UM  > 中華醫藥研究院
Blends of hydrophobic and swelling agents in the swelling layer in the preparation of delayed-release pellets of a hydrophilic drug with low MW: Physicochemical characterizations and in-vivo evaluations
You C.1,2; Liang X.1; Sun J.1,3; Sun L.1; Wang Y.1; Fan T.4; Zheng Y.1
2014
Source PublicationAsian Journal of Pharmaceutical Sciences
Volume9Issue:4Pages:199
Abstract

In this study, a hydrophobic material, ethylcellulose, which was used as its aqueous suspension Surelease®, was combined with a swelling agent as the swelling layer to prepare delayed-release pellets for Danshensu, which is a hydrophilic drug with low MW. A rupturable, delayed-release pellet consists of a drug core, a swelling layer containing a swelling agent (cross-linked sodium carboxymethyl cellulose) with a hydrophobic agent (Surelease®), and a controlled layer composed by an insoluble, water-permeable polymeric coating (aqueous ethylcellulose dispersions) was developed in a fluidised bed. Results showed that blending Surelease® into the swelling layer could effectively extend the release of Danshensu from the pellets, which may be attributed to the slowed swelling rate by reduction of water penetration and improvement of mechanical integrity of the swelling layer. Drug in the delayed pellets showed sustained release in beagle dogs after oral administration with comparable in-vivo exposure to the uncoated drug pellets. In conclusion, blends of hydrophobic and swelling agents in the swelling layer in double-membrane pellets could achieve a delayed drug-release profile in vitro, as well as delayed and sustained absorption in vivo for highly soluble, low-MW drug. The present study highlighted the potential use of a delayed-release system for other hydrophilic, low-MW drugs to meet the formulation requirements for chronopharmacological diseases. © 2014 Shenyang Pharmaceutical University.

KeywordCross-linked Sodium Carboxymethyl Cellulose (Cc-na) Danshensu Delayed-release Pellets Fluidised Bed Surelease® Swelling Agent
DOI10.1016/j.ajps.2014.06.003
URLView the original
Language英语
The Source to ArticleScopus
Fulltext Access
Citation statistics
Document TypeJournal article
CollectionInstitute of Chinese Medical Sciences
Affiliation1.State Key Laboratory of Quality Research in Chinese Medicine, Institute of Chinese Medical Sciences, University of Macau, Macau
2.Beijing Institute for Drug Control, Beijing, China
3.National Institute for Food and Drug Control, Beijing, China
4.Department of Pharmaceutics, School of Pharmaceutical Sciences, Peking University, Beijing, China
First Author AffilicationInstitute of Chinese Medical Sciences
Recommended Citation
GB/T 7714
You C.,Liang X.,Sun J.,et al. Blends of hydrophobic and swelling agents in the swelling layer in the preparation of delayed-release pellets of a hydrophilic drug with low MW: Physicochemical characterizations and in-vivo evaluations[J]. Asian Journal of Pharmaceutical Sciences,2014,9(4):199.
APA You C..,Liang X..,Sun J..,Sun L..,Wang Y..,...&Zheng Y..(2014).Blends of hydrophobic and swelling agents in the swelling layer in the preparation of delayed-release pellets of a hydrophilic drug with low MW: Physicochemical characterizations and in-vivo evaluations.Asian Journal of Pharmaceutical Sciences,9(4),199.
MLA You C.,et al."Blends of hydrophobic and swelling agents in the swelling layer in the preparation of delayed-release pellets of a hydrophilic drug with low MW: Physicochemical characterizations and in-vivo evaluations".Asian Journal of Pharmaceutical Sciences 9.4(2014):199.
Files in This Item:
There are no files associated with this item.
Related Services
Recommend this item
Bookmark
Usage statistics
Export to Endnote
Google Scholar
Similar articles in Google Scholar
[You C.]'s Articles
[Liang X.]'s Articles
[Sun J.]'s Articles
Baidu academic
Similar articles in Baidu academic
[You C.]'s Articles
[Liang X.]'s Articles
[Sun J.]'s Articles
Bing Scholar
Similar articles in Bing Scholar
[You C.]'s Articles
[Liang X.]'s Articles
[Sun J.]'s Articles
Terms of Use
No data!
Social Bookmark/Share
All comments (0)
No comment.
 

Items in the repository are protected by copyright, with all rights reserved, unless otherwise indicated.