Preparation, Characterization and in Vitro and in Vivo Absorption Characteristics of Daidzein Nanosuspension Capsules

Xiao-ming YANG; Zun HUANG; Jun ZHANG; Tian-tian ZUO; Qi SHEN

doi:10.13422/j.cnki.syfjx.20182301

您当前的位置：

首页 >

文章列表页 >

Preparation, Characterization and in Vitro and in Vivo Absorption Characteristics of Daidzein Nanosuspension Capsules

Pharmacy and Processing | 更新时间：2021-02-09

- Preparation, Characterization and in Vitro and in Vivo Absorption Characteristics of Daidzein Nanosuspension Capsules
- Chinese Journal of Experimental Traditional Medical Formulae Vol. 25, Issue 2, Pages: 40-47(2019)
- 作者机构：
  
  上海交通大学　药学院，上海　 200240
- 作者简介：
- 基金信息：
- DOI：10.13422/j.cnki.syfjx.20182301
  CLC： R22; O433; R285.5; R283.6; R94
- Received：17 May 2018，
  
  Published Online：13 September 2018，
  
  Published：20 January 2019
- 稿件说明：
移动端阅览
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：

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

references

王艳梅，吕立勋．黄豆苷元的药理作用及临床应用 [J]. 中国药师， 2007 , 10 ( 9 ): 910 - 912 .

姜铁夫，康万军，杜妙，等．葛根黄豆苷元衍生物的合成及理化性质研究 [J]. 解放军药学学报， 2006 , 22 ( 3 ): 228 - 230 .

王廉卿，戎欣玉，刘魁，等．纳米药物晶体的制备技术及其应用 [J]. 河北科技大学学报， 2014 , 35 ( 4 ): 339 - 348 .

M?schwitzer J P . Drug nanocrystals in the commercial pharmaceutical development process [J]. Int J Pharm , 2013 , 453 ( 1 ): 142 - 156 .

国家药典委员会．中华人民共和国药典．四部 [M]. 北京：中国医药科技出版社， 2015 ： 59 - 61 .

Kayser O , Olbrich C , Yardley V , et al . Formulation of amphotericin B as nanosuspension for oral administration [J]. Int J Pharm , 2003 , 254 ( 1 ): 73 - 75 .

Jacobs C , Müller R H. Production and characterization of a budesonide nanosuspension for pulmonary administration [J]. Pharm Res , 2002 , 19 ( 2 ): 189 - 194 .

GAO Y , LI Z , SUN M , et al . Preparation，characterization，pharmacokinetics，and tissue distribution of curcumin nanosuspension with TPGS as stabilizer [J]. Drug Dev Ind Pharm , 2010 , 36 ( 10 ): 1225 - 1234 .

Verma S , Huey B D , Burgess D J. Scanning probe microscopy method for nanosuspension stabilizer selection [J]. Langmuir , 2009 , 25 ( 21 ): 12481 - 12487 .

吴超群，李小芳，牟倩倩，等．甘草总黄酮纳米混悬剂冻干粉的表征及稳定性考察 [J]. 中国实验方剂学杂志， 2018 , 24 ( 2 ): 29 - 33 .

许海舰，刘一鑫，刘喜纲，等．黄芩苷镁盐和黄芩苷的肠吸收动力学和药代动力学比较 [J]. 中国实验方剂学杂志， 2018 , 24 ( 4 ): 78 - 83 .

Hecq J , Deleers M , Fanara D , et al . Preparation and in vitro/in vivo evaluation of nano-sized crystals for dissolution rate enhancement of ucb-35440-3，a highly dosed poorly water-soluble weak base [J]. Eur J Pharm Biopharm , 2006 , 64 ( 3 ): 360 - 368 .

MOU D , CHEN H , WAN J , et al . Potent dried drug nanosuspensions for oral bioavailability enhancement of poorly soluble drugs with pH-dependent solubility [J]. Int J Pharm , 2011 , 413 ( 1/2 ): 237 - 244 .

Lenhardt T , Vergnault G , Grenier P , et al . Evaluation of nanosuspensions for absorption enhancement of poorly soluble drugs：in vitro transport studies across intestinal epithelial monolayers [J]. AAPS J , 2008 , 10 ( 3 ): 435 - 438 .

GAO Y , WANG C , SUN M , et al . In vivo evaluation of curcumin loaded nanosuspensions by oral administration [J]. J Biomed Nanotechnol , 2012 , 8 ( 4 ): 659 - 668 .

Kawabata Y , Wada K , Nakatani M , et al . Formulation design for poorly water-soluble drugs based on biopharmaceutics classification system：basic approaches and practical applications [J]. Int J Pharm , 2011 , 420 ( 1 ): 1 - 10 .

Mane V , Muro S. Biodistribution and endocytosis of ICAM-1-targeting antibodies versus nanocarriers in the gastrointestinal tract in mice [J]. Int J Nanomed , 2012 , 7 : 4223 - 4237 .

Blanchfield J T , Gallagher O P , Cros C , et al . Oral absorption and in vivo biodistribution of alpha-conotoxin MII and a lipidic analogue [J]. Biochem Biophys Res Commun , 2007 , 361 ( 1 ): 97 - 102 .

Bhavsar M D , Amiji M M. Gastrointestinal distribution and in vivo gene transfection studies with nanoparticles-in-microsphere oral system(NiMOS) [J]. J Control Release , 2007 , 119 ( 3 ): 339 - 348 .

Kimura T , Higaki K. Gastrointestinal transit and drug absorption [J]. Biol Pharm Bull , 2002 , 25 ( 2 ): 149 - 164 .

Shingaki T , Takashima T , Wada Y , et al . Imaging of gastrointestinal absorption and biodistribution of an orally administered probe using positron emission tomography in humans [J]. Clin Pharmacol Ther , 2012 , 91 ( 4 ): 653 - 659 .

Ponchel G , Montisci M J , Dembri A , et al . Mucoadhesion of colloidal particulate systems in the gastro-intestinal tract [J]. Eur J Pharm Biopharm , 1997 , 44 ( 1 ): 25 - 31 .

ZHANG J Y , SHEN Z G , ZHONG J , et al . Preparation of amorphous cefuroxime axetil nanoparticles by controlled nanoprecipitation method without surfactants [J]. Int J Pharm , 2006 , 323 ( 1/2 ): 153 - 160 .

Views

下载量

CSCD

Alert me when the article has been cited

提交

Tools

Publicity Resources

In vivo Pharmacokinetic Analysis of Shenbai Nanosuspension in Rats Based on Overall Composition of Chinese Materia Medica

Infulence of Aidi Injection on Pharmacokinetics of Ifosfamide in Rabbit

Pharmacokinetics of ZhiBing In-Situ Gel in Rabbits

Pharmacokinetic and Tissue Distribution of 3-Keto-dehydrosulfurenic from in Rats

Related Author

LIU Weiting

JIAN Fengjiao

HUANG Kexin

LI Xiaodong

ZHANG Wei-wei

LIANG Ning-sheng

ZHOU Chang-hong

WANG Xin-xin

Related Institution

School of Pharmacy，Fujian University of Traditional Chinese Medicine

School of Life Sciences，Beijing University of Chinese Medicine

School of Pharmacy，Shanghai University of Traditional Chinese Medicine

School of Chinese Materia Medica，Shanghai University of Traditional Chinese Medicine

School of Pharmacy，Soochow University

AI问答

Postal code：100700
Tel：010-84076882 Email：syfjx_2010@188.com
Technical support is provided by Beijing Founder electronics co., LTD 京ICP备11006657号-10 京公网安备11010802024621
It is recommended to read the content of this site in Chrome&IE9+. Please switch to extreme mode in browser 360.
Cookies We use cookies to help provide and enhance our service and tailor content. By continuing, you agree to the use of cookies.

⁰