Formulation Optimization and Preparation Evaluation on Sustained-release Particles of Dual Drugs
10.13748/j.cnki.issn1007-7693.20233293
- VernacularTitle:双载药缓释颗粒的处方优化与制剂评价
- Author:
Chen LIU
1
;
Boli LI
2
;
Ya'nan WU
2
;
Wenping WANG
3
Author Information
1. General Hospital of Ningxia Medical University, Yinchuan 750000, China
2. Ningxia Medical University, Yinchuan 750000, China
3. Ningxia Medical University, Yinchuan 750000, ChinaCollege of Chinese Materia Medica, Yunnan University of Chinese Medicine, Kunming 650500, China
- Publication Type:Journal Article
- Keywords:
matrine ；paeonol ；central composite design-response surface method ；sustained-release particles；in vitro release
- From:
Chinese Journal of Modern Applied Pharmacy
2024;41(13):1735-1742
- CountryChina
- Language:Chinese
-
Abstract:
OBJECTIVE :To optimize the formulation for sustained-release particles of matrine(MAT) and paeonol(PAE) and to primarily evaluate their quality.
METHODS
The sustained-release particles were fabricated by the extrusion-spheronization method. Single factor analysis was conducted on the main sustained-release materials and their dosage, auxiliary sustained-release materials, and the total amount and proportion of mixed sustained-release materials, using the cumulative release rates of MAT and PAE in vitro as evaluation indicators. By combining central composition design-response surface methodology, the formulation of sustained-release materials was optimized, and the effects of the total amount and mass ratio of ethyl cellulose(EC) and chitosan(CS) on the cumulative release rate and release synchronization of MAT and PAE were investigated. The formulation characteristics, in vitro release, and preliminary stability tests of MAT-PAE-SRPs were evaluated, and the release process kinetic equation was fitted.
RESULTS
The optimized formulation contained 23.5% EC and 17.1% CS as sustained-release materials. The yield, repose angle, bulk density and friability of final particles were 97.23%, 38.1°, 0.74 g·mL−1 and 0.74%, respectively. The particles showed sustained release pattern in various media and released faster in acidic media with its release percentage >90% at 12 h. The release profile of MAT was fitted best with first order equation, and that of paeonol with Higuchi equation. The formation of SRPs improved the stability of both drugs.
CONCLUSION
The sustained-release effect of MAT-PAE-SRPs prepared by sustained-release materials EC and CS is significant, and the cumulative release rate and release synchronization of MAT and PAE are good, which can provide reference for the research of dual loaded sustained-release formulations.
