GASTROINTESTINAL ABSORPTION OF CHLOROTHIAZIDE - EVALUATION OF A METHOD USING SALICYLAZOSULFAPYRIDINE AND ACETAMINOPHEN AS THE MARKER COMPOUNDS FOR DETERMINATION OF THE GASTROINTESTINAL TRANSIT-TIME IN THE DOG

被引:35
作者
MIZUTA, H
KAWAZOE, Y
OGAWA, K
机构
[1] Research Laboratories, Yoshitomi Pharmaceutical Industries, Ltd., Fukuoka 871, Koiwai, Yoshitomi-cho, Chikujo-gun
关键词
absorption; acetaminophen; atropine sulfate; chlorothiazide; dog; gastric emptying rate: small intestinal transit time; gastrointestinal transit; salicylazosulfapyridine; small intestinal segment; upper;
D O I
10.1248/cpb.38.2810
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Gastrointestinal absorption properties of chlorothiazide was investigated in dogs by a double-marker method using acetaminophen and salicylazosulfapyridine as the markers. The mean absorption time of acetaminophen (MA TAAP) and the time for first appearance of sulfapyridine in plasma (TFASP) were used for the assessment of gastric emptying and oro-colonic transit times, respectively. Chlorothiazide absorption efficiency was increased by pretreatment with atropine sulfate. There was a good correlation between MA TAAPand the extent of bioavailability of chlorothiazide, however, there was no correlation between TFASPand the extent of bioavailability of the drug. These results indicate that chlorothiazide absorption takes place primarily in a limited segment of the upper small intestine, supporting the assumption reported previously. This double-marker method seems to be a useful tool for the investigation of the relationship between drug absorption and its gastrointestinal transit. © 1990, The Pharmaceutical Society of Japan. All rights reserved.
引用
收藏
页码:2810 / 2813
页数:4
相关论文
共 16 条
[1]   ENHANCEMENT OF GASTROINTESTINAL ABSORPTION OF HYDROCHLOROTHIAZIDE BY PROPANTHELINE [J].
BEERMANN, B ;
GROSCHINSKYGRIND, M .
EUROPEAN JOURNAL OF CLINICAL PHARMACOLOGY, 1978, 13 (05) :385-387
[2]   THE USE OF GAMMA-SCINTIGRAPHY TO FOLLOW THE GASTROINTESTINAL TRANSIT OF PHARMACEUTICAL FORMULATIONS [J].
CHRISTENSEN, FN ;
DAVIS, SS ;
HARDY, JG ;
TAYLOR, MJ ;
WHALLEY, DR ;
WILSON, CG .
JOURNAL OF PHARMACY AND PHARMACOLOGY, 1985, 37 (02) :91-95
[3]   TRANSIT OF PHARMACEUTICAL DOSAGE FORMS THROUGH THE SMALL-INTESTINE [J].
DAVIS, SS ;
HARDY, JG ;
FARA, JW .
GUT, 1986, 27 (08) :886-892
[4]   THE GASTRIC-EMPTYING OF HARD GELATIN CAPSULES [J].
HUNTER, E ;
FELL, JT ;
SHARMA, H .
INTERNATIONAL JOURNAL OF PHARMACEUTICS, 1983, 17 (01) :59-64
[5]   GASTRIC-EMPTYING RATES OF DRUG PREPARATIONS .1. EFFECTS OF SIZE OF DOSAGE FORMS, FOOD AND SPECIES ON GASTRIC-EMPTYING RATES [J].
KANIWA, N ;
AOYAGI, N ;
OGATA, H ;
EJIMA, A .
JOURNAL OF PHARMACOBIO-DYNAMICS, 1988, 11 (08) :563-570
[6]   SULFAPYRIDINE APPEARANCE IN PLASMA AFTER SALICYLAZOSULFAPYRIDINE - ANOTHER SIMPLE MEASURE OF INTESTINAL TRANSIT [J].
KELLOW, JE ;
BORODY, TJ ;
PHILLIPS, SF ;
HADDAD, AC ;
BROWN, ML .
GASTROENTEROLOGY, 1986, 91 (02) :396-400
[7]  
MANNINEN V, 1973, LANCET, V1, P398
[8]   EFFECT OF SIZE AND DENSITY ON CANINE GASTRIC-EMPTYING OF NONDIGESTIBLE SOLIDS [J].
MEYER, JH ;
DRESSMAN, J ;
FINK, A ;
AMIDON, G .
GASTROENTEROLOGY, 1985, 89 (04) :805-813
[9]   DETERMINATION OF SMALL INTESTINAL TRANSIT-TIME IN BEAGLE DOGS USING SALICYLAZOSULFAPYRIDINE [J].
MIZUTA, H ;
KAWAZOE, Y ;
HAGA, K ;
OGAWA, K ;
YOKOBE, T .
YAKUGAKU ZASSHI-JOURNAL OF THE PHARMACEUTICAL SOCIETY OF JAPAN, 1989, 109 (10) :760-765
[10]   BIOAVAILABILITY OF CHLOROTHIAZIDE FROM 50, 100, AND 250 MG SOLUTION DOSES [J].
OSMAN, MA ;
PATEL, RB ;
IRWIN, DS ;
CRAIG, WA ;
WELLING, PG .
BIOPHARMACEUTICS & DRUG DISPOSITION, 1982, 3 (02) :89-94