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标题：Effect of Dosage Form on Stereoisomeric Inversion of Ibuprofen in Volunteers
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作者：Tetsuya AIBA ; Mary M TSE ; Emil T LIN 等
期刊名称：Biological and Pharmaceutical Bulletin
印刷版ISSN：0918-6158
电子版ISSN：1347-5215
出版年度：1999
卷号：22
期号：6
页码：616-622
DOI：10.1248/bpb.22.616
出版社：The Pharmaceutical Society of Japan
摘要：Twelve healthy volunteers were given ibuprofen racemate in two different dosage forms, a suspension and a tablet. The plasma concentration-time profiles of S- and R-ibuprofen were determined and the R-ibuprofen inversion clearance was calculated. Although the area under the curve was almost the same in both the suspension and tablet studies, the inversion clearance was larger in the suspension study than in the tablet study (1.18±0.65 and 0.72±0.63l/h, shown as the mean±S.D.). The Michaelis-Menten parameters for this inversion process were then determined in vitro with human liver microsomes (1.3±0.2 mM for K_m and 3.1±0.3 nmol/min/mg protein for V_max, shown as the mean±S.D.). These parameters indicated that the stereoisomeric inversion of R-ibuprofen in the liver was not likely to be saturated at the plasma concentrations measured in the volunteer study. The profile of the plasma concentration ratio between S-ibuprofen and R-ibuprofen revealed a difference in the early phase of these two studies. Therefore the inversion defference between those two studies probably resulted from the difference in the absorption phase of each dosage form. Our study demonstrated that R-ibuprofen inversion could be affected by alteration of dosage from.
关键词：ibuprofen;stereospecific inversion;dosage form;healthy volunteer;human liver microsome