ORAL DELAYED-RELEASE SYSTEM FOR COLONIC SPECIFIC DELIVERY

被引:139
作者
GAZZANIGA, A
IAMARTINO, P
MAFFIONE, G
SANGALLI, ME
机构
[1] BOEHRINGER INGELHEIM ITALIA,I-20139 MILAN,ITALY
[2] UNIV PAVIA,DIPARTIMENTO CHIM FARMACEUT,PAVIA,ITALY
关键词
COLONIC SPECIFIC DELIVERY; ORAL TIME-BASED SYSTEM; DELAYED RELEASE; FILM COATING; HIGH-VISCOSITY HPMC; SMALL INTESTINE TRANSIT TIME;
D O I
10.1016/0378-5173(94)90418-9
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
The paper describes a novel oral time-based drug release system for colonic specific delivery. The system, designed to exploit the relatively constant small intestine transit time of dosage forms, consists of drug-containing cores coated with three polymeric layers. The outer layer dissolves at pH > 5, then the intermediate swellable layer, made of high-viscosity HPMC, interacts slowly with aqueous fluids, thus providing the delay phase. The inner film is made of an enteric material. The system provides the expected delayed release pattern, as also indicated by the preliminary in vivo experiments on rats.
引用
收藏
页码:77 / 83
页数:7
相关论文
共 24 条
[1]   AN IN-VIVO INVESTIGATION INTO THE SUITABILITY OF PH DEPENDENT POLYMERS FOR COLONIC TARGETING [J].
ASHFORD, M ;
FELL, JT ;
ATTWOOD, D ;
SHARMA, H ;
WOODHEAD, PJ .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 1993, 95 (1-3) :193-199
[2]  
ASHFORD M, 1992, 6 C INT TECHNOL PHAR, V2, P59
[3]   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
[4]   DRUG RELEASE MODULATION BY PHYSICAL RESTRICTIONS OF MATRIX SWELLING [J].
COLOMBO, P ;
CONTE, U ;
GAZZANIGA, A ;
MAGGI, L ;
SANGALLI, ME ;
PEPPAS, NA ;
LAMANNA, A .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 1990, 63 (01) :43-48
[5]  
DAVIS S S, 1985, Journal of Controlled Release, V2, P27, DOI 10.1016/0168-3659(85)90030-6
[6]   TRANSIT OF PHARMACEUTICAL DOSAGE FORMS THROUGH THE SMALL-INTESTINE [J].
DAVIS, SS ;
HARDY, JG ;
FARA, JW .
GUT, 1986, 27 (08) :886-892
[7]   AN ORAL PREPARATION TO RELEASE DRUGS IN THE HUMAN-COLON [J].
DEW, MJ ;
HUGHES, PJ ;
LEE, MG ;
EVANS, BK ;
RHODES, J .
BRITISH JOURNAL OF CLINICAL PHARMACOLOGY, 1982, 14 (03) :405-408
[8]   MEASUREMENT OF GASTROINTESTINAL PH PROFILES IN NORMAL AMBULANT HUMAN-SUBJECTS [J].
EVANS, DF ;
PYE, G ;
BRAMLEY, R ;
CLARK, AG ;
DYSON, TJ ;
HARDCASTLE, JD .
GUT, 1988, 29 (08) :1035-1041
[9]   A COLON-SPECIFIC DRUG-DELIVERY SYSTEM BASED ON DRUG GLYCOSIDES AND THE GLYCOSIDASES OF COLONIC BACTERIA [J].
FRIEND, DR ;
CHANG, GW .
JOURNAL OF MEDICINAL CHEMISTRY, 1984, 27 (03) :261-266
[10]   ON THE RELEASE MECHANISM FROM COATED SWELLABLE MINIMATRICES [J].
GAZZANIGA, A ;
SANGALLI, ME ;
CONTE, U ;
CARAMELLA, C ;
COLOMBO, P ;
LAMANNA, A .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 1993, 91 (2-3) :167-171