罗红霉素颗粒剂人体生物利用度研究

Bioavailability of Roxithromycin Granule in Normal Volunteers

１０名健康男性志愿者交叉口服３００ｍｇ国产罗红霉素颗粒剂和进口片剂，进行国产制剂生物利用度研究，采用微生物法测定不同时间的血药浓度。结果罗红霉素颗粒剂和进口片剂两种制剂的血药浓度曲线均符合二室模型。Ｃｍａｘ分别为８．２８±０．５６ｍｇ／Ｌ和８．４２±０．７８ｍｇ／Ｌ，达峰时间分别为１．５１±０．２２ｈ和１．４２±０．１８ｈ，Ｔ１／２β分别为１２．２０±０．８５ｈ和１２．５８±０．９３ｈ，ＡＵＣ分别为１２０．５８±１２．９５ｍｇ／Ｌ·ｈ－１，和１１７．８０±１３．６８ｍｇ／Ｌ·ｈ－１两种制剂的药代动力学参数统计学检查无显著性差异。国产罗红霉素颗粒剂相对于进口片剂的生物利用度为１０２．７９±８．６８％，两种制剂生物等效。

he bioavailability of roxithromycin granule was studied in 10 normal male volunteers.A single oral dose of 300 mg roxithromycin made in China or Indonesia was given. Serum concentrations of roxithromycin were measured by bioassay at different intervals of time. The serum concentrationtime curves of domestic and imported products coincided with a twocompartment open model. The serum levels (Cmax) of domestic granules and imported tablets were 8.28±0.56 mg/L and 8.42±0.78 mg/L with the time of reaching peak in 1.51±0.22 h and 1.42±0.18 h respectively. The T1/2 β were 12.20±0.85 h and 12.58±0.93 h;the AUC 120.58±12.95 mg·L1·h1 and 117.80±13.68 mg·L1·h1 respectively.The pharmacokinetic parameters obtained from our studies showed no significant difference between the two products, P>0.05.The relative bioabailavility of domestic granules to imported tablets was 102.79%,indicating bioequivalence of the two pharmaceutics.