[硫普罗宁肠溶胶囊在健康志愿者中的生物等效性]
[Bioequivalence of tiopronin enteric capsules in healthy volunteers].
作者信息
Xu Chong-yuan, Yang Lin, Tang Wen-yan, Xiang Yi, Qian Zhen-yu, Yuan Jin, Yang Bin-bin, Zheng Heng
机构信息
Department of Pharmacy, Nanfang Hospital, Southern Medical University, Guangzhou 510515, China.
出版信息
Nan Fang Yi Ke Da Xue Xue Bao. 2009 Aug;29(8):1632-4.
OBJECTIVE
To evaluate the bioequivalence of tiopronin enteric capsules (testing preparation, T) versus tablets (reference preparation, R).
METHODS
A single oral dose of tiopronin enteric capsules or tablets at 200 mg was administered in 2 groups of Chinese healthy volunteers (n=9) in a randomized crossover design at the interval of 2 weeks. The plasma concentrations of tiopronin were measured by HPLC-MS/MS, and the pharmacokinetic parameters were calculated by DAS 2.0 program. The bioequivalence between the two preparations was evaluated.
RESULTS
The main pharmacokinetic parameters were as follows: C(max)(microg.ml(-1)) 3.612-/+1.2393 (R), 3.644-/+1.540 (T); t(max) 4.333-/+1.0853 (R), 3.611-/+1.420 (T); t((1/2))(h) 18.245-/+11.270 (R), 23.403-/+10.500 (T); AUC0-t (microg.h.ml(-1)) 18.732-/+6.92318 (R), 18.713-/+6.585 (T); AUC0-infinity (microg.h.ml(-1)) 21.900-/+7.31220 (R), 20.780-/+7.965 (T). The relative bioavailability of tiopronin enteric capsule was 103.712-/+23.956%, with 90% confidential intervals of ln(AUC0-->72), ln(AUC0-infinity) and ln(C(max)) of 91.1%-111.8%, 96.8%-118.3%, and 85.1%-113.0%, respectively.
CONCLUSION
The tiopronin enteric capsules were bioequivalent to the tablets.
目的
评价硫普罗宁肠溶胶囊（受试制剂，T）与硫普罗宁片（参比制剂，R）的生物等效性。
方法
采用随机交叉试验设计，将2组（每组9名）中国健康志愿者随机分为2组，分别单次口服200mg硫普罗宁肠溶胶囊或硫普罗宁片，服药间隔为2周。采用高效液相色谱 - 串联质谱法（HPLC - MS/MS）测定血浆中硫普罗宁浓度，用DAS 2.0程序计算药代动力学参数，并评价两种制剂的生物等效性。
结果
主要药代动力学参数如下：C(max)（μg·ml⁻¹）：参比制剂为3.612±1.2393，受试制剂为3.644±1.540；t(max)（h）：参比制剂为4.333±1.0853，受试制剂为3.611±1.420；t(1/2)（h）：参比制剂为18.245±11.270，受试制剂为23.403±10.500；AUC0 - t（μg·h·ml⁻¹）：参比制剂为18.732±6.92318，受试制剂为18.713±6.585；AUC0 - infinity（μg·h·ml⁻¹）：参比制剂为21.900±7.31220，受试制剂为20.780±7.965。硫普罗宁肠溶胶囊的相对生物利用度为103.712±23.956%，ln(AUC0→72)、ln(AUC0 - infinity)和ln(C(max))的90%置信区间分别为91.1% - 111.8%、96.8% - 118.3%和85.1% - 113.0%。
结论
硫普罗宁肠溶胶囊与硫普罗宁片生物等效。
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