国产去羟肌苷散剂与进口去羟肌苷片剂的人体生物等效性

目的:评价国产去羟肌苷散剂与进口去羟肌苷片剂的人体生物等效性。方法:20名健康男性受试者,随机分为A和B两组,自身交叉口服单剂量国产去羟肌苷散剂250mg和进口去羟肌苷片剂200mg。血浆采用固相萃取处理,以HPLC测定去羟肌苷的经时血药浓度,计算2种制剂相对生物利用度参数,并评价其生物等效性。结果:国产去羟肌苷散剂和进口去羟肌苷片剂的主要药动学参数,tmax为(0.67±s0.04)h和(0.66±0.06)h,cmax为(0.84±0.26)mg·L-1和(0.9±0.3)mg·L-1,t1/2为(2.6±0.4)h和(2.5±0.3)h,AUC0~10为(1.7±0.8)mg·h·L-1和(1.7±0.7)mg·h·L-1,AUC0~∞为(1.8±0.9)mg·h·L-1和(1.9±0.9)mg·h·L-1。国产去羟肌苷散剂的相对人体生物利用度是(96±21)%(n=20,以AUC0~10计)。去羟肌苷散剂和片剂的主要药动学参数经交叉试验方差分析显示差异无显著意义(P>0.05)。2种制剂的AUC0~10,AUC0~∞,cmax经双单侧t检验示90%置信区间位于有效区间80%~125%范围内。结论:国产去羟肌苷散剂与进口去羟肌苷片剂具有生物等效性。

Bioequivalence of domestic didanosine powders and imported didanosine tablets in human

AIM: To evaluate the bioequivalence between didanosine’s domestic powders and imported tablets in human. METHODS:According to the random crossover design, twenty healthy male volunteers were administered didanosine powders 250 mg and tablets 200 mg.Plasma samples were collected by solid-phase extraction, and the plasma concentrations of didanosine were determined by HPLC assay. RESULTS:The plasma concentration-time curves of didanosine powders and tablets took a nearly identical course. The main pharmacokinetic parameters were as follows: ((0.67)±s 0.04) h vs (0.66±0.06) h for t_(max), ((0.8±0.3)) mg·L~(-1) vs (0.9±0.3) mg·L~(-1) for c_(max),(2.6±0.4) h vs (2.5±0.3) h for t_(1/2), ((1.7±0.8) mg·h·L~(-1)) vs (1.7±0.7) (mg·)h·L~(-1) for AUC_(0-10), (1.8±0.9) (mg·)h·L~(-1) vs (1.9±(0.9) mg·h·L~(-1)) for AUC_(0-∞), respectively.The relative bioavailability of the test powders versus the reference tablets was (96±(21) %). CONCLUSION:The domestic didanosine powders and imported didanosine tablets are bioequivalent.