DEVELOPMENT OF A MULTIPLE UNIT DRUG DELIVERY SYSTEM FOR POSITIONED RELEASE IN THE GASTROINTESTINAL-TRACT

被引：20

作者：

KLOKKERSBETHKE, K

FISCHER, W

机构：

来源：

JOURNAL OF CONTROLLED RELEASE | 1991年 / 15卷 / 02期

关键词：

COLONIC ABSORPTION; DILTIAZEM HYDROCHLORIDE; PELLETS; POSITIONED RELEASE;

D O I：

10.1016/0168-3659(91)90068-O

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

An oral drug delivery system providing a uniform drug delivery can only partly satisfy therapeutic and biopharmaceutical needs, as it does not take into account site specific absorption rates within the gastrointestinal tract. A drug delivery system guaranteeing site and rate specific delivery is needed to release locally effective drugs at their target site, to achieve a prolongation of effective plasma levels or to provide a pulsed drug release. It is shown, for a multiple dose formulation of the model drug diltiazem hydrochloride being absorbed from the small and the large intestine, how the site specific drug delivery system was developed. The in vivo targeting properties of two formulations containing 120 mg of drug per capsule were investigated in a bioavailability study. Both formulations targeted the drug to lower parts of the intestine: one formulation released diltiazem in the lower part of the small bowel and the second one in the colon. The t(max) values were 7.3 +/- 1.0 h and 14.3 +/- 5.0 h; the relative AUC values were 100% and 60%.

引用

页码：105 / 112

页数：8

共 21 条

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