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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...

  2. 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.

  3. 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

  4. International Conference on Harmonisation; guidance on good manufacturing practice for active pharmaceutical ingredients; availability. Notice.

    Science.gov (United States)

    2001-09-25

    The Food and Drug Administration (FDA) is announcing the availability of a guidance entitled "Q7A Good Manufacturing Practice Guidance for Active Pharmaceutical Ingredients." The guidance was prepared under the auspices of the International Conference on Harmonisation of Technical Requirements for Registration of Pharmaceuticals for Human Use (ICH). The guidance describes current good manufacturing practice (CGMP) for manufacturing of active pharmaceutical ingredients (APIs). The guidance is intended to help ensure that all APIs meet the standards for quality and purity they purport or are represented to possess.

  5. 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.

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

    OpenAIRE

    Bharate, Sonali S.; Bharate, Sandip B.; Bajaj, Amrita N

    2016-01-01

    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 literature reports of interaction and incompatibilities of commonly used pharmaceutical excipients with differen...

  7. The Potential of Cyclodextrins as Novel Active Pharmaceutical Ingredients: A Short Overview

    Directory of Open Access Journals (Sweden)

    Massimiliano Pio di Cagno

    2016-12-01

    Full Text Available Cyclodextrins (CDs are cyclic oligosaccharides of natural origin that were discovered more than 100 years ago. The peculiar cone-like conformation of the sugar ring, expressing a lipophilic cavity and a hydrophilic external surface, allows these substances to spontaneously complex poorly soluble compounds in an aqueous environment. For more than 50 years, these substances have found applicability in the pharmaceutical and food industries as solubilizing agents for poorly soluble chemical entities. Nowadays, several research groups all over the world are investigating their potential as active pharmaceutical ingredients (APIs for the treatment of several illnesses (e.g., hypercholesterolemia, cancer, Niemann-Pick Type C disease. The aim of this review is to briefly retrace cyclodextrins’ legacy as complexing agents and describe the current and future prospects of this class of chemical entities in pharmaceutics as new APIs.

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

    Science.gov (United States)

    2013-01-17

    ... drug active pharmaceutical ingredient (API) and finished dosage form (FDF) facilities user fees for... applications in the backlog as of October 1, 2012, on finished dosage form (FDF) and active pharmaceutical... Finished Dosage Form Facility Fee Rates for Fiscal Year 2013 AGENCY: Food and Drug Administration,...

  9. Determination of nickel in active pharmaceutical ingredients by electrothermal atomic absorption spectrometry.

    Science.gov (United States)

    Bubnič, Zoran; Urleb, Uroš; Kreft, Katjuša; Veber, Marjan

    2010-03-01

    An electrothermal atomic absorption spectrometric procedure for the determination of nickel in active pharmaceutical ingredients was developed. Since the recoveries of nickel by the direct dissolution of samples in diluted nitric acid were low and caused errors in the determination of Ni in pharmaceutical samples, different approaches for sample pre-treatment were examined. It was found that the microwave digestion was the most suitable way for sample preparation. Various combinations of digestion agents and different microwave conditions were tested. The combination of nitric acid and hydrogen peroxide was found to be the most appropriate. The validity of the method was evaluated by recovery studies of spiked samples and by the comparison of the results obtained by inductively coupled plasma mass spectrometry (ICP-MS). The recovery ranged from 87.5 to 104.0% and a good agreement was achieved between both methods. The detection limit and the limit of quantification were 0.6 and 2.1 µg g-1 respectively. The precision of the method was confirmed by the determination of Ni in the spiked samples and was below 4%, expressed in terms of a relative standard deviation. The method was applied to the determination of nickel in production samples of active pharmaceutical ingredients and intermediates.

  10. Peculiar surface behavior of some ionic liquids based on active pharmaceutical ingredients.

    Science.gov (United States)

    Restolho, José; Mata, José Luis; Saramago, Benilde

    2011-02-21

    The ionic liquids based on biologically active cations and anions, commonly designated by ionic liquids based on active pharmaceutical ingredients (ILs-APIs), are interesting compounds for use in pharmaceutical applications. Lidocaine docusate, ranitidine docusate, and didecyldimethylammonium ibuprofen are examples of promising ILs-APIs that were recently synthesized. They were submitted to biological testing and calorimetric measurements, but nothing is known about their surface properties. In this work, we measured the surface tension and the contact angles on both hydrophilic and hydrophobic surfaces in a temperature range as wide as possible. Based on the wettability data, the polarity fractions were estimated using the Fowkes theory. The peculiar surface behavior observed was tentatively attributed to the presence of mesophases.

  11. 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 pharmaceutical potency of eggs from the parasite Trichuris suis (pig whipworm), used as an active pharmaceutical ingredient in medicine against chronic autoimmune diseases of the intestines such as Crohn's disease and Ulcerative colitis. The analysis will combine spectral and morphological characteristics...... in order to first detect and then classify the parasite eggs based on a set of biologically inspired, quantitative features. The egg classification is currently done manually using transmitted light microscopy, but to allow for validation of this process and to reduce the operator bias, an automated system...... and the classification was based on the orientation of the larva inside the egg: The ratio of longitudinal vs. latitudinal ‘lines’ inside the egg is higher for eggs containing a larva....

  12. 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...... removed at 5 mg/l ClO2 dose. Removal of the same APIs from the high COD effluent was observed when the ClO2 dose was increased to 1.25 mg/l and an increase in API removal only after treatment with 8 mg/l ClO2. This illustrates that treatment of wastewater effluents with chlorine dioxide has potential...... to remove pharmaceuticals traces from wastewater treatment plant effluents....

  13. 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......, it is important to be aware of this drug-excipient interaction, as it can reduce the shelf-life of a low-average molecular weight PEG formulation considerably. © 2014 Wiley Periodicals, Inc. and the American Pharmacists Association J Pharm Sci 103:2424-2433, 2014....

  14. Continuous Processing of Active Pharmaceutical Ingredients Suspensions via Dynamic Cross-Flow Filtration.

    Science.gov (United States)

    Gursch, Johannes; Hohl, Roland; Toschkoff, Gregor; Dujmovic, Diana; Brozio, Jörg; Krumme, Markus; Rasenack, Norbert; Khinast, Johannes

    2015-10-01

    Over the last years, continuous manufacturing has created significant interest in the pharmaceutical industry. Continuous filtration at low flow rates and high solid loadings poses, however, a significant challenge. A commercially available, continuously operating, dynamic cross-flow filtration device (CFF) is tested and characterized. It is shown that the CFF is a highly suitable technology for continuous filtration. For all tested model active pharmaceutical ingredients, a material-specific strictly linear relationship between feed and permeate rate is identified. Moreover, for each tested substance, a constant concentration factor is reached. A one-parameter model based on a linear equation is suitable to fully describe the CFF filtration performance. This rather unexpected finding and the concentration polarization layer buildup is analyzed and a basic model to describe the observed filtration behavior is developed.

  15. Electrochemical flow injection analysis of hydrazine in an excess of an active pharmaceutical ingredient: achieving pharmaceutical detection limits electrochemically.

    Science.gov (United States)

    Channon, Robert B; Joseph, Maxim B; Bitziou, Eleni; Bristow, Anthony W T; Ray, Andrew D; Macpherson, Julie V

    2015-10-06

    The quantification of genotoxic impurities (GIs) such as hydrazine (HZ) is of critical importance in the pharmaceutical industry in order to uphold drug safety. HZ is a particularly intractable GI and its detection represents a significant technical challenge. Here, we present, for the first time, the use of electrochemical analysis to achieve the required detection limits by the pharmaceutical industry for the detection of HZ in the presence of a large excess of a common active pharmaceutical ingredient (API), acetaminophen (ACM) which itself is redox active, typical of many APIs. A flow injection analysis approach with electrochemical detection (FIA-EC) is utilized, in conjunction with a coplanar boron doped diamond (BDD) microband electrode, insulated in an insulating diamond platform for durability and integrated into a two piece flow cell. In order to separate the electrochemical signature for HZ such that it is not obscured by that of the ACM (present in excess), the BDD electrode is functionalized with Pt nanoparticles (NPs) to significantly shift the half wave potential for HZ oxidation to less positive potentials. Microstereolithography was used to fabricate flow cells with defined hydrodynamics which minimize dispersion of the analyte and optimize detection sensitivity. Importantly, the Pt NPs were shown to be stable under flow, and a limit of detection of 64.5 nM or 0.274 ppm for HZ with respect to the ACM, present in excess, was achieved. This represents the first electrochemical approach which surpasses the required detection limits set by the pharmaceutical industry for HZ detection in the presence of an API and paves the wave for online analysis and application to other GI and API systems.

  16. 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.

  17. Consequences of new approach of chemical stability tests of active pharmaceutical ingredients (APIs

    Directory of Open Access Journals (Sweden)

    Marzena eJamrógiewicz

    2016-02-01

    Full Text Available There is a great need of broaden look on stability tests of active pharmaceutical ingredients (APIs in comparison with current requirements contained in pharmacopoeia. 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.

  18. Use of prediction methods to estimate true density of active pharmaceutical ingredients.

    Science.gov (United States)

    Cao, Xiaoping; Leyva, Norma; Anderson, Stephen R; Hancock, Bruno C

    2008-05-01

    True density is a fundamental and important property of active pharmaceutical ingredients (APIs). Using prediction methods to estimate the API true density can be very beneficial in pharmaceutical research and development, especially when experimental measurements cannot be made due to lack of material or sample handling restrictions. In this paper, two empirical prediction methods developed by Girolami and Immirzi and Perini were used to estimate the true density of APIs, and the estimation results were compared with experimentally measured values by helium pycnometry. The Girolami method is simple and can be used for both liquids and solids. For the tested APIs, the Girolami method had a maximum error of -12.7% and an average percent error of -3.0% with a 95% CI of (-3.8, -2.3%). The Immirzi and Perini method is more involved and is mainly used for solid crystals. In general, it gives better predictions than the Girolami method. For the tested APIs, the Immirzi and Perini method had a maximum error of 9.6% and an average percent error of 0.9% with a 95% CI of (0.3, 1.6%).

  19. 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

    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...... 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...

  20. Core-shell column Tanaka characterization and additional tests using active pharmaceutical ingredients.

    Science.gov (United States)

    Ludvigsson, Jufang Wu; Karlsson, Anders; Kjellberg, Viktor

    2016-12-01

    In the last decade, core-shell particles have gained more and more attention in fast liquid chromatography separations due to their comparable performance with fully porous sub-2 μm particles and their significantly lower back pressure. Core-shell particles are made of a solid core surrounded by a shell of classic fully porous material. To embrace the developed core-shell column market and use these columns in pharmaceutical analytical applications, 17 core-shell C18 columns purchased from various vendors with various dimensions (50 mm × 2.1 mm to 100 mm × 3 mm) and particle sizes (1.6-2.7 μm) were characterized using Tanaka test protocols. Furthermore, four selected active pharmaceutical ingredients were chosen as test probes to investigate the batch to batch reproducibility for core-shell columns of particle size 2.6-2.7 μm, with dimension of 100 × 3 mm and columns of particle size 1.6 μm, with dimension 100 × 2.1 mm under isocratic elution. Columns of particle size 2.6-2.7 μm were also tested under gradient elution conditions. To confirm the claimed comparable efficiency of 2.6 μm core-shell particles as sub-2 μm fully porous particles, column performances of the selected core-shell columns were compared with BEH C18 , 1.7 μm, a fully porous column material as well.

  1. 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.

  2. 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.

  3. 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.

  4. Microwave-assisted extraction of active pharmaceutical ingredient from solid dosage forms.

    Science.gov (United States)

    Hoang, T H; Sharma, R; Susanto, D; Di Maso, M; Kwong, E

    2007-07-13

    The microwave assisted extraction (MAE) technique has been evaluated for the extraction of active pharmaceutical ingredients (API) from various solid dosage forms. Using immediate release tablets of Compound A as a model, optimization of the extraction method with regards to extraction solvent composition, extraction time and temperature was briefly discussed. Complete recovery of Compound A was achieved when samples were extracted using acetonitrile as the extraction solvent under microwave heating at a constant cell temperature of 50 degrees C for 5 min. The optimized MAE method was applied for content uniformity (single tablet extraction) and potency (multiple tablets extraction) assays of release and stability samples of two products of Compound A (5 and 25mg dose strength) stored at various conditions. To further demonstrate the applicability of MAE, the instrumental extraction conditions (50 degrees C for 5 min) were adopted for the extraction of montelukast sodium (Singulair) from various solid dosage forms using methanol-water (75:25, v/v) as the extraction solvent. The MAE procedure demonstrated an extraction efficiency of 97.4-101.9% label claim with the greatest RSD at 1.4%. The results compare favorably with 97.6-102.3% label claim with the greatest RSD at 2.9% obtained with validated mechanical extraction procedures. The system is affordable, user-friendly and simple to operate and troubleshoot. Rapid extraction process (7 min/run) along with high throughput capacity (up to 23 samples simultaneously) would lead to reduced cycle time and thus increased productivity.

  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. Quantitative analysis of active pharmaceutical ingredients (APIs) using a potentiometric electronic tongue in a SIA flow system

    OpenAIRE

    2016-01-01

    An advanced potentiometric electronic tongue and Sequential Injection Analysis (SIA) measurement system was applied for the quantitative analysis of mixtures containing three active pharmaceutical ingredients (APIs): acetaminophen, ascorbic acid and acetylsalicylic acid, in the presence of various amounts of caffeine as interferent. The flow-through sensor array was composed of miniaturized classical ion-selective electrodes based on plasticized PVC membranes containing only ion exchangers. P...

  8. 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

  9. 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

    Continuous hydrolysis of an active pharmaceutical ingredient intermediate, and subsequent liquid–liquid (L-L) separation of the resulting organic and aqueous phases, have been achieved using a simple PTFE tube reactor connected to a miniscale hydrophobic membrane separator. An alkoxide product...... 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...

  10. 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.

  11. 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.

  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. 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.

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

    Science.gov (United States)

    Reeuwijk, Noortje M; Venhuis, Bastiaan J; de Kaste, Dries; Hoogenboom, Ron L A P; Rietjens, Ivonne M C M; Martena, Martijn 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 loss properties. Herbal food supplements intended for weight loss (n = 50) were sampled from August 2004 to May 2013. An HPLC-DAD-MS/MS method was used to screen for the presence of the APIs in herbal supplements. In 24 samples the APIs sibutramine, desmethylsibutramine (DMS), didesmethylsibutramine (DDMS), rimonabant, sildenafil and/or the laxative phenolphthalein were identified 41 times. The presence of these APIs was, however, not stated on the label. The potential pharmacological effects of the detected APIs were estimated using data from reported effective doses of approved drugs. Use of 20 of the 24 herbal food supplements may result in potential pharmacological effects. Furthermore, risk assessment of phenolphthalein, a suspected carcinogen and found to be present in 10 supplements, based on the margin of exposure (MOE) approach, resulted in MOE values of 96-30,000. MOE values lower than 10,000 (96-220) were calculated for the daily intake levels of four out of these 10 supplements in which phenolphthalein was found. However, taking into account that weight loss preparations may be used for only a few weeks or months rather than during a lifetime, MOE values may be two to three orders of magnitude higher. The current study shows that the use of food supplements with sibutramine, DMS, DDMS and/or phenolphthalein could result in pharmacological effects.

  15. Effect of particle shape of active pharmaceutical ingredients prepared by fluidized-bed jet-milling on cohesiveness.

    Science.gov (United States)

    Fukunaka, Tadashi; Sawaguchi, Kohta; Golman, Boris; Shinohara, Kunio

    2005-05-01

    Milling is a common procedure to improve bioavailability of many active pharmaceutical ingredients (APIs), which typically have low solubility in water. But such micronization can yield an increase in the cohesiveness of particles. Although particle cohesiveness is desirable for tablet strength in the subsequent formulation process, increased particle cohesiveness can lead to operational difficulties in a milling equipment due to compaction of particles inside. In this article, the impact of milling via a fluidized-bed jet-mill on the cohesive strength and interparticle force was studied using Ethenzamide as a pharmaceutical model compound. As a result, the particle shape was found to affect both the tensile strength of powder bed and the interparticle cohesive force. A powder bed, having relatively high void fraction by direct tensile test, shows a positive correlation between the cohesive force and the particle sphericity, while powders with low void fraction by diametral compression test show a positive correlation between the cohesive force and the angularity of the particle.

  16. Kinetics of the esterification of active pharmaceutical ingredients containing carboxylic acid functionality in polyethylene glycol: formulation implications.

    Science.gov (United States)

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

    2014-08-01

    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, whereas HPLC-MS was used to identify reaction products. The esterification reactions were observed to be reversible. A second-order reversible kinetic model was applied and rate constants were determined. The rate constants demonstrated that cetirizine was esterified about 240 times faster than indomethacin at 80 °C. The shelf-life for cetirizine in a PEG 400 formulation at 25 °C expressed as t(95%) was predicted to be only 30 h. Further, rate constants for esterification of cetirizine in PEG 1000 in relation to PEG 400 decreased by a factor of 10, probably related to increased viscosity. However, it is important to be aware of this drug-excipient interaction, as it can reduce the shelf-life of a low-average molecular weight PEG formulation considerably.

  17. 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.

  18. 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.

  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 and...... with a huge excess of HEP and reaction times of up to 24h. Acceleration of the reaction from 24 down to 4h is achieved by switching from batch operation mode in toluene to either solvent-free batch mode or microwave-assisted hydroamination with tetrahydrofuran as a solvent....

  20. 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.

  1. Assessment of active pharmaceutical ingredient particle size in tablets by Raman chemical imaging validated using polystyrene microsphere size standards.

    Science.gov (United States)

    Kuriyama, Atsushi; Ozaki, Yukihiro

    2014-04-01

    Particle size is a critical parameter for controlling pharmaceutical quality. The aim of this study was to assess the size of the micrometer-scale active pharmaceutical ingredients (API) in tablets using Raman chemical imaging and to understand the effects of formulation on particle size. Model tablets containing National Institute of Standards and Technology traceable polystyrene microsphere size standards were developed to determine the binarization threshold value of Raman chemical images for API particle sizing in specific formulations and processes. Three sets of model tablets containing 5, 10, and 15 μm polystyrene microspheres, used to mimic API, were prepared using a commercial tablet formulation (Ebastel tablets, mean API particle size was about 5 μm). Raman mapping with a 50× objective (NA, 0.75) was applied to tablet cross-sections, and particle size of polystyrene microspheres was estimated from binary images using several binarization thresholds. Mean particle size for three sets of polystyrene microspheres showed good agreement between pre- and postformulation (the slope = 1.024, R = 1.000) at the specific threshold value ((mean + 0.5σ) of the polystyrene-specific peak intensity histogram), regardless of particle agglomeration, tablet surface roughness, and laser penetration depth. The binarization threshold value showed good applicability to Ebastel tablets, where the API-specific peak intensity histogram showed a pattern similar to that of polystyrene microspheres in model tablets. The model tablets enabled determination of an appropriate binarization threshold for assessing the mean particle size of micrometer-scale API in tablets by utilizing the unique physicochemical properties of polystyrene microspheres.

  2. 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

  3. Occurrence and behaviour of 105 active pharmaceutical ingredients in sewage waters of a municipal sewer collection system.

    Science.gov (United States)

    Lindberg, Richard H; Östman, Marcus; Olofsson, Ulrika; Grabic, Roman; Fick, Jerker

    2014-07-01

    The concentrations and behaviour of 105 different active pharmaceutical ingredients (APIs) in the aqueous phase of sewage water within a municipal sewer collection system have been investigated. Sewage water samples were gathered from seven pump stations (one of which was located within a university hospital) and from sewage water treatment influent and effluent. The targeted APIs were quantified using a multi-residue method based on online solid phase extraction liquid chromatography tandem mass spectrometry. The method was thoroughly validated and complies with EU regulations on sample handling, limits of quantification, quality control and selectivity. 51 APIs, including antibiotics, antidepressants, hypertension drugs, analgesics, NSAIDs and psycholeptics, were found frequently within the sewer collection system. API concentrations and mass flows were evaluated in terms of their frequency of detection, daily variation, median/minimum/maximum/average concentrations, demographic dissimilarities, removal efficiencies, and mass flow profiles relative to municipal sales data. Our results suggest that some APIs are removed from, or introduced to, the aqueous phase of sewage waters within the studied municipal collection system.

  4. Understanding the glass-forming ability of active pharmaceutical ingredients for designing supersaturating dosage forms.

    Science.gov (United States)

    Kawakami, Kohsaku; Usui, Toshinori; Hattori, Mitsunari

    2012-09-01

    Amorphous solid dispersions have great potential for enhancing oral absorption of poorly soluble drugs. Crystallization behavior during storage and after exposure to aqueous media must be examined in detail for designing stable and effective amorphous formulations, and it is significantly affected by the intrinsic properties of an amorphous drug. Many attempts have been made to correlate various thermodynamic parameters of pharmaceutical glasses with their crystallization behavior; however, variations in model drugs that could be used for such investigation has been limited because the amorphous characteristics of drugs possessing a high crystallization tendency are difficult to evaluate. In this study, high-speed differential scanning calorimetry, which could inhibit their crystallization using high cooling rates up to 2000°C/s, was employed for assessing such drugs. The thermodynamic parameters of the glasses, including glass transition temperature (T(g)) and fragility, were obtained to show that their crystallization tendency cannot be explained simply by the parameters, although there have been general thought that fragility may be correlated with crystallization tendency. Also investigated was correlation between the thermodynamic parameters and crystallization tendency upon contact with water, which influences in vivo efficacy of amorphous formulations. T(g) was correlated well with the crystallization tendency upon contact with water.

  5. Stability indicating LC method for rapid determination of related substances of O-desmethyl venlafaxine in active pharmaceutical ingredients and pharmaceutical formulations.

    Science.gov (United States)

    Rao, Karri Visweswara; Reddy, Kesareddy Padmaja; Kumar, Yelavarthi Ravindra

    2014-01-01

    A simple, precise and accurate stability-indicating reversed phase-high performance liquid chromatography method was developed for the quantitative determination of O-desmethyl venlafaxine (ODV) and its related substances in active pharmaceutical ingredient and pharmaceutical formulation. The method was developed using YMC-pack ODS-A (150 × 4.6 mm, 3 μm) column with mobile phase containing a gradient mixture of solvents A and B. Solvent A contained a mixture of buffer and acetonitrile in the ratio of 85:15 (v/v). The buffer consisted of 10 mM potassium dihydrogen phosphate and 2 mM 1-octane sulfonic acid sodium salt (pH adjusted to 6.0 by using diluted potassium hydroxide solution). Solvent B contained a mixture of water and acetonitrile in the ratio of 20:80 (v/v). The eluted compounds were monitored at 230 nm. ODV and its six impurities were well separated within 14 min run time. It was subjected under the stress conditions of oxidative, acid, base, water, thermal and photolytic degradation. It was sensitive towards acidic, basic, oxidative and water stress conditions, stable in photolytic and thermal degradation conditions. The degradation products were well resolved from main peak and its impurities, the mass balance in each case was >99.0%, proving the stability-indicating power of the method. The developed method was validated as per International Conference on Harmonization (ICH) guidelines with respect to its specificity, linearity (correlation coefficient >0.9996), limit of detection, limit of quantification, accuracy (recovery range 97.1-103.2%), precision (% relative standard deviation ≤1.9%) and robustness.

  6. 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.

  7. 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.

  8. 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

    OpenAIRE

    2010-01-01

    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 th...

  9. 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.

  10. 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.

  11. Stability-indicating UPLC method for determination of Valsartan and their degradation products in active pharmaceutical ingredient and pharmaceutical dosage forms.

    Science.gov (United States)

    Krishnaiah, Ch; Reddy, A Raghupathi; Kumar, Ramesh; Mukkanti, K

    2010-11-02

    A simple, precise, accurate stability-indicating gradient reverse phase ultra-performance liquid chromatographic (RP-UPLC) method was developed for the quantitative determination of purity of Valsartan drug substance and drug products in bulk samples and pharmaceutical dosage forms in the presence of its impurities and degradation products. The method was developed using Waters Aquity BEH C18 (100 mm x 2.1 mm, 1.7 microm) column with mobile phase containing a gradient mixture of solvents A and B. The eluted compounds were monitored at 225 nm, the run time was within 9.5 min, which Valsartan and its seven impurities were well separated. Valsartan was subjected to the stress conditions of oxidative, acid, base, hydrolytic, thermal and photolytic degradation. Valsartan was found to degrade significantly in acid and oxidative stress conditions and stable in base, hydrolytic and photolytic degradation conditions. The degradation products were well resolved from main peak and its impurities, proving the stability-indicating power of the method. The developed method was validated as per international conference on harmonization (ICH) guidelines with respect to specificity, linearity, limit of detection, limit of quantification, accuracy, precision and robustness. This method was also suitable for the assay determination of Valsartan in pharmaceutical dosage forms.

  12. 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.

  13. 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

  14. Comparison of adsorption equilibrium and kinetic models for a case study of pharmaceutical active ingredient adsorption from fermentation broths: parameter determination, simulation, sensitivity analysis and optimization

    Directory of Open Access Journals (Sweden)

    B. Likozar

    2012-09-01

    Full Text Available Mathematical models for a batch process were developed to predict concentration distributions for an active ingredient (vancomycin adsorption on a representative hydrophobic-molecule adsorbent, using differently diluted crude fermentation broth with cells as the feedstock. The kinetic parameters were estimated using the maximization of the coefficient of determination by a heuristic algorithm. The parameters were estimated for each fermentation broth concentration using four concentration distributions at initial vancomycin concentrations of 4.96, 1.17, 2.78, and 5.54 g l−¹. In sequence, the models and their parameters were validated for fermentation broth concentrations of 0, 20, 50, and 100% (v/v by calculating the coefficient of determination for each concentration distribution at the corresponding initial concentration. The applicability of the validated models for process optimization was investigated by using the models as process simulators to optimize the two process efficiencies.

  15. 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.

  16. 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.

  17. 77 FR 60124 - Draft Guidance for Industry on Initial Completeness Assessments for Type II Active Pharmaceutical...

    Science.gov (United States)

    2012-10-02

    ... Assessments for Type II Active Pharmaceutical Ingredient Drug Master Files Under the Generic Drug User Fee... Amendments of 2012 (GDUFA), holders of certain drug master files, namely, Type II active...

  18. 21 CFR 358.310 - Ingrown toenail relief active ingredient.

    Science.gov (United States)

    2010-04-01

    ... 21 Food and Drugs 5 2010-04-01 2010-04-01 false Ingrown toenail relief active ingredient. 358.310... (CONTINUED) DRUGS FOR HUMAN USE MISCELLANEOUS EXTERNAL DRUG PRODUCTS FOR OVER-THE-COUNTER HUMAN USE Ingrown Toenail Relief Drug Products § 358.310 Ingrown toenail relief active ingredient. The active ingredient...

  19. 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...

  20. NOVEL HYDROXAMIC ACIDS HAVING HISTONE DEACETYLASE INHIBITING ACTIVITY AND ANTI-CANCER COMPOSITION COMPRISING THE SAME AS AN ACTIVE INGREDIENT

    DEFF Research Database (Denmark)

    2013-01-01

    The present invention relates to a pharmaceutical composition for anticancer including novel hydroxamic acid with histone deacetylase inhibiting activity as an active ingredient. Hydroxamic acid compound of the present invention has inhibitory activity of histone deacetylase (HDAC) and shows cyto...... cytotoxicity to a variety of cancer cells, being useful in strong anti-cancer drug....

  1. 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.

  2. 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.

  3. Photocatalytic degradation of sunscreen active ingredients mediated by nanostructured materials

    Science.gov (United States)

    Soto-Vazquez, Loraine

    Water scarcity and pollution are environmental issues with terrible consequences. In recent years several pharmaceutical and personal care products, such as sunscreen active ingredients, have been detected in different water matrices. Its recalcitrant behavior in the environment has caused controversies and generated countless questions about its safety. During this research, we employed an advanced oxidation process (photocatalysis) to degrade sunscreen active ingredients. For this study, we used a 3x3 system, evaluating three photocatalysts and three different contaminants. From the three catalysts employed, two of them were synthesized. ZnO nanoparticles were obtained using zinc acetate dihydrated as the precursor, and TiO2 nanowires were synthesized from titanium tetrachloride precursor. The third catalyst employed (namely, P25) was obtained commercially. The synthesized photocatalysts were characterized in terms of the morphology, elemental composition, crystalline structure, elemental oxidation states, vibrational modes and surface area, using SEM-EDS, XRD, XPS, Raman spectroscopy and BET measurements, respectively. The photocatalysts were employed during the study of the degradation of p-aminobenzoic acid, phenylbenzimidazole sulfonic acid, and benzophenone-4. In all the cases, at least 50% degradation was achieved. P25 showed degradation efficiencies above 90%, and from the nine systems, 7 of them degraded at least 86%.

  4. Endocrine-Active Pharmaceuticals: An Environmental Concern?

    Science.gov (United States)

    Recently, there has been growing interest in pharmaceuticals that are specifically designed to have endocrine activity, such as the estrogens used in birth control pills, exerting unintended effects on fish and other aquatic organisms. These pharmaceuticals may not be persistent...

  5. Research Progression of Anti-HIV Chinese Medicines and Their Natural Active Ingredients

    Institute of Scientific and Technical Information of China (English)

    Chen Jing; Fu Linchun; Li Maoqing; Chen Jiantao

    2014-01-01

    Objective: To review the research progression of Chinese medicines for anti-human immunodeifciency virus (HIV) and their natural active ingredients at home and abroad so as to provide references for pharmaceutical research and clinical medication. Methods:Abundant representative literatures at home and abroad were classiifed to introduce the anti-HIV monomers, compounds and natural active ingredients of Chinese medicines. Results:The researches on anti-HIV natural medicines have obtained great achievements, in which medicines with anti-virus and immunity-improving functions have had rapid progression and new-types for anti-virus also have had dramatic development. Conclusion:The progression of anti-HIV Chinese medicines and their active ingredients has favorable prospect.

  6. 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.

  7. Nanocarriers for the delivery of active ingredients and fractions extracted from natural products used in traditional Chinese medicine (TCM).

    Science.gov (United States)

    Liu, Ying; Feng, Nianping

    2015-07-01

    Traditional Chinese medicine (TCM) has been practiced for thousands of years with a recent increase in popularity. Despite promising biological activities of active ingredients and fractions from TCM, their poor solubility, poor stability, short biological half-life, ease of metabolism and rapid elimination hinder their clinical application. Therefore, overcoming these problems to improve the therapeutic efficacy of TCM preparations is a major focus of pharmaceutical sciences. Recently, nanocarriers have drawn increasing attention for their excellent and efficient delivery of active TCM ingredients or fractions. This review discusses problems in the delivery of active TCM ingredients or fractions; focuses on recent advances in nanocarriers that represent potential solutions to these problems, including lipid-based nanoparticles and polymeric, inorganic, and hybrid nanocarriers; and discusses unanswered questions in the field and criteria for the development of better nanocarriers for the delivery of active TCM ingredients or fractions to be focused on in future studies.

  8. A survey of Chinese herbal ingredients with liver protection activities

    Directory of Open Access Journals (Sweden)

    Lien Linda

    2007-05-01

    Full Text Available Abstract A literature survey was conducted on herbs, their preparations and ingredients with reported liver protection activities, in which a total of 274 different species and hundreds of active ingredients have been examined. These ingredients can be roughly classified into two categories according to their activities: (1 the main ingredients, such as silybin, osthole, coumarin, glycyrrhizin, saikosaponin A, schisandrin A, flavonoids; and (2 supporting substances, such as sugars, amino acids, resins, tannins and volatile oil. Among them, some active ingredients have hepatoprotective activities (e.g. anti-inflammatory, anticancer, antioxidant, immunomodulating and liver cirrhosis-regulating effects. Calculation of physicochemical parameters indicates that the main ingredients with negative and positive Elumo values possibly display their hepatoprotective effects through different mechanisms, such as antioxidative, anti-inflammatory and immunomodulating effects. As the combination of herbs may achieve some treatment effects synergistically and/or additively, it is common in Chinese medicine to use mixtures of various medicinal herbs with pharmacologically active compounds to have synergistic and/or additive effects, or to reduce harmful effects of some pharmacologically active compounds. In particular, the active compounds with Clog P around 2 are suitable for passive transport across membranes and accessible to the target sites. Thus, Elumo and Clog P values are good indicators among the calculated parameters. Seven different physicochemical parameters (MW, Clog P, CMR, μ, Ehomo, Elumo and Hf and four major biological activities (antioxidant, anti-inflammatory, antiviral/antitumor and immunomodulating are discussed in this review. It is hoped that the discussion may provide some leads in the development of new hepatoprotective drugs.

  9. 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...

  10. 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.

  11. 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) DRUGS FOR HUMAN USE COLD, COUGH, ALLERGY, BRONCHODILATOR, AND ANTIASTHMATIC DRUG PRODUCTS FOR...

  12. Agglomeration Control during Ultrasonic Crystallization of an Active Pharmaceutical Ingredient

    Directory of Open Access Journals (Sweden)

    Bjorn Gielen

    2017-02-01

    Full Text Available Application of ultrasound during crystallization can efficiently inhibit agglomeration. However, the mechanism is unclear and sonication is usually enabled throughout the entire process, which increases the energy demand. Additionally, improper operation results in significant crystal damage. Therefore, the present work addresses these issues by identifying the stage in which sonication impacts agglomeration without eroding the crystals. This study was performed using a commercially available API that showed a high tendency to agglomerate during seeded crystallization. The crystallization progress was monitored using process analytical tools (PAT, including focus beam reflectance measurements (FBRM to track to crystal size and number and Fourier transform infrared spectroscopy (FTIR to quantify the supersaturation level. These tools provided insight in the mechanism by which ultrasound inhibits agglomeration. A combination of improved micromixing, fast crystal formation which accelerates depletion of the supersaturation and a higher collision frequency prevent crystal cementation to occur. The use of ultrasound as a post-treatment can break some of the agglomerates, but resulted in fractured crystals. Alternatively, sonication during the initial seeding stage could assist in generating nuclei and prevent agglomeration, provided that ultrasound was enabled until complete desupersaturation at the seeding temperature. FTIR and FBRM can be used to determine this end point.

  13. ANTIOXIDANT AND ANTITUMOR ACTIVITY OF INDONESIAN HERBAL INGREDIENTS

    OpenAIRE

    2015-01-01

    The present study was to aimed to evaluated and compare in vitro antioxidant activities of 2 Indonesian herbal ingredients (A and B), determined total phenol content., cytotoxic and apoptosis induction activities on HL-60 cells. These data were providing some useful information for people healthy dietary and the new potential application of natural antioxidant containing food materials in functional foods and also as new cancer therapeutics promising candidates. The parameters were total anti...

  14. Preparation and evaluation of combination tablet containing incompatible active ingredients.

    Science.gov (United States)

    Wang, Xiaoyan; Cui, Fude; Yonezawa, Yorinobu; Sunada, Hisakazu

    2003-07-01

    Combination preparation plays an important role in clinical treatment because of its better and wider curative synergism and weaker side effects. However, the existence of incompatibility between active ingredients or between active ingredients and excipients presents a serious obstacle in the preparation of such combination solid dosage forms. In this study, aspirin and ranitidine hydrochloride, between which there existed a chemical interaction, were selected as model drugs. Aspirin powders without any additives were granulated with hydroxypropyl methyl cellulose (HPMC) water solution as a binder using a Wurster coating apparatus and the operation conditions were optimized by Artificial Neural Network (ANN) analysis. Under these conditions, the aspirin granules prepared showed good flowability and compressibility. On the other hand, ranitidine hydrochloride was coated with Aquacoat (ethyl cellulose aqueous dispersion) after preliminary granulation with the Wurster coating apparatus. The aspirin granules and coated ranitidine hydrochloride particles were compressed into tablets with suitable excipients. The combination tablets showed good dissolution, content uniformity and improved stability of active ingredients.

  15. 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;...

  16. Nano-microdelivery systems for oral delivery of an active ingredient

    DEFF Research Database (Denmark)

    2014-01-01

    A composition for oral delivery of one or more active ingredients in the form of a lipid nano-micro-delivery system comprising a lipid nano-micro-structure comprising at least one lipid and at least one active ingredient, said at least one active ingredient being immobilized in said lipid nano...

  17. 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...

  18. Availability, Pharmaceutics, Security, Pharmacokinetics, and Pharmacological Activities of Patchouli Alcohol

    Directory of Open Access Journals (Sweden)

    Guanying Hu

    2017-01-01

    Full Text Available Patchouli alcohol (PA, a tricyclic sesquiterpene, is one of the critical bioactive ingredients and is mainly isolated from aerial part of Pogostemon cablin (known as guanghuoxiang in China belonging to Labiatae. So far, PA has been widely applied in perfume industries. This review was written with the use of reliable information published between 1974 and 2016 from libraries and electronic researches including NCKI, PubMed, Reaxys, ACS, ScienceDirect, Springer, and Wiley-Blackwell, aiming at presenting comprehensive outline of security, pharmacokinetics, and bioactivities of PA and at further providing a potential guide in exploring the PA and its use in various medical fields. We found that PA maybe was a low toxic drug that was acquired numerously through vegetable oil isolation and chemical synthesis and its stability and low water dissolution were improved in pharmaceutics. It also possessed specific pharmacokinetic characteristics, such as two-compartment open model, first-order kinetic elimination, and certain biometabolism and biotransformation process, and was shown to have multiple biological activities, that is, immunomodulatory, anti-inflammatory, antioxidative, antitumor, antimicrobial, insecticidal, antiatherogenic, antiemetic, whitening, and sedative activity. However, the systematic evaluations of preparation, pharmaceutics, toxicology, pharmacokinetics, and bioactivities underlying molecular mechanisms of action also required further investigation prior to practices of PA in clinic.

  19. Comparative Solid-State Stability of Perindopril Active Substance vs. Pharmaceutical Formulation

    Science.gov (United States)

    Buda, Valentina; Andor, Minodora; Ledeti, Adriana; Ledeti, Ionut; Vlase, Gabriela; Vlase, Titus; Cristescu, Carmen; Voicu, Mirela; Suciu, Liana; Tomescu, Mirela Cleopatra

    2017-01-01

    This paper presents the results obtained after studying the thermal stability and decomposition kinetics of perindopril erbumine as a pure active pharmaceutical ingredient as well as a solid pharmaceutical formulation containing the same active pharmaceutical ingredient (API). Since no data were found in the literature regarding the spectroscopic description, thermal behavior, or decomposition kinetics of perindopril, our goal was the evaluation of the compatibility of this antihypertensive agent with the excipients in the tablet under ambient conditions and to study the effect of thermal treatment on the stability of perindopril erbumine. ATR-FTIR (Attenuated Total Reflectance Fourier Transform Infrared) spectroscopy, thermal analysis (thermogravimetric mass curve (TG—thermogravimetry), derivative thermogravimetric mass curve (DTG), and heat flow (HF)) and model-free kinetics were chosen as investigational tools. Since thermal behavior is a simplistic approach in evaluating the thermal stability of pharmaceuticals, in-depth kinetic studies were carried out by classical kinetic methods (Kissinger and ASTM E698) and later with the isoconversional methods of Friedman, Kissinger-Akahira-Sunose and Flynn-Wall-Ozawa. It was shown that the main thermal degradation step of perindopril erbumine is characterized by activation energy between 59 and 69 kJ/mol (depending on the method used), while for the tablet, the values were around 170 kJ/mol. The used excipients (anhydrous colloidal silica, microcrystalline cellulose, lactose, and magnesium stearate) should be used in newly-developed generic solid pharmaceutical formulations, since they contribute to an increased thermal stability of perindopril erbumine. PMID:28098840

  20. Comparative Solid-State Stability of Perindopril Active Substance vs. Pharmaceutical Formulation

    Directory of Open Access Journals (Sweden)

    Valentina Buda

    2017-01-01

    Full Text Available This paper presents the results obtained after studying the thermal stability and decomposition kinetics of perindopril erbumine as a pure active pharmaceutical ingredient as well as a solid pharmaceutical formulation containing the same active pharmaceutical ingredient (API. Since no data were found in the literature regarding the spectroscopic description, thermal behavior, or decomposition kinetics of perindopril, our goal was the evaluation of the compatibility of this antihypertensive agent with the excipients in the tablet under ambient conditions and to study the effect of thermal treatment on the stability of perindopril erbumine. ATR-FTIR (Attenuated Total Reflectance Fourier Transform Infrared spectroscopy, thermal analysis (thermogravimetric mass curve (TG—thermogravimetry, derivative thermogravimetric mass curve (DTG, and heat flow (HF and model-free kinetics were chosen as investigational tools. Since thermal behavior is a simplistic approach in evaluating the thermal stability of pharmaceuticals, in-depth kinetic studies were carried out by classical kinetic methods (Kissinger and ASTM E698 and later with the isoconversional methods of Friedman, Kissinger-Akahira-Sunose and Flynn-Wall-Ozawa. It was shown that the main thermal degradation step of perindopril erbumine is characterized by activation energy between 59 and 69 kJ/mol (depending on the method used, while for the tablet, the values were around 170 kJ/mol. The used excipients (anhydrous colloidal silica, microcrystalline cellulose, lactose, and magnesium stearate should be used in newly-developed generic solid pharmaceutical formulations, since they contribute to an increased thermal stability of perindopril erbumine.

  1. Active ingredients in anti-stigma programmes in mental health.

    Science.gov (United States)

    Pinfold, Vanessa; Thornicroft, Graham; Huxley, Peter; Farmer, Paul

    2005-04-01

    This paper draws upon a review of the relevant literature and the results of the recent Mental Health Awareness in Action (MHAA) programme in England to discuss the current evidence base on the active ingredients in effective anti-stigma interventions in mental health. The MHAA Programme delivered educational interventions to 109 police officers, 78 adults from different community groups whose working lives involved supporting people with mental health problems but who had received no mental health training and 472 schools students aged 14-15. Each adult target group received two intervention sessions lasting two hours. The two school lessons were 50 minutes each. Knowledge, attitudes and behavioural intent were assessed at baseline and follow-up. In addition focus groups were held with mental health service users to explore the impact of stigma on their lives and facilitators of educational workshops were interviewed to provide expert opinion on 'what works' to reduce psychiatric stigma. Personal contact was predictive of positive changes in knowledge and attitudes for the school students but not the police officers or community adult group. The key active ingredient identified by all intervention groups and workshop facilitators were the testimonies of service users. The statements of service users (consumers) about their experience of mental health problems and of their contact with a range of services had the greatest and most lasting impact on the target audiences in terms of reducing mental health stigma.

  2. 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.

  3. 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.

  4. 77 FR 48519 - Registration Applications for Pesticide Products Containing New Active Ingredients

    Science.gov (United States)

    2012-08-14

    ... be affected. The North American Industrial Classification System (NAICS) codes have been provided to..., 235 South Kresson Street, Baltimore, MD 21224-2616. Active Ingredient: Bacillus thuringiensis...

  5. Intestinal, portal, and peripheral profiles of daikenchuto (TU-100)'s active ingredients after oral administration.

    Science.gov (United States)

    Watanabe, Junko; Kaifuchi, Noriko; Kushida, Hirotaka; Matsumoto, Takashi; Fukutake, Miwako; Nishiyama, Mitsue; Yamamoto, Masahiro; Kono, Toru

    2015-10-01

    A pharmaceutical grade Japanese traditional medicine, daikenchuto (TU-100), consisting of Japanese pepper, processed ginger, and ginseng, has been widely used for various intestinal disorders in Japan and now under development as a new therapeutic drug in the US. It is suggested that TU-100 ingredients exert pharmacological effects on intestines via two routes, from the luminal side before absorption and the peripheral blood stream after absorption. Therefore, in order to fully understand the pharmacological actions of TU-100, it is critically important to know the intraluminal amounts and forms of ingested TU-100 ingredients. In the present study, after administrating TU-100 to rats, the concentrations of TU-100 ingredients and their conjugates in the peripheral and portal blood and ileal contents were determined by LC-MS/MS. Next, TU-100 was administered to patients with ileostomy bags, but whose small intestines are diagnosed as healthy, and the ingredients/conjugates in the ileal effluent were analyzed. The results suggest that: (1) Pepper ingredients hydroxysanshools are rapidly absorbed and enter systemic circulation, (2) Ginseng ingredients ginsenosides are transported to the colon with the least absorption, (3) Ginger ingredients gingerols are absorbed and some conjugated in the small intestine and transported via the portal vein. While only a small amount of gingerols/gingerol conjugates enter systemic circulation, considerable amounts reappear in the small intestine. Thus, the effect of TU-100 on the intestines is believed to be a composite of multiple actions by multiple compounds supplied via multiple routes.

  6. 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....

  7. 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....

  8. 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,...

  9. Using Indices of Fidelity to Intervention Core Components to Identify Program Active Ingredients

    Science.gov (United States)

    Abry, Tashia; Hulleman, Chris S.; Rimm-Kaufman, Sara E.

    2015-01-01

    Identifying the active ingredients of an intervention--intervention-specific components serving as key levers of change--is crucial for unpacking the intervention black box. Measures of intervention fidelity can be used to identify specific active ingredients, yet such applications are rare. We illustrate how fidelity measures can be used to…

  10. 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

  11. Studies of beneficial interactions between active medicaments and excipients in pharmaceutical formulations.

    Science.gov (United States)

    Kalinkova, G N

    1999-09-30

    A review of "up to date" research findings leading to new concepts of the pharmaceutical formulations and their interactions has been presented. The rational approaches to the excipients choice as well as to their interactions with medicaments have been shown as a basis for modern modelling of pharmaceutical formulations. The importance of complexation, hydrogen bonding, ion-dipole, dipole-dipole and van der Waals attractions as the tools which can modify the physicochemical, pharmacological or pharmacokinetical behaviour of the medicaments has been emphasised. In vivo studies (carried out in healthy human subjects-volunteers, in beagle dogs, in rats etc.) and in vitro studies (on excised human skin, hairless mouse skin etc.) as well as studies of chemical stability and bioavailability serve also as a proof of these interactions. Therefore, excipients are important components of pharmaceutical formulations and they can take an active part in the improvement of the characteristics of formulations (but they may also reduce the effectiveness of some preparations). In this context, the so called active and inactive ingredients in pharmaceutical formulations are inexact, old and "out-of date". Their further use is only conventional. In conclusion, among the various modern techniques applied the combination of infrared spectroscopy and X-ray diffraction has been estimated as the most successful in proving the interactions between drugs and excipients. Finally, pharmaceutical formulations and their interactions have constituted a diverse and rapidly expanding field of Pharmacy (Pharmaceutical Technology, Pharmaceutical Industry and Pharmaceutical Sciences) which covers a wide range of numerical topics within an unified framework.

  12. 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.

  13. [Pharmaceutical technology: development and research].

    Science.gov (United States)

    Traisnel, M

    1994-06-01

    Production of pharmaceutics cannot be compared to the manufacture of consumer goods: pharmaceutical manufacturing is the study and bulk manufacture of the ingredients from which medicines are made, and is concerned with the mixing, preparing, packing, of the ingredients into a dosage form for the patient, in according to the good manufacturing practices (GMP). Development and manufacture are not discrete activities but links in a single chain of activity. Research and development, pharmaceutical training, regulatory requirements: these concepts are present with three ways: bioavailability, targeting and compliance.

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

    DEFF Research Database (Denmark)

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

    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 task...

  15. Selected Pharmaceuticals Entering an Estuary: Concentrations, Temporal Trends, Partitioning and Fluxes

    Science.gov (United States)

    In many coastal watersheds and ecosystems, rivers discharging to estuaries receive waters from domestic wastewater-treatment plants resulting in the release and distribution of pharmaceuticals to the marine environment. In the present study, 15 active pharmaceutical ingredients w...

  16. 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 ...

  17. 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.

  18. 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.

  19. 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...... and attached solids for the carriers) of diclofenac, ketoprofen, gemfibrozil, clofibric acid and mefenamic acid compared to the sludges. Among the target pharmaceuticals, only ibuprofen and naproxen showed similar removal rates per unit biomass for the sludges and biofilm carriers. In contrast...

  20. Direct determination of cadmium and lead in pharmaceutical ingredients using anodic stripping voltammetry in aqueous and DMSO/water solutions.

    Science.gov (United States)

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

    2015-09-17

    A new electrochemical method has been developed to detect and quantify the elemental impurities, cadmium(II) (Cd(2+)) and lead(II) (Pb(2+)), either simultaneously or individually in pharmaceutical matrices. The electro-analytical approach, involving the use of anodic stripping voltammetry (ASV) on an unmodified glassy carbon electrode, was performed in both aqueous and in a 95/5 dimethyl sulfoxide (DMSO)/water solutions, without acid digestion or dry ashing to remove organic matrices. Limits of detection (LODs) in the μg L(-1) [or parts per billion (ppb), mass/volume] range were obtained for both heavy metals - in the presence and absence of representative pharmaceutical components. To the best of our knowledge, the work demonstrates the first analysis of heavy metals in DMSO/water solutions through ASV. The strong reproducibility and stability of the sensing platform, as well as obviation of sample pretreatment show the promise of utilizing ASV as a sensitive, robust, and inexpensive alternative to inductively-coupled-plasma (ICP)-based approaches for the analysis of elemental impurities in, e.g., pharmaceutical-related matrices.

  1. 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.

  2. 21 CFR 358.710 - Active ingredients for the control of dandruff, seborrheic dermatitis, or psoriasis.

    Science.gov (United States)

    2010-04-01

    ..., seborrheic dermatitis, or psoriasis. 358.710 Section 358.710 Food and Drugs FOOD AND DRUG ADMINISTRATION... Psoriasis § 358.710 Active ingredients for the control of dandruff, seborrheic dermatitis, or psoriasis. The... psoriasis. (1) Coal tar, 0.5 to 5 percent. When a coal tar solution, derivative, or fraction is used as...

  3. Nano-microdelivery systems for oromucosal delivery of an active ingredient

    DEFF Research Database (Denmark)

    2014-01-01

    A composition for oromucosal delivery of at least one active ingredient, more particularly a lipid nano-microdelivery system comprising a nicotine component and/or a flavour component, wherein the nicotine component may be delivered to the oral cavity via absorption through the mucosal membranes...... thereof and/or wherein the flavour component may be delivered to the oral mucosa by controlled release....

  4. 78 FR 70043 - Pesticide Product Registration; Receipt of an Application for a New Active Ingredient

    Science.gov (United States)

    2013-11-22

    ... name: DAS-81419-2 Soybean. Active ingredients: Bacillus thuringiensis Cry1Ac protein expressed in soybean and Bacillus thuringiensis Cry1F protein expressed in soybean. Proposed classification/Use: Plant... list of North American Industrial Classification System (NAICS) codes is not intended to be...

  5. 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...

  6. 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.

  7. 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...

  8. 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.

  9. Review article: health benefits of some physiologically active ingredients and their suitability as yoghurt fortifiers

    OpenAIRE

    Fayed, A. E

    2014-01-01

    The article is concerned with health benefits of two main physiologically active ingredients namely, Isoflavones and γ-Aminobutyric acid, with emphasis on their fitness for fortification of yoghurt to be consumed as a functional food. Isoflavones (ISO) are part of the diphenol compounds, called “phytoestrogens,” which are structurally and functionally similar to estradiol, the human estrogen, but much less potent. Because of this similarity, ISO were suggested to have preventive effects for m...

  10. 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

  11. 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.

  12. 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.

  13. [Studies on pharmacokinetics features of characteristic active ingredients of daidai flavone extract in different physiological status].

    Science.gov (United States)

    Zeng, Ling-Jun; Chen, Dan; Zheng, Li; Lian, Yun-Fang; Cai, Wei-Wei; Huang, Qun; Lin, Yi-Li

    2014-01-01

    In order to explore the clinical hypolipidemic features of Daidai flavone extract, the pharmacokinetics features of characteristic active ingredients of Daidai flavone extract in normal and hyperlipemia rats were studied and compared. The study established the quantitative determination method of naringin and neohesperidin in plasma by UPLC-MS. Study compared the pharmacokinetics differences of naringin and noehesperidin in normal and hyperlipemia rats on the basis of establishment of hyperlipemia model. Results indicated that the pharmacokinetics features of characteristic active ingredients of Daidai flavone extract in normal and hyperlipemia rats showed significant differences. The C(max) of naringin and neohesperidin in hyperlipemia rats plasma after oral administration of Daidai flavone extract increased obviously, while t1/2, MRT and AUC0-24 h decreased, compared to normal rats. But t(max) showed no differences to that of normal rats. The results further proved Daidai flavone extract would have better hypolipidemic effect in the hyperlipemia pathological status. And the characteristic active ingredients naringin and noehesperidin were the material base of Daidai flavone extract to express the hypolipidemic effect.

  14. 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.

  15. 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.

  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. [Important application of intestinal transporters and metabolism enzymes on gastrointestinal disposal of active ingredients of Chinese materia medica].

    Science.gov (United States)

    Bi, Xiaolin; Du, Qiu; Di, Liuqing

    2010-02-01

    Oral drug bioavailability depends on gastrointestinal absorption, intestinal transporters and metabolism enzymes are the important factors in drug gastrointestinal absorption and they can also be induced or inhibited by the active ingredients of Chinese materia medica. This article presents important application of intestinal transporters and metabolism enzymes on gastrointestinal disposal of the active ingredients of Chinese materia medica, and points out the importance of research on transport and metabolism of the active ingredients of Chinese materia medica in Chinese extract and Chinese medicinal formulae.

  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

    ...), anticholinergic, antihistamine, oral antitussive, or stimulant active ingredient. (7) Dandruff/seborrheic... Mono- and di-glycerides Niacinamide Organic vegetables Pancreatin Pantothenic acid Papain Papaya... blue Natural estrogenic hormone Niacinamide Nutmeg oil (oil of nutmeg) Oil of erigeron...

  19. 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

    . 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...

  20. 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.

  1. 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.

  2. 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).

  3. 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.

    Aspergillus species, yeast and dermatophytes revealed that Cyclosporine A would be a potential compound for life threatening diseases caused by above fungi in both human and animals. Furthermore, we have reported herewith another source of Cyclosporin A...

  4. Interactions between active pharmaceutical ingredients and excipients affecting bioavailability: impact on bioequivalence.

    Science.gov (United States)

    García-Arieta, Alfredo

    2014-12-18

    The aim of the present paper is to illustrate the impact that excipients may have on the bioavailability of drugs and to review existing US-FDA, WHO and EMA regulatory guidelines on this topic. The first examples illustrate that small amounts of sorbitol (7, 50 or 60mg) affect the bioavailability of risperidone, a class I drug, oral solution, in contrast to what is stated in the US-FDA guidance. Another example suggests, in contrast to what is stated in the US-FDA BCS biowaivers guideline, that a small amount of sodium lauryl sulphate (SLS) (3.64mg) affects the bioavailability of risperidone tablets, although the reference product also includes SLS in an amount within the normal range for that type of dosage form. These factors are considered sufficient to ensure that excipients do not affect bioavailability according to the WHO guideline. The alternative criterion, defined in the WHO guideline and used in the FIP BCS biowaivers monographs, that asserts that excipients present in generic products of the ICH countries do not affect bioavailability if used in normal amounts, is shown to be incorrect with an example of alendronate (a class III drug) tablets, where 4mg of SLS increases bioavailability more than 5-fold, although a generic product in the USA contains SLS. Finally, another example illustrates that a 2mg difference in SLS may affect bioavailability of a generic product of a class II drug, even if SLS is contained in the comparator product, and in all cases its amount was within the normal range. Therefore, waivers of in vivo bioequivalence studies (e.g., BCS biowaivers, waivers of certain dosage forms in solution at the time of administration and variations in the excipient composition) should be assessed more cautiously.

  5. 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

    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...

  6. After-brush rinsing protocols, frequency of toothpaste use: fluoride and other active ingredients.

    Science.gov (United States)

    Parnell, C; O'Mullane, D

    2013-01-01

    The intra-oral retention or substantivity of active ingredients in toothpastes is important for their effectiveness, and this is influenced by product-related and user-related factors. Product-related factors include the formulation and the compatibility of active and other agents in the toothpaste and the concentration of the active ingredient. User-related factors include biological aspects such as salivary flow and salivary clearance, and behavioural aspects, such as frequency and duration of brushing, amount of toothpaste used and post-brushing rinsing behaviour. To date, product-related factors have dominated the research agenda for toothpastes, but user-related factors have the potential to significantly enhance or reduce the effectiveness of toothpaste. In this chapter, we will focus on two of the user-related factors that have been most widely studied: (1) frequency of toothbrushing and (2) post-brushing rinsing behaviour. We will then provide an overview of how evidence on these two behaviours has been used to produce guidance both for the profession and for the public, and make suggestions for the future direction of research in this area.

  7. Identification of the main active ingredients of agrochemicals used around the Lake of Tota, Colombia

    Directory of Open Access Journals (Sweden)

    Wilson Javier Pérez-Holguín

    2016-01-01

    Full Text Available This paper presents a descriptive study aimed at identifying the main active ingredients, frequency of use, and the processes employed in the application of the agrochemicals most used around the Lake of Tota, which is considered the most important freshwater ecosystem in Colombia. A key source for this study is a survey to farmers, which sampling frame was established from a Geographical Institute Agustin Codazzi (IGAC digital map, considering only the plots with some agricultural activity and runoff into the lake. This information was supplemented with geographic data obtained from Google Maps®. As control mechanism, two additional sources were used: i a manual count of packaging of agrochemicals in a certified collection center, and ii a census of stores that supply such products in the study area. The results allow knowing the set of agrochemicals most used around the lake, their active ingredients, and the most common farming practices, some of which could entail some risk to farmers, consumers and the environment.

  8. 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.

  9. 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.

  10. 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.

  11. Pharmaceutical Cocrystals: Regulatory and Strategic Aspects, Design and Development

    Science.gov (United States)

    Gadade, Dipak Dilip; Pekamwar, Sanjay Sudhakar

    2016-01-01

    Cocrystal is a concept of the supramolecular chemistry which is gaining the extensive interest of researchers from pharmaceutical and chemical sciences and of drug regulatory agencies. The prominent reason of which is its ability to modify physicochemical properties of active pharmaceutical ingredients. During the development of the pharmaceutical product, formulators have to optimize the physicochemical properties of active pharmaceutical ingredients. Pharmaceutical cocrystals can be employed to improve vital physicochemical characteristics of a drug, including solubility, dissolution, bioavailability and stability of pharmaceutical compounds while maintaining its therapeutic activity. It is advantageous being a green synthesis approach for production of pharmaceutical compounds. The formation polymorphic forms, solvates, hydrates and salts of cocrystals during the synthesis reported in the literature which can be a potential issue in the development of pharmaceutical cocrystals. The approaches like hydrogen bonding rules, solubility parameters, screening through the CSD database or thermodynamic characteristics can be utilized for the rational design of cocrystals and selection of coformers for synthesis multi-component cocrystals. Considering the significance of pharmaceutical cocrystals pharmaceutical regulatory authorities in the United States and Europe issued guidance documents which may be helpful for pharmaceutical product registration in these regions. In this article, we deal with the design, synthesis, strategic aspects and characteristics of cocrystals along perspectives on its regulatory and intellectual property considerations.

  12. 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%.

  13. 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.

  14. Review article: health benefits of some physiologically active ingredients and their suitability as yoghurt fortifiers.

    Science.gov (United States)

    Fayed, A E

    2015-05-01

    The article is concerned with health benefits of two main physiologically active ingredients namely, Isoflavones and γ-Aminobutyric acid, with emphasis on their fitness for fortification of yoghurt to be consumed as a functional food. Isoflavones (ISO) are part of the diphenol compounds, called "phytoestrogens," which are structurally and functionally similar to estradiol, the human estrogen, but much less potent. Because of this similarity, ISO were suggested to have preventive effects for many kinds of hormone-dependent diseases. In nature, ISO usually occur as glycosides and, once deconjugated by the intestinal microflora, the ISO can be absorbed into the blood. At present, it seems convincing their possible protective actions against various cancers, osteoporosis and menopausal symptoms and high levels of blood cholesterol as well as the epidemiological evidence. Γ-Aminobutyric acid (GABA), it is an amino acid that has long been reported to lower blood pressure by intravenous administration in experimental animals and in human subjects. GABA is present in many vegetables and fruits but not in dairy products. GABA was reported to lower blood pressure in people with mild hypertension. It was suggested that low-dose oral GABA has a hypotensive effect in spontaneously hypertensive. Yoghurt beyond its ability to be probiotic food via its culturing with the gut strains, it could further carry more healthy benefits when it was fortified with physiological active ingredients, especially GABA versus ISO preferring, whether, bacteriologically or biochemically, a fortification level of 50 mg ISO/kg or 200 mg GABA/kg.

  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. [Amorphization in pharmaceutical technology].

    Science.gov (United States)

    Révész, Piroska; Laczkovich, Orsolya; Eros, István

    2004-01-01

    The amorphization of crystalline active ingredients may be necessary because of the polymorphism of the active substance, the poor water-solubility of the drug material, difficult processing in the crystalline form and the taking out of a patent for a new (amorphous) form. This article introduces protocols for amorphization, which use methods traditionally applied in pharmaceutical technology. The protocols involve three possible routes: solvent methods, hot-melt technologies and milling procedures. With this presentation, the authors suggest help for practising experts to find the correct amorphization method.

  17. Gallic Acid, the Active Ingredient of Terminalia bellirica, Enhances Adipocyte Differentiation and Adiponectin Secretion.

    Science.gov (United States)

    Makihara, Hiroko; Koike, Yuka; Ohta, Masatomi; Horiguchi-Babamoto, Emi; Tsubata, Masahito; Kinoshita, Kaoru; Akase, Tomoko; Goshima, Yoshio; Aburada, Masaki; Shimada, Tsutomu

    2016-01-01

    Visceral obesity induces the onset of metabolic disorders such as insulin resistance and diabetes mellitus. Adipose tissue is considered as a potential pharmacological target for treating metabolic disorders. The fruit of Terminalia bellirica is extensively used in Ayurvedic medicine to treat patients with diseases such as diabetes mellitus. We previously investigated the effects of a hot water extract of T. bellirica fruit (TB) on obesity and insulin resistance in spontaneously obese type 2 diabetic mice. To determine the active ingredients of TB and their molecular mechanisms, we focused on adipocyte differentiation using mouse 3T3-L1 cells, which are widely used to study adipocyte physiology. We show here that TB enhanced the differentiation of 3T3-L1 cells to mature adipocytes and that one of the active main components was identified as gallic acid. Gallic acid (10-30 µM) enhanced the expression and secretion of adiponectin via adipocyte differentiation and also that of fatty acid binding protein-4, which is the target of peroxisome proliferator-activated receptor gamma (PPARγ), although it does not alter the expression of the upstream genes PPARγ and CCAAT enhancer binding protein alpha. In the PPARγ ligand assay, the binding of gallic acid to PPARγ was undetectable. These findings indicate that gallic acid mediates the therapeutic effects of TB on metabolic disorders by regulating adipocyte differentiation. Therefore, TB shows promise as a candidate for preventing and treating patients with metabolic syndrome.

  18. 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.

  19. Approaches for predicting effects of unintended environmental exposure to an endocrine active pharmaceutical, tamoxifen

    Science.gov (United States)

    Tamoxifen is an endocrine-active pharmaceutical (EAP) that is used world-wide. Because tamoxifen is a ubiquitous pharmaceutical and interacts with estrogen receptors, a case study was conducted with this compound to (1) determine effects on reproductive endpoints in a nontarget s...

  20. 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.

  1. 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)

  2. Active Ingredients of Instructional Coaching: Developing a Conceptual Framework. R2Ed Working Paper 2015-3

    Science.gov (United States)

    White, Andrew S.; Howell Smith, Michelle; Kunz, Gina M.; Nugent, Gwen C.

    2015-01-01

    Although researchers have explored the impact of instructional coaching and named possible elements believed essential to effective coaching, there has yet to emerge from the literature a coherent model of those essential elements ("active ingredients"). This qualitative study sought to identify those elements through a systematic…

  3. 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.

  4. 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.

  5. 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.

  6. Understanding real-world implementation quality and "active ingredients" of PBIS.

    Science.gov (United States)

    Molloy, Lauren E; Moore, Julia E; Trail, Jessica; Van Epps, John James; Hopfer, Suellen

    2013-12-01

    Programs delivered in the "real world" often look substantially different from what was originally intended by program developers. Depending on which components of a program are being trimmed or altered, such modifications may seriously undermine the effectiveness of a program. In the present study, these issues are explored within a widely used school-based, non-curricular intervention, Positive Behavioral Intervention and Supports. The present study takes advantage of a uniquely large dataset to gain a better understanding of the "real-world" implementation quality of PBIS and to take a first step toward identifying the components of PBIS that "matter most" for student outcomes. Data from 27,689 students and 166 public primary and secondary schools across seven states included school and student demographics, indices of PBIS implementation quality, and reports of problem behaviors for any student who received an office discipline referral during the 2007-2008 school year. Results of the present study identify three key components of PBIS that many schools are failing to implement properly, three program components that were most related to lower rates of problem behavior (i.e., three "active ingredients" of PBIS), and several school characteristics that help to account for differences across schools in the quality of PBIS implementation. Overall, findings highlight the importance of assessing implementation quality in "real-world" settings, and the need to continue improving understanding of how and why programs work. Findings are discussed in terms of their implications for policy.

  7. Capturing the Active Ingredients of Multicomponent Participatory Organizational Stress Interventions Using an Adapted Study Design.

    Science.gov (United States)

    Biron, Caroline; Ivers, Hans; Brun, Jean-Pierre

    2016-10-01

    Adapted study designs use process evaluation to incorporate a measure of intervention exposure and create an artificial control and intervention groups. Taking into account exposure levels to interventions combines process and outcome evaluation and strengthens the design of the study when exposure levels cannot be controlled. This study includes longitudinal data (two assessments) with added process measures at time 2 gathered from three complex participatory intervention projects in Canada in a hospital and a university. Structural equation modelling was used to explore the specific working mechanisms of particular interventions on stress outcomes. Results showed that higher exposure to interventions aiming to modify tasks and working conditions reduced demands and improved social support, but not job control, which in turn, reduced psychological distress. Exposure to interventions aiming to improve relationships was not related to psychosocial risks. Most studies cannot explain how interventions produce their effects on outcomes, especially when there are multiple concurrent interventions delivered in several contexts. This study advances knowledge on process evaluation by using an adapted study design to capture the active ingredients of multicomponent interventions and suggesting some mechanisms by which the interventions produce their effects on stress outcomes. It provides an illustration of how to conduct process evaluation and relate exposure levels to observed outcomes. Copyright © 2016 John Wiley & Sons, Ltd.

  8. 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...

  9. The adsorption of pharmaceutically active compounds from aqueous solutions onto activated carbons.

    Science.gov (United States)

    Rakić, Vesna; Rac, Vladislav; Krmar, Marija; Otman, Otman; Auroux, Aline

    2015-01-23

    In this study, the adsorption of pharmaceutically active compounds - salicylic acid, acetylsalicylic acid, atenolol and diclofenac-Na onto activated carbons has been studied. Three different commercial activated carbons, possessing ∼650, 900 or 1500m(2)g(-1) surface areas were used as solid adsorbents. These materials were fully characterized - their textural, surface features and points of zero charge have been determined. The adsorption was studied from aqueous solutions at 303K using batch adsorption experiments and titration microcalorimetry, which was employed in order to obtain the heats evolved as a result of adsorption. The maximal adsorption capacities of investigated solids for all target pharmaceuticals are in the range of 10(-4)molg(-1). The obtained maximal retention capacities are correlated with the textural properties of applied activated carbon. The roles of acid/base features of activated carbons and of molecular structures of adsorbate molecules have been discussed. The obtained results enabled to estimate the possibility to use the activated carbons in the removal of pharmaceuticals by adsorption.

  10. 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.

  11. A Comprehensive and System Review for the Pharmacological Mechanism of Action of Rhein, an Active Anthraquinone Ingredient

    OpenAIRE

    Hao Sun; Guangwen Luo; Dahui Chen; Zheng Xiang

    2016-01-01

    AbstractRhein is a major medicinal ingredient isolated from several traditional Chinese medicines, including Rheum palmatum L., Aloe barbadensis Miller, Cassia angustifolia Vahl., and Polygonum multiflorum Thunb. Rhein has various pharmacological activities, such as anti-inflammatory, antitumor, antioxidant, antifibrosis, hepatoprotective, and nephroprotective activities. Although more than 100 articles in PubMed are involved in the pharmacological mechanism of action of rhein, only a few foc...

  12. 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...

  13. 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...

  14. MICROWAVE-ASSISTED GREENER SYNTHESIS OF PHARMACEUTICALLY ACTIVE HETEROCYCLES UNDER BENIGN CONDITIONS

    Science.gov (United States)

    Green chemistry is a rapidly developing new field that provides us a proactive avenue for the sustainable development of future science and technologies. Environmentally benign protocols have been developed for the synthesis of various pharmaceutically active heterocycles namely ...

  15. PHARMACEUTICAL AND PERSONAL CARE PRODUCTS AS UBIQUITOUS POLLUTANTS FROM PERSONAL USE AND ACTIVITIES

    Science.gov (United States)

    Perhaps more so than with any other class of pollutants, the occurrence of pharmaceuticals and personal care products (PPCPS) in the environment highlights the immediate, intimate, and inseparable connection between the individual activities of consumers and their environment. In...

  16. The Active Ingredients of Jiang-Zhi-Ning: Study of the Nelumbo nucifera Alkaloids and Their Main Bioactive Metabolites

    Directory of Open Access Journals (Sweden)

    Wei Wang

    2012-08-01

    Full Text Available The object of this study was to identify the major active ingredients of the Chinese Traditional Medicine Jiang-Zhi-Ning (JZN based on the high performance liquid chromatography (HPLC profiles of plasma samples obtained from beagle dogs at different times after intragastric administration of JZN, crude JZN extracts, different extracted fractions, different subfractions of the active fraction and different isolated ingredients. 2-Hydroxy-1-methoxyaporphin (2H1M, an alkaloid from Nelumbo nucifera, one of the herbs that make up JZN, was identified as the constituent showing the major pharmacodynamic effect. The major metabolites of 2H1M were analyzed and identified as N-demethyl-2-hydroxy-1-methoxyaporphine-2-O-glycuronic acid, 2-hydroxy-1-methoxy-aporphine-2-O-glycuronic acid and 2-hydroxy-1-methoxy-aporphine-2-O-sulphate. This study provided a comprehensive insight into the active components of JZN.

  17. 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.

  18. 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.

  19. Mathematical Modeling of the Release of Active Ingredients from a Contraceptive Patch: Ortho Evra® as a Case Study

    OpenAIRE

    Trujillo-de Santiago, Grissel; Patricio Sáenz-Collins, Carlos; García-Arellano, Lizette; Moisés Álvarez, Mario

    2014-01-01

    Contraceptive patches have become a frequently used contraceptive method. We present a mathematical model that describes the serum concentration profiles of Norelgestromin (NGMN) and Ethinylestradiol (EE) released from the contraceptive patch Ortho Evra®. We propose a simple one-compartment model based on pharmacokinetics data reported in previous studies. The model assumes a time-dependent release rate and a first order elimination rate for each of the active ingredients contained in the pat...

  20. 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.

  1. Analysis of molecular interactions in solid dosage forms; challenge to molecular pharmaceutics.

    Science.gov (United States)

    Yamamoto, Keiji; Limwikrant, Waree; Moribe, Kunikazu

    2011-01-01

    The molecular states of active pharmaceutical ingredients (APIs) in pharmaceutical dosage forms strongly affect the properties and quality of a drug. Various important fundamental physicochemical studies were reviewed from the standpoint of molecular pharmaceutics. Mechanochemical effects were evaluated in mixtures of APIs and pharmaceutical additives. Amorphization, complex formation and nanoparticle formation are observed after grinding process depending on the combination of APIs and pharmaceutical additives. Sealed-heating method and mesoporous materials have been used to investigate drug molecular interactions in dosage forms. Molecular states have been investigated using powder X-ray diffraction, thermal analysis, IR, solid state fluorometry, and NMR.

  2. 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

  3. 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.

  4. 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.

  5. 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

  6. Artepillin C, a major ingredient of Brazilian propolis, induces a pungent taste by activating TRPA1 channels.

    Directory of Open Access Journals (Sweden)

    Taketoshi Hata

    Full Text Available Brazilian green propolis is a popular health supplement because of its various biological properties. The ethanol extract of Brazilian green propolis (EEBP is characteristic for its herb-like smell and unique pungent taste. However, the ingredients responsible for its pungency have not yet been identified. This study provides the first evidence that artepillin C is the main pungent ingredient in EEBP and that it potently activates human transient receptor potential ankyrin 1 (TRPA1 channels. EEBP was fractionated using column chromatography with a step gradient elution of an ethanol-water solution, and the fractions having the pungent taste were determined by sensory tests. HPLC analysis revealed that the pungent fraction was composed primarily of artepillin C, a prenylated derivative of cinnamic acid. Artepillin C was also identified as the pungent compound of EEBP by organoleptic examiners. Furthermore, the effects of artepillin C and other cinnamic acids found in EEBP on TRPA1 channels were examined by calcium imaging and plate reader-based assays in human TRPA1-expressing cells to investigate the molecular mechanisms underlying their pungent tastes. Artepillin C and baccharin activated the TRPA1 channel strongly, whereas drupanin caused a slight activation and p-coumaric acid showed no activation. Because the EC(50 values of artepillin C, baccharin, and allyl isothiocyanate were 1.8 µM, 15.5 µM, and 6.2 µM, respectively, artepillin C was more potent than the typical TRPA1 agonist allyl isothiocyanate. These findings strongly indicate that artepillin C is the main pungent ingredient in EEBP and stimulates a pungent taste by activating TRPA1 channels.

  7. 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

  8. 2010年登记或上市农药品种%New Active Ingredients Registered or Launched in 2010

    Institute of Scientific and Technical Information of China (English)

    杨吉春; 吴峤; 李学建; 刘长令

    2011-01-01

    概述了2010年登记或上市的36个新农药品种,其中杀菌剂11个、杀虫剂4个、除草剂10个、熏蒸剂2个、杀线虫剂1个、生物农药和信息素8个.%A review of 36 new active ingredients registered or launched in 2010, in which there are 11 with fungicidal activity, 4 with insecticidal activity and acaricide, 10 with herbicidal activity, 2 with fumigation activity, 1 with nematicidal activity, 8 as biopesticides and pheromones.

  9. 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…

  10. 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.

  11. Corporate colonization of health activism? Irish health advocacy organizations' modes of engagement with pharmaceutical corporations.

    Science.gov (United States)

    O'Donovan, Orla

    2007-01-01

    This article is based on a study that aimed to shed light on the "cultures of action" of Irish health advocacy organizations, and particularly their modes of engagement with pharmaceutical corporations. Debates about what some interpret as the "corporate colonization" of health activism provide the backdrop for the analysis. The empirical dimension of the study involved a survey of 112 organizations and in-depth study of a small number of organizations that manifest diverse modes of engagement with the pharmaceutical industry. The varying modes of interaction are plotted along a continuum and characterized as corporatist, cautious cooperation, and confrontational. Evidence is presented of a strong and growing cultural tendency in Irish health advocacy organizations to frame pharmaceutical corporations as allies in their quests for better health. The analysis of four constitutive dimensions of organizations' cultures of action can reveal the legitimating logics underlying their diverging positions around pharmaceutical industry sponsorship. While the research shows that pharmaceutical corporations have largely succeeded in defining themselves as a philanthropic force and rightful players in Irish health activism, it cautions against a simplistic conclusion that this is evidence of corporate colonization.

  12. 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.

  13. Physio-chemical Investigation and Natural Bond Orbital Analysis of the Most Actives Ingredient of Fennel Plant

    Directory of Open Access Journals (Sweden)

    Mansoureh Pishehabadi

    2016-10-01

    Full Text Available In this study, physio-chemical properties of effective compounds of fennel plant were investigated through using computational chemistry. To do this, trans-anethole, estragole, 3'- hydroxyanethole and 4- methoxycinnamyl alcohol compounds that the most active ingredient combinations make up the fennel plant have been carried out at three different levels of HF, BLYP and B3LYP theories using 6-31G*, 6-311G*, 6-311G**, 6-311+G and 6-311++G basis sets. Additionally, ab initio calculation in the gas phase have been studied and physio-chemical parameters including Gibbs free energy, thermal energy, enthalpy, entropy, and thermal capacity in constant volume (CV of these compounds have been computed as well as Gibbs free energy in polar solvents such as ethanol and methanol and water. Based on these obtained data the structural stabilities of these flavorful compounds have been discussed. However, in these herbal effective compounds presented here the natural bond orbital (NBO analysis has been performed which seemed quite informative to show some important atomic and structural features. The result lead to the issue that all those compounds in polar solvents, particularly alcoholic solvents solved and the compounds can be used sufficiently to extract the active ingredients of herb fennel.

  14. A Unique Combination of Nutritionally Active Ingredients Can Prevent Several Key Processes Associated with Atherosclerosis In Vitro.

    Directory of Open Access Journals (Sweden)

    Joe W E Moss

    Full Text Available Atherosclerosis is the underlying cause of cardiovascular disease that leads to more global mortalities each year than any other ailment. Consumption of active food ingredients such as phytosterols, omega-3 polyunsaturated fatty acids and flavanols are known to impart beneficial effects on cardiovascular disease although the combined actions of such agents in atherosclerosis is poorly understood. The aim of this study was to screen a nutritional supplement containing each of these active components for its anti-atherosclerotic effect on macrophages in vitro.The supplement attenuated the expression of intercellular adhesion molecule-1 and macrophage chemoattractant protein-1 in human and murine macrophages at physiologically relevant doses. The migratory capacity of human monocytes was also hindered, possibly mediated by eicosapentaenoic acid and catechin, while the ability of foam cells to efflux cholesterol was improved. The polarisation of murine macrophages towards a pro-inflammatory phenotype was also attenuated by the supplement.The formulation was able to hinder multiple key steps of atherosclerosis development in vitro by inhibiting monocyte recruitment, foam cell formation and macrophage polarisation towards an inflammatory phenotype. This is the first time a combination these ingredients has been shown to elicit such effects and supports its further study in preclinical in vivo models.

  15. 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.

  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

    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. HybasTM is a hyb...

  17. Pharmaceutically active ionic liquids with solids handling, enhanced thermal stability, and fast release

    DEFF Research Database (Denmark)

    Bica, Katharina; Rodríguez, Héctor; Gurau, Gabriela

    2012-01-01

    Pharmaceutically active compounds in ionic liquid form immobilized onto mesoporous silica are stable, easily handled solids, with fast and complete release from the carrier material when placed into an aqueous environment. Depending on specific ion-surface interactions, they may also exhibit...

  18. 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.

  19. Cichorium intybus root extract: A "vitamin D-like" active ingredient to improve skin barrier function.

    Science.gov (United States)

    Maia Campos, P M B G; G Mercurio, D; O Melo, M; Closs-Gonthier, B

    2017-02-01

    During the aging process, the human skin suffers many alterations including dryness, skin barrier function damage. The skin barrier function is important to the prevention of skin alterations and maintenance of homeostasis. So, the objective of this study was to assess the clinical efficacy on skin barrier function of Cichorium intybus root extract in cosmetic formulations with or without UV filters. Fifty women, aged between 45 and 60 years, were divided into two groups. One group received vehicle formulations containing UV filters, and the other group received formulations without UV filters. Both groups received a formulation containing the extract and the vehicle. The formulations were applied twice daily to the upper arms after washing with sodium lauryl sulphate. Transepidermal water loss (TEWL) and skin microrelief were evaluated before and after a 14- and 28-day period of treatment. The control regions and regions where the vehicles were applied showed an increase in the TEWL. For the formulations containing the extract, decreased TEWL and improved microrelief were observed when compared to the vehicle and control areas after a 28-day period. In conclusion, Cichorium intybus root extract showed protective and restructuring effects on the skin and stands out as an innovative ingredient to improve skin barrier function.

  20. 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

    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. HybasTM is a hyb......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...... 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......, the measured removal rates 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 could be attributed to de-conjugation or formation from other metabolites....

  1. 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.

  2. 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.

  3. Identification, characterization and quantification of a new impurity in deferasirox active pharmaceutical ingredient by LC-ESI-QT/MS/MS.

    Science.gov (United States)

    Thomas, Saji; Chandra Joshi, Subhash; Vir, Dharam; Agarwal, Ashutosh; Rao, Raghavendra Desai; Sridhar, I; Xavier, Cijo M; Mathela, Chandra S

    2012-04-07

    An unknown impurity was detected in deferasirox drug substance by a newly developed high performance liquid chromatography (HPLC) method. The unknown impurity was identified by liquid chromatography-tandem mass spectrometry using electrospray ionization source and Q-trap mass analyzer (LC-ESI-QT/MS/MS). Based on LC-MS/MS data and knowledge of the synthetic scheme of deferasirox, this impurity was proposed as the regio-isomer of deferasirox. Structural confirmation of this impurity was unambiguously carried out by synthesis followed by characterization using nuclear magnetic resonance (NMR), infrared spectroscopy (IR), mass spectrometry, elemental analysis (EA) and the impurity was confirmed as 2-[3,5-bis(2-hydroxy-phenyl)-[1,2,4]-triazol-1-yl]-benzoic acid (Imp-1). The newly developed method was validated according to ICH guidelines. The resolution between Imp-1 and deferasirox was found to be more than 6.0 and the detection limit of impurities was in the range of 0.0005-0.01%, indicating high selectivity and sensitivity of the newly developed method.

  4. A novel application of α-glucosyl hesperidin for nanoparticle formation of active pharmaceutical ingredients by dry grinding.

    Science.gov (United States)

    Tozuka, Yuichi; Imono, Masaaki; Uchiyama, Hiromasa; Takeuchi, Hirofumi

    2011-11-01

    The effectiveness of α-glucosyl hesperidin (Hsp-G) as a novel grinding aid for the preparation of drug nanoparticles by dry grinding was investigated. Poorly water-soluble drugs and Hsp-G were mixed at a weight ratio of 1/5 and ground for 60 min by a vibrational ball mill. It was evident that all poorly water-soluble drugs used in this study formed nanoparticles after the ground mixtures were dispersed into distilled water. The dissolution profile of glibenclamide from the ground mixtures of glibenclamide/Hsp-G showed dramatic improvement from that of untreated drug crystals. Administration of the ground mixture of glibenclamide/Hsp-G to rats resulted in a significantly higher rate of decrease in blood glucose levels than that of untreated glibenclamide. The area above the time-curve of plasma-glucose concentrations using the ground mixture of glibenclamide/Hsp-G was 6-fold higher than that using untreated glibenclamide. The improved dissolution rate due to nanoparticle formation of glibenclamide, induced by co-grinding with Hsp-G, was responsible for this improvement.

  5. 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

  6. 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.

  7. 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.

  8. Validation of an in-line Raman spectroscopic method for continuous active pharmaceutical ingredient quantification during pharmaceutical hot-melt extrusion.

    Science.gov (United States)

    Saerens, L; Segher, N; Vervaet, C; Remon, J P; De Beer, T

    2014-01-02

    A calibration model for in-line API determination was developed based on Raman spectra collected during hot-melt extrusion. This predictive model was validated by calculating the accuracy profile based on the analysis results of validation experiments. Furthermore, based on the data of the accuracy profile, the measurement uncertainty was determined. Finally, the robustness of the model was evaluated. A Raman probe was implemented in the die of a twin-screw extruder, to monitor the drug concentration during extrusion of physical mixtures containing 15, 20, 25, 30 and 35% (w/w) metoprolol tartrate (MPT) in Eudragit(®) RS PO, an amorphous copolymer of acrylic and methacrylic acid esters with a low content of quaternary ammonium groups, which are present as salts. Several different calibration models for the prediction of the MPT content were developed, based on the use of single spectra or averaged spectra, and using partial least squares (PLS) regression or multivariate curve resolution (MCR). These predictive models were validated by extruding and monitoring mixtures containing 17.5, 22.5, 25.0, 27.5 and 32.5% (w/w) MPT. Each validated concentration was monitored on three different days, by two different operators. The β-expectation tolerance intervals were calculated for each model and for each of the validated MPT concentration levels (β was set at 95%), and acceptance limits were set at 10% (relative bias), indicating that at least 95% of future measurements should not deviate more than 10% from the true value. The only model where these acceptance limits were not exceeded was the MCR model based on averaged Raman spectra. The uncertainty measurements for this model showed that the unknown true value can be found at a maximum of ±7.00% around the measured result, with a confidence level of 95%. The robustness of this model was evaluated via an experimental design varying throughput, screw speed and barrel temperature. The robustness designs showed no significant influence of any of the process settings on the predicted concentration values. Raman spectroscopy proved to be a fast, non-destructive and reliable method for the quantification of MPT during hot-melt extrusion. From the accuracy profile of the MCR model based on averaged spectra, it was concluded that for each MPT concentration in the validated concentration range, 95 out 100 future routine measurements will be included within the acceptance limits (10%).

  9. [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

  10. 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.

  11. [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.

  12. 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.

  13. 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.

  14. 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.

  15. A Comprehensive and System Review for the Pharmacological Mechanism of Action of Rhein, an Active Anthraquinone Ingredient.

    Science.gov (United States)

    Sun, Hao; Luo, Guangwen; Chen, Dahui; Xiang, Zheng

    2016-01-01

    Rhein is a major medicinal ingredient isolated from several traditional Chinese medicines, including Rheum palmatum L., Aloe barbadensis Miller, Cassia angustifolia Vahl., and Polygonum multiflorum Thunb. Rhein has various pharmacological activities, such as anti-inflammatory, antitumor, antioxidant, antifibrosis, hepatoprotective, and nephroprotective activities. Although more than 100 articles in PubMed are involved in the pharmacological mechanism of action of rhein, only a few focus on the relationship of crosstalk among multiple pharmacological mechanisms. The mechanism of rhein involves multiple pathways which contain close interactions. From the overall perspective, the pathways which are related to the targets of rhein, are initiated by the membrane receptor. Then, MAPK and PI3K-AKT parallel signaling pathways are activated, and several downstream pathways are affected, thereby eventually regulating cell cycle and apoptosis. The therapeutic effect of rhein, as a multitarget molecule, is the synergistic and comprehensive result of the involvement of multiple pathways rather than the blocking or activation of a single signaling pathway. We review the pharmacological mechanisms of action of rhein by consulting literature published in the last 100 years in PubMed. We then summarize these pharmacological mechanisms from a comprehensive, interactive, and crosstalk perspective. In general, the molecular mechanism of action of drug must be understood from a systematic and holistic perspective, which can provide a theoretical basis for precise treatment and rational drug use.

  16. Lack of sustained efficacy for alcohol-based surgical hand rubs containing 'residual active ingredients' according to EN 12791.

    Science.gov (United States)

    Kampf, G; Kramer, A; Suchomel, M

    2017-02-01

    The World Health Organization recommends the use of hand rubs with 'sustained activity' for surgical hand preparation. This review aims to verify whether any of the alcohol-based hand rubs containing non-volatile 'active ingredients' such as chlorhexidine digluconate (CHG), mecetronium ethylsulphate (MES), or ortho-phenylphenol (OPP) provides such sustained efficacy for surgical hand disinfection. Literature was searched to find studies according to EN 12791. Published data sets were analysed to verify whether any of the formulations has a superior efficacy (Phand rub with 0.1% OPP in 78.2% ethanol was also not superior to the reference treatment when applied as recommended for 1.5min. It appears reasonable and responsible to limit the dermal exposure and environmental input to biocidal agents with a clear benefit such as the alcohols. In analogy to avoiding dyes and fragrances in hand rubs, formulations containing 'active' substances without a clear benefit but with potential risks should be avoided when alternative formulations with the same level of antimicrobial activity, dermal tolerance, and user acceptability are available.

  17. Bactericidal active ingredient in cryopreserved plasma-treated water with the reduced-pH method for plasma disinfection

    Science.gov (United States)

    Kitano, Katsuhisa; Ikawa, Satoshi; Nakashima, Yoichi; Tani, Atsushi; Yokoyama, Takashi; Ohshima, Tomoko

    2016-09-01

    For the plasma disinfection of human body, plasma sterilization in liquid is crucial. We found that the plasma-treated water (PTW) has strong bactericidal activity under low pH condition. Physicochemical properties of PTW is discussed based on chemical kinetics. Lower temperature brings longer half-life and the bactericidal activity of PTW can be kept by cryopreservation. High performance PTW, corresponding to the disinfection power of 22 log reduction (B. subtilis spore), can be obtained by special plasma system equipped with cooling device. This is equivalent to 65% H2O2, 14% sodium hypochlorite and 0.33% peracetic acid, which are deadly poison for human. But, it is deactivated soon at higher temperature (4 sec. at body temperature), and toxicity to human body seems low. For dental application, PTW was effective on infected models of human extracted tooth. Although PTW has many chemical components, respective chemical components in PTW were isolated by ion chromatography. In addition to peaks of H2O2, NO2- and NO3-, a specific peak was detected. and only this fraction had bactericidal activity. Purified active ingredient of PTW is the precursor of HOO, and further details will be discussed in the presentation. MEXT (15H03583, 23340176, 25108505). NCCE (23-A-15).

  18. A Comprehensive and System Review for the Pharmacological Mechanism of Action of Rhein, an Active Anthraquinone Ingredient

    Directory of Open Access Journals (Sweden)

    Hao Sun

    2016-08-01

    Full Text Available AbstractRhein is a major medicinal ingredient isolated from several traditional Chinese medicines, including Rheum palmatum L., Aloe barbadensis Miller, Cassia angustifolia Vahl., and Polygonum multiflorum Thunb. Rhein has various pharmacological activities, such as anti-inflammatory, antitumor, antioxidant, antifibrosis, hepatoprotective, and nephroprotective activities. Although more than 100 articles in PubMed are involved in the pharmacological mechanism of action of rhein, only a few focus on the relationship of crosstalk among multiple pharmacological mechanisms. The mechanism of rhein involves multiple pathways which contain close interactions. From the overall perspective, the pathways which are related to the targets of rhein, are initiated by the membrane receptor. Then, MAPK and PI3K-AKT parallel signaling pathways are activated, and several downstream pathways are affected, thereby eventually regulating cell cycle and apoptosis. The therapeutic effect of rhein, as a multitarget molecule, is the synergistic and comprehensive result of the involvement of multiple pathways rather than the blocking or activation of a single signaling pathway. We review the pharmacological mechanisms of action of rhein by consulting literature published in the last 100 years in PubMed. We then summarize these pharmacological mechanisms from a comprehensive, interactive, and crosstalk perspective. In general, the molecular mechanism of action of drug must be understood from a systematic and holistic perspective, which can provide a theoretical basis for precise treatment and rational drug use.

  19. 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.

  20. Quantitative structure property relationships for the adsorption of pharmaceuticals onto activated carbon.

    Science.gov (United States)

    Dickenson, E R V; Drewes, J E

    2010-01-01

    Isotherms were determined for the adsorption of five pharmaceutical residues, primidone, carbamazepine, ibuprofen, naproxen and diclofenac, to Calgon Filtrasorb 300 powdered activated carbon (PAC). The sorption behavior was examined in ultra-pure and wastewater effluent organic matter (EfOM) matrices, where more sorption was observed in the ultra-pure water for PAC doses greater than 10 mg/L suggesting the presence of EfOM hinders the sorption of the pharmaceuticals to the PAC. Adsorption behaviors were described by the Freundlich isotherm model. Quantitative structure property relationships (QSPRs) in the form of polyparameter linear solvation energy relationships were developed for simulating the Freundlich adsorption capacity in both ultra-pure and EfOM matrices. The significant 3D-based descriptors for the QSPRs were the molar volume, polarizability and hydrogen-bond donor parameters.

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

    OpenAIRE

    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...

  2. 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…

  3. 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…

  4. The hallucinogenic herb Salvia divinorum and its active ingredient salvinorin A reduce inflammation-induced hypermotility in mice.

    Science.gov (United States)

    Capasso, R; Borrelli, F; Zjawiony, J; Kutrzeba, L; Aviello, G; Sarnelli, G; Capasso, F; Izzo, A A

    2008-02-01

    The hallucinogenic plant Salvia divinorum has been used for medical treatments of gastrointestinal disorders. Here, we evaluated the effect of a standardized extract from the leaves of Salvia divinorum (SDE) and of its active ingredient salvinorin A on motility in vivo, both in physiological states and during croton oil-induced intestinal inflammation. SDE (1-100 mg kg(-1)) significantly inhibited motility only in inflamed, but not in control, mice. In control mice, salvinorin A (0.01-10 mg kg(-1)) significantly inhibited motility only at the highest doses tested (3 and 10 mg kg(-1)) and this effect was not counteracted by naloxone or by the kappa-opioid receptor (KOR) antagonist nor-binaltorphimine. Inflammation significantly increased the potency of salvinorin A (but not of the KOR agonist U-50488) in reducing motility. The inhibitory effects of both salvinorin A and U-50488 in inflamed mice were counteracted by naloxone or by nor-binaltorphimine. We conclude that salvinorin A may reduce motility through activation of different targets. In physiological states, salvinorin A, at high doses, inhibited motility through a non-KOR mediated mechanism. Gut inflammation increased the potency of salvinorin A; this effect was mediated by KOR, but it was not shared by U-50488, thus suggesting that salvinorin A may have target(s) other than KOR in the inflamed gut.

  5. 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.

  6. 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.

  7. 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.

  8. 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.

  9. Use of Active Ingredient Information for Low Socioeconomic Status Parents’ Decision-making Regarding Cough and Cold Medications: Role of Health Literacy

    Science.gov (United States)

    Yin, H. Shonna; Mendelsohn, Alan L.; Nagin, Perry; van Schaick, Linda; Cerra, Maria E.; Dreyer, Benard P.

    2013-01-01

    OBJECTIVE Parent administration of multiple medications with overlapping active ingredients places children at risk for overdose. We sought to examine how parents use active ingredient information as part of the process of selecting a cough/cold medication for their child, and how health literacy plays a role. METHODS Experimental study of parents of children presenting for care in an urban public hospital pediatric clinic. Parents were asked to determine which of 3 cough/cold medications could be given to relieve a child’s cold symptoms, as part of a scenario in which they had already given a dose of acetaminophen; only 1 did not contain acetaminophen. Primary dependent variable: correct selection of cough/cold medication, using active ingredient as the rationale for choice. Primary independent variable: parent health literacy (Newest Vital Sign (NVS)). RESULTS Of 297 parents, 79.2% had low health literacy (NVS score 0–3). 35.4% correctly chose the cough/cold medication which did not contain acetaminophen. The proportion of those who made the correct choice was no different than expected from chance alone (Goodness of fit test; χ2=2.1, p=0.3). Only 7.7% chose the correct medication and used active ingredient as the rationale. Those with adequate literacy skills were more likely to have selected the correct medication and rationale (25.8% vs. 3.0% (p=0.001); AOR=11.1 [95%CI: 3.6–33.7], adjusting for sociodemographics, including English proficiency and education). CONCLUSIONS Many parents, especially those with low health literacy, do not use active ingredient information as part of decision-making related to administering multiple medications. PMID:23680341

  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. 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.

  12. Mathematical Modeling of the Release of Active Ingredients from a Contraceptive Patch: Ortho Evra® as a Case Study

    Science.gov (United States)

    Trujillo-de Santiago, Grissel; Patricio Sáenz-Collins, Carlos; García-Arellano, Lizette; Moisés Álvarez, Mario

    2014-01-01

    Contraceptive patches have become a frequently used contraceptive method. We present a mathematical model that describes the serum concentration profiles of Norelgestromin (NGMN) and Ethinylestradiol (EE) released from the contraceptive patch Ortho Evra®. We propose a simple one-compartment model based on pharmacokinetics data reported in previous studies. The model assumes a time-dependent release rate and a first order elimination rate for each of the active ingredients contained in the patch. The model was applied to noncompliance scenarios, such as total and partial detachment of the patch or prolonged use without patch replacement. The proposed model adequately describes the clinically observed evolution of NGMN and EE in serum. Predictions from the model were successfully validated using reported experimental data of serum concentrations of NGMN and EE. This simple model can be a valuable tool to predict pharmacokinetic profiles in diverse scenarios such us non-compliance situations. Alternatively, the model can be conveniently adapted to anticipate the effect of variations on patch characteristics such as differences in contact area, doses, materials, among others. PMID:24734055

  13. The effect of active learning methodologies on the teaching of pharmaceutical care in a Brazilian pharmacy faculty.

    Directory of Open Access Journals (Sweden)

    Alessandra R Mesquita

    Full Text Available In recent years, pharmacists have been involved in expanded patient care responsibilities, for example patient counseling in self-medication, medication review and pharmaceutical care, which require graduates to develop the necessary competences. Consequently, reorientation of pharmacy education has become necessary. As such, active learning strategies have been introduced into classrooms to increase problem-solving and critical thinking skills of students. The objective of this study was to evaluate the performance and perceptions of competency of students in a new pharmaceutical care course that uses active learning methodologies.This pharmaceutical care course was conducted in the first semester of 2014, in the Federal University of Sergipe. In the pharmaceutical care course, active learning methods were used, consisting of dialogic classroom expository, simulation and case studies. Student learning was evaluated using classroom tests and instruments that evaluated the perception of competency in pharmaceutical care practice. Furthermore, students' satisfaction with the course was evaluated.Thirty-three students completed the four evaluations used in the course (i.e., a discursive written exam, seminars, OSCE, and virtual patient; 25 were female (75.75%, and the median age was 23.43 (SD 2.82 years. The overall mean of student scores, in all evaluation methods was 7.97 (SD 0.59 on a scale of 0 to 10 points, and student performance on the virtual patient method was statistically superior to other methods. With respect to the perception of competency in pharmaceutical care practice, a comparison of pre- and post-test scores revealed statistically significant improvement for all evaluated competences. At the end of the semester, the students presented positive opinions of the pharmaceutical care course.The results suggest that an active learning course can enhance the learning of pharmaceutical care competences. In future studies it will be

  14. Quantitative Analysis of Active Ingredients in Compound Acetylsalicylic Acid Tablets by DOSY%复方乙酰水杨酸片中有效成分的DOSY技术分析

    Institute of Scientific and Technical Information of China (English)

    王丽敏; 仇汝臣; 黄少华

    2016-01-01

    Compound acetylsalicylic acid tablet is a clinical drug having antipyretic, analgesic and anti-inflammatory effects. The present methods to analyze the active ingredients in this drug have many disadvantages. In this study, we used polydimethylsiloxane (PDMS)-assisted diffusion ordered NMR spectroscopy (DOSY), DOSY-correlated spectroscopy (COSY), and relative quantitative1H NMR techniques to analyze the three main active ingredients in this drug. The content ratios among the 3 components could be obtained. It is argued that PDMS-assisted DOSY provides a convenient and efficient method for pharmaceutical quality control of compound acetylsalicylic acid tablets.%复方乙酰水杨酸片是临床常用的解热镇痛消炎药物,目前其有效成分的分析方法存在操作繁琐而分析速度慢等不足。该文利用二甲基硅油(PDMS)辅助的扩散排序(DOSY)技术以及扩散排序-同核相关(DOSY-COSY)联用技术,成功地对复方乙酰水杨酸片中三种有效成分的分子结构进行了快速定性分析,并且利用核磁共振氢谱(1H NMR)技术进行了相对定量分析。该方法具有方便、快捷等特点,可作为借鉴和参考用于药物的质量评价。

  15. 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

  16. 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

  17. Adsorption of pharmaceuticals to microporous activated carbon treated with potassium hydroxide, carbon dioxide, and steam.

    Science.gov (United States)

    Fu, Heyun; Yang, Liuyan; Wan, Yuqiu; Xu, Zhaoyi; Zhu, Dongqiang

    2011-01-01

    Adsorption of sulfapyridine, tetracycline, and tylosin to a commercial microporous activated carbon (AC) and its potassium hydroxide (KOH)-, CO-, and steam-treated counterparts (prepared by heating at 850°C) was studied to explore efficient adsorbents for the removal of selected pharmaceuticals from water. Phenol and nitrobenzene were included as additional adsorbates, and nonporous graphite was included as a model adsorbent. The activation treatments markedly increased the specific surface area and enlarged the pore sizes of the mesopores of AC (with the strongest effects shown on the KOH-treated AC). Adsorption of large-size tetracycline and tylosin was greatly enhanced, especially for the KOH-treated AC (more than one order of magnitude), probably due to the alleviated size-exclusion effect. However, the treatments had little effect on adsorption of low-size phenol and nitrobenzene due to the predominance of micropore-filling effect in adsorption and the nearly unaffected content of small micropores causative to such effect. These hypothesized mechanisms on pore-size dependent adsorption were further tested by comparing surface area-normalized adsorption data and adsorbent pore size distributions with and without the presence of adsorbed antibiotics. The findings indicate that efficient adsorption of bulky pharmaceuticals to AC can be achieved by enlarging the adsorbent pore size through suitable activation treatments.

  18. 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.

  19. Magnetic nanop articles for use in a pharmaceutical composition

    OpenAIRE

    Morales, M. P.; Gómez Roca, Alejandro; Serna, C. J.; Veintemillas-Verdaguer, S; Barber, Domingo F.; Mejías, Raquel; Pérez-Yagüe, Sonia

    2010-01-01

    [EN] The invention relates to a pharmaceutical composition that includes a magnetic nanoparticle and at least one active ingredient, preferably an antineoplastic or immunomodulator, for treating illnesses, in particular cancer. The nucleus of the magnetic nanoparticle includes a magnetic iron AA oxide. The surface of the nanoparticle includes ligands 'c".,,,' BB bonded thereto by means of an ionic bond, a covalent bond, a hydrogen bridge, a hydrophobic bond, an electro...

  20. 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

  1. Molecular structure activity on pharmaceutical applications of Phenacetin using spectroscopic investigation

    Science.gov (United States)

    Madanagopal, A.; Periandy, S.; Gayathri, P.; Ramalingam, S.; Xavier, S.

    2017-01-01

    The pharmaceutical compound; Phenacetin was investigated by analyzing FT-IR, FT-Raman and 1H &13C NMR spectra. The hybrid efficient computational calculations performed for computing physical and chemical parameters. The cause of pharmaceutical activity due to the substitutions; carboxylic, methyl and amine groups in appropriate positions on the pedestal compound was deeply investigated. Moreover, 13C NMR and 1H NMR chemical shifts correlated with TMS standard to explain the truth of compositional ratio of base and ligand groups. The bathochromic shift due to chromophores over the energy levels in UV-Visible region was strongly emphasized the Anti-inflammatory chemical properties. The chemical stability was pronounced by the strong kubo gap which showed the occurring of charge transformation within the molecule. The occurrence of the chemical reaction was feasibly interpreted by Gibbs free energy profile. The standard vibrational analysis stressed the active participation of composed ligand groups for the existence of the analgesic as well as antipyretic properties of the Phenacetin compound. The strong dipole interaction energy utilization for the transition among non-vanishing donor and acceptor for composition of the molecular structure was interpreted.

  2. 21 CFR 310.538 - Drug products containing active ingredients offered over-the-counter (OTC) for use for ingrown...

    Science.gov (United States)

    2010-04-01

    ... offered over-the-counter (OTC) for use for ingrown toenail relief. 310.538 Section 310.538 Food and Drugs... ingredients offered over-the-counter (OTC) for use for ingrown toenail relief. (a) Any product that bears labeling claims such as for “temporary relief of discomfort from ingrown toenails,” or “ingrown...

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

    OpenAIRE

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

  4. Supersaturation of Calcipotriene and Betamethasone Dipropionate in a Novel Aerosol Foam Formulation for Topical Treatment of Psoriasis Provides Enhanced Bioavailability of the Active Ingredients

    OpenAIRE

    2016-01-01

    Introduction Previous studies have demonstrated the superior efficacy of a novel aerosol foam formulation of fixed combination calcipotriene 0.005% (Cal) and betamethasone dipropionate 0.064% (BD), compared with the ointment formulation. The aim of this study is to ascertain whether enhanced bioavailability of the active ingredients due to supersaturation and/or occlusive properties can explain the observed greater clinical efficacy. Methods Solubility and evaporation experiments were conduct...

  5. Removal of pharmaceuticals in biologically treated wastewater by chlorine dioxide or peracetic acid

    DEFF Research Database (Denmark)

    Hey, G.; Ledin, Anna; La Cour Jansen, Jes

    2012-01-01

    Removal of six active pharmaceutical ingredients in wastewater was investigated using chlorine dioxide (ClO2) and peracetic acid (PAA) as chemical oxidants. Four non-steroidal anti -inflammatory drugs (ibuprofen, naproxen, diclofenac, and mefenamic acid) and two l ipid regulating agents (gemfibrozi...... compounds, only clofibric acid and ibuprofen were not removed when treated wi th ClO2 up to 20 mg/L. Wi th increasing PAA dose up to 50 mg/L, signi ficant removal of most of the pharmaceutical s was observed except for the wastewater wi th the highest COD. Thi s indicates that chemical oxidation wi th ClO2...... could be used for tertiary treatment at WWTPs for active pharmaceutical ingredients whi le PAA was not sufficiently efficient....

  6. Method for microbiological testing of nonsterile pharmaceuticals.

    Science.gov (United States)

    Bühlmann, X

    1968-12-01

    A method for testing nonsterile pharmaceutical preparations for their microbial content is described. As far as possible, only solid culture media were used to obtain quantitative results. Aqueous and water-soluble products were tested with membrane-filter techniques. Nonfilterable products were first emulsified or suspended and the homogenate was used for examination. In both procedures, the total number of colonies is determined for aerobic bacteria and fungi. Tests for certain undesirable microbial groups were conducted with selected media. The method described is applicable for finished products, bulk products, raw materials, and active ingredients.

  7. 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.

  8. 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.

  9. [Studies on effects of Achyranthes bidentata on tongsaimai pellets main active ingredients chlorogenic acid, isoliquiritin, harpagoside and glycyrrhizin in vivo pharmacokinetics].

    Science.gov (United States)

    Cheng, Jian; Di, Liu-Qing; Shan, Jin-Jun; Zhao, Xiao-Li; Kang, An; Bi, Xiao-Lin; Li, Jun-Song

    2014-04-01

    To study on the effects of Achyranthes bidentata on Tongsaimai pellets main active ingredients chlorogenic acid, isoliquiritin, harpagoside and glycyrrhizin in rats in vivo pharmacokinetic behaviors, a method for the simultaneous determination of chlorogenic acid, isoliquiritin, harpagoside and liquiritigenin in rat plasma was established by UPLC-MS/MS. The analysis was performed on a waters Acquity BEH C18 column (2.1 mm x 100 mm, 1.7 microm) with the mixture of acetonitrile and 0.1% formic acid/water as mobile phase, and the gradient elution at a flow rate of 0.3 mL x min(-1). The analytes were detected by tandem mass spectrometry with the electrospray ionization (ESI) source and in the multiple reaction monitoring (MRM) mode. It turned out that the analytes of Tongsaimai pellets groups C(max) and AUC(Q-infinity) values were higher than that with A. bidentata group, and the C(max) values of chlorogenic acid had significantly difference (P < 0.05), the AUC(0-infinity) values of chlorogenic acid and glycyrrhizin had significantly difference (P < 0.05); The T(max) and CL values of two groups had no significantly difference. Results showed that the established method was specific, rapid, accurate and sensitive for the studies of Tongsaimai pellets four main active ingredients in rat in vivo pharmacokinetic, and A. bidentata have varying degrees of effects on Tongsaimai pellets four main active ingredients in rat in vivo pharmacokinetic behaviors.

  10. In-stream attenuation of neuro-active pharmaceuticals and their metabolites

    Science.gov (United States)

    Writer, Jeffrey; Antweiler, Ronald C.; Ferrar, Imma; Ryan, Joseph N.; Thurman, Michael

    2013-01-01

    In-stream attenuation was determined for 14 neuro-active pharmaceuticals and associated metabolites. Lagrangian sampling, which follows a parcel of water as it moves downstream, was used to link hydrological and chemical transformation processes. Wastewater loading of neuro-active compounds varied considerably over a span of several hours, and thus a sampling regime was used to verify that the Lagrangian parcel was being sampled and a mechanism was developed to correct measured concentrations if it was not. In-stream attenuation over the 5.4-km evaluated reach could be modeled as pseudo-first-order decay for 11 of the 14 evaluated neuro-active pharmaceutical compounds, illustrating the capacity of streams to reduce conveyance of neuro-active compounds downstream. Fluoxetine and N-desmethyl citalopram were the most rapidly attenuated compounds (t1/2 = 3.6 ± 0.3 h, 4.0 ± 0.2 h, respectively). Lamotrigine, 10,11,-dihydro-10,11,-dihydroxy-carbamazepine, and carbamazepine were the most persistent (t1/2 = 12 ± 2.0 h, 12 ± 2.6 h, 21 ± 4.5 h, respectively). Parent compounds (e.g., buproprion, carbamazepine, lamotrigine) generally were more persistent relative to their metabolites. Several compounds (citalopram, venlafaxine, O-desmethyl-venlafaxine) were not attenuated. It was postulated that the primary mechanism of removal for these compounds was interaction with bed sediments and stream biofilms, based on measured concentrations in stream biofilms and a column experiment using stream sediments.

  11. Understanding the risks associated with the use of new psychoactive substances (NPS): high variability of active ingredients concentration, mislabelled preparations, multiple psychoactive substances in single products.

    Science.gov (United States)

    Zamengo, Luca; Frison, Giampietro; Bettin, Chiara; Sciarrone, Rocco

    2014-08-17

    New psychoactive substances (NPS), are now a large group of substances of abuse not yet completely controlled by international drug conventions, which may pose a public health threat. Anxiety, paranoia, hallucinations, seizures, hyperthermia and cardiotoxicity are some of the common adverse effects associated with these compounds. In this paper, three case reports taken from the archive of processed cases of the authors' laboratory are presented and discussed to stress the risks of possible adverse consequences for NPS users: in particular, (i) the risk deriving from the difficulty of predicting the actual consumed dose, due to variability of active ingredients concentration in consumed products, (ii) the risk deriving from the difficulty of predicting the actual active ingredients present in consumed products, as opposed to those claimed by the manufacturer, and (iii) the risk deriving from the difficulty of predicting the actual pharmacological and toxicological effects related to the simultaneous consumption of different psychoactive ingredients contained in single products, whose interactions are mostly unknown. Each of them individually provide a source of concern for possible serious health related consequences. However, they should be considered in conjunction with each others, with the worldwide availability of NPS through the web and also with the incessantly growing business derived from the manipulation and synthesis of new substances. The resulting scenario is that of a cultural challenge which demands a global approach from different fields of knowledge.

  12. 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.

  13. 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.

  14. [6]-gingerol and [6]-shogaol, active ingredients of the traditional Japanese medicine hangeshashinto, relief oral ulcerative mucositis-induced pain via action on Na(+) channels.

    Science.gov (United States)

    Hitomi, Suzuro; Ono, Kentaro; Terawaki, Kiyoshi; Matsumoto, Chinami; Mizuno, Keita; Yamaguchi, Kiichiro; Imai, Ryota; Omiya, Yuji; Hattori, Tomohisa; Kase, Yoshio; Inenaga, Kiyotoshi

    2017-03-01

    The traditional Japanese herbal medicine hangeshashinto (HST) has beneficial effects for the treatment of oral ulcerative mucositis (OUM) in cancer patients. However, the ingredient-based mechanism that underlies its pain-relieving activity remains unknown. In the present study, to clarify the analgesic mechanism of HST on OUM-induced pain, we investigated putative HST ingredients showing antagonistic effects on Na(+) channels in vitro and in vivo. A screen of 21 major ingredients using automated patch-clamp recordings in channel-expressing cells showed that [6]-gingerol and [6]-shogaol, two components of a Processed Ginger extract, considerably inhibited voltage-activated Na(+) currents. These two ingredients inhibited the stimulant-induced release of substance P and action potential generation in cultured rat sensory neurons. A submucosal injection of a mixture of [6]-gingerol and [6]-shogaol increased the mechanical withdrawal threshold in healthy rats. In a rat OUM model, OUM-induced mechanical pain was alleviated 30min after the swab application of HST despite the absence of anti-bacterial and anti-inflammatory actions in the OUM area. A swab application of a mixture of [6]-gingerol and [6]-shogaol induced sufficient analgesia of OUM-induced mechanical or spontaneous pain when co-applied with a Ginseng extract containing abundant saponin. The Ginseng extract demonstrated an acceleration of substance permeability into the oral ulcer tissue without an analgesic effect. These findings suggest that Na(+) channel blockage by gingerol/shogaol plays an essential role in HST-associated analgesia of OUM-induced pain. This pharmacological mechanism provides scientific evidence supporting the use of this herbal medicine in patients suffering from OUM-induced pain.

  15. Survey on Disaster Relief Activities to the Pharmacists Belonging to Kobe-city Pharmaceutical Organization.

    Science.gov (United States)

    Yasuhara, Tomohisa; Kondo, Hiroki; Nagata, Misa; Iwata, Kana; Kushihata, Taro; Katsuragi, Satoko; Ikeuchi, Junko; Sone, Tomomichi

    2016-10-01

     In 2014, there were about 160 thousands community pharmacists in Japan. Community pharmacists are health care workers who help victims in a disaster and are potential resources who can provide disaster relief. However, currently the disaster relief activities of community pharmacists are merely a resourceful and flexible demonstration of their professional abilities and not a specifically organized activity. Therefore, disaster relief education programs for community pharmacists are being explored and studies are still in the nascent stage. In this study, pharmacists of a pharmaceutical organization in Kobe City were asked to reply to a questionnaire survey so that their hopes and ideas about the disaster relief activities that they carry out can help build effective educational programs to enhance relief activities. Finally, 8 factors (cumulative contribution rate: 90.9%) were extracted by factor analysis (maximum likelihood method, the diagonal elements: squared multiple correlation, quartimin rotation) of the 25 questions. In addition, a hierarchical cluster analysis (Ward method) by the factor scores of the extracted 8 factors resulted in 7 groups. The findings revealed the groups into which the community pharmacists were divided and their hopes and ideas about disaster relief. We expect that these results could bring awareness about the disaster relief activities suitable for each community pharmacist, provide appropriate training opportunities for those who volunteer, and motivate daily studies and preparations for disaster relief activities among community pharmacists.

  16. 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.

  17. Negatively charged silver nanoparticles with potent antibacterial activity and reduced toxicity for pharmaceutical preparations

    Directory of Open Access Journals (Sweden)

    Salvioni L

    2017-03-01

    Full Text Available Lucia Salvioni,1 Elisabetta Galbiati,1 Veronica Collico,1 Giulia Alessio,1 Svetlana Avvakumova,1 Fabio Corsi,2,3 Paolo Tortora,1 Davide Prosperi,1 Miriam Colombo1 1Nanobiolab, Department of Biotechnology and Bioscience, University of Milano-Bicocca, 2Biological and Clinical Science Department, University of Milan, Milano, 3Surgery Department, Breast Unit, IRCCS S Maugeri Foundation, Pavia, Italy Background: The discovery of new solutions with antibacterial activity as efficient and safe alternatives to common preservatives (such as parabens and to combat emerging infections and drug-resistant bacterial pathogens is highly expected in cosmetics and pharmaceutics. Colloidal silver nanoparticles (NPs are attracting interest as novel effective antimicrobial agents for the prevention of several infectious diseases.Methods: Water-soluble, negatively charged silver nanoparticles (AgNPs were synthesized by reduction with citric and tannic acid and characterized by transmission electron microscopy, dynamic light scattering, zeta potential, differential centrifuge sedimentation, and ultraviolet–visible spectroscopy. AgNPs were tested with model Gram-negative and Gram-positive bacteria in comparison to two different kinds of commercially available AgNPs.Results: In this work, AgNPs with higher antibacterial activity compared to the commercially available colloidal silver solutions were prepared and investigated. Bacteria were plated and the antibacterial activity was tested at the same concentration of silver ions in all samples. The AgNPs did not show any significant reduction in the antibacterial activity for an acceptable time period. In addition, AgNPs were transferred to organic phase and retained their antibacterial efficacy in both aqueous and nonaqueous media and exhibited no toxicity in eukaryotic cells.Conclusion: We developed AgNPs with a 20 nm diameter and negative zeta potential with powerful antibacterial activity and low toxicity compared

  18. Polysaccharide-Containing Macromolecules in a Kampo (Traditional Japanese Herbal Medicine, Hochuekkito: Dual Active Ingredients for Modulation of Immune Functions on Intestinal Peyer's Patches and Epithelial cells

    Directory of Open Access Journals (Sweden)

    Hiroaki Kiyohara

    2011-01-01

    Full Text Available A traditional Japanese herbal (Kampo medicine, Hochuekkito (Bu-Zhong-Yi-Qi-Tang in Chinese, TJ-41 is a well-known Kampo formula, and has been found to enhance antigen-specific antibody response in not only local mucosal immune system in upper respiratory tract, but also systemic immune system through upper respiratory mucosal immune system. Although this immunopharmacological effect has been proposed to express by modulation of intestinal immune system including Peyer's patches and intestinal epithelial cells, active ingredients are not known. TJ-41 directly affected the production of bone marrow cell-proliferative growth factors from murine Peyer's patch immunocompetent cells in vitro. Among low molecular, intermediate size and macromolecular weight fractions prepared from TJ-41, only fraction containing macromolecular weight ingredients showed Peyer's patch-mediated bone marrow cell-proliferation enhancing activity. Anion-exchange chromatography and gel filtration gave 17 subfractions comprising polysaccharides and lignins from the macromolecular weight fraction of TJ-41, and some of the subfractions showed significant enhancing activities having different degrees. Some of the subfractions also expressed stimulating activity on G-CSF-production from colonic epithelial cells, and statistically significant positive correlation was observed among enhancing activities of the subfractions against Peyer's patch immunocompetent cells and epithelial cells. Among the fractions from TJ-41 oral administration of macromolecular weight ingredient fraction to mice succeeded to enhance antigen-specific antibody response in systemic immune system through upper respiratory mucosal immune system, but all the separated fractions failed to enhance the in vivo antibody response in upper respiratory tract.

  19. "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.

  20. 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.

  1. Caveat medicus: consequences of federal investigations of marketing activities of pharmaceutical suppliers of prostate cancer drugs.

    Science.gov (United States)

    McKoy, June M; Lyons, E Allison; Obadina, Eniola; Carson, Kenneth; Pickard, A Simon; Schellhammer, Paul; McLeod, David; Boyd, Cynthia E; McWilliams, Norene; Sartor, Oliver; Schumock, Glen T; McCaffery, Kathryn; Bennett, Charles L

    2005-12-01

    In the course of recent health care fraud investigations against TAP Pharmaceuticals (Lake Forest, IL) and AstraZeneca International (London, United Kingdom), each pled guilty to one violation of the Prescription Drug Marketing Act, settled claims related to alleged violations of the False Claims Act without admitting guilt, and paid fines, settlements for liabilities, and reimbursements of dollar 850 million and dollar 355 million, respectively. In a unique aspect of these cases, federal investigators brought criminal charges against 14 TAP employees and investigated the billing practices of several urologists. These investigations resulted in guilty pleas from both urologists and industry employees relative to the Prescription Drug Marketing Act or the False Claims Act and probationary sentences with payments of fines and restitution to the government for urologists who cooperated with federal investigations. One uncooperative urologist was found guilty of violating the Federal False Claims Act and sentenced to 6 months of home arrest, excluded from Medicare for 5 years, required to provide 600 hours of free medical care to indigent patients and patients covered by Medicare or Medicaid, and paid fines and restitution to the government. The cases against TAP and AstraZeneca have been followed by federal and state investigations of allegedly illegal marketing practices of other pharmaceutical firms and have resulted in negotiated settlements of dollar 3.8 billion and dollar 71.5 million, respectively. Believing that an Average Wholesale Price-based reimbursement system was an important driving factor for these marketing activities, Medicare has shifted to an Average Sales Price-based reimbursement system. This is expected to greatly impact the practice of outpatient oncology nationwide.

  2. Activities of the Pharmaceutical Technology Institute of the Oswaldo Cruz Foundation with medicinal, insecticidal and insect repellent plants.

    Science.gov (United States)

    Gilbert, B; Teixeira, D F; Carvalho, E S; De Paula, A E; Pereira, J F; Ferreira, J L; Almeida, M B; Machado, R da S; Cascon, V

    1999-01-01

    In addition to original research, Far-Manguinhos, the Pharmaceutical Division of the Brazilian Ministry of Health's Oswaldo Cruz Foundation (FIOCRUZ), devotes major attention to the finalising of products for use in public health campaigns or, under contract, for private industrial development. Emphasis is on standardisation, adequate supply, safety in use and efficacy. Among the products discussed in this summary of some of its activities in the chemical and pharmaceutical fields are medicinal plants Bidens pilosa, Cymbopogon citratus, Copaifera species, Mentha crispa, Phyllanthus tenellus Roxb. and other Phyllanthus species, insecticidal plants, Lonchocarpus urucu and Quassia amara, and the insect antifeedant plants Carapa guianensis and Pterodon emarginatus.

  3. Achromobactor denitrificans SP1 produces pharmaceutically active 25C prodigiosin upon utilizing hazardous di(2-ethylhexyl)phthalate

    Science.gov (United States)

    Achromobacter denitrificans SP1 isolated from soil sludge heavily contaminated with plastic waste produced a novel pharmaceutically-active 25C prodigiosin analog during growth in a simple mineral salt medium supplemented with hazardous di(2-ethylhexyl)phthalate (DEHP) blended PVC plastics (in situ) ...

  4. 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.

  5. Silver sucrose octasulfate (IASOS™ as a valid active ingredient into a novel vaginal gel against human vaginal pathogens: in vitro antimicrobial activity assessment.

    Directory of Open Access Journals (Sweden)

    Cinzia Marianelli

    Full Text Available This in vitro study assessed the antimicrobial properties of a novel octasilver salt of Sucrose Octasulfate (IASOS as well as of an innovative vaginal gel containing IASOS (SilSOS Femme, against bacterial and yeast pathogens isolated from human clinical cases of symptomatic vaginal infections. In BHI and LAPT culture media, different ionic silver concentrations and different pHs were tested. IASOS exerted a strong antimicrobial activity towards all the pathogens tested in both culture media. The results demonstrated that salts and organic compounds present in the culture media influenced IASOS efficacy only to a moderate extent. Whereas comparable MBCs (Minimal Bactericidal Concentrations were observed for G. vaginalis (10 mg/L Ag+, E. coli and E. aerogenes (25 mg/L Ag+ in both media, higher MBCs were found for S. aureus and S. agalactiae in LAPT cultures (50 mg/L Ag+ versus 25 mg/L Ag+. No minimal concentration totally inhibiting the growth of C. albicans was found. Nevertheless, in both media at the highest ionic silver concentrations (50-200 mg/L Ag+, a significant 34-52% drop in Candida growth was observed. pH differently affected the antimicrobial properties of IASOS against bacteria or yeasts; however, a stronger antimicrobial activity at pH higher than the physiological pH was generally observed. It can be therefore concluded that IASOS exerts a bactericidal action against all the tested bacteria and a clear fungistatic action against C. albicans. The antimicrobial activity of the whole vaginal gel SilSOS Femme further confirmed the antimicrobial activity of IASOS. Overall, our findings support IASOS as a valid active ingredient into a vaginal gel.

  6. Direct Analysis of Pharmaceutical Drugs Using Nano-DESI MS

    Directory of Open Access Journals (Sweden)

    Carlos Cardoso-Palacios

    2016-01-01

    Full Text Available Counterfeit pharmaceutical drugs imply an increasing threat to the global public health. It is necessary to have systems to control the products that reach the market and to detect falsified medicines. In this work, molecules in several pharmaceutical tablets were directly analyzed using nanospray desorption electrospray ionization mass spectrometry (nano-DESI MS. Nano-DESI is an ambient surface sampling technique which enables sampling of molecules directly from the surface of the tablets without any sample pretreatment. Both the active pharmaceutical ingredients (APIs and some excipients were detected in all analyzed tablets. Principal component analysis was used to analyze mass spectral features from different tablets showing strong clustering between tablets with different APIs. The obtained results suggest nano-DESI MS as future tool for forensic analysis to discern APIs present in unknown tablet samples.

  7. SELECTED ASPECTS OF TERAHERTZ SPECTROSCOPY IN PHARMACEUTICAL SCIENCES.

    Science.gov (United States)

    Nowak, Kacper; Pliński, Edward F; Karolewicz, Bożena; Jarząb, Przemysław P; Plińska, Stanisława; Fuglewicz, Bogusław; Walczakowski, Michał J; Augustyn, Łukasz; Sterczewsk, Łukasz A; Grzelczak, Michał P; Hruszowiec, Mariusz; Beziuk, Grzegorz; Mikulic, Martin; Pałka, Norbert; Szustakowskip, Mieczysław

    2015-01-01

    THz-TDS techniques are applied to investigate selected pharmaceutical samples. Investigations were performed on selected pharmaceutical samples with active pharmaceutical ingredients (API)--famotidine, ranitidine, fenofibrate, lovastatin, simvastatin, aspirin, ketoconazole, acyclovir (hydrated and non-hydrated), on excipients--lactose, glucose (hydrated and non-hydrated), Pluronic 127, and on mixtures of selected compounds. Pseudo-polymorphism effects are considered as well. Examples of the terahertz imaging technique are also given. APIs and excipients can be easily recognized in the terahertz band by their specific "fingerprints" as individual components and in mixtures. The hydration process as a variety of polymorphism can also be easily monitored using the THz technique. Moreover, terahertz light can be useful for the penetration of tablets, giving clear pictures of possible defects in tablet coatings.

  8. Early pharmaceutical profiling to predict oral drug absorption

    DEFF Research Database (Denmark)

    Bergström, Christel A S; Holm, René; Jørgensen, Søren Astrup

    2014-01-01

    of the pharmaceutical profiling methods available, with focus on in silico and in vitro models typically used to forecast active pharmaceutical ingredient's (APIs) in vivo performance after oral administration. An overview of the composition of human, animal and simulated gastrointestinal (GI) fluids is provided...... are discussed in detail and future demands on pharmaceutical profiling are identified. It is expected that innovative computational and experimental methods that better describe molecular processes involved in vivo during dissolution and absorption of APIs will be developed in the OrBiTo. These methods...... will provide early insights into successful pathways (medicinal chemistry or formulation strategy) and are anticipated to increase the number of new APIs with good oral absorption being discovered....

  9. 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.

  10. 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。

  11. The hallucinogenic herb Salvia divinorum and its active ingredient salvinorin A inhibit enteric cholinergic transmission in the guinea-pig ileum.

    Science.gov (United States)

    Capasso, R; Borrelli, F; Capasso, F; Siebert, D J; Stewart, D J; Zjawiony, J K; Izzo, A A

    2006-01-01

    Salvia divinorum is a widespread hallucinogenic herb traditionally employed for divination, as well as a medicament for several disorders including disturbances of gastrointestinal motility. In the present study we evaluated the effect of a standardized extract from the leaves of S. divinorum (SDE) on enteric cholinergic transmission in the guinea-pig ileum. SDE reduced electrically evoked contractions without modifying the contractions elicited by exogenous acetylcholine, thus suggesting a prejunctional site of action. The inhibitory effect of SDE on twitch response was abolished by the opioid receptor antagonist naloxone and by the kappa-opioid antagonist nor-binaltorphimine, but not by naltrindole (a delta-opioid receptor antagonist), CTOP (a mu-opioid receptor antagonist), thioperamide (a H(3) receptor antagonist), yohimbine (an alpha(2)-receptor antagonist), methysergide (a 5-hydroxytryptamine receptor antagonist), N(G)-nitro-L-arginine methyl ester (an inhibitor of NO synthase) or apamin (a blocker of Ca(2+)-activated K(+) channels). Salvinorin A, the main active ingredient of S. divinorum, inhibited in a nor-binaltorphimine- and naloxone-sensitive manner electrically induced contractions. It is concluded that SDE depressed enteric cholinergic transmission likely through activation of kappa-opioid receptors and this may provide the pharmacological basis underlying its traditional antidiarrhoeal use. Salvinorin A might be the chemical ingredient responsible for this activity.

  12. 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

  13. 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

    The aim of this study was to optimize the epithelioma papillosum cyprini (EPC) cell line handling procedure for the comet assay to investigate the genotoxic potential of widely used pesticides. The effects of various media and handling of the EPC cell line were examined. Results indicated...... 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...

  14. Activated sludge systems removal efficiency of veterinary pharmaceuticals from slaughterhouse wastewater.

    Science.gov (United States)

    Carvalho, Pedro N; Pirra, António; Basto, M Clara P; Almeida, C Marisa R

    2013-12-01

    The knowledge on the efficiency of wastewater treatment plants (WWTPs) from animal food production industry for the removal of both hormones and antibiotics of veterinary application is still very limited. These compounds have already been reported in different environmental compartments at levels that could have potential impacts on the ecosystems. This work aimed to evaluate the role of activated sludge in the removal of commonly used veterinary drugs, enrofloxacin (ENR), tetracycline (TET), and ceftiofur, from wastewater during a conventional treatment process. For that, a series of laboratory-controlled experiments using activated sludge were carried out in batch reactors. Sludge reactors with 100 μg/L initial drug charge presented removal rates of 68 % for ENR and 77 % for TET from the aqueous phase. Results indicated that sorption to sludge and to the wastewater organic matter was responsible for a significant percentage of drugs removal. Nevertheless, these removal rates still result in considerable concentrations in the aqueous phase that will pass through the WWTP to the receiving environment. Measuring only the dissolved fraction of pharmaceuticals in the WWTP effluents may underestimate the loading and risks to the aquatic environment.

  15. Pharmaceutical applications of vibrational chemical imaging and chemometrics: a review.

    Science.gov (United States)

    Gendrin, C; Roggo, Y; Collet, C

    2008-11-04

    The emergence of chemical imaging (CI) has gifted spectroscopy an additional dimension. Chemical imaging systems complement chemical identification by acquiring spatially located spectra that enable visualization of chemical compound distributions. Such techniques are highly relevant to pharmaceutics in that the distribution of excipients and active pharmaceutical ingredient informs not only a product's behavior during manufacture but also its physical attributes (dissolution properties, stability, etc.). The rapid image acquisition made possible by the emergence of focal plane array detectors, combined with publication of the Food and Drug Administration guidelines for process analytical technology in 2001, has heightened interest in the pharmaceutical applications of CI, notably as a tool for enhancing drug quality and understanding process. Papers on the pharmaceutical applications of CI have been appearing in steadily increasing numbers since 2000. The aim of the present paper is to give an overview of infrared, near-infrared and Raman imaging in pharmaceutics. Sections 2 and 3 deal with the theory, device set-ups, mode of acquisition and processing techniques used to extract information of interest. Section 4 addresses the pharmaceutical applications.

  16. 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.

  17. 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.

  18. 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

    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...... during launch are forecasting inaccuracy and the risk of a required label change from local regulatory authorities. Robust solutions are found by implementing the Robust Optimization framework....

  19. 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...... of the bench scale results for MFR and ASP for treating a complex pharmaceutical waste mixture in the soil and groundwater beneath the Kærgård Plantage megasite....

  20. Antifungal activity of food additives in vitro and as ingredients of hydroxypropyl methylcellulose-lipid edible coatings against Botrytis cinerea and Alternaria alternata on cherry tomato fruit.

    Science.gov (United States)

    Fagundes, Cristiane; Pérez-Gago, María B; Monteiro, Alcilene R; Palou, Lluís

    2013-09-16

    The antifungal activity of food additives or 'generally recognized as safe' (GRAS) compounds was tested in vitro against Botrytis cinerea and Alternaria alternata. Radial mycelial growth of each pathogen was measured in PDA Petri dishes amended with food preservatives at 0.2, 1.0, or 2.0% (v/v) after 3, 5, and 7 days of incubation at 25 °C. Selected additives and concentrations were tested as antifungal ingredients of hydroxypropyl methylcellulose (HPMC)-lipid edible coatings. The curative activity of stable coatings was tested in in vivo experiments. Cherry tomatoes were artificially inoculated with the pathogens, coated by immersion about 24 h later, and incubated at 20 °C and 90% RH. Disease incidence and severity (lesion diameter) were determined after 6, 10, and 15 days of incubation and the 'area under the disease progress stairs' (AUDPS) was calculated. In general, HPMC-lipid antifungal coatings controlled black spot caused by A. alternata more effectively than gray mold caused by B. cinerea. Overall, the best results for reduction of gray mold on cherry tomato fruit were obtained with coatings containing 2.0% of potassium carbonate, ammonium phosphate, potassium bicarbonate, or ammonium carbonate, while 2.0% sodium methylparaben, sodium ethylparaben, and sodium propylparaben were the best ingredients for coatings against black rot.

  1. 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 aerobic sludge age from 1-3 to 7 days seemed to be critical for the removal of naproxen and ketoprofen, with markedly higher rates of removal at sludge ages of 7 days or more. No removal was shown for diclofenac and clofibric acid, while high rates were observed for ibuprofen in all investigated sludges....... Parallel examinations of activated sludge batches with and without allylthiourea (12 mg/L), an inhibitor of ammonia monooxygenase, showed minor to moderate influence on the removal rates of ketoprofen and naproxen. These results suggest that the removal rates of biodegradable pharmaceuticals in municipal...

  2. 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.

  3. Effects of pharmaceutical processing on pepsin activity during the formulation of solid dosage forms.

    Science.gov (United States)

    Kristó, Katalin; Pintye-Hódi, Klára

    2013-02-01

    The main aim of this study was to investigate the effects of pharmaceutical technological methods on pepsin activity during the formulation of solid dosage forms. The circumstances of direct compression and wet granulation were modeled. During direct compression, the heat and the compression force must be taken into consideration. The effects of these parameters were investigated in three materials (pure pepsin, and 1:1 (w/w) pepsin-tartaric acid and 1:1 (w/w) pepsin-citric acid powder mixtures). It was concluded that direct compression is appropriate for the formulation of solid dosage forms containing pepsin through application without acids or with acids at low compression force. The effects of wet granulation were investigated with a factorial design for the same three materials. The factors were time, temperature and moisture content. There was no significant effect of the factors when acids were not applied. Temperature was a significant factor when acids were applied. The negative effect was significantly higher for citric acid than for tartaric acid. It was found that wet granulation can be utilized for the processing of pepsin into solid dosage forms under well-controlled circumstances. The application of citric acid is not recommended during the formulation of solid dosage forms through wet granulation. A mathematically based optimization may be necessary for preformulation studies of the preparation of dosage forms containing sensitive enzymes.

  4. 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.

  5. 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.

  6. 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

  7. Digestible energy requirement for females of Rhamdia quelen on reproductive activity fed with ration based on vegetal ingredients

    Directory of Open Access Journals (Sweden)

    Robie A Bombardelli

    2015-07-01

    Full Text Available The present experiment was carried out to evaluate the growth and reproductive parameters of Rhamdia quelen females fed with pelleted ration containing different levels of digestible energy, and to evaluate the vigor of their offspring. The breeders were placed in tanks under conditions of photoperiod and natural temperature. The fishes were fed for 255 days with isoproteic rations pelleted containing 35% of crude protein (CP and five levels of the digestible energy (DE (2700, 2950, 3200, 3450, 3700 kcal kg-1. The fishes were distributed in a randomized experimental design compounded by five treatments and three repetitions. A 16-m² tank containing six females and three males was considered as one experimental unit. The weight and weight gain was evaluated. During the reproductive season the females were induced to breeding by hormonal manipulation and were evaluated the percentage of spawning females, the total fecundity, relative fecundity (number of oocytes per gram of spawning females, the fertilization ratio, the time to hatching and the vigor of larvae. The growth and reproductive parameters were not influenced (P > 0.05 by the increasing levels of digestible energy of the rations. The feeding of R. quelen females in breeding fit can be carried out with 2700 kcal kg-1 pelletized ration based on vegetal ingredients, without damage to reproductive performance.

  8. What are the active ingredients in cognitive and behavioral psychotherapy for anxious and depressed children? A meta-analytic review.

    Science.gov (United States)

    Spielmans, Glen I; Pasek, Leigh F; McFall, Joseph P

    2007-06-01

    Prior meta-analytic reviews have indicated that cognitive and behavioral treatments are efficacious in treating child and adolescent depression and anxiety. Further, a meta-analysis has suggested that behavioral treatments are superior to nonbehavioral treatments for treating anxiety and depression in youth. However, the prior meta-analysis did not examine direct comparisons between cognitive and behavioral treatments (CBT) and non-CBT treatments, leaving open the possibility that their results were artifactual. The present meta-analysis aggregated results of studies in which CBT treatments were compared with either other bona fide treatments (including other CBT therapies) or non-bona fide therapies. The heterogeneity of the distribution of differences between bona fide treatments as well as a comparison of full (e.g. CBT+Parent training) versus component treatments (e.g., CBT only) were examined. The results indicated that: (a) CBT was more efficacious than non-bona fide therapies; (b) CBT was no more efficacious than bona fide non-CBT treatments (c) the differences between bona fide treatments were homogenously distributed around zero; and (d) full CBT treatments offered no significant benefit over their components. The results strongly suggest that the theoretically purported critical ingredients of CBT are not specifically ameliorative for child and adolescent depression and anxiety.

  9. New PAT tools for assessing content uniformity, sampling error, and degree of crystallinity in pharmaceutical tablets

    DEFF Research Database (Denmark)

    Warnecke, Solveig

    of the pharmaceutical drug, both during development and throughout the production. The usage of PAT tools is encouraged by the regulatory authorities, and therefore the interest in new and improved PAT tools is increasing. The main purpose of introducing Quality by Design (QbD) and PAT in pharmaceutical production...... practice in traditional pharmaceutical industry. In this thesis, three spectroscopic PAT tools are investigated, near-infrared-, terahertz-, and fluorescence-spectroscopy. These techniques have been evaluated with chemometrics and theory of sampling. The first study focused on the critical but rather...... overlooked sampling uncertainty that exist in all analytical measurements. The sampling error was studied using an example involving near infrared transmission (NIT) spectroscopy to study content of uniformity of five batches of escitalopram tablets, produced at different active pharmaceutical ingredients...

  10. 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.

  11. 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

    2016-01-05

    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.

  12. 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。

  13. Qualitative Analysis of Iranian Crack to Determine the Active Ingredient in Committing Crime in order to Determine Criminal Punishment

    Directory of Open Access Journals (Sweden)

    Ali Hassan Rahmani

    2016-12-01

    Full Text Available Crime (the basis of criminal law is the behavior that intentionallyleadsto violation of legal orders and one of the things that hinder the realization of criminal liability is the condition called insanity. People lacking the healthy will, or unaware of the essence of the consequences their acts if they commit crimes they are not addressed in the law and do not have criminal responsibility.In a cross sectional study in Khuzestan forensic toxicology lab after 61 TLCsamplesof crack street, drug recognition tests was doneby HPLC and GC / MS. Examination of data (V22 SPSS (p value <0.05:% 93/4of crack samples were containing morphine,% 83/6 with caffeine, noscapine or dextromethorphan,% 27/9 heroin and codeine,% 37/7 six mono-acetylphloroglucinol morphine,% 34/4 acetyl codeine,% 13/1 narceine and acetaminophen, % 16/4 diazepam and% 9/8 chloramphenicol and other components of methyl amphetamines, diphenhydramine, lidocaine, thebaine, amoxicillin, amitriptyline and nortriptyline % 6/6 of samples were a mixture of methyl amphetamine - diphenhydramine and acetaminophen, it was a special type of Iraniancrack, due to the existence of amphetamines play a major role in dementia and mental illness like schizophrenia.Iraniancrack is not only different from a real crack (cocaine, but differs in the types, number and amount of additives drug ,Opioid and diluent. Crack has different amount of effective substances on the central nervous system pharmacological and non-pharmacological and psychedelic properties.Different Clinical manifestations like dementia and lack of determinationthat leads to crime.As a result, the need to determine the ingredients in the crack used in the examination of crime and helpingthe criminal justice system in determining the penalty is definite.

  14. Effects of human pharmaceuticals on cytotoxicity, EROD activity and ROS production in fish hepatocytes.

    OpenAIRE

    2004-01-01

    Pharmaceuticals are found in the aquatic environment but their potential effects on non-target species like fish remain unknown. This in vitro study is a first approach in the toxicity assessment of human drugs on fish. Nine pharmaceuticals were tested on two fish hepatocyte models: primary cultures of rainbow trout hepatocytes (PRTH) and PLHC-1 fish cell line. Cell viability, interaction with cytochrome P450 1A (CYP1A) enzyme and oxidative stress were assessed by using 3-(4,5-dimethylthiazol...

  15. 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

  16. 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

  17. Automated evaluation of pharmaceutically active ionic liquids' (eco)toxicity through the inhibition of human carboxylesterase and Vibrio fischeri.

    Science.gov (United States)

    Costa, Susana P F; Justina, Vanessa D; Bica, Katharina; Vasiloiu, Maria; Pinto, Paula C A G; Saraiva, M Lúcia M F S

    2014-01-30

    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 (EC50). The EC50 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.

  18. Mechanochemistry of magnesium oxide revisited: facile derivatisation of pharmaceuticals using coordination and supramolecular chemistry.

    Science.gov (United States)

    Chow, Ernest H H; Strobridge, Fiona C; Friscić, Tomislav

    2010-09-14

    Liquid-assisted grinding allows the rapid, waste-free and one-pot synthesis of a variety of magnesium drug derivatives directly from the excipient MgO; such reactivity is relevant for the behaviour of ibuprofen formulations involving MgO and can be used for oxide-based mechanosynthesis of metal-organic salts, discrete complexes and carboxylate clusters involving magnesium and pharmaceutically active ingredients.

  19. Hot-Melt Extrusion: from Theory to Application in Pharmaceutical Formulation

    OpenAIRE

    Patil, Hemlata; Tiwari, Roshan V.; Repka, Michael A.

    2015-01-01

    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, th...

  20. Rapid and Sensitive Determination of Major Active Ingredients and Toxic Components in GinkgoBiloba Leaves Extract (EGb 761) by a Validated UPLC-MS-MS Method.

    Science.gov (United States)

    Wang, Yao; Liu, Yuan; Wu, Qi; Yao, Xin; Cheng, Zongqi

    2017-01-08

    An accurate, precise and sensitive ultra-performance liquid chromatography tandem mass spectrometric (UPLC-MS-MS) method was developed for the determination of flavonoids, terpene lactones, together with ginkgolic acids in Ginkgo biloba leaves extract (EGb 761). This is the first report of the simultaneous analysis of major active ingredients and toxic components in EGb 761 using UPLC-MS-MS. This analysis afforded good linearity, precision, repeatability and accuracy. In addition, the content of those major bioactive components in EGb 761 prepared by different manufacturers of China was determined to establish the effectiveness of the method. The results indicated that the quantification analysis could be readily utilized as a quality control method for EGb 761 and its other related products using flavonoids, terpene lactones and ginkgolic acids as markers.

  1. 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...

  2. 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.

  3. 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

  4. 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.

  5. 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.

  6. The use of atomic spectroscopy in the pharmaceutical industry for the determination of trace elements in pharmaceuticals.

    Science.gov (United States)

    Lewen, Nancy

    2011-06-25

    The subject of the analysis of various elements, including metals and metalloids, in the pharmaceutical industry has seen increasing importance in the last 10-15 years, as modern analytical instrumentation has afforded analysts with the opportunity to provide element-specific, accurate and meaningful information related to pharmaceutical products. Armed with toxicological data, compendial and regulatory agencies have revisited traditional approaches to the testing of pharmaceuticals for metals and metalloids, and analysts have begun to employ the techniques of atomic spectroscopy, such as flame- and graphite furnace atomic absorption spectroscopy (FAAS, Flame AA or FAA and GFAAS), inductively coupled plasma-atomic emission spectroscopy (ICP-AES) and inductively coupled plasma-mass spectrometry (ICP-MS), to meet their analytical needs. Newer techniques, such as laser-induced breakdown spectroscopy (LIBS) and Laser Ablation ICP-MS (LAICP-MS) are also beginning to see wider applications in the analysis of elements in the pharmaceutical industry.This article will provide a perspective regarding the various applications of atomic spectroscopy in the analysis of metals and metalloids in drug products, active pharmaceutical ingredients (API's), raw materials and intermediates. The application of atomic spectroscopy in the analysis of metals and metalloids in clinical samples, nutraceutical, metabolism and pharmacokinetic samples will not be addressed in this work.

  7. Botanical ingredients in cosmeceuticals.

    Science.gov (United States)

    Baumann, Leslie

    2007-11-01

    During the last 10 to 15 years, complementary and alternative medicine (CAM) has become increasingly popular in the US. Within this realm of health care, oral and topical herbal supplements have become some of the most frequently used alternative therapies. Most herbal supplements are based on, or include, several botanical ingredients with long histories of traditional or folk medicine usage. Among the numerous botanical ingredients available on the market today, several are believed to confer dermatologic benefits. This article will focus on a select group of botanical compounds, many of which have long traditions in Asian medicine, with potential or exhibited dermatologic applications, including curcumin, Ginkgo biloba, ginseng, silymarin, soy, and tea tree oil. Other botanical agents, such as arnica, bromelain, chamomile, pomegranate, caffeine, green tea, licorice, and resveratrol, are also briefly considered. Some of these ingredients have been incorporated into topical formulations.

  8. 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.

  9. Oxidation of pharmaceuticals by chlorine dioxide in biologically treated wastewater

    DEFF Research Database (Denmark)

    Hey, G.; Grabic, R.; Ledin, A.

    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......O2, while in high COD effluent a significant increase in API oxidation was observed after treatment with 8mg/L ClO2. This study illustrates the successful degradation of several APIs during treatment of wastewater effluents with chlorine dioxide....

  10. 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

    Front end innovation (FEI) represents the first building blocks of product development, but is often regarded as a weak link in innovation literature. Various theorists emphasize that a firm’s innovation can benefit substantially by improving the front end of innovation process (Reinertsen, 1999......, Steven & Burly, 2003, and Vernorn et al., 2008) and that innovation strategies play a central role in optimization of innovation (Clark & Wheelwright, 1995; Cottam et al., 2001; Morgan & Berthon, 2008). Innovation strategies are suggested in literature (e.g. Page, 1993; Oke, 2002; Adams et al., 2006......; 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...

  11. Grazing-angle fiber-optic fourier transform infrared reflection-absorption spectroscopy for the in situ detection and quantification of two active pharmaceutical ingredients on glass.

    Science.gov (United States)

    Perston, Benjamin B; Hamilton, Michelle L; Williamson, Bryce E; Harland, Peter W; Thomson, Mary A; Melling, Peter J

    2007-02-01

    Fourier transform infrared reflection-absorption spectroscopy has been used with a fiber-optic grazing-angle reflectance probe as a rapid, in situ method for trace surface analysis of acetaminophen and aspirin at loadings of approximately 0-2 microg cm(-2) on glass. Partial least-squares multivariate regression permits the loadings to be quantified, simultaneously, with root-mean-squared errors of prediction of RMSEP approximately 0.1 microg cm(-2) for both compounds. The detection limits are estimated to be LD approximately 0.2 microg cm(-2).

  12. 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

    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...... applications that can be found when exploiting the fast and rich information provided by NIR spectroscopy....

  13. 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.

  14. 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

  15. 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

  16. Effective Teachers for Students with Emotional/Behavioral Disorders: Active Ingredients Leading to Positive Teacher and Student Outcomes

    Science.gov (United States)

    Conroy, Maureen A.; Sutherland, Kevin S.

    2012-01-01

    Teachers of students with emotional/behavioral disorders (E/BD) have varied skills and abilities. Within the field there are some teachers, who teach students with E/BD by actively engaging them in learning tasks and who have few behavior problems in comparison to other teachers, who struggle with classroom management. Many researchers have found…

  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. 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.

  19. Induction of rat hepatic cytochromes P450 by toxic ingredients in plants: lack of correlation between toxicity and inductive activity.

    Science.gov (United States)

    Yamada, H; Nakamura, T; Oguri, K

    1998-12-01

    "Animal-Plant Warfare" is one of the hypotheses for the evolution of drug-metabolizing P450s. To address the validity of this hypothesis, we examined the induction of xenobiotic-metabolizing P450s by 12 plant toxins in rats, using hepatic activity for testosterone metabolism as the index. The compounds tested were aconitine, morphine, tubocurarine, physostigmine, pilocarpine, muscarine, cocaine, atropine, amygdalin, digitonin, nicotine and solanine. Drinking water containing a test compound was given to rats for 4 days, and the hepatic activity of testosterone metabolism was determined together with monitoring body weight gain and liver weight as the indices of toxicity. The results showed that while cocaine and nicotine have a minor ability to increase testosterone 16 beta-hydroxylase activity, a marker activity for the CYP2B1 and 2, all other compounds did not have any such effect. No correlation was observed between a change in 16 beta-hydroxylase and toxicity caused by toxins. Therefore, these results did not support the idea that the inducibility of the CYP2B subfamily in animals is acquired through "Animal-Plant Warfare". Several compounds examined here increased or decreased hepatic activities of testosterone 2 alpha-, 6 beta-, 7 alpha- and 16 alpha-hydroxylation and 17-oxidation, indicating a possible effect on the CYP2A, 2C and 3A subfamily. Of these effects, a moderate correlation (r toxicity. It is therefore suggested that inhibition or suppression of the expression of CYP2C11 is one of the mechanisms in the toxicity of plant toxins for rats, although it comes from an examination using limited numbers of compounds.

  20. 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.

  1. Kinetics of Inhibition of Monoamine Oxidase Using Cymbopogon martinii (Roxb.) Wats.: A Potential Antidepressant Herbal Ingredient with Antioxidant Activity.

    Science.gov (United States)

    Gacche, R N; Shaikh, R U; Chapole, S M; Jadhav, A D; Jadhav, S G

    2011-07-01

    The study was designed to evaluate the antioxidant activity and effect of Cymbopogon martinii (Roxb.) Wats. (Poaceae) leaves on the activity of monoamine oxidase and kinetics of enzyme inhibition. Ethanol extract of C. martinii and rat brain mitochondrial monoamine oxidase preparation ware used to study the kinetics of enzyme inhibition using double reciprocal Lineweaver-Burk plot. The DPPH was used as a source of free radical to evaluate antioxidant potential. It is observed that, the ethanolic extract of C. martinii inhibits the monoamine oxidase activity with competitive mode of inhibition. The V(max) (0.01 mM/min) remained constant while, K(m) varied from 21.00 ± 1.1, 43.33 ± 1.5 and 83.33 ± 1.4 mM for 100-500 μg/ml concentration of C. martinii. The K(i) values were calculated to be 90.00 ± 0.87, 75.00 ± 0.69, 68.18 ± 0.68 μg for 100-500 μg/ml concentration of C. martini. It also shows a significant DPPH (1,1-diphenyl-2-picryl hydrazine) radical scavenging (IC(50) = 0.34 ± 0.05 mg/ml) and reducing activity (IC(50) = 0.70 ± 0.22 mg/ml). The C. martini can be considered as a possible source of MAO inhibitor used in the treatment of depression and other neurological disorders.

  2. 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.

  3. 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

  4. Microencapsulation as a tool for incorporating bioactive ingredients into food.

    Science.gov (United States)

    Kuang, S S; Oliveira, J C; Crean, A M

    2010-11-01

    Microencapsulation has been developed by the pharmaceutical industry as a means to control or modify the release of drug substances from drug delivery systems. In drug delivery systems microencapsulation is used to improve the bioavailability of drugs, control drug release kinetics, minimize drug side effects, and mask the bitter taste of drug substances. The application of microencapsulation has been extended to the food industry, typically for controlling the release of flavorings and the production of foods containing functional ingredients (e.g. probiotics and bioactive ingredients). Compared to the pharmaceutical industry, the food industry has lower profit margins and therefore the criteria in selecting a suitable microencapsulation technology are more stringent. The type of microcapsule (reservoir and matrix systems) produced and its resultant release properties are dependent on the microencapsulation technology, in addition to the physicochemical properties of the core and the shell materials. This review discusses the factors that affect the release of bioactive ingredients from microcapsules produced by different microencapsulation technologies. The key criteria in selecting a suitable microencapsulation technology are also discussed. Two of the most common physical microencapsulation technologies used in pharmaceutical processing, fluidized-bed coating, and extrusion-spheronization are explained to highlight how they might be adapted to the microencapsulation of functional bioactive ingredients in the food industry.

  5. Analysis of bioactive ingredients in the brown alga Fucus vesiculosus by capillary electrophoresis and neutron activation analysis.

    Science.gov (United States)

    Truus, Kalle; Vaher, Merike; Koel, Mihkel; Mähar, Andres; Taure, Imants

    2004-07-01

    Two different types of bioactive components of the seaweed Fucus vesiculosus were analysed: (1) polyphenols (phlorotannins) by capillary electrophoresis (CE) and (2) mineral part (including bioactive microelements) by neutron activation analysis (NAA). CE experiments were carried out using a UV detector (at 210 nm) and an uncoated silica capillary. The best separation was achieved at a voltage of 20 kV using borate or acetate buffer in a methanol/acetonitrile mixture as background electrolyte. The CE analysis data were confirmed by high-performance liquid chromatography (HPLC). Determination of mineral composition of algal biomass by NAA was performed on the basis of various nuclides; the best results (from 38 elements determined) were obtained for Mn, Fe, Zn, As, Br, Sr, I, Ba, Au and Hg.

  6. 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.

  7. 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.

  8. 肉桂降糖活性成分提取方法的研究%Study on cinnamon hypoglycemic active ingredient extraction method

    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% .

  9. Preparation of Fe3O4 Magnetic Surface Imprinted Microspheres and the Ethyl Acetate Extract Flavonoids Raspberry Concentration of Active Ingredient Applied

    Directory of Open Access Journals (Sweden)

    Xie YiHui

    2016-01-01

    Full Text Available the study is used by the co-precipitation method to make some uniform particle size and have good Fe3O4 magnetic nanoparticles and their surface modified with oleic acid ; oleic acid as the carrier of Fe3O4, quercetin as template molecule, prepared by the microwave assisted molecular imprinted polymer magnetic nanospheres; In raspberry ethyl acetate extract fingerprints for the assessment index, with orthogonal design best preparation; Characterization of equilibrium adsorption constant Kd and maximum adsorption capacity Qmax by Scatchard model.The results show that: This study explores the preparation of MIPs polymerization time by ten times, prepared by the Fe3O4 nanometer level, greatly increase the MIPs of the specific surface area, thereby increase the amount of adsorption (Kd = 0.7322mg / L, Qmax = 18.92μmol / g. Successfully extract raspberry flavonoids active ingredients from ethyl acetate which can be used for rapid and large parts of ethyl acetate enrichment raspberry flavonoids.

  10. 臭参活性成分乙酸乙酯部分的分离%Separating the Active Ingredient Ethyl Smelly Reference Section

    Institute of Scientific and Technical Information of China (English)

    栾云鹏; 王启明

    2016-01-01

    The purpose of the experiment:the separation of smelly and the activity of the main ingredients. Methods:prelimi-nary extraction with 95%ethanol by petroleum ether, ethyl acetate extraction, part of the ethyl acetate extract of gradient elution with chloroform, methanol (100:0~70:30). Results:ethyl acetate extraction part of the elution of the A, B, C, D, A total of four parts.%此实验的目的:分离臭参中主要的活性成分。方法:先用95%乙醇初步提取在经过石油醚、乙酸乙酯萃取,把得到的乙酸乙酯萃取的部分用氯仿——甲醇梯度洗脱(100:0~70:30)。结果:乙酸乙酯萃取的部分洗脱出A、B、C、D共4个部分。

  11. 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).

  12. 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.

  13. 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.

  14. Pharmaceutical cocrystals, salts and multicomponent systems; intermolecular interactions and property based design.

    Science.gov (United States)

    Berry, David J; Steed, Jonathan W

    2017-03-23

    As small molecule drugs become harder to develop and less cost effective for patient use, efficient strategies for their property improvement become increasingly important to global health initiatives. Improvements in the physical properties of Active Pharmaceutical Ingredients (APIs), without changes in the covalent chemistry, have long been possible through the application of binary component solids. This was first achieved through the use of pharmaceutical salts, within the last 10-15years with cocrystals and more recently coamorphous systems have also been consciously applied to this problem. In order to rationally discover the best multicomponent phase for drug development, intermolecular interactions need to be considered at all stages of the process. This review highlights the current thinking in this area and the state of the art in: pharmaceutical multicomponent phase design, the intermolecular interactions in these phases, the implications of these interactions on the material properties and the pharmacokinetics in a patient.

  15. Implementation of Supply Chain Management (SCM in pharmaceutical company, general principles and case study

    Directory of Open Access Journals (Sweden)

    Zoran Nakov

    2014-12-01

    Full Text Available Supply Chain Management (SCM in pharmaceutical industry is defined as a “responsible SCM” and its implementation is according to the principles of: business ethics, rights of labor and principles of healthy and safe working environment. Pharmaceutical companies with implemented “responsible SCM” have to use management systems to facilitate continuous improvement in accordance with their working principles. The main purpose of this management system is to ensure the consistency, reliability and continuous improvement of all workflows within an organization.The analyzed case describes the project of European generic pharmaceutical company, which intends to implement best practice SCM operations for five European manufacturing sites and European logistics organizations (active ingredients supply, distribution centers, affiliate customers and third party manufacturers. The main objectives of the project were the creation of the future improved To-Be situation through implementation of new SCM models to the existing To-Day situation.

  16. 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.

  17. 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.

  18. 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.

  19. Adsorption of Selected Pharmaceutical Compounds onto Activated Carbon in Dilute Aqueous Solutions Exemplified by Acetaminophen, Diclofenac, and Sulfamethoxazole.

    Science.gov (United States)

    Chang, E-E; Wan, Jan-Chi; Kim, Hyunook; Liang, Chung-Huei; Dai, Yung-Dun; Chiang, Pen-Chi

    2015-01-01

    The adsorption of three pharmaceuticals, namely, acetaminophen, diclofenac, and sulfamethoxazole onto granular activated carbon (GAC), was investigated. To study competitive adsorption, both dynamic and steady-state adsorption experiments were conducted by careful selection of pharmaceuticals with various affinities and molecular size. The effective diffusion coefficient of the adsorbate was increased with decease in particle size of GAC. The adsorption affinity represented as Langmuir was consistent with the ranking of the octanol-water partition coefficient, K(ow). The adsorption behavior in binary or tertiary systems could be described by competition adsorption. In the binary system adsorption replacement occurred, under which the adsorbate with the smaller K(ow) was replaced by the one with larger K(ow). Results also indicated that portion of the micropores could be occupied only by the small target compound, but not the larger adsorbates. In multiple-component systems the competition adsorption might significantly be affected by the macropores and less by the meso- or micropores.

  20. 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

  1. Systems pharmacology-based approach for dissecting the active ingredients and potential targets of the Chinese herbal Bufei Jianpi formula for the treatment of COPD

    Science.gov (United States)

    Zhao, Peng; Li, Jiansheng; Li, Ya; Tian, Yange; Wang, Yonghua; Zheng, Chunli

    2015-01-01

    Background The Chinese herbal Bufei Jianpi formula (BJF) provides an effective treatment option for chronic obstructive pulmonary disease (COPD). However, the systems-level mechanism underlying the clinical effects of BJF on COPD remains unknown. Methods In this study, a systems pharmacology model based on absorption filtering, network targeting, and systems analyses was applied specifically to clarify the active compounds and therapeutic mechanisms of BJF. Then, a rat model of cigarette smoke- and bacterial infection-induced COPD was used to investigate the therapeutic mechanisms of BJF on COPD and its comorbidity. Results The pharmacological system successfully identified 145 bioactive ingredients from BJF and revealed 175 potential targets. There was a significant target overlap between the herbal constituents of BJF. These results suggested that each herb of BJF connected with similar multitargets, indicating potential synergistic effects among them. The integrated target–disease network showed that BJF probably was efficient for the treatment of not only respiratory tract diseases but also other diseases, such as nervous system and cardiovascular diseases. The possible mechanisms of action of BJF were related to activation of inflammatory response, immune responses, and matrix metalloproteinases, among others. Furthermore, we demonstrated that BJF treatment could effectively prevent COPD and its comorbidities, such as ventricular hypertrophy, by inhibition of inflammatory cytokine production, matrix metalloproteinases expression, and other cytokine production in vivo. Conclusion This study using the systems pharmacology method, in combination with in vivo experiments, helped us successfully dissect the molecular mechanism of BJF for the treatment of COPD and predict the potential targets of the multicomponent BJF, which provides a new approach to illustrate the synergetic mechanism of the complex prescription and discover more effective drugs against COPD

  2. Comprehensive analysis of pharmaceutical products using simultaneous mixed-mode (ion-exchange/reversed-phase) and hydrophilic interaction liquid chromatography.

    Science.gov (United States)

    Kazarian, Artaches A; Nesterenko, Pavel N; Soisungnoen, Phimpha; Burakham, Rodjana; Srijaranai, Supalax; Paull, Brett

    2014-08-01

    Liquid chromatographic assays were developed using a mixed-mode column coupled in sequence with a hydrophilic interaction liquid chromatography column to allow the simultaneous comprehensive analysis of inorganic/organic anions and cations, active pharmaceutical ingredients, and excipients (carbohydrates). The approach utilized dual sample injection and valve-mediated column switching and was based upon a single high-performance liquid chromatography gradient pump. The separation consisted of three distinct sequential separation mechanisms, namely, (i) ion-exchange, (ii) mixed-mode interactions under an applied dual gradient (reversed-phase/ion-exchange), and (iii) hydrophilic interaction chromatography. Upon first injection, the Scherzo SS C18 column (Imtakt) provided resolution of inorganic anions and cations under isocratic conditions, followed by a dual organic/salt gradient to elute active pharmaceutical ingredients and their respective organic counterions and potential degradants. At the top of the mixed-mode gradient (high acetonitrile content), the mobile phase flow was switched to a preconditioned hydrophilic interaction liquid chromatography column, and the standard/sample was reinjected for the separation of hydrophilic carbohydrates, some of which are commonly known excipients in drug formulations. The approach afforded reproducible separation and resolution of up to 23 chemically diverse solutes in a single run. The method was applied to investigate the composition of commercial cough syrups (Robitussin®), allowing resolution and determination of inorganic ions, active pharmaceutical ingredients, excipients, and numerous well-resolved unknown peaks.

  3. Dropwise additive manufacturing of pharmaceutical products for melt-based dosage forms.

    Science.gov (United States)

    Içten, Elçin; Giridhar, Arun; Taylor, Lynne S; Nagy, Zoltan K; Reklaitis, Gintaras V

    2015-05-01

    The US Food and Drug Administration introduced the quality by design approach and process analytical technology guidance to encourage innovation and efficiency in pharmaceutical development, manufacturing, and quality assurance. As part of this renewed emphasis on the improvement of manufacturing, the pharmaceutical industry has begun to develop more efficient production processes with more intensive use of online measurement and sensing, real-time quality control, and process control tools. Here, we present dropwise additive manufacturing of pharmaceutical products (DAMPP) as an alternative to conventional pharmaceutical manufacturing methods. This mini-manufacturing process for the production of pharmaceuticals utilizes drop on demand printing technology for automated and controlled deposition of melt-based formulations onto edible substrates. The advantages of drop-on-demand technology, including reproducible production of small droplets, adjustable drop sizing, high placement accuracy, and flexible use of different formulations, enable production of individualized dosing even for low-dose and high-potency drugs. In this work, DAMPP is used to produce solid oral dosage forms from hot melts of an active pharmaceutical ingredient and a polymer. The dosage forms are analyzed to show the reproducibility of dosing and the dissolution behavior of different formulations.

  4. Removal of pharmaceuticals in biologically treated wastewater by chlorine dioxide or peracetic acid.

    Science.gov (United States)

    Hey, G; Ledin, A; Jansen, J la Cour; Andersen, H R

    2012-01-01

    Removal of six active pharmaceutical ingredients in wastewater was investigated using chlorine dioxide (ClO2) or peracetic acid (PAA) as chemical oxidants. Four non-steroidal anti-inflammatory drugs (ibuprofen, naproxen, diclofenac and mefenamic acid) and two lipid-regulating agents (gemfibrozil and clofibric acid, a metabolite of clofibrate) were used as target substances at 40 microg/L initial concentration. Three different wastewaters types originating from two wastewater treatment plants (WWTPs) were used. One wastewater was collected after extended nitrogen removal in activated sludge, one after treatment with high-loaded activated sludge without nitrification, and one from the final effluent from the same plant where nitrogen removal was made in trickling filters for nitrification and moving-bed biofilm reactors for denitrification following the high-loaded plant. Of the six investigated compounds, only clofibric acid and ibuprofen were not removed when treated with ClO2 up to 20 mg/L. With increasing PAA dose up to 50 mg/L, significant removal of most of the pharmaceuticals was observed except for the wastewater with the highest chemical oxygen demand (COD). This indicates that chemical oxidation with ClO2 could be used for tertiary treatment at WWTPs for active pharmaceutical ingredients, whereas PAA was not sufficiently efficient.

  5. 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.

  6. 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.

  7. 21 CFR 310.529 - Drug products containing active ingredients offered over-the-counter (OTC) for oral use as insect...

    Science.gov (United States)

    2010-04-01

    ... offered over-the-counter (OTC) for oral use as insect repellents. 310.529 Section 310.529 Food and Drugs... ingredients offered over-the-counter (OTC) for oral use as insect repellents. (a) Thiamine hydrochloride... insect repellent (an orally administered drug product intended to keep insects away). There is a lack...

  8. Salt forms of the pharmaceutical amide dihydrocarbamazepine.

    Science.gov (United States)

    Buist, Amanda R; Kennedy, Alan R

    2016-02-01

    Carbamazepine (CBZ) is well known as a model active pharmaceutical ingredient used in the study of polymorphism and the generation and comparison of cocrystal forms. The pharmaceutical amide dihydrocarbamazepine (DCBZ) is a less well known material and is largely of interest here as a structural congener of CBZ. Reaction of DCBZ with strong acids results in protonation of the amide functionality at the O atom and gives the salt forms dihydrocarbamazepine hydrochloride {systematic name: [(10,11-dihydro-5H-dibenzo[b,f]azepin-5-yl)(hydroxy)methylidene]azanium chloride, C15H15N2O(+)·Cl(-)}, dihydrocarbamazepine hydrochloride monohydrate {systematic name: [(10,11-dihydro-5H-dibenzo[b,f]azepin-5-yl)(hydroxy)methylidene]azanium chloride monohydrate, C15H15N2O(+)·Cl(-)·H2O} and dihydrocarbamazepine hydrobromide monohydrate {systematic name: [(10,11-dihydro-5H-dibenzo[b,f]azepin-5-yl)(hydroxy)methylidene]azanium bromide monohydrate, C15H15N2O(+)·Br(-)·H2O}. The anhydrous hydrochloride has a structure with two crystallographically independent ion pairs (Z' = 2), wherein both cations adopt syn conformations, whilst the two hydrated species are mutually isostructural and have cations with anti conformations. Compared to neutral dihydrocarbamazepine structures, protonation of the amide group is shown to cause changes to both the molecular (C=O bond lengthening and C-N bond shortening) and the supramolecular structures. The amide-to-amide and dimeric hydrogen-bonding motifs seen for neutral polymorphs and cocrystalline species are replaced here by one-dimensional polymeric constructs with no direct amide-to-amide bonds. The structures are also compared with, and shown to be closely related to, those of the salt forms of the structurally similar pharmaceutical carbamazepine.

  9. [Pharmaceutical technology and pharmaceutical care in the dispensary].

    Science.gov (United States)

    Remon, J P

    2007-01-01

    In this lecture the science 'Pharmaceutical Technology' was briefly elucidated, but the main part was about the concept of 'Pharmaceutical Care' in the community pharmacy. Pharmaceutical Care aims at ensuring a safe, efficacious, and cost-effective pharmacotherapy. Thus the pharmacist tries--in collaboration with other healthcare professionals --to improve the clinical and humanistic outcomes of the therapy. Moreover, an efficacious and rational drug therapy is cost-saving, for the patient as well as for the health insurer. A pharmacist delivering Pharmaceutical Care not only dispenses medication, but also takes responsibility about the outcome of the drug therapy. Pharmaceutical Care in community pharmacies encompasses the following activities: Advice about prescribed drugs, to ensure that patients take their medication as correct, as safe and as compliant as possible. Advice about self-care: counselling about OTC-medication. Prevention of medication errors, for example drug interactions. Pay attention to prevention of diseases: for example stimulation of vaccination. Collaboration with physicians, especially general practitioners, both aiming at an optimal drug therapy for the patient Pharmaceutical Care in the hospital setting ('Clinical Pharmacy'): clinical pharmacists participate in drawing up, evaluating and following up the pharmacotherapy of every individual patient, in close collaboration with physicians, nurses and other healthcare professionals on the ward. In Belgium Pharmaceutical Care is in the making. Scientific research on this topic is carried out by the Pharmaceutical Care Unit of Ghent University. An overview of their ongoing research projects was given. Finally, the problems encountered with the implementation of Pharmaceutical Care were highlighted.

  10. 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.

  11. 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)

  12. Systems pharmacology-based approach for dissecting the active ingredients and potential targets of the Chinese herbal Bufei Jianpi formula for the treatment of COPD

    Directory of Open Access Journals (Sweden)

    Zhao P

    2015-12-01

    Full Text Available Peng Zhao,1,2 Jiansheng Li,1,2 Ya Li,1,2 Yange Tian,1,2 Yonghua Wang,2,3 Chunli Zheng3 1Key Laboratory of Chinese Internal Medicine, Henan University of Traditional Chinese Medicine, 2Key Laboratory of Chinese Internal Medicine, Collaborative Innovation Center for Respiratory Disease Diagnosis and Treatment and Chinese Medicine Development of Henan Province, Zhengzhou, 3Center of Bioinformatics, College of Life Science, Northwest A&F University, Yangling, People’s Republic of China Background: The Chinese herbal Bufei Jianpi formula (BJF provides an effective treatment option for chronic obstructive pulmonary disease (COPD. However, the systems-level mechanism underlying the clinical effects of BJF on COPD remains unknown. Methods: In this study, a systems pharmacology model based on absorption filtering, network targeting, and systems analyses was applied specifically to clarify the active compounds and therapeutic mechanisms of BJF. Then, a rat model of cigarette smoke- and bacterial infection-induced COPD was used to investigate the therapeutic mechanisms of BJF on COPD and its comorbidity. Results: The pharmacological system successfully identified 145 bioactive ingredients from BJF and revealed 175 potential targets. There was a significant target overlap between the herbal constituents of BJF. These results suggested that each herb of BJF connected with similar multitargets, indicating potential synergistic effects among them. The integrated target–disease network showed that BJF probably was efficient for the treatment of not only respiratory tract diseases but also other diseases, such as nervous system and cardiovascular diseases. The possible mechanisms of action of BJF were related to activation of inflammatory response, immune responses, and matrix metalloproteinases, among others. Furthermore, we demonstrated that BJF treatment could effectively prevent COPD and its comorbidities, such as ventricular hypertrophy, by inhibition

  13. Antioxidative activities of white rose flower extract and pharmaceutical advantages of its hexane fraction via free radical scavenging effects.

    Science.gov (United States)

    Park, Dongsun; Jeon, Jeong Hee; Kwon, Sang-Chul; Shin, Sunhee; Jang, Ja Young; Jeong, Heon Sang; Lee, Do Ik; Kim, Yun-Bae; Joo, Seong Soo

    2009-12-01

    In this study, we determined the antioxidant activities of two different solvent fractions(butanol and hexane) obtained from white Rosa rugosa flowers by employing various assays such as 2,2-diphenyl-1-picrylhydrazyl hydrate (DPPH), 2,2'-azino-bis(3-ethylbenzthiazoline-6-sulfonic acid) (ABTS) radical scavenging activity, and nitric oxide (NO) scavenging and inhibition activity in S-nitroso-N-acetylpenicillamine (SNAP) in the RAW264.7 model. In addition, more advanced antioxidant assays were conducted, including lipid peroxidation, hydroxyl radical-mediated oxidation, DNA fragmentation, apoptosis, and cell growth. The results revealed that the hexane fraction, which contained a significant amount of polyphenols and volatile components, had excellent antioxidant potency and could scavenge free radicals of DPPH and ABTS. Interestingly, the hexane fraction inhibited lipid peroxidation to almost the same degree as a chemical antioxidant. In the NO assay, the hexane fraction effectively scavenged free radicals at all dose ranges and is expected to inhibit NO production in mammalian cells. The hexane fraction effectively prevented oxidative damage, which was induced by Cu2+/H2O2, to target proteins at lower concentrations (>1 microg x mL(-1)). The DNA fragmentation and the cell-level assays suggest that the hexane fraction may play a crucial role in inhibiting peroxynitrite and H2O2 attack. Based on the findings described in this study, the hexane fraction holds promise for use as a novel pharmaceutical antioxidant.

  14. Simultaneous determination of ranitidine and metronidazole in pharmaceutical formulations at poly(chromotrope 2B modified activated glassy carbon electrodes

    Directory of Open Access Journals (Sweden)

    Xiaobo Li

    2014-09-01

    Full Text Available A simple and sensitive electrochemical method for the simultaneous and quantitative detection of ranitidine (RT and metronidazole (MT was developed, based on a poly(chromotrope 2B modified activated glassy carbon electrode (PCHAGCE. The PCHAGCE showed excellent electrocatalytic activity toward the reduction of both RT and MT in 0.1 mol/L phosphate buffer solution (pH 6.0. The peak-to-peak separations for the simultaneous detection of RT and MT between the two reduction waves in cyclic voltammetry were increased significantly from ∼0.1 V at activated GCE, to ∼0.55 V at PCHAGCE. By differential pulse voltammetry techniques, the reduction peak currents of RT and MT were both linear over the range of 1.0 × 10−5–4.0×10−4 mol/L. The detection limits (S/N = 3 were 5.4 × 10−7 mol/L and 3.3 × 10−7 mol/L for RT and MT, respectively. The modified electrode was successfully applied to the determination of RT and MT in pharmaceutical preparations and human serum as real samples with stable and reliable recovery data.

  15. 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.

  16. 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.

  17. 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.

  18. 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.

  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. Utility of Activated Glassy Carbon and Pencil Graphite Electrodes for Voltammetric Determination of Nalbuphine Hydrochloride in Pharmaceutical and Biological Fluids

    Directory of Open Access Journals (Sweden)

    Hoda M. Elqudaby

    2016-01-01

    Full Text Available This work compares voltammetric response of nalbuphine hydrochloride (NP·HCl at both activated glassy carbon and pencil graphite electrodes. The electrochemical oxidation of the drug was studied using cyclic voltammetry (CV, differential pulse voltammetry (DPV, and square wave voltammetry (SWV techniques. For analytical purpose a well-resolved irreversible diffusion controlled voltammetric peak was established in Britton-Robinson (B-R buffer solution of pH 6.00 using pencil graphite electrode (PGE. Using activated glassy carbon electrode (GCE a well-resolved irreversible diffusion controlled voltammetric peak was obtained at pH 7.00 using the same buffer solution. According to the linear relationship between the peak current and NP·HCl concentration, DPV and SWV methods were developed for their quantitative determination in pharmaceutical and human biological fluids. The linear response was obtained in the range from 1.6×10-5 to 1.5×10-4 mol L−1 using PGE and from 12.5×10-6 to 13.75×10-5 mol L−1 using a GC electrode, respectively. Precision and accuracy of the developed method were checked by recovery studies.

  1. Factory-discharged pharmaceuticals could be a relevant source of aquatic environment contamination: review of evidence and need for knowledge.

    Science.gov (United States)

    Cardoso, Olivier; Porcher, Jean-Marc; Sanchez, Wilfried

    2014-11-01

    Human and veterinary active pharmaceutical ingredients (APIs) are involved in contamination of surface water, ground water, effluents, sediments and biota. Effluents of waste water treatment plants and hospitals are considered as major sources of such contamination. However, recent evidences reveal high concentrations of a large number of APIs in effluents from pharmaceutical factories and in receiving aquatic ecosystems. Moreover, laboratory exposures to these effluents and field experiments reveal various physiological disturbances in exposed aquatic organisms. Also, it seems to be relevant to increase knowledge on this route of contamination but also to develop specific approaches for further environmental monitoring campaigns. The present study summarizes available data related to the impact of pharmaceutical factory discharges on aquatic ecosystem contaminations and presents associated challenges for scientists and environmental managers.

  2. 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.

  3. 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.

  4. [Spectral Analysis about the Pharmaceutical Cocrystal Formation of Piracetam and 3-Hydroxybenzoic Acid].

    Science.gov (United States)

    Zhang, Hui-li; Xia, Yi; Hong, Zhi; Du, Yong

    2015-07-01

    Pharmaceutical cocrystal can improve physical and chemical properties of active pharmaceutical ingredient (API), meanwhile this feature has shown great potential in improving the pharmaceutical's properties and characteristics. In this study, cocrystal formation between piracetam and 3-hydroxybenzoic acid (3HBA) using grinding method has been characterized by Fourier transform infrared (FTIR), Raman and terahertz (THz) spectroscopical techniques. The vibrational modes of different motions are obtained by the assignment of the peaks in the spectra of the starting materials and the cocrystal components. FTIR, Raman and THz spectroscopical results show that the vibrational modes of the cocrystal are different from those of the starting materials. In addition, the dynamic process of the above cocrystal formation is investigated in-depth with Raman and THz spec- tra. Piracetam-3HBA cocrystal is formed pretty fast in first several minutes, and then the formation rate becomes slow. After 35 minutes, such formation process has been completed. The results offer the theoretical benchmark and unique means for real-time monitoring pharmaceutical cocrystal formation and also the corresponding quantitative analysis in the pharmaceutical field.

  5. Impact of humic acid fouling on membrane performance and transport of pharmaceutically active compounds in forward osmosis.

    Science.gov (United States)

    Xie, Ming; Nghiem, Long D; Price, William E; Elimelech, Menachem

    2013-09-01

    The impact of humic acid fouling on the membrane transport of two pharmaceutically active compounds (PhACs) - namely carbamazepine and sulfamethoxazole - in forward osmosis (FO) was investigated. Deposition of humic acid onto the membrane surface was promoted by the complexation with calcium ions in the feed solution and the increase in ionic strength at the membrane surface due to the reverse transport of NaCl draw solute. The increase in the humic acid deposition on the membrane surface led to a substantial decrease in the membrane salt (NaCl) permeability coefficient but did not result in a significant decrease in the membrane pure water permeability coefficient. As the deposition of humic acid increased, the permeation of carbamazepine and sulfamethoxazole decreased, which correlated well with the decrease in the membrane salt (NaCl) permeability coefficient. It is hypothesized that the hydrated humic acid fouling layer hindered solute diffusion through the membrane pore and enhanced solute rejection by steric hindrance, but not the permeation of water molecules. The membrane water and salt (NaCl) permeability coefficients were fully restored by physical cleaning of the membrane, suggesting that humic acid did not penetrate into the membrane pores.

  6. 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.

  7. 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.

  8. 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

  9. Combination of electrochemical, spectrometric and other analytical techniques for high throughput screening of pharmaceutically active compounds.

    Science.gov (United States)

    Suzen, Sibel; Ozkan, Sibel A

    2010-08-01

    Recently, use of electrochemistry and combination of this method with spectroscopic and other analytical techniques are getting one of the important approaches in drug discovery and research as well as quality control, drug stability, determination of physiological activity, measurement of neurotransmitters. Many fundamental physiological processes are depending on oxido-reduction reactions in the body. Therefore, it may be possible to find connections between electrochemical and biochemical reactions concerning electron transfer pathways. Applications of electrochemical techniques to redox-active drug development and studies are one of the recent interests in drug discovery. In this review, the latest developments related to the use of electrochemical techniques in drug research in order to evaluate possible combination spectrometric methods with electrochemical techniques.

  10. 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.

  11. 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。

  12. Antioxidant Activities, Metabolic Profiling, Proximate Analysis, Mineral Nutrient Composition of Salvadora persica Fruit Unravel a Potential Functional Food and a Natural Source of Pharmaceuticals

    Science.gov (United States)

    Kumari, Asha; Parida, Asish K.; Rangani, Jaykumar; Panda, Ashok

    2017-01-01

    Salvadora persica is a medicinally important plant mainly used in oral hygiene. However, little attention has been given towards the nutritional prominence of this plant. This study encloses the proximate and mineral nutrient contents, amino acid composition, metabolite profiling and antioxidant potential of S. persica fruit. The ripen fruit contained substantial amount of sugars, mineral nutrients, carotenoids, polyphenols and flavonoids. The metabolic profiling of the fruit extract by GC-MS revealed a total of 22 metabolites comprising of sugars, sugar alcohols, organic acids, organic base, and aromatic silica compound. The identified metabolites have been previously reported to have potential antioxidant, antimicrobial, anti-hyperglycemic, and antitumor properties. The GC-MS analysis indicated high glucose and glucopyranose (247.62 and 42.90 mg g-1 FW respectively) contents in fruit of S. persica. The fruit extract demonstrated a significantly higher antioxidant and ROS scavenging properties along with high contents of mineral nutrients and essential amino acids. HPLC analysis revealed presence of essential and non-essential amino acid required for healthy body metabolism. The cysteine was found to be in highest amount (733.69 mg 100 g-1 DW) among all amino acids quantified. Specifically, compared to similar medicinal plants, previously reported as a source of non-conventional food and with some of the commercially important fruits, S. persica fruit appears to be a potential source of essential mineral nutrients, amino acids, vitamins (ascorbic acid and carotenoid) and pharmaceutically important metabolites contributing towards fulfilling the recommended daily requirement of these for a healthy human being. This is the first report establishing importance of S. persica fruit as nutraceuticals. The data presented here proposed that fruit of S. persica may be used as functional food or reinvigorating ingredient for processed food to reduce deficiency of nutrients

  13. Inter- and intra-manufacturer variability in pharmaceutical grades and lots of xanthan gum.

    Science.gov (United States)

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

    2010-12-01

    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 compendial standards to monitor and control the variability of excipients, this study focuses on the adequacy of the NF specifications, in particular the viscosity specification, to discern the variability in solution properties of different pharmaceutical grades and lots of xanthan gum. All the grades and lots in this study were NF grade materials. Xanthan gum solutions were prepared in accordance with NF test methodology and were rheologically evaluated using a rotational rheometer. Both steady shear measurements and small amplitude oscillatory measurements were carried out on 1% w/w xanthan gum solutions. Results showed significant inter- and intra-manufacturer variability among the NF grades and lots of xanthan gum that was not reflected in the NF viscosity test specifications.

  14. The contribution of oxazolidinone frame to the biological activity of pharmaceutical drugs and natural products.

    Science.gov (United States)

    Zappia, Giovanni; Menendez, Pilar; Monache, Giuliano Delle; Misiti, Domenico; Nevola, Laura; Botta, Bruno

    2007-04-01

    The development of resistance by the antibiotics in the Gram-positive pathogenic bacteria over the last twenty years and continuing today has created a need for new antibiotic classes, which may be unaffected by existing bacterial resistance. The oxazolidin-2-ones represent not only a new class with a novel mechanism of action, but also satisfy the requirement for overcoming the resistance mechanisms. Both linezolid and eperozolid, the first chemical candidates, arose from the piperazine subclass, with the first one being chosen further development because of its enhanced pharmacokinetic properties. The main attractive traits of the oxazolidinone series has encouraged further work in the area, and the patent literature reveals that extensive chemical investigation is currently being made. The unexpected early resistance development emphasizes the need for further exploration of features of the oxazolidinone to eliminate these deficiencies. Recently, several changes, involving the C5 side chain as well the N-phenyl heterocyclic ring, give promise for such improvement. Oxazolidinone antibacterial agents comprise also ketolides, derivatives of macrolides, such as erythromycin A, with a newly formed carbamate cycle, with a largely unexplored potential. The oxazolidinone nucleus does not appear only in the structures of antimicrobial drugs, but a number of biological activities are connected with frameworks including the oxazolidinone ring. A partial list of these activities comprises enzyme inhibitors, agonists and antagonists, with a particular citation for a new generation of selective monoamino oxidase inhibitors (befloxatone). The oxazolidinone moiety was found in the structure of few biologically active natural products, such as (-)-cytoxazone and streptazolin. Moreover, in some cases the oxazolidinone ring has been chosen for the preparation of isosteric aza analogues of natural compounds (podophyllotoxin, pilocarpine) that can be more easily synthesised and more

  15. Separation of cold medicine ingredients using a precise MEKC method at elevated pH.

    Science.gov (United States)

    Hasemann, Phillip; ter Balk, Marieke; Preu, Lutz; Wätzig, Hermann

    2007-06-01

    An MEKC method was developed in order to separate a cold medicine formulation containing acetaminophen, ephedrine sulfate, doxylamine succinate, and dextromethorphan hydrobromide as active pharmaceutical ingredients. Because of their similar physical and chemical properties, it was a challenge to separate the basic compounds without sample pretreatment. In addition, the high content of alcohol and sucrose together with the variety of further excipients had to be considered. Thus, the complex matrix required several optimization steps. These included the search for the optimum pH and for a suitable sodium dodecyl sulfate concentration to avoid matrix-capillary wall interaction and to ensure precision. As a second developing step, an internal standard (benzocaine) was chosen to guarantee a high level of quantitative performance. An RSD% value of the peak areas between 1.0 and 2.0 was reached. The employed method development strategy can be generalized to similar separation approaches in the future.

  16. Study on the in vitro Antimicrobial Activities of Some Spice Essential Oils and Their Ingredients%香辛料精油及单体的体外抑菌活性研究

    Institute of Scientific and Technical Information of China (English)

    张海江; 王向红; 毛宇豪; 孙佳

    2014-01-01

    The in vitro antimicrobial activities of spice essential oils including Cinnamomum Verum, Syringa oblata, 0riganum vulgare L.and their main ingredients were studied using filter-paper and serial two-fold methods.The common food-borne pathogens and spoilage bacteria including E.coli, staphylococcus aureus, Salmonella, Shigella, S.cerevisiae and B.subtilis were employed as the test strains.Furthermore, the effect of pH value on the antimicrobial activity was investigated.The results indicated that all the spice essential oils and their ingredients showed good in vitro antibacterial activities against all the microbials and the acidic conditions could strengthen the activities of Cinnamomum Verum, Syringa oblata essential oil and their ingredients.%采用滤纸片法和溶液二倍稀释法研究肉桂、丁香、牛至等天然香辛料精油及其单体对大肠杆菌、金黄色葡萄球菌、沙门氏菌、志贺菌、枯草芽孢杆菌等常见食源性致病菌、腐败菌的体外抑菌活性,并考察了pH值对抑菌活性的影响。结果表明各精油及其单体对各菌株均具有良好的体外抑制作用,酸性条件有利于增强肉桂、丁香精油及其单体的抑菌活性。

  17. 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.

  18. Adsorption characteristics of selected pharmaceuticals and an endocrine disrupting compound-Naproxen, carbamazepine and nonylphenol-on activated carbon.

    Science.gov (United States)

    Yu, Zirui; Peldszus, Sigrid; Huck, Peter M

    2008-06-01

    The adsorption of two representative pharmaceutically active compounds (PhACs) (naproxen and carbamazepine) and one endocrine disrupting compound (nonylphenol) were evaluated on two types of activated carbon. When determining their isotherms at environmentally relevant concentration levels, it was found that at this low concentration range (10-800 ng/L), removals of the target compounds were contrary to expectations based on their hydrophobicity. Nonylphenol (log K(ow) 5.8) was most poorly adsorbed, whereas carbamazepine (log K(ow) 2.45) was most adsorbable. Nonylphenol Freundlich isotherms at this very low concentration range had a much higher 1/n compared to isotherms at much higher concentrations. This indicates that extrapolation from an isotherm obtained at a high concentration range to predict the adsorption of nonylphenol at a concentration well below the range of the original isotherm, leads to a substantial overestimation of its removals. Comparison of isotherms for the target compounds to those for other conventional micropollutants suggested that naproxen and carbamazepine could be effectively removed by applying the same dosage utilized to remove odorous compounds (geosmin and MIB) at very low concentrations. The impact of competitive adsorption by background natural organic matter (NOM) on the adsorption of the target compounds was quantified by using the ideal adsorbed solution theory (IAST) in combination with the equivalent background compound (EBC) approach. The fulfilment of the requirements for applying the simplified IAST-EBC model, which leads to the conclusion that the percentage removal of the target compounds at a given carbon dosage is independent of the initial contaminant concentration, was confirmed for the situation examined in the paper. On this basis it is suggested that the estimated minimum carbon usage rates (CURs) to achieve 90% removal of these emerging contaminants would be valid at concentrations of less than 500 ng/L in

  19. 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

  20. [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).

  1. An iterative approach for compound detection in an unknown pharmaceutical drug product: Application on Raman microscopy.

    Science.gov (United States)

    Boiret, Mathieu; Gorretta, Nathalie; Ginot, Yves-Michel; Roger, Jean-Michel

    2016-02-20

    Raman chemical imaging provides both spectral and spatial information on a pharmaceutical drug product. Even if the main objective of chemical imaging is to obtain distribution maps of each formulation compound, identification of pure signals in a mixture dataset remains of huge interest. In this work, an iterative approach is proposed to identify the compounds in a pharmaceutical drug product, assuming that the chemical composition of the product is not known by the analyst and that a low dose compound can be present in the studied medicine. The proposed approach uses a spectral library, spectral distances and orthogonal projections to iteratively detect pure compounds of a tablet. Since the proposed method is not based on variance decomposition, it should be well adapted for a drug product which contains a low dose product, interpreted as a compound located in few pixels and with low spectral contributions. The method is tested on a tablet specifically manufactured for this study with one active pharmaceutical ingredient and five excipients. A spectral library, constituted of 24 pure pharmaceutical compounds, is used as a reference spectral database. Pure spectra of active and excipients, including a modification of the crystalline form and a low dose compound, are iteratively detected. Once the pure spectra are identified, multivariate curve resolution-alternating least squares process is performed on the data to provide distribution maps of each compound in the studied sample. Distributions of the two crystalline forms of active and the five excipients were in accordance with the theoretical formulation.

  2. 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.

  3. 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.

  4. 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

  5. 酸枣仁抗氧化成分的分离及其相互作用研究%Separation and Interaction of the Ingredients of Antioxidant Activities in Zizyphi Spinosi Semen

    Institute of Scientific and Technical Information of China (English)

    丁轲; 马崟松; 韩涛; 陈湘宁

    2013-01-01

    In order to study the antioxidant activity of Zizyphi Spinosi Semen (ZSS) which is known as a traditional Chinese herb for treatment of insomnia and anxiety, extracts of ZSS was extracted by ethyl acetate, separated by polyamide resin and isolated by C18 reverse-phase medium, orderly. The antioxidant activity of products obtained from each step was measured. The extracts of ethyl acetate, fraction B and 6' '-feruloylspinosin have the best antioxidant activity. At the same time, other two effective ingredients zizyphusine and spinosin were also separated. The antioxidant activity of the three effective ingredients was measured. The antioxidant activity was also studied by mixing zizyphusine, spinosin and 6' '-feruloylspinosin with different proportions. The results prove that the three ingredients have antagonistic effect on both the removal of free radical DPPH and total antioxidant capacity. But they have synergistic effect on chelating with metal ions. The results show that the flavone is the effective part of ZSS for the antioxidant activity, 6' '-feruloylspinosin is the ingredient of flavone in ZSS with the best antioxidant activity. However antagonistic effect on antioxidant activity of ZSS exists among the ingredients of flavone in ZSS .%为了研究酸枣仁这种传统中药的抗氧化活性,采用多项抗氧化活性指标进行评价,通过活性追踪,酸枣仁提取物依次经过乙酸乙酯萃取,聚酰胺树脂分离和 C18反相快速制备色谱分离,顺次得到抗氧化活性最好的萃取物、馏分B和黄酮组分6''-阿魏酰斯皮诺素,同时还分离得到另外两个组分斯皮诺素和酸李碱。在进一步比较了三种组分酸李碱、斯皮诺素与6''-阿魏酰斯皮诺素抗氧化活性的基础上,将三种组分按照不同配比混合后进行了抗氧化活性的研究,证明这三种物质在清除DPPH自由基的反应中呈现拮抗作用,在总抗氧化能力的反应中为拮抗作用,而在与

  6. Difficulties in the production of identical drug products from a pharmaceutical technology viewpoint.

    Science.gov (United States)

    Genazzani, Armando A; Pattarino, Franco

    2008-01-01

    Generic products reduce healthcare expenditure and create market competition, and it is broadly assumed that these drugs are identical to the original branded reference drug product. In practice, despite legislation demanding demonstration of pharmaceutical equivalence and bioequivalence, thereby ensuring the safety and efficacy of the product, generic products can differ significantly from the reference drug and amongst themselves, particularly in terms of pharmacokinetic properties. These differences most often relate to pharmaceutical technical differences in production of the active principle ingredient (e.g. different crystalline forms or particle size), to use of excipients (such as sugars) or to the manufacturing process itself (such as tablet manufacture). Furthermore, from the patient's perspective, changing from branded to generic drugs can give rise to concerns about switching. Although sufficient safeguards exist to ensure patient safety and generic drug efficacy, it should not be assumed that all generics are entirely identical.

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

    Directory of Open Access Journals (Sweden)

    Rath Kalyani

    2011-08-01

    Full Text Available 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 in combating many diseases and as therapeutic agents. In addition to this their role as antiadhesive agents against several disease causing pathogens makes their utility as suitable antiadhesive coating agents for medical insertional materials which helps in the reduction in a large number of hospital infections without the use of synthetic drugs and chemicals. This review looks at the various pharmaceutical, biomedical and therapeutic perspectives on biosurfactant applications.

  8. Multicomponent chemical imaging of pharmaceutical solid dosage forms with broadband CARS microscopy.

    Science.gov (United States)

    Hartshorn, Christopher M; Lee, Young Jong; Camp, Charles H; Liu, Zhen; Heddleston, John; Canfield, Nicole; Rhodes, Timothy A; Hight Walker, Angela R; Marsac, Patrick J; Cicerone, Marcus T

    2013-09-03

    We compare a coherent Raman imaging modality, broadband coherent anti-Stokes Raman scattering (BCARS) microscopy, with spontaneous Raman microscopy for quantitative and qualitative assessment of multicomponent pharmaceuticals. Indomethacin was used as a model active pharmaceutical ingredient (API) and was analyzed in a tabulated solid dosage form, embedded within commonly used excipients. In comparison with wide-field spontaneous Raman chemical imaging, BCARS acquired images 10× faster, at higher spatiochemical resolution and with spectra of much higher SNR, eliminating the need for multivariate methods to identify chemical components. The significant increase in spatiochemical resolution allowed identification of an unanticipated API phase that was missed by the spontaneous wide-field method and bulk Raman spectroscopy. We confirmed the presence of the unanticipated API phase using confocal spontaneous Raman, which provided spatiochemical resolution similar to BCARS but at 100× slower acquisition times.

  9. 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...... wastewater treatment plants (WWTP) were spiked with 42 APIs (nominal concentration 1μg/L) and treated with different O3 doses (0.5–12.0mg/L ozone) in bench-scale experiments.In order to compare the sensitivity of APIs in each matrix, the specific dose of ozone required to achieve reduction by one decade...... of each investigated API (DDO3) was determined for each effluent by fitting a first order equation to the remaining concentration of API at each applied ozone dose. Ozone dose requirements were found to vary significantly between effluents depending on their matrix characteristics.The specific ozone dose...

  10. Protic pharmaceutical ionic liquids and solids: aspects of protonics.

    Science.gov (United States)

    Stoimenovski, Jelena; Dean, Pamela M; Izgorodina, Ekaterina I; MacFarlane, Douglas R

    2012-01-01

    A series of new protic compounds based on active pharmaceutical ingredients have been synthesised and characterised. Some of the salts synthesised produced ionic liquids, while others that were associated with rigid molecular structures tended to produce high melting points. The "protonic" behaviour of these compounds was found to be a major determinant of their properties. Indicator studies, FTIR-ATR and transport properties (Walden plot) were used to probe the extent of proton transfer and ion association in these ionic liquids. While proton transfer was shown to have taken place in all cases, the Walden plot indicated strong ion association in the primary amine based examples due to hydrogen bonding. This was further explored via crystal structures of related compounds, which showed that extended hydrogen bonded clusters tend to form in these salts. These clusters may dictate membrane transport properties of these compounds in vivo.

  11. 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.

  12. [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".

  13. TECHNOLOGICAL BASIS FOR THE CREATION OF IMPLANTS WITH A PHARMACEUTICAL COMPOSITION OF CIPROFLOXACIN AND THEIR ANTIMICROBIAL ACTIVITY IN EXPERIMENTS IN VITRO

    Directory of Open Access Journals (Sweden)

    V. V. Sheykin

    2016-01-01

    Full Text Available The article is devoted to the investigation of the possibility of immobilized on the surface of the titanium implantable devices (model plates, “U-shaped” brackets antimicrobial substances.Material and methods. The object of research were modeling titanium plates and titanium “U-shaped” brackets for implantation. Ciprofloxacin, hydroxypropylmethylcellulose and methylcellulose has been proposed as materials for the creation of antimicrobial pharmaceutical composition to immobilization. The antimicrobial properties of titanium implantable “U-shaped” brackets with ciprofloxacin was evaluated for potential antimicrobial activity against medically important bacterial (S. aureus, P. aeruginosa, E. coli, E. faecalis and S. pyogenes using method of diffusion in agar. Results. The results showed the possibility of putting and holding а ciprofloxacin in grooves on the modified surface of titanium implants. In the course of the study was developed a pharmaceutical composition, comprising ciprofloxacin and hydroxypropylmethylcellulose. The results showed high antimicrobial activity of pharmaceutical composition with ciprofloxacin against the test organisms (S. aureus, P. aeruginosa, E. coli, E. faecalis and S. pyogenes.

  14. 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.

  15. 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

  16. 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.

  17. 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...

  18. 黄秋葵茶叶的成分分析及其水提物的抗氧化活性测定%Ingredient analysis and antioxidant activity of water extract of Abelmoschus esculentus tea

    Institute of Scientific and Technical Information of China (English)

    周兆祥; 白石琦; 邹烨; 冯伟伟; 赵婷; 王鑫彤; 朱昀; 张漪静; 仰榴青

    2015-01-01

    目的:对黄秋葵茶叶营养成分和活性成分进行分析,并对其水提取物进行抗氧化活性测定。方法:采用国标法和农业行业标准方法分析黄秋葵茶叶的营养成分和活性成分,同时测定其水提物对 DPPH 自由基、羟自由基的清除作用。结果:黄秋葵茶叶(以干基计)中灰分含量为15.32%,粗蛋白含量为27.58%,粗脂肪含量为2.27%,总糖含量为12.06%;氨基酸分析结果表明,黄秋葵茶叶含有多种人体必需氨基酸;元素分析结果表明,黄秋葵茶叶中含有丰富的钾、钙、镁、铁等元素;活性成分黄酮和多糖的含量分别为1.36%和4.70%。黄秋葵茶叶水提物清除 DPPH 自由基、羟自由基的半数抑制浓度分别为156.8 mg/L 和674.5 mg/L。结论:黄秋葵茶叶具有较好的营养价值和抗氧化保健功能,为消费者提供了一种新型的绿色健康饮品。%Objective:To analyze nutritional ingredient and active ingredient of Abelmoschus esculentus tea,and study on antioxidant activity of water extract.Methods:To analyze nutritional ingredient and ac-tive ingredient of Abelmoschus esculentus tea with GB method and agriculture standard method.Scavenging effects of water extract on DPPH and OH were determined.Results:The content of ash ,crude protein, crude fat and total carbohydrate were 1 5.32%,27.58%,2.27% and 1 2.06% of dried sample,respective-ly.The amino acid analysis results showed that Abelmoschus esculentus tea contained many kinds of essential amino acid.The trace element analysis results showed that Abelmoschus esculentus tea contained K,Ca,Mg, Fe,et al.The active ingredient flavonoids and polysaccharide were 1 .36% and 4.70%,respectively.The IC50 of water extract scavenging DPPH and OH were 1 56.8 mg/L and 674.5 mg/L,respectively.Conclu-sion:Abelmoschus esculentus tea has good nutritional value and antioxidant effect which can provide a new green health drinks

  19. 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。

  20. Temporal and spatial behavior of pharmaceuticals in ...

    Science.gov (United States)

    The behavior of active pharmaceutical ingredients (APIs) in urban estuaries is not well understood. In this study, 15 high volume usage APIs were measured over a one year period throughout Narragansett Bay, RI, USA to determine factors controlling their concentration and distribution. Dissolved APIs ranged in concentration from not detected to 310 ng/L, with numerous APIs present at all sites and sampling periods. Eight APIs were present in suspended particulate material, ranging in concentration from <1 ng/g to 44 ng/g. Partitioning coefficients (Kds) were determined for APIs present in both the dissolved and particulate phases, with their range and variability remaining relatively constant during the study. Organic carbon normalization reduced the observed variability of several APIs to a small extent; however, other factors appear to play a role in controlling partitioning behavior. The continuous discharge of wastewater treatment plant effluents into upper Narragansett Bay resulted in sustained levels of APIs, resulting in a zone of “pseudo-persistence.” For most of the APIs, there was a strong relationship with salinity, indicating conservative behavior within the estuary. Short flushing times in Narragansett Bay coupled with APIs present primarily in the dissolved phase suggests that most APIs will be diluted and transported out of the estuary, with only small amounts of several compounds removed to and sequestered in sediments. This study ide

  1. 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.

  2. 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.

  3. 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.

  4. Quality Control: microbial limit tests for nonsterile pharmaceuticals, part 2.

    Science.gov (United States)

    Vu, Nicole; Lou, Jessica R; Kupiec, Thomas C

    2014-01-01

    Cases of contaminated nonsterile products have been reported in increasing numbers. Often, these contaminated products are associated with the presence of objectionable microorganisms. The major contaminants of nonsterile pharmaceutical products and ingredients are bacteria, yeasts, and molds. The combination of parts 1 and 2 of this series of articles provides a thorough examination of microbiological quality testing for nonsterile products.

  5. [Pharmaceutical technology of Cordaflex tablets].

    Science.gov (United States)

    Erdös, S

    1996-01-01

    First the possibilities of solubilization and the photosensibility of nifedipine (the active ingredient of Cordaflex tablets) were investigated. The technology of retard tablet involves the preparation of a coprecipitate through spraying a solution containing nifedipine, a hydrotropic and a reardizing substance on carrier. After drying the produced granulated material was blended with common auxiliary ingredients, compressed into tablet and coated. The ratio of the two types of coprecipitating substances has a direct effect on the dissolution, so it proved predictable. The reproducibility of technology was good.

  6. Mineralization of synthetic and industrial pharmaceutical effluent containing trimethoprim by combining electro-Fenton and activated sludge treatment

    OpenAIRE

    Mansour, Dorsaf; Fourcade, Florence; Soutrel, Isabelle; Hauchard, Didier; Bellakhal, Nizar; Amrane, Abdeltif

    2015-01-01

    International audience; A combined process coupling of an electro-Fenton and a biological degradation was investigated in order to mineralize synthetic and industrial pharmaceutical effluent containing trimethoprim, a bacteriostatic antibiotic. Electro-Fenton degradation of trimethoprim was optimized by means of a Doehlert experimental design, showing that 0.69 mM Fe2+, 466 mA and 30 min electrolysis time were optimal, leading to total trimethoprim removal, while mineralization remained limit...

  7. 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

  8. Main Reasons for Registration Application Refusal of Generic and Similar Pharmaceutical Drug Products by the Brazilian Health Regulatory Agency (ANVISA)

    Science.gov (United States)

    do Carmo, Ana Cerúlia Moraes; Piras, Stefânia Schimaneski; Rocha, Nayrton Flávio Moura

    2017-01-01

    Objective. The marketing authorization of generic and similar pharmaceutical drug products involves the analysis of proposing company's administrative aspects as well as drug product technical description and scientific evaluations. This study evaluated the main reasons for registration refusal of generic and similar pharmaceutical drug products in Brazil. The aim is to help future applicants to better organize the proposal. Methods. A retrospective search of drug products registration processes was performed on the Brazilian Government Official Gazette from January 1, 2015, and December 31, 2015. Results. Drug product quality control, drug product stability study, deadline accomplishment, API quality control made by drug manufacturer, active pharmaceutical ingredient (API), and production report were the main reasons for marketing authorization application refusal of generic and similar pharmaceutical drug products in 2015. Conclusion. Disclosure of the reasons behind failed applications is a step forward on regulatory transparency. Sharing of experiences is essential to international regulatory authorities and organizations to improve legislation requirements for the marketing authorization of generic and similar pharmaceutical drug products. PMID:28280742

  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. An empirical analysis of primary and secondary pharmaceutical patents in Chile.

    Science.gov (United States)

    Abud, María José; Hall, Bronwyn; Helmers, Christian

    2015-01-01

    We analyze the patent filing strategies of foreign pharmaceutical companies in Chile distinguishing between "primary" (active ingredient) and "secondary" patents (patents on modified compounds, formulations, dosages, particular medical uses, etc.). There is prior evidence that secondary patents are used by pharmaceutical originator companies in the U.S. and Europe to extend patent protection on drugs in length and breadth. Using a novel dataset that comprises all drugs registered in Chile between 1991 and 2010 as well as the corresponding patents and trademarks, we find evidence that foreign originator companies pursue similar strategies in Chile. We find a primary to secondary patents ratio of 1:4 at the drug-level, which is comparable to the available evidence for Europe; most secondary patents are filed over several years following the original primary patent and after the protected active ingredient has obtained market approval in Chile. This points toward effective patent term extensions through secondary patents. Secondary patents dominate "older" therapeutic classes like anti-ulcer and anti-depressants. In contrast, newer areas like anti-virals and anti-neoplastics (anti-cancer) have a much larger share of primary patents.

  11. 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。

  12. 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.

  13. Suppressing effect of saikosaponin A, an active ingredient of Bupleurum falcatum, on chocolate self-administration and reinstatement of chocolate seeking in rats.

    Science.gov (United States)

    Lorrai, Irene; Maccioni, Paola; Carai, Mauro A M; Capra, Alessandro; Castelli, M Paola; Riva, Antonella; Morazzoni, Paolo; Gessa, Gian Luigi; Colombo, Giancarlo

    2017-01-18

    Recent lines of experimental evidence have indicated that saikosaponin A (SSA) - a bioactive ingredient of the medicinal plant, Bupleurum falcatum L. - suppressed alcohol, morphine, and cocaine self-administration in rats. The present paper was designed to assess whether the protective properties of SSA on addiction-related behaviors generalize to a hyperpalatable food such as a chocolate-flavored beverage (CFB). To this end, rats were initially trained to lever-respond for CFB [5% (w/v) Nesquik(®) powder in water] under fixed ratio (FR) 10 (FR10) schedule of reinforcement. Once lever-responding reached stable levels, rats were treated acutely with two different dose ranges of SSA (0, 0.25, 0.5, and 1mg/kg; 0, 1, 2.5, and 5mg/kg; i.p.) and exposed to the FR10 and progressive ratio (PR) schedules of reinforcement in four independent experiments. The effect of acutely administered SSA (0, 0.25, 0.5, and 1mg/kg; i.p.) on cue-induced reinstatement of seeking behavior for CFB was also assessed. Under the FR and PR schedules of reinforcement, treatment with SSA diminished lever-responding for CFB, amount of self-administered CFB, and breakpoint for CFB. All variables were virtually completely suppressed after treatment with 5mg/kg SSA. Treatment with SSA also suppressed reinstatement of CFB-seeking behavior. No dose of SSA altered rat motor-performance, evaluated exposing all rats to an inverted screen test immediately after the self-administration session. These results demonstrate that acute treatment with SSA potently suppressed several addictive-like behaviors motivated by highly hedonic nourishment. These data extend to a highly rewarding natural stimulus the anti-addictive properties of SSA recently disclosed in rats self-administering alcohol, morphine, and cocaine.

  14. Do consumers really trust their doctors’ suggestions and drugs they prescribe? : the relationship between perceived risk and trust in consumer buying decisions on prescription drugs, and how pharmaceutical companies can improve consumer’s trust through marketing activities in China

    OpenAIRE

    Jin, Meina

    2016-01-01

    This thesis examines how perceived risk and trust affect consumer’s buying decisions during the process of buying and consuming prescription drugs, and investigates how pharmaceutical companies can improve consumer’s trust by strategically designing and performing their marketing activities in the Chinese pharmaceutical market. Previous literature has generally introduced the overview of consumer buying process and the two important factors that may influence the buying decisions: percei...

  15. 黄花棘豆抑制植物病原菌的活性成分研究%Antifungal activity and isolation of active ingredients in Oxytropis ochrocephala

    Institute of Scientific and Technical Information of China (English)

    杨震发; 袁呈山; 杨顺义; 柳利龙; 杨晋伟; 沈慧敏

    2014-01-01

    In order to find new botanical antifungal compounds,antifungal ingredients of Oxytropis ochrocephala Bunge were isolated. Using bioassay-guided fractionation methods,antifungal ingredients were isolated and mono-meric compounds were identified by modern spectroscopy techniques from O. ochrocephala. All data were pro-cessed statistically by using SPSS 17.0. Ethanol extract of O. ochrocephala showed strong activity against the se-lected pathogenic fungi with an inhibition ratio of 82.08 % at the concentration of 10 mg/mL. The methylene chloride and ethyl acetate phases displayed a significant antifungal activity against Botrytiscinerea,with an inhibi-tion ratio of 84.30% and 83.13% ,respectively. Six compounds were isolated and identified through comparing the data obtained via spectroscopic methods and the values reported in the literature. The screening of antifungal activity showed that 3-hydroxy-4,9-dimethoxypterocarpan,3-hydroxy-9-dimethoxy pterocarpan and 3-hydroxy-8, 9-dimethoxypterocarpan had higher EC50 on tested fungi. The EC50 of 3-hydroxy-4,9-dimethoxypterocarpan against B.cinerea was 10.42μg/mL and the EC50 of 3-hydroxy-8,9-dimethoxypterocarpan against Fusarium oxys-porum was 27.09μg/mL. O. ochrocephala could be used as a biological antifungal agent and pterocarpan com-pounds are its significant antifungal ingredients.%为了测定黄花棘豆(Oxytropis ochrocephala Bunge)提取物对常见病原真菌的活性,明确其中的有效成分,以黄花棘豆为材料,结合生物活性追踪法,对黄花棘豆的抑菌活性物质进行分离,并利用现代波谱学技术进行结构鉴定。结果表明,黄花棘豆乙醇提取物对供试4种病原真菌均表现出较强的活性,10 mg/mL对番茄灰霉病菌的抑菌率达到82.08%;粗提物萃取后的二氯甲烷相和乙酸乙酯相为其活性部分,10 mg/mL对番茄灰霉病菌的抑菌率分别为84.30%和83.13%;从合并后的二氯甲烷和乙酸乙酯

  16. 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.

  17. Analytical characterization of an orally-delivered peptide pharmaceutical product.

    Science.gov (United States)

    Kelley, Wayne P; Chen, Shujun; Floyd, Philip D; Hu, Ping; Kapsi, Shiva G; Kord, Alireza S; Sun, Mingjiang; Vogt, Frederick G

    2012-05-15

    The characterization of orally-delivered peptide pharmaceuticals presents several challenges to analytical methods in comparison to characterization of conventional small-molecule drugs. These challenges include the analysis and characterization of difficult-to-separate impurities, secondary structure, the amorphous solid-state form, and the integrity of enteric-coated drug delivery systems. This work presents the multidisciplinary analytical characterization of a parathyroid hormone (PTH) peptide active pharmaceutical ingredient (API) and an oral formulation of this API within enteric-coated sucrose spheres. The analysis of impurities and degradation products in API and formulated drug product was facilitated by the development of an ultrahigh-performance liquid chromatography (UHPLC) method for analysis by high-resolution mass spectrometry (MS). The use of UHPLC allowed for additional resolution needed to detect impurities and degradation products of interest. The secondary structure was probed using a combination of solution-state NMR, infrared, and circular dichroism spectroscopic methods. Solid-state NMR is used to detect amorphous API in a nondestructive manner directly within the coated sucrose sphere formulation. Fluorescence and Raman microscopy were used in conjunction with Raman mapping to show enteric coating integrity and observe the distribution of API beneath the enteric-coating on the sucrose spheres. The methods are combined in a multidisciplinary approach to characterize the quality of the enteric-coated peptide product.

  18. LC determination of rosiglitazone in bulk and pharmaceutical formulation.

    Science.gov (United States)

    Radhakrishna, T; Satyanarayana, J; Satyanarayana, A

    2002-07-31

    An isocratic reversed phase liquid chromatographic (RP-LC) method has been developed and subsequently validated for the determination of rosiglitazone and its related impurities. Separation was achieved with a Symmetry C18 column and sodium phosphate buffer (pH adjusted to 6.2):acetonitrile (50:50, v/v) as eluent, at a flow rate of 1.0 ml/min. UV detection was performed at 245 nm. The method is simple, rapid, selective and stability indicating. Indole was used as internal standard for the purpose of quantification of rosiglitazone. The described method is linear over a range of 0.45-10 microg/ml for related impurities and 180-910 microg/ml for assay of rosiglitazone. The method precision for the determination of assay and related compounds was below 1.0 and 3.6% RSD, respectively. The mean recoveries of impurities were found to be in the range of 95-102%. The percentage recoveries of Active Pharmaceutical Ingredient (API) from dosage forms ranged from 99.02 to 101.30. The method is useful in the quality control of bulk manufacturing and also in pharmaceutical formulations.

  19. Multiblock PLS analysis of an industrial pharmaceutical process.

    Science.gov (United States)

    Lopes, J A; Menezes, J C; Westerhuis, J A; Smilde, A K

    2002-11-20

    The performance of an industrial pharmaceutical process (production of an active pharmaceutical ingredient by fermentation, API) was modeled by multiblock partial least squares (MBPLS). The most important process stages are inoculum production and API production fermentation. Thirty batches (runs) were produced according to an experimental planning. Rather than merging all these data into a single block of independent variables (as in ordinary PLS), four data blocks were used separately (manipulated and quality variables for each process stage). With the multiblock approach it was possible to calculate weights and scores for each independent block. It was found that the inoculum quality variables were highly correlated with API production for nominal fermentations. For the nonnominal fermentations, the manipulations of the fermentation stage explained the amount of API obtained (especially the pH and biomass concentration). Based on the above process analysis it was possible to select a smaller set of variables with which a new model was built. The amount of variance predicted of the final API concentration (cross-validation) for this model was 82.4%. The advantage of the multiblock model over the standard PLS model is that the contributions of the two main process stages to the API volumetric productivity were determined.

  20. 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。

  1. ACTIVE INGREDIENTS ACTION IN THE PLASMA JET AID COAL GASIFICATION%等离子体炬辅助煤气化中活性组分的作用

    Institute of Scientific and Technical Information of China (English)

    董光华; 庞先勇

    2012-01-01

    On the basis of the analysis for the active species character and the reaction pa rameter in the process of the plasma jet aid coal gasification, the experiments for confirming ac tive species action has been designed in this paper. Through quantum chemistry calculation, it is found that the water molecule structure was changed observably by direct action between the ac tive ingredients: singlet oxygen, O2+ etc and oxygen atom in the water molecule in the coal gasifi cation , and these actions was favorable to form free radical OH ? , which react with the carbon in the coal by the broken O-H bond. Likely reaction channel induced by the active ingredients has been posed according to the regression equations on oxygen contents in the working gas to the volume fractions of the staple- H2, CO and CO2 in the experiment.%在对等离子体炬辅助煤气化过程中活性物种的特征和反应参数分析的基础上,设计了以证实活性组分的作用实验.通过量子化学计算,发现活性组分单线态氧和O2+等与水分子的氧原子直接作用更显著地改变了水分子结构,更有利于断键形成自由基OH·,OH·可以与煤中的碳发生反应.根据实验工作气体中氧含量对实验主要产物H2,CO和CO2体积分数的回归方程,提出活性组分诱发煤气化反应的可能化学反应通道.

  2. Phlorotannins from Ecklonia cava (Phaeophyceae): biological activities and potential health benefits.

    Science.gov (United States)

    Wijesekara, Isuru; Yoon, Na Young; Kim, Se-Kwon

    2010-01-01

    The importance of bioactive derivatives as functional ingredients has been well recognized due to their valuable health beneficial effects. Therefore, isolation and characterization of novel functional ingredients with biological activities from seaweeds have gained much attention. Ecklonia cava Kjellman is an edible seaweed, which has been recognized as a rich source of bioactive derivatives mainly, phlorotannins. These phlorotannins exhibit various beneficial biological activities such as antioxidant, anticancer, antidiabetic, anti-human immunodeficiency virus, antihypertensive, matrix metalloproteinase enzyme inhibition, hyaluronidase enzyme inhibition, radioprotective, and antiallergic activities. This review focuses on biological activities of phlorotannins with potential health beneficial applications in functional foods, pharmaceuticals, and cosmeceuticals.

  3. 辛夷不同组分抗过敏作用活性比较研究%Research on the Antiallergenic Activity of the Different Ingredients from Flos Magnolia

    Institute of Scientific and Technical Information of China (English)

    孙蓉; 钱晓路; 吕莉莉

    2013-01-01

    the alcohol extract and water extract or volatile oil components by compareing the antiallergenic effect of different extract of Flos Magnolia. Conclusion The antiallergenic activity of the different ingredients from Flos Magnolia were alcohol extract >water extract> volatile oil components, and under the guidance of antiallergenic activity, the effective ingredients of Flos Magnolia was the alcohol extract. But as the complex of pharmacodynamics characteristics of TCM and the interaction between the components and molecular mechanisms of l ia were not very clear, so it is necessary to take more research of the multi-components between the pharmacological and molecular mechanisms, in order to provide references and research ideas for innovative drugs.

  4. 21 CFR 701.30 - Ingredient names established for cosmetic ingredient labeling.

    Science.gov (United States)

    2010-04-01

    ... 21 Food and Drugs 7 2010-04-01 2010-04-01 false Ingredient names established for cosmetic... AND HUMAN SERVICES (CONTINUED) COSMETICS COSMETIC LABELING Labeling of Specific Ingredients § 701.30 Ingredient names established for cosmetic ingredient labeling. The Commissioner establishes the...

  5. 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.

  6. 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

  7. 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.

  8. 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 <2% (e.g., caseinates, milk protein isolates) to 100% in 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

  9. Improving the Concentrations of the Active Components in the Herbal Tea Ingredient, Uraria crinita: The Effect of Post-harvest Oven-drying Processing

    Science.gov (United States)

    Chao, Jung; Dai, Yuntao; Cheng, Hao-Yuan; Lam, Wing; Cheng, Yung-Chi; Li, Ke; Peng, Wen-Huang; Pao, Li-Heng; Hsieh, Ming-Tsuen; Qin, Xue-Mei; Lee, Meng-Shiou

    2017-01-01

    Uraria crinita is widely used as a popular folk drink; however, little is known about how the post-harvest operations affect the chemical composition and bioactivity of UC. We assessed three drying methods (Oven-drying, Air-drying, Sun-drying), as well as the Oven-drying temperature using metabolomics approaches and bioactivity assays. The samples processed at 40 degree show a greater effect on the levels of estrogen receptor-alpha activity and nuclear factor erythroid 2–related factor 2 activity, anti-oxidative activity, and cyclooxygenase-2 inhibition compared with the other samples. A multivariate analysis showed a clear separation between the 40 degree Oven-dried samples and the other samples, which is consistent with the results of bioactivity assay. These results are ascribed to at least two-fold increase in the concentrations of flavonoids, spatholosineside A and triterpenoids in the oven-dried samples compared with the other groups. The proposed Oven-drying method at 40 degree results in an improved quality of UC. PMID:28079108

  10. Chemical profiling analysis of Maca using UHPLC-ESI-Orbitrap MS coupled with UHPLC-ESI-QqQ MS and the neuroprotective study on its active ingredients

    Science.gov (United States)

    Zhou, Yanyan; Li, Peng; Brantner, Adelheid; Wang, Hongjie; Shu, Xinbin; Yang, Jian; Si, Nan; Han, Lingyu; Zhao, Haiyu; Bian, Baolin

    2017-03-01

    Lepidium meyenii (Maca), originated from Peru, has been cultivated widely in China as a popular health care food. However, the chemical and effective studies of Maca were less in-depth, which restricted its application seriously. To ensure the quality of Maca, a feasible and accurate strategy was established. One hundred and sixty compounds including 30 reference standards were identified in 6 fractions of methanol extract of Maca by UHPLC-ESI-Orbitrap MS. Among them, 15 representative active compounds were simultaneously determined in 17 samples by UHPLC-ESI-QqQ MS. The results suggested that Maca from Yunnan province was the potential substitute for the one from Peru. Meanwhile, the neuroprotective effects of Maca were investigated. Three fractions and two pure compounds showed strong activities in the 1-methyl-4-phenyl-1, 2, 3, 6-tetrahydropyridine (MPTP)-induced zebrafish model. Among them, 80% methanol elution fraction (Fr5) showed significant neuroprotective activity, followed by 100% part (Fr6). The inhibition of acetylcholinesterase (AChE) and butyrylcholinesterase (BuChE) was a possible mechanism of its neuroprotective effect.

  11. 超临界萃取技术在蓝色化妆品活性成分提取分离中的应用进展%Application Progress of Supercritical Fluid Extraction in Development of Blue Cosmetic Active ingredients

    Institute of Scientific and Technical Information of China (English)

    毕永贤; 蒋丽刚; 陆海英

    2014-01-01

    To summarize the recent development on the utilization of supercritical fluid extraction in development of blue cos-metic active ingredients,the published articles on extracting blue cosmetic active ingredients by supercritical fluid extraction technology were reviewed and analyzed. The results showed,the supercritical fluid extraction technology in blue cosmetic ac-tive ingredients extracting especially for polyunsaturated fat acid,polyphenols,natural pigments and terpenes has its unique ad-vantages. This review will provide a reference for the further research and development of blue cosmetic active ingredients.%为探讨超临界萃取技术在蓝色化妆品活性成分提取分离中的应用现状,查阅相关文献,并对其进行归纳、分析和总结。结果发现,超临界萃取技术在在多不饱和脂肪酸、多酚、天然色素、萜类等蓝色化妆品活性成分的提取分离中有其独特的优势,可为超临界萃取技术在蓝色化妆品活性成分提取分离中的进一步发展应用提供参考依据。

  12. 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.

  13. 丹参治疗冠心病的有效成分分析及其药理学探析%An analysis on the active ingredients and the pharmacology of Danshen on treating coronary heart disease

    Institute of Scientific and Technical Information of China (English)

    廖天南

    2012-01-01

      Objective:To investigate the active ingredients and the pharmacology of Danshen on treating coronary heart disease. Method: ①The closed microwave assisted extraction Salvia the active ingredient tanshinone; ②Cultured mouse cardiomyocytes, manufacturing mice myocardial hypoxia-reperfusion injury model, to simulate myocardial ischemia-reperfusion injury that caused by vivo coronary heart disease; ③Used salvia feeding mice, to observe toxicity; ④To observe teratogenic effects of salvia against mice sperm. Results: The effective tanshinone of salvia that treated coronary heart disease can inhibit of myocardial damage, the inhibitory rate was 84.3%, toxicological studies to prove that medicinal salvia was safe and non-toxic, non-teratogenic, effected on mouse sperm. Conclusion:The pharmacod-ynamic of Danshen sure and nontoxic.%  目的:探讨丹参治疗冠心病的有效成分并对其药理学进行分析.方法:①密闭微波辅助萃取丹参有效成分丹参酮;②培养小白鼠心肌细胞,制造小白鼠心肌细胞缺氧再灌注损伤模型,来模拟体内冠心病所致的心肌缺血再灌注损伤;③用丹参喂养小白鼠,观察其毒副反应;④观察丹参对小白鼠精子的致畸作用.结果:丹参治疗冠心病的有效成分丹参酮能有效的抑制心肌的损伤,损伤抑制率84.3%;经毒理学研究证明药用丹参安全无毒;对小白鼠精子无致畸作用.结论:丹参治疗冠心病药效肯定且无毒.

  14. 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.

  15. 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.

  16. 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.

  17. Bioavailability & Bioequivalence Studies ? Pharmaceutical Importance

    OpenAIRE

    Pratibha Muntha

    2015-01-01

    Pharmacokinetics has now emerged as an important part of drug development especially in the development of new drugs. The combined studies of Pharmacodynamics and pharmacokinetics present a thorough understanding on how the drug affects the body and how the body affects the drug.Bioavailability is the study of the rate and extent to which the active ingredient is absorbed from a dosage form and it is available at the required action site. Bioequivalence is that the...

  18. Comparative research between Bai-hua Qian-hu, a Chinese traditional plant, and its active ingredient on nuclear factor-κB and tumor necrosisfactor-α in isolated ischemia-reperfusion heart of rat

    Institute of Scientific and Technical Information of China (English)

    王弛; 常天辉

    2004-01-01

    @@Ischemia-reperfusion (I/R) injury is a complicated pathophysiological process, which is involved in calcium overload, free radical production, metabolic abnormalities, and inflammatory reaction. With the development of modern molecular biology, the expression and regulation of gene in myocardial I/R injury are focused on NF-κB.1Inflammatory reactions play an important role in I/R injury.2 TNF-α, an important inflammatory cytokine, is regulated by NF-κB and counteracts the activation of NF-κB. Sometimes, improper activation of NF-κB can induce excessive inflammatory responses and injury, so, modulation of NF-κB activation may dedicate a new target in alleviation of myocardial I/R injury.3Our previous studies have proved that Bai-hua Qian-hu (Peucedanum praeruptorum Dunn, BQ), a Chinese traditional plant had cardioprotective action in I/R animals.4 Its active ingredient Pd-Ia, a Ca2+-influx blocker5 and K+-channel opener,6 had similar effects. Meanwhile, it relieved inflammatory reaction and apoptosis in I/R myocardium through inhibition of interleukin-6 and Fas, bax, bcl-2 protein expression.7 However, the effects of BQ and Pd-Ia on the activation of NF-κB and the expression of TNF-α in I/R myocardium have not been clear yet. In this study, the effects of BQ and Pd-Ia on these two factors were investigated to further ascertain the molecular protective mechanism of BQ in I/R myocardium.

  19. Identification of some factors affecting pharmaceutical active compounds (PhACs) removal in real wastewater. Case study of fungal treatment of reverse osmosis concentrate.

    Science.gov (United States)

    Badia-Fabregat, Marina; Lucas, Daniel; Gros, Meritxell; Rodríguez-Mozaz, Sara; Barceló, Damià; Caminal, Glòria; Vicent, Teresa

    2015-01-01

    Many technologies are being developed for the efficient removal of micropollutants from wastewater and, among them, fungal degradation is one of the possible alternative biological treatments. In this article, some factors that might affect pharmaceutically active compounds (PhACs) removal in a fungal treatment of real wastewater were identified in batch bioreactor treating reverse osmosis concentrate (ROC) from urban wastewater treatment plant (WWTP). We found that degradation of PhACs by Trametes versicolor was enhanced by addition of external nutrients (global removal of 44%). Moreover, our results point out that high aeration might be involved in the increase in the concentration of some PhACs. In fact, conjugation and deconjugation processes (among others) affect the removal assessment of emerging contaminants when working with real concentrations in comparison to experiments with spiked samples. Moreover, factors that could affect the quantification of micropollutants at lab-scale experiments were studied.

  20. 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.

  1. The use of differential scanning calorimetry for the purity verification of pharmaceutical reference standards.

    Science.gov (United States)

    Mathkar, S; Kumar, S; Bystol, A; Olawoore, K; Min, D; Markovich, R; Rustum, A

    2009-04-05

    Reference standards are routinely used in pharmaceutical industry to determine strength, content, and the quality of drug products, active pharmaceutical ingredients (API), preservatives, antioxidants and excipients. Traditionally, chromatographic techniques such as High Performance Liquid Chromatography (HPLC) and Gas Chromatography (GC) in conjunction with other analytical techniques have been used to determine the purity and strength of a specific lot of a compound for the purpose of qualifying the lot to use as a reference standard. The assigned purity of the reference standard for a wide variety of compounds can be verified using an absolute method such as Differential Scanning Calorimetry (DSC). In this paper, purity of 16 reference standards was determined by DSC and the results were then compared to the purity values that were obtained using HPLC and other analytical techniques. The results indicate that the purity obtained from DSC analysis is comparable to the chromatographic purity for organic compounds that are at least 98% pure. Use of DSC for purity determination is not appropriate if a compound lacks sharp melting point, decomposes in the defined temperature range or exhibits other thermal event(s) which interfere with the melting point of the compound. The use of DSC as an alternative and or complementary method to verify the purity of a compound as part of the pharmaceutical reference standard certification process is discussed.

  2. 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.

  3. 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.

  4. 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.

  5. 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.

  6. 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.

  7. 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...

  8. 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.

  9. Irradiation effects of ChuanBei active ingredients with cobalt 60%钴-60辐照对川贝活性成分的影响

    Institute of Scientific and Technical Information of China (English)

    宋九华; 成英; 刘素君

    2012-01-01

    考查不同Co-60辐照剂量对川贝活性成分的影响,为川贝的灭菌贮存和质量评价提供参考.采用HPLC法分析成分的变化.在不同辐射剂量照射后,川贝的化学成分的组成基本不变(各组分的保留时间tR不受辐照影响),但钴-60辐照剂量会对川贝药材某些组分的含量有不同程度的影响,在川贝的贮存和质量评价中应引起注意.%To provide guidance of ChuanBei storage and quality evaluation through examining different Co irradiation dose. The column Shim-pack VP-ODS( 150mmx4. 6mm,5. 0μm) was used. The mobile phase consisted of A(2. 5% of phosphoric acid sodium hydrogen and 10%sodium dihydrogen phosphate solution)and B( methanol) with a gradient elution,and the flow rate was l.0mL/ min. The detection wavelength were 200 nm, and the column temperature was 30°C. The composition structure of same original ChuanBei in different radiation dose was same based on retention time( tR ) ,but some components were affected by cobalt 60 irradiation doses. There are obvious effect on some active component content of ChuanBei by Cobalt 60 irradiation. This method can be used as a means of ChuanBei storage and quality assessment.

  10. 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.

  11. 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.

  12. Confiscated black market products and nutritional supplements with non-approved ingredients analyzed in the Cologne Doping Control Laboratory 2009.

    Science.gov (United States)

    Kohler, Maxie; Thomas, Andreas; Geyer, Hans; Petrou, Michael; Schänzer, Wilhelm; Thevis, Mario

    2010-01-01

    Doping control laboratories are frequently confronted with new substances that may be misused by athletes. Besides new pharmaceuticals, where method development for their detection is dependent on the availability of the substance and corresponding administration studies, some professional and amateur athletes are using illicit 'black market' products, which either differ from known pharmaceuticals but cause similar effects or still are undergoing clinical trials and are therefore rarely available to doping control laboratories. In the Cologne Doping Control Laboratory, different confiscated products and legally obtained nutritional supplements were analyzed in 2009, and various findings were reported including GH-labelled injection vials without any pharmacologically active content; combinations of products indicating the attempt to mask growth hormone abuse; unpurified long-R(3) -IGF-1; nutritional supplements containing the growth hormone releasing peptide-2 (GHRP-2); and ampoules containing the selective androgen receptor modulator Andarine (S-4). This review provides an overview on the substances that were analyzed in 2009. Ingredients relevant for doping control were identified by means of liquid chromatography and mass spectrometry methods. The awareness of new products on the black market and in nutritional supplements is of utmost importance for laboratories to develop detection methods accordingly and screen for new substances as early as possible.

  13. Benefits of using algae as natural sources of functional ingredients.

    Science.gov (United States)

    Ibañez, Elena; Cifuentes, Alejandro

    2013-03-15

    Algae have been suggested as a potential source of bioactive compounds to be used in the food and pharmaceutical industries. With the strong development of functional foods as a method to improve or maintain health, the exploration of new compounds with real health effects is now an intense field of research. The potential use of algae as source of functional food ingredients, such as lipids, proteins, polysaccharides, phenolics, carotenoids, etc., is presented, together with the different possibilities of improving valuable metabolites production either using the tools and the knowledge provided by marine biotechnology or improving the different factors involved in the production on a large scale of such metabolites. The bio-refinery concept is also presented as a way to improve the efficient use of algae biomass while favouring process sustainability.

  14. 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.

  15. Effect on the growth and development and induction of abnormalities by a glyphosate commercial formulation and its active ingredient during two developmental stages of the South-American Creole frog, Leptodactylus latrans.

    Science.gov (United States)

    Bach, Nadia Carla; Natale, Guillermo Sebastián; Somoza, Gustavo Manuel; Ronco, Alicia Estela

    2016-12-01

    We evaluated the acute lethal and sublethal effects of technical-grade glyphosate (GLY) and the GLY-based commercial formulation Roundup ULTRA MAX® (RU) on two Gosner stages (Gss) 25 and 36 of the South-American Creole frog, Leptodactylus latrans. Bioassays were performed following standardized methods within a wide range of concentrations (0.0007-9.62 mg of acid equivalents per liter-a.e./L-of RU and 3-300 mg/L of GLY). The endpoints evaluated were mortality, swimming activity, growth, development, and the presence of morphologic abnormalities, especially in the mouthparts. No lethal effects were observed on larvae exposed to GLY during either Gs-25 or Gs-36. The concentrations inducing 50 % lethality in RU-exposed larvae at different exposure times and Gss ranged from 3.26 to 9.61 mg a.e./L. Swimming activity was affected by only RU. Effects on growth and development and the induction of morphologic abnormalities-like oral abnormalities and edema-were observed after exposure to either GLY or RU. Gs-25 was the most sensitive stage to both forms of the herbicide. The commercial formulation was much more toxic than the active ingredient on all the endpoints assessed. Effects on growth, development, and the induction of morphologic abnormalities observed in the range of environmental concentrations reported for agroecosystems of Argentina constitute an alert to the potential detrimental effects of the herbicide that could be affecting the fitness and survival of anurans in agroecosystems.

  16. Occurrence and fate of pharmaceutically active compounds in the largest municipal wastewater treatment plant in Southwest China: mass balance analysis and consumption back-calculated model.

    Science.gov (United States)

    Yan, Qing; Gao, Xu; Huang, Lei; Gan, Xiu-Mei; Zhang, Yi-Xin; Chen, You-Peng; Peng, Xu-Ya; Guo, Jin-Song

    2014-03-01

    The occurrence and fate of twenty-one pharmaceutically active compounds (PhACs) were investigated in different steps of the largest wastewater treatment plant (WWTP) in Southwest China. Concentrations of these PhACs were determined in both wastewater and sludge phases by a high-performance liquid chromatography coupled with electrospray ionization tandem mass spectrometry. Results showed that 21 target PhACs were present in wastewater and 18 in sludge. The calculated total mass load of PhACs per capita to the influent, the receiving water and sludge were 4.95mgd(-1)person(-1), 889.94μgd(-1)person(-1) and 78.57μgd(-1)person(-1), respectively. The overall removal efficiency of the individual PhACs ranged from "negative removal" to almost complete removal. Mass balance analysis revealed that biodegradation is believed to be the predominant removal mechanism, and sorption onto sludge was a relevant removal pathway for quinolone antibiotics, azithromycin and simvastatin, accounting for 9.35-26.96% of the initial loadings. However, the sorption of the other selected PhACs was negligible. The overall pharmaceutical consumption in Chongqing, China, was back-calculated based on influent concentration by considering the pharmacokinetics of PhACs in humans. The back-estimated usage was in good agreement with usage of ofloxacin (agreement ratio: 72.5%). However, the back-estimated usage of PhACs requires further verification. Generally, the average influent mass loads and back-calculated annual per capita consumption of the selected antibiotics were comparable to or higher than those reported in developed countries, while the case of other target PhACs was opposite.

  17. Method for manufacturing carrier containing e.g. proteins for human during oral drug delivery operation for food and drug administration application in pharmaceutical industry, involves providing active ingredient to core layer

    DEFF Research Database (Denmark)

    2015-01-01

    or plastically deformable layer to increase stiction of the release layer. The method enables manufacturing the micro-container including an outer diameter of 200-500 pm and a height of 2-70 pm such that wall thickness is larger than 5 m to increase geometrical stability and reduce buckling. The method enables......), polymethacrylate (PMMA), Eudragits Poly-methacylic acid-co-methyl methacrylate, ethyl cellulose (EC), polyvinyl alcohol (PVA), polyvinylpyrollidone (PVP), polyethylene glycol (PEG), polyethylene glycol methacrylate (PEGMA), polyethylene glycol dimethacrylate (PEGDMA), poly-lactic-co-glycolic acid (PGLA...

  18. [Inulin and derivates as key ingredients in functional foods].

    Science.gov (United States)

    Madrigal, Lorena; Sangronis, Elba

    2007-12-01

    Inulin is a non-digestible carbohydrate that is contained in many vegetables, fruits and cereals. It is industrially produced from the chicory's root (Cichorium intybus) and it is widely used as ingredient in functional foods. Inulin and its derivate compounds (oligofructose, fructooligosaccharides) are usually called fructans, as they are basically based on linear fructose chains. This review presents a description of inulin and its most common derivate compounds: chemical structure, natural sources, physic-chemical properties, technological functionality, industrial manufacturing, analytical method for determination and health benefits: prebiotic, dietary fiber, low caloric value, hypoglycemic action, enhancement of calcium and magnesium bioavailability. Potential benefits: lipid parameters regulation, reduction of colon cancer risk and others, improvement of immune response, intestinal disorders protection. From technological point of view, these compounds exhibit a variety of properties: thickener, emulsifier, gel forming, sugar and fat substitute, humectant, freezing point depression. Inulin and derivates are been used in pharmaceutical, chemical and processing industry as technological additives and excipients. They are also been used for animal feeding. They are been considered as "bioactive" compounds to be proposed as future packaging material. Fructans are proposed to be classified as "functional fiber", according to recent concepts based on physiological effects on individuals. This review of inulin and its derivates was useful to show the broad boundaries of these compounds in the food industry and why they may be considered as key ingredients in the expanding functional food market.

  19. Comparison of the Nutrient and Active Ingredients in Three Kinds of Jinxiang Allium sativum L.%3种金乡大蒜中营养活性成分的含量比较

    Institute of Scientific and Technical Information of China (English)

    周宇; 王文军; 李茜; 杨丹; 孔庆胜

    2016-01-01

    [目的]检测3种金乡大蒜中营养成分和活性物质含量,从化学分子水平探讨不同品种的差异,对于优化种质资源、提升大蒜后期加工利用的品质和附加值具有指导作用。[方法]采用食品化学的常规方法并结合大型仪器检测,测定大蒜中营养成分和活性成分的含量。[结果]基本营养成分可溶性糖、粗脂肪、蛋白质含量,以金乡紫皮蒜最高,金乡白皮蒜次之,独头蒜最少;金乡紫皮蒜维生素C含量最高,独头蒜次之,金乡白皮蒜最少;金乡白皮蒜的过氧化氢酶(CAT)活性最高,紫皮蒜次之,独头蒜最差;锗和大蒜素DADS含量则是独头蒜最高。[结论]对于偏重营养成分的利用,金乡紫皮蒜有较大优势;而对于大蒜素和锗的特色保健功能利用,独头蒜有更大优势。%Objective] The research aimed to detect the difference of contents of nutrient and active ingredients in 3 kinds of Jinxiang Allium sa-tivum L.and to explore the differences of different varieties from the chemical molecular level .It performs important functions in optimizing the germplasm resourses and improving the quality additional value of late garlic processing.[Method]The nutrient and active ingredients of 3 kinds of Jinxiang Allium sativum L.were detected by traditional chemical methods and large-scale instruments methods.[Result]In the basic nutrients, such as soluble sugar, crude fat, protein and vitamin C,the Jinxiang purple skin Allium sativum L.had the highest content, the white skin Allium sativum L.took the second place and the single clove Allium sativum L.was the least.In the contents of vitamin C ,the Jinxiang purple skin Alli-um sativum L.had the highest content,the single clove Allium sativum L.took the second place and the white skin Allium sativum L.was the least.While in the activity of catalase(CAT), the Jinxiang white skin Allium sativum L.showed the maximum activity,the purple skin Allium

  20. 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.

  1. 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.

  2. 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.

  3. Processed Meat Ingredients: Past, Present and Future

    Science.gov (United States)

    Ingredients were first utilized to preserve meat and improve its palatability which date back to when our ancestors used salt and fire to preserve meat. Since that time man has incorporated a wide variety of ingredients to develop unique meat products and find ways to extend the shelf life of these ...

  4. Consumers' choice-blindness to ingredient information.

    Science.gov (United States)

    Cheung, T T L; Junghans, A F; Dijksterhuis, G B; Kroese, F; Johansson, P; Hall, L; De Ridder, D T D

    2016-11-01

    Food manufacturers and policy makers have been tailoring food product ingredient information to consumers' self-reported preference for natural products and concerns over food additives. Yet, the influence of this ingredient information on consumers remains inconclusive. The current study aimed at examining the first step in such influence, which is consumers' attention to ingredient information on food product packaging. Employing the choice-blindness paradigm, the current study assessed whether participants would detect a covertly made change to the naturalness of ingredient list throughout a product evaluation procedure. Results revealed that only few consumers detected the change on the ingredient lists. Detection was improved when consumers were instructed to judge the naturalness of the product as compared to evaluating the product in general. These findings challenge consumers' self-reported use of ingredient lists as a source of information throughout product evaluations. While most consumers do not attend to ingredient information, this tendency can be slightly improved by prompting their consideration of naturalness. Future research should investigate the reasons for consumers' inattention to ingredient information and develop more effective strategies for conveying information to consumers.

  5. Inulin-type fructans: functional food ingredients.

    Science.gov (United States)

    Roberfroid, Marcel B

    2007-11-01

    A food (ingredient) is regarded as functional if it is satisfactorily demonstrated to affect beneficially 1 or more target functions in the body beyond adequate nutritional effects. The term inulin-type fructans covers all beta(2inulin (DP 2-60, DP(av) = 12), oligofructose (DP 2-8, DP(av) = 4), and inulin HP (DP 10-60, DP(av) = 25) as well as Synergy 1, a specific combination of oligofructose and inulin HP. Inulin-type fructans resist digestion and function as dietary fiber improving bowel habits. But, unlike most dietary fibers, their colonic fermentation is selective, thus causing significant changes in the composition of the gut microflora with increased and reduced numbers of potentially health-promoting bacteria and potentially harmful species, respectively. Both oligofructose and inulin act in this way and thus are prebiotic: they also induce changes in the colonic epithelium and in miscellaneous colonic functions. In particular, the claim "inulin-type fructans enhance calcium and magnesium absorption" is scientifically substantiated, and the most active product is oligofructose-enriched inulin (Synergy 1). A series of studies furthermore demonstrate that inulin-type fructans modulate the secretion of gastrointestinal peptides involved in appetite regulation as well as lipid metabolism. Moreover, a large number of animal studies and preliminary human data show that inulin-type fructans reduce the risk of colon carcinogenesis and improve the management of inflammatory bowel diseases. Inulin-type fructans are thus functional food ingredients that are eligible for enhanced function claims, but, as more human data become available, risk reduction claims will become scientifically substantiated.

  6. PharmacoIogicaI Effects of Cortex phellodendri and Its Active Ingredient Extraction%黄柏的药理作用及其活性成分提取

    Institute of Scientific and Technical Information of China (English)

    陈阳峰; 钟晓红

    2015-01-01

    Cortex phellodendri is the dry bark of rutaceae plants Phellodendron chinense Schneid or Cortex phellodendri, which has characters of bitter and cold and effects of clearing heat,drying dampness,removing firelight and excepting steam,curing poison and sore.Cortex phellodendri has extensive pharmacological activities,such as antibacterial,antivi-ral,relieving cough,depressurization and enhance immunity,etc.Alkaloids are the main active ingredients in Cortex phellodendri,in which content of berberine is highest,which reaches to 1.4% ~5.8%.In addition,jateorrhizine,phel-lodendrine,palmatine,obaculactone and obacunone also occupy certain proportion.This article summarized the research progress on pharmacological effects of Cortex phellodendri and the extraction processes of its alkaloids.%黄柏为芸香科植物黄皮树或黄檗的干燥树皮,其性味苦寒,有清热燥湿,泻火除蒸,解毒疗疮之功效。黄柏具有广泛的药理活性,如抗菌、抗病毒、镇咳、降压以及增强免疫等。黄柏的主要活性成分为生物碱,其中小檗碱是含量最高的生物碱,可达1.4%~5.8%,另外药根碱、黄柏碱、掌叶防己碱以及黄柏内酯、黄柏酮等活性成分也占有一定比重。综述了黄柏的药理作用及其生物碱提取工艺研究进展。

  7. Simultaneous quantitation of 14 active components in Yinchenhao decoction by using ultra high performance liquid chromatography with diode array detection: Method development and ingredient analysis of different commonly prepared samples.

    Science.gov (United States)

    Yi, YaXiong; Zhang, Yong; Ding, Yue; Lu, Lu; Zhang, Tong; Zhao, Yuan; Xu, XiaoJun; Zhang, YuXin

    2016-11-01

    We developed a novel quantitative analysis method based on ultra high performance liquid chromatography coupled with diode array detection for the simultaneous determination of the 14 main active components in Yinchenhao decoction. All components were separated on an Agilent SB-C18 column by using a gradient solvent system of acetonitrile/0.1% phosphoric acid solution at a flow rate of 0.4 mL/min for 35 min. Subsequently, linearity, precision, repeatability, and accuracy tests were implemented to validate the method. Furthermore, the method has been applied for compositional difference analysis of 14 components in eight normal-extraction Yinchenhao decoction samples, accompanied by hierarchical clustering analysis and similarity analysis. The result that all samples were divided into three groups based on different contents of components demonstrated that extraction methods of decocting, refluxing, ultrasonication and extraction solvents of water or ethanol affected component differentiation, and should be related to its clinical applications. The results also indicated that the sample prepared by patients in the family by using water extraction employing a casserole was almost same to that prepared using a stainless-steel kettle, which is mostly used in pharmaceutical factories. This research would help patients to select the best and most convenient method for preparing Yinchenhao decoction.

  8. Simple and rapid high performance liquid chromatography method for the determination of polidocanol as bulk product and in pharmaceutical polymer matrices using charged aerosol detection.

    Science.gov (United States)

    Ilko, David; Puhl, Sebastian; Meinel, Lorenz; Germershaus, Oliver; Holzgrabe, Ulrike

    2015-02-01

    Currently, neither the European nor the United States Pharmacopoeia provide a method for the determination of polidocanol (PD) content despite the fact that PD, besides being an excipient, is also used as an active pharmaceutical ingredient. We therefore developed a method where the PD content was determined using a Kinetex C18 column operated at 40°C with water-acetonitrile (15:85, v/v) as mobile phase. A Corona(®) charged aerosol detector was employed for the detection of PD that is lacking a suitable UV chromophore. The method was fully validated. Additionally, the method was applied for the determination of PD release from a pharmaceutical polymer matrix consisting of poly-ɛ-caprolactone and poly(lactic-co-glycolic acid) and PD.

  9. HPLC Determination of 9 Active Ingredients in Arundina Graminifolia%高效液相色谱法测定竹叶兰中9种活性成分含量

    Institute of Scientific and Technical Information of China (English)

    李银科; 舒丽丹; 杨海英; 叶艳青; 李明

    2014-01-01

    A method of HPLC for the determination of 9 active ingredients in Arundina Graminifolia was proposed.The sample was extracted with methanol (8+2)solution by speedy and homogeneous pulping,and an aliquot of 5.0 mL of the extract was purified by passing through MCI-GEL RP-resin SPE column.An aliquot of 2.00 mL of the eluate was taken for HPLC analysis.Waters Xbridge chromatographic column was used as stationary phase and mixtures of methanol and acetic acid (0.5 +99.5)solution with different mixing ratios were used as mobile phase in the gradient elution.UV-detection at 275 nm was adopted in the determination.Linear relationships between values of peak area and mass concentration of the 9 active ingredients were kept in definite ranges.Detection limits (3S/N)found were ranged from 20 to 30 μg·L-1 .Values of recovery found by standard addition method were in the range of 96.4%-105%,with values of RSD′s (n=7)in the range of 1.5%-2.4%.%提出了高效液相色谱法测定竹叶兰中9种活性成分含量的方法。竹叶兰样品经甲醇(8+2)溶液高速匀浆提取,分取提取液5.0 mL,经 MCI-GEL 反相树脂固相萃取小柱净化,取2.00 mL净化液供色谱分析。净化液采用 Waters Xbridge 色谱柱为分离柱,用甲醇和乙酸(0.5+99.5)溶液以不同比例混合的混合液为流动相进行梯度洗脱,在检测波长275 nm 处进行测定。9种活性成分在一定的质量浓度范围内与其峰面积呈线性关系,方法的检出限(3S/N)在20~30μg·L-1之间。加标回收率在96.4%~105%之间,测定值的相对标准偏差(n=7)在1.5%~2.4%之间。

  10. Method development and validation for pharmaceutical tablets analysis using transmission Raman spectroscopy.

    Science.gov (United States)

    Li, Yi; Igne, Benoît; Drennen, James K; Anderson, Carl A

    2016-02-10

    The objective of the study is to demonstrate the development and validation of a transmission Raman spectroscopic method using the ICH-Q2 Guidance as a template. Specifically, Raman spectroscopy was used to determine niacinamide content in tablet cores. A 3-level, 2-factor full factorial design was utilized to generate a partial least-squares model for active pharmaceutical ingredient quantification. Validation of the transmission Raman model was focused on figures of merit from three independent batches manufactured at pilot scale. The resultant model statistics were evaluated along with the linearity, accuracy, precision and robustness assessments. Method specificity was demonstrated by accurate determination of niacinamide in the presence of niacin (an expected related substance). The method was demonstrated as fit for purpose and had the desirable characteristics of very short analysis times (∼2.5s per tablet). The resulting method was used for routine content uniformity analysis of single dosage units in a stability study.

  11. Development and validation of a method for active drug identification and content determination of ranitidine in pharmaceutical products using near-infrared reflectance spectroscopy: a parametric release approach.

    Science.gov (United States)

    Rosa, Sílvia S; Barata, Pedro A; Martins, José M; Menezes, José C

    2008-05-15

    In this paper we describe the strategy used in the development and validation of a near-infrared diffuse reflectance spectroscopy method for identification and quantification of ranitidine in pharmaceutical products (granulates, cores and coated tablets) at-line, with a fiber optic probe. This method was developed in a pharmaceutical industry for routine application, to replace reference methods and was submitted and approved to the National Medicine Regulatory Agency (Infarmed). We consider that this is the first step of a broader parametric release approach to pharmaceutical products.

  12. GC-MS Fingerprint of an Active Ingredients Group from Jinxuan Zhike Xunxi Powders%金玄痔科熏洗散有效部位制剂的GC-MS指纹图谱研究

    Institute of Scientific and Technical Information of China (English)

    别文华; 刘蔚; 李力; 周道年

    2015-01-01

    目的::对金玄痔科熏洗散及有效部位新制剂进行GC-MS分析,建立了有效部位新制剂的GC-MS指纹图谱。方法:采用GC-MS方法对金玄痔科熏洗散及有效部位新制剂中的主要组分进行分析,并确定指纹图谱中的特征指纹信息。结果:对10个批次的有效部位新制剂进行了测定,并得到了较为理想的包含特征信息的有效部位新制剂的GC-MS指纹图谱。结论:方法重复性好,所建立的指纹图谱为金玄痔科熏洗散有效部位新制剂的质量控制提供了有效手段。%Objective:To analyze Jinxuan Zhike Xunxi powders ( JZX) and an active ingredients group ( AIG) obtained from JZX by GC-MS, and develop a characteristic fingerprint of AIG. Methods: A gas chromatography-mass spectrum ( GC-MS) method was applied to analyze the main compositions in JZX and AIG, and the characteristic fingerprint information in the fingerprint spectrum was determined. Results:Totally 10 batches of AIG were detected, and a promising GC-MS fingerprint spectrum containing characteristic information for AIG was obtained. Conclusion: The developed fingerprint with good repeatability can be successfully applied in the quality control of AIG.

  13. [Pharmaceutical technology of Tensiomin].

    Science.gov (United States)

    Fekete, P

    1997-07-01

    The physical chemical properties, stability and incompatibility of captopril (the active ingredient of Tensiomin tablets) have been discussed. Captopril has two polimorphic crystal modifications, the form I. of higher melting point is applied in the therapy. Captopril has a better stability in solutions below pH 4, the degradation is accelerated by metallic ions (Cu, Fe). In solid phase the degradation is accelerated by the humidity of the air. No incompatibility was found with the tabletting excipients but stearic acid and sodium-carboxymethyl-starch. Under compaction at higher pressure captopril itself shows tendency for lamination. The dissolution rate of the Tensiomin tablets can meet the requirement of USP if direct tabletting method was used. In this case the breaking strength of the tablets has no influence on the dissolution rate. The main properties (weight uniformity, content uniformity, tensile strength, friability, disintegration time, dissolution time) of the Tensiomin tablets of 12.5 mg, 25 mg, 50 mg and 100 mg of captopril meet the requirement of USP not only after manufacturing but after the accelerated stability test of three month as well.

  14. Metabolic engineering: the ultimate paradigm for continuous pharmaceutical manufacturing.

    Science.gov (United States)

    Yadav, Vikramaditya G; Stephanopoulos, Gregory

    2014-07-01

    Research and development (R&D) expenditures by pharmaceutical companies doubled over the past decade, yet candidate attrition rates and development times rose markedly during this period. Understandably, companies have begun downsizing their pipelines and diverting investments away from R&D in favor of manufacturing. It is estimated that transitioning to continuous manufacturing could enable companies to compete for a share in emerging markets. Accordingly, the model for continuous manufacturing that has emerged commences with the conversion of late-stage intermediates into the active pharmaceutical ingredient (API) in a series of continuous flow reactors, followed by continuous solid processing to form finished tablets. The use of flow reactions for API synthesis will certainly generate purer products at higher yields in shorter times compared to equivalent batch reactions. However, transitioning from batch to flow configuration simply alleviates transport limitations within the reaction milieu. As the catalogue of reactions used in flow syntheses is a subset of batch-based chemistries, molecules such as natural products will continue to evade drug prospectors. Also, it is uncertain whether flow synthesis can deliver improvements in the atom and energy economies of API production at the scales that would achieve the levels of revenue growth targeted by companies. Instead, it is argued that implementing metabolic engineering for the production of oxidized scaffolds as gateway molecules for flow-based addition of electrophiles is a more effective and scalable strategy for accessing natural product chemical space. This new paradigm for manufacturing, with metabolic engineering as its engine, would also permit rapid optimization of production variables and allow facile scale-up from gram to ton scale to meet material requirements for clinical trials, thus recasting manufacturing as a tool for discovery.

  15. HPLC determination of 4 compounds in Jinxuan Zhike Xunxi powder and its active ingredients group%新老工艺的金玄痔科熏洗散4种成分含量比较

    Institute of Scientific and Technical Information of China (English)

    刘蔚; 叶晓川; 段雪云; 陈树和; 刘焱文

    2012-01-01

    目的:建立测定金玄痔科熏洗散(JZXS)及新工艺制备的金玄痔科熏洗散(AIG)中绿原酸、咖啡酸、金丝桃苷和木犀草素的HPLC分析方法.方法:采用Venusil XBP C18柱(250mm×4.6mm,5μm);柱温30℃;流速1.0mL·min-1;流动相:乙腈-0.4%磷酸水溶液,梯度洗脱;进样量10μL;检测波长为335nm.结果:绿原酸、咖啡酸、金丝桃苷、木犀草素的线形范围分别和回归方程分别为0.760~4.560μg (r=0.999 9),Y=2 254.9X+ 131.66;0.058~0.348μg (r=0.999 9),Y=3 610.8X+7.913 5;0.046~0.276 μg(r=0.999 9),y=1 446.7X+2.124 3;0.024~0.144μg(r=0.999 9),y=2 344.5 X -0.716 2;JZXS 平均加样回收率(n=5)分别为97.4%(RSD=1.8%),98.6%(RSD=2.3%)和97.8%(RSD=2.9%);AIG平均加样回收率(n=5)为97%(RSD=1.2%),97.3%(RSD=2.5%),98.12% (RSD=2.7%)和96.9% (RSD=1.9%).结论:该方法专属性好,准确度高,为进一步完善JZXS的质量标准提供了科学依据,并为该传统制剂二次开发为创新中药品种奠定了基础.%OBJECTIVE To establish an HPLC method for determination of chlorogenic acid, caffeic acid, hyperoside and luteoloside in Jinxuan Zhike Xunxi powder(JZXS) and its active ingredients group(AIG). METHODS RP-HPLC was used, the separation was performed on Venusil XBP C18 (250 m×4. 6 mm,5μm) column by gradient elution with acetonitrile -0. 4% phosphoric acid as the mobil phase. The detection wavelength was set at 335 nm and the flow rate was 1. 0 mL·min-1 , and column temperature was 30 ℃. RESULTS The linear ranges were 0. 760-4. 560μg (Y = 2 254. 9X + 131. 66, r = 0. 999 9) for chlorogenic acid, 0. 058 - 0. 348μg (Y = 3 610. 8X +7. 913 5, r=0.9999) for caffeic acid, 0. 046 - 0. 276μg (Y = 1 446.7X + 2. 124 3, r= 0. 999 9) for hyperoside and 0. 024 - 0. 144μg (Y= 2 344. 5X - 0. 716 2,r= 0. 999 9) for luteoloside. The recoveries (n = 5) were 97. 4%(RSD= 1. 8%) ,98. 6%(RSD=2. 3%) and 97. 8%(RSD= 2. 9%), respectively in Jinxuan Zhike Xunxi paoder, and

  16. [Importance of interfacial characteristics in pharmaceutical technology].

    Science.gov (United States)

    Dredán, Judit; Csóka, Gabriella; Marton, Sylvia; Antal, István

    2003-01-01

    Since drug release from the dosage forms has priority to absorption from the gastrointestinal system, physico-chemical characterisation of pharmaceutical systems is essential during the development of an optimal formulation with high efficacy and quality. Interfacial parameters of several pharmaceutical excipients were studied regarding their possible modifying effect on drug release from the dosage form. These inactive ingredients may influence the interfacial phenomena of the drug carrier system, which behaviour determines both the efficacy and the quality of the pharmaceutical preparation In this work authors deal mainly with the two introducing steps of the LADME model influenced by interfacial parameters on them, namely with the liberation of drug from the dosage form and with the characteristics influencing the absorption through biological membranes, respectively. The objective of the present work was to study modifying effects of excipients on drug liberation in connection with their physical and chemical characteristics such as interfacial tension of solid and liquid phases, wetting contact angle of solid phase and--a calculated quantity,--adhesion tension of the solid particles.

  17. Efficiency of membrane technology, activated charcoal, and a micelle-clay complex for removal of the acidic pharmaceutical mefenamic acid.

    Science.gov (United States)

    Khalaf, Samer; Al-Rimawi, Fuad; Khamis, Mustafa; Nir, Shlomo; Bufo, Sabino A; Scrano, Laura; Mecca, Gennaro; Karaman, Rafik

    2013-01-01

    The efficiency of sequential advanced membrane technology wastewater treatment plant towards removal of a widely used non-steroid anti-inflammatory drug (NSAID) mefenamic acid was investigated. The sequential system included activated sludge, ultrafiltration by hollow fibre membranes with 100 kDa cutoff, and spiral wound membranes with 20 kDa cutoff, activated carbon and a reverse osmosis (RO) unit. The performance of the integrated plant showed complete removal of mefenamic acid from spiked wastewater samples. The activated carbon column was the most effective component in removing mefenamic acid with a removal efficiency of 97.2%. Stability study of mefenamic acid in pure water and Al-Quds activated sludge revealed that the anti-inflammatory drug was resistant to degradation in both environments. Batch adsorption of mefenamic acid by activated charcoal and a composite micelle (otadecyltrimethylammonium (ODTMA)-clay (montmorillonite) was determined at 25.0°C. Langmuir isotherm was found to fit the data with Qmax of 90.9 mg g(-1) and 100.0 mg g(-1) for activated carbon and micelle-clay complex, respectively. Filtration experiment by micelle-clay columns mixed with sand in the mg L(-1) range revealed complete removal of the drug with much larger capacity than activated carbon column. The combined results demonstrated that an integration of a micelle-clay column in the plant system has a good potential to improve the removal efficiency of the plant towards NSAID drugs such as mefenamic acid.

  18. An introduction to toothpaste - its purpose, history and ingredients.

    Science.gov (United States)

    Lippert, Frank

    2013-01-01

    Toothpaste is a paste or gel to be used with a toothbrush to maintain and improve oral health and aesthetics. Since their introduction several thousand years ago, toothpaste formulations have evolved considerably - from suspensions of crushed egg shells or ashes to complex formulations with often more than 20 ingredients. Among these can be compounds to combat dental caries, gum disease, malodor, calculus, erosion and dentin hypersensitivity. Furthermore, toothpastes contain abrasives to clean and whiten teeth, flavors for the purpose of breath freshening and dyes for better visual appeal. Effective toothpastes are those that are formulated for maximum bioavailability of their actives. This, however, can be challenging as compromises will have to be made when several different actives are formulated in one phase. Toothpaste development is by no means complete as many challenges and especially the poor oral substantivity of most active ingredients are yet to overcome.

  19. 基于均匀设计的中药有效组分复方配伍研究%Uniform designed research on the active ingredients assembling of Chinese herbal for antioxidative capacity

    Institute of Scientific and Technical Information of China (English)

    杨鸿; 吴彦; 马琰岩; 吕俊海; 李晶哲

    2012-01-01

    Objective To find a suitable way of quantitative composition-activity relationship of Chinese herbal for antioxidative capacity based on uniform design. Method Chinese herbal active ingredient formula was composed of Total flavonoids of Glycyrrhiza (TFG) , ginkgo biloba extract (GBE) , Total fa-vonoids of epimedium (TFE) and astragaloside (AST) . The herbal efficacy was detected by scavenging the free radical of DPPH in vitro, and the mathematical model was constructed to describe the connection between different combinations and their antioxidative capacity by the method of LARS regression. Result The best effect was in the ratio of TFG 0. 8 mg/ml,GBE 3.144 mg/ml,TFE 0.024 mg/ml,AST 0.036 mg/ml. Conclusion Uniform designed research is one of efficient ways to describe the quantitative composition-activity relationship.%目的 探索基于均匀设计的中药抗氧化有效组分复方的研究分析方法.方法 采用均匀设计和改进最小角回归分析,对甘草总黄酮、银杏叶提取物、淫羊藿总黄酮和黄芪总苷组成的中药组分复方不同配比体外清除DPPH自由基的作用进行研究.结果 通过分析获得了中药组分配伍清除DPPH的回归方程,优化组合后进行药效学验证,结果显示该中药组分配伍最佳剂量组合为甘草总黄酮0.8 mg/ml、银杏叶提取物3.144 mg/ml、淫羊藿总黄酮0.024 mg/ml和黄芪总苷0.036 mg/ml.结论 上述中药组分配伍后能有效清除DPPH自由基;本实验采用的均匀设计结合改进最小角回归分析适合"非线性、小样本"生物实验数据数据分析,为筛选评价抗氧化中药有效组分复方提供了合适的研究方法.

  20. UV-vis light activated Ag decorated monodisperse TiO2 for treatment of pharmaceuticals in water

    Science.gov (United States)

    Recently, many researchers have made a lot of effort to utilize the visible light portion of the solar spectrum to activate TiO2 photocatalyst for environmental applications, such as water, air, and soil remediation. The deposition of noble metals on photocatalysts is of great in...

  1. Public policy and pharmaceutical innovation.

    Science.gov (United States)

    Grabowski, H G

    1982-09-01

    Historically, new drug introductions have played a central role in medical progress and the availability of cost-effective therapies. Nevertheless, public policy toward pharmaceuticals has been characterized in recent times by increasingly stringent regulatory controls, shorter effective patent terms, and increased encouragement of generic product usage. This has had an adverse effect on the incentives and capabilities of firms to undertake new drug research and development activity. The industry has experienced sharply rising research and development costs, declining annual new drug introductions, and fewer independent sources of drug development. This paper considers the effects of government regulatory policies on the pharmaceutical innovation process from several related perspectives. It also examines the merits of current public policy proposals designed to stimulate drug innovation including patent restoration and various regulatory reform measures.

  2. Effects of effluent organic matter characteristics on the removal of bulk organic matter and selected pharmaceutically active compounds during managed aquifer recharge: Column study

    Science.gov (United States)

    Maeng, Sung Kyu; Sharma, Saroj K.; Abel, Chol D. T.; Magic-Knezev, Aleksandra; Song, Kyung-Guen; Amy, Gary L.

    2012-10-01

    Soil column experiments were conducted to investigate the effects of effluent organic matter (EfOM) characteristics on the removal of bulk organic matter (OM) and pharmaceutically active compounds (PhACs) during managed aquifer recharge (MAR) treatment processes. The fate of bulk OM and PhACs during an MAR is important to assess post-treatment requirements. Biodegradable OM from EfOM, originating from biological wastewater treatment, was effectively removed during soil passage. Based on a fluorescence excitation-emission matrix (F-EEM) analysis of wastewater effluent-dominated (WWE-dom) surface water (SW), protein-like substances, i.e., biopolymers, were removed more favorably than fluorescent humic-like substances under oxic compared to anoxic conditions. However, there was no preferential removal of biopolymers or humic substances, determined as dissolved organic carbon (DOC) observed via liquid chromatography with online organic carbon detection (LC-OCD) analysis. Most of the selected PhACs exhibited removal efficiencies of greater than 90% in both SW and WWE-dom SW. However, the removal efficiencies of bezafibrate, diclofenac and gemfibrozil were relatively low in WWE-dom SW, which contained more biodegradable OM than did SW (copiotrophic metabolism). Based on this study, low biodegradable fractions such as humic substances in MR may have enhanced the degradation of diclofenac, gemfibrozil and bezafibrate by inducing an oligotrophic microbial community via long term starvation. Both carbamazepine and clofibric acid showed persistent behaviors and were not influenced by EfOM.

  3. Changes in phytochemical synthesis, chalcone synthase activity and pharmaceutical qualities of sabah snake grass (Clinacanthus nutans L.) in relation to plant age.

    Science.gov (United States)

    Ghasemzadeh, Ali; Nasiri, Alireza; Jaafar, Hawa Z E; Baghdadi, Ali; Ahmad, Izham

    2014-10-30

    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 contents of TF (6.32 mg/g dry weight [DW]) and total phenolic (TP) (18.21 mg/g DW) were recorded in 6-month-old buds. Among the flavonoids isolated in this study the most important ones based on concentration were from high to low as follows: catechin > quercetin > kaempferol > luteolin. Production of phenolic acids increased from 1 to 6 months, but after 6 months up to 1 year of age, they decreased significantly. The highest contents of caffeic acid (0.307 mg/g DW) and gallic acid (5.96 mg/g DW) were recorded in 1-year and 6-month-old buds, respectively. The lowest and highest activity of CHS was recorded in 1-month and 6-month-old buds with values of 3.6 and 9.5 nkat/mg protein, respectively. These results indicate that the increment in flavonoids and phenolic acids in 6-month-old buds can be attributed to an increase in CHS activity. The highest 1,1-diphenyl-2-picrylhydrazyl (DPPH) activity was observed in the extract of 1-year-old buds followed by 6-month-old buds, with 50% of free radical scavenging (IC50) values of 64.6 and 73.5 µg/mL, respectively. Interestingly, a ferric reducing antioxidant power (FRAP) assay showed a higher activity in 6-month-old buds (488 μM of Fe(II)/g) than in 1-year-old buds (453 μM of Fe(II)/g), in contrast to the DPPH result. Significant correlations (p < 0.05) were observed between CHS enzyme activity and FRAP activity, TF, catechin, and kaempferol content. Extracts of 6-month-old bud exhibited a significant in vitro anticancer activity against

  4. Changes in Phytochemical Synthesis, Chalcone Synthase Activity and Pharmaceutical Qualities of Sabah Snake Grass (Clinacanthus nutans L. in Relation to Plant Age

    Directory of Open Access Journals (Sweden)

    Ali Ghasemzadeh

    2014-10-01

    Full Text Available 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 contents of TF (6.32 mg/g dry weight [DW] and total phenolic (TP (18.21 mg/g DW were recorded in 6-month-old buds. Among the flavonoids isolated in this study the most important ones based on concentration were from high to low as follows: catechin > quercetin > kaempferol > luteolin. Production of phenolic acids increased from 1 to 6 months, but after 6 months up to 1 year of age, they decreased significantly. The highest contents of caffeic acid (0.307 mg/g DW and gallic acid (5.96 mg/g DW were recorded in 1-year and 6-month-old buds, respectively. The lowest and highest activity of CHS was recorded in 1-month and 6-month-old buds with values of 3.6 and 9.5 nkat/mg protein, respectively. These results indicate that the increment in flavonoids and phenolic acids in 6-month-old buds can be attributed to an increase in CHS activity. The highest 1,1-diphenyl-2-picrylhydrazyl (DPPH activity was observed in the extract of 1-year-old buds followed by 6-month-old buds, with 50% of free radical scavenging (IC50 values of 64.6 and 73.5 µg/mL, respectively. Interestingly, a ferric reducing antioxidant power (FRAP assay showed a higher activity in 6-month-old buds (488 μM of Fe(II/g than in 1-year-old buds (453 μM of Fe(II/g, in contrast to the DPPH result. Significant correlations (p < 0.05 were observed between CHS enzyme activity and FRAP activity, TF, catechin, and kaempferol content. Extracts of 6-month-old bud exhibited a significant in vitro anticancer activity

  5. [Rapid analysis of added ingredients in heroin].

    Science.gov (United States)

    Wang, Ji-fen; Yu, Jing; Guo, Xin; Sun, Xing-long; Wang, Ding-fang

    2011-07-01

    The method of rapid analysis of added ingredients in heroin was studied in the present paper. Adding sucrose, fructose, glucose, starch, caffeine and phenacetin to heroin with a certain percentage, the changes in the infrared spectrum with the concentration of heroin increasing and the detection limit of the additives were determined. Whether or not heroin can be detected in the sample with high concentration of added ingredients was studied using Raman spectroscopy. Similarly, in high purity of heroin, whether or not Raman spectroscopy can detect the added ingredients was tested. Through systematic experiments, the results showed that: using infrared spectroscopy and Raman spectroscopy to test the added ingredients of heroin is a rapid and effective method. Each has both advantages and disadvantages. We should select the appropriate method according to the actual cases.

  6. Amorphous pharmaceutical solids.

    Science.gov (United States)

    Vranić, Edina

    2004-07-01

    Amorphous forms are, by definition, non-crystalline materials which possess no long-range order. Their structure can be thought of as being similar to that of a frozen liquid with the thermal fluctuations present in a liquid frozen out, leaving only "static" structural disorder. The amorphous solids have always been an essential part of pharmaceutical research, but the current interest has been raised by two developments: a growing attention to pharmaceutical solids in general, especially polymorphs and solvates and a revived interest in the science of glasses and the glass transition. Amorphous substances may be formed both intentionally and unintentionally during normal pharmaceutical manufacturing operations. The properties of amorphous materials can be exploited to improve the performance of pharmaceutical dosage forms, but these properties can also give rise to unwanted effects that need to be understood and managed in order for the systems to perform as required.

  7. Pharmaceutical Industry Develops Steadily

    Institute of Scientific and Technical Information of China (English)

    2007-01-01

    @@ With the development of the economy, the growth of the total population, the growing proportion of older citizens, and the increasing awareness of people's health care,the pharmaceutical market in China has seen a sustained and rapid expansion.

  8. ENRICHMENT OF POULTRY PRODUCTS WITH FUNCTIONAL INGREDIENTS

    OpenAIRE

    Gordana Kralik; Zlata Kralik; Manuela Grčević; Zoran Škrtić

    2012-01-01

    Primary role of food is to provide nutritive stuffs in sufficient amounts to meet nutritive requirements. However, recent scientific findings confirm assumptions that particular food or its ingredients had positive physiological and psychological effects on health. Functional food is referred to food rich in ingredients, having beneficial effects on one or more functions in an organism. By consuming functional food consumers can expect some health benefits. Production of poultry products as f...

  9. Pharmaceuticals: pharmaceutical cost controls--2005. End of Year Issue Brief.

    Science.gov (United States)

    Seay, Melicia; Varma, Priya

    2005-12-31

    and 2005 legislative activity surrounding the most commonly used and emerging pharmaceutical cost control measures.

  10. Linear model applied to the evaluation of pharmaceutical stability data

    Directory of Open Access Journals (Sweden)

    Renato Cesar Souza

    2013-09-01

    Full Text Available The expiry date on the packaging of a product gives the consumer the confidence that the product will retain its identity, content, quality and purity throughout the period of validity of the drug. The definition of this term in the pharmaceutical industry is based on stability data obtained during the product registration. By the above, this work aims to apply the linear regression according to the guideline ICH Q1E, 2003, to evaluate some aspects of a product undergoing in a registration phase in Brazil. With this propose, the evaluation was realized with the development center of a multinational company in Brazil, with samples of three different batches composed by two active principal ingredients in two different packages. Based on the preliminary results obtained, it was possible to observe the difference of degradation tendency of the product in two different packages and the relationship between the variables studied, added knowledge so new models of linear equations can be applied and developed for other products.

  11. Rational coformer or solvent selection for pharmaceutical cocrystallization or desolvation.

    Science.gov (United States)

    Abramov, Yuriy A; Loschen, Christoph; Klamt, Andreas

    2012-10-01

    It is demonstrated that the fluid-phase thermodynamics theory conductor-like screening model for real solvents (COSMO-RS) as implemented in the COSMOtherm software can be used for accurate and efficient screening of coformers for active pharmaceutical ingredient (API) cocrystallization. The excess enthalpy, H(ex) , between an API-coformer mixture relative to the pure components reflects the tendency of those two compounds to cocrystallize. Thus, predictive calculations may be performed with decent effort on a large set of molecular data in order to identify potentially new cocrystal systems. In addition, it is demonstrated that COSMO-RS theory allows reasonable ranking of coformers for API solubility improvement. As a result, experiments may be focused on those coformers, which have an increased probability of cocrystallization, leading to the largest improvement of the API solubility. In a similar way as potential coformers are identified for cocrystallization, solvents that do not tend to form solvates may be determined based on the highest H(ex) s with the API. The approach was successfully tested on tyrosine kinase inhibitor axitinib, which has a propensity to form relatively stable solvated structures with the majority of common solvents, as well as on thiophanate-methyl and thiophanate-ethyl benzimidazole fungicides, which form channel solvates.

  12. Commercial production of specialty chemicals and pharmaceuticals from biomass

    Energy Technology Data Exchange (ETDEWEB)

    McChesney, J.D. [Univ. of Mississippi, University, MS (United States)

    1993-12-31

    The chemical substances utilized in consumer products, and for pharmaceutical and agricultural uses are generally referred to as specialty chemicals. These may be flavor or fragrance substances, intermediates for synthesis of drugs or agrochemicals or the drugs or agrochemicals themselves, insecticides or insect pheromones or antifeedants, plant growth regulators, etc. These are in contrast to chemicals which are utilized in large quantities for fuels or preparation of plastics, lubricants, etc., which are usually referred to as industrial chemicals. The specific utilization of specialty chemicals is associated with a specific important physiochemical or biological property. They may possess unique properties as lubricants or waxes or have a very desirable biological activity such as a drug, agrochemical or perfume ingredient. These unique properties convey significant economic value to the specific specialty chemical. The economic commercial production of specialty chemicals commonly requires the isolation of a precursor or the specialty chemical itself from a natural source. The discovery, development and commercialization of specialty chemicals is presented and reviewed. The economic and sustainable production of specialty chemicals is discussed.

  13. Engineering an enantioselective amine oxidase for the synthesis of pharmaceutical building blocks and alkaloid natural products.

    Science.gov (United States)

    Ghislieri, Diego; Green, Anthony P; Pontini, Marta; Willies, Simon C; Rowles, Ian; Frank, Annika; Grogan, Gideon; Turner, Nicholas J

    2013-07-24

    The development of cost-effective and sustainable catalytic methods for the production of enantiomerically pure chiral amines is a key challenge facing the pharmaceutical and fine chemical industries. This challenge is highlighted by the estimate that 40-45% of drug candidates contain a chiral amine, fueling a demand for broadly applicable synthetic methods that deliver target structures in high yield and enantiomeric excess. Herein we describe the development and application of a "toolbox" of monoamine oxidase variants from Aspergillus niger (MAO-N) which display remarkable substrate scope and tolerance for sterically demanding motifs, including a new variant, which exhibits high activity and enantioselectivity toward substrates containing the aminodiphenylmethane (benzhydrylamine) template. By combining rational structure-guided engineering with high-throughput screening, it has been possible to expand the substrate scope of MAO-N to accommodate amine substrates containing bulky aryl substituents. These engineered MAO-N biocatalysts have been applied in deracemization reactions for the efficient asymmetric synthesis of the generic active pharmaceutical ingredients Solifenacin and Levocetirizine as well as the natural products (R)-coniine, (R)-eleagnine, and (R)-leptaflorine. We also report a novel MAO-N mediated asymmetric oxidative Pictet-Spengler approach to the synthesis of (R)-harmicine.

  14. Syntheses of biologically active natural products and leading compounds for new pharmaceuticals employing effective construction of a polycyclic skeleton.

    Science.gov (United States)

    Ihara, Masataka

    2006-06-01

    Cascade reactions are useful methods for the construction of polycyclic skeletons, which are important cores for biological activities. A variety of cascade reactions carried out under multiple reaction conditions, such as pericyclic, polar, radical, and transition metal-catalyzed reaction conditions, have been investigated. Culmorin, pentalenene, pentalenic acid, deoxypentalenic acid, longiborneol, cedrandiol, 8,14-cedranoxide, atisirene, atisine, and estrane-type steroids were synthesized via the intramolecular double Michael reaction. Aza double Michael reaction was applied to the syntheses of tylophorine, epilupinine, tacamonine, and paroxetine. Furthermore, sequential Michael and aldol reactions were performed in both intramolecular and intermolecular manners, leading to the formation of polycyclic compounds fused to a four-membered ring. Synthesis of paesslerin A utilizing a multicomponent cascade reaction revealed an error in the proposed structure. Unique cascade reactions carried out under radical and transition metal-catalyzed reaction conditions were also investigated. With the combination of several cascade reactions, serofendic acids and methyl 7beta-hydroxykaurenoate, both of which have neuroprotective activity, were synthesized in a selective manner.

  15. [The methods for the protection against counterfeit medications. Part 1. The estimation of the quality of metoprolol succinate substance and tablets from different manufacturers in terms of "identity" and "active ingredient content"].

    Science.gov (United States)

    Iakushev, V A; Morozova, M A; Elizarova, T E; Fitilev, S B; Pletneva, T V

    2012-01-01

    This paper was designed to report the results of analysis of metoprolol succinate substance and tablets obtained from two manufacturers, Akrikhin (Russia) and AstraZeneca (Sweden). The analysis was performed by spectroscopy in the near IR region and followed by the chemometric treatment of the data obtained. The method was used to confirm the "identity" of metoprolol succinate tablets. The approach to distinguishing the differences between pharmaceutical dosage forms produced by different manufacturers is proposed. Also, the method for the qualitative determination of metoprolol succinate in the pharmaceutical formulations has been developed.

  16. Pharmaceutical dust exposure at pharmacies using automatic dispensing machines: a preliminary study.

    Science.gov (United States)

    Fent, Kenneth W; Durgam, Srinivas; Mueller, Charles

    2014-01-01

    Automatic dispensing machines (ADMs) used in pharmacies concentrate and dispense large volumes of pharmaceuticals, including uncoated tablets that can shed dust. We evaluated 43 employees' exposures to pharmaceutical dust at three pharmacies where ADMs were used. We used an optical particle counter to identify tasks that generated pharmaceutical dust. We collected 72 inhalable dust air samples in or near the employees' breathing zones. In addition to gravimetric analysis, our contract laboratory used internal methods involving liquid chromatography to analyze these samples for active pharmaceutical ingredients (APIs) and/or lactose, an inactive filler in tablets. We had to choose samples for these additional analyses because many methods used different extraction solvents. We selected 57 samples for analysis of lactose. We used real-time particle monitoring results, observations, and information from employees on the dustiness of pharmaceuticals to select 28 samples (including 13 samples that were analyzed for lactose) for analysis of specific APIs. Pharmaceutical dust was generated during a variety of tasks like emptying and refilling of ADM canisters. Using compressed air to clean canisters and manual count machines produced the overall highest peak number concentrations (19,000-580,000 particles/L) of smallest particles (count median aerodynamic diameter ≤ 2 μm). Employees who refilled, cleaned, or repaired ADM canisters, or hand filled prescriptions were exposed to higher median air concentrations of lactose (5.0-12 μg/m(3)) than employees who did other jobs (0.04-1.3 μg/m(3)), such as administrative/office work, labeling/packaging, and verifying prescriptions. We detected 10 APIs in air, including lisinopril, a drug prescribed for high blood pressure, levothyroxine, a drug prescribed for hypothyroidism, and methotrexate, a hazardous drug prescribed for cancer and other disorders. Three air concentrations of lisinopril (1.8-2.7 μg/m(3)) exceeded the lower

  17. PHARMACEUTICALS AS UBIQUITOUS POLLUTANTS ...

    Science.gov (United States)

    Those chemical pollutants that are regulated under various international, federal, and state programs represent but a small fraction of the universe of chemicals that occur in the environment as a result of both natural processes and human influence. Although this galaxy of targeted chemicals might be minuscule compared with the universe of both known and yet-to-be identified chemicals, an implicit assumption is that these selective lists of chemicals are responsible for the most significant share of risk with respect to environmental or economic impairment or to human health. Pharmaceuticals and personal care products (PPCPs) comprise a particularly large and diverse array of unregulated pollutants that occur in the environment from the combined activities and actions of multitudes of individuals as well as from veterinary and agricultural use. Although the concentration of any individual PPCP rarely ever exceeds the sub-ppm level (if present in drinking water, concentrations of individual PPCPs are generally less than the ppt-ppb level), evidence is accumulating that these trace-Ievel pollutants are ubiquitous, they can have a continuous presence regardless of environmental half-lives ( e.g., where sanitary wastewaters enter the environment), and the numbers of distinct and varied chemical entities could be extremely large (given that thousands are in commercial use). The research focused on in the subtasks is the development and application of state-of the-ar

  18. Analytical protocol for the sensitive determination of mannitol, sorbitol and glucose containing powders in pharmaceutical workplaces by ion chromatography using a pulsed amperometric detector.

    Science.gov (United States)

    Butler, Owen; Forder, James; Saunders, John

    2015-03-15

    Workers in the pharmaceutical industry can potentially be exposed to airborne dusts and powders that can contain potent active pharmaceutical ingredients (API). Occupational hygienists and health and safety professionals need to assess and ultimately minimise such inhalation and dermal exposure risks. Containment of dusts at source is the first line of defence but the performance of such technologies needs to be verified, for which purpose the good practice guide: assessing the particulate containment performance of pharmaceutical equipment, produced by the International Society for Pharmaceutical Engineering (ISPE), is a widely used reference document. This guide recommends the use of surrogate powders that can be used to challenge the performance of such containment systems. Materials such as lactose and mannitol are recommended as their physical properties (adhesion, compactability, dustiness, flow characteristics and particle sizes) mimic those of API-containing materials typically handled. Furthermore they are safe materials to use, are available in high purity and can be procured at a reasonable cost. The aim of this work was to develop and validate a sensitive ion-chromatography based analytical procedure for the determination of surrogate powders collected on filter samples so as to meet analytical requirements set out in this ISPE guide.

  19. ¹³C solid-state NMR analysis of the most common pharmaceutical excipients used in solid drug formulations, Part I: Chemical shifts assignment.

    Science.gov (United States)

    Pisklak, Dariusz Maciej; Zielińska-Pisklak, Monika Agnieszka; Szeleszczuk, Łukasz; Wawer, Iwona

    2016-04-15

    Solid-state NMR is an excellent and useful method for analyzing solid-state forms of drugs. In the (13)C CP/MAS NMR spectra of the solid dosage forms many of the signals originate from the excipients and should be distinguished from those of active pharmaceutical ingredient (API). In this work the most common pharmaceutical excipients used in the solid drug formulations: anhydrous α-lactose, α-lactose monohydrate, mannitol, sucrose, sorbitol, sodium starch glycolate type A and B, starch of different origin, microcrystalline cellulose, hypromellose, ethylcellulose, methylcellulose, hydroxyethylcellulose, sodium alginate, magnesium stearate, sodium laurilsulfate and Kollidon(®) were analyzed. Their (13)C CP/MAS NMR spectra were recorded and the signals were assigned, employing the results (R(2): 0.948-0.998) of GIPAW calculations and theoretical chemical shifts. The (13)C ssNMR spectra for some of the studied excipients have not been published before while for the other signals in the spectra they were not properly assigned or the assignments were not correct. The results summarize and complement the data on the (13)C ssNMR analysis of the most common pharmaceutical excipients and are essential for further NMR studies of API-excipient interactions in the pharmaceutical formulations.

  20. The supernova rate: a critical ingredient and an important tool

    CERN Document Server

    Mannucci, F

    2009-01-01

    In this review I summarize the role of supernova rate as a critical ingredient of modern astrophysics, and as an important tool to understand SN explosions. Many years of active observations and theoretical modeling have produced several important results. In particular, linking SN rates with parent stellar populations has proved to be an important strategy. Despite these advances, the situation is far from clear, in particular for the SNe Ia.

  1. Role of biodegradation in the removal of pharmaceutically active compounds with different bulk organic matter characteristics through managed aquifer recharge: Batch and column studies

    KAUST Repository

    Maeng, Sungkyu

    2011-10-01

    Natural water treatment systems such as bank filtration have been recognized as providing effective barriers in the multi-barrier approach for attenuation of organic micropollutants for safe drinking water supply. In this study, the role of biodegradation in the removal of selected pharmaceutically active compounds (PhACs) during soil passage was investigated. Batch studies were conducted to investigate the removal of 13 selected PhACs from different water sources with respect to different sources of biodegradable organic matter. Neutral PhACs (phenacetine, paracetamol, and caffeine) and acidic PhACs (ibuprofen, fenoprofen, bezafibrate, and naproxen) were removed with efficiencies greater than 88% from different organic matter water matrices during batch studies (hydraulic retention time (HRT): 60 days). Column experiments were then performed to differentiate between biodegradation and sorption with regard to the removal of selected PhACs. In column studies, removal efficiencies of acidic PhACs (e.g., analgesics) decreased under conditions of limited biodegradable carbon. The removal efficiencies of acidic PhACs were found to be less than 21% under abiotic conditions. These observations were attributed to sorption under abiotic conditions established by a biocide (20 mM sodium azide), which suppresses microbial activity/biodegradation. However, under biotic conditions, the removal efficiencies of these acidic PhACs were found to be greater than 59%. This is mainly attributed to biodegradation. Moreover, the average removal efficiencies of hydrophilic (polar) neutral PhACs (paracetamol, pentoxifylline, and caffeine) with low octanol/water partition coefficients (log K ow less than 1) were low (11%) under abiotic conditions. However, under biotic conditions, removal efficiencies of the neutral PhACs were greater than 98%. In contrast, carbamazepine persisted and was not easily removed under either biotic or abiotic conditions. This study indicates that biodegradation

  2. Phenolic content and antioxidant properties of green chilli paste and its ingredients

    Directory of Open Access Journals (Sweden)

    Griangsak Chairote

    2010-05-01

    Full Text Available Green chilli paste and its ingredients (chilli, red onion and garlic from different stages of processing were analysed for total phenolic content and antioxidant properties, i.e. total antioxidant capacity, DPPH radical scavenging activity, and β-carotene bleaching activity. The effects of processing stage on total phenolic content and antioxidant properties of green chilli paste and its ingredients were discussed, along with the correlation between the total phenolic content and the antioxidant properties.

  3. Infrared imaging spectroscopy and chemometric tools for in situ analysis of an imiquimod pharmaceutical preparation presented as cream

    Science.gov (United States)

    Carneiro, Renato Lajarim; Poppi, Ronei Jesus

    2014-01-01

    In the present work the homogeneity of a pharmaceutical formulation presented as a cream was studied using infrared imaging spectroscopy and chemometric methodologies such as principal component analysis (PCA) and multivariate curve resolution with alternating least squares (MCR-ALS). A cream formulation, presented as an emulsion, was prepared using imiquimod as the active pharmaceutical ingredient (API) and the excipients: water, vaseline, an emulsifier and a carboxylic acid in order to dissolve the API. After exposure at 45 °C during 3 months to perform accelerated stability test, the presence of some crystals was observed, indicating homogeneity problems in the formulation. PCA exploratory analysis showed that the crystal composition was different from the composition of the emulsion, since the score maps presented crystal structures in the emulsion. MCR-ALS estimated the spectra of the crystals and the emulsion. The crystals presented amine and C-H bands, suggesting that the precipitate was a salt formed by carboxylic acid and imiquimod. These results indicate the potential of infrared imaging spectroscopy in conjunction with chemometric methodologies as an analytical tool to ensure the quality of cream formulations in the pharmaceutical industry.

  4. Hot-melt extruded filaments based on pharmaceutical grade polymers for 3D printing by fused deposition modeling.

    Science.gov (United States)

    Melocchi, Alice; Parietti, Federico; Maroni, Alessandra; Foppoli, Anastasia; Gazzaniga, Andrea; Zema, Lucia

    2016-07-25

    Fused deposition modeling (FDM) is a 3D printing technique based on the deposition of successive layers of thermoplastic materials following their softening/melting. Such a technique holds huge potential for the manufacturing of pharmaceutical products and is currently under extensive investigation. Challenges in this field are mainly related to the paucity of adequate filaments composed of pharmaceutical grade materials, which are needed for feeding the FDM equipment. Accordingly, a number of polymers of common use in pharmaceutical formulation were evaluated as starting materials for fabrication via hot melt extrusion of filaments suitable for FDM processes. By using a twin-screw extruder, filaments based on insoluble (ethylcellulose, Eudragit(®) RL), promptly soluble (polyethylene oxide, Kollicoat(®) IR), enteric soluble (Eudragit(®) L, hydroxypropyl methylcellulose acetate succinate) and swellable/erodible (hydrophilic cellulose derivatives, polyvinyl alcohol, Soluplus(®)) polymers were successfully produced, and the possibility of employing them for printing 600μm thick disks was demonstrated. The behavior of disks as barriers when in contact with aqueous fluids was shown consistent with the functional application of the relevant polymeric components. The produced filaments were thus considered potentially suitable for printing capsules and coating layers for immediate or modified release, and, when loaded with active ingredients, any type of dosage forms.

  5. The use of net analyte signal (NAS) in near infrared spectroscopy pharmaceutical applications: interpretability and figures of merit.

    Science.gov (United States)

    Sarraguça, Mafalda Cruz; Lopes, João Almeida

    2009-05-29

    Near infrared spectroscopy (NIRS) has been extensively used as an analytical method for quality control of solid dosage forms for the pharmaceutical industry. Pharmaceutical formulations can be extremely complex, containing typically one or more active product ingredients (API) and various excipients, yielding very complex near infrared (NIR) spectra. The NIR spectra interpretability can be improved using the concept of net analyte signal (NAS). NAS is defined as the part of the spectrum unique to the analyte of interest. The objective of this work was to compare two different methods to estimate the API's NAS vector of different pharmaceutical formulations. The main difference between the methods is the knowledge of API free formulations NIR spectra. The comparison between the two methods was assessed in a qualitative and quantitative way. Results showed that both methods produced good results in terms of the similarity between the NAS vector and the pure API spectrum, as well as in the ability to predict the API concentration of unknown samples. Moreover, figures of merit such as sensitivity, selectivity, and limit of detection were estimated in a straightforward manner.

  6. [E-commerce of pharmaceuticals].

    Science.gov (United States)

    Shani, Segev

    2003-05-01

    The emergence of the Internet as a new communications and information technology caused major social and cultural changes. The dramatic increase in accessibility and availability of information empowered the consumer by closing the information gap between the consumer and different suppliers. The objective of this article is to review many new internet-supported applications related to the pharmaceutical market. E-commerce is divided into two major components: Business to Consumer (B to C), and Business to Business (B to B). The main applications in B to C are dissemination of medical and drug information, and the sale of drugs through the Internet. Medical information on the Internet is vast and very helpful for patients, however, its reliability is not guaranteed. Online pharmacies increase the accessibility and availability of drugs. Nevertheless, several obstacles such as security of the data provided (both financial and clinical) prevent the widespread use of online pharmacies. Another risk is the health authorities' inability to regulate Internet sites effectively. Therefore, unregulated sale of prescription drugs, fake or substandard, often occurs on the Internet. B to B relates to physicians, clinics, hospitals, HMO's and pharmaceutical companies. There is a vast number of applications ranging from clinical research, marketing and sales promotion, to drug distribution and logistics. In conclusion, the Internet is dynamic and has contributed to the development of numerous new applications in the field of pharmaceuticals. Regulatory authorities should be active in developing new policies that will deal with those new Internet-based applications.

  7. Burning characteristics of chemically isolated biomass ingredients

    Energy Technology Data Exchange (ETDEWEB)

    Haykiri-Acma, H.; Yaman, S.; Kucukbayrak, S. [Istanbul Technical University, Chemical and Metallurgical Engineering Faculty, Chemical Engineering Department, 34469 Maslak, Istanbul (Turkey)

    2011-01-15

    This study was performed to investigate the burning characteristics of isolated fractions of a biomass species. So, woody shells of hazelnut were chemically treated to obtain the fractions of extractives-free bulk, lignin, and holocellulose. Physical characterization of these fractions were determined by SEM technique, and the burning runs were carried out from ambient to 900 C applying thermal analysis techniques of TGA, DTG, DTA, and DSC. The non-isothermal model of Borchardt-Daniels was used to DSC data to find the kinetic parameters. Burning properties of each fraction were compared to those of the raw material to describe their effects on burning, and to interpret the synergistic interactions between the fractions in the raw material. It was found that each of the fractions has its own characteristic physical and thermal features. Some of the characteristic points on the thermograms of the fractions could be followed definitely on those of the raw material, while some of them seriously shifted to other temperatures or disappeared as a result of the co-existence of the ingredients. Also, it is concluded that the presence of hemicellulosics and celluloses makes the burning of lignin easier in the raw material compared to the isolated lignin. The activation energies can be arranged in the order of holocellulose < extractives-free biomass < raw material < lignin. (author)

  8. Biochemical basis for functional ingredient design from fruits.

    Science.gov (United States)

    Jacob, Jissy K; Tiwari, Krishnaraj; Correa-Betanzo, Julieta; Misran, Azizah; Chandrasekaran, Renu; Paliyath, Gopinadhan

    2012-01-01

    Functional food ingredients (nutraceuticals) in fruits range from small molecular components, such as the secondary plant products, to macromolecular entities, e.g., pectin and cellulose, that provide several health benefits. In fruits, the most visible functional ingredients are the color components anthocyanins and carotenoids. In addition, several other secondary plant products, including terpenes, show health beneficial activities. A common feature of several functional ingredients is their antioxidant function. For example, reactive oxygen species (ROS) can be oxidized and stabilized by flavonoid components, and the flavonoid radical can undergo electron rearrangement stabilizing the flavonoid radical. Compounds that possess an orthodihydroxy or quinone structure can interact with cellular proteins in the Keap1/Nrf2/ARE pathway to activate the gene transcription of antioxidant enzymes. Carotenoids and flavonoids can also exert their action by modulating the signal transduction and gene expression within the cell. Recent results suggest that these activities are primarily responsible for the health benefits associated with the consumption of fruits and vegetables.

  9. Stability and structure of protein-lipoamino acid colloidal particles: toward nasal delivery of pharmaceutically active proteins.

    Science.gov (United States)

    Bijani, Christian; Arnarez, Clément; Brasselet, Sabrina; Degert, Corinne; Broussaud, Olivier; Elezgaray, Juan; Dufourc, Erick J

    2012-04-03

    To circumvent the painful intravenous injection of proteins in the treatment of children with growth deficiency, anemia, and calcium insufficiency, we investigated the stability and structure of protein-lipoamino acid complexes that could be nasally sprayed. Preparations that ensure a colloidal and structural stability of recombinant human growth hormone (rhGH), recombinant human erythropoietin (rhEPO), and salmon calcitonin (sCT) mixed with lauroyl proline (LP) were established. Protein structure was controlled by circular dichroism, and very small sizes of ca. 5 nm were determined by dynamic light scattering. The colloidal preparations could be sprayed with a droplet size of 20-30 μm. The molecular structure of aggregates was investigated by all-atom molecular dynamics. Whereas a lauroyl proline capping of globular proteins rhGH and rhEPO with preservation of their active structure was observed, a mixed micelle of sCT and lipoamino acids was formed. In the latter, aggregated LP constitutes the inner core and the surface is covered with calcitonins that acquire a marked α-helix character. Hydrophobic/philic interaction balance between proteins and LP drives the particles' stability. Passage through nasal cells grown at confluence was markedly increased by the colloidal preparations and could reach a 20 times increase in the case of EPO. Biological implications of such colloidal preparations are discussed in terms of furtiveness.

  10. Extraction of active ingredients in Honey suckle and their function in cosmetics%金银花活性成分提取及其抗氧化和抑菌功效研究

    Institute of Scientific and Technical Information of China (English)

    宋小锋; 原增艳; 许平辉

    2012-01-01

    利用超声波预处理结合乙醇回流提取法从金银花中提取活性成分,通过响应面分析法设计实验,得到了较佳的提取工艺:超声波预处理30.9 min,乙醇的体积分数为73.7%,提取温度为68.5℃,每次提取2.1h,提取2次,在此条件下绿原酸提取率达到88.39%.通过与阳性物质Vc比较检验了提取物的功效,证明金银花提取物具有较好的体外抗氧化能力;通过对大肠杆菌、金黄色葡萄球菌、黑曲霉的抑制分析,证明金银花提取物具有良好的抑菌防腐能力.%Active ingredients in Honey suckle were extracted by ultrasonic -aided ethanol method. The optimal processing conditions for the extraction were identified by using the software "Design Expert 7. 1. 3 Tril". Pretreatment time is 30. 9 min under aid of ultrasonic wave. Ethanol with volume fraction of 73. 7% was used as the solvent. Temperature was 68. 5 ℃. Extraction of two times was operated with each of 2. 1 h. Under the afore - said conditions, yield of chlorogenic acid achieves 88.39%. Comparing with positive material vitamin C,the efficacy of the extract was investigated and experimental results showed that the extract has a good in - vitro antioxidation capability. Bacteriostasis tests were carried out against colibacillus, Staphylococcus aureus and Aspergillus niger and the results showed that the Honey suckle extract has strong bacteriostatic and antiseptic capabilities.

  11. Analysis on safety assessment and active ingredient of functional textiles%功能性纺织品的安全性评