Stereoselective Pharmacokinetics of Ketoprofen After Oral Administration of Modified-Release Formulations in Caucasian Healthy Subjects

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• 作者：Marianela Lorier ; Laura Magallanes…
• 刊名：European Journal of Drug Metabolism and Pharmacokinetics
• 出版年：2016
• 出版时间：December 2016
• 年：2016
• 卷：41
• 期：6
• 页码：787-793
• 全文大小：
• 刊物主题：Pharmacology/Toxicology; Pharmacy; Human Physiology; Pharmaceutical Sciences/Technology; Medical Biochemistry;
• 出版者：Springer International Publishing
• ISSN：2107-0180
• 卷排序：41

文摘

Background and ObjectivesKetoprofen, a potent nonsteroidal anti-inflammatory drug, is clinically administered as a racemic mixture. One of the possible metabolism routes of ketoprofen is the inversion of the R- to S-enantiomer in the gastrointestinal tract. Ketoprofen, as a weak acid drug, might undergo recirculation through pancreatic/intestinal juices. The aim of the work was to investigate if a plasma-gastrointestinal tract recirculation of ketoprofen could explain its R-to-S chiral inversion after the oral administration of two modified-release formulations: a gastro-resistant delayed-release tablet (Reference) and an extended-release-plus-immediate-release bilayer tablet (Test).