国产瑞巴匹特片人体药代动力学及相对生物利用度研究

PHARMACOKINETICS AND BIOAVAILABILITY OF DOMESTIC REBAMIPIDE TABLET IN HEALTHY VOLUNTEERS

１０名男性健康志愿者交叉口服单剂量（６００ｍｇ）国产瑞巴匹特片剂和进口瑞巴匹特片剂两种制剂，用高效液相色谱法测定血浆中瑞巴匹特浓度，进行相对生物利用度研究。试验结果表明，口服国产和进口瑞巴匹特片剂的血药浓度－时间曲线均符合具有滞后时间的一级吸收一级消除的一房室模型，体内药物达峰时间分别为１．９５±０．７３和１．５７±０．５５ｈ；Ｃｍａｘ分别为５１０．８±１５２．０和５６４．８±１８７．７μｇ／Ｌ；Ｔ１／２分别为１．７５±０．６３和１．６６±０．３１ｈ；ＡＵＣ分别为２５０６．９±４１３．９和２５４９．７±５１３．１μｇ·ｈ·Ｌ－１；国产瑞巴匹特片的相对生物利用度为９９．３６±７．８７％。经统计分析，两种制剂的药代动力学参数均无显著性差异（Ｐ＞０．０５），两种制剂具有生物等效性。

A singal oral dose of 600 mg domestic and imported rebamipide was given to 10 healthy volunteers in a randomized crossover study. Drug concentrations in plasma were determined by HPLC method. The relative bioavailability was studied. The results showed that the plasma concentration-time curve of the two preparations were all fitted to a one-compartment model with first order absorption and elimination. Tmax of domestic and imported tablets were 1.95±0.73 and 1.57±0.55 h;Cmax were 510.8±152.0 and 564.8±187.7μ g/L; T1/2 were 1.75±0.63 and 1.66±0.31 h;AUC were 2506.9±413.9 and 2549.7±513.1 μg·h·L-1 respectively. The pharmacokinetic parameters obtained from our studies showed no significant difference between two products (P>0.05). The relative bioavailability of domestic to imported tablets were 99.36±7.87%. So it demonstrated that both formulations were bioequvalence.