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Comparative evaluation of the use of dry binders in a physical mixture or as a coprocessed dry binder in matrix tablets with extended drug release

Compaction Technology (Eds. G. Alderborn and Ch. Nyström), Marcel Dekker Inc., New York 1996, pp. 77–96. 18. A. Stamm and C. Mathis, Verpressbarkeit von Festen Hilfsstoffen für Direkttablettierung, Acta Pharm. Technol . 22 (1976) 7–16. 19. J. T. Fell and J. M. Newton, Determination of tablet strength by diametral-compression test, J. Pharm. Sci . 59 (1970) 688–691; https://doi.org/10.1002/jps.2600590523 20. C. E. Bos, G. K. Bolhuis, H. van Doorne and C. F. Lerk, Native starch in tablet formulations: properties on compaction, Pharm. Weekbl. Sci

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Gellan gum and polyvinylpyrrolidone (PVP) as binding agents in extrusion/spheronization pellet formulations

Abstract

The aim of this work was to evaluate gellan gum as binder in pellet formulations, with theophylline as the model drug, in comparison with polyvinylpyrrolidone (PVP). A full 32 factorial design was realized, with binder and diluent factors at three levels each. Pellets were produced by the extrusion/spheronization technique, and dried in a fluid-ized bed. Physical tests and dissolution tests were conducted. The results showed that the binder factor was not significant for pellet size and granulometry distribution. Rather, trends of a different response of gellan gum were identified, in comparison with PVP, in aspect ratio and dissolution tests: more round pellets were obtained in formulations with gellan gum, and more variable dissolution resulted when this polysaccharide was present. Therefore, if the usage of this compound in immediate release pellet formulations is verified, this justifies the interest in the development of sustained release systems using gellan gum.

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Biphasic dissolution method for quality control and assurance of drugs containing active substances in the form of weak acid salts

solubility testing, Eur. Pharmaceut. Rev. October 2013; http://www.americanpharmaceu-ticalreview.com/22313/news/featured-news-instrument-automated-biorelevant-biphasic-dissolution-solubility-testing/ ; last access date September 24, 2015. 5. A. Franc and J. Muselik, Method for Preparing Solid Drug from Warfarin Sodium Salt in Form of Isopropanol Clathrate, Involves Determining Total Weight of Solid Drug and Distribution Ratio of Warfarin Sodium Salt, Pat. CZ304136-B6, October 2013. 6. J. Muselik, A. Franc, P. Dolezel, R. Gonec, A. Krondlova and I. Lukasova

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Potential of the Essential Oil from Pimenta Pseudocaryophyllus as an Antimicrobial Agent

Abstract

This study evaluated the effectiveness of the essential oil of Pimenta pseudocaryophyllus in inhibiting the growth of the main bacteria responsible for bad perspiration odor (Staphylococcus epidermidis, Proteus hauseri, Micrococcus yunnanensis and Corynebacterium xerosis). The chemical profile of the essential oil was evaluated by high-resolution gas chromatography (HR-GC) and four constituents were identified, eugenol being the major component (88.6 %). The antimicrobial activity was evaluated by means of the turbidimetric method, using the microdilution assay. The minimum inhibitory concentration (MIC) values of the essential oil ranged from 500 to 1,000 μg mL-1. Scanning electron microscope (SEM) observations confirmed the physical damage and morphological alteration of the test bacteria treated with the essential oil, reference drugs and eugenol. The findings of the study demonstrated that this essential oil can be used in the formulation of personal care products.

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„Z”-scores of anthropometric and motor parameters of girls in aerobic gymnastics

References [1] Drinkwater DT, Ross WD. Antropometric fraction of body mass. In: Kinantropometry II. International Seminar of Sports Science. Baltimore: University ParkPress; 1980. [2] Feč K. Sport Training of Young Gymnasts. Prešov: FHPV - PU; 2000. [3] Hatiar B. et al. Rhythmic, Modern and Sport Gymnastics. University Scripts. 3rd Ed. Bratislava: Comenius University in Bratislava; 1998. [4] Jacík V. Comprehensive motor test. In: Ontogenesis of Human Motorics. Set of Papers from 5th Seminar of [5] Athropomotorics. Praha: Olympia; 1985. [6

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Synthesis, in vitro anticancer and antioxidant activity of thiadiazole substituted thiazolidin-4-ones

Abstract

A series of novel 5-alkyl/aryl thiadiazole substituted thiazolidin-4-ones were synthesized by a two-step process. In the first step, 5-alkyl/aryl substituted 2-aminothiadiazoles were synthesized, which on reaction with substituted aromatic aldehydes and thioglycolic acid in the presence of dicyclohexylcarbodiimide afforded thiazolidin- 4-ones. All the compounds were synthesized in fairly good yields and their structures were confirmed by spectral and physical data. The title compounds were screened for in vitro anti-proliferative activity on human breast adenocarcinoma cells (MCF-7) by MTT assay. Most of the derivatives showed an IC50 less than 150 μmol L-1. Among the compounds tested, 2-(2-nitrophenyl)- 3-(5-methyl-1,3,4-thiadiazol-2-yl)-thiazolidin-4-one (3f), 2-(3-fluorophenyl)-3-(5-methyl-1,3,4-thiadiazol-2- -yl)-thiazolidin-4-one (3b), and 2-(4-chlorophenyl)-3- -(5-methyl-1,3,4-thiadiazol-2-yl)-thiazolidin-4-one (3c) were found to be the most active derivatives with IC50 values of 46.34, 66.84, and 60.71 μmol L-1, respectively. Antioxidant studies of all the synthesized compounds were carried out by diphenylpicrylhydrazyl (DPPH) assay. Among the compounds tested, 2-phenyl-3-(5-styryl- -1,3,4-thiadiazol-2-yl)-thiazolidin-4-one (3s) elicited superior antioxidant activity with IC50 of 161.93 μmol L-1.

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Effects of drug solubility on the release kinetics of water soluble and insoluble drugs from HPMC based matrix formulations

Effects of drug solubility on the release kinetics of water soluble and insoluble drugs from HPMC based matrix formulations

The purpose of the present research work was to observe the effects of drug solubility on their release kinetics of water soluble verpamil hydrochloride and insoluble aceclofenac from hydrophilic polymer based matrix formulations. Matrix formulations were prepared by the direct compression method. The formulations were evaluated for various physical parameters. Along with the dynamics of water uptake and erosion, SEM and in vitro drug release of the tablets were studied. Applying an exponential equation, it was found that the kinetics of soluble drug release followed anomalous non-Fickian diffusion transport whereas insoluble drug showed zero-order release. SEM study showed pore formation on the tablet surface that differed depending on drug solubility. t-Test pointed to a significant difference in amount of both drugs released due to the difference in solubility. Solubility of the drug effects kinetics and the mechanism of drug release.

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Investigation of in situ gelling alginate formulations as a sustained release vehicle for co-precipitates of dextromethrophan and Eudragit S 100

Abstract

Alginate vehicles are capable of forming a gel matrix in situ when they come into contact with gastric medium in the presence of calcium ions. However, the gel structure is pH dependent and can break after gastric emptying, leading to dose dumping. The aim of this work was to develop modified in situ gelling alginate formulations capable of sustaining dextromethorphan release throughout the gastrointestinal tract. Alginate solution (2 %, m/m) was used as a vehicle for the tested formulations. Solid matrix of the drug and Eudragit S 100 was prepared by dissolving the drug and polymer in acetone. The organic solvent was then evaporated and the deposited solid matrix was micronized, sieved and dispersed in alginate solution to obtain candidate formulations. The release behavior of dextromethorphan was monitored and evaluated in a medium simulating the gastric and intestinal pH. Drug-polymer compatibility and possible solid-state interactions suggested physical interaction through hydrogen bonding between the drug and the polymer. A significant decrease in the rate and extent of dextromethorphan release was observed with increasing Eudragit S 100 concentration in the prepared particles. Most formulations showed sustained release profiles similar to that of a commercial sustained-release liquid based on ion exchange resin. The release pattern indicated strict control of drug release both under gastric and intestinal conditions, suggesting the potential advantage of using a solid dispersion of drug-Eudragit S 100 to overcome the problem of dose dumping after the rupture of the pH dependent alginate gels

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Topical dosage form of valdecoxib: Preparation and pharmacological evaluation

. Ethnopharmacol. 65 (1999) 237-241; DOI: 10.1016/S0378-8741(98)00176-7. W. J. Herbert, The mode of action of mineral oil emulsion adjuvants on antibody production in mice, J. Immunol. 14 (1968) 301-318. M. Fronza, M. Wrasse, L. Brun, M. S. Sangoi and S. Dalmora, Evaluation of the changes on hemostatic parameters induced by valdecoxib in male Wistar rats, Rev. Bras. Hematol. Hemoter. 28 (2006) 28-32. A. G. Manzano, J. G. Llavan, C. Lemini and C. R. Poo, Standardization of rat blood clotting tests

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Financial aspects of community pharmacies in Slovakia (2009-2014) Finančné aspekty verejných lekární na Slovensku v rokoch 2009-2014

Abstract

Community pharmacies play an important role in the process of ensuring public health. Pharmacists provide pharmaceutical care that includes acquiring, storing, preparing, reviewing and dispensing medicines, medical devices and dietary food to the inhabitants; providing them with information and advice; acquiring, storing and dispensing additional assortment; carrying out physical and biochemical testing for primary prevention and monitoring of drug efficacy and safety. At present, there are constant changes which have direct or potential and often negative impact on community pharmacies. For providing affordable and good quality pharmaceutical care, it is important to continuously monitor and analyse the developments in the financial data in community pharmacy business management. The data file from 2009-2014 on financial performance of selected community pharmacies were obtained from the Register of Financial Statements at Ministry of Finance Slovak Republic. A group of 194 community pharmacies were selected that represented more than 10 percent of all pharmacies. The selection criteria respected the territorial division of the Slovak Republic on districts, the size of municipalities (cities and villages) and location (at or near health centres, shopping centres, housing estates, etc.). The evaluation parameters were gross profit, net profit, revenue from sales of goods and services, operating expenses, total assets, inventory, short-term receivables, total receivables, financial assets, owner’s equity, total liabilities, current liabilities and their characteristics (25th, 50th, 75th percentile, minimum, maximum, mean). The financial parameters obtained and their characteristics presented the basic information on the management of community pharmacies. The data also provided information for further assessment on factors that might have an impact on their value and direction of evolution.

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