文章基本信息

标题：Drug Targeting Efficacy to Underlying Muscle Following Topical Application. I. Evaluation Based on a Physiological Pharmacokinetic Model
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作者：Tomomi HATANAKA ; Eiichiro MANABE ; Tomohiro OHTSUKI 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：2000
卷号：23
期号：7
页码：860-865
DOI：10.1248/bpb.23.860
出版社：The Pharmaceutical Society of Japan
摘要：A physiological pharmacokinetic model describing the absorption and disposition of topically applied drugs was proposed, and the effect of various pharmacokinetic and physiological parameters on the drug delivery into the targeted muscle was simulated. The proposed model consists of vehicle, and stratum corneum, viable epidermis and muscle below the application and referene sites, and plasma, each joined with transfer clearance and plasma flow. Indomethacin concentrations in tissues and plasma after topical application to rats could be explained by the model. Most indomethacin delivered into the underlying muscle was via direct penetration. The model simulation showed that the increase in plasma clearance and clearance between viable skin and muscle, and the decrease in application area and plasma flow rate into viable skin and muscle would promote the targeting efficacy of topically applied drugs to the underlying muscle.
关键词：drug targeting;topical application;physiological pharmacokinetic model;indomethacin;nonsteroidal antiinflammatory drug;site-specific delivery