国产罗红霉素人体生物利用度研究

BIOAVAILABILITY OF DOMESTIC ROXITHROMICIN CAPSULES IN NORMAL VOLUNTEERS

８名男性健康志愿者交叉口服３００ｍｇ国产罗红霉素胶囊和进口片剂，进行国产制剂生物利用度研究，血药浓度用微生物法测定。结果表明：口服国产和进口两种制剂的血药浓度时间曲线均符合二室模型，Ｃｍａｘ分别为８．５９±１．０４和８．０５±１．３９ｍｇ／Ｌ，于１．３９±０．２５和１．５４±０．３５ｈ达峰，Ｔ１／２分别为１３．４５±３．３２和１４．０９±４．８７ｈ，ＡＵＣ是１１７．５±３２．０和１１５．２±２１．８ｍｇ·ｈ－１·Ｌ－１，比较两种制剂的药代动力学参数均无显著性差异，Ｐ＞０．０５。国产罗红霉素胶囊的相对生物利用度为１０２．０％，两种制剂生物等效。本项研究为国产罗红霉素胶囊的临床应用提供了指标和依据。

The bioavailability of domestic roxithromycin capsules was studied in 8 normal male volunteers.A single oral dose of 300 mg roxithromycin made in China or France was given according to a crossover design.Serum concentrations of roxithromycin were measured by bioassay.The concentration-time curves of domestic and imported products fitted to a two-compartment open model.Peak serum levels of domestic capsules and imported tablets reached 8.59±1.04 and 8.05±1.39 mg/L.at 1.39±0.25 and 1.54±0.35 h respectively.The T1/2β was 13.45±3.32 and 14.09±4.87 h.The AUC was 117.5±32.0 and 115.2±21.8 mg·h-1·L-1 respectively.The pharmacokinetic parameters obtained from our studies showed no significant difference between two products,P>0.05.The relative bioavailability of domestic capsules to imported tablets were 102.0%,so it demonstrated that both formations had bioequivalence.