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布洛芬缓释微球的体外评价

In-vitro evaluation of sustained release ibuprofen microspheres.

作者信息

Ghaly E S, Sepúlveda S

机构信息

School of Pharmacy, University of Puerto Rico, San Juan.

出版信息

P R Health Sci J. 1996 Jun;15(2):97-100.

PMID:8936613
Abstract

Microspheres for oral use have been employed to target and to sustain the release of the drug. The objective of this study was to use the melt dispersion technique and aqueous vehicle to entrap ibuprofen into wax carrier (carnauba wax) with the aid of surfactant (Pluronic L-62). The effects of different levels of Pluronic L-62, stirring speed, and ibuprofen levels, as well as the in-vitro release rate of ibuprofen were evaluated. The in-vitro dissolution of ibuprofen in phosphate buffer pH 7.2 showed that microspheres prepared with low amount of drug (1.5 g) released 58.1% of ibuprofen after 6 hours, while microspheres prepared with high amount of drug (6.0 g) released only 38.9% of ibuprofen. Microsphere formulations prepared by using aqueous vehicle were spherical and of smooth surface. In general the melt dispersion technique was a successful method for preparing sustained release ibuprofen microspheres.

摘要

口服微球已被用于药物的靶向和缓释。本研究的目的是借助表面活性剂(普朗尼克L - 62),采用熔融分散技术和水性载体将布洛芬包封于蜡质载体(巴西棕榈蜡)中。评估了不同水平的普朗尼克L - 62、搅拌速度、布洛芬水平以及布洛芬的体外释放速率。布洛芬在pH 7.2磷酸盐缓冲液中的体外溶出表明,用少量药物(1.5 g)制备的微球在6小时后释放了58.1%的布洛芬,而用大量药物(6.0 g)制备的微球仅释放了38.9%的布洛芬。用水性载体制备的微球制剂呈球形且表面光滑。总体而言,熔融分散技术是制备布洛芬缓释微球的成功方法。

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