Interchangeability of medications and biopharmaceutical implication of taking drugs with fluids other than water: ibuprofen case study

Abstract The aim of this study was to compare the dissolution properties of ibuprofen solid oral dosage forms commercially available in Bosnia and Herzegovina and to estimate the influence of dissolution medium composition on the drug release. Eight products (A-H) were subjected to in vitro dissolution test using experimental conditions described in USP42-NF37. Dissolution properties of one selected product were examined in the presence of alcohol (22.2% v/v) and fruit juice (22.2% v/v). Products marked B-H complied with the pharmacopeial criteria. Dissolution profile of product B was similar with dissolution profiles of products D, E, F and G and similarity was also found between products A-D, C-G, D-G and E-F. Drug release from most of the examined preparations fitted best to the Weibull kinetic model. In the presence of alcohol in the medium, higher amount of ibuprofen was dissolved. Contrary, ibuprofen dissolved in the presence of fruit juice was significantly lower. Differences in the dissolution profiles of investigated preparations suggest that their interchangeability should be additionally considered and demonstrated with in vivo bioequivalence studies. Presence of different substances in the medium can affect dissolution properties of ibuprofen, emphasizing the importance of the patient's compliance.

Dissolution profile of different brands of low solubility drugs available in the Nigerian and Brazilian pharmaceutical markets / Dissolution profile of different brands of low solubility drugs available in the Nigerian and Brazilian pharmaceutical markets

The purpose of this work was to elaborate a diagnosis of the dissolution test in Africa in comparison with Brazil, evaluating the dissolution profile of low solubility drugs such as albendazole, ibuprofen, furosemide, glibenclamide, hydrochlorothiazide and carvedilol to ascertain their quality. The dissolution profiles were evaluated by utilizing the United States Pharmacopeia (USP). The glibenclamide medicine was evaluated according to the Food and Drug Administration (FDA), while a dissolution method was developed for the carvedilol medicine. A filter selection test for all the drugs showed that cannula is suitable for all, except for carvedilol, which is centrifuged. The various brands of Nigerian and Brazilian medicines tested showed some statistical differences. The suitable conditions that allowed the dissolution of carvedilol to be determined were the USP type II apparatus at 75 rpm containing 900 mL of acetate buffer, pH 4.5. The results of the dissolution test showed that out of the 17 different brands of Brazilian medicines and 17 different products from Nigeria, 94.12% and 58.82% passed respectively

O objetivo deste trabalho foi elaborar um diagnóstico do teste de dissolução na África em comparação ao Brasil, avaliando o perfil de dissolução de medicamentos de baixa solubilidade como albendazol, ibuprofeno, furosemida, glibenclamida, hidroclorotiazida e carvedilol para verificar sua qualidade.Os perfis de dissolução foram avaliados utilizando a Farmacopeia dos Estados Unidos (USP). O medicamento glibenclamida foi avaliado de acordo com a Food and Drug Administration (FDA), enquanto um método de dissolução foi desenvolvido para o medicamento carvedilol.Um teste de seleção de filtro para todos os medicamentos mostrou que a cânula é adequada para todos, exceto para o carvedilol, que é centrifugado. As diversas marcas de medicamentos Nigerianos e Brasileiros testadas apresentaram algumas diferenças estatísticas. As condições adequadas que permitiram a determinação da dissolução do carvedilol foram o aparelho USP tipo II a 75 rpm contendo 900 mL de tampão acetato, pH 4,5. Os resultados do teste de dissolução mostraram que das 17 diferentes marcas de medicamentos brasileiros e 17 diferentes produtos da Nigéria, 94,12% e 58,82% foram aprovados, respectivamente

Portable and automated analyzer for rapid and high precision in vitro dissolution of drugs / 药物分析学报

We developed a novel portable and automated dissolution test analyzer for rapid and high precision in vitro dissolution testing of drugs.The analyzer consists of a flow-through-cell drug dissolution system,an automated sequential sampling system,a high-speed capillary electrophoresis (HSCE) system,and a data acquisition system.Combining the high-temporal resolution flow-gating sampling approach with HSCE,which has outstanding advantages of efficient separation and resolution,the analyzer can achieve rapid analysis and exhibits the ability in miniaturization for on-site assessment of different active pharmaceutical ingredients.To integrate the flow-through-cell dissolution system with HSCE,a specially designed flow-gating-injection (FGI) interface was employed.The performance of the analyzer was investigated by analyzing the dissolution of immediate-release drugs including single dose (amoxicillin dispersible tablets) and fixed dose combination (amoxicillin and clavulanate potassium) drug tablets with the high-temporal resolutions of 12 s and 20 s,respectively.The dissolution profiles of different active pharmaceutical ingredients could be simultaneously and automatically monitored with high repeatability and accuracy.The analyzer was successfully utilized for the pharmaceutical quality control and bio-relevant dissolution testing,as well as in vivo-in vitro correlation analysis.Our portable analyzer is miniaturized,convenient and of low-cost,and will provide a valuable tool for dissolution testing in pharmaceutical research and development.

Preparation and characterization of SiO2 solid dispersions of Curcumae longae Rhizoma extract / 中成药

AIM To prepare and characterize SiO2 solid dispersions of Curcumae longae Rhizoma extract.METHODS For the solid dispersions prepared by solvent evaporation method,its ratio of extract to carrier (SiO2) was screened by in vitro dissolution test,and the characterization was achieved by determination of particle size,specific surface area,porosity,micromorphology observation,infrared spectroscopy and X-ray.RESULTS When the ratio of extract to carfer was 1:8,three main components (bisdemethoxycurcumin,demethoxycurcumin and curcumin) in the extract reached the highest accumulative dissolution rates.Compared with physical mixture,the solid dispersions demonstrated lower particle size,specific surface area and porosity.Extract was dispensed in the carrier in an amorphous state.CONCLUSION SiO2 solid dispersions can obviously improve the dissolution rates of the main components in Curcumae longae Rhizoma extract.

A new method based on flow-through cell apparatus to evaluate dissolution consistency of nimodipine tablets / 中国药科大学学报

A new method of dissolution test was established to better simulate the in vivo dissolution behavior of drugs from preparations and to distinguish the quality difference between drug preparations. With flow-through cell being chosen to be the dissolution apparatus and nimodipine tablet to be the model drugs,this study developed,on the basis of IVIVC theory,a new dissolution method which was subsequently used to evaluate the dissolution con-sistency of domestically produced nimodipine tablet as test preparation and its reference preparation. Meanwhile, conventional four-dissolution-curves method based on paddle apparatus was selected for comparison to evaluate the efficiency of the new dissolution method. The results indicated that the new dissolution method not only had a good correlation with the in vivo process of drugs,but also could reveal the internal quality differences between pharmaceutical preparations effectively. This research will provide further theoretical support for the application of flow-through cell apparatus in IVIVC study.

Determination and validation of secnidazole in tablets by UV spectrophotometric / Determinação e validação do secnidazol em comprimidos por espectrofotometria na região do ultravioleta

Secnidazole, a 5-nitroimidazole, is a drug used in the treatment against protozoa, and several bacterial infections. This study purpose was to develop and validate a UV spectrophotometric method to determine secnidazole in pharmaceutical tablet dosage forms once there is no method reported in the pharmacopoeia yet. The quantification was performed using methanol as solvent at 325 nm (maximum wavelength) and three kinds of products marketed in Brazil (reference, generic and similar tablets) containing 1g of secnidazole. The method obeyed Beer's law in the concentration range of 4 - 20 µgmL-1 respectively. The method was validated according to the International Conference on Harmonization (ICH) and Brazil National Health Surveillance Agency (ANVISA) guidelines, showing accuracy, precision, selectivity, robustness and linearity. Tests such as weight range, friability, disintegration, hardness and dissolution were carried out to check tablets' quality and all the trials showed to be in accordance with the general test guidelines of the Brazilian Pharmacopoeia. The dissolution test was carried out and the developed method was applied. The method developed is suitable for the estimation of secnidazole in tablets without any interference from the excipients and can be used for routine in quality control. Still, it's a simple, fast and low cost method.

Secnidazol, um nitroimidazólico, é um fármaco utilizado no tratamento para protozoários, e várias infecções bacterianas. Este trabalho propôs o desenvolvimento e validação de um método espectrofotométrico na região do ultravioleta para a determinação de Secnidazol na forma farmacêutica de comprimidos, uma vez que não há nenhum método relatado nas farmacopeias. A quantificação foi realizada utilizando metanol como solvente a 325 nm (máximo de comprimento de onda) e usando três tipos de produtos comercializados no Brasil (de referência, genéricos e comprimidos similares) contendo 1g de Secnidazol. O método obedeceu a lei de Beer no intervalo de concentração de 4 - 20 µgmL-1, respectivamente. O método foi validado de acordo com a Conferência Internacional de Harmonização (ICH) e diretrizes da Agência Nacional de Vigilância Sanitária do Brasil (ANVISA), apresentando exatidão, precisão, seletividade, robustez e linearidade. Testes como variação de peso, friabilidade, desintegração, dureza e dissolução foram realizados para verificar a qualidade de comprimidos e mostrou-se de acordo com os testes gerais da Farmacopeia Brasileira. O teste de dissolução realizado e o método desenvolvido pode ser aplicado. O método desenvolvido é adequado para a estimativa de secnidazole em comprimidos sem qualquer interferência dos excipientes e pode ser usado para a rotina de controlo de qualidade. Ainda, é um método simples, rápido e de baixo custo.

Measurement uncertainty of dissolution test of acetaminophen immediate release tablets using Monte Carlo simulations

ABSTRACT Analytical results are widely used to assess batch-by-batch conformity, pharmaceutical equivalence, as well as in the development of drug products. Despite this, few papers describing the measurement uncertainty estimation associated with these results were found in the literature. Here, we described a simple procedure used for estimating measurement uncertainty associated with the dissolution test of acetaminophen tablets. A fractionate factorial design was used to define a mathematical model that explains the amount of acetaminophen dissolved (%) as a function of time of dissolution (from 20 to 40 minutes), volume of dissolution media (from 800 to 1000 mL), pH of dissolution media (from 2.0 to 6.8), and rotation speed (from 40 to 60 rpm). Using Monte Carlo simulations, we estimated measurement uncertainty for dissolution test of acetaminophen tablets (95.2 ± 1.0%), with a 95% confidence level. Rotation speed was the most important source of uncertainty, contributing about 96.2% of overall uncertainty. Finally, it is important to note that the uncertainty calculated in this paper reflects the expected uncertainty to the dissolution test, and does not consider variations in the content of acetaminophen.

In vitro Dissolution and Virtual Bioequivalence of Domestic Nifedipine Sustained Release Tablets / 中国药师

Objective: To evaluate the quality consistency of four domestic nifedipine sustained release tablets by dissolution test and virtual bioequivalence study by GastroPlus software.Methods: The dissolution curves of the four preparations were determined with the methods described in Japanese orange book and Chinese Pharmacopeia.The f2 factor of dissolution curves was calculated to compare the similarity.The in vitro dissolution data of the original preparation were combined with GastroPlus software to obtain the simulated in vivo absorption curves which were correlated with the actual concentration-time curves.The suitable dissolution medium was selected to evaluate the quality of domestic nifedipine sustained release tablets according to the better in vivo-in vitro correlation (IVIVC).The simulated in vivo absorption parameters obtained from the dissolution data combined with GastroPlus software were used to conduct the virtual bioequivalence study of domestic nifedipine sustained release tablets compared with the original products.Results: The f2 similar factors of the four domestic nifedipine sustained release tablets compared with the original preparation were all less than 50.Compared with that from the method in Japanese orange book, the correlation between the dissolution profiles in vitro and in vivo of original nifedipine sustained release tablets obtained from the method in Chinese Pharmacopoeia was better.The deviation between the simulated Cmax and AUC0-∞ values of the four test tablets and the measured values of the original preparation was within the range of ±20%.Conclusion: The dissolution curves of the four domestic nifedipine sustained release tablets are not similar to that of the original preparation, however, the four preparations are all bioequivalent to the original preparation according to the simulated absorption parameters based on the dissolution method in Chinese Pharmacopeia and GastroPlus software.

Effects of different grinding methods on in vitro dissolution of ursodeoxycholic acid capsules / 中国药学杂志

OBJECTIVE: To compare the in vitro dissolution of ursodeoxycholic acid capsules prepared by different grinding methods and screen the best grinding method. METHODS: Using the large cup method, HPLC was used to investigate the similarity of dissolution behaviors between the reference preparation Ursofalk® (the original drug) and the self-made ursodeoxycholic acid capsules in four dissolution media. The grinding method which obtained product with qualified similarity factor f2 was determined as the best technology. RESULTS: The ursodeoxycholic acid capsules made with raw material micronized by ball grinder for 3 min had similar dissolution curve to the original drug. CONCLUSION: Rational preparation process is established for ursodeoxycholic acid capsules.

Monolithic LC method applied to fesoterodine fumarate low dose extended-release tablets:Dissolution and release kinetics / 药物分析学报

A dissolution test for fesoterodine low dose extended-release tablets using liquid chromato-graphic (LC) method equipped with a C18 monolithic column was developed and validated. LC system was operated isocratically at controlled temperature (40 1C) using a mobile phase of acetonitrile:methanol:0.03 M ammonium acetate (pH 3.8) (30:15:55, v/v/v), run at a flow rate of 1.5 mL/min and detected at 208 nm. The best dissolution conditions for this formulation were achieved using a USP apparatus 2 (paddle) at 100 rpm and 900 mL of phosphate buffer at pH 6.8 as the dissolution medium. Validation parameters such as the specificity, linearity, accuracy, precision, and robustness were evaluated according to international guidelines, giving results within the acceptable range. The kinetic parameters of drug release were also investigated using model-dependent methods and the dissolution profiles were best described by the Higuchi model. The validated dissolution test can be applied for quality control of this formulation.

Test of dissolution and comparison of in vitro dissolution profiles of coated ranitidine tablets marketed in Bahia, Brazil

Ranitidine is an antisecretory drug with H2 antagonist action useful in treating gastric and duodenal disorders. The dissolution test is used to obtain and compare dissolution profiles and establish similarities of pharmaceutical forms. The aim of this study was to compare the dissolution profiles of 150-mg coated ranitidine tablets of a reference drug (product A) and a generic (product B) and a similar (product C) drug marketed in Bahia, Brazil using a simple, fast and inexpensive ultraviolet method. Dissolution was determined using a USP type 2 apparatus at 50 rpm with 900 mL of distilled water at 37.0 ± 0.5 oC for 1h. The dissolution test was performed in compliance with the American Pharmacopoeia (USP-32). Dissolution efficiency and difference (f1) and similarity (f2) factors were calculated and evaluated. The proposed quantification methodology for drug dissolution test was validated, presenting accuracy, linearity and precision within the acceptance criteria. Products A, B and C showed dissolution efficiency values of 59.29, 73.59 and 66.67%, respectively. Factors f1 and f2 were calculated and showed that the profiles of products A, B and C were dissimilar. However, all the products released ranitidine satisfactorily, with at least 80% of the drug dissolved within 30 min.

A ranitidina é um fármaco antissecretor, antagonista H2, usado no tratamento de desordens gástricas e duodenais. O teste de dissolução é utilizado para obter e comparar perfis de dissolução, estabelecendo semelhança de formas farmacêuticas. Este estudo tem por objetivo comparar perfis de dissolução de comprimidos revestidos contendo 150 mg de ranitidina, em medicamentos de referência (produto A), genérico (produto B) e similar (produto C) comercializados na Bahia-Brasil, usando um método ultravioleta simples, rápido e de baixo custo. As condições que permitiram a determinação da dissolução foram: aparelho USP tipo 2 a 50 rpm, contendo 900 mL de água destilada mantida a 37,0 ± 0,5 °C, durante 1 h. O teste de dissolução foi realizado em conformidade com a Farmacopeia Americana (USP-32). Cálculo da eficiência de dissolução e fatores de diferença (f1) e semelhança (f2) foram avaliados. A metodologia proposta para a quantificação do fármaco no ensaio de dissolução foi validada apresentando precisão, linearidade e exatidão dentro dos critérios de aceitação. Os produtos A, B e C mostraram eficiência de dissolução de 59,29, 73,59 e 66,67%, respectivamente. Calcularam-se os fatores f1 e f2 e mostrou-se que os perfis não foram semelhantes para os comprimidos de produtos A, B e C. No entanto, todos os produtos liberaram o fármaco satisfatoriamente, pois, pelo menos, 80% de ranitidina foram dissolvidos em 30 min.

Pharmacokinetics evaluation of curcumin-phospholipid complex / 第二军医大学学报

Objective: To evaluate the pharmacokinetics of curcumin phospholipid complex (CCPC) in rats following oral administration. Methods: Blood samples were collected from the retinal venous plexus of SD rats after oral administration of CCPC or curcumin (CC), and the blood concentration of curcumin was determined by high-performance liquid chromatography (HPLC). Results: The solubility and cumulative dissolution of CCPC (0.150 g/L and 68.04%, respectively) were higher than those of CC (0.057 g/L and 50.68%, respectively). The pharmacokinetic parameter of CCPC and CC were calculated as follows: Cmax (74.34±5.57) μg/L and (61.64±4.29) μg/L, Tmax (0.17±0) h and (0.25±0) h, AUC0-t (637.38±30.04) μg·h·L-1 and (172.41±31.66) μg·h·L-1, and AUC0-∞ (857.80±223.69) μg·h·L-1 and (191.08±43.27) μg·h·L-1, respectively. The intra-day, inter-day precision, and recovery rate met the criteria for content determination. Conclusion: Compared with curcumin, CCPC can be absorbed more rapidly and eliminated more slowly.

Development of dissolution test method for a telmisartan/amlodipine besylate combination using synchronous derivative spectrofluorimetry

The dissolution process is considered an important in vitro tool to evaluate product quality and drug release behavior. Single dissolution methods for the analysis of combined dosage forms are preferred to simplify quality control testing. The objective of the present work was to develop and validate a single dissolution test for a telmisartan (TEL) and amlodipine besylate (AML) combined tablet dosage form. The sink conditions, stability and specificity of both drugs in different dissolution media were tested to choose a discriminatory dissolution method, which uses an USP type-II apparatus with a paddle rotating at 75 rpm, with 900 mL of simulated gastric fluid (SGF without enzymes) as the dissolution medium. This dissolution methodology provided good dissolution profiles for both TEL and AML and was able to discriminate changes in the composition and manufacturing process. To quantify both drugs simultaneously, a synchronous first derivative spectrofluorimetric method was developed and validated. Drug release was analyzed by a fluorimetric method at 458 nm and 675 nm for AML and TEL, respectively. The dissolution method was validated as per ICH guidance.

O processo de dissolução é considerado como uma importante ferramenta in vitro para avaliar a qualidade do produto e o comportamento de liberação do fármaco. Prefere-se um ensaio único de dissolução para formas farmacêuticas contendo associação de fármacos pela simplificação dos testes de controle de qualidade. O objetivo do presente trabalho foi desenvolver e validar um teste de dissolução único para forma farmacêutica comprimidos contendo telmisartana (TEL) e besilato de anlodipino (AML) associados. Condições "sink", estabilidade e especificidade de ambos os fármacos nos diferentes meios de dissolução foram avaliadas para selecionar um método de dissolução discriminatório, que utiliza um aparato do tipo II da USP, com pás girando a 75 rpm e 900 mL de fluido gástrico simulado (SGF sem enzima) como o meio de dissolução. Estas condições proporcionaram bons perfis de dissolução para ambos, TEL e AML, sendo capaz de discriminar as mudanças na composição e processo de fabricação. Para quantificar os dois fármacos simultaneamente, um método de fluorescência derivada sincronizado foi desenvolvido e validado. A quantidade de fármaco liberado foi analisada pelo método fluorimétrico em 458 e 675 nm para a AML e TEL, respectivamente. O método de dissolução foi validado de acordo com a orientação da ICH.

Ensayo de disolución para las tabletas de Tilo ® elaboradas con extracto seco de Justicia pectoralis Jacq / Dissolution Assay for Tilo ® tablets prepared with dry extract of Justicia pectoralis Jacq

Introducción: el ensayo de disolución es una técnica analítica de empleo común en un laboratorio farmacéutico. Un proceso tecnológico para la elaboración de tabletas fue desarrollado. El ingrediente farmacéutico activo usado fue Tilo ® extracto seco. Objetivo: el objetivo de este trabajo fue desarrollar y validar un ensayo de disolución para evaluar la estabilidad y la calidad de dicho producto. Método: se utilizaron muestras de un lote experimental, un lote placebo y lotes pilotos de tabletas de Tilo ® de 100 mg. Se evaluaron como medios de disolución agua destilada y solución de ácido clorhídrico 0,1 mol/L, realizándose perfiles de disolución a 50, 75 y 100 rpm, empleándose los dos tipos de aparatos establecidos en la literatura para este ensayo (cesta y paleta). El contenido de cumarina fue analizado por HPLC. El ensayo fue validado según la USP. Resultados: los resultados mostraron que el agua destilada fue un medio de disolución adecuado, alcanzándose porcientos de disolución de la droga por encima del 85 por ciento a los 30 minutos, no existiendo diferencias significativas entre los tipos de aparatos recomendados por la USP. Mientras que, los perfiles de disolución a diferentes tiempos y velocidades de agitación mostraron una liberación gradual del principio activo en el tiempo, donde a medida que se incrementa la velocidad de agitación, se incrementa el porcentaje de disolución de la droga en el medio. La validación del ensayo demostró que el mismo era específico y preciso. Conclusiones: se estableció como ensayo de disolución las siguientes condiciones de trabajo: Aparato: paleta, 100 rpm; medio: agua destilada, 500 mL; tiempo: 60 minutos y Temperatura: 37 ± 0,5 ºC

Introduction: dissolution testing is one of the most common analytical techniques performed in a pharmaceutical analytical laboratory. A technological process for the production of tablets was developed. The active pharmaceutical ingredient used was Tilo ® dry extract. Objective: to develop and to validate the dissolution assay aimed at evaluating the stability study and the quality of this product. Methods: some samples from the experimental batch, the placebo batch and the pilot batches were used in this study. Distilled water and 0,1 mol/L chlorhidric acid were evaluated as dissolution media. The dissolution profiles at 50, 75 and 100 rpm and two types of dissolution devices (basket and paddle) recommended for the USP were evaluated. Coumarin content was analyzed by HPLC method. The dissolution assay was validated according to the United States Pharmacopeia. Results: the results showed that the distilled water was an appropriate dissolution medium, where percentages of released drug higher to 85 percent in 30 minutes were obtained; there were no significant differences among the types of dissolution devices recommended by the USP. The dissolution profiles at different shaking times and speeds showed gradual release of the active principle. As the shaking speed increases, the percentage of the drug dissolution increases in the medium. The assay was considered specific and precise. Conclusions: a type II (paddle) dissolution device, 500 ml of distilled water at 37 ± 0,5 ºC and 100 rpm, were established as parameters of the dissolution assay

COMPARATIVE ANALYSIS OF SOME CAPSULES REGISTERED IN MONGOLIA / Монголын эм зүй, эм судлал

Introduction: Mongolian national drug manufacturers produce only 20% of required medicines and most raw materials used for the manufacturing are imported from China [1]. 2574 medicines and active pharmaceutical ingredients were registered in 2011 and 488 of them were antibiotics [2]. There were 36 medicine manufacturers and only two of them manufactured antibiotic capsules in 2010 [3]. In last year number of manufacturing capsule has been increasing.Aim: The main aim of this investigation was to define items of imported and manufactured capsules and do comparative analysis of some capsules and determine types of the capsule drugs registered in Mongolia.Material and methods: Registered medicine list of Mongolia and questionnaire with 22 questions, and capsules of 2 domestic and 3 foreign manufacturers were used for this investigation. Pharmacists working in seven domestic manufacturers were involved in the questionnaire study. Capsules were analyzed at the Drug Control Laboratory of Monos Pharm Manufacturer.Results, conclusion: 10.84% of registered medicines are capsules, of which 16.33% from India, 7.82% from China, 5.78% from Indonesia, 8.5% from Slovenia, and other countries. 3.4% of registered capsules are manufactured in Mongolia.All medicine manufacturers import hard gelatin capsules from China and use for the manufacturing. 71.4% of domestic manufacturers use technological parameters, 57.1% stability and dissolution, 28.5% chemical properties and interaction with active pharmaceutical ingredients and excepients as the main criteria for the capsule selection used for the manufacturing. 40.0% of capsules used for the manufacturing are 0 size capsule.72.2% of manufactured capsules are antibiotics. Quality parameters of imported and manufactured Quality of manufactured and imported Ampicilline capsules were determined in the frame of this investigation. All Ampicilline capsules were met the requirements of MNS 5097:2007.Conclusion: Items of imported and manufactured capsules, selection criteria of capsules used for the manufacturing were determined. Comparative quality analysis of Ampicilline capsule was done and some quality parameters of imported and manufactured Ampicilline capsule were in accordance of MNS 5097:2007.Key words: Ampicillin trihydrate 500 mg, dissolution testReference:1. д. Цэндээхүү, “Эмийн чанарûн хяналтûн зарим асуудалд”, “зшЭ-ийн хүртээмж, хэрэглээ, чанар, аюулгүй байдлûн талаар туршлага солилцъё” олон улсûн бага хурлûн илтгэлийн хураангуй; 2006.2. Эрүүл мэндийн үзүүлэлт 2011. згха-Эмг. уБ. 20113. Эрүүл мэндийн үзүүлэлт 2010. згха-Эмг. уБ. 20104. монгол улсûн эмийн бүртгэлийн жагсаалт 2013

Preparation technology of Dracocephalum moldevica total flavonoids pellets and its release mechanism / 中草药

Objective: To optimize the preparation technology of the Dracocephalum moldevica total flavonoids pellets (DMTFP), and to study its release mechanism. Methods: The Box-Behnken central composite design was used, and the extrusion speed, spheronisation speed, and spheronisation time were taken as the independent variables; The yield, friability, sphericity, and general normalized value were taken as dependent variables. The response surface methodology (RSM) was used to estimate the relationship between the dependent and independent variables, and to validate the optimal formulation. Then the dissolution behaviors of DMTFP were investigated by in vitro dissolution test. The internal structure of DMTFP was observed by scanning electron microscopy (SEM). Results: The optimal conditions were as follows: the extrusion speed was 36.96 Hz, the spheronisation speed was 37.18 Hz, and the spheronisation time was 5 min. Under these conditions, the measured value was consistent with the predicated value with RSD < 4 %. The dissolution rate of DMTFP was good, and the internal structure of DMTFP was matrix type by SEM. Conclusion: The preparation technology of DMTFP is optimized, which is simple and feasible. The bulge of low-substituted hydroxypropyl cellulose is the reason of disintegration of DMTFP.

Formulation and evaluation of fast dissolving tablet of albendazole.

Albendazole is broad spectrum anthelmintic use against many helminths. It is used for treatment of Threadworm, Hookworm, and Tapeworm. It has low bioavailability due to its first pass metabolism. In the present work, fast dissolving tablet of Albendazole was design with a view to and provide a quick onset of action. The main objective of the study was to formulate fast dissolving tablets of Albendazole to achieve a better dissolution rate and further improving the bioavailability of the drug. Fast dissolving tablets prepared by direct compression and using super disintegrants in different concentration and evaluated for the pre-compression parameters. The prepared tablets were evaluated for post compressional evaluation. Among all, the formulation F3 containing 5%w/w superdisintegrant Crospovidone and 20%w/w Microcrystalline Cellulose was considered to be best formulation, which release up to 99.097% in 40 min.

Comparative Evaluation of Physicochemical Properties of Some Commercially Available Brands of Metformin Hcl Tablets in Lagos, Nigeria.

There are several generics of metformin hydrochloride tablets available within the drug delivery system globally. Availability of numerous brands of Metformin tablets in Nigerian drug market today places health practitioners in a dilemma of generic substitution. The objective of the study was to determine the biopharmaceutical and chemical equivalence of eight brands of Metformin tablets marketed in Nigeria using in vitro tests. The physicochemical equivalence of eight brands of Metformin hydrochloride tablets were assessed through the evaluation of both official and non-official standards such as uniformity of weight, friability, hardness, disintegration, Assay and dissolution rate. All the brands complied with the official specifications for uniformity of weight, disintegration and dissolution tests. Brand B and C had the highest and lowest crushing strength respectively. However, for the friability test, one of the eight brands failed to meet the British pharmacopoeia specification for friability. Seven brands had values within the range specified for assay in the BP while Brand G failed the test. Only brand F, G and H met the BCS biowaiver criteria for very rapidly or rapidly dissolving tablets. Of all the eight brands evaluated in this study, only four brands could be regarded as being biopharmaceutically and chemically equivalent and therefore can be interchanged in the clinical practice.

ISSUES ON PROVIDING AND STRUCTURE IMPROVEMENT OF PRESCRIPTION DRUGS / Монголын эм зүй, эм судлал

Introduction: There were 36 medicine manufacturers and only two of them manufactured antibiotic capsules in 2010. In last year number of manufacturing capsule has been increasing. 2574 medicines and active pharmaceutical ingredients were registered in 2011 and 488 of them were antibiotics. Aim: The main aim of this investigation was to define items of imported and manufactured capsules and do comparative analysis of some capsules. Material and methods: Registered medicine list of Mongolia and questionnaire with 22 questions, and capsules of 2 domestic and 3 foreign manufacturers were used for this investigation. Results, conclusion: 10.84% of registered medicines is capsules, of which and 16.33% from India, 7.82% from China, 5.78% from Indonesia, 8.5% from Slovenia, and other countries. 3.4% of registered capsules are manufactured in Mongolia. All medicine manufacturers import hard gelatin capsules from China and use for the manufacturing. 71.4% of domestic manufacturers use technological parameters, 57.1% stability and dissolution, 28.5% chemical properties and interaction with active pharmaceutical ingredients and excepients as the main criteria for the capsule selection used for the manufacturing. 40.0% of capsules used for the manufacturing is 0 size capsule. 72.2% of manufactured capsules are antibiotics. Quality parameters of imported and manufactured Ampicilline capsule were determined in the frame of this investigation. Conclusion: Items of imported and manufactured capsules, selection criteria of capsules used for the manufacturing were determined. Comparative quality analysis of Ampicilline capsule was done and some quality parameters of imported and manufactured Ampicilline capsule were in accordance of MNS 5097:2007. Key words: Ampicillin trihydrate 500 mg, dissolution test

Formulation and evaluation of fast dissolving tablet of albendazole.

Albendazole is broad spectrum anthelmintic use against many helminths. It is used for treatment of Threadworm, Hookworm, and Tapeworm. It has low bioavailability due to its first pass metabolism. In the present work, fast dissolving tablet of Albendazole was design with a view to and provide a quick onset of action. The main objective of the study was to formulate fast dissolving tablets of Albendazole to achieve a better dissolution rate and further improving the bioavailability of the drug. Fast dissolving tablets prepared by direct compression and using super disintegrants in different concentration and evaluated for the pre-compression parameters. The prepared tablets were evaluated for post compressional evaluation. Among all, the formulation F3 containing 5%w/w superdisintegrant Crospovidone and 20%w/w Microcrystalline Cellulose was considered to be best formulation, which release up to 99.097% in 40 min.