国产吗氯贝胺片的人体相对生物利用度研究

BIOAVAILABILITY OF DOMESTIC MOCLOBEMIDE IN NORMAL VOLUNTEERS

８名男性健康受试者交叉口服１５０ｍｇ国产与进口吗氯贝胺片剂，进行国产片的药代动力学和相对生物利用度研究，血药浓度采用高效液相色谱法测定。结果表明：口服国产和进口片剂的血药浓度时间曲线符合血管外给药二室模型，国产片和进口片的主要药代动力学参数Ｃｍａｘ分别为１１２０±４５９．１９和１１２７．６９±３４８．５７μｇ·Ｌ－１，Ｔｐｅａｋ分别为１．６４６±０．６０４和１．４７９±０．５２５ｈ，Ｔ１／２β分别为２．２３９±０．８２２和２．２２３±０．６４７ｈ，ＡＵＣ分别为５６３４．９６±２５２４．２０和５２５３．０２±１９３８．０６μｇ·ｈ·Ｌ－１。两种片剂的药代动力学参数经统计学分析无显著性差异（Ｐ＞０．０５）。国产吗氯贝胺片的的相对生物利用度为１０５．４±２３．９％，国产与进口制剂生物等效。

The pharmacokinetic profiles and the bioavailability of domestic moclobemide tablets were studied in 8 normal male volunteers. A single oral dose of 150 mg moclobemide made in China or Germany was given according to a cross-over design. Serum concentrations of moclobemide were measured by HPLC. The concentration-time curves of domestic and imported products were fitted to a two-compartment open model. Peak serum levels of domestic and imported tablets reached 1120±459.19 and 1127.69±348.57 μg·L-1, Tmax was 1.646±0.604 and 1.479±0.525 h,T1/2β was 2.239±0.822 and 2.223±0.647 h, AUC was 5634.96±2524.20 and 5253.02±1938.06 μg·h·L-1, respectively。The pharmacokinetic parameters obtained from our studies showed no significant difference between two tablets, P>0.05.The relative bioavailability of domestic to imported tablets was 105.4%,it demonstrated that both formations had bioequivalence.