Kim T K, Yoo H H, Kim E J, Lee B-Y, Park J H
College of Pharmacy, Seoul National University, Seoul, Republic of Korea.
Arzneimittelforschung. 2012 Jun;62(6):280-4. doi: 10.1055/s-0032-1306305. Epub 2012 Apr 16.
SID530 is a new parenteral formulation of docetaxel containing hydroxypropyl-beta-cyclodextrin (HP-β-CD). In this study, a comparative pharmacokinetic study of 2 docetaxel parenteral solutions, SID530 and Taxotere, was carried out. In a crossover experimental design, 6 male cynomolgus monkeys received each formulation by intravenous infusion of a single dose. The concentration of docetaxel in whole blood and plasma was determined using liquid chromatography-tandem mass spectrometry (LC-MS/MS). The 2 formulations showed similar pharmacokinetic parameters in both whole blood and plasma, and displayed comparable values for maximum serum concentration (Cmax), time to peak concentration (Tmax), and area under the concentration-time curve (AUC). The 90% confidence intervals for the ratios of Cmax and AUC values for SID530 to Taxotere were within the acceptable range of 0.80-1.20 in both plasma and whole blood. These findings indicate that SID530 and Taxotere are comparable in terms of their distribution in the blood and their plasma profile; consequently, these drugs are bioequivalent in the monkey.
SID530是一种含有羟丙基-β-环糊精（HP-β-CD）的多西他赛新的肠胃外制剂。在本研究中，对两种多西他赛肠胃外溶液SID530和泰索帝进行了比较药代动力学研究。在交叉实验设计中，6只雄性食蟹猴接受了每种制剂的单剂量静脉输注。使用液相色谱-串联质谱法（LC-MS/MS）测定全血和血浆中多西他赛的浓度。两种制剂在全血和血浆中均显示出相似的药代动力学参数，并且在最大血清浓度（Cmax）、达峰时间（Tmax）和浓度-时间曲线下面积（AUC）方面显示出相当的值。SID530与泰索帝的Cmax和AUC值之比的90%置信区间在血浆和全血的可接受范围0.80-1.20内。这些发现表明，SID530和泰索帝在血液中的分布及其血浆特征方面具有可比性；因此，这些药物在猴子体内具有生物等效性。
