An in vitro in vivo investigation of oral bioadhesive controlled release furosemide formulations

被引:44
作者
Santus, G
Lazzarini, C
Bottoni, G
Sandefer, EP
Page, RC
Doll, WJ
Ryo, UY
Digenis, GA
机构
[1] RECORDATI SPA,I-20148 MILAN,ITALY
[2] UNIV KENTUCKY,LEXINGTON,KY
关键词
bioadhesion; gamma-scintigraphy; neutron activation; controlled release formulation; gastrointestinal transit; furosemide; samarium-153;
D O I
10.1016/S0939-6411(97)00100-8
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
The in vitro controlled release and bioadhesive properties of furosemide formulations were evaluated with standard dissolution tests and with a specially developed model using rabbit intestine. The results showed that the controlled release properties were not affected by the application of the bioadhesive polymer but that the bioadhesive properties were substantially different. In order to assess the gastrointestinal transit time in vivo, a gamma-scintigraphy study was performed in six volunteers testing the same controlled release formulation with and without bioadhesive polymer. Plasma levels of furosemide, evaluation of urinary flux and measures of urinary excretion of furosemide in the six volunteers allowed correlations to be made between gastrointestinal transit and furosemide absorption. (C) 1997 Elsevier Science B.V.
引用
收藏
页码:39 / 52
页数:14
相关论文
共 21 条
[1]   BIOADHESIVE POLYMERS - SYNTHESIS, EVALUATION AND APPLICATION IN CONTROLLED RELEASE TABLETS [J].
CHITNIS, VS ;
MALSHE, VS ;
LALLA, JK .
DRUG DEVELOPMENT AND INDUSTRIAL PHARMACY, 1991, 17 (06) :879-892
[2]   TRANSIT OF PHARMACEUTICAL DOSAGE FORMS THROUGH THE SMALL-INTESTINE [J].
DAVIS, SS ;
HARDY, JG ;
FARA, JW .
GUT, 1986, 27 (08) :886-892
[3]   THE EFFECT OF FOOD ON THE GASTROINTESTINAL TRANSIT OF PELLETS AND AN OSMOTIC DEVICE (OSMET) [J].
DAVIS, SS ;
HARDY, JG ;
TAYLOR, MJ ;
WHALLEY, DR ;
WILSON, CG .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 1984, 21 (03) :331-340
[4]  
DIGENIS GA, 1991, CRIT REV THER DRUG, V7, P309
[5]   DUAL-ISOTOPE IMAGING OF NEUTRON-ACTIVATED ER-171 AND SM-153 AND THE INVIVO EVALUATION OF A DUAL-LABELED BILAYER TABLET BY GAMMA-SCINTIGRAPHY [J].
DIGENIS, GA ;
SANDEFER, EP ;
BEIHN, RM ;
PARR, AF .
PHARMACEUTICAL RESEARCH, 1991, 8 (10) :1335-1340
[6]  
Digenis GA, 1989, DRUG DELIVERY GASTRO, P111
[7]   GI TRANSIT OF POTENTIAL BIOADHESIVE FORMULATIONS IN MAN - A SCINTIGRAPHIC STUDY [J].
HARRIS, D ;
FELL, JT ;
SHARMA, HL ;
TAYLOR, DC .
JOURNAL OF CONTROLLED RELEASE, 1990, 12 (01) :45-53
[8]   MUCOADHESIVE DRUG DELIVERY SYSTEMS [J].
JIMENEZCASTELLANOS, MR ;
ZIA, H ;
RHODES, CT .
DRUG DEVELOPMENT AND INDUSTRIAL PHARMACY, 1993, 19 (1-2) :143-194
[9]   INTESTINAL TRANSIT OF BIOADHESIVE MICROSPHERES IN AN INSITU LOOP IN THE RAT - A COMPARATIVE-STUDY WITH COPOLYMERS AND BLENDS BASED ON POLY(ACRYLIC ACID) [J].
LEHR, CM ;
BOUWSTRA, JA ;
TUKKER, JJ ;
JUNGINGER, HE .
JOURNAL OF CONTROLLED RELEASE, 1990, 13 (01) :51-62
[10]  
LONGER MA, 1986, PHARM INT, V7, P114