Enantioselective transport of R/S-propranolol in Caco-2 cell monolaysers

LONG Xiao-hong; et al

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Enantioselective transport of R/S-propranolol in Caco-2 cell monolaysers

更新时间：2024-01-17

- Enantioselective transport of R/S-propranolol in Caco-2 cell monolaysers
- Journal of Chongqing Medical University Issue 9, Pages: 1038-1041(2008)
- 作者机构：
  
  1. 重庆医科大学药学院药物分析教研室
  2. 重庆医科大学附属第一医院药剂科
- 作者简介：
- 基金信息：
- DOI：
  CLC： R969.1
- Published：2008，
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[1]龙潇鸿,邱峰,徐霞,李惠芝.药物体外转运模型及普萘洛尔异构体转运动力学研究[J].重庆医科大学学报,2008(09):1038-1041.

LONG Xiao-hong, et al. Enantioselective transport of R/S-propranolol in Caco-2 cell monolaysers. [J]. Journal of Chongqing Medical University (9):1038-1041(2008)
[1]龙潇鸿,邱峰,徐霞,李惠芝.药物体外转运模型及普萘洛尔异构体转运动力学研究[J].重庆医科大学学报,2008(09):1038-1041. DOI：

LONG Xiao-hong, et al. Enantioselective transport of R/S-propranolol in Caco-2 cell monolaysers. [J]. Journal of Chongqing Medical University (9):1038-1041(2008) DOI：

摘要

目的:用近年来最具代表性的研究口服药物吸收机制的Caco-2细胞单层模型

研究盐酸普萘洛尔异构体的吸收及其吸收机制。方法:建立Caco-2细胞单层模型

研究不同浓度不同时间点该药物异构体的转运情况

通过柱前衍生化的RP—HPLC法检测盐酸普萘洛尔的异构体。结果:盐酸普萘洛尔吸收完全

主要为被动吸收

其异构体在Caco-2细胞模型上吸收无手性选择性。结论:本文建立了Caco-2细胞模型

并进行了完整性评价

表明Caco-2细胞模型完整性良好

将其用于手性药物盐酸普萘洛尔的吸收转运实验。同时还建立了柱前衍生化的RP-HPLC法

可以在20min内分离测定盐酸普萘洛尔异构体

方法操作简便、精密度好、结果准确可靠。

Abstract

Objective:to study the absorption and absorption characteristics of isomer of propranolol hydrochloride in Caco-2cell monolayers model

which have taken as the most representative model to investigate the absorption mechanism of oral drug in recent years. Methods:Caco-2 cell monolayers model was set up to study transport of isomer of propranolol hydrochloride. RP-HPLC method was applied to analyze isomer of propranolol hydrochloride through precolumn derivatization. Results: Propranolol hydrochloride was absorbed completely

and was a passive diffusion mechanism. There was no chiral selectivity of transport and absorption of them across Caco-2 cell monolayers. Conclusion: Caco-2 cell model was established and the cell integrity was evaluated. The integrity of Caco-2 cell was in good condition

which could be used to study the absorption and transport. RP-HPLC method was established to separated isomer of propranolol hydrochloride within 20 min by precolumn derivatization. The method is convenient

sensitive

accurate and suitable for the analysis of telbivudine.

关键词

手性衍生化HPLC盐酸普萘洛尔Caco-2细胞GITC表观通透系数对映选择性

Keywords

Chiral derivatizationHPLCPropranolol hydrochlorideCaco-2 cellsGITCPappEnantioselectivityl

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