萜烯类手性促进剂对氟比洛芬经皮渗透对映体选择性的影响

发布时间：2019-04-19 22:58

【摘要】：目的:考察萜烯类手性促进剂芳樟醇和薄荷醇对氟比洛芬(flurbiprofen,FP)经皮渗透的对映体选择性作用。方法:采用Valia-Chien双室渗透扩散池,以大鼠离体皮肤为渗透屏障,以稳态经皮渗透速率为评价指标,用对映体选择性高效液相色谱法对FP对映体进行浓度测定,考察手性促进剂芳樟醇或薄荷醇对FP对映体选择性的影响。结果:无论供给液是否含单个对映体或消旋体,若供给液中不含促透剂,FP经大鼠离体皮肤渗透未见对映体选择性。当供给液中含有dl-薄荷醇时,RSFP的稳态渗透速率分别为R-FP、S-FP的1.34,1.27倍,差异有显著性(P0.05);而供给液中含有l-薄荷醇时,FP对映体及消旋体间的皮肤渗透速率无显著差异(P0.05)。l-薄荷醇和dl-薄荷醇对同一药物构型R-FP或S-FP的促透效果相当;然而,dl-薄荷醇对RS-FP的促透作用是l-薄荷醇的1.44倍。l-芳樟醇或dl-芳樟醇作为手性促透剂时,未发现对映体选择性渗透现象。结论:dl-薄荷醇对FP的促透作用出现了对映体选择性,而l-薄荷醇、l-芳樟醇和dl-芳樟醇未引起FP的对映体选择性渗透,且所有渗透实验均未发现对映体转化。
[Abstract]:Aim: to investigate the enantioselectivity of linalool and menthol as chiral promoters of terpene on the percutaneous permeation of flurbiprofen (flurbiprofen,FP). Methods: the concentration of Valia-Chien enantiomers was determined by enantiomeric selective high performance liquid chromatography (HPLC) using Valia-Chien two-compartment osmotic diffusion cell, isolated rat skin as osmotic barrier, steady-state percutaneous permeation rate as the evaluation index, and enantiomeric selective high performance liquid chromatography (HPLC). The effects of chiral promoters linalool or menthol on the enantioselectivity of FP were investigated. Results: no matter whether there was a single enantiomer or racemate in the donor solution, no enantioselective enantioselectivity was found in the FP permeation through the rat skin in vitro if there was no transdermal enhancer in the donor solution. When dl- menthol was contained in the feed solution, the steady-state permeation rate of RSFP was 1.34,1.27 times higher than that of RFP, respectively (P0.05). There was no significant difference in skin penetration rate between FP enantiomers and racemates (P0.05). L-menthol and dl- menthol had the same effect on the penetration of R-FP or S-FP of the same drug configuration. However, the transmissibility of dl- menthol on RS-FP was 1.44 times higher than that of l-menthol. When l-linalool or dl- linalool was used as chiral enhancer, enantiomeric selective permeation was not found. Conclusion: the enantioselective enantioselectivity of dl- menthol on FP was observed, while lmenthol, llinalool and dl- linalool did not induce enantioselective permeation of FP, and no enantiomeric transformation was found in all permeation experiments.
【作者单位】： 浙江省医学科学院药物研究所;
【基金】：浙江省科技计划项目(编号:2014F10034)
【分类号】：R943

【相似文献】

相关期刊论文 前10条

1 荣毅;俞文英;郭霞;曾珊珊;沈正荣;曾苏;叶金翠;;芳樟醇对十八甲基炔诺酮经皮渗透对映体选择性的影响[J];药学学报;2014年08期

2 ;[J];;年期

3 ;[J];;年期

4 ;[J];;年期

5 ;[J];;年期

6 ;[J];;年期

7 ;[J];;年期

8 ;[J];;年期

9 ;[J];;年期

10 ;[J];;年期

相关会议论文 前1条

1 伍贻康;;Brefeldin A的高效对映体选择性全合成[A];中国化学会第26届学术年会有机化学分会场论文集[C];2008年

相关博士学位论文 前2条

1 王鲁梅;两种典型手性农药内分泌干扰效应的对映体选择性研究[D];浙江大学;2008年

2 王红;氧化硅负载双VA唑啉金属催化剂上不对称Diels-Alder反应研究[D];中国科学院研究生院（大连化学物理研究所）;2006年

相关硕士学位论文 前2条

1 张烨;手性农药对映体选择性环境行为的研究[D];河北科技大学;2010年

2 张聪;联苯菊酯的细胞毒性及杀虫活性的对映体选择性研究[D];浙江工业大学;2009年

，

本文编号：2461366