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随机交叉直肠给予１２名健康男性受试者１００ ｍｍ进口和国产盐酸曲马多栓。采用气相色谱法测定给药后同时间的血浆药物浓度，研究国产盐酸曲马多栓在人体内的药代动力学和相对生物利用度。研究结果表明：进口和国产盐酸曲马多栓的药代动力学参数（均数±标准差）：Ｔｍａｘ分别为２．６±１．０和２．７±１．１ｈ；Ｃｍａｘ分别为３８４± ６７和３９２± ７１ｕ ｇ·Ｌ－１； Ｔ１／２分别为８．７± ２．５和８．９± ２．６ ｈ； Ｖｄ／Ｆ分别为 ４．２±１．２和 ４．４±１．３ Ｌ· ｋｇ－１； ＣＬ／Ｆ分别为 ２２．８± １０．９和 ２２．８ ±９．２ Ｌ· ｈ－１；ＡＵＣ０－４８分别为４７９２± １５７６和４７１９ ± １５８９ ｕ ｇ·ｈ·Ｌ－１。经配对ｔ检验上述参数差异均无显著性意义。国产盐酸曲马多栓相对生物利用度Ｆ为９８％±１０％；其９０％的可信区间为９３％－１１３％。结果提示国产盐酸曲马多栓和进口盐酸曲马多栓具有生物等效性。
Twelve healthy male subjects were randomized to 100 mm rectal import and domestic tramadol hydrochloride suppositories. Gas chromatography was used to measure plasma drug concentration at the same time after administration. The pharmacokinetics and relative bioavailability of domestic tramadol suppository were studied. The results showed that the pharmacokinetic parameters (mean ± standard deviation) of imported and domestic tramadol suppositories were 2.6 ± 1.0 and 2.7 ± 1.1 h for Tmax and 384 ± 67 and 392 ± 71 u g · L-1, respectively; T1 / 2 was 8.7 ± 2.5 and 8.9 ± 2.6 h, respectively; Vd / F were 4.2 ± 1.2 and 4.4 ± 1.3 L · kg-1; CL / F were 22.8 ± 10.9 and 22.8 ± 9.2 L · h-1; AUC0-48 were 4792 ± 1576 and 4719 ± 1589 ug · h · L-1. Paired t test the above parameters were no significant difference. The relative bioavailability of domestic tramadol suppository F was 98% ± 10%; its 90% confidence interval was 93% -113%. The results suggest that domestic tramadol hydrochloride suppository and imported tramadol hydrochloride suppository have bioequivalence.