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对１０名健康男性受试者分别多剂量交叉口服盐酸曲马多普通片５０ｍｇ６ｈ一次，共服５ｄ和缓释片１００ｍｇ１２ｈ一次，共服５ｄ的药代动力学及生物利用度进行研究。采用反相高效液相色谱－荧光法测定盐酸曲马多血浆药物浓度。结果表明，盐酸曲马多缓释片和普通片的Ｔｍａｘ分别为４．３３±０．３９ｈ和１．７２±０．３２ｈ（Ｐ＜０．０１），前者的缓释效果明显，ＡＵＣ０－１２分别为３７６７．６３±５７０．３７μｇ·ｈ·Ｌ－１和３８３８．７９±９１４．３１μｇ·ｈ·Ｌ－１（Ｐ＞０．０５），缓释片对普通片的相对生物利用度为９７．９％。缓释片和普通片的Ｃｍｉｎ分别为２１９．０６±４４．５３μｇ·Ｌ－１和１７５．２８±８６．２６μｇ·Ｌ－１（Ｐ＜０．０５）；Ｃｍａｘ分别为４５１．０６±４０．９８μｇ·ｈ·Ｌ－１和４８３．７３±８３．１７μｇ·Ｌ－１（Ｐ＞０．０５）；ＦＩ分别为０．６６±０．１５和０．９３±０．３４。缓释片在服药次数减少的情况下，血药浓度波动仍小于普通片。
10 healthy male subjects were given multiple doses of crossover oral tramadol hydrochloride tablets 50mg6h once for a total of 5d and sustained-release tablets 100mg12h once a total of 5d of pharmacokinetics and bioavailability were studied. Determination of Tramadol Hydrochloride Plasma Drug Concentration by Reversed-Phase High Performance Liquid Chromatography-Fluorescence Spectrometry. The results showed that the Tmax of tramadol hydrochloride sustained release tablets and ordinary tablets were 4.33 ± 0.39h and 1.72 ± 0.32h, respectively (P <0.01), and the former had a sustained release effect. The AUC0-12 (3767.63 ± 570.37μg · h · L-1 and 3838.79 ± 914.31μg · h · L-1, respectively) (P> 0.05). The relative bioavailability of sustained-release tablets to common tablets was 97 .9%. The Cmin of sustained-release tablets and ordinary tablets were 219.06 ± 44.53μg · L-1 and 175.28 ± 86.26μg · L-1, respectively (P <0.05), and the Cmax were 451.06 ± 40 respectively. 98μg · h · L-1 and 483.73 ± 83.17μg · L-1, respectively (P> 0.05); FI was 0.66 ± 0.15 and 0.93 ± 0.34, respectively. Sustained-release tablets in the case of medication decreases, the fluctuations in plasma concentration is still smaller than normal tablets.