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Preparation and pharmacokinetics in beagle dogs of ganershu sustained-release pellets

Authors :
Ye-Xia Zhang
Ting Zhang
Xin Jin
Guo-jun Yan
Shao-bo Ge
Jian-Chun Wang
Jinhuo Pan
Zhitao Jiang
Source :
Pharmacognosy Magazine
Publication Year :
2014
Publisher :
Medknow Publications & Media Pvt Ltd, 2014.

Abstract

Background: The active ingredients of Ganershu compound recipe, which are effective for hepatitis treatment in liver protection and transaminase reduction. However, the active ingredients of Ganershu compound recipe are poor absorption, which conduct it has a low oral bioavailability. Objective: We prepared Ganershu sustained-release pellets (GSPs) by fluidized-bed on central composite design-response surface methodology and increase its bioavailability in beagle dogs. Materials and Methods: In this study, GSPs were successfully prepared. The Drug-loaded pellets and sustained-release coated were carried out in fluidized-bed machine. GSP was optimized for fitting release, roundness, and the overall desirability by central composite design-response surface methodology. Results: To optimize cumulative release profile, the outermost ethyl cellulose coating layer and the hydroxypropyl methyl cellulose (HPMC) swelling layer were employed, which were respectively given coating levels in terms of weight gain of 22% and 6%, the concentration of HPMC is 4.5% (g/ml). The pharmacokinetics of Ganershu normal pellets (GNPs) and GSP was studied in beagle dogs after oral administration. The naringenin as an index, the area under the curve 0-∞ of naringenin in GSP was 1.38 times greater than that of GNP. Meanwhile, T max of GSP was prolonged for about 74%. Conclusion: This study can clearly indicate that we enhanced the oral bioavailability of Ganershu by preparing the GSP, which had the sustained dissolution and improved the potential of it for clinical application.

Details

Language :
English
ISSN :
09764062 and 09731296
Volume :
10
Issue :
39
Database :
OpenAIRE
Journal :
Pharmacognosy Magazine
Accession number :
edsair.doi.dedup.....5dd9cefd65b4c9418f4f8800c161cec6