BIOAVAILABILITY OF SINGLE AND MULTIPLE DOSES OF ENTERIC-COATED MESALAMINE AND SULFASALAZINE

被引:17
作者
COREY, AE
ROSE, GM
CONKLIN, JD
机构
[1] Biopharmaceutics Section, Norwich Eaton Pharmaceuticals, Inc., Norwich, New York
关键词
bioavailability; healthy volunteers; Mesalamine; N-aceryl-5-aminosalicylic acid; pharmacokinetics; steady state; sulphasalazine;
D O I
10.1177/030006059001800601
中图分类号
R-3 [医学研究方法]; R3 [基础医学];
学科分类号
1001 ;
摘要
The bioavailibility of mesalamine from enteric-coated mesalamine and sulphasalazine was determined following a single dose and at steady state in healthy subjects in crossover studies. Plasma concentrations and urinary excretion of mesalamine and its major metabolite, N-acetyl-5-aminosalicylic acid, were measured. After a single dose of enteric-coated mesalamine, about 10 h elapsed before the onset of measurable plasma drug concentrations, probably representing gastro-intestinal transit prior to drug release near the ileocaecal junction. The elimination kinetics were similar for a single oral dose and steady state using enteric-coated mesalamine, but after both single and multiple administration of enteric-coated mesalamine only about 20% of the mesalamine given was absorbed, with about 80% estimated to remain for colon therapeutic activity. It is concluded that, despite different mechanisms of mesalamine release, enteric-coated mesalamine and sulphasalazine produced similar mesalamine absorption. © 1990, SAGE Publications. All rights reserved.
引用
收藏
页码:441 / 453
页数:13
相关论文
共 18 条
[1]   ADVERSE REACTIONS DURING SALICYLAZOSULFAPYRIDINE THERAPY AND RELATION WITH DRUG-METABOLISM AND ACETYLATOR PHENOTYPE [J].
DAS, KM ;
EASTWOOD, MA ;
MCMANUS, JPA ;
SIRCUS, W .
NEW ENGLAND JOURNAL OF MEDICINE, 1973, 289 (10) :491-495
[2]   COMPARISON OF THE ABSORPTION AND METABOLISM OF SULPHASALAZINE AND ACRYLIC-COATED 5-AMINO SALICYLIC-ACID IN NORMAL SUBJECTS AND PATIENTS WITH COLITIS [J].
DEW, MJ ;
EBDEN, P ;
KIDWAI, NS ;
LEE, G ;
EVANS, BK ;
RHODES, J .
BRITISH JOURNAL OF CLINICAL PHARMACOLOGY, 1984, 17 (04) :474-476
[3]   COLONIC RELEASE OF 5-AMINO SALICYLIC-ACID FROM AN ORAL PREPARATION IN ACTIVE ULCERATIVE-COLITIS [J].
DEW, MJ ;
RYDER, REJ ;
EVANS, N ;
EVANS, BK ;
RHODES, J .
BRITISH JOURNAL OF CLINICAL PHARMACOLOGY, 1983, 16 (02) :185-187
[4]   CONTROLLED THERAPEUTIC TRIAL OF LONG-TERM MAINTENANCE TREATMENT OF ULCERATIVE-COLITIS WITH SULFASALAZINE (SALAZOPYRIN) [J].
DISSANAYAKE, AS ;
TRUELOVE, SC .
GUT, 1973, 14 (12) :923-926
[5]   SPECIFIC MEASUREMENT OF 5-AMINOSALICYLIC ACID AND ITS ACETYLATED METABOLITE IN HUMAN BILE [J].
FISCHER, C ;
MAIER, K ;
KLOTZ, U .
BRITISH JOURNAL OF CLINICAL PHARMACOLOGY, 1983, 15 (02) :273-274
[6]   RATE LIMITING STEPS IN METABOLITE KINETICS - FORMATION OF 5-ACETYLAMINOSALICYLATE AFTER ADMINISTRATION OF 5-AMINOSALICYLATE [J].
HOUSTON, JB ;
CASSIDY, MK .
JOURNAL OF PHARMACY AND PHARMACOLOGY, 1982, 34 (08) :536-538
[7]  
IRELAND A, 1987, GASTROENTEROLOGY, V92, P1447
[8]  
KAHN AKA, 1977, LANCET, V2, P892
[9]  
LEVI AJ, 1979, LANCET, V2, P276
[10]   METABOLISM AND URINARY-EXCRETION OF 5-AMINO SALICYLIC-ACID IN HEALTHY-VOLUNTEERS WHEN GIVEN INTRAVENOUSLY OR RELEASED FOR ABSORPTION AT DIFFERENT SITES IN THE GASTROINTESTINAL-TRACT [J].
MYERS, B ;
EVANS, DNW ;
RHODES, J ;
EVANS, BK ;
HUGHES, BR ;
LEE, MG ;
RICHENS, A ;
RICHARDS, D .
GUT, 1987, 28 (02) :196-200