Improvement of in Vitro Dissolution Rate of Daidzein by Solid Dispersion Technology / 医药导报

Objective Daidzein solid dispersions were prepared by solid dispersion technology to improve in vitro dissolution rate. Methods Daidzein solid dispersions were prepared by solvent method using polyvinyl pyrrolidone K30 ( PVP K30) as carrier.The in vitro dissolution characteristics of solid dispersions were evaluated,and the properties were detected by IR and XRD. Results The dissolution rates of different mass ratio of daidzein-PVP solid dispersion were significantly improved compared with that of daidzein API.The cumulative dissolution of solid dispersion with mass ratio of 1∶6 within 30 minutes was up to 87.8%,equivalent to six times of API. The in vitro drug release kinetics were fitted mathematically to Korsemeyer-Peppas model. Conclusion Solid dispersion with PVP K30 as carrier could significantly improve dissolution rate of daidzein.

Solubility enhancement of ibuprofen in the presence of hydrophilic polymer and surfactant.

Solid dispersions of ibuprofen (IBU) were prepared by solvent evaporation method using polyvinyl pyrrolidone (PVP) and/or sodium lauryl sulphate (SLS). Physicochemical properties of the various solid dispersion systems were determined by differential scanning calorimetry (DSC) and X-ray diffraction (XRD) analysis. The results from dissolution studies indicated that ternary solid dispersion systems were more efficacious than the corresponding binary ones. The increase in the dissolution rate of ibuprofen from its solid dispersions with the PVP and/or SLS used in this study could be attributed to several factors such as improved wettability, local solubilisation, and drug particle size reduction. The most effective solid dispersion was the 20:180:10 w/w IBUPVP- SLS ternary system, which allowed dissolution of 85 % drug after only 9.15 minutes (in comparison with 94.61 minutes for drug alone and 17.92 minutes for the binary system).

Evaluation of physicochemical properties and in-vitro release profile of glipizide-matrix patch

OBJECTIVES: The aim of the present investigation was to form matrix patches with ethyl cellulose (EC) as the base polymer, polyvinyl pyrrolidone (PVP) as the copolymer, plasticizer with dibutyl phthalate (DBP) or acetyl tributyl citrate (ATBC) and the drug glipizide (gz) by the solvent casting method. Physicochemical properties of the patches and in vitro drug release were determined in a modified Keshary-chien diffusion cell to optimize the patch formulations with the help of experimental data and figures for further studies. TECHNIQUES: EC and PVP of different proportions with different weight percentages of either DBP or ATBC and a fixed amount of glipizide were taken for matrix patch formations. The dried patches were used for measuring their drug contents as well as their thicknesses, tensile strengths, moisture contents and water absorption amounts in percentage. In vitro release amounts at different intervals were measured by UV-spectrophotometer. RESULTS: Drug contents varied from 96 - 99 percent. Thickness and tensile strength varied due to weight variation of the ingredients in the matrix patches. Moisture content and water absorption in wt percent were greater for the patches containing higher amount of PVP due to its hydrophilic nature. Variations in drug release were observed among various formulations. It was found that all of the releases followed diffusion controlled zero order kinetics. Two DBP patches yielded better and more adequate release. CONCLUSIONS: The two formulations with DBP were the preferred choice for making matrix patches for further studies.

O objetivo da presente pesquisa foi formar matrizes para bandagens de liberação transdérmica com etilcelulose (EC) como polímero base, polivinilpirrolidona (PVP), como copolímero, plastificante com ftalato de dibutila (DBP) ou citrato de tributilacetila (ATBC) e o fármaco glipizida (gz) pelo método de evaporação do solvente (moldagem com solvente). As propriedades físico-químicas das bandagens e a liberação do fármaco in vitro na célula de difusão de Keshary-chien modificada foram determinadas para aperfeiçoar as formulações das bandagens com o auxílio de dados experimentais e figuras para estudos posteriores. EC e PVP em diferentes proporções com porcentagens diferentes de massa tanto de DBP quanto de ATBC e quantidade fixa de glipizida foram utilizadas como matrizes para a formação de bandagens de liberação transdérmica. As bandagens secas foram empregadas para medir seus conteúdos em fármaco e, também, a sua espessura, resistência à tensão, conteúdos de umidade e porcentagem de absorção de água. As quantidades liberadas in vitro em diferentes intervalos de tempo foram medidas por espectrofotômetro de UV. Os conteúdos de fármaco variaram de 96 a 99 por cento. A espessura e a resistência à ruptura variaram devido à variação de massa dos componentes da matriz das bandagens. O conteúdo de umidade e a água absorvida, em porcentagem de massa, foram maiores para as bandagens que continham grandes quantidades de PVP devido à sua natureza hidrofílica. As variações na liberação de fármaco foram observadas entre as várias formulações. Todas as liberações seguiram a cinética de difusão controlada de ordem zero. Duas bandagens DBP resultaram em melhor e mais adequada liberação. As duas formulações com DBP foram escolhidas para a preparação de matriz de bandagens para estudos posteriores.

Antimicrobial Activity of Hydrophilic Polyvinyl Pyrrolidone Coated Bioflex / 대한남성과학회지

PURPOSE: A major concern of implanting urologists is infection, which occurs in 2% to 4.5% of cases. The present study was undertaken to investigate whether a hydrophilic coating which is designed to reduce bacterial adherence, applied to an inflatable penile prosthesis (IPP), would prolong the effect of antibiotics utilized intraoperatively. MATERIALS AND METHODS: The efficacy of antibiotics-soaked Bioflex(penile prosthetic substrate material) disc with and without hydrophilic coating was examined using an in-vivo rabbit model. A total of 320 Bioflex discs were used. 160 discs were coated with hydrophilic coating, and the remaining 160 disc, which were not coated, served as controls. All discs were soaked in an aqueous solution of gentamycin and bacitracin. Each group of 16 animals contained 64 discs. Two coated and 2 uncoated Bioflex discs were implanted subcutaneously in the dorsal region of each rabbit. The implanted antibiotic-soaked discs were extracted at 0, 1, 2, 3, and 5 days following implantation, and the zone of inhibition against S. epidermidis, S. aureus, E. coli, and P. aeruginosa in vitro was determined. RESULTS: A zone of inhibition for each of the microorganisms was present for all discs (coated and uncoated) at day 0. From day 1 to day 3, the coated discs demonstrated continued microbial inhibition against S. epidermidis compared to the uncoated discs, which did not. CONCLUSIONS: This study demonstrated that the use of a hydrophilic coating as a penile implant coating does not reduce the effectiveness of antibiotics utilized intraoperatively. Additionally, the coated discs demonstrated a sustained antibiotics activity against S. epidermidis for at least 3 days. This effect, along with the reduced adherence properties of the hydrophilic coating, may prevent the adhesion and colonization of S. epidermidis to penile implants and thereby reduce the chance of prosthetic infection.

Study on Solid Dispersion of Quercetin / 中国药房

OBJECTIVE:To prepare solid dispersion for increasing solubility of quercetin METHODS:Using polyvinyl pyrrolidone(PVP) as the carrier,solid dispersion of quercetin was prepared by solvent -volatilization method The solubility of the solid dispersion was detected IR spectrometer and UV spectrometer were used to investigate the physical and chemical properties of the solid dispersion RESULTS:The solubility of solid dispersion was significantly increased compared with quercetin and the physical mixture Quercetin existed as ultrafine crystalline or molecular form in solid dispersion,so there was no chemical reaction between quercetin and PVP CONCLUSION:PVP could be used as the carrier of solid dispersion to increase the solubility of quercetin in water