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首页> 外文期刊>Current therapeutic research, clinical and experimental. >Comparative Bioavailability and Tolerability of a Single 2-mg Dose of 2 Repaglinide Tablet Formulations in Fasting, Healthy Chinese Male Volunteers: An Open-Label, Randomized-Sequence, 2-Period Crossover Study
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Comparative Bioavailability and Tolerability of a Single 2-mg Dose of 2 Repaglinide Tablet Formulations in Fasting, Healthy Chinese Male Volunteers: An Open-Label, Randomized-Sequence, 2-Period Crossover Study

机译：禁食，健康的中国男性志愿者中2种瑞格列奈片的2 mg剂量的比较生物利用度和耐受性：一项开放标签，随机序列，2期交叉研究

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Background: Repaglinide, an oral insulin secretagogue, was the first meglitinide analogue to be approved for use in patients with type 2 diabetes mellitus.Objective: In our study, the bioavailability and tolerability of the proposed generic formulation with the established reference formulation of repaglinide 2 mg were compared in a fasting, healthy Chinese male population.Methods: This 2-week, open-label, randomized-sequence, single-dose, 2-period crossover study was conducted in 22 healthy native Han Chinese male volunteers. Eligible subjects were randomly assigned in a 1:1 ratio to receive a single 2-mg dose of the test or reference formulation, followed by a 7-day washout period and administration of the alternate formulation. After an overnight fast, subjects received a single oral dose of repaglinide (2 mg). Blood samples were drawn at predetermined time points (0, 0.25, 0.5, 0.75, 1, 1.25, 1.5, 2.0, 2.5, 3.0, 4.0, 5.0, and 6.0 hours). All plasma concentrations of repaglinide were measured by LC-MS/MS. The observed Cmax, Tmax, tip., and AUC were assessed. The formulations were to be considered bioequivalent if the In-transformed ratios of Cnla>( and AUC were within the predetermined bioequivalence range of 80% to 125% established by the State Food and Drug Administration of the People's Republic of China. Tolerability was assessed throughout the study via subject interview, vital signs, and blood sampling.Results: The mean (SD) age of the subjects was 24.2 (2.3) years; their mean (SD) weight was 62.6 (5.8) kg, their mean (SD) height was 172 (5.7) cm, and their mean (SD) body mass index was 21.0 (1.1). The mean (SD) Cmax for repaglinide with the test and reference formulations were 20.0 (5.1) and 18.7 (8.7) ng/mL The AUCo-t for the test formulation was 46.3 (15.1) and AUC0-^ was 47.9 (16.5) ng*h/mL With the reference formulation, the corresponding values were 46.4 (26.1) and 49.0 (31.3) ng*h/mL The mean (SD) Tmax values with the test and reference formulations were 1.2 (0.7) hours and 1.5 (0.8) hours and the mean (SD) values ti/2 values were 1.0 (0.3), and 0.9 (0.3) hours, respectively. The In-transformed ratios of Cmali, AUC0_t, and AUQ,.^ were 113.6:1,105.6:1, and 104.7:1. The corresponding 90% CIs were 99.8 to 129.2, 93.4 to 119.5, and 91.8 to 119.5. respectively.Conclusions: This single-dose study found that the test and reference formulations of repaglinide met the regulatory criteria for bioequivalence in these fasting, healthy Chinese male volunteers. Both formulations appeared to be well tolerated. ClinicalTrials.gov identifier: 2012L01684.
机译：背景：瑞格列奈是一种口服胰岛素促分泌剂，是首个被批准用于2型糖尿病患者的美格替尼类似物。目的：在我们的研究中，拟议的通用制剂与已确定的瑞格列奈2的参考制剂的生物利用度和耐受性方法：在22名健康的中国汉族男性汉族志愿者中进行了为期2周，开放标签，随机序列，单剂量，2期交叉研究。将符合条件的受试者以1：1的比例随机分配，以接受2 mg剂量的测试或参考制剂，然后为期7天的洗脱期并使用替代制剂。过夜禁食后，受试者接受单次口服瑞格列奈（2 mg）。在预定的时间点（0、0.25、0.5、0.75、1、1.25、1.5、2.0、2.5、3.0、4.0、5.0和6.0小时）抽取血样。通过LC-MS / MS测量瑞格列奈的所有血浆浓度。评估观察到的Cmax，Tmax，tip和AUC。如果Cnla>（和AUC）的转化率在国家食品药品监督管理局规定的80％至125％的预定生物等效性范围内，则认为该制剂具有生物等效性。结果：受试者的平均（SD）年龄为24.2（2.3）岁;平均（SD）体重为62.6（5.8）kg，其平均（SD）身高为172（5.7）cm，其平均（SD）体重指数为21.0（1.1）。瑞格列奈在测试和参考配方中的平均（SD）Cmax为20.0（5.1）和18.7（8.7）ng / mL。测试配方的AUCo-t为46.3（15.1），AUC0- ^为47.9（16.5）ng * h / mL对于参考配方，相应的值为46.4（26.1）和49.0（31.3）ng * h / mL。测试和参考配方的平均（SD）Tmax值为1.2（0.7）小时和1.5（0.8）小时，平均（SD）值ti / 2值分别为1.0（0.3）和0.9（0.3）小时。 Cmali，AUC 0_t和AUQ的转化率分别为113.6：1、105.6：1和104.7：1。相应的90％CI为99.8至129.2、93.4至119.5和91.8至119.5。结论：这项单剂量研究发现瑞格列奈的测试和参考制剂符合这些禁食，健康的中国男性志愿者体内生物等效性的管理标准。两种制剂似乎都具有良好的耐受性。 ClinicalTrials.gov标识符：2012L01684。

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