文章基本信息

标题：Extended Release Dosage Form of Glipizide: Development and Validation of a Level A in Vitro–in Vivo Correlation
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作者：Animesh Ghosh ; Uttam Kumar Bhaumik ; Anirbandeep Bose 等
期刊名称：Biological and Pharmaceutical Bulletin
印刷版ISSN：0918-6158
电子版ISSN：1347-5215
出版年度：2008
卷号：31
期号：10
页码：1946-1951
DOI：10.1248/bpb.31.1946
出版社：The Pharmaceutical Society of Japan
摘要：Defining a quantitative and reliable relationship between in vitro drug release and in vivo absorption is highly desired for rational development, optimization, and evaluation of controlled-release dosage forms and manufacturing process. During the development of once daily extended-release (ER) tablet of glipizide, a predictive in vitro drug release method was designed and statistically evaluated using three formulations with varying release rates. In order to establish internally and externally validated level A in vitro – in vivo correlation (IVIVC), a total of three different ER formulations of glipizide were used to evaluate a linear IVIVC model based on the in vitro test method. For internal validation, a single-dose four-way cross over study ( n =6) was performed using fast-, moderate-, and slow-releasing ER formulations and an immediate-release (IR) of glipizide as reference. In vitro release rate data were obtained for each formulation using the United States Pharmacopeia (USP) apparatus II, paddle stirrer at 50 and 100 rev. min⁻¹ in 0.1 m hydrochloric acid (HCl) and pH 6.8 phosphate buffer. The f ₂ metric (similarity factor) was used to analyze the dissolution data. The formulations were compared using area under the plasma concentration–time curve, AUC _0—∞, time to reach peak plasma concentration, T _max, and peak plasma concentration, C _max, while correlation was determined between in vitro release and in vivo absorption. A linear correlation model was developed using percent absorbed data versus percent dissolved from the three formulations. Predicted glipizide concentrations were obtained by convolution of the in vivo absorption rates. Prediction errors were estimated for C _max and AUC _0—∞ to determine the validity of the correlation. Apparatus II, pH 6.8 at 100 rev. min⁻¹ was found to be the most discriminating dissolution method. Linear regression analysis of the mean percentage of dose absorbed versus the mean percentage of in vitro release resulted in a significant correlation ( r ²≥0.9) for the three formulations.
关键词：controlled release;in vitro–in vivo correlation;bioavailability;dissolution;in vitro model