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首页> 外文期刊>International journal of clinical pharmacology and therapeutics >Comparative bioavailability of two oral formulations of mycophenolate mofetil in healthy adult Uruguayan subjects: a case of highly variable rate of drug absorption.
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Comparative bioavailability of two oral formulations of mycophenolate mofetil in healthy adult Uruguayan subjects: a case of highly variable rate of drug absorption.

机译：两种麦考酚酸酯口服制剂在健康成人乌拉圭受试者中的比较生物利用度：药物吸收率变化很大的情况。

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OBJECTIVE: To assess the bioequivalence and safety of a new formulation of mycophenolate mofetil (MMF) 500 mg (Suprimun(R), Clausen, Montevideo, Uruguay) marketed in Uruguay and other South American countries, and to test Cmax/AUC as a characteristic of its absorption rate. MATERIAL AND METHODS: A randomized, open-label, two-way, two-treatment, two-period crossover study in 24 healthy male volunteers was carried out. One tablet (500 mg) of each formulation was administered after an overnight fast. After dosing, serial blood samples were collected for a period of 36 hours. Plasma concentrations of MPA were determined by high-performance liquid chromatography and pharmacokinetic parameters were calculated. Analysis of variance was carried out using log-transformed AUC0-36, Cmax, and Cmax/AUC0-36. 90% confidence intervals and within-subject between-subject variance were calculated. The bioequivalence of the two formulations was established at the 80% - 125% acceptance limits and untransformed tmax medians were compared using Wilcoxon test. Subjects were monitored for adverse events throughout the study. RESULTS: The means (test and reference) were 21.14 and 20.86 microg x h x ml-1 for AUC0-36, 24.92 and 24.18 microg x h x ml-1 for AUC0-inf, 11.86 and 10.76 microg x ml-1 for Cmax and 0.51 and 0.54 h-1 for Cmax/AUC0-36. The geometric mean ratios (confidence interval 90%) of Test/Reference were 1.00 (0.95 - 1.06) for AUC0-36, 1.09 (0.96 - 1.24) for Cmax and 1.04 (0.99 - 1.09) for Cmax/ AUC0-36. The extra peaks observed are due to enterohepatic recycling of MPA. No serious or unexpected adverse events were observed during the study. CONCLUSIONS: The test formulation containing mycophenolate mofetil 500 mg met regulatory requirements for bioequivalence. Moreover, Cmax/AUC shows interesting features as a putative metric to evaluate the absorption rate of highly variable drugs like mycophenolate mofetil. Generally, both formulations were well tolerated.
机译：目的：评估在乌拉圭和其他南美国家销售的500 mg霉酚酸酯（MMF）新配方（MMF）500 mg（Suprimun（R，Clausen，Montevideo，Uruguay））的生物等效性和安全性，并测试Cmax / AUC作为特征吸收率。材料与方法：在24名健康男性志愿者中进行了一项随机，开放标签，双向，两次治疗，两个时期的交叉研究。禁食过夜后，每片服用一片（500毫克）。给药后，收集连续血样36小时。通过高效液相色谱法测定MPA的血浆浓度，并计算药代动力学参数。使用对数转换后的AUC0-36，Cmax和Cmax / AUC0-36进行方差分析。计算了90％的置信区间和受试者内部受试者间差异。两种制剂的生物等效性确定在80％-125％的接受限，并使用Wilcoxon检验比较未转化的tmax中位数。在整个研究过程中对受试者进行不良事件监测。结果：AUC0-36的平均值（测试和参考）分别为21.14和20.86 microg xhx ml-1，AUC0-inf的平均值为24.92和24.18 microg xhx ml-1，Cmax为11.86和10.76 microg x ml-1,0.51和0.54 Cmax / AUC0-36的h-1。对于AUC0-36，测试/参考的几何平均比率（置信区间90％）为1.00（0.95-1.06），对于Cmax为1.09（0.96-1.24），对于Cmax / AUC0-36为1.04（0.99-1.09）。观察到的额外峰归因于MPA的肝肠循环。在研究过程中未观察到严重或意外的不良事件。结论：含有霉酚酸酯500 mg的测试制剂符合生物等效性的法规要求。此外，Cmax / AUC表现出有趣的功能，可作为评估高度可变的药物（如霉酚酸酯）的吸收率的推定指标。通常，两种制剂均具有良好的耐受性。

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