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冬凌草甲素自微乳化药物传递系统的体外释放动力学

[Release kinetics of oridonin self-microemulsifying drug delivery system in vitro].

作者信息

Liu Ying, Zhang Ping, Feng Nian-Ping, Zhang Xin, Xu Jie

机构信息

Department of Pharmaceutics, Shanghai University of Traditional Chinese Medicine, Shanghai 201203, China.

出版信息

Zhongguo Zhong Yao Za Zhi. 2008 Sep;33(18):2049-52.

Abstract

OBJECTIVE

To investigate the release characteristics and mechanism of oridnonin self-microemulsifying drug delivery system (SMEDDS) in vitro.

METHOD

The concentration of oridonin was determined by HPLC. In vitro release studies were conducted by reverse dialysis technique. The effects of release medium, agitation rate and preparations on the oridonin release were studied. The similarity factor (f2) was applied to the release profile comparisons. Model fitting was used to determine the kinetics and mechanism.

RESULT

The release media and agitation rate from 50-100 r x min(-1) had no distinctive effect on the oridonin release kinetics, which the similarity factors were greater than 50. The oridonin release profiles for oridonin SMEDDS and oridonin ethanol solution were similar. 65% of oridonin were released in 30 min for oridonin SMEDDS in pH 7.8 PBS. Oridonin SMEDDS fit the Hixson-Crowell model best.

CONCLUSION

The release data from oridonin SMEDDS showed it release fast. The deduced release mechanism is that the surface and particle sizes of self-microemulsion in water solution are changing during the process of release and the drug penetration through membrane is a passive diffusion process.

摘要

目的

考察冬凌草甲素自微乳化给药系统(SMEDDS)的体外释放特性及机制。

方法

采用高效液相色谱法测定冬凌草甲素的浓度。采用反向透析技术进行体外释放研究。考察释放介质、搅拌速度和制剂对冬凌草甲素释放的影响。应用相似因子(f2)对释放曲线进行比较。采用模型拟合确定动力学和机制。

结果

释放介质和50 - 100 r·min⁻¹的搅拌速度对冬凌草甲素释放动力学无显著影响,相似因子大于50。冬凌草甲素SMEDDS和冬凌草甲素乙醇溶液的释放曲线相似。在pH 7.8的磷酸盐缓冲液中,冬凌草甲素SMEDDS在30分钟内释放了65%的冬凌草甲素。冬凌草甲素SMEDDS最符合Hixson - Crowell模型。

结论

冬凌草甲素SMEDDS的释放数据表明其释放迅速。推测的释放机制是,自微乳剂在水溶液中的表面和粒径在释放过程中发生变化,药物透过膜的过程是一个被动扩散过程。

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