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冰片对微乳基经皮治疗系统中川芎嗪的促经皮吸收及脑内分布作用

Percutaneous absorption and brain distribution facilitation of borneol on tetramethylpyrazine in a microemulsion-based transdermal therapeutic system.

作者信息

Hu Xiaoge, Cheng Ning, Zhao Jihui, Piao Xianghua, Yan Yulu, Zhang Qibo, Zhou Kuan, Zhang Yongtai, Feng Nianping

机构信息

School of Pharmacy, Shanghai University of Traditional Chinese Medicine, Shanghai 201203, China.

出版信息

Asian J Pharm Sci. 2019 May;14(3):305-312. doi: 10.1016/j.ajps.2018.06.003. Epub 2018 Jul 29.

Abstract

In this study, we show that the percutaneous absorption and brain distribution of tetramethylpyrazine (TMP) is enhanced when combined with borneol (BN) in a microemulsion-based transdermal therapeutic system (ME-TTS). The formulation of the TMP and BN microemulsion (TEM-BN-ME) was optimized in skin permeation studies following a uniform experimental design. Male Sprague-Dawley rats were used for the pharmacokinetic and tissue distribution studies of TMP-BN-ME-TTS. In the pharmacokinetic study, the TMP-BN-ME-TTS treated rats had significantly higher ( < 0.05) and AUC of TMP than the TMP-ME-TTS treated rats, indicating that BN improves the rate and extent of TMP percutaneous absorption. In the tissue distribution study, the AUC of TMP in brain was significantly higher in the TMP-BN-ME-TTS group ( < 0.05), indicating that BN facilitates the distribution of TMP in brain. In summary, BN enhanced the percutaneous absorption and brain distribution of TMP in a microemulsion-based transdermal therapeutic system.

摘要

在本研究中,我们表明,在基于微乳的透皮治疗系统(ME-TTS)中,当川芎嗪(TMP)与冰片(BN)联合使用时,其经皮吸收和脑内分布会增强。在均匀实验设计后的皮肤渗透研究中,对TMP和BN微乳(TEM-BN-ME)的配方进行了优化。使用雄性Sprague-Dawley大鼠进行TMP-BN-ME-TTS的药代动力学和组织分布研究。在药代动力学研究中,TMP-BN-ME-TTS处理的大鼠的TMP的Cmax和AUC显著高于(P<0.05)TMP-ME-TTS处理的大鼠,表明BN提高了TMP经皮吸收的速率和程度。在组织分布研究中,TMP-BN-ME-TTS组脑内TMP的AUC显著更高(P<0.05),表明BN促进了TMP在脑内的分布。总之,在基于微乳的透皮治疗系统中,BN增强了TMP的经皮吸收和脑内分布。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/f77c/7042483/647b031c36ba/fx1.jpg

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