姜黄素磷脂复合物的制备及药代动力学评价.docVIP

姜黄素磷脂复合物的制备及药代动力学评价 罗见春1，杨林 2，尹华峰1，赵德璋 1，张景勍1* 重庆医科大学药物高校工程研究中心，重庆400016；2. 重庆市食品药品检验，重庆401121 [摘要] 目的 通过对大鼠口服给药，评价姜黄素磷脂复合物在SD大鼠体内药物代谢动学性质。 方法 SD大鼠只，给姜黄素磷脂复合物，不同时间点于大鼠眼底静脉丛取血。采用高效液相法测定血浆中姜黄素的浓度。结果 姜黄素磷脂复合物的0.150 g·L-1、68.04 %，较姜黄素(0.057 g·L-1、50.68 %)均有所增加。药代动力学参数如下Cmax为(74.34±5.57) μg/L61.64±4.29) μg/L，Tmax 为(0.17±0) h0.25±0) h，AUC 0-t 为(637.38±30.04) μg/L*h172.41±31.66) μg/L*h，AUC 0-∞为(857.80±223.69) μg/L*h191.08±43.27) μg/L*h。精密度回收率含量测定方法结论 姜黄素磷脂复合物混悬液吸收，消除慢 [关键词] 姜黄素；姜黄素磷脂复合物；药代动力学 [中图分类号]文献标识码 The Preparation and Pharmacokinetics Evaluation of the Curcumin Phospholipid Complex LUO Jianchun1, YANG Lin2, YIN Huafeng1, ZHAO Dezhang1, ZHANG Jingqing 1* Medicine Engineering Research Center, Chongqing Medical University, Chongqing 400016, China; 2. Chongqing Institute for Food and Drug Control, Chongqing, 401121, China [Abstract] Objective To evaluate the pharmacokinetics of curcumin phospholipid complex in rat with oral administration. Methods Blood was collected from retinal venous plexus of SD rat after oral administration of curcumin phospholipid complex, and the blood concentration was determined by HPLC. Results The solubility and cumulative dissolution of CCPC were 0.150 g·L-1 and 68.04 %, which were much higher than CC (0.057 g·L-1 and 50.68 %). The pharmacokinetic parameter of CCPC and CC were calculated as follows: Cmax (74.34±5.57) μg/L and (61.64±4.29) μg/L, Tmax (0.17±0) h and (0.25±0) h, AUC0-t (637.38±30.04) μg/L*h and (172.41±31.66) μg/L*h, AUC0-∞ (857.80±223.69) μg/L*h and (191.08±43.27) μg/L*h. Intra-day and inter-day precision, recovery rate could meet with the content determination. Conclusion Curcumin phospholipid complex was absorbed faster and eliminated more slowly compared with Curcumin. [Key words] curcumin; curcumin phospholipid complex; pharmacokinetics 从中药姜黄中分离出来的总姜黄色素[1]，具有广泛的药理活性，如抗癌、抗菌、抗病毒、防氧化等。大量的动物实验和体外细胞实验也表明总姜黄素有较强的诱导肺癌细胞凋亡作用。碱性条件下易降解，对光热强酸强碱均不稳定，口服后大部分以原形排出体外(约89 % )，大剂量时胃肠道不良反应严重[3]，并且由于总姜黄色素极低的水溶性和生物利用度，其药