| 引用本文: | 刘晨,王文苹.双载药缓释颗粒的处方优化与制剂评价[J].中国现代应用药学,2024,41(13):51-59. |
| Liu Chen,Wang Wen Ping.Formulation Optimization and Preparation Evaluation on Sustained-release Particles of Dual Drugs[J].Chin J Mod Appl Pharm(中国现代应用药学),2024,41(13):51-59. |
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| 摘要: |
| 目的 优化载苦参碱(matrine,MAT)和丹皮酚(paeonol,PAE)缓释颗粒(sustained-release particles,SRPs)中缓释材料的配方,并初步评价制剂质量。方法 采用挤出-滚圆法制备缓释颗粒。以MAT和PAE体外累积释放率为考察指标,对主要缓释材料及用量、辅助缓释材料、混合缓释材料总量与比例进行单因素考察；结合星点设计-效应面法优化缓释材料处方,考察缓释材料乙基纤维素(EC)与壳聚糖(CS)的总量及其质量比对MAT和PAE的累积释放率及释放同步性的影响。从MAT-PAE- SRPs的制剂特性、体外释放度以及初步稳定性实验等方面进行评价,并进行释药过程动力学方程拟合。结果 优化的缓释材料处方为23.5% EC和17.1% CS；MAT-PAE- SRPs的成型率、休止角、堆密度、脆碎度分别为97.23 %、38.1°、0.74 gmL-1、0.74 %。该制剂在不同介质中均体现出一定的缓释特性、在酸性介质中释放较快,12h累积释放度均超过90 %。MAT的释放曲线呈现First-order释药特性,PAE的释药特性符合Higuchi释放；SRPs提高了MAT、PAE的药物稳定性。 结论 缓释材料EC与CS制备的MAT-PAE- SRPs缓释效果明显,MAT和PAE累积释放率与释放同步性良好,可为双载药缓释制剂研究提供参考。 |
| 关键词: 苦参碱 丹皮酚 星点设计-效应面法 缓释颗粒 体外释放 |
| DOI：10.13748/j.cnki.issn1007-7693.20233293 |
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| Formulation Optimization and Preparation Evaluation on Sustained-release Particles of Dual Drugs |
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Liu Chen1, Wang Wen Ping2
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1.宁夏医科大学总医院;2.College of Chinese Materia Medica, Yunnan University of Chinese/Ningxia Medical University Medicine/
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| Abstract: |
| ABSTRACT: OBJECTIVE To optimize the formulation for sustained-release particles of matrine and paeonol and to primarily evaluate their quality. METHODS The sustained-release particles were fabricated by the extrusion-spheronization method. The type, ratio and total amount of matrix materials in formulation were screened by single factor experiments using in vitro drug release as the index. Furthermore, the central composition design- response surface methodology was adopted for optimize the ratio of EC and CS according to their influences on accumulative drug release and the synchronized profiles. The obtained particles were evaluated on their particle characteristics, in vitro drug release and stability properties. Also, the release data were fitted for various kinetic equations. RESULTS The optimized formulation contained 23.5% EC and 17.2% CS as sustained-release materials. The yield, repose angle, bulk density and friability of final Particles are 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 over 90 % at 12 h. The release profile of matrine 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 As a good reference for development of dual drug-loaded sustaine/controlled-release oral preparations, MAT-PAE-SRPs showed a preferable sustained-release pattern with acceptable release rate and synchronism. |
| Key words: matrine paeonol central composite design-response surface method sustained-release particles in vitro release |
