| 徐恒武,范煜航.双位点微透析探究盐酸青藤碱传递体皮肤及血液药代动力学[J].浙江中西医结合杂志,2024,34(8): |
| 双位点微透析探究盐酸青藤碱传递体皮肤及血液药代动力学 |
| Pharmacokinetics study of skin and blood of sinomenine hydrochloride transfersomes using double-site microdialysis |
| 投稿时间：2024-03-14 修订日期：2024-06-12 |
| DOI： |
| 中文关键词: 传递体 微透析 药代动力学 青藤碱 |
| 英文关键词:Transfersomes Microdialysis Pharmacokinetics Sinomenine |
| 基金项目:金华市科技局重点科研计划项目(2021-3-116) |
|
| 摘要点击次数: 757 |
| 全文下载次数: 2 |
| 中文摘要: |
| 目的 考察盐酸青藤碱(sinomenine hydrochloride,SH)传递体(SH transfersomes,SHTs)的皮肤与血液双位点药代动力学过程,探究SHTs的经皮药代动力学特性。方法 本文以脱氧胆酸钠为边缘活化剂制备了SHTs,以SH脂质体(SH liposomes,SHLs)为对照制剂。为了对比两者的经皮渗透差异,采用双位点微透析技术结合UPLC-MS同时检测SHTs和SHLs不同时间点血液与皮肤的透析液中SH浓度,绘制药时曲线,采用DAS3.1和统计矩方法得出皮肤/血液中SH药代动力学参数。对探针的体内外回收率进行考察,并比较传递体和脂质体两种载体的经皮药动学特性。结果 皮肤药代动力学数据显示,SHTs的Css为(1401.87±464.07)ng×mL-1, AUC0-t为(817476.04±289135.62)ng×mL-1×min-1,分别约为SHLs 的8.8倍和8.0倍,且SHTs的MRT0-t较短。血液药动学数据显示,SHTs的Css为(45.76±19.42)ng×mL-1,AUC0-t为(21172.99±2009.38)ng×mL-1×min-1,分别约为SHLs的3.7倍和2.9倍。结论 传递体相较于脂质体对于SH具有更好的促渗作用,其可作为促进SH透皮吸收的有效载体。 |
| 英文摘要: |
| Objective To investigate double-site pharmacokinetic processes of sinomenine hydrochloride (SH) transfersomes (SHTs) in the skin and blood and probe into the transdermal pharmacokinetic characteristics of SHTs. Methods SHTs was prepared with sodium deoxycholate as edge activator and SH liposomes (SHLs) as control preparation. In order to compare the difference of percutaneous penetration between SHTs and SHLs, the SH concentration in blood and skin dialysate at different time points of SHTs and SHLs was simultaneously detected by double-site microdialysis technology combined with UPLC-MS, and drug-time curves were drawn. The pharmacokinetic parameters of SH in skin or blood were obtained by DAS3.1 and statistical moment methods. The recovery rate of probes in vitro and in vivo was investigated, and the transdermal pharmacokinetics of transfersomes and liposomes were compared. Results Skin pharmacokinetic data showed that Css of SHTs was (1401.87 ± 464.07) ng?mL-1, and AUC0-t was（817476.04±289135.62）ng?mL-1?min-1, which were about 8.8 and 8.0 times that of SHLs, respectively. Moreover, the MRT0-t of SHTs was relatively short. Blood pharmacokinetic data showed that the Css of SHTs was（45.76±19.42）ng?mL-1, and the AUC0-t was （21172.99±2009.38）ng?mL-1?min-1, which were about 3.7 times and 2.9 times that of SHLs, respectively. Conclusion Compared with liposome, transfersomes has a good promoting effect on the permeability of SH and can serve as an effective carrier for promoting the transdermal absorption of SH. |
| 查看全文 查看/发表评论 下载PDF阅读器 |
| 关闭 |
|
|
|
