changed by pharmaceutical cocrystal.

  18. Fucoxanthin: A Promising Medicinal and Nutritional Ingredient

    OpenAIRE

    Hui Zhang; Yibo Tang; Ying Zhang; Shuofeng Zhang; Jing Qu; Xu Wang; Ran Kong; Chunchao Han; Zhenquan Liu

    2015-01-01

    Fucoxanthin, an allenic carotenoid, can be isolated from edible brown seaweeds. Recent studies have reported that fucoxanthin has many physiological functions and biological properties, such as antiobesity, antitumor, antidiabetes, antioxidant, anti-inflammatory, and hepatoprotective activities, as well as cardiovascular and cerebrovascular protective effects. Therefore, fucoxanthin can be used as both medicinal and nutritional ingredient to prevent and treat chronic diseases. Although fucoxa...

  19. Comparative study of the effect of pharmaceutical additives on the elimination of antibiotic activity during the treatment of oxacillin in water by the photo-Fenton, TiO2-photocatalysis and electrochemical processes.

    Science.gov (United States)

    Serna-Galvis, Efraim A; Silva-Agredo, Javier; Giraldo, Ana L; Flórez-Acosta, Oscar A; Torres-Palma, Ricardo A

    2016-01-15

    Synthetic pharmaceutical effluents loaded with the β-lactam antibiotic oxacillin were treated using advanced oxidation processes (the photo-Fenton system and TiO2 photocatalysis) and chloride mediated electrochemical oxidation (with Ti/IrO2 anodes). Combinations of the antibiotic with excipients (mannitol or tartaric acid), an active ingredient (calcium carbonate, i.e. bicarbonate ions due to the pH) and a cleaning agent (sodium lauryl ether sulfate) were considered. Additionally, urban wastewater that had undergone biological treatment was doped with oxacillin and treated with the tested systems. The evolution of antimicrobial activity was monitored as a parameter of processes efficiency. Although the two advanced oxidation processes (AOPs) differ only in the way they produce OH, marked differences were observed between them. There were also differences between the AOPs and the electrochemical system. Interestingly, each additive had a different effect on each treatment. For water loaded with mannitol, electrochemical treatment was the most suitable option because the additive did not significantly affect the efficiency of the system. Due to the formation of a complex with Fe(3+), tartaric acid accelerated the elimination of antibiotic activity during the photo-Fenton process. For TiO2 photocatalysis, the presence of bicarbonate ions contributed to antibiotic activity elimination through the possible formation of carbonate and bicarbonate radicals. Sodium lauryl ether sulfate negatively affected all of the processes. However, due to the higher selectivity of HOCl compared with OH, electrochemical oxidation showed the least inhibited efficiency. For the urban wastewater doped with oxacillin, TiO2 photocatalysis was the most efficient process. These results will help select the most suitable technology for the treatment of water polluted with β-lactam antibiotics.

  20. Product Quality Review in Pharmaceutical Manufacturers%药品生产企业产品质量回顾分析的研究

    Institute of Scientific and Technical Information of China (English)

    丁越; 梁毅

    2011-01-01

    介绍了产品质量回顾分析,将其与欧盟GMP、ICHQ7A中的内容进行了对比,并介绍了质量回顾分析的编写方法。%This article introduced product quality review in pharmaceutical manufacturers,compared the content in GMP with it in Good Manufacturing Practice for Active Pharmaceutical Ingredients and in EU GMP.The method of writing product quality review was also included.

  1. Water soluble active ingredients of Danshen--review on the Salvianolic acids%丹参水溶性有效成分--丹酚酸研究进展

    Institute of Scientific and Technical Information of China (English)

    杜冠华; 张均田

    2000-01-01

    Danshen-Radix Salviae Miltiorrhizae,is one of the common traditional Chinese medicines,which has been used clinically in the treatment of cardiovascular diseases more than 20 centuries.The active ingredients of Danshen has been researched 5 decades by the modern methods.Many researchers investigated the pharmacological effects of water soluble ingredients of Danshen-salvianolic acids in vivo and in vitro.The results demonstrated that salvianolic acids have different pharmacological effects such as potent antioxidative effects,scavenging free radicals,protect neural cells against injuries caused by anoxia, etc.In present paper,the pharmacological effects of salvianolic acids and the mechanisms of their actions are reviewed based on the research results obtained in our laboratory and other authors.

  2. Pharmacodynamic Study and Active Ingredient of Endophyte in Medicinal Plants%药用植物内生菌活性成分及药效学研究进展

    Institute of Scientific and Technical Information of China (English)

    丁仁伟; 邓毅

    2012-01-01

    查阅国内外近年相关文献,对药用植物内生菌代谢产物的种类及药效进行分析总结,概述药用植物内生菌的活性成分和药效学研究现状,提出药用植物内生菌可产生多种活性成分和药理作用,此项研究对于解决药用植物资源匮乏和发现新成分、新疗效具有重要价值.%Metabolites types of endophytes in medicinal plants and efficacy were analyzed and summarized; active ingredient and pharmacodynamic study of endophytes in medicinal plants were outlined through consulting associated literature at home and abroad in recent years, endophytes in medicinal plants can produce many kinds of active ingredients and pharmacological action. The study is valuable for covering scarcity of medicinal plants and discovering new ingredient and curative effects.

  3. Reducing effect of saikosaponin A, an active ingredient of Bupleurum falcatum, on alcohol self-administration in rats: Possible involvement of the GABAB receptor.

    Science.gov (United States)

    Maccioni, Paola; Lorrai, Irene; Carai, Mauro A M; Riva, Antonella; Morazzoni, Paolo; Mugnaini, Claudia; Corelli, Federico; Gessa, Gian Luigi; Colombo, Giancarlo

    2016-05-16

    Recent studies demonstrated that treatment with saikosaponin A (SSA) - an active ingredient of the medicinal herb, Bupleurum falcatum L. - selectively suppressed, likely via a GABAB receptor-mediated mechanism, intravenous self-administration of morphine and cocaine in rats [Yoon et al., 2012; 2013]. The present study was designed to investigate whether the capacity of SSA to suppress morphine and cocaine self-administration extends to oral alcohol self-administration. To this end, selectively bred Sardinian alcohol-preferring (sP) rats were trained to lever-respond on a Fixed Ratio (FR) 4 (FR4) schedule of reinforcement for alcohol (15%, v/v) in daily 30-min sessions. Once responding had stabilized, rats were tested under the FR4 (measure of alcohol reinforcing properties) and Progressive Ratio (PR; measure of alcohol motivational properties) schedules of reinforcement. The possible involvement of the GABAB receptor system was investigated testing the effect of (a) pretreatment with the GABAB receptor antagonist, SCH50911, and (b) combined treatment with the positive allosteric modulator of the GABAB receptor, GS39783. Treatment with SSA (0, 0.25, 0.5, and 1mg/kg, i.p.) markedly reduced lever-responding for alcohol, amount of self-administered alcohol, and breakpoint for alcohol (defined as the lowest response requirement not achieved in the PR experiment). Pretreatment with 2mg/kg SCH50911 (i.p.) resulted in a partial blockade of the reducing effect of 0.5mg/kg SSA on lever-responding for alcohol and amount of self-administered alcohol. Combination of per se ineffective doses of GS39783 (5mg/kg, i.g.) and SSA (0.1mg/kg, i.p.) reduced lever-responding for alcohol and amount of self-administered alcohol. These results (a) extend to alcohol self-administration the capacity of SSA to suppress morphine and cocaine self-administration in rats and (b) suggest that the GABAB receptor system is likely part of the neural substrate underlying the reducing effect of SSA on

  4. Recent patents and patented technology platforms for pharmaceutical taste masking.

    Science.gov (United States)

    Kaushik, Deepak; Dureja, Harish

    2014-04-01

    Taste masking is an important factor in the development of oral dosage forms containing bitter active pharmaceutical ingredients. Currently numerous techniques are being applied to overcome this problem. Realizing this, several researchers and pharmaceutical companies are now engaged in developing novel techniques to address the problem of taste masking evident by numerous patents filed in this area in recent times. In this review the most recent patents for taste masking are discussed and how these patents overcome the limitations of conventional approaches of taste masking is also highlighted. Novel techniques based on some recent patents such as nanohybrid, melt extrusion, non-complex cyclodextrin compositions and off taste masking are providing new realms to taste masking of bitter drugs. The present article also provides an overview of various patented platform technologies based on different techniques/mechanisms employed for taste masking. The unique features and principles of taste-masking approaches used in various patented technologies are also discussed. A better understanding of these new patents and patented technologies will help researchers and pharmaceutical industries to select the appropriate platform, or to develop innovative products with improved taste masking properties. PMID:24499438

  5. Thiomers: A Blessing to Evaluating Era of Pharmaceuticals

    Directory of Open Access Journals (Sweden)

    Muhammad Hanif

    2015-01-01

    Full Text Available Thiomers are the polymers modified for the mucoadhesive properties and other additive properties by incorporating thiol moieties in the backbone of the unmodified polymeric chain by substitution reactions or simple oxidation reactions. Drugs that are less soluble and permeable can be complexed with thiomers for their increased absorption through the mucosal membranes by increase in contact time and prolonged stay in body due to mucoadhesion. Immobilization of thiol group therefore increases the mucoadhesive properties of the modified polymer by 2–140-folds. The prepared thiomers are characterized and made stable by different techniques. Thiomers also give the controlled delivery of the active pharmaceutical ingredients in the body. Different polymers that are modified by thiolation are chitosan, polyacrylic acid, sodium alginate, sodium carboxy methyl cellulose, guar gum, and so forth. Thiomeric formulations are a challenge to deliver drugs with low therapeutic compatibility. Micro- and nanopreparations containing thiomers can be prepared by different techniques such as covalent crosslinking, in situ gelation, radical emulsion polymerization, and emulsification. Nowadays thiomers have wide range of applications as a promising pharmaceutical excipient in the evaluating era of pharmaceutical technology.

  6. Improving the performance of an aerobic membrane bioreactor (MBR) treating pharmaceutical wastewater with powdered activated carbon (PAC) addition.

    Science.gov (United States)

    Kaya, Yasemin; Bacaksiz, A Murat; Golebatmaz, Ugur; Vergili, Ilda; Gönder, Z Beril; Yilmaz, Gulsum

    2016-04-01

    In this study, the effects of organic loading rate (OLR) and the addition of powdered activated carbon (PAC) on the performance and membrane fouling of MBR were conducted to treat real pharmaceutical process wastewater. Over 145 days of operation, the MBR system was operated at OLRs ranging from 1 to 2 kg COD m(-3) day(-1) without sludge wasting. The addition of PAC provided an improvement in the flux, despite an increase in the OLR:PAC ratio. The results demonstrated that the hybrid PAC-MBR system maintained a reduced amount of membrane fouling and steadily increased the removal performance of etodolac. PAC addition reduced the deposition of extracellular polymeric substance and organic matter on the membrane surface and resulted an increase in COD removal even at higher OLRs with low PAC addition. Membrane fouling mechanisms were investigated using combined adsorption fouling models. Modified fouling index values and normalized mass transfer coefficient values indicated that predominant fouling mechanism was cake adsorption. PMID:26846538

  7. Adsorption of pharmaceuticals onto activated carbon fiber cloths - Modeling and extrapolation of adsorption isotherms at very low concentrations.

    Science.gov (United States)

    Fallou, Hélène; Cimetière, Nicolas; Giraudet, Sylvain; Wolbert, Dominique; Le Cloirec, Pierre

    2016-01-15

    Activated carbon fiber cloths (ACFC) have shown promising results when applied to water treatment, especially for removing organic micropollutants such as pharmaceutical compounds. Nevertheless, further investigations are required, especially considering trace concentrations, which are found in current water treatment. Until now, most studies have been carried out at relatively high concentrations (mg L(-1)), since the experimental and analytical methodologies are more difficult and more expensive when dealing with lower concentrations (ng L(-1)). Therefore, the objective of this study was to validate an extrapolation procedure from high to low concentrations, for four compounds (Carbamazepine, Diclofenac, Caffeine and Acetaminophen). For this purpose, the reliability of the usual adsorption isotherm models, when extrapolated from high (mg L(-1)) to low concentrations (ng L(-1)), was assessed as well as the influence of numerous error functions. Some isotherm models (Freundlich, Toth) and error functions (RSS, ARE) show weaknesses to be used as an adsorption isotherms at low concentrations. However, from these results, the pairing of the Langmuir-Freundlich isotherm model with Marquardt's percent standard of deviation was evidenced as the best combination model, enabling the extrapolation of adsorption capacities by orders of magnitude.

  8. Influence of excipients in comilling on mitigating milling-induced amorphization or structural disorder of crystalline pharmaceutical actives.

    Science.gov (United States)

    Balani, Prashant N; Ng, Wai Kiong; Tan, Reginald B H; Chan, Sui Yung

    2010-05-01

    The feasibility of using excipients to suppress the amorphization or structural disorder of crystalline salbutamol sulphate (SS) during milling was investigated. SS was subjected to ball-milling in the presence of alpha-lactose monohydrate (LAC), adipic acid (AA), magnesium stearate (MgSt), or polyvinyl pyrrolidone (PVP). X-ray powder diffraction, dynamic vapor sorption (DVS), high sensitivity differential scanning calorimetry (HSDSC) were used to analyze the crystallinity of the milled mixtures. Comilling with crystalline excipients, LAC, AA, and MgSt proved effective in reducing the amorphization of SS. LAC, AA, or MgSt acting as seed crystals to induce recrystallization of amorphous SS formed by milling. During comilling, both SS and LAC turned predominantly amorphous after 45 min but transformed back to a highly crystalline state after 60 min. Amorphous content was below the detection limits of DVS (0.5%) and HSDSC (5%). Comilled and physical mixtures of SS and ALM were stored under normal and elevated humidity conditions. This was found to prevent subsequent changes in crystallinity and morphology of comilled SS:LAC as compared to significant changes in milled SS and physical mixture. These results demonstrate a promising application of comilling with crystalline excipients in mitigating milling induced amorphization of pharmaceutical actives. PMID:19902526

  9. The contribution of pharmaceutically active compounds from healthcare facilities to a receiving sewage treatment plant in Canada.

    Science.gov (United States)

    Kleywegt, Sonya; Pileggi, Vince; Lam, Yuet Ming; Elises, Alan; Puddicomb, Aaron; Purba, Gurminder; Di Caro, Joanne; Fletcher, Tim

    2016-04-01

    Concentrations and percent loadings of pharmaceutically active compounds (PhACs) and other emerging contaminants released from healthcare facilities (2 hospitals and a long-term care facility) to a sewage treatment plant (STP) in a large urban sewershed were evaluated. An additional hospital outside the sewershed was also monitored. Fourteen of the 24 steroids/hormones and 88 of the 117 PhACs and emerging contaminants were detected at least once. Commonly used substances, including cotinine, caffeine and its metabolite 1,7-dimethylxanthine, ibuprofen and naproxen (analgesics), venlafaxine (antidepressant), and N,N-diethyl-meta-toluamide (insect repellant), were detected in all samples at all sites. Concentrations detected in the large specialty hospital outside the sewershed were similar to those within the sewershed. Cytotoxic drugs (tamoxifen and cyclophosphamide) and x-ray contrast media (iopamidol and diatrizoic acid) were infrequently detected in hospital effluents. Analysis for antibiotics indicated that azithromycin, clarithromycin, ciprofloxacin, erythromycin, ofloxacin, and sulfamethoxazole were consistently detected in hospital wastewaters, as was triclosan (antibacterial agent). Fifteen compounds individually contributed greater than 1% to the total PhAC and emerging contaminant load to the STP from the 2 hospitals in the sewershed, and 9 compounds in the STP effluent exceeded ecotoxicological criteria. The present survey demonstrates that point source discharges from healthcare facilities in this sewershed make a small contribution to the overall PhAC and emerging contaminant loading compared with the total concentrations entering the receiving STP.

  10. Occurrence and fate of pharmaceutically active compounds in the environment, a case study: Hoeje River in Sweden

    International Nuclear Information System (INIS)

    Pharmaceutically active compounds (PhACs) in the environment lately have been acknowledged to constitute a health risk for humans and terrestrial and aquatic ecosystems. Human and veterinary applications are the main sources of PhACs in the environment and the major pathways are excretion and discharge to the environment through sewage treatment plants (STPs). In this study, the occurrence and fate of selected human PhACs belonging to different therapeutic classes (non-steroidal anti-inflammatory drugs, lipid regulators, anti-epileptics, antibiotics and β-blockers) were investigated in a small river in the very south of Sweden. The objectives of the study were to evaluate the impact of a high and rather constant load in sewage influent on downstream concentrations and whether substances that are metabolized to a high degree in humans also show a low persistency in a natural aquatic environment. Water samples were collected from the influent and effluent of the STP, in a series of dammed reservoirs leading to discharge into the Hoeje River in Sweden, and at several locations in the river downstream of the outfall. After enrichment by solid-phase extraction, the compounds were analyzed using GC-MS (methylated derivatives) or LC-MS/MS. In addition to the targeted pharmaceuticals, GC-MS analysis of the samples revealed the presence of other sewage-related pollutants (triclosan, caffeine, flame-retardants, antioxidants) and these results where included for comparison. Removal efficiencies were calculated in the STP and found to display a wide range with numerous species surviving treatment at greater than half their influent concentrations, including diclofenac, the anti-epileptic carbamazepine, a β-blocker (propanolol), and antibiotics trimetoprim and sulfamethoxazole. Low removals were also observed for Tris(2-chloroisopropyl)phosphate (flame retardant), BHT-aldehyde (oxidation product of BHT) and synthetic musk (HHCB). The concentrations of chloride (Cl-) and boron

  11. Occurrence and fate of pharmaceutically active compounds in the environment, a case study: Hoeje River in Sweden

    Energy Technology Data Exchange (ETDEWEB)

    Bendz, David [Swedish Geotechnical Institute, Department of Environmental Technology, Hospitalsgatan 16A, S-211 33 Malmoe (Sweden)]. E-mail: David.Bendz@swedgeo.se; Paxeus, Nicklas A. [Gryaab, Karl IX:s vaeg, S-418 34 Gothenburg (Sweden); Ginn, Timothy R. [University of California, Department of Civil and Environmental Engineering, 1 Shields Avenue, 2001 Engineering III, Davis, CA 95616 (United States); Loge, Frank J. [University of California, Department of Civil and Environmental Engineering, 1 Shields Avenue, 2001 Engineering III, Davis, CA 95616 (United States)

    2005-07-15

    Pharmaceutically active compounds (PhACs) in the environment lately have been acknowledged to constitute a health risk for humans and terrestrial and aquatic ecosystems. Human and veterinary applications are the main sources of PhACs in the environment and the major pathways are excretion and discharge to the environment through sewage treatment plants (STPs). In this study, the occurrence and fate of selected human PhACs belonging to different therapeutic classes (non-steroidal anti-inflammatory drugs, lipid regulators, anti-epileptics, antibiotics and {beta}-blockers) were investigated in a small river in the very south of Sweden. The objectives of the study were to evaluate the impact of a high and rather constant load in sewage influent on downstream concentrations and whether substances that are metabolized to a high degree in humans also show a low persistency in a natural aquatic environment. Water samples were collected from the influent and effluent of the STP, in a series of dammed reservoirs leading to discharge into the Hoeje River in Sweden, and at several locations in the river downstream of the outfall. After enrichment by solid-phase extraction, the compounds were analyzed using GC-MS (methylated derivatives) or LC-MS/MS. In addition to the targeted pharmaceuticals, GC-MS analysis of the samples revealed the presence of other sewage-related pollutants (triclosan, caffeine, flame-retardants, antioxidants) and these results where included for comparison. Removal efficiencies were calculated in the STP and found to display a wide range with numerous species surviving treatment at greater than half their influent concentrations, including diclofenac, the anti-epileptic carbamazepine, a {beta}-blocker (propanolol), and antibiotics trimetoprim and sulfamethoxazole. Low removals were also observed for Tris(2-chloroisopropyl)phosphate (flame retardant), BHT-aldehyde (oxidation product of BHT) and synthetic musk (HHCB). The concentrations of chloride (Cl

  12. Manufacturing capability as a technological development indicator in the pharmaceutical industry

    Directory of Open Access Journals (Sweden)

    John Jairo Gallo Castro

    2010-05-01

    Full Text Available The pharmaceutical industrial has five subsectors: medicines, cosmetics, phytotherapeutics, cleaning products and medical devices. The medicine subsector consists of organisations producing, importing and selling these products. Most studies about this industry have been guided by economic interests without assessing technological aspects of production. This article was aimed at proposing a methodology for assessing and describing the medicine sector according to its technological development by using the manufacturing capability concept. The main information was taken from the Colombian Medicaments and Food Surveillance Institute’s (Instituto Nacional de Vigilancia de Medicamentos y Alimentos - INVIMA databases related to pharmaceutical plant production in Bogotá, including material transformation facilities. This study led to three characteristics being identified for defining the pharmaceutical industry’s manufacturing capability: that related to the pharmacological group to which active pharmaceutical ingredients belong, that linked to specifications regarding medicines’ sterility and that related to the technology required for manufacturing each pharmaceutical product. An analysis of these features has thus been presented and some technologies have been identified which have not been transferred or assimilated by the organisations being studied. It was found that manufacturing capability should be considered as being an indicator of the degree of technological development in these subsectors in Colombia.

  13. THERMODYNAMICS OF BINARY ALLOYS OF PHARMACEUTICAL ACTIVE IMIDAZOLE WITH O- PHENYLENEDIAMINE

    Directory of Open Access Journals (Sweden)

    Shekhar H.

    2012-04-01

    Full Text Available The present study describes the investigation of eutectic and non-eutectic alloys of imidazole (IM with o - Phenylenediamine (OPD. the solid-liquid equilibrium (SLE data determined by thaw melt method in the form of melting temperature with their corresponding composition construct the solid-liquid equilibrium phase diagram which suggests simple eutectic behaviour is followed by the binary system. The activity co-efficient model based on enthalpy of fusion was employed to calculate the excess partial and integral thermodynamic functions such as gE, hE and sE. These values help to predict the nature of molecular interaction, ordering and stability between the components. The spontaneity of mixing of eutectic and non eutectic alloys was discussed by the partial and integral mixing quantities ∆GM, ∆HM and ∆SM. Using Gibbs-Duhem equation the solution of partial molar heat of mixing, activity and activity coefficient of the component in the binary mix have been resolved.

  14. Curcumin derivatives as metal-chelating agents with potential multifunctional activity for pharmaceutical applications.

    Science.gov (United States)

    Ferrari, Erika; Benassi, Rois; Sacchi, Stefania; Pignedoli, Francesca; Asti, Mattia; Saladini, Monica

    2014-10-01

    Curcuminoids represent new perspectives for the development of novel therapeutics for Alzheimer's disease (AD), one probable mechanism of action is related to their metal complexing ability. In this work we examined the metal complexing ability of substituted curcuminoids to propose new chelating molecules with biological properties comparable with curcumin but with improved stability as new potential AD therapeutic agents. The K2T derivatives originate from the insertion of a -CH2COOC(CH3)3 group on the central atom of the diketonic moiety of curcumin. They retain the diketo-ketoenol tautomerism which is solvent dependent. In aqueous solution the prevalent form is the diketo one but the addition of metal ion (Ga(3+), Cu(2+)) causes the dissociation of the enolic proton creating chelate complexes and shifting the tautomeric equilibrium towards the keto-enol form. The formation of metal complexes is followed by both NMR and UV-vis spectroscopy. The density functional theory (DFT) calculations on K2T21 complexes with Ga(3+) and Cu(2+) are performed and compared with those on curcumin complexes. [Ga(K2T21)2(H2O)2](+) was found more stable than curcumin one. Good agreement is detected between calculated and experimental (1)H and (13)C NMR data. The calculated OH bond dissociation energy (BDE) and the OH proton dissociation enthalpy (PDE), allowed to predict the radical scavenging ability of the metal ion complexed with K2T21, while the calculated electronic affinity (EA) and ionization potential (IP) represent yardsticks of antioxidant properties. Eventually theoretical calculations suggest that the proton-transfer-associated superoxide-scavenging activity is enhanced after binding metal ions, and that Ga(3+) complexes display possible superoxide dismutase (SOD)-like activity.

  15. Expanding the Therapeutic Spectrum of Artemisinin:Activity Against Infectious Diseases Beyond Malaria and Novel Pharmaceutical Developments

    Institute of Scientific and Technical Information of China (English)

    Thomas Efferth; Jose J.G. Marin; Marta R. Romero; Anna Rita Bilia; Ahmed Galal Osman; Mahmoud ElSohly; Michael Wink; Rudolf Bauer; Ikhlas Khan; Maria Camilla Bergonzi

    2016-01-01

    The interest of Western medicine in Traditional Chinese Medicine (TCM) as a source of drug leads/new drugs to treat diseases without available efficient therapies has been dramatical y augmented in the last decades by the extensive work and the outstanding findings achieved within this kind of medicine. The practice of TCM over thousands of years has equipped scientists with substantial experience with hundreds of plants that led to the discovery of artemisinin (qinghaosu), which is extracted from the medicinal plant Artemisia annua L. (qinghao). The unexpected success of artemisinin in combating malaria has drawn strong attention from the scientific community towards TCM. Artemisinin was discovered by Youyou Tu in 1972. Since then, several novel pharmacological activities based on the well-known properties of the sesquiterpene lactone structure with the oxepane ring and an endoperoxide bridge have been unravelled. Beyond malaria, artemisinin and its derivatives (artemisinins) exert profound activities towards other protozoans (Leishmania, Trypanosoma, amoebas, Neospora caninum, and Eimeria tenella), trematodes (Schistosoma, liver flukes), and viruses (human cytomegalovirus, hepatitis B and C viruses). Less clear is the effect against bacteria and fungi. Based on the promising results of artemisinin and the first generation derivatives (artesunate, artemether, arteether), novel drug development strategies have been pursued. These included the synthesis of acetal-and non-acetal-type artemisinin dimeric molecules as wel as developing nanotechnological approaches, e.g. artemisinin-based liposomes, niosomes, micel es, solid lipid nanocarriers, nanostructured lipid carriers, nanoparticles, fullerenes and nanotubes. The current review presents an overview on different aspects of artemisinins, including sources, chemistry, biological/pharmacological properties, types of infectious pathogens that are susceptible to artemisinins in vitro and in vivo, in addition to the

  16. Evaluation of new pharmaceuticals using in vivo neutron inelastic scattering and neutron activation analysis

    International Nuclear Information System (INIS)

    Nutritional status of patients can be evaluated by monitoring changes in body composition, including depletion of protein and muscle, adipose tissue distribution and changes in hydration status, bone or cell mass. Fast neutron activation (for N and P) and neutron inelastic scattering (for C and O) are used to assess in vivo elements characteristic of specific body compartments. The fast neutrons are produced with a sealed deuterium-tritium (D-T) neutron generator. This method provides the most direct assessment of body composition. Non-bone phosphorus for muscle is measured by the 31P(n,α)28Al reaction, and nitrogen for protein via the (n,2n) fast neutron reaction. Inelastic neutron scattering is used for the measurement of total body carbon and oxygen. Carbon is used to derive body fat, after subtracting carbon contributions due to protein, bone and glycogen. Carbon-to-oxygen (C/O) ratio is used to measure distribution of fat and lean tissue in the body and to monitor small changes of lean mass and its quality. In addition to evaluating the efficacy of new treatments, the system is used to study the mechanisms of lean tissue depletion with aging and to investigate methods for preserving function and quality of life in the elderly. (author)

  17. Life cycle analysis of solvent reduction in pharmaceutical synthesis using continuous adsorption for palladium removal.

    Science.gov (United States)

    Slater, C Stewart; Savelski, Mariano J; Ruiz-Felix, Marie Nydia

    2013-01-01

    The life cycle emissions associated with the reduction of wastes from an adsorption process to remove palladium complexes in drug manufacture have been evaluated. The study assessed a green improvement to a process step in an active pharmaceutical ingredient synthesis where palladium catalyst is removed from a reaction mixture. The greener process uses a continuous adsorption system, composed of a more efficient adsorbent, consuming less organic solvent and rinse water, which results in less waste disposal. The newer process is also more energy and cost efficient from an operational perspective. There is a 94% reduction in the carbon footprint of the new process when compared to the current operation. PMID:23947697

  18. Design of cost controller based on activity based costing for pharmaceutical enterprises%基于ABC的药业企业成本控制系统设计

    Institute of Scientific and Technical Information of China (English)

    王晓艳; 吴锋

    2012-01-01

    精确的企业成本信息是企业进行生产管理、实施生产控制、乃至生产决策的重要依据.然而传统作业成本法扭曲成本信息的现象很可能导致成本失控,经营决策失败.本文引入了新的作业成本法(Activity Based Costing,ABC),探讨了ABC在药业企业成本核算中的基本原理,针对药业企业的运作模式、流程和特点,构建了基于作业成本法的药业企业成本控制系统模型,该模型对药业企业市场营销及竞争战略制定提供了重要的决策依据.%The precise cost information is an important basis for production management, production control, and even production decisions of enterprises. However, the phenomenon that the traditional activity-based costing methods distort cost information often lead to cost out of control and the failure of management decision. This paper introduces the new operating cost method (Activity Based Costing, ABC), and discusses the basic principle of ABC in cost accounting of pharmaceutical enterprise, in allusion to pharmaceutical enterprise operation mode, process and characteristics, it constructs the cost control system model about pharmaceutical enterprise Based on the activity-based Costing method. The model provides an important basis for decision-making on the marketing and competition strategy formulation of pharmaceutical enterprise.

  19. Changes in Phytochemical Synthesis, Chalcone Synthase Activity and Pharmaceutical Qualities of Sabah Snake Grass (Clinacanthus nutans L.) in Relation to Plant Age

    OpenAIRE

    Ali Ghasemzadeh; Alireza Nasiri; Jaafar, Hawa Z. E.; Ali Baghdadi; Izham Ahmad

    2014-01-01

    In the current study, changes in secondary metabolite synthesis and the pharmaceutical quality of sabah snake grass leaves and buds were considered in relation to plant age (1 month, 6 months, and 1 year old). The activity of the enzyme chalcone synthase (CHS, EC 2.3.1.74) was measured, as it is a key enzyme for flavonoid production. Significant differences in total flavonoid (TF) production were observed between the three plant growth periods and the different plant parts. The highest conten...

  20. Effect of Different Processing Technology of Acer. Ginnala. Maxim on the Active Ingredients and Antioxidant Activity%加工工艺对苦茶槭有效成分和抗氧化活性的影响

    Institute of Scientific and Technical Information of China (English)

    孔成诚; 方成武; 张传标; 张明燕

    2016-01-01

    To study on the effects of different processing method of Acer. Ginnala. Maxim main active ingredient and antioxidant activity, used Acer Ginnala Maxim as raw material in different processing methods, HPLC method was used to measure main active ingredient content of gallic acid. DPPH method was used to determine the scavenging effect on free radicals. Result showed that Acer. Ginnala. Maxim processing method of Black tea, gallic acid content was ( 18. 49±1. 13) mg/g, higher than processing method of green tea of (12. 45±1. 92) mg/g and dried in shade of (14. 28±1. 13) mg/g. Antioxidant activity of the different processing methods of Acer. Ginnala. Maxim was in the following order:the method of green tea (0. 443 mg/mL) < the method of dried in shade (0. 726 mg/mL) < the method of black tea (1. 286 mg/mL) . From the angle of improve the content of Gallic acid and increased the antioxidant activity, the processing method of black tea was much better.%研究了不同加工工艺对苦茶槭主要活性成分和抗氧化活性的影响,以期筛选最适合苦茶槭加工方式。对所采集的苦茶槭鲜叶以不同加工方式进行加工处理,采取HPLC法对苦茶槭主要有效成分没食子酸含量进行检测。采用DPPH法评价不同加工方法苦茶槭自由基的抗氧化活动。结果显示,采用红茶加工法的苦茶槭没食子酸含量为(18.49依1.13) mg/g高于绿茶加工法(12.45依1.92) mg/g和自然阴干法(14.28依1.13) mg/g。不同加工方法的苦茶槭IC50依次为:绿茶工艺(0.443 mg/mL)<自然阴干(0.726 mg/mL)<红茶工艺(1.286 mg/mL)。从提高苦茶槭没食子酸含量,增加抗氧化活性角度建议采用红茶加工方法。

  1. Risk-based prioritization of pharmaceuticals in the natural environment in Iraq.

    Science.gov (United States)

    Al-Khazrajy, Omar S A; Boxall, Alistair B A

    2016-08-01

    Numerous studies have demonstrated the occurrence of pharmaceuticals in the natural environment, raising concerns about their impact on non-target organisms or human health. One region where little is known about the exposure and effects of pharmaceuticals in the environment is Iraq. Due to the high number of pharmaceuticals used by the public health sector in Iraq (hospitals and care centres) and distributed over the counter, there is a need for a systematic approach for identifying substances that should be monitored in the environment in Iraq and assessed in terms of environmental risk. In this study, a risk-based prioritization approach was applied to 99 of the most dispensed pharmaceuticals in three Iraqi cities, Baghdad, Mosul and Basrah. Initially, information on the amounts of pharmaceuticals used in Iraq was obtained. The top used medicines were found to be paracetamol, amoxicillin and metformin with total annual consumption exceeding 1000 tonnes per year. Predicted environmental concentrations (PECs) and predicted no-effect concentrations (PNECs), derived from ecotoxicological end-points and effects related to the therapeutic mode of action, were then used to rank the pharmaceuticals in terms of risks to different environmental compartments. Active pharmaceutical ingredients used as antibiotics, antidepressants and analgesics were identified as the highest priority in surface water, sediment and the terrestrial environment. Antibiotics were also prioritized according to their susceptibility to kill or inhibit the growth of bacteria or to accelerate the evolution and dissemination of antibiotic-resistant genes in water. Future work will focus on understanding the occurrence, fate and effects of some of highly prioritized substances in the environment. PMID:27137195

  2. Pharmaceutical Advertisements in Indian Scientific Journals: Analysis of Completeness of Information Content

    Directory of Open Access Journals (Sweden)

    Dr. Jignesh K Ved,

    2010-10-01

    Full Text Available Purpose: In India, pharmaceutical advertising is governed by ‘The Drugs and Magic Remedies (Objectionable Advertisements Act, 1954’, and ‘The Drugs and Cosmetics Rules, 1945’. These acts do not specify the ‘minimum essential information requirements’ for an dvertisement, keeping this area ill-defined. The ‘Organization ofPharmaceutical Producers of India (OPPI’, in its ‘Code of Pharmaceutical Marketing Practices’, provides a guideline for the information requirements in advertisements. Our study is intended to analyze the ‘completeness of information content’, in pharmaceutical advertisements, published in 2009-10 in Indian Scientific journals, in the context of OPPI code. Method: Indian Scientific Journals (2009-10 issues were surveyed for pharmaceutical advertisements.Advertisements were classified as ‘Full’ or ‘Reminder’ advertisements and were separately analyzed for the presence of information on ‘Brand name’; ‘Active ingredient(s’; ‘Marketer’s Name and Address’; ‘Date of Production of advertisement’; ‘Abbreviated Prescribing Information (only for Full advertisements’ and ‘Overall completeness’. Data was expressed as absolute numbers and percentage.Results: Full advertisements (n=34 demonstrated 41.2% of ‘Overall completeness’. ‘Date’ was missing in 52.9%, while ‘Marketer’s Name and Address’ in 17.6% of advertisements. ‘Active ingredient’ was mentioned in all, while ‘Abbreviated Prescribing Information’ was complete in 97.1% of Full advertisements. Reminder advertisements (n=134 demonstrated 10.4% of ‘Overall completeness’. ‘Date’ was issing in 88.1%, ‘Marketer’s Name and Address’ in 29.1% and ‘Active ingredient’ in 8.2% of Reminder advertisements.Conclusion: Low percentage of completeness, as observed in our study, indicates a lack of adherence to OPPI code and need for mandatory regulations, to ensure information completeness in

  3. Phlorizin, an Active Ingredient of Eleutherococcus senticosus, Increases Proliferative Potential of Keratinocytes with Inhibition of MiR135b and Increased Expression of Type IV Collagen.

    Science.gov (United States)

    Choi, Hye-Ryung; Nam, Kyung-Mi; Lee, Hyun-Sun; Yang, Seung-Hye; Kim, Young-Soo; Lee, Jongsung; Date, Akira; Toyama, Kazumi; Park, Kyoung-Chan

    2016-01-01

    E. senticosus extract (ESE), known as antioxidant, has diverse pharmacologic effects. It is also used as an antiaging agent for the skin and phlorizin (PZ) is identified as a main ingredient. In this study, the effects of PZ on epidermal stem cells were investigated. Cultured normal human keratinocytes and skin equivalents are used to test whether PZ affects proliferative potential of keratinocytes and how it regulates these effects. Skin equivalents (SEs) were treated with ESE and the results showed that the epidermis became slightly thickened on addition of 0.002% ESE. The staining intensity of p63 as well as proliferating cell nuclear antigen (PCNA) is increased, and integrin α6 was upregulated. Analysis of ESE confirmed that PZ is the main ingredient. When SEs were treated with PZ, similar findings were observed. In particular, the expression of integrin α6, integrin β1, and type IV collagen was increased. Levels of mRNA for type IV collagen were increased and levels of miR135b were downregulated. All these findings suggested that PZ can affect the proliferative potential of epidermal cells in part by microenvironment changes via miR135b downregulation and following increased expression of type IV collagen. PMID:27042261

  4. Phlorizin, an Active Ingredient of Eleutherococcus senticosus, Increases Proliferative Potential of Keratinocytes with Inhibition of MiR135b and Increased Expression of Type IV Collagen

    Directory of Open Access Journals (Sweden)

    Hye-Ryung Choi

    2016-01-01

    Full Text Available E. senticosus extract (ESE, known as antioxidant, has diverse pharmacologic effects. It is also used as an antiaging agent for the skin and phlorizin (PZ is identified as a main ingredient. In this study, the effects of PZ on epidermal stem cells were investigated. Cultured normal human keratinocytes and skin equivalents are used to test whether PZ affects proliferative potential of keratinocytes and how it regulates these effects. Skin equivalents (SEs were treated with ESE and the results showed that the epidermis became slightly thickened on addition of 0.002% ESE. The staining intensity of p63 as well as proliferating cell nuclear antigen (PCNA is increased, and integrin α6 was upregulated. Analysis of ESE confirmed that PZ is the main ingredient. When SEs were treated with PZ, similar findings were observed. In particular, the expression of integrin α6, integrin β1, and type IV collagen was increased. Levels of mRNA for type IV collagen were increased and levels of miR135b were downregulated. All these findings suggested that PZ can affect the proliferative potential of epidermal cells in part by microenvironment changes via miR135b downregulation and following increased expression of type IV collagen.

  5. On-demand continuous-flow production of pharmaceuticals in a compact, reconfigurable system.

    Science.gov (United States)

    Adamo, Andrea; Beingessner, Rachel L; Behnam, Mohsen; Chen, Jie; Jamison, Timothy F; Jensen, Klavs F; Monbaliu, Jean-Christophe M; Myerson, Allan S; Revalor, Eve M; Snead, David R; Stelzer, Torsten; Weeranoppanant, Nopphon; Wong, Shin Yee; Zhang, Ping

    2016-04-01

    Pharmaceutical manufacturing typically uses batch processing at multiple locations. Disadvantages of this approach include long production times and the potential for supply chain disruptions. As a preliminary demonstration of an alternative approach, we report here the continuous-flow synthesis and formulation of active pharmaceutical ingredients in a compact, reconfigurable manufacturing platform. Continuous end-to-end synthesis in the refrigerator-sized [1.0 meter (width) × 0.7 meter (length) × 1.8 meter (height)] system produces sufficient quantities per day to supply hundreds to thousands of oral or topical liquid doses of diphenhydramine hydrochloride, lidocaine hydrochloride, diazepam, and fluoxetine hydrochloride that meet U.S. Pharmacopeia standards. Underlying this flexible plug-and-play approach are substantial enabling advances in continuous-flow synthesis, complex multistep sequence telescoping, reaction engineering equipment, and real-time formulation. PMID:27034366

  6. Supply Network Planning for New Product Market Entry in the Pharmaceutical Industry

    DEFF Research Database (Denmark)

    Hansen, Klaus Reinholdt Nyhuus; Grunow, Martin

    2011-01-01

    in succession and each drug is only produced few times annually. Assuming fixed intermediate availability of API, supply network planning consists of finding inventory levels and production volumes for downstream stages to cope with the highly fluctuating demand of new markets. Unique for the pharmaceutical...... planning before and during the market entry of the drug after the drug has been approved. Production of the active pharmaceutical ingredient [API] is characterized by long change-over times due to cleaning requirements. Production planning is long term, multiple batches of each drug are produced...... products have to be scrapped. We have developed an MILP supply network planning model, which sets time phased market entries and finds inventory levels and production volumes to balance fluctuating demand with fixed periodic production of the API. Our model is recourse-based and considers demand...

  7. [Antiperspirants and deodorants--ingredients and evaluation].

    Science.gov (United States)

    Lukacs, V A; Korting, H C

    1989-01-01

    Antitranspirants and deodorants gain more and more interest. Aluminium chlorohydrate and aluminium zirkonium tetrachlorohydrate glycine complex are the most frequently used active ingredients in commercial antitranspirants today. Aluminium chloride and propantheline bromide, the anticholinergic substance, are important alternatives although less common. Active ingredients of deodorants are mainly perfumes or bactericidal/bacteriostatic substances, such as triclosan. In addition, there are substances which are meant to bind offending smells (e.g. zinc ricinoleate) or to influence the skin surface pH (e.g. triethyl citrate). As in the cosmetics industry in general, both safety and efficacy of a product are major parameters in the experimental and clinical evaluation. Establishment of efficacy is based on olfactory tests in model situations as well as on the detection of associated effects (e.g. influence on cutaneous microflora). PMID:2656175

  8. 复方卡力孜然凝胶剂主要活性成分体外经皮渗透%In vitro Percutaneous Penetration of Main Active Ingredient from Fufang Kali Ziran Gel

    Institute of Scientific and Technical Information of China (English)

    邢建国; 王新春; 赵媛; 马建红; 薛桂蓬; 刘桂花

    2012-01-01

    目的:研究不同透皮促进剂对复方卡力孜然凝胶剂3种有效成分体外经皮渗透的影响,筛选有效的透皮吸收促进剂.方法:采用改良Franz扩散池法、离体鼠皮进行体外透皮试验,HPLC测定透皮吸收促进剂对3种有效成分补骨脂素、异补骨脂素及蛇床子素的累积透过量及透皮速率的影响.结果:不同促透剂对复方卡力孜然凝胶剂中补骨脂素、异补骨脂素及蛇床子素体外透皮吸收产生不同的影响,确定2%氮酮为促进剂时3种有效成分的促透效果最好.结论:2%氮酮能够促进复方卡力孜然凝胶剂3种有效成分的有效渗透,透皮吸收过程符合Higuchi方程.%Objective: To study on effects of in vitro percutaneous penetration of different penetration enhancers for three active ingredients from Fufang Kali Ziran gel, and to screen out effective transdermal absorption enhancers. Method;In vitro transdermal test was used by modified Franz diffusion cell method and in vitro rat skin, effect of cumulative penetration volume and penetration rate from transdermal absorption enhancers for three active ingredients ( psoralen, isopsoralen and osthole) was determined by HPLC. Result; Different enhancers were found to have different degree in vitro penetration enhancing effect on psoralen, isopsoralen and osthole in Fufang Kali Ziran gel,determined 2% azone had optimum promoting effect as enhancers to three active ingredients. Conclusion;2% azone could promote effective penetration of three active ingredients from Fufang Kali Ziran gel. This process of penetration absorption could be in line with Higuchi equation.

  9. 药用辅料对药品安全性的影响%The impact of pharmaceutical excipients on the drug safety

    Institute of Scientific and Technical Information of China (English)

    杨锐; 孙会敏; 于丽娜; 袁松

    2012-01-01

    药用辅料和药物活性成分共同组成了我们日常使用的药品,药用辅料同药物活性成分一样全程参与了体内的吸收、分布、代谢、排泄过程,所以药用辅料的安全性直接影响到了药物制剂的安全性,本文从药用辅料本身的毒副作用、药用辅料同药物活性物质(API)的配伍禁忌、药用辅料有毒副作用的杂质以及其他引起的药品安全性问题的辅料因素等四个方面阐述了药用辅料同药品安全性的关系.%Our daily used medicines were composed of pharmaceutical excipients and active pharmaceutical ingredients (API). The pharmaceutical excipients also involved in the whole process of absorption,distribution,metabolism and excretion in vivo as well as API. Therefore,the safety of pharmaceutical excipients was closely related to that of the pharmaceutical preparations. This review explained the relationship between the pharmaceutical excipients and medicines from the four aspects as below;the toxicity and side effects of pharmaceutical excipients itself,incompatibility of pharmaceutical excipients and API,the toxic impurity of pharmaceutical excipients and the other influencing factors of pharmaceutical excipients to the drug safety.

  10. [Pharmaceutical chemistry of general anaesthetics].

    Science.gov (United States)

    Szász, György; Takácsné, Novák Krisztina

    2004-01-01

    The paper represents the first part of a planned series of reviews about pharmaceutical chemistry of drugs acting on the central nervous system. The authorial aim and editorial concepts are the same were followed in a former series of papers about pharmaceutical chemistry of agents effecting the heart, blood circulation and vegetative nervous system. Consequently, general anaesthetics are discussed in the present paper through the chapters "history, preparation; structure-properties-activity; application; analysis".

  11. Toxicological and ecotoxicological risk-based prioritization of pharmaceuticals in the natural environment.

    Science.gov (United States)

    Guo, Jiahua; Sinclair, Chris J; Selby, Katherine; Boxall, Alistair B A

    2016-06-01

    Approximately 1500 active pharmaceutical ingredients are currently in use; however, the environmental occurrence and impacts of only a small proportion of these have been investigated. Recognizing that it would be impractical to monitor and assess all pharmaceuticals that are in use, several previous studies have proposed the use of prioritization approaches to identify substances of most concern so that resources can be focused on these. All of these previous approaches suffer from limitations. In the present study, the authors draw on experience from previous prioritization exercises and present a holistic approach for prioritizing pharmaceuticals in the environment in terms of risks to aquatic and soil organisms, avian and mammalian wildlife, and humans. The approach considers both apical ecotoxicological endpoints as well as potential nonapical effects related to the therapeutic mode of action. Application of the approach is illustrated for 146 active pharmaceuticals that are used either in the community or in hospital settings in the United Kingdom. Using the approach, 16 compounds were identified as a potential priority. These substances include compounds belonging to the antibiotic, antidepressant, anti-inflammatory, antidiabetic, antiobesity, and estrogen classes as well as associated metabolites. In the future, the prioritization approach should be applied more broadly around the different regions of the world. Environ Toxicol Chem 2016;35:1550-1559. © 2016 SETAC. PMID:26799673

  12. Stimuli-sensitive hydrogels for pharmaceutical and medical applications

    Directory of Open Access Journals (Sweden)

    Ilić-Stojanović Snežana

    2011-01-01

    Full Text Available Hydrogels are three-dimensional cross-linked hydrophilic polymers that swell in water and aqueous solutions without dissolving in them. They are very sensitive to environmental stimulus, which is manifested by a sharp phase transition. This feature is important for their application in the pharmaceutical field, especially for making formulations with controlled release of active ingredients, with the correction of the solubility, degradation and their toxicity reducing. Because of the compatibility with living tissues, hydrogels can be used in different medical purposes (for making contact lenses, stents, balloon catheters, artificial muscles, substitutes for arteries and veins, trachea, oviduct. This work presents methods (chemical and physical for obtaining hydrogels, their properties and sensitivity to environmental stimuli (temperature, pH, magnetic field, as well as their potential application in medicine and pharmacy.

  13. Effects of Manufacturing Conditions on Pharmaceutical Properties of Petrolatum Ointment.

    Science.gov (United States)

    Ashizuka, Yuki; Horisawa, Eijiro

    2016-08-01

    Oleaginous white petrolatum ointment (WP ointment) is one of the most commonly used dosage forms in the preparation of topical products. In general, WP ointments containing medium chain fatty acid triglycerides (MCT) are manufactured through a process of melting, mixing, agitating, and cooling. To investigate the pharmaceutical properties of WP ointments in greater detail, we examined manufacturing factors which could potentially influence the pharmaceutical properties of the finished product. WP ointment samples containing 10% MCT were stirred with a homogenizer and a paddle mixer at 65°C, then the homogenizer was stopped. Next, the paddle-mixer was stopped at several planned temperature points at which different samples were taken. Each sample was then cooled under the following planned conditions: rapid-cooling [-50°C/h] and slow-cooling [-7.5°C/h]. The pharmaceutical properties of each WP ointment sample, along with the appearance (Optical/digital microscope), hardness (Rheometer), and bleeding ability (100 Mesh wire-net cone) were measured. Then, release profiles were performed with a WP ointment using the model active ingredient Vitamin D. As a result, high hardness, low bleeding ability and low release profile were observed in the WP ointment samples that were manufactured under the condition of stopping the paddle-mixer at 40°C. However, the influence of cooling speed was observed to affect only hardness. Through optical microscopic observation, it was found that the appearance of WP ointment samples differed depending on the conditions under which they were manufactured. In this study, it was clear that the pharmaceutical properties of WP ointment samples were particularly influenced by the paddle-mixer stopping temperature. PMID:27193304

  14. Food Ingredients as Anti-Obesity Agents.

    Science.gov (United States)

    Saito, Masayuki; Yoneshiro, Takeshi; Matsushita, Mami

    2015-11-01

    Brown adipose tissue (BAT) is a site of adaptive non-shivering thermogenesis after cold exposure, and is involved in the regulation of energy expenditure and body fatness. BAT can be activated and recruited by not only cold exposure but also by various food ingredients including capsaicin in chili pepper and catechins in green tea, which would be easily and safely applicable to our daily life for preventing obesity. PMID:26421678

  15. On the relationship of inter-particle cohesiveness and bulk powder behavior: Flowability of pharmaceutical powders.

    Science.gov (United States)

    Capece, Maxx; Silva, Karina Ruiz; Sunkara, Divya; Strong, John; Gao, Ping

    2016-09-10

    This study investigates the relationship between particle interactions dominated by the cohesive van der Waals force and powder flowability for materials commonly used by the pharmaceutical industry in oral solid dosage formulation. This study first sought to correlate the granular Bond number, defined as the ratio of the inter-particle cohesion force to particle weight, to the flow function coefficient, a metric commonly used to assess powder flowability. However, the granular Bond number which strictly quantifies inter-particle cohesiveness was found to correlate poorly with powder flowability due to the complexity associated with particle assemblies. To account for the multitude of interactions between particles of different sizes within a powder and to more precisely predict bulk powder behavior, a population-dependent granular Bond number was proposed. The population-dependent granular Bond number which explicitly accounts for particle size distribution and described herein as a quantification of powder cohesiveness (instead of inter-particle cohesiveness) was shown to correlate well with the flow function coefficient for a wide variety of materials including four active pharmaceutical ingredients (APIs) and fourteen common pharmaceutical excipients. Due to the success of the population-dependent granular Bond number, it was extended to predict the flowability of powder blends. This so-called population-dependent multi-component granular Bond number takes into account relevant material properties and particle interactions and was used to predict the flowability of 6-component powder blends containing acetaminophen as a model cohesive active pharmaceutical ingredient. Prediction of bulk powder behavior from individual material properties as accomplished here may be highly useful in formulation development. PMID:27353729

  16. Niosomes as Nano-Delivery Systems in the Pharmaceutical Field.

    Science.gov (United States)

    Cerqueira-Coutinho, Cristal; Dos Santos, Elisabete P; Mansur, Claudia Regina E

    2016-01-01

    Nanosystems used in the pharmaceutical field aim to guarantee a controlled release and efficacy boost with dose reduction of the drug. The same active ingredient could be vehiculated in different concentrations in distinct nanosystems. Among these nanostructures, the vesicular ones present a versatile delivery system that could be applied to encapsulate lipophilic, amphiphilic, and hydrophilic compounds. Liposomes are the most well-known vesicular nanosystems; however, there are others, such as niosomes, that are composed of nonionic surfactants that are polymeric or conventional. Niosomes could be prepared using the thin film hydration method, in which the active ingredient is solubilized in organic solvent with the surfactant or in aqueous solution depending on its polarity. In addition, co-surfactants could be used to improve stabilization and vesicle integrity because they occupy regions in the interface where the mainly surfactant could not reach. Vesicular nanosystems could be characterized by different techniques, such as microscopy, dynamic light scattering, nuclear magnetic resonance, and others. These nanostructures could be applied to drugs (administered by different routes) or to gene and cosmetic delivery systems. PMID:27651102

  17. The removal of endocrine disrupting compounds, pharmaceutically activated compounds and cyanobacterial toxins during drinking water preparation using activated carbon--a review.

    Science.gov (United States)

    Delgado, Luis F; Charles, Philippe; Glucina, Karl; Morlay, Catherine

    2012-10-01

    This paper provides a review of recent scientific research on the removal by activated carbon (AC) in drinking water (DW) treatment of 1) two classes of currently unregulated trace level contaminants with potential chronic toxicity-pharmaceutically activate compounds (PhACs) and endocrine disrupting compounds (EDCs); 2) cyanobacterial toxins (CyBTs), which are a group of highly toxic and regulated compounds (as microcystin-LR); and 3) the above mentioned compounds by the hybrid system powdered AC/membrane filtration. The influence of solute and AC properties, as well as the competitive effect from background natural organic matter on the adsorption of such trace contaminants, are also considered. In addition, a number of adsorption isotherm parameters reported for PhACs, EDCs and CyBTs are presented herein. AC adsorption has proven to be an effective removal process for such trace contaminants without generating transformation products. This process appears to be a crucial step in order to minimize PhACs, EDCs and CyBTs in finished DW, hence calling for further studies on AC adsorption removal of these compounds. Finally, a priority chart of PhACs and EDCs warranting further study for the removal by AC adsorption is proposed based on the compounds' structural characteristics and their low removal by AC compared to the other compounds. PMID:22885596

  18. The removal of endocrine disrupting compounds, pharmaceutically activated compounds and cyanobacterial toxins during drinking water preparation using activated carbon--a review.

    Science.gov (United States)

    Delgado, Luis F; Charles, Philippe; Glucina, Karl; Morlay, Catherine

    2012-10-01

    This paper provides a review of recent scientific research on the removal by activated carbon (AC) in drinking water (DW) treatment of 1) two classes of currently unregulated trace level contaminants with potential chronic toxicity-pharmaceutically activate compounds (PhACs) and endocrine disrupting compounds (EDCs); 2) cyanobacterial toxins (CyBTs), which are a group of highly toxic and regulated compounds (as microcystin-LR); and 3) the above mentioned compounds by the hybrid system powdered AC/membrane filtration. The influence of solute and AC properties, as well as the competitive effect from background natural organic matter on the adsorption of such trace contaminants, are also considered. In addition, a number of adsorption isotherm parameters reported for PhACs, EDCs and CyBTs are presented herein. AC adsorption has proven to be an effective removal process for such trace contaminants without generating transformation products. This process appears to be a crucial step in order to minimize PhACs, EDCs and CyBTs in finished DW, hence calling for further studies on AC adsorption removal of these compounds. Finally, a priority chart of PhACs and EDCs warranting further study for the removal by AC adsorption is proposed based on the compounds' structural characteristics and their low removal by AC compared to the other compounds.

  19. Pharmaceutical market in Serbia

    Directory of Open Access Journals (Sweden)

    Veselin Tima Dickov

    2012-02-01

    Full Text Available Marketing concept formed around the focus on the consumers, their needs, wants and demands, evolves in the case of pharmaceutical into a care of the complex interest of constituents generating demand on this market and #8211; pres scribers whose role is to select therapies, pharmacists who dispense drugs within a specialized distribution channel to the final consumer -patient, alongside the payers and #8211; the state and or insurance companies refund a part of or total costs of the pharmaceutical product. A special challenge that the subject raises is the existence of controversy generated from two sources. Marketing controversy stems from criticism leveled at the effectiveness and efficiency of marketing activities and the debatable ethical code of conduct. [J Intercult Ethnopharmacol 2012; 1(1.000: 44-51

  20. Ecotoxicological assessment using six pharmaceuticals commonly found in wastewaters

    OpenAIRE

    Taipale, Paula; Ursin, Sisko

    2011-01-01

    Pharmaceutical residues in wastewaters are relatively new concern in environment protection. The usage of pharmaceuticals has increased a lot and their impact on the environment is unknown. Low levels of pharmaceuticals have been detected in many countries in sewage treatment plant effluents, surface waters, seawaters, groundwater and some drinking waters. Pharmaceutically-active compounds until recently have not been studied however even small residues of pharmaceuticals can have an effect o...

  1. Anti-Phytopthora capsici Activities and Potential Use as Antifungal in Agriculture of Alpinia galanga Swartz, Curcuma longa Linn, Boesenbergia pandurata Schut and Chromolaena odorata: Bioactivities Guided Isolation of Active Ingredients

    Directory of Open Access Journals (Sweden)

    Wilart Pompimon

    2009-01-01

    Full Text Available Problem statement: Plant derived fungicides are now being subjects of many research groups. These secondary metabolites have enormous potential to inspire and influence modern agrochemical research. The study aimed to investigate the antifungal activity and their potential use as fungicides in the agriculture of crude extracts and purified compounds derived from plants used in traditional medicines. Approach: Four medicinal plants including A. galanga, C. longa, B. pandurata and C. odorata were selected and percolated with hexane, ethyl acetate, acetone or methanol. The extracts were purified and elucidated their chemical structures. Disc mycelial growth inhibition was applied in order to determine their anti P. capsici activity and the field study was performed to determine their potential use in controlling fungal infection in chili plants compared with commercial fungicides such as captan and bio-control Trichoderma virens. Results: All crude extract inhibited mycelial growth of the fungus performed with similar efficacy. ED90 was equal to 300 ppm. Among plants studied B. pandurata was the most potent against P. capsici. The proposed active ingredients were pinostrobin and pinocembrin. In the field study, pinocembrin mediated the same anti P. capsici activity as captan. B. pandurata can protect chili from infection, thus increasing crop yield of chili comparable to Trichoderma virens. Conclusion: The results clearly showed that the extracts of the four plants studied could be considered as potential sources of novel fungicides. Particularly, B. pandurata has a very high potential as raw material for developing the antifungal molecule of non-petrochemical, naturally eco-friendly, easily obtainable and not toxic to human beings and environment, at least for use in chili growing.

  2. 药品招标采购活动中相关质量术语解读%Interpretation of the Quality Related Terminology in Pharmaceutical Bidding Activities

    Institute of Scientific and Technical Information of China (English)

    王爱杰; 付加雷

    2013-01-01

    Objective: To conduct a monographic study and analysis on the issues of varied interpretations of the related terminology of drug quality in the pharmaceutical bidding schemes of various provinces and cities . Methods:The drug-related quality terminology used in each provincial pharmaceutical bidding scheme was summarized and ana-lyzed . Results:The new interpretations of the quality terms were worked out with more scientific explanations and sug-gestions as well . Conclusion: The standardization and unification of quality related terminology are not only conducive to the country ’ s pharmaceutical bidding activities , but also benefit to the level classification of pharmaceutical quality .%目的:针对目前各省市药品招标采购方案中药品相关的质量术语的解释存在不同的问题,进行专题研究和分析。方法:对各省药品招标采购方案中药品相关的质量术语进行总结、归纳与分析。结果:对各术语进行了新的解读,并给出了更为科学的解释和建议。结论:各个质量术语的规范与统一,不仅有利于全国的药品招标采购活动,更有利于药品的质量层次划分。

  3. Pharmaceutically active compounds: Their removal during slow sand filtration and their impact on slow sand filtration bacterial removal.

    Science.gov (United States)

    D'Alessio, Matteo; Yoneyama, Bunnie; Kirs, Marek; Kisand, Veljo; Ray, Chittaranjan

    2015-08-15

    Slow sand filtration (SSF) has been widely used as a means of providing potable water due to its efficacy, low cost, and minimal maintenance. Advances in analytical instrumentation have revealed the occurrence of pharmaceutically active compounds (PhACs) in surface water as well as in groundwater. It is unclear if the presence of these compounds in the feed water can interfere with the performances of an SSF unit. The aim of this work was to examine i) the ability of two SSF units to remove six PhACs (caffeine, carbamazepine, 17-β estradiol [E2], estrone [E1], gemfibrozil, and phenazone), and ii) the impact of these PhACs on the removal of bacteria by two SSF units. The presence of PhACs in feed water for SSF can occur in surface waters impacted by wastewater or leakage from sewers and septic tanks, as well as in developing countries where unregulated use and improper disposal are prevalent. Two pilot-scale SSF units were used during the study. Unit B1 was fed with stream water with 1% of primary effluent added, while unit B2 was fed with stream water alone. Although limited removal (gemfibrozil, and phenazone occurred, the complete removal of caffeine, and the partial removal (11-92%) of E2 and E1 were observed in the two SSF units. The results of this study suggest that the occurrence of the selected PhACs, probably estrogens and caffeine, in the feed water at 50 μg L(-1) affected the ability of the schmutzdecke to remove total coliform and Escherichia coli. The bacterial removal achieved within the schmutzdecke dropped from 95% to less than 20% by the end of the study. This decrease in removal may be related to the change in the microbial community within the schmutzdecke. A diverse microbial community, including Bacteroidetes and several classes of Proteobacteria, was replaced by a microbial community in which Gammaproteobacteria was the predominant phylum (99%). Despite the low removal achieved within the schmutzdecke, removal of total coliform and E. coli

  4. 77 FR 17484 - Agency Information Collection Activities; Submission for Office of Management and Budget Review...

    Science.gov (United States)

    2012-03-26

    ... submission of listing. Note that unfinished products and active pharmaceutical ingredient listings will not... Register of August 29, 2006 (the 2006 proposed rule) (71 FR 51276), FDA proposed to revise part 207. The... Register of June 1, 2009 (74 FR 26248), FDA announced the availability of a guidance for industry...

  5. Automated visual inspection of imprinted pharmaceutical tablets

    Science.gov (United States)

    Bukovec, Marko; Špiclin, Žiga; Pernuš, Franjo; Likar, Boštjan

    2007-09-01

    This paper is on automated visual inspection of tablets that may, in contrast to manual tablet sorting, provide objective and reproducible tablet quality assurance. Visual inspection of the ever-increasing numbers of produced imprinted tablets, regulatory enforced for unambiguous identification of active ingredients and dosage strength of each tablet, is especially demanding. The problem becomes more tractable by incorporating some a priori knowledge of the imprint shape and/or appearance. For this purpose, we consider two alternative automated tablet defect detection methods. The geometrical method, incorporating geometrical a priori knowledge of the imprint shape, enables specific inspection of the imprinted and non-imprinted tablet surface, while the statistical method exploits statistical a priori knowledge of tablet surface appearance, derived from a training image database. The two methods were evaluated on a large tablet image database, consisting of 3445 images of four types of imprinted tablets, with and without typical production defects. A 'gold standard' for testing the performances of the two inspection methods was established by manually classifying the tablets into good and five defective classes. The results, obtained by ROC (receiver operating characteristics) analysis, indicate that the statistical method yields better defect detection sensitivity and specificity than the geometrical method. Both presented image analysis methods are quite general and promising tools for automated visual inspection of imprinted pharmaceutical tablets.

  6. Ion mobility spectrometry: a comprehensive and versatile tool for occupational pharmaceutical exposure assessment.

    Science.gov (United States)

    Armenta, S; Blanco, M

    2012-05-15

    The qualitative and quantitative capabilities of ion mobility spectrometry (IMS) as a comprehensive and powerful tool in workplace air monitoring have been demonstrated on the example of a Spanish pharmaceutical company. The developed IMS based procedure is capable of detecting and determining in air samples the active pharmaceutical ingredients (APIs) manipulated and/or produced in this pharmaceutical industry. Sensitivity, in the ng-pg range, selectivity, possibly to provide results in near real time, and reduction of analysis costs are the most important properties that ratify IMS as a serious alternative in occupational exposure assessment. The possibility of false positives by drift time interferences and false negatives by competitive ionization and also desorption process interferences has been deeply evaluated. Moreover, chemometric strategies based on self-modeling curve resolution (SMCR) have been applied to obtain qualitative and quantitative individual component information from overlapped peaks. The IMS procedure has been successfully applied to evaluate the concentration of APIs (nimesulide, dexketoprofen, deflazacort) handled by the pharmaceutical company employees in the making of tablets and granulates, and control measures have been suggested in accordance.

  7. Hot-Melt Extrusion: from Theory to Application in Pharmaceutical Formulation.

    Science.gov (United States)

    Patil, Hemlata; Tiwari, Roshan V; Repka, Michael A

    2016-02-01

    Hot-melt extrusion (HME) is a promising technology for the production of new chemical entities in the developmental pipeline and for improving products already on the market. In drug discovery and development, industry estimates that more than 50% of active pharmaceutical ingredients currently used belong to the biopharmaceutical classification system II (BCS class II), which are characterized as poorly water-soluble compounds and result in formulations with low bioavailability. Therefore, there is a critical need for the pharmaceutical industry to develop formulations that will enhance the solubility and ultimately the bioavailability of these compounds. HME technology also offers an opportunity to earn intellectual property, which is evident from an increasing number of patents and publications that have included it as a novel pharmaceutical formulation technology over the past decades. This review had a threefold objective. First, it sought to provide an overview of HME principles and present detailed engineered extrusion equipment designs. Second, it included a number of published reports on the application of HME techniques that covered the fields of solid dispersions, microencapsulation, taste masking, targeted drug delivery systems, sustained release, films, nanotechnology, floating drug delivery systems, implants, and continuous manufacturing using the wet granulation process. Lastly, this review discussed the importance of using the quality by design approach in drug development, evaluated the process analytical technology used in pharmaceutical HME monitoring and control, discussed techniques used in HME, and emphasized the potential for monitoring and controlling hot-melt technology. PMID:26159653

  8. Alkaloids in the pharmaceutical industry: Structure, isolation and application

    Directory of Open Access Journals (Sweden)

    Nikolić Milan

    2003-01-01

    Full Text Available By the end of the 18th and the beginning of the 19th century a new era began in medicine, pharmaceutics and chemistry that was strongly connected with alkaloids and alkaloid drugs. Even before that it was known that certain drugs administered in limited doses were medicines, and toxic if taken in larger doses (opium, coke leaves, belladonna roots, monkshood tubers crocus or hemlock seeds. However, the identification, isolation and structural characterization of the active ingredients of the alkaloid drugs was only possible in the mid 20th century by the use of modern extraction equipment and instrumental methods (NMR, X-ray diffraction and others.In spite of continuing use over a long time, there is still great interest in investigating new drugs, potential raw materials for the pharmaceutical industry, as well as the more detailed investigation and definition of bio-active components and the indication of their activity range, and the partial synthesis of new alkaloid molecules based on natural alkaloids. The scope of these investigations, especially in the field of semi-synthesis is to make better use of the bio-active ingredients of alkaloid drugs, i.e. to improve the pharmacological effect (stronger and prolonged effect of the medicine, decreased toxicity and side effects, or to extend or change the applications. A combined classification of alkaloids was used, based on the chemical structure and origin, i.e. the source of their isolation to study alkaloid structure. For practical reasons, the following classification of alkaloids was used: ergot alkaloids, poppy alkaloids, tropanic alkaloids purine derivative alkaloids, carbon-cyclic alkaloids, and other alkaloids. The second part of this report presents a table of general procedures for alkaloid isolation from plant drugs (extraction by water non-miscible solvents, extraction by water-miscible solvents and extraction by diluted acid solutions. Also, methods for obtaining chelidonine and

  9. 药物共晶研究进展及应用%Pharmaceutical cocrystal research progress and application

    Institute of Scientific and Technical Information of China (English)

    弋东旭; 洪鸣凰; 徐军; 赵文杰; 任国宾

    2011-01-01

    Pharmaceutical cocrystal could be obtained by combining active pharmaceutical ingredient (API) and cocrystal former (CCF) in one crystal lattice through noncovalent interaction.It is a new pharmaceutical physical form which can improve the physicochemical properties, such as solubility, stability and bioavailability of API.It has becoming a novel hot spot in pharmaceutical research and development field.This paper mainly introduces the pharmaceutical cocrystal on its application, design, preparation and analysis method.%药物共晶是活性药物成分通过非共价键和共晶形成物结合在一个晶格中形成的.它是一种新的药物固体型态,可以改善药物的理化性质,比如改善溶解度、增加稳定性、提高生物利用度等,是目前药物研发的一个新的热点.本文主要介绍了药物共晶在药物研发中的应用及其设计、制备以及分析方法.

  10. A simple and sensitive method to analyze genotoxic impurity hydrazine in pharmaceutical materials.

    Science.gov (United States)

    Wang, Jenny; Yang, Samuel; Zhang, Kelly

    2016-07-15

    Hydrazine (N2H4) is a known genotoxic impurity that typically needs to be controlled down to low ppm level in pharmaceutical development. Hydrazine, however, is a challenging molecule to analyze using conventional analytical techniques due to its physical and chemical properties (e.g. lack of chromophore, absence of any carbon atom, low molecular weight, high polarity and volatility). Additionally, analysis in pharmaceutical samples commonly encounters significant interference from matrix components that greatly overshadow the response of hydrazine. This work describes a simple, accurate and sensitive reversed-phase liquid chromatography-UV derivatization method for determination of trace amount hydrazine in pharmaceutical materials featuring three prominent strategies to address the problems associated with hydrazine analysis. First, the derivatization reaction attaches chromophores to hydrazine, which greatly increases its sensitivity by UV-vis detection. Secondly, the derivatization reaction generates a lambda max that is well-shifted away from the absorption wavelengths of pharmaceutical matrix interferences. Thirdly, from a separation standpoint, the derivatization further removes matrix interference effects through chromatography by achieving higher resolution of the derivative product from the active pharmaceutical ingredient (API) and its related impurities for accurate quantitation for trace level of genotoxic impurities (GTIs). 2-Hydroxy-1-Naphthalaldehyde (HNA) was chosen as the derivatizing reagent, and the resulting hydrazone product has a maximum UV absorbance at wavelength of 406/424nm which is in the visible range. Since most drug substance and impurities have UV absorbance ranging from 190 to 380nm, interference from the matrix was minimized and the appropriate selectivity was obtained, the detection limit is 0.25ppm (0.25μg/g API). This method was validated and applied as a generic method to determine hydrazine for pharmaceutical process control

  11. Bioremediation Kinetics of Pharmaceutical Industrial Effluent

    OpenAIRE

    Šabić, M.; Vuković Domanovac, M.; Findrik Blažević, Z.; Meštrović, E.

    2015-01-01

    In recent years, concerns about the occurrence and fate of pharmaceuticals that could be present in water and wastewater has gained increasing attention. With the public’s enhanced awareness of eco-safety, environmentally benign methods based on microorganisms have become more accepted methods of removing pollutants from aquatic systems. This study investigates bioremediation of pharmaceutical wastewater from pharmaceutical company Pliva Hrvatska d.o.o., using activated sludge and bioaugmente...

  12. In Silico Models for Ecotoxicity of Pharmaceuticals.

    Science.gov (United States)

    Roy, Kunal; Kar, Supratik

    2016-01-01

    Pharmaceuticals and their active metabolites are one of the significantly emerging environmental toxicants. The major routes of entry of pharmaceuticals into the environment are industries, hospitals, or direct disposal of unwanted or expired drugs made by the patient. The most important and distinct features of pharmaceuticals are that they are deliberately designed to have an explicit mode of action and designed to exert an effect on humans and other living systems. This distinctive feature makes pharmaceuticals and their metabolites different from other chemicals, and this necessitates the evaluation of the direct effects of pharmaceuticals in various environmental compartments as well as to living systems. In this background, the alarming situation of ecotoxicity of diverse pharmaceuticals have forced government and nongovernment regulatory authorities to recommend the application of in silico methods to provide quick information about the risk assessment and fate properties of pharmaceuticals as well as their ecological and indirect human health effects. This chapter aims to offer information regarding occurrence of pharmaceuticals in the environment, their persistence, environmental fate, and toxicity as well as application of in silico methods to provide information about the basic risk management and fate prediction of pharmaceuticals in the environment. Brief ideas about toxicity endpoints, available ecotoxicity databases, and expert systems employed for rapid toxicity predictions of ecotoxicity of pharmaceuticals are also discussed.

  13. Removal of selected pharmaceuticals from domestic wastewater in an activated sludge system followed by a horizontal subsurface flow bed - analysis of their respective contributions.

    Science.gov (United States)

    Verlicchi, P; Galletti, A; Petrovic, M; Barceló, D; Al Aukidy, M; Zambello, E

    2013-06-01

    Seventy-three commonly administered pharmaceuticals from twelve different therapeutic classes were investigated at a municipal wastewater treatment plant in northern Italy featuring a conventional activated sludge system (full-scale) and a polishing horizontal subsurface flow bed (pilot plant). Removal of these micro-pollutants by the two systems was assessed in order to evaluate their respective contributions. Mean concentrations and standard deviations were calculated and found to differ for the compounds detected, ranging from few ng/L to over 1,165 ng/L in the secondary effluent and from 11 to 533 in the polished effluent. Eighteen compounds were consistently below the detection limit and the remaining 55 compounds were found at a minimum of one sampling point. Average removal efficiencies of both treatment steps and in treatment train as a whole are evaluated and discussed, highlighting the difficulties in predicting the fate of pharmaceuticals in both an activated sludge system and a horizontal subsurface flow bed. Comparison between the observed average removal efficiencies and those reported in the literature was also carried out for the pharmaceuticals of interest, and the discrepancies that emerged are discussed. The investigated constructed wetland did show efficacy in removing some of these compounds, and it contributed to the overall removal efficiency of each therapeutic class. Indeed, evaluation of the specific mass loadings of each class of PhC detected in the raw wastewaters, secondary and polished effluent evidences that the investigated constructed wetland is able to further reduce the load of micropollutants, which could become a necessity, especially where the receiving water body is an effluent-dominant river and mitigation measures of the discharge impact are required to protect and safeguard the aquatic environment. PMID:23563255

  14. Modulation of steroidogenic gene expression and hormone production of H295R cells by pharmaceuticals and other environmentally active compounds

    International Nuclear Information System (INIS)

    The H295R cell bioassay was used to evaluate the potential endocrine disrupting effects of 18 of the most commonly used pharmaceuticals in the United States. Exposures for 48 h with single pharmaceuticals and binary mixtures were conducted; the expression of five steroidogenic genes, 3βHSD2, CYP11β1, CYP11β2, CYP17 and CYP19, was quantified by Q-RT-PCR. Production of the steroid hormones estradiol (E2), testosterone (T) and progesterone (P) was also evaluated. Antibiotics were shown to modulate gene expression and hormone production. Amoxicillin up-regulated the expression of CYP11β2 and CYP19 by more than 2-fold and induced estradiol production up to almost 3-fold. Erythromycin significantly increased CYP11β2 expression and the production of P and E2 by 3.5- and 2.4-fold, respectively, while production of T was significantly decreased. The β-blocker salbutamol caused the greatest induction of CYP17, more than 13-fold, and significantly decreased E2 production. The binary mixture of cyproterone and salbutamol significantly down-regulated expression of CYP19, while a mixture of ethynylestradiol and trenbolone, increased E2 production 3.7-fold. Estradiol production was significantly affected by changes in concentrations of trenbolone, cyproterone, and ethynylestradiol. Exposures with individual pharmaceuticals showed the possible secondary effects that drugs may exert on steroid production. Results from binary mixture exposures suggested the possible type of interactions that may occur between drugs and the joint effects product of such interactions. Dose-response results indicated that although two chemicals may share a common mechanism of action the concentration effects observed may be significantly different

  15. Pharmaceutical cocrystals: a comparison of sulfamerazine with sulfamethazine

    Science.gov (United States)

    Lu, Jie; Li, Yi-Ping; Wang, Jing; Li, Zhen; Rohani, Sohrab; Ching, Chi-Bun

    2011-11-01

    Although there has been much debate about its definition among scientists, a cocrystal may be defined as a crystalline material that consists of two or more electrically neutral molecular species held together by non-covalent forces, and meanwhile all components are solids at room temperature. Obviously it is great to introduce predictable structural motifs to an active pharmaceutical ingredient (API) by design. One widely used approach to cocrystal design is based on the consideration of Δp Ka, which can represent the propensity of molecular species to form a cocrystal or a salt. In this work, p-aminobenzoic acid (PABA) was mixed with sulfamerazine (SMZ) or sulfamethazine (STH) by use of neat cogrinding and solvent-drop cogrinding. It was found that PABA and SMZ with a Δp Ka of 2.13 would form a binary eutectic, while PABA and STH with a larger Δp Ka of 2.59 can form a cocrystal in the ratio of 1:1. The phenomenon indicates that not only the Δp Ka but also the stereo-hindrance effect (geometric fit) should be considered during the design of pharmaceutical cocrystals.

  16. Application of Refractometry in Purification Technology of Active Ingredients from Citrus aurantium by Macroporous Resin%折光法在树脂精制枳实中有效成分的应用

    Institute of Scientific and Technical Information of China (English)

    曾文雪; 姚珍珍; 涂瑶生; 陈银芳; 宋小玲; 王跃生

    2013-01-01

    目的:探讨折光法在大孔树脂纯化工艺中应用的可行性.方法:选取枳实提取物为研究对象,经AB-8型大孔吸附树脂精制有效部位,用水与50%乙醇洗脱,间隔取样,在线监测洗脱液的折光率并分析其变化规律,同时以HPLC和UV检测作为参比,判断洗脱过程中始点和终点.结果:枳实有效部位精制过程中水洗终点为第4 BV(折光率0),亦即50%乙醇洗脱始点,50%乙醇洗脱终点为第9 BV(折光率16).结论:折光法准确可靠、便捷快速,具有较强的实践指导意义.%Objective: To explore application feasibility of refractometry in purification technology of macroporous resin. Method: Taking extract of Citrus aurantium as research object, active ingredients in it was refined by AB-8 macroporous resin, washed with water and 50% ethanol, interval sampled, refractive ratio of eluent was monitored on line and analyzed its regularity. At the same time, HPLC and UV spectrophotometric method was used to determine hesperidin as references, and to judge initiation point and terminal point during elution. Result: In purification process of active ingredients from C. aurantium, water elution terminal point 4 BV ( refractive index 0) of which was the initiation point by 50% ethanol, 9 BV (refractive index 16) of 50% ethanol elution was the terminal point. Conclusion: Refractometry was accurate, reliable, convenient, quickly in purification technology of active ingredients of TCM, it had a strong practical significance.

  17. A comparative analysis of nutrition components and functional active ingredients in Avena nuda and Avena sativa%裸燕麦和皮燕麦的营养及功能活性成分对比分析

    Institute of Scientific and Technical Information of China (English)

    李笑蕊; 王世霞; 幺杨; 婷婷; 刘珊; 任贵兴; 綦文涛

    2015-01-01

    The differences of nutrition components and active ingredient between Avena nuda and Avena sativa were compared.The contents of basic components (moisture and ash),nutritional compositions (starch,protein and fat)and functional active ingredient (flavonoids,polyphenols and oligosaccharide) in 5 kinds of Avena nuda and 3 kinds of Avena sativa were determined.The results showed that there were no significant differences in the contents of moisture and ash between Avena nuda and Avena sativa. The contents of crud fat,crud protein,stearic acid,oleic acid,linoleic acid,linolenic acid,flavonoids and amino acid in Avena nuda were significantly higher than those in Avena sativa,while the contents of slowly digestible starch and stachyose in Avena nuda were significantly lower than those in Avena sativa. Both Avena nuda and Avena sativa had similar composition of nutritional and functional active ingredients but the contents of them higher in Avena nuda than in Avena sativa.%对比研究裸燕麦和皮燕麦营养组分及功能活性成分的差异。以5种裸燕麦和3种皮燕麦为材料,分别测定其中基本组分(水分和灰分)、营养组分(淀粉、蛋白质和脂肪)以及功能组分(黄酮、多酚和低聚糖等)的含量。结果表明,裸燕麦和皮燕麦的水分和灰分含量无显著性差异;裸燕麦在粗脂肪、粗蛋白、硬脂酸、油酸、亚油酸、亚麻酸、黄酮和氨基酸等营养及功能组分的含量方面显著高于皮燕麦,而慢消化淀粉和水苏糖2种组分含量显著低于皮燕麦。裸燕麦和皮燕麦含有相同种类的营养及功能组分,但裸燕麦的多种营养组分及功能组分含量高于皮燕麦。

  18. A preliminary analysis of the active ingredients from the seeds of Polygonum orientale against Mythimna separata%红蓼种子中杀黏虫活性成分的初步分析

    Institute of Scientific and Technical Information of China (English)

    姚赛群; 胡冠芳; 刘敏艳; 张新瑞

    2011-01-01

    [目的]对红蓼种子乙酸乙酯萃取物中具有潜在杀虫活性的化合物进行初步分析,为指导开发利用杀虫植物资源提供依据.[方法]采用硅胶柱层析和气相色谱-质谱(GC-MS)联用法,以5龄黏虫为试虫;对红蓼种子萃取物的有效杀虫活性成分进行分析,应用色谱峰面积归一法测定各组分的相对百分含量.[结果]极性(甲醇)组分共分离出37个色谱峰,鉴定了其中的35个组分,占总含量的94.46%.弱极性(二氯甲烷)组分共分离出39个色谱峰,鉴定出39个组分.[结论]从成分的化学结构推断,红蓼种子的杀虫活性可能存在于14种成分中,主要成分为酮、醇、开环萜和五环三萜烷类化合物.%[Objective] Active ingredients of the ethyl acetate fraction from seeds of Polygonum orientale Linn, were analyzed to provide the basis for the exploitation of the insecticidal plant resources. [Method] Insecticidal ingredients from the seeds of P. orientale fractions were analyzed against the 5th instar larvae of Mythimna separata Walker by using silica gel colurnn-chromatographer (CO and gas chromatography-mass spectrometry (GC-MS). The relative percentage of each composition was determined by area normalization. [Result] Thirty-seven peaks were found, 35 of which were identified, representing 94.46% of the total contents in polar fraction. Thirty-nine peaks were found, all of which were identified in low polar fraction. [Conclusion] It was deduced that the insecticidal active ingredients in P. orientale seeds were 14 chemical compounds, belonging to ketone, alcohol, terpene with open-ring and pentacyclic triterpene classes.

  19. 基于均匀设计法对酸枣仁抗抑郁有效组分的配伍研究%Uniform Designed Research on the Active Ingredients Assembling of Semen Ziziphi Spinosae for Anti-depression

    Institute of Scientific and Technical Information of China (English)

    郭蕾

    2014-01-01

    Objective To screen out the optimized compatibility proportion of three active ingredients of semen ziziphi spinosae foranti-depression.Methods Groups were ar anged fol owing uniform design. The forced swimming test,tail suspension test were car ied out to determine theanti-depressantactivity in mice.Mice immobility duration in forced swimming test and tail suspension test were observed.Results The optimized dosage of total fat y oil was 10mg/kg,total flavonoids was 100mg/kg and total saponins was 10mg/kg.Conclusion It would be possible to use uniform design combined with pharmacodynamics method in defining the optimized compatibility of active ingredients of semen ziziphi spinosae.%目的优选酸枣仁中3种抗抑郁有效组分的最佳配伍比例。方法根据均匀设计法进行分组,采用小鼠强迫游泳实验和悬尾实验,用小鼠不动时间作为药效学评价指标。结果酸枣仁抗抑郁有效组分的最优配伍为总脂肪油10mg/Kg,总黄酮100mg/Kg,总皂苷10mg/Kg。验证实验证明,酸枣仁抗抑郁有效组分的最佳配伍组合抗抑郁疗效确切。结论应用均匀设计法与药效学相结合确定酸枣仁活性组分配伍的方法是可行的。

  20. Thermal stability of synthetic thyroid hormone l-thyroxine and l-thyroxine sodium salt hydrate both pure and in pharmaceutical formulations.

    Science.gov (United States)

    Ledeţi, Ionuţ; Ledeţi, Adriana; Vlase, Gabriela; Vlase, Titus; Matusz, Petru; Bercean, Vasile; Şuta, Lenuţa-Maria; Piciu, Doina

    2016-06-01

    In this paper, the thermal stability of pure l-thyroxine (THY) and l-thyroxine sodium salt hydrate (THYSS) vs. two pharmaceutical solid formulations commercialized on both Romanian and European market (with a content of 100μg, respectively 200μg THYSS per tablet) were investigated. In order to determine whether the presence of excipients affects the thermal stability of the active pharmaceutical ingredient (API), the preliminary study of thermal stability in air atmosphere was completed with an in-depth solid-state kinetic study. By kinetic analysis, the non-isothermal degradation of the selected active pharmaceutical ingredients vs. the solid formulation with strength of 200μg THYSS per tablet was investigated. Isoconversional methods (Kissinger-Akahira-Sunose, Flynn-Wall-Ozawa and Friedman) were employed for the estimation of activation energies values, at five different heating rates, β=5, 7, 10, 12 and 15°Cmin(-1). Also, a fourth method was applied in the processing of data, namely NPK, allowing an objective separation in the physical and chemical processes that contribute to the thermal degradation of the selected compounds. A discussion of thermal stability from the kinetic point of view is also presented. PMID:26999320

  1. Development of a simple, rapid and validated spectrophotometric method for nitazoxanide in pharmaceutical formulations and comparison with HPLC

    Directory of Open Access Journals (Sweden)

    Marcelo Donadel Malesuik

    2010-01-01

    Full Text Available A rapid, economical, reproducible, and simple direct spectrophotometric method was developed and validated for the assay of nitazoxanide in pharmaceutical formulations. Nitazoxanide concentration was estimated in water at 345 nm and pH 4.5. The method was suitable and validated for specificity, linearity, precision, and accuracy. There was no interference of the excipients in the determination of the active pharmaceutical ingredient. The proposed method was successfully applied in the determination of nitazoxanide in coated tablets and in powders for oral suspension. This method was compared to a previously developed and validated method for liquid chromatography to the same drug. There was no significative difference between these methods for nitazoxanide quantitation.

  2. A PHARMACEUTICAL COMPARISON OF GUDUCHI GHRITA PREPARED FROM MALE AND FEMALE PLANTS OF TINOSPORA CORDIFOLIA (WILLD. MIERS.

    Directory of Open Access Journals (Sweden)

    BK Ashok

    2011-04-01

    Full Text Available Pharmaceutical study appreciates the importance of formulation preparation which ultimately determines the nature and magnitude of pharmacological activity expressed. Guduchi is one among the most important medicinal plants of India and various formulations of Guduchi ghrita are mentioned in different Ayurvedic classical texts. In the present study, a simple formulation of Guduchi ghrita which is used for treatment of chronic fever wherein no other ingredient except Guduchi was selected and a comparative pharmaceutical study of Guduchi ghrita prepared from male and female plants was carried out. The preparation of Guduchi ghrita formulations were carried out by adopting standard operative procedure. The result of this study shows that ghrita prepared from male plant yielded more quantity of finished product than that of female plant.

  3. The occurrence and removal of selected pharmaceutical compounds in a sewage treatment works utilising activated sludge treatment

    International Nuclear Information System (INIS)

    Pharmaceutical substances have been detected in sewage effluents as well as receiving waters in many parts of the world. In this study, the occurrence and removal of a number of drug compounds were studied within a large sewage treatment plant in the south of England. Samples were processed using solid phase extraction and analysed using gas chromatography-mass spectrometry (GC-MS). The results demonstrate that ibuprofen, paracetamol, salbutamol and mefenamic acid were present in both the influent and effluent of the works while propranolol-HCl was not found above the limit of quantification in any sample. Elimination rates were circa 90% for each compound but several hundred nanograms per litre were still present in the final effluent. - This report looks at the occurrence and removal rates of drugs in English wastewater

  4. The occurrence and removal of selected pharmaceutical compounds in a sewage treatment works utilising activated sludge treatment

    Energy Technology Data Exchange (ETDEWEB)

    Jones, O.A.H. [Institute of Environmental Policy, Imperial College, London SW7 2AZ (United Kingdom); Voulvoulis, N. [Institute of Environmental Policy, Imperial College, London SW7 2AZ (United Kingdom); Lester, J.N. [School of Water Sciences, Cranfield University, Cranfield, Bedfordshire MK43 0AL (United Kingdom)]. E-mail: j.lester@cranfield.ac.uk

    2007-02-15

    Pharmaceutical substances have been detected in sewage effluents as well as receiving waters in many parts of the world. In this study, the occurrence and removal of a number of drug compounds were studied within a large sewage treatment plant in the south of England. Samples were processed using solid phase extraction and analysed using gas chromatography-mass spectrometry (GC-MS). The results demonstrate that ibuprofen, paracetamol, salbutamol and mefenamic acid were present in both the influent and effluent of the works while propranolol-HCl was not found above the limit of quantification in any sample. Elimination rates were circa 90% for each compound but several hundred nanograms per litre were still present in the final effluent. - This report looks at the occurrence and removal rates of drugs in English wastewater.

  5. 羽裂蟹甲草对家蝇和白纹伊蚊的杀虫活性和活性成分%Insecticidal activities and active ingredients of Cacalia tangutica against Musca domestica and Aedes albopictus

    Institute of Scientific and Technical Information of China (English)

    黄继光; 赵欢欢; 苗辉; 徐汉虹

    2012-01-01

    To study the insecticidal activities and active ingredients of Cacalia tangutica,the methanol extracts of C.tangutica against Musca domestica and Aedes albopictus were bioassayed with feeding method and dipping method.The active ingredients of C.tangutica were isolated and identified.Results indicated that the methanol extracts from different parts of C.tangutica showed highly insecticidal activities against adult M.domestica and the 4th instar larvae of A.albopictus.Nine compounds (stigmasterol,friedelin,7-hydroxy-8-methoxycoumarin,umbelliferone,daphnetin,daphnetin-8-O-β-D-glucopyranoside,quercetin,kaempferol and β-daucosterol) were isolated and identified from extracts of leaves and flowers of C.tangutica.Among them,friedelin,quercetin and kaempferol were firstly isolated from this plant.At 48 h after treatment,the corrected mortalities of adult M.domestica caused by friedelin,quercetin and kaempferol at the dosage of 500 μg/g were 88.33%,69.90% and 77.04%,respectively.At 72 h after treatment,the corrected mortalities of the 4th instar larvae of A.albopictus caused by friedelin,quercetin and kaempferol at the concentration of 50 μg/g were 88.49%,72.22%and 71.06%,respectively.The studies suggest that C.tangutica would be a promising control agent on medical insects and deserves a further study.%为探明羽裂蟹甲草Cacalia tangutica的杀虫活性及其活性成分,通过拌糖饲喂法和浸渍法测定了羽裂蟹甲草甲醇提取物对家蝇Musca domestica成虫和白纹伊蚊Aedes albopictus 4龄幼虫的毒杀活性,并采用色谱分离技术和现代波谱技术对羽裂蟹甲草中的化学成分进行了分离鉴定.结果表明:该植物不同部位甲醇提取物对家蝇成虫和白纹伊蚊4龄幼虫均具有较高的生物活性.从该植物叶和花甲醇提取物中分离鉴定了豆甾醇、无羁萜、7-羟基-8-甲氧基香豆素、7-羟基香豆素、7,8-二羟基香豆素、瑞香素-8-O-β-D-葡萄糖苷、槲皮素

  6. Pharmaceutical evaluation of cultivated Glycyrrhiza uralensis roots in comparison of their antispasmodic activity and glycycoumarin contents with those of licorice.

    Science.gov (United States)

    Nagai, Hidemasa; Yamamoto, Yutaka; Sato, Yuji; Akao, Teruaki; Tani, Tadato

    2006-12-01

    In China, the collection of wild Glycyrrhiza uralensis, one of the raw materials of Chinese licorice, has been restricted to prevent desertification. To compensate for the reduced supply of wild Glycyrrhiza plants, cultivation programs of G. uralensis have been initiated in eastern Inner Mongolia. The goal of the present study was to compare the chemical and pharmacological properties of cultivated G. uralensis roots to those of licorice prepared from wild Glycyrrhiza plants. The antispasmodic effect of boiled water extract of 4-year-old cultivated G. uralensis roots and licorice on carbachol-induced contraction in mice jejunum was similar (ED(50): 134+/-21 microg/ml vs. 134+/-16 microg/ml). In addition, glycycoumarin content, which is an antispasmodic and species-specific ingredient of G. uralensis, was similar when comparing the boiled water extracts of 4-year-old cultivated roots and licorice (0.10+/-0.02% vs. 0.10+/-0.06%). These data suggest that cultivated G. uralensis roots may be an adequate replacement for the generation of licorice in the context of the restriction of wild Glycyrrhiza plant collection. PMID:17142979

  7. Advances in Neuroprotective Ingredients of Medicinal Herbs by Using Cellular and Animal Models of Parkinson’s Disease

    Directory of Open Access Journals (Sweden)

    Sandeep Vasant More

    2013-01-01

    Full Text Available Parkinson’s disease (PD is a multifactorial disorder, which is neuropathologically identified by age-dependent neurodegeneration of dopaminergic neurons in the substantia nigra. Development of symptomatic treatments has been partly successful for PD research, but there remain a number of inadequacies in therapeutic strategies for the disease. The pathogenesis of PD remains intricate, and the present anti-PD treatments appears to be clinically insufficient. Comprehensive research on discovery of novel drug candidates has demonstrated that natural products, such as medicinal herbs, plant extracts, and their secondary metabolites, have great potential as therapeutics with neuroprotective activity in PD. Recent preclinical studies suggest that a number of herbal medicines and their bioactive ingredients can be developed into optimum pharmaceuticals for treating PD. In many countries, traditional herbal medicines are used to prevent or treat neurodegenerative disorders, and some have been developed as nutraceuticals or functional foods. Here we focus on recent advances of the evidence-linked neuroprotective activity of bioactive ingredients of herbal origin in cellular and animal models of PD research.

  8. Fate of bulk organic matter, nitrogen, and pharmaceutically active compounds in batch experiments simulating soil aquifer treatment (SAT) using primary effluent

    KAUST Repository

    Abel, Chol D T

    2013-06-30

    Reduction of bulk organic matter, nitrogen, and pharmaceutically active compounds from primary effluent during managed aquifer recharge was investigated using laboratory-scale batch reactors. Biologically stable batch reactors were spiked with different concentrations of sodium azide to inhibit biological activity and probe the effect of microbial activity on attenuation of various pollutants of concern. The experimental results obtained revealed that removal of dissolved organic carbon correlated with active microbial biomass. Furthermore, addition of 2 mM of sodium azide affected nitrite-oxidizing bacteria leading to accumulation of nitrite-nitrogen in the reactors while an ammonium-nitrogen reduction of 95.5 % was achieved. Removal efficiencies of the hydrophilic neutral compounds phenacetin, paracetamol, and caffeine were independent of the extent of the active microbial biomass and were >90 % in all reactors, whereas removal of pentoxifylline was dependent on the biological stability of the reactor. However, hydrophobic ionic compounds exhibited removal efficiency >80 % in batch reactors with the highest biological activity as evidenced by high concentration of adenosine triphosphate. © 2013 Springer Science+Business Media Dordrecht.

  9. Ba-Wei-Di-Huang-Wan through its active ingredient loganin counteracts substance P-enhanced NF-κB/ICAM-1 signaling in rats with bladder hyperactivity.

    Science.gov (United States)

    Tsai, Wen-Hsin; Wu, Chung-Hsin; Cheng, Chen-Hung; Chien, Chiang-Ting

    2016-09-01

    Overt bladder afferent activation may exacerbate endogenous substance P (SP) release to induce intercellular adhesion molecule-1 (ICAM-1)-mediated inflammation and reactive oxygen species (ROS) production leading to hyperactive bladder. Ba-Wei-Die-Huang-Wan (BWDHW), a traditional Chinese medicine, has been used to treat lower urinary tract symptoms in patients by undefined mechanisms. We explored the possible mechanisms and the active components of BWDHW on exogenous SP-induced bladder hyperactivity. BWDHW contained six major components: loganin, paeoniflorin, 5-hydroxymethylfurfural, cinnamic acid, cinnamaldehyde, and paeonol by high-performance liquid chromatography. In urethane-anesthetized female Wistar rats, we evaluated transcystometrogram, pelvic afferent nerve activity by electrophysiologic recording techniques, ICAM-1 expression by Western blot and immunohistochemistry, ROS amount by an ultrasensitive chemiluminescence method and possible ROS sources from the different leukocytes by specific stains in SP-treated bladder. BWDHW and its major component loganin dose-dependently inhibited H2 O2 and HOCl activity in vitro. Intragastrical BWDHW (250 mg/kg) and loganin (5 mg/kg) twice daily for 2 weeks did not affect the baseline micturition parameters. Intra-arterial SP (20 µg/rat) through neurokinin-1 receptor activation increased voiding frequency (shortened intercontraction intervals), pelvic afferent nerve activity, bladder NF-κB/ICAM-1 expression, bladder ROS amount, neutrophils adhesion to venous endothelium, CD68 (monocyte/macrophage), and mast cell infiltration in the inflamed bladder. BWDHW and loganin pretreatment significantly depressed SP-enhanced pelvic afferent nerve activity, bladder NF-κB/ICAM-1 expression, leukocyte infiltration, and ROS amount, and subsequently improved bladder hyperactivity. In conclusion, our results suggest that BWDHW and its active component loganin improves bladder hyperactivity via inhibiting SP/neurokinin-1

  10. Development and Validation of a Stability Indicating RP-HPLC Method for Hydrocortisone Acetate Active Ingredient, Propyl Parahydroxybenzoate and Methyl Parahydroxybenzoate Preservatives, Butylhydroxyanisole Antioxidant, and Their Degradation Products in a Rectal Gel Formulation.

    Science.gov (United States)

    Ascaso, Magda; Pérez-Lozano, Pilar; García, Mireia; García-Montoya, Encarna; Miñarro, Montse; Ticó, Josep R; Fàbregas, Anna; Carrillo, Carolina; Sarrate, Rocío; Suñé-Negre, Josep M

    2015-01-01

    A stability indicating method was established through a stress study, wherein different methods of degradation (oxidation, hydrolysis, photolysis, and temperature) were studied simultaneously to determine the active ingredient hydrocortisone acetate, preservatives propyl parahydroxybenzoate, and methyl parahydroxybenzoate, antioxidant butylhydroxyanisole (BHA), and their degradation products in a semisolid dosage gel form. The proposed method was suitably validated using a Zorbax SB-Phenyl column and gradient elution. The mobile phase consisted of a mixture of methanol, acetonitrile, and water in different proportions according to a planned program at a flow rate of 1.5 mL/min. The diode array detector was set at 240 nm for the active substance and two preservatives, and 290 nm for BHA. The validation study was conducted according to International Conference on Harmonization guidelines for specificity, linearity, repeatability, precision, and accuracy. The method was used for QC of hydrocortisone acetate gel and for the stability studies with the aim of quantifying the active substance, preservatives, antioxidant, and degradation products. It has proved to be suitable as a fast and reliable method for QC. PMID:25857875

  11. Development and Validation of a Stability Indicating RP-HPLC Method for Hydrocortisone Acetate Active Ingredient, Propyl Parahydroxybenzoate and Methyl Parahydroxybenzoate Preservatives, Butylhydroxyanisole Antioxidant, and Their Degradation Products in a Rectal Gel Formulation.

    Science.gov (United States)

    Ascaso, Magda; Pérez-Lozano, Pilar; García, Mireia; García-Montoya, Encarna; Miñarro, Montse; Ticó, Josep R; Fàbregas, Anna; Carrillo, Carolina; Sarrate, Rocío; Suñé-Negre, Josep M

    2015-01-01

    A stability indicating method was established through a stress study, wherein different methods of degradation (oxidation, hydrolysis, photolysis, and temperature) were studied simultaneously to determine the active ingredient hydrocortisone acetate, preservatives propyl parahydroxybenzoate, and methyl parahydroxybenzoate, antioxidant butylhydroxyanisole (BHA), and their degradation products in a semisolid dosage gel form. The proposed method was suitably validated using a Zorbax SB-Phenyl column and gradient elution. The mobile phase consisted of a mixture of methanol, acetonitrile, and water in different proportions according to a planned program at a flow rate of 1.5 mL/min. The diode array detector was set at 240 nm for the active substance and two preservatives, and 290 nm for BHA. The validation study was conducted according to International Conference on Harmonization guidelines for specificity, linearity, repeatability, precision, and accuracy. The method was used for QC of hydrocortisone acetate gel and for the stability studies with the aim of quantifying the active substance, preservatives, antioxidant, and degradation products. It has proved to be suitable as a fast and reliable method for QC.

  12. Fabrication of a live cell-containing multilayered polymer hydrogel membrane with micrometer-scale thickness to evaluate pharmaceutical activity.

    Science.gov (United States)

    Gao, Botao; Konno, Tomohiro; Ishihara, Kazuhiko

    2015-01-01

    We propose a spinning-assisted layer-by-layer method for simple fabrication of a multilayered polymer hydrogel membrane that contains living cells. Hydrogel formation occurred based on the spontaneous cross-linking reaction between two polymers in aqueous solution. A water-soluble 2-methacryloyloxyethyl phosphorylcholine polymer bearing phenylboronic acid groups (PMBV) and poly(vinyl alcohol) (PVA) were used as polymers for hydrogel membrane formation. Changing the number of hydrogel membrane layers, polymer concentration, spinning rate, and processing time for diffusion-dependent gelation of PMBV and PVA facilitated the regulation of the multilayered polymer hydrogel membrane thickness and morphology. We concluded that a multilayered polymer hydrogel membrane prepared using 5.0 wt% PMBV and 5.0 wt% PVA at a spinning rate of 2000 rpm was suitable for precise spatial control of cells in single layers. This multilayered polymer hydrogel membrane was used to prepare a single cell-laden layer to minimize barriers to the diffusion of bioactive compounds while preserving the three-dimensional (3-D) context. The pharmaceutical effects of one of the anticancer agents, paclitaxel, on a human cervical cancer line, HeLa cells, were evaluated in vitro, and the usability of this culture model was demonstrated. PMID:26374190

  13. The World Bank and pharmaceuticals.

    Science.gov (United States)

    Falkenberg, T; Tomson, G

    2000-03-01

    Within less than a decade the World Bank has become the largest single source of finance (loans) for health in low and middle income countries as well as a major player in the field of pharmaceuticals. Often 20-50% of the recurrent government health budget in developing countries is used to procure drugs. Drugs are among the most salient and cost-effective elements of health care and often a key factor for the success of a health sector reform. However, pharmaceuticals are frequently being used irrationally, mainly due to market imperfections in health care, such as information asymmetries, leading to serious health problems and a heavy financial burden on the health system. Lending priorities set by the World Bank could be used to promote public health sector reform, leading to the rational use of affordable and available drugs of good quality in developing countries. This report provides the first analysis of World Bank activity in the pharmaceutical sector worldwide. The analysis of 77 staff appraisal reports, describing the planning phase of World Bank country projects, shows that 16% of the total World Bank health, nutrition and population budget, or approximately US$1.3 billion, has been committed to loans or credits supporting pharmaceutical activities in the programme countries between 1989-95. Roughly US$1.05 billion has been committed to procurement of drugs and medical equipment. Only 5% of the total pharmaceutical sector lending is committed to software components such as drug policy work and rational use of drugs. No more than 45% of the projects were developed in collaboration with pharmaceutical expertise. The World Bank is recommended to improve its pharmaceutical sector involvement by promoting drug policy research and development including national and international dialogue on pharmaceutical issues to ensure rational use of both drugs and loans. In this, the World Bank has an advantage given its experience from working with both the private and

  14. Near infra red spectroscopy as a multivariate process analytical tool for predicting pharmaceutical co-crystal concentration.

    Science.gov (United States)

    Wood, Clive; Alwati, Abdolati; Halsey, Sheelagh; Gough, Tim; Brown, Elaine; Kelly, Adrian; Paradkar, Anant

    2016-09-10

    The use of near infra red spectroscopy to predict the concentration of two pharmaceutical co-crystals; 1:1 ibuprofen-nicotinamide (IBU-NIC) and 1:1 carbamazepine-nicotinamide (CBZ-NIC) has been evaluated. A partial least squares (PLS) regression model was developed for both co-crystal pairs using sets of standard samples to create calibration and validation data sets with which to build and validate the models. Parameters such as the root mean square error of calibration (RMSEC), root mean square error of prediction (RMSEP) and correlation coefficient were used to assess the accuracy and linearity of the models. Accurate PLS regression models were created for both co-crystal pairs which can be used to predict the co-crystal concentration in a powder mixture of the co-crystal and the active pharmaceutical ingredient (API). The IBU-NIC model had smaller errors than the CBZ-NIC model, possibly due to the complex CBZ-NIC spectra which could reflect the different arrangement of hydrogen bonding associated with the co-crystal compared to the IBU-NIC co-crystal. These results suggest that NIR spectroscopy can be used as a PAT tool during a variety of pharmaceutical co-crystal manufacturing methods and the presented data will facilitate future offline and in-line NIR studies involving pharmaceutical co-crystals.

  15. Near infra red spectroscopy as a multivariate process analytical tool for predicting pharmaceutical co-crystal concentration.

    Science.gov (United States)

    Wood, Clive; Alwati, Abdolati; Halsey, Sheelagh; Gough, Tim; Brown, Elaine; Kelly, Adrian; Paradkar, Anant

    2016-09-10

    The use of near infra red spectroscopy to predict the concentration of two pharmaceutical co-crystals; 1:1 ibuprofen-nicotinamide (IBU-NIC) and 1:1 carbamazepine-nicotinamide (CBZ-NIC) has been evaluated. A partial least squares (PLS) regression model was developed for both co-crystal pairs using sets of standard samples to create calibration and validation data sets with which to build and validate the models. Parameters such as the root mean square error of calibration (RMSEC), root mean square error of prediction (RMSEP) and correlation coefficient were used to assess the accuracy and linearity of the models. Accurate PLS regression models were created for both co-crystal pairs which can be used to predict the co-crystal concentration in a powder mixture of the co-crystal and the active pharmaceutical ingredient (API). The IBU-NIC model had smaller errors than the CBZ-NIC model, possibly due to the complex CBZ-NIC spectra which could reflect the different arrangement of hydrogen bonding associated with the co-crystal compared to the IBU-NIC co-crystal. These results suggest that NIR spectroscopy can be used as a PAT tool during a variety of pharmaceutical co-crystal manufacturing methods and the presented data will facilitate future offline and in-line NIR studies involving pharmaceutical co-crystals. PMID:27429366

  16. Dropwise additive manufacturing of pharmaceutical products for solvent-based dosage forms.

    Science.gov (United States)

    Hirshfield, Laura; Giridhar, Arun; Taylor, Lynne S; Harris, Michael T; Reklaitis, Gintaras V

    2014-02-01

    In recent years, the US Food and Drug Administration has encouraged pharmaceutical companies to develop more innovative and efficient manufacturing methods with improved online monitoring and control. Mini-manufacturing of medicine is one such method enabling the creation of individualized product forms for each patient. This work presents dropwise additive manufacturing of pharmaceutical products (DAMPP), an automated, controlled mini-manufacturing method that deposits active pharmaceutical ingredients (APIs) directly onto edible substrates using drop-on-demand (DoD) inkjet printing technology. The use of DoD technology allows for precise control over the material properties, drug solid state form, drop size, and drop dynamics and can be beneficial in the creation of high-potency drug forms, combination drugs with multiple APIs or individualized medicine products tailored to a specific patient. In this work, DAMPP was used to create dosage forms from solvent-based formulations consisting of API, polymer, and solvent carrier. The forms were then analyzed to determine the reproducibility of creating an on-target dosage form, the morphology of the API of the final form and the dissolution behavior of the drug over time. DAMPP is found to be a viable alternative to traditional mass-manufacturing methods for solvent-based oral dosage forms. PMID:24311373

  17. Physical and Chemical Aspects of Pharmaceutical Solids: Fundamentals of Polymorphs, Hydrates and Solvates

    Science.gov (United States)

    Reutzel-Edens, Susan

    2007-03-01

    Crystal polymorphs are solid phases of a given compound resulting from the possibility of at least two different arrangements of the molecules of that compound in the solid state. Solvates form when the solvent is incorporated in the crystal structure of a compound; hydrates form when water is the solvent of crystallization. The potential effects of crystal polymorphism and hydration on the quality and performance of drug products is widely recognized by the pharmaceutical industry. Investigations of crystal polymorphism and hydration are usually conducted early in drug development to optimize the physical properties of a pharmaceutical solid. Although the thermodynamically most stable crystal form is generally selected for commercial development to mitigate the risk of undesired phase transformations, form selection oftentimes involves a compromise among different physical properties of various drug crystal forms. Controlling polymorph (or hydrate) appearance must be accomplished through careful evaluation of both thermodynamic (tendency toward the formation of more stable crystal forms) and kinetic parameters (which lead to the formation of metastable forms) in the crystallization process. In this presentation, fundamental aspects of polymorphs and solvates (hydrates) will be explored. Particular attention will be given to the structure and stability relationships between polymorphs and hydrates, kinetic vs. thermodynamic transitions, and the impact of polymorphism and hydration on the chemical and physical stability of an active pharmaceutical ingredient.

  18. Validation of a liquid chromatographic method for the pharmaceutical quality control of products containing elacridar

    Directory of Open Access Journals (Sweden)

    Emilia Sawicki

    2016-08-01

    Full Text Available Many anticancer drugs have an impaired bioavailability and poor brain penetration because they are substrates to drug efflux pumps such as P-glycoprotein and Breast Cancer Resistance Protein. Elacridar is a strong inhibitor of these two drug efflux pumps and therefore has great potential to improve oral absorption and brain penetration of many anticancer drugs. Currently, a clinical formulation of elacridar is unavailable and therefore the pharmaceutical development of a drug product is highly warranted. This also necessitates the availability of an analytical method for its quality control. A reverse-phase high-performance liquid chromatographic method with ultraviolet detection was developed for the pharmaceutical quality control of products containing elacridar as the active pharmaceutical ingredient. The analytical method was validated for linearity, accuracy, precision, selectivity, carry-over, stability of stock and reference solutions, stability of the final extract, stability-indicating capability and impurity testing. We found that elacridar is unstable in aqueous solutions that are exposed to light because a hydroxylation product of elacridar is formed. Therefore, sample solutions with elacridar must be protected from light.

  19. Validation of a liquid chromatographic method for the pharmaceutical quality control of products containing elacridar$

    Institute of Scientific and Technical Information of China (English)

    Emilia Sawicki; Michel J. Hillebrand; Hilde Rosing; Jan H.M. Schellens; Bastiaan Nuijen; Jos H. Beijnen

    2016-01-01

    Many anticancer drugs have an impaired bioavailability and poor brain penetration because they are sub-strates to drug efflux pumps such as P-glycoprotein and Breast Cancer Resistance Protein. Elacridar is a strong inhibitor of these two drug efflux pumps and therefore has great potential to improve oral absorption and brain penetration of many anticancer drugs. Currently, a clinical formulation of elacridar is unavailable and therefore the pharmaceutical development of a drug product is highly warranted. This also necessitates the availability of an analytical method for its quality control. A reverse-phase high-performance liquid chro-matographic method with ultraviolet detection was developed for the pharmaceutical quality control of products containing elacridar as the active pharmaceutical ingredient. The analytical method was validated for linearity, accuracy, precision, selectivity, carry-over, stability of stock and reference solutions, stability of the final extract, stability-indicating capability and impurity testing. We found that elacridar is unstable in aqueous solutions that are exposed to light because a hydroxylation product of elacridar is formed. Therefore, sample solutions with elacridar must be protected from light.

  20. Variation transmission model for setting acceptance criteria in a multi-staged pharmaceutical manufacturing process.

    Science.gov (United States)

    Montes, Richard O

    2012-03-01

    Pharmaceutical manufacturing processes consist of a series of stages (e.g., reaction, workup, isolation) to generate the active pharmaceutical ingredient (API). Outputs at intermediate stages (in-process control) and API need to be controlled within acceptance criteria to assure final drug product quality. In this paper, two methods based on tolerance interval to derive such acceptance criteria will be evaluated. The first method is serial worst case (SWC), an industry risk minimization strategy, wherein input materials and process parameters of a stage are fixed at their worst-case settings to calculate the maximum level expected from the stage. This maximum output then becomes input to the next stage wherein process parameters are again fixed at worst-case setting. The procedure is serially repeated throughout the process until the final stage. The calculated limits using SWC can be artificially high and may not reflect the actual process performance. The second method is the variation transmission (VT) using autoregressive model, wherein variation transmitted up to a stage is estimated by accounting for the recursive structure of the errors at each stage. Computer simulations at varying extent of variation transmission and process stage variability are performed. For the scenarios tested, VT method is demonstrated to better maintain the simulated confidence level and more precisely estimate the true proportion parameter than SWC. Real data examples are also presented that corroborate the findings from the simulation. Overall, VT is recommended for setting acceptance criteria in a multi-staged pharmaceutical manufacturing process.

  1. Prioritization of pharmaceuticals for potential environmental hazard through leveraging a large-scale mammalian pharmacological dataset.

    Science.gov (United States)

    Berninger, Jason P; LaLone, Carlie A; Villeneuve, Daniel L; Ankley, Gerald T

    2016-04-01

    The potential for pharmaceuticals in the environment to cause adverse ecological effects is of increasing concern. Given the thousands of active pharmaceutical ingredients (APIs) that can enter the aquatic environment through human and/or animal (e.g., livestock) waste, a current challenge in aquatic toxicology is identifying those that pose the greatest risk. Because empirical toxicity information for aquatic species is generally lacking for pharmaceuticals, an important data source for prioritization is that generated during the mammalian drug development process. Applying concepts of species read-across, mammalian pharmacokinetic data were used to systematically prioritize APIs by estimating their potential to cause adverse biological consequences to aquatic organisms, using fish as an example. Mammalian absorption, distribution, metabolism, and excretion (ADME) data (e.g., peak plasma concentration, apparent volume of distribution, clearance rate, and half-life) were collected and curated, creating the Mammalian Pharmacokinetic Prioritization For Aquatic Species Targeting (MaPPFAST) database representing 1070 APIs. From these data, a probabilistic model and scoring system were developed and evaluated. Individual APIs and therapeutic classes were ranked based on clearly defined read-across assumptions for translating mammalian-derived ADME parameters to estimate potential hazard in fish (i.e., greatest predicted hazard associated with lowest mammalian peak plasma concentrations, total clearance and highest volume of distribution, half-life). It is anticipated that the MaPPFAST database and the associated API prioritization approach will help guide research and/or inform ecological risk assessment. PMID:25772004

  2. A harmonization effort for acceptable daily exposure application to pharmaceutical manufacturing - Operational considerations.

    Science.gov (United States)

    Hayes, Eileen P; Jolly, Robert A; Faria, Ellen C; Barle, Ester Lovsin; Bercu, Joel P; Molnar, Lance R; Naumann, Bruce D; Olson, Michael J; Pecquet, Alison M; Sandhu, Reena; Shipp, Bryan K; Sussman, Robert G; Weideman, Patricia A

    2016-08-01

    A European Union (EU) regulatory guideline came into effect for all new pharmaceutical products on June 1st, 2015, and for all existing pharmaceutical products on December 1st, 2015. This guideline centers around the use of the Acceptable Daily Exposure (ADE) [synonymous with the Permitted Daily Exposure (PDE)] and operational considerations associated with implementation are outlined here. The EU guidance states that all active pharmaceutical ingredients (API) require an ADE; however, other substances such as starting materials, process intermediates, and cleaning agents may benefit from an ADE. Problems in setting ADEs for these additional substances typically relate to toxicological data limitations precluding the ability to establish a formal ADE. Established methodologies such as occupational exposure limits or bands (OELs or OEBs) and the threshold of toxicological concern (TTC) can be used or adjusted for use as interim ADEs when only limited data are available and until a more formal ADE can be established. Once formal ADEs are derived, it is important that the documents are routinely updated and that these updates are communicated to appropriate stakeholders. Another key operational consideration related to data-poor substances includes the use of maximum daily dose (MDD) in setting cross-contamination limits. The MDD is an important part of the maximum allowable/safe concentration (MAC/MSC) calculation and there are important considerations for its use and definition. Finally, other considerations discussed include operational aspects of setting ADEs for pediatrics, considerations for large molecules, and risk management in shared facilities. PMID:27267172

  3. 美白活性原料的筛选及其特性研究%Study of selection and properties of active ingredients in whitening cosmetics

    Institute of Scientific and Technical Information of China (English)

    王鹏; 王勇刚; 李素霞; 韩福森; 吴巧玲; 王素英

    2009-01-01

    Tyrosinase inhibiting activity and anti-oxidizing capacity (scavenging activity against hydroxyl free radicals and super-oxidizing anionic free radicals in vitro) of extracts of twenty kinds of plant material, including green tea, grape seed and Brazil cherry were investigated. Experimental results showed that, all the extracts of twenty kinds of plant material display tyrosinase inhibiting activity and anti-oxidizing capacity in vitro with different extent;while the extracts from green tea, grape seed and Brazil cherry display very strong ty-rosinase inhibiting activity,which are much higher than that of arbutin. Further,the above-mentioned three extracts display significant scavenging activity against hydroxyl free radicals and super-oxdizing anionic free radicals in vitro. Thus the three kinds of plant material have the potential to be used in whitening cosmetics.%对绿茶、葡萄籽和巴西大樱桃等23种植物提取物对酪氨酸酶的抑制作用以及其抗氧化能力(清除羟基自由基和超氧阴离子自由基的能力)进行了研究.实验结果表明,20种样品均表现出不同程度的酪氨酸酶抑制作用和抗氧化能力,其中绿茶、巴西大樱桃和葡萄籽提取物表现出极强的酪氨酸酶活性抑制率,且抑制活性远高于熊果苷;同时这3种植物提取物也表现出显著的清除羟基自由基和超氧阴离子自由基的能力,具有应用于美白化妆品的潜力.

  4. Lactose in dairy ingredients: Effect on processing and storage stability.

    Science.gov (United States)

    Huppertz, Thom; Gazi, Inge

    2016-08-01

    Lactose is the main carbohydrate in the milk of most species. It is present in virtually all dry dairy ingredients, with levels ranging from lactose powders. The presence of lactose has a strong effect on ingredient processing and stability. Lactose can negatively influence powder properties and lead to undesirable effects, such as the stickiness of powder resulting in fouling during drying, or caking and related phenomena during storage. In addition, being a reducing carbohydrate, lactose can also participate in the Maillard reaction with free amino groups of proteins, peptides, and free AA. In this review, the influence of the presence (or absence) of lactose on physiochemical properties of dairy ingredients is reviewed, with particular emphasis on behavior during processing and storage. Particularly important features in this respect are whether lactose is in the (glassy) amorphous phase or in the crystalline phase, which is strongly affected by precrystallization conditions (e.g., in lactose, permeate, and whey powders) and by drying conditions. Furthermore, the moisture content and water activity of the ingredients are important parameters to consider, as they determine both mobility and reactivity, influencing Maillard reactions and concomitant browning, the crystallization of amorphous lactose during storage of dairy ingredients, glass transitions temperatures, and associated stickiness and caking phenomena. For the stickiness and caking, a crucial aspect to take into account is powder particle surface composition in relation to the bulk powder. Lactose is typically underrepresented at the powder surface, as a result of which deviations between observed lactose-induced caking and stickiness temperatures, and determined glass transition temperatures arise. By considering lactose as an integral part of ingredient composition along with all other compositional and environmental properties, lactose behavior in dairy ingredients can be understood, controlled, and

  5. Rapid separation of desloratadine and related compounds in solid pharmaceutical formulation using gradient ion-pair chromatography.

    Science.gov (United States)

    Zheng, Jinjian; Rustum, Abu M

    2010-01-01

    We reported the development of an ion-pair chromatographic method to separate desloratadine and all known related compounds in Clarinex Tablets, which use desloratadine as active pharmaceutical ingredient (API). For the first time, baseline separation for desloratadine and all known related compounds was achieved by utilizing a YMC-Pack Pro C(18) column (150 mm x 4.6 mm I.D., 3 microm particle size, 120A pore size) and a gradient elution method. The mobile phase A contains 3 mM sodium dodecylsulfate (SDS), 15 mM sodium citrate buffer at pH 6.2, and 40 mM sodium sulfate, while the mobile phase B is acetonitrile. Chromsword, an artificial intelligence method development tool, was used to optimize several key chromatographic parameters simultaneously including buffer pH/solvent strength, and temperature/gradient profile. The resolution of desloratadine and desloratadine 3,4-dehydropiperidine derivative, one of the critical pairs was improved by adding 40 mM sodium sulfate. Ultraviolet detection at 267 nm was used to achieve the detection for desloratadine and all compounds. This method has been successfully validated according to ICH guidelines in terms of linearity, accuracy, quantitation limit/detection limit, precision, specificity and robustness. It could be used as a stability indicating method for desloratadine drug substances or drug products that use desloratadine as active pharmaceutical ingredient.

  6. 石榴籽油冷榨技术及活性成分生理作用研究%Pomegranate Seed Oil Cold Pressing and Physiological Role of Its Active Ingredient

    Institute of Scientific and Technical Information of China (English)

    李勇

    2011-01-01

    石榴籽油冷榨技术采用低温62℃,使脂肪氧化酶灭活,既可提高出油率,又可防止挥发油、多酚、维生素等活性物质的损失.冷榨技术与莘取法相比,出油率仅低3%-5%,但没有萃取溶剂有害物质的残留.本文介绍了冷榨技术工艺流程及操作要点,分析了石榴籽油的活性成分及其生理作用.%Pomegranate seed oil cold pressing technology inactives lipoxygenase at low temperature 62℃ ,which can increase oil yield and prevent the loss of volatile oils, polyphenols, vitamins and other active substances. Compared with extraction technology,oil yield of cold pressing technology is 3%-5% lower, but no harmful substances residues in extraction solvent. Process and operating points of cold pressing technology were introduced and physiological role of active ingredients in pomegranate seed oil was analyzed.

  7. RP-HPLC测定水蛭中3种蝶啶类活性成分的含量%Content Determination of Three Pteridine Active Ingredients in Leech by RP-HPLC

    Institute of Scientific and Technical Information of China (English)

    郑云枫; 程建明; 彭国平

    2011-01-01

    目的 建立RP-HPLC测定水蛭药材中3种蝶啶类活性成分含量的方法.方法 采用Kromsail C18色谱柱,以甲醇:0.05%三氟乙酸水(20:80)为流动相,检测波长为354 nm,流速为1.0mL/min,柱温30℃.结果 在以上色谱条件下3种成分可以完全分离.水蛭甲素:Y=12.181 4X+0.075 3,r=0.999 6;(36.0~0.90) μg/mL,水蛭乙素:Y=12.024X-2.124 5,r=0.999 5;(40.4~1.01)μg/mL,水蛭丙素:Y=12.814 5X-3.686 l,r=0.999 8;(42.8~1.07) μg/mL.结论 该方法简单、快速,专属性好,可用于水蛭药材的质量控制方法之一.%OBJECTIVE To establish RP-HPLC determination of the content of three pteridine active ingredients in leech. METHODS Kromsail Cu chromatographic column was used with methanol to 0.05% trifluoroacetic acid (20 '? 80) as mobile phase, detecting wave length of 354 nm, flow speed of 1.0 mL/min and column temperature of 30 "C. RESULTS Three active ingredients were separated on the conditions mentioned above. Hirudin A: Y=12.181 4X+0.075 3,r=0. 9996; (36.0~0.90)fig/mL. Hirudin B:Y = 12.024 X - 2.124 5, r=0.9995; (40. 4~1. 01)ng/mL. Hirudin C: Y = 12.814 5X-3.686 1, r=0.999 8; (42.8~1.07)f±g/mL. CONCLUSION The method proves to be easy and fast with good specificity, which can be used to control quality of leeches.

  8. Biological and Pharmaceutical Nanomaterials

    Science.gov (United States)

    Kumar, Challa S. S. R.

    2006-01-01

    This first comprehensive yet concise overview of all important classes of biological and pharmaceutical nanomaterials presents in one volume the different kinds of natural biological compounds that form nanomaterials or that may be used to purposefully create them. This unique single source of information brings together the many articles published in specialized journals, which often remain unseen by members of other, related disciplines. Covering pharmaceutical, nucleic acid, peptide and DNA-Chitosan nanoparticles, the book focuses on those innovative materials and technologies needed for the continued growth of medicine, healthcare, pharmaceuticals and human wellness. For chemists, biochemists, cell biologists, materials scientists, biologists, and those working in the pharmaceutical and chemical industries.

  9. Ionic Liquids in Pharmaceuticals%具有药物活性的离子液体

    Institute of Scientific and Technical Information of China (English)

    杨亭亭; 高国华

    2012-01-01

    In order to solve the problems associated with the solid form of conventional pharmaceuticals including polymorphic conversion, low solubility, low bioavailability, and the tendency of amorphous forms to spontaneously crystallize, the liquid form pharmaceuticals have attracted much attention. Recent developments of ionic liquids (ionic liquids are loosely defined as salts with melting points below 100℃) might prove beneficial. Ionic liquids exhibit controlled solubility, unique surface activity, high thermostability and enhancement in bioavailability or bioactivity, which make ionic liquids have the advantage of elimination of polymorphism, new delivery options, or having customized pharmaceutical cocktails. In some cases, an active cation and an active anion can be combined to produce a liquid possessing dual functionality. These make ionic liquids have the possibility of being used in the pharmaceutical industry. The aim of this mini-review is to summarize the recent development of ionic liquids as active pharmaceutical ingredients, antimicrobial agents and agricuhure chemicals, and discuss the existing problems and the future research of ionic liquids in pharmaceuticals.%离子液体阴阳离子的可设计性使其具有可控溶解性、独特表面活性、高热稳定性、增强的生物利用率和生物活性,这些特点使离子液体在消除同质多晶现象、改变药物传输模式及可包含传统药物组分等方面具有优势,成为当前离子液体研究领域的热点之一。本文对离子液体在医药领域的应用做了全面的阐述,主要介绍了近十年来离子液体在活性药物组分、抗菌剂及除草剂方面的成果,探讨了当前存在的问题及研究方向,并对其应用做了展望。

  10. Pharmaceutical care in smoking cessation.

    Science.gov (United States)

    Marín Armero, Alicia; Calleja Hernandez, Miguel A; Perez-Vicente, Sabina; Martinez-Martinez, Fernando

    2015-01-01

    As a determining factor in various diseases and the leading known cause of preventable mortality and morbidity, tobacco use is the number one public health problem in developed countries. Facing this health problem requires authorities and health professionals to promote, via specific programs, health campaigns that improve patients' access to smoking cessation services. Pharmaceutical care has a number of specific characteristics that enable the pharmacist, as a health professional, to play an active role in dealing with smoking and deliver positive smoking cessation interventions. The objectives of the study were to assess the efficacy of a smoking cessation campaign carried out at a pharmaceutical care center and to evaluate the effects of pharmaceutical care on patients who decide to try to stop smoking. The methodology was an open, analytical, pre-post intervention, quasi-experimental clinical study performed with one patient cohort. The results of the study were that the promotional campaign for the smoking cessation program increased the number of patients from one to 22, and after 12 months into the study, 43.48% of the total number of patients achieved total smoking cessation. We can conclude that advertising of a smoking cessation program in a pharmacy increases the number of patients who use the pharmacy's smoking cessation services, and pharmaceutical care is an effective means of achieving smoking cessation. PMID:25678779

  11. A successful virtual screening application: prediction of anticonvulsant activity in MES test of widely used pharmaceutical and food preservatives methylparaben and propylparaben.

    Science.gov (United States)

    Talevi, Alan; Bellera, Carolina L; Castro, Eduardo A; Bruno-Blanch, Luis E

    2007-09-01

    A discriminant function based on topological descriptors was derived from a training set composed by anticonvulsants of clinical use or in clinical phase of development and compounds with other therapeutic uses. This model was internally and externally validated and applied in the virtual screening of chemical compounds from the Merck Index 13th. Methylparaben (Nipagin), a preservative widely used in food, cosmetics and pharmaceutics, was signaled as active by the discriminant function and tested in mice in the Maximal Electroshock (MES) test (i.p. administration), according to the NIH Program for Anticonvulsant Drug Development. Based on the results of Methylparaben, Propylparaben (Nipasol), another preservative usually used in association with the former, was also tested. Both methyl and propylparaben were found active in mice at doses of 30, 100, and 300 mg/kg. The discovery of the anticonvulsant activities in the MES test of methylparaben and propylparaben might be useful for the development of new anticonvulsant medications, specially considering the well-known toxicological profile of these drugs.

  12. Qualitative Confirmation of Active Ingredient of Arbutin in Pear Leaves and Quantitative Determination by HPLC%梨树叶中有效成分熊果苷的确证及HPLC检测

    Institute of Scientific and Technical Information of China (English)

    赵洁; 何强; 姚秉华; 孔祥虹

    2011-01-01

    目的 确证梨树叶中含有熊果苷,并建立高效液相色谱法测定梨树叶中熊果苷的含量.方法 将充分粉碎的梨树叶样品用甲醇提取,蒸去甲醇后用ENVITM- 18固相萃取柱净化,采用在线获取的紫外光谱及扫描质谱对熊果苷进行确证.高效液相色谱分析时用Inertsil ODS-3色谱柱分离,甲醇-水(1:9)洗脱,282 nm检测.结果 梨树叶样品中目标物的紫外吸收光谱及子离子扫描质谱图与熊果苷标准品相同.高效液相色谱法定量分析时线性关系良好,熊果苷的回收率>93%,RSD<2.1%.结论 梨树叶中含有熊果苷有效成分,高效液相色谱法检测梨树叶中熊果苷的含量简便、快速、准确.%OBJECTIVE To confirm arbutin as an ingredient in pear leaves, and develop a method for the determination of arbutin content in pear leaves by HPLC. METHODS The full powdered pear leaves were extracted with methanol, then cleanup was performed on ENVI-18 SPE columns after methanol boiled off. Qualitative confirmation using the UV spectrum and mass spectra was acquired on-line. HPLC was performed on Inertsil ODS-3 column with DAD detection wavelength of 282 nm using methanol-water( 1: 9) as mobile phase. RESULTS The UV spectrum and mass spectra of the target chromatographic peak were the same as arbutin standard. The HPLC method showed good linear relationship, the recoveries of arbutin were all more than 93% and RSD was less than 2.1%. CONCLUSION Arbutin is an active ingredient in pear leaves, and HPLC as the content analysis method is simple, rapid and accurate.

  13. Dielectronic recombination of Fe 3p^q ions: a key ingredient for describing X-ray absorption in active galactic nuclei

    CERN Document Server

    Badnell, N R

    2006-01-01

    We have carried-out multi-configuration Breit-Pauli AUTOSTRUCTURE calculations for the dielectronic recombination (DR) of Fe^{8+} - Fe^{12+} ions. We obtain total DR rate coefficients for the initial ground-level which are an order of magnitude larger than those corresponding to radiative recombination (RR), at temperatures where Fe 3p^q (q=2-6) ions are abundant in photoionized plasmas. The resultant total (DR+RR) rate coefficients are then an order of magnitude larger than those currently in use by photoionized plasma modeling codes such as CLOUDY, ION and XSTAR. These rate coefficients, together with our previous results for q=0 and 1, are critical for determining the ionization balance of the M-shell Fe ions which give rise to the prominent unresolved-transition-array X-ray absorption feature found in the spectrum of many active galactic nuclei. This feature is poorly described by CLOUDY and ION, necessitating an ad hoc modification to the low-temperature DR rate coefficients. Such modifications are no lo...

  14. 抗肝纤维化的中药有效成分及其作用机制研究进展%Advances in active ingredients and action mechanism of TCM in treatment of hepatic fibrosis

    Institute of Scientific and Technical Information of China (English)

    孙蕾; 邓华平; 席忠新; 李霞; 孙连娜

    2012-01-01

    肝纤维化是多数慢性肝病所共有的病理特征,肝纤维化逐步发展形成肝硬化,最终导致肝癌.本文将近年报道的具有抗HF作用的中药有效成分作简单综述,归纳为黄酮类、生物碱类、萜类、酚类化合物,并总结了各类有效成分抗HF的作用机制,为深入开展中药抗HF的研究提供一定的参考.%Hepatic fibrosis was the common feature of pathology in almost all patients with chronic liver injury, which led to cirrhosis gradually and liver cancer ultimately. The anti-hepatic fibrosis active ingredients from TCM, including flavones, alkaloids, terpenes and phenols compounds were reviewed with the action mechanism in this paper, which could provide some references for the further study about the anti-hepatic fibrosis of TCM.

  15. Research advances in garlic's main active ingredients and their pharmacological effects%大蒜主要活性成分及药理作用研究进展

    Institute of Scientific and Technical Information of China (English)

    马丽娜; 李峰杰; 陈坚; 李贻奎

    2014-01-01

    大蒜为广义百合科植物大蒜( Allium sativum L.)的鳞茎,具有防治心血管疾病、抗肿瘤及抗病原微生物等多方面的作用。该文通过查阅国内外文献,对大蒜的主要活性成分及药理作用进行综述,并针对国内大蒜研究中存在的问题和研究进展进行了初步的分析,为大蒜的进一步研究及新药开发提供一定的参考。%Garlic is a bulb from generalized liliaceous plant Alli-um sativum, it plays an essential role in the prevention and treat-ment of cardiovascular diseases, tumors and pathogenic microor-ganisms. Through consulting domestic and foreign references, the main active ingredients of garlic and their pharmacological effects are reviewed, the problems and achievement in Chinese research are also discussed. It can provide a certain reference for the further study of garlic and new drug development.

  16. Dynamic Determination of Active Ingredients in Introduced Echinacea purpurea%引种紫锥菊不同部位有效成分含量的动态测定

    Institute of Scientific and Technical Information of China (English)

    韩琳娜; 孙俊英; 郭庆梅

    2014-01-01

    目的:研究引种紫锥菊中有效成分的动态积累规律。方法:分别采用HPLC和比色法测定紫锥菊生长过程中不同部位菊苣酸和总多酚含量。结果:一年生紫锥菊中总多酚含量变化不大,不同时期不同部位的菊苣酸含量存在差异,各部位菊苣酸含量在盛花期达最大值。结论:紫锥菊采收期取决于菊苣酸含量。研究结果可为山东引种紫锥菊提供理论依据。%This study was aimed to analyze the dynamic accumulation of active ingredients of Echinacea purpurea. Contents of cichoric acid and total polyphenols in different parts through the whole growth process were determined by HPLC and colorimetry. The results showed that the content of total polyphenol changed little in annual plant. There were differences in content of cichoric acid of different parts in different periods. And the content reached the maximum at flowering stage. It was concluded that the harvest stage depended on the content of cichoric acid. The results provided theoretical basis for induced plant in Shandong province.

  17. Research Progress of TCM Medicinal Herbs and Their Active Ingredients in Anti-bacterial Biofilms of Caries%中草药及其活性成分抗龋病细菌生物膜研究进展

    Institute of Scientific and Technical Information of China (English)

    刘玉梅; 徐静舒

    2015-01-01

    龋病是一种最常见的慢性进行性口腔疾病。中草药与传统治疗龋病的药物(如氟化物)相比有诸多优势,因此,近年来中草药抗龋成为国内外众多学者关注的热点。龋病不是单因素疾病,龋病的发生与变形链球菌、血链球菌、内氏放线菌、黏性放线菌、乳酸杆菌形成的细菌生物膜密切相关。本文就中草药及其活性成分抗龋病细菌生物膜相关研究进行简要概述。%Caries is one of the most common chronic progressive oral diseases. TCM medicinal herbs have many advantages compared with traditional dental drugs for caries (such as fluoride). In recent years, cariogenic TCM medicinal herbs have attracted the attention of many domestic and foreign scholars. Caries is not caused by a single factor. The development of caries is closely related to bacterial biofilms that are formed by streptococcus mutans, streptococcus sanguis, actinomyces inside, actinomyces and lactobacillus. Therefore, this article took a brief overview of TCM medicinal herbs and their active ingredients that inhibit the bacterial biofilms.

  18. Strategic Management of Innovations at Pharmaceutical Enterprises

    Directory of Open Access Journals (Sweden)

    Honcharova Svіtlana Yu.

    2014-01-01

    Full Text Available The article is devoted to theoretical and practical issues of the use of the concept of strategic management of innovations at pharmaceutical enterprises. It studies main barriers, which restrict development of Ukrainian pharmaceutical enterprises. It analyses the state and tendencies of development of innovation activity of pharmaceutical enterprises and studies foreign experience of innovation activity. It marks out specific features of strategic management of innovation development in pharmaceutical industry. It specifies the role and advantages of methods of strategic analysis in the system of management of a pharmaceutical enterprise. It considers the essence of “innovation development” and “innovation model of development” notions and analyses their organisational and legal provision. It justifies strategic tasks of the pharmaceutical filed to focus on in order to achieve a breakthrough when building an innovation model of economic development. The article proves that the most important factors that ensure growth of efficiency of pharmaceutical production are: wide application of the concept of strategic management and creation of innovations.

  19. Novel botanical ingredients for beverages.

    Science.gov (United States)

    Gruenwald, Joerg

    2009-01-01

    Natural substances are generally preferred over chemical ones and are generally seen as healthy. The increasing demand for natural ingredients, improving health and appearance, is also attracting beverages as the fastest growing segment on the functional food market. Functional beverages are launched as fortified water, tea, diary or juices claiming overall nutrition, energy, anti-aging or relaxing effects. The substitution of so called superfruits, such as berries, grapes, or pomegranate delivers an effective range of beneficial compounds, including vitamins, fatty acids, minerals, and anti-oxidants. In this context, new exotic and African fruits could be useful sources in the near future. Teas and green botanicals, such as algae or aloe vera are also rich in effective bioactives and have been used traditionally. The botanical kingdom offers endless possibilities. PMID:19168002

  20. Process and technical requirement for the development of the active pharmaceutical ingredient (API) generic drugs%仿制原料药研究开发流程及技术要求

    Institute of Scientific and Technical Information of China (English)

    刘旭亮; 张立颖; 臧恒昌

    2009-01-01

    本文针对国家食品药品监督管理局对仿制原料药研究开发出台的一些新法规和技术指导原则,研究确定了仿制药研发流程及技术要求,以期对仿制原料药的研发具有一定的指导意义.