国产舒他西林片剂人体生物利用度研究

RELATIVE BIOAVAILABILITY OF THE SULTAMICILLIN TABLET

本文进行了８名健康男性志愿者交叉口服两种舒他西林片剂的生物等效性试验，给药剂量为７５０ｍｇ，建立了ＨＰＬＣ法测定血清中氨苄西林（ＡＭＰ）、舒巴坦（ＳＢＴ）的药物浓度。药物的体内过程经药代动力学程序拟合后，发现符合二室模型，其主要的药代动力学参数如下。Ｃｍａｘ６．５９，８．７５（ＡＭＰ），３．８５，５．７４ｍｇ／ｌ（ＳＢＴ）；Ｔｍａｘ８０．３，５５．１（ＡＭＰ），７５．６，４６．３ｍｉｎ（ＳＢＴ）；Ｔ１／２（β）６３．３，７１．９（ＡＭＰ），５１．６，６２．１ｍｉｎ（ＳＢＴ）；ＡＵＣ１１９２．１，１３４１．９（ＡＭＰ），５６２．３，６０４．２ｍｇ·ｍｉｎ·Ｌ－１（ＳＢＴ）；Ｆ８９．３（ＡＭＰ），９４．２（ＳＢＴ）。统计学检验发现两药在吸收速度方面存在差异（Ｐ＜０．０５）

healthy male volunteers were enrolled in a two period cross-over bioequivalent study of sultamicillin tablet, HPLC method was established and used to assay the concentration of the active metabolites of sultamicillin-ampicillin and sulbactam in human serum after oral administration of 750 mg sultamicillin tablets. Two compartment model was fitted to the concentration-time profiles, Pharmacokinetic parameters for ampicillin (AMP) and sulbactam (SBT) were calculated as the follows: For imported sultamicillin tablets Cmax 8.75 (AMP), 5.74 mg/l (SBT); Tmax 55.1 (AMP), 46.3 min (SBT); T1/2 71.9 (AMP), 62.1 min (SBT); AUC 1341.9 (AMP), 604.2 mg·l-1 ·min (SBT). For domestic made tablets, Cmax 6.95 (AMP), 3.85 mg/l (SBT); Tmax 80.3 (AMP), 75.6 min (SBT); T1/2 63.3 (AMP), 51.6 min (SBT); AUC 1192.1 (AMP), 562.3 mg·l-1 ·min (SBT). F 89.3% (AMP), 94.2% (SBT). Statistical indicated there was significantly different between the two drugs in the rate of absorption (P<0.05).