Wu Xian-Chuang, Hao Hai-Jun, Liu Yu-Xin, Song Xiao-Yong, Zhang Yong-Zhou, Zhang Hong-Qin
Department of Pharmacy, Huaihe Hospital of Henan University, Kaifeng 475000, China.
Shanghai Institute of Pharmaceutical Industry, Shanghai 200437, China.
Zhongguo Zhong Yao Za Zhi. 2016 Mar;41(6):1130-1134. doi: 10.4268/cjcmm20160626.
To improve the bioavailability of 10-hydroxycamptothecin, 10-hydroxycamptothecin solid dispersion(HCPT-SD) and 10-hydroxycamptothecin-phospholipid complex-solid dispersion(HCPT-PC-SD) were prepared, and their solubility and dissolution rate were evaluated in this study. SD rates were administered intragastrically with HCPT-SD or HCPT-PC-SD respectively, then their blood samples were collected at different time intervals. The concentration of HCPT in blood was detected by HPLC method with camptothecin as internal standard, and then its pharmacokinetic parameters were calculated and obtained. The results showed that the Cmax, AUC0-t and AUC0-∞ of both kinds of solid dispersion of HCPT were significantly increased than those of crude drug. The AUC0-t of HCPT-SD was increased by 176.87%, and AUC0-t of HCPT-PC-SD was increased by 254.31% as compared with crude drug. Therefore, the two kinds of solid dispersion of HCPT could significantly enhance the bioavailability of HCPT in SD rates, and the effect of HCPT-PC-SD was more obvious.
为提高10-羟基喜树碱的生物利用度,制备了10-羟基喜树碱固体分散体(HCPT-SD)和10-羟基喜树碱-磷脂复合物-固体分散体(HCPT-PC-SD),并对其溶解度和溶出速率进行了评价。分别将HCPT-SD或HCPT-PC-SD灌胃给予SD大鼠,然后在不同时间间隔采集血样。以喜树碱为内标,采用高效液相色谱法检测血液中HCPT的浓度,进而计算并得出其药代动力学参数。结果表明,两种HCPT固体分散体的Cmax、AUC0-t和AUC0-∞均比原料药显著提高。与原料药相比,HCPT-SD的AUC0-t提高了176.87%,HCPT-PC-SD的AUC0-t提高了254.31%。因此,两种HCPT固体分散体均可显著提高HCPT在SD大鼠体内的生物利用度,且HCPT-PC-SD的效果更明显。