Design and evaluation of a new capsule-type dosage form for colon-targeted delivery of drugs

被引：40

作者：

Ishibashi, T ^{[1
]}

Hatano, H ^{[1
]}

Kobayashi, M ^{[1
]}

Mizobe, M ^{[1
]}

Yoshino, H ^{[1
]}

机构：

[1] Tanabe Seiyaku Co Ltd, Pharmaceut Res Lab, Yodogawa Ku, Osaka 532, Japan

来源：

INTERNATIONAL JOURNAL OF PHARMACEUTICS | 1998年 / 168卷 / 01期

关键词：

colon-targeted delivery; hard gelatin capsule; organic acid; Eudragit (R) E; HPMC (R)-AS;

D O I：

10.1016/S0378-5173(98)00082-9

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

A new capsule-type dosage form was investigated for colon-targeted delivery of drugs. The system was designed by imparting a tinted-release function and a pH-sensing function to a hard gelatin capsule. The technical characteristics of the system are to contain an organic acid together with an active ingredient in a capsule coated with a three-layered film consisting of an acid-soluble polymer, a water-soluble polymer, and an enteric polymer. In order to find the suitable formulation, various formulation factors were investigated through a series of in vitro dissolution studies. As a result, it was found that: (1) various organic acids can be used for this system; (2) a predictable timed-release mechanism of a drug can be attained by adjusting the thickness of the Eudragit(R) layer; and (3) the outer enteric coating with HPMC(R)-AS provided acceptable acid-resistibility. All these results suggested that this approach can provide a useful and practical means for colon-targeted delivery of drugs. (C) 1998 Elsevier Science B.V. All rights reserved.

引用

页码：31 / 40

页数：10

共 14 条

[1] AN INVITRO INVESTIGATION INTO THE SUITABILITY OF PH-DEPENDENT POLYMERS FOR COLONIC TARGETING [J].

ASHFORD, M ;

FELL, JT ;

ATTWOOD, D ;

WOODHEAD, PJ .

INTERNATIONAL JOURNAL OF PHARMACEUTICS, 1993, 91 (2-3) :241-245

[2] NON-INVASIVE METHOD FOR DELIVERY OF TRACER SUBSTANCES OR SMALL QUANTITIES OF OTHER MATERIALS TO THE COLON [J].

CHACKO, A ;

SZAZ, KF ;

HOWARD, J ;

CUMMINGS, JH .

GUT, 1990, 31 (01) :106-110

[3] TRANSIT OF PHARMACEUTICAL DOSAGE FORMS THROUGH THE SMALL-INTESTINE [J].

DAVIS, SS ;

HARDY, JG ;

FARA, JW .

GUT, 1986, 27 (08) :886-892

[4]

GAZZANIGA A, 1995, STP PHARMA SCI, V5, P83

[5] ORAL DELAYED-RELEASE SYSTEM FOR COLONIC SPECIFIC DELIVERY [J].

GAZZANIGA, A ;

IAMARTINO, P ;

MAFFIONE, G ;

SANGALLI, ME .

INTERNATIONAL JOURNAL OF PHARMACEUTICS, 1994, 108 (01) :77-83

[6]

MILOJEVIC S, 1995, STP PHARMA SCI, V5, P47

[7]

MOOTER VD, 1994, PHARMACEUT RES, V11, P1737

[8] FILM-FORMING POLYMERS FOR COLONIC DRUG-DELIVERY .1. SYNTHESIS AND PHYSICAL AND CHEMICAL-PROPERTIES OF METHYL-DERIVATIVES OF EUDRAGIT-S [J].

PEETERS, R ;

KINGET, R .

INTERNATIONAL JOURNAL OF PHARMACEUTICS, 1993, 94 (1-3) :125-134

[9]

RUBINSTEIN A, 1993, J PHARM SCI, V82, P867

[10]

SAFFRAN M, 1979, SCIENCE, V223, P1081

← 1 2 →