微渗析技术用于盐酸奥旦西酮的大鼠在体透皮吸收研究

微渗析技术用于盐酸奥旦西酮的大鼠在体透皮吸收研究

丁平田, 徐晖, 郑俊民

沈阳药科大学药学系, 沈阳 110015

收稿日期:1999-05-05 修回日期:1999-10-25 出版日期:2000-06-15 发布日期:2000-06-15

Microdialysis Sampling for Transdermal Delivery Study of Ondansetron HCl in Rats

Ding Pingtian, Xu Hui, Zheng Junmin

Deportment of Pharmacy Shenyang Pharmaceutical University Shenyang 110015

Received:1999-05-05 Revised:1999-10-25 Online:2000-06-15 Published:2000-06-15

摘要/Abstract

摘要： 本文进行了微渗析探针的体内、外校正,浓差法和反渗析法分别用于测定探针的体内和体外回收率。在探针校正的基础上,研究了盐酸奥旦西酮(ON)丙二醇(PG)溶液的大鼠在体经皮吸收及渗透促进剂油酸(OA)的作用。微渗析样品用高效液相法测定。结果证明:探针的体外回收率(35.46±42%)和体内回收率(32.53±1.8%)没有显著的差别(P>0.1)。以2%和5%OA的PG溶液为渗透促进剂时,ON在渗析液和真皮中达到坪浓度的时间分别为3.5及1.5 h:后者的坪浓度约是前者的两倍。当OA的浓度从0提高到2%、5%时,药物的稳态传递速度从0.001增大到0.030和0.058 μg·h^-1。实验证明OA对于ON的大鼠在体透皮吸收是一种有效的促进剂。

关键词: 微渗析, 盐酸奥旦西酮, 透皮吸收, 促进剂

Abstract: The characterization of microdialysis probe was performed in vitro and in vivo. No net flux method and retrodialysis method were used to find the recovery in vitro and in vivo respectively. On the basis of the probe characterization, transdermal delivery of ondansetron HCI (ON) solution in propylene glycol (PG) with a widely used enhancer oleic acid (OA) was carried out in rats. Dialysate samples collected from the probe were analyzed by HPLC. There was no significant difference between the in vitro recovery (35.46±4.2%) and the in vivo recovery (32.53±1.8%) (P>0.1). The ON concentration in both dialysate and dermis reached a plateau at 1.5 h by coapplication of 5% OA in solution of ON in PG, while at about 3.5 h by co-application of 2% OA. And the plateau ON concentration in case of 5% OA was about two fold of that of 2% OA. Oleic acid at concentrations of 2% and 5% (w/v) increased the delivery rates from 0.001 to 0.030 and 0.058 μg·h^-1 respectively. OA proved to be an effective enhancer for transdermal delivery of ON in rats.

Key words: Microdialysis, Microdialysis, Ondansetron HCI, Ondansetron HCI, Transdermal delivery, Transdermal delivery, Enhancer, Enhancer

Supporting:

丁平田, 徐晖, 郑俊民. 微渗析技术用于盐酸奥旦西酮的大鼠在体透皮吸收研究[J]. .

Ding Pingtian, Xu Hui, Zheng Junmin. Microdialysis Sampling for Transdermal Delivery Study of Ondansetron HCl in Rats[J]. .

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