文章基本信息

标题：Transdermal Absorption of Bupranolol in Rabbit Skin in Vitro and in Vivo
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作者：Taro OGISO ; Tomona HATA ; Masahiro IWAKI 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：2001
卷号：24
期号：5
页码：588-591
DOI：10.1248/bpb.24.588
出版社：The Pharmaceutical Society of Japan
摘要：This study was designed to clarify the percutaneous penetration of bupranolol (BP), a β-adrenoceptor antagonist, through rabbit skin and to compare the in vitro penetration with the in vivo absorption. BP penetrated across the skin slowly in the absence of enhancers in vitro. Isopropyl myristate and N-methyl-2-pyrrolidone enhanced the in vitro penetration, with a 3.6 times higher flux compared with that without enhancers. However, in the in vivo percutaneous absorption, the maximal penetration was obtained with the formulation added d-limonene, with a 3.0 times higher area under the concentration-time curve (AUC) than that for the formulation without enhancers. The plasma levels of BP determined, however, were extremely lower than the theoretical plasma steady-state concentrations predicted. The plasma levels of BP after application of these formulations were maintained in the range of 7—22 ng/ml for 30 h, of which concentrations were above the therapeutically effective concentration (1.5—4 ng/ml). Therefore, the transdermal systems will offer an efficient drug delivery system for the treatment of angina pectoris and tachycardia.
关键词：bupranolol skin penetration;in vitro penetration;in vivo absorption;penetration enhancer;rabbit skin