Preparation of monolithic osmotic tablet of quercetin loaded by solid dispersion

槲皮素固体分散体单层渗透泵片的研制（英文）

The objective of this study was to prepare monolithic osmotic tablet of quercetin for controlled drug release. Quercetin-PVP solid dispersion was prepared to enhance its solubility and dissolution rate. Solid dispersion, suspending agents, osmotic agents and other conventional excipients were used as tablet core composition and cellulose acetate （CA） with plasticizer as release controlling membrane. Different formulation variables, the amounts of PEO （polyethylene oxide）, NaC1, plasticizer, and coating weight gain were optimized to gain the optimum formulation. The mechanism of drug release from monolithic osmotic tablet was also discussed. The optimal monolithic osmotic pump tablet could deliver quercetin at the rate of approximate zero-order up to 12 h, and the cumulative release was 90.74%. The developed monolithic osmotic system for quercetin loaded by solid dispersion was found to be a promising approach for controlled release of poorly-water soluble drug candidates.

本文主要介绍槲皮素单层渗透泵控释片的制备方法,采用固体分散体技术提高槲皮素的溶解度和溶出速率。采用槲皮素固体分散体、助悬剂、渗透活性物质和其他辅料作为渗透泵片片芯,以添加增塑剂的醋酸纤维素作为渗透泵片的控释膜;通过优化处方中PEO用量、Na Cl用量、增塑剂用量和包衣增重得到最优处方,并探讨药物从单层渗透泵片中的释放机理。优化后的槲皮素固体分散体单层渗透泵片处方,药物释放呈零级释药特征,且12小时内释放度达到90.74%。本方法为制备其他难溶性药物控释片提供了新的策略。