白藜芦醇膜剂的制备及大鼠体内药动学研究  

Preparation of resveratrol oral film and it′s in vivo pharmacokinetic in rats

作　　者：马俊媛 温梦 马佳 田蕾[3] 王绍宁[1] 徐晖[3] MA Junyuan;WEN Meng;MA Jia;TIAN Lei;WANG Shaoning;XU Hui(School of Pharmaceutical Engineering,Shenyang Pharmaceutical University,Shenyang 110016,China;School of Pharmacy,Jinzhou Medical University,Jinzhou 121001,China;School of Pharmacy,Shenyang Pharmaceutical University,Shenyang 110016,China)

机构地区：[1]沈阳药科大学制药工程学院,辽宁沈阳110016 [2]锦州医科大学药学院,辽宁锦州121001 [3]沈阳药科大学药学院,辽宁沈阳110016

出　　处：《沈阳药科大学学报》2021年第2期107-114,共8页Journal of Shenyang Pharmaceutical University

摘　　要：目的以水溶性的高分子材料为载体,制备白藜芦醇载药膜剂,改善BCS II类药物白藜芦醇的溶解度、释放速率及生物利用度。方法采用溶液流延法制备白藜芦醇载药膜剂,分别采用光学显微镜法和扫描电子显微镜法对膜剂外观进行观察;傅里叶变换红外光谱法、X-射线粉末衍射法对载药膜剂进行表征;在纯水、模拟胃液和模拟肠液中,考察白藜芦醇药物释放行为;同时以白藜芦醇原料药混悬液为对照进行大鼠体内药动学研究。结果白藜芦醇膜剂表面光滑平整,傅里叶变换红外光谱法及X-射线粉末衍射法显示,白藜芦醇在膜剂内以分子或无定形形式存在;膜剂中白藜芦醇的释放不受介质种类的影响,释放速率及累计释放量远高于白藜芦醇原料药;大鼠体内药动学研究结果显示,膜剂显著提高白藜芦醇吸收速率。结论膜剂相较于原料药,体外释放速率,累积释放量,体内吸收速率方面均显著提高。Objective The resveratrol film was prepared by using the water-soluble polymer material polyvinylpyrrolidone K30 as a carrier to improve the solubility,dissolution rate and bioavailability of BCS II drug resveratrol.Methods The resveratrol films were prepared by solution casting method.The characterization of film were carried out by optical microscopy,scanning electron microscopy,Fourier transform infrared spectroscopy,and X ray powder diffraction.The in vitro drug release behavior of resveratrol was investigated in purified water,simulated gastric fluid,and simulated intestinal fluid;Meanwhile,pharmacokinetic studies in rats were performed using resveratrol suspension as control group.Results The surface of the resveratrol film is smooth and flat.Fourier transform infrared spectroscopy and X-ray powder diffraction showed that resveratrol in the film exists in a molecular or amorphous form;The in vitro dissolution of resveratrol in the film is not affected by the type of medium,and the dissolution rate and cumulative release amount are much higher than the resveratrol raw drug;The pharmacokinetic study in rats showed that the cmax of the film group was much higher than that of the raw drug.Conclusion Compared with the pure drug,the film has a significant increase in both in vitro dissolution rate and in vivo absorption rate.

关 键 词：白藜芦醇 膜剂 体外释放 药动学 

分 类 号：R94[医药卫生—药剂学]