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薄荷醇对旋光性和外消旋普萘洛尔透过豚鼠皮肤通透性的影响。

Effect of menthol on permeability of an optically active and racemic propranolol across guinea pig skin.

作者信息

Zahir A, Kunta J R, Khan M A, Reddy I K

机构信息

College of Pharmacy and Allied Health Professions, St. John's University, Jamaica, New York 11439, USA.

出版信息

Drug Dev Ind Pharm. 1998 Sep;24(9):875-8. doi: 10.3109/03639049809088534.

DOI:10.3109/03639049809088534
PMID:9876540
Abstract

The effect of menthol on the percutaneous penetration of S(-)-propranolol (SPL) and racemic form of propranolol (RSPL) was investigated in vitro using excised abdominal skin of guinea pig. In the presence of menthol, the permeability coefficient of SPL was high compared with that of RSPL. The enhancement factors for SPL and RSPL were 2.12 and 0.85, respectively. The lag times for SPL and RSPL were reduced considerably in the presence of menthol compared to those for control (without enhancer). The present findings suggest the enantio-selective permeation of SPL across the guinea pig skin in the presence of menthol.

摘要

利用豚鼠离体腹部皮肤,在体外研究了薄荷醇对S(-)-普萘洛尔(SPL)和普萘洛尔外消旋体(RSPL)经皮渗透的影响。在薄荷醇存在的情况下,SPL的渗透系数高于RSPL。SPL和RSPL的增强因子分别为2.12和0.85。与对照(无增强剂)相比,在薄荷醇存在的情况下,SPL和RSPL的滞后时间显著缩短。目前的研究结果表明,在薄荷醇存在的情况下,SPL在豚鼠皮肤中的对映体选择性渗透。

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