黄豆苷元纳米混悬剂胶囊的制备、表征及其体内外吸收特性考察

杨晓茗; 黄尊; 张君; 左甜甜; 沈琦

doi:10.13422/j.cnki.syfjx.20182301

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黄豆苷元纳米混悬剂胶囊的制备、表征及其体内外吸收特性考察

药剂与炮制 | 更新时间：2021-02-09

- 黄豆苷元纳米混悬剂胶囊的制备、表征及其体内外吸收特性考察
- Preparation, Characterization and in Vitro and in Vivo Absorption Characteristics of Daidzein Nanosuspension Capsules
- 中国实验方剂学杂志 2019年25卷第2期页码：40-47
- 作者机构：
  
  上海交通大学　药学院，上海　 200240
- 作者简介：
  
  杨晓茗，在读硕士，从事纳米制剂研究，E-mail：miny@sjtu.edu.cng
  *沈琦，博士，教授，从事纳米制剂研究，Tel：021-34204049，E-mail：qshen@sjtu.edu.cn
- 基金信息：
- DOI：10.13422/j.cnki.syfjx.20182301
  中图分类号： R22; O433; R285.5; R283.6; R94
- 收稿日期：2018-05-17，
  
  网络出版日期：2018-09-13，
  
  纸质出版日期：2019-01-20
- 稿件说明：
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杨晓茗, 黄尊, 张君, 等. 黄豆苷元纳米混悬剂胶囊的制备、表征及其体内外吸收特性考察[J]. 中国实验方剂学杂志, 2019,25(2):40-47.

Xiao-ming YANG, Zun HUANG, Jun ZHANG, et al. Preparation, Characterization and in Vitro and in Vivo Absorption Characteristics of Daidzein Nanosuspension Capsules[J]. Chinese journal of experimental traditional medical formulae, 2019, 25(2): 40-47.
杨晓茗, 黄尊, 张君, 等. 黄豆苷元纳米混悬剂胶囊的制备、表征及其体内外吸收特性考察[J]. 中国实验方剂学杂志, 2019,25(2):40-47. DOI： 10.13422/j.cnki.syfjx.20182301.

Xiao-ming YANG, Zun HUANG, Jun ZHANG, et al. Preparation, Characterization and in Vitro and in Vivo Absorption Characteristics of Daidzein Nanosuspension Capsules[J]. Chinese journal of experimental traditional medical formulae, 2019, 25(2): 40-47. DOI： 10.13422/j.cnki.syfjx.20182301.

摘要

目的：

制备黄豆苷元纳米混悬剂胶囊，以市售黄豆苷元胶囊为参考，考察两者对小肠吸收与口服生物利用度的影响。

方法：

采用沉淀法联用高压均质技术制备黄豆苷元纳米混悬剂，通过正交试验优化其处方，利用X射线粉末衍射分析(XRPD)，傅里叶红外光谱(FT-IR)，透射电子显微镜(TEM)以及粒径，多分散指数和Zeta电位等指标对黄豆苷元纳米混悬剂进行表征。采用外翻肠囊法研究自制制剂与市售黄豆苷元胶囊的体外肠吸收情况，考察了黄豆苷元纳米混悬剂在体内胃肠道的分布，并通过HPLC测定大鼠体内黄豆苷元的血药浓度，以考察口服给药后的生物利用度。

结果：

以市售黄豆苷元胶囊内容物为参比制剂，自制黄豆苷元纳米混悬剂胶囊的小肠吸收促进率2.49(

0.01)，胃肠道生物分布评价证实了纳米混悬液的生物黏附性，相对生物利用度294%。

结论：

沉淀法联用高压均质技术制备的黄豆苷元纳米混悬剂冻干后可用于胶囊剂等剂型的生产，有益于增加药物的小肠吸收并改善口服以后的体内生物利用度。

Abstract

Objective:

To prepare daidzein nanosuspension capsules

and to investigate intestinal absorption and oral bioavailability by comparing with commercial daidzein capsules.

Method:

Daidzein nanosuspensions were prepared by precipitation method combined with high pressure homogenization

orthogonal design method was utilized to optimize its formulation.Daidzein nanosuspensions was characterized by X-ray powder diffraction(XRPD)

Fourier transform infrared spectroscopy(FT-IR)

transmission electron microscope(TEM)

and indexes including mean particle size

polydispersity index(PDI)

and Zeta potential.Intestinal absorption study was carried out to compare the accumulative permeated amount of daidzein from daidzein nanosuspensions and commercial daidzein capsules.Biodistribution of daidzein in gastrointestinal tract was investigated

and oral bioavailability was examined through pharmacokinetic study by HPLC.

Result:

The

in vitro

small intestinal absorption enhancement ratio of daidzein nanosuspension capsules was approximately 2.49-fold higher than that of commercial capsules(

0.01). Biodistribution evaluation in gastrointestinal tract verified the bioadhesion of the nanosuspensions.Pharmacokinetic study calculated by DAS 2.0 revealed that the relative bioavailability of daidzein nanosuspension capsules was 294%.

Conclusion:

Daidzein nanosuspensions prepared by combined method can be applied to the production of capsules

which is beneficial to increase the absorption of drug in small intestine and improve its bioavailability after oral administration.

关键词

Keywords

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