Enteric coated HPMC capsules designed to achieve intestinal targeting

被引:182
作者
Cole, ET
Scott, RA
Connor, AL
Wilding, IR
Petereit, HU
Schminke, C
Beckert, T
Cadé, D
机构
[1] Pfizer Inc, Capsugel Div, CH-4144 Basel, Switzerland
[2] Pharmaceut Profiles Ltd, Nottingham NG11 6JS, England
[3] Roehm GmbH & Co KG, DE-64293 Darmstadt, Germany
关键词
hydroxypropyl methylcellulose capsule; enteric coating; Eudragit (R); scintigraphic evaluation;
D O I
10.1016/S0378-5173(01)00871-7
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
The enteric coating of HPMC capsules containing paracetamol was investigated. Two enteric polymers, Eudragit(R) L 30 D-55 and Eudragit(R) FS 30 D were studied, which are designed to achieve enteric properties and colonic release, respectively. The capsules were coated in an Accela Cota 10, and, as shown by optical microscopy, resulted in capsules with a uniform coating. Scanning electron microscopy of the surface of the capsules illustrate that, in contrast to gelatin, HPMC has a rough surface, which provides for good adhesion to the coating. Dissolution studies demonstrated that capsules coated with Eudragit(R) L 30 D-55 were gastro resistant for 2 h at pH 1.2 and capsules coated with Eudragit(R) FS 30 D were resistant for a further 1h at pH 6.8. The product visualisation technique of gamma scintigraphy was used to establish the in vivo disintegration properties of capsules coated with 8 mg cm(-2) Eudragit(R) L 30 D-55 and 6 Mg cm(-2) Eudragit(R) FS 30 D. For HPMC units coated with Eudragit(R) L 30 D-55, complete disintegration occurred predominately in the small bowel in an average time of 2.4 It post dose. For HPMC capsules coated with Eudragit(R) FS 30 D, complete disintegration did not occur until the distal small intestine and proximal colon in an average time of 6.9 h post dose. (C) 2002 Elsevier Science B.V. All rights reserved.
引用
收藏
页码:83 / 95
页数:13
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