罗红霉素胶囊剂的临床药物动力学及相对生物利用度

Clinical pharmacokinetics and relative bioavailability of roxithromycin capsule

目的：进行国产与进口罗红霉素的生物利用度研究。方法：通过交叉试验对８名男性志愿者（２２．６ａ±ｓ２．１ａ）交叉口服罗红霉素３００ｍｇ国产胶囊剂和进口片剂，进行单剂量药物动力学研究。血药浓度采用微生物法进行测定。结果：口服国产胶囊和进口片剂的血药浓度＿时间曲线均符合二室模型，Ｃｍａｘ分别为９．５ｍｇ／Ｌ±１．３ｍｇ／Ｌ与９．０ｍｇ／Ｌ±１．０ｍｇ／Ｌ，Ｔｍａｘ为１．１４ｈ±０．１８ｈ与１．３１ｈ±０．２１ｈ，Ｔ１２β为１３．１ｈ±２．４ｈ与１３．６ｈ±２．２ｈ，ＡＵＣ为１０７ｍｇ·ｈ／Ｌ±２３ｍｇ·ｈ／Ｌ与１０８ｍｇ·ｈ／Ｌ±１４ｍｇ·ｈ／Ｌ。比较２种制剂的药物动力学参数，其差别均无显著意义（Ｐ＞０．０５）。与进口罗红霉素片相比较，国产罗红霉素胶囊剂的相对生物利用度为（９８±１３）％。口服该药４８ｈ尿药回收率为给药量的（１５±５）％。结论：国产罗红霉素胶囊体内过程与进口罗红霉素片剂相仿，２种制剂生物等效。

AIM: To observe the relative bioavailability of domestic or import roxithromycin. METHODS: A single oral dose of 300 mg roxithromycin of domestic capsule and imported tablet were given to 8 adult male volunteers (22.6 a±s 2.1 a) in a randomized cross_over study. Plasma concentrations were measured by microbial method. RESULTS: The plasma concentrations_time curves of the two preparations were fitted to a two_compartment model with C max 9.5 mg/L±1.3 mg/L and 9.0 mg/L±1.0 mg/L, T max 1.14 h±0.18 h and 1.31 h±0.21 h, T 12β 13.1 h±2.4 h and 13.6 h±2.2 h, AUC 107 mg·h/L±23 mg·h/L and 108 mg·h/L±14 mg·h/L, respectively. There was no significant difference between the pharmacokinetic parameters of the two kinds of pharmaceutics. The relative bioavailability of the capsule was (98±13)% to the reference tablet. The urinary recovery rate of the roxithromycin was (15±5)% during the period of 48 h after oral adminstration of domestic capsule. CONCLUSION: The pharmacokinetic profile of domestic roxithromycin capsule was similar to that of imported roxithromycin tablet, with similar biological availabilities.