奥美拉唑在健康人体内的药物动力学研究

Pharmacokinetics of omeprazole in volunteers

本实验建立了奥美拉唑在人体内血药浓度的ＨＰＬＣ测定方法，并对奥美拉唑片（供试品）及胶囊剂（对照品）在健康人体内的药物动力学进行了研究。结果表明，奥美拉唑片与胶囊剂的达峰时间（Ｔｍ）分别为３．３ｈ和３．５ｈ（Ｐ＞０．０５）；Ｃｍ分别为７７４．５ｎｇ／ｍｌ和６１６．５ｎｇ／ｍｌ（Ｐ＜０．０５）；ＡＵＣ分别为３２７４．９（ｎｇ·ｈ）／ｍｌ和２９６８．１（ｎｇ·ｈ）／ｍｌ（Ｐ＜０．０５）。供试品的相对生物利用度为１０７．０±０．０９％，显示奥美拉唑片生物利用度优于对照品。但以２０％作为等效性判断检验标准，两者显示生物等效。

After oral administration of omeprazole tablets and capsules in 8 healthy volunteers,the plasma concentration of omeprezole was determined by HPLC.The concentration time profiles fitted to one compartment model.The pharmacokinetic parameters for tablets were T m= 3.3 h; C m= 774.5 ng/ml; AUC = 3274.9 (ng·h)/ml; T 1/2 = 1.4 h; K e= 0.57 h,for capsules were T m= 3.5 h; C m= 616.5 ng/ml; AUC = 2968.1 (ng·h)/ml; T 1/2 = 1.6 h; K e= 0.58 h.Relative bioavailability of tablets was 107.0% compared with capsules.It suggested that the tablets be the same as capsules in bioavailability.The two preparations were similar in bioequivalence.