Physicochemical characterization of cyclovirobuxine D hydroxypropyl-β-cyclodextrin and its oral bioavailability in rats

Chen Jing; Zhang Jingqing; Zhao Hua; Wang Hong; Sun Quan; Yuan Yuming; Jiang Xinhui

doi:10.13406/j.cnki.cyxb.000948

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Physicochemical characterization of cyclovirobuxine D hydroxypropyl-β-cyclodextrin and its oral bioavailability in rats

更新时间：2024-01-17

- Physicochemical characterization of cyclovirobuxine D hydroxypropyl-β-cyclodextrin and its oral bioavailability in rats
- Journal of Chongqing Medical University Vol. 42, Issue 2, Pages: 200-204(2017)
- 作者机构：
  
  1. 重庆医科大学药学院高校药物工程研究中心
  2. 重庆市中医院药剂科
- 作者简介：
- 基金信息：
- DOI：10.13406/j.cnki.cyxb.000948
  CLC： R965
- Published：2017，
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Chen Jing, Zhang Jingqing, Zhao Hua, et al. Physicochemical characterization of cyclovirobuxine D hydroxypropyl-β-cyclodextrin and its oral bioavailability in rats. [J]. Journal of Chongqing Medical University 42(2):200-204(2017)
DOI：

Chen Jing, Zhang Jingqing, Zhao Hua, et al. Physicochemical characterization of cyclovirobuxine D hydroxypropyl-β-cyclodextrin and its oral bioavailability in rats. [J]. Journal of Chongqing Medical University 42(2):200-204(2017) DOI： 10.13406/j.cnki.cyxb.000948.

摘要

目的:本研究对制备的环维黄杨星D羟丙基-β-环糊精包合物（D hydroxypropyl-β-cyclodextrin complex

CBHD）理化性质进行表征

并考察其在大鼠体内的药动学特征。方法:采用红外光谱法、差示扫描量热法对CBHD物进行表征。大鼠灌胃给予CBHD和环维黄杨星D（CB）混悬液后

于不同时间点大鼠眼底静脉丛取血。采用HPLC/FLD测定血浆中CB的浓度。结果:CBHD的理化性质与CB和物理混合物明显不同

差示扫描量热法测定结果显示形成包合物后一种新物相峰出现;CBHD和CB的主要药动学参数如下:Cmax为（76.83±6.73）μg/L和（69.27±8.66）μg/L;Tmax为（6.00±0.00）h和（4.33±0.00）h;AUC0

为（1 541.04±178.61）μg/（L·h）和（619.93±75.67）μg/（L·h）。结论:CBHD的相对生物利用度为248.58%

CBHD明显提高了CB在大鼠体内的生物利用度。

Abstract

Objective:To characterize the physicochemical properties of cyclovirobuxine D hydroxypropyl-β-cyclodextrin complex（CBHD）and to explore its pharmacokinetic features in rats. Methods:CBHD were characterized by infrared spectroscopy and differential scanning calorimetry. Blood was collected from retinal venous plexus of SD rats after oral administration of CBHD and CB

and the blood concentration was determined by HPLC/FLD. Results:CBHD showed different physicochemical propertie;a new substance peak was shown in the DSC analysis of CBHD. The pharmacokinetic parameters of CBHD and CB were calculated as follows:Cmax（76.83±6.73）μg/L and（69.27±8.66）μg/L

Tmax（6.00±0.00）h and（4.33±0.00）h

AUC0

（1 541.04±178.61）μg/（L·h）and（619.93±75.67） μg/（L·h）. Conclusion:The relative bioavailability of CBHD is 248.58%. CBHD significantly increases the bioavailability of CB in rats.

关键词

环维黄杨星D羟丙基-β-环糊精包合物表征生物利用度

Keywords

cyclovirobuxine Dhydroxypropyl-β-cyclodextrincomplexcharacterizationbioavailability

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