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水飞蓟素前体脂质体的制备及其在大鼠体内的药代动力学

[Preparation of silymarin proliposomes and its pharmacokinetics in rats].

作者信息

Xiao Yan-yu, Song Yun-mei, Chen Zhi-peng, Ping Qi-neng

机构信息

Department of Pharmaceutics, China Pharmaceutical University, Nanjing 210009, China.

出版信息

Yao Xue Xue Bao. 2005 Aug;40(8):758-63.

Abstract

AIM

To study the preparation of silymarin proliposomes. To study its physicochemic properties, its pharmacokinetical characteristics and bioavailability in rats after oral administration.

METHODS

Silymarin proliposomes were prepared by film-deposition on carriers. When the proliposomes were contacted with water to form liposome suspensions, the tests of physicochemical properties including encapsulation efficiency, particle size and stability of the formed liposome suspensions were determined by HPLC, laser-particle-sizer and etc. The concentrations of non-conjugated and overall silymarin in plasma of rats and their pharmacokinetic behaviors after oral administration were studied by RP-HPLC. The pharmacokinetic parameters were computed by software program 3P97.

RESULTS

The encapsulation efficiency of silymarin liposomes could be more than 90%, with an average particle size of about 238.8 nm and a very good stability. The high bioavailability of silymarin proliposomes could be gotten by oral administration.

CONCLUSION

Compared with silymarin, silymarin proliposome is a stable and easily industrialized preparation and did enchance the gastrointestinal absorption of silymarin.

摘要

目的

研究水飞蓟素前体脂质体的制备方法。研究其理化性质、药代动力学特征以及大鼠口服给药后的生物利用度。

方法

采用薄膜载体沉积法制备水飞蓟素前体脂质体。当该前体脂质体与水接触形成脂质体混悬液后,采用高效液相色谱法(HPLC)、激光粒度分析仪等对所形成脂质体混悬液的包封率、粒径及稳定性等理化性质进行测定。采用反相高效液相色谱法(RP-HPLC)研究大鼠口服给药后血浆中游离水飞蓟素及总水飞蓟素的浓度及其药代动力学行为。通过3P97软件程序计算药代动力学参数。

结果

水飞蓟素脂质体包封率可达90%以上,平均粒径约为238.8 nm,稳定性良好。口服水飞蓟素前体脂质体可获得较高的生物利用度。

结论

与水飞蓟素相比,水飞蓟素前体脂质体是一种稳定且易于工业化生产的制剂,确实提高了水飞蓟素的胃肠道吸收。

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