Biopharmaceutics classification by high throughput solubility assay and PAMPA

被引:42
作者
Obata, K [1 ]
Sugano, K [1 ]
Machida, M [1 ]
Aso, Y [1 ]
机构
[1] Chugai Pharmaceut Co Ltd, Preclin Res Dept 1, Shizuoka 4128513, Japan
关键词
solubility; permeability; high throughput; biopharmaceutics classification system (BCS);
D O I
10.1081/DDC-120028713
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
The purpose of the present Study was to examine the relevancy of the high throughput solubility assay and permeability assay to the biopharmaceutics classification system (BCS). Solubility and permeability were measured by high throughput Solubility assay (HTSA) and parallel artificial membrane permeation assay (PAMPA), respectively. High throughput solubility assay was performed Using simulated gastric fluid (SGF, pH 1.2) and simulated intestinal fluid without bile acid (SIF, pH 6.8). We categorize 18 drugs based on the BCS using HTSA and PAMPA. Fourteen out of 18 drugs were correctly classified (78% Success rate). The result of the present study showed that HTSA could predict BCS class with a high Success rate, and PAMPA Could also be useful to predict the permeation of drugs.
引用
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页码:181 / 185
页数:5
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