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目的研制山楂叶总黄酮缓释胶囊,并考察其释药机制。方法采用喷雾干燥法制备山楂叶总黄酮缓释固体分散体,以乙基纤维素等为载体,以2,6,12 h的释放度为指标,筛选最佳缓释固体分散体处方;采用X-射线衍射、扫描电镜和红外光谱法考察固体分散体中药物分散状态;拟合川北方程,以粉体流动性参数为指标,筛选缓释胶囊的处方辅料,制备山楂叶总黄酮缓释固体分散体胶囊,考察缓释胶囊释药机制,拟合释放动力学方程。结果山楂叶总黄酮缓释固体分散体最佳处方组成为山楂叶总黄酮∶乙基纤维素∶卡波姆940P=4∶1∶0.5;X-射线衍射和扫描电镜结果表明,药物以无定形或分子形式分散于固体分散体中;红外光谱法结果表明,乙基纤维素峰强度增强;缓释胶囊最佳处方组成为固体分散体∶微粉硅胶=1∶0.3%,所制备缓释胶囊释放度2,6,12 h分别为27.56%,69.50%和96.78%。结论该缓释胶囊在12 h内呈现良好缓释特征,释放行为符合一级动力学方程,释放机制为扩散和溶蚀相结合机制,且为降解控释型。
Objective To develop hawthorn leaves flavonoids sustained release capsules, and investigate the mechanism of drug release. Methods The sustained-release solid dispersions of hawthorn leaves flavonoids were prepared by spray-drying method. The optimal sustained-release solid dispersions prescriptions were screened with release rate of 2,6,12 h using ethyl cellulose as carrier, Ray diffraction, scanning electron microscopy and infrared spectroscopy to investigate the disperse state of the drug in the solid dispersion; fitting the equation of the north of Sichuan province, screening the formulation excipients of the sustained-release capsule with the powder fluidity parameter as the index, Capsule, investigate release mechanism of sustained release capsules, fitting release kinetic equation. Results hawthorn leaf flavonoids sustained-release solid dispersion of the best prescription for hawthorn leaf flavonoids: ethyl cellulose: Carbopol 940P = 4: 1: 0.5; X-ray diffraction and scanning electron microscopy results show that the drug amorphous Or molecular form dispersed in the solid dispersion; infrared spectroscopy results show that the ethyl cellulose peak intensity enhancement; sustained-release capsules the best prescription for the composition of the solid dispersion: silica powder = 1:0.3%, the release of the sustained-release capsules prepared The degrees of 2, 6 and 12 h were 27.56%, 69.50% and 96.78% respectively. Conclusion The sustained-release capsules showed good sustained-release characteristics within 12 h. The release behavior accorded with the first-order kinetic equation. The release mechanism was a combination of diffusion and dissolution, and it was a controlled-release model.