槲皮素微乳剂的处方优化及其在大鼠肠道中的原位吸收
Formulation optimization and in situ absorption in rat intestinal tract of quercetin-loaded microemulsion.
作者信息
Gao Yan, Wang Yuqiang, Ma Yukun, Yu Aihua, Cai Fengqun, Shao Wei, Zhai Guangxi
机构信息
Department of Pharmaceutics, College of Pharmacy, Shandong University, 44 Wenhua Xilu, Jinan 250012, China.
出版信息
Colloids Surf B Biointerfaces. 2009 Jul 1;71(2):306-14. doi: 10.1016/j.colsurfb.2009.03.005. Epub 2009 Mar 24.
A new microemulsion system has been developed to increase the solubility and oral absorption of quercetin, a poorly water-soluble drug. The formulation of quercetin-loaded microemulsion was optimized by a simplex lattice experiment design. The optimized microemulsion formulation consisted of oil (7%, w/w), surfactant (48%, w/w), and cosurfactant (45%, w/w). Under this condition, the mean droplet diameter of microemulsion was 38.9 nm and solubility of quercetin in the microemulsion was 4.138 mg/ml. The in situ absorption property of quercetin-loaded microemulsion in rat intestine was studied and the results showed there was significant difference in absorption parameters such as K(a), t(1/2) and uptake percentages between microemulsion and micelle solution containing quercetin. The study on absorption percentage in different regions of rat intestine attested that the colon had the best permeability, followed by ileum, duodenum in order. It can be concluded that microemulsion can improve the solubility and oral absorption of quercetin, a poorly water-soluble drug.
已开发出一种新型微乳体系，以提高槲皮素（一种难溶于水的药物）的溶解度和口服吸收。通过单纯形格子实验设计对载槲皮素微乳的配方进行了优化。优化后的微乳配方由油（7%，w/w）、表面活性剂（48%，w/w）和助表面活性剂（45%，w/w）组成。在此条件下，微乳的平均液滴直径为38.9 nm，槲皮素在微乳中的溶解度为4.138 mg/ml。研究了载槲皮素微乳在大鼠肠道中的原位吸收特性，结果表明，微乳与含槲皮素的胶束溶液在吸收参数如K(a)、t(1/2)和摄取百分比方面存在显著差异。对大鼠肠道不同区域吸收百分比的研究证明，结肠的通透性最佳，其次是回肠、十二指肠。可以得出结论，微乳可以提高槲皮素（一种难溶于水的药物）的溶解度和口服吸收。
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