Centro de Estudios Científicos y Clínicos Pharma, S.A. de C.V., Mexico City, Mexico.
Clin Ther. 2010 Feb;32(2):357-64. doi: 10.1016/j.clinthera.2010.02.002.
BACKGROUND: Piroxicam is an NSAID indicated for the treatment of rheumatoid diseases. Although there are generic formulations of oral piroxicam marketed in Mexico, a literature search did not identify published data concerning the bioavailability of these formulations in the Mexican population. OBJECTIVES: The aims of this study were to determine the bioequivalence of a generic (test) and a reference formulation of oral piroxicam 20 mg and to generate data regarding the oral bioavailability of this drug in a Mexican population. METHODS: This single-dose, randomized-sequence, open-label, 2-period crossover study was conducted in healthy Mexican adult volunteers. Subjects were randomly assigned to receive the test formulation followed by the reference formulation, or vice versa, with a 15-day washout period between doses. Study drugs were administered after a 10-hour overnight fast. For pharmacokinetic analysis, blood samples were drawn at 0 (baseline), 0.5, 1, 1.5, 2, 2.5, 3, 4, 5, 6, 8, 12, 24, 48, 72, 96, 120, and 168 hours after administration. Plasma concentrations of piroxicam were determined using HPLC. The test and reference formulations were to be considered bioequivalent if the 90% CIs for the geometric mean test/reference ratios were within a predetermined range of 80% to 125%. Tolerability was determined using clinical assessment, monitoring of vital signs, laboratory analysis, and subject interviews regarding adverse events (AEs). RESULTS: A total of 28 subjects were enrolled (15 men, 13 women; mean [SD] age, 24 [4] years [range, 19-35 years]; weight, 63.0 [8.9] kg [range, 47.5-81.9 kg]; height, 165 [10] cm [range, 149-179 cm]; and body mass index, 23.2 [1.4] kg/m(2) [range, 20.6-26.0 kg/m(2)]). The 90% CIs for piroxicam C(max), AUC(0-infinity), and AUC(0-infinity)) were 89.98% to 101.04%, 91.46% to 101.19%, and 93.51% to 105.86%, respectively. Thirteen subjects reported a total of 17 AEs during the study. None of the AEs were considered serious or related to the administered formulations. The most common AE was local postvenipuncture ecchymosis, reported in 8 subjects (28.6%). CONCLUSIONS: In this small study in healthy Mexican adult subjects, a single 20-mg dose of the test formulation of orally administered piroxicam met the regulatory requirements to assume bioequivalence, based on the rate and extent of absorption. Both formulations were well tolerated. Mexican national registry code: CE-PEC.0875.
背景：吡罗昔康是一种 NSAID，用于治疗类风湿疾病。虽然墨西哥有口服吡罗昔康的仿制药上市，但文献检索并未发现有关这些制剂在墨西哥人群中生物利用度的已发表数据。
目的：本研究的目的是确定一种通用（测试）和一种参考制剂的口服吡罗昔康 20mg 的生物等效性，并生成有关该药物在墨西哥人群中口服生物利用度的数据。
方法：这是一项单剂量、随机序列、开放标签、2 期交叉研究，在健康的墨西哥成年志愿者中进行。受试者随机分配接受测试制剂，然后接受参考制剂，或反之亦然，两次给药之间有 15 天的洗脱期。在 10 小时的禁食后给予研究药物。进行药代动力学分析时，在给药后 0（基线）、0.5、1、1.5、2、2.5、3、4、5、6、8、12、24、48、72、96、120 和 168 小时采集血样。使用 HPLC 测定吡罗昔康的血浆浓度。如果测试和参考制剂的几何均数测试/参考比值的 90%置信区间在 80%至 125%的预定范围内，则认为它们具有生物等效性。通过临床评估、生命体征监测、实验室分析和对不良事件（AE）的受试者访谈来确定耐受性。
结果：共纳入 28 名受试者（15 名男性，13 名女性；平均[标准差]年龄为 24[4]岁[范围，19-35 岁]；体重为 63.0[8.9]kg[范围，47.5-81.9kg]；身高为 165[10]cm[范围，149-179cm]；体重指数为 23.2[1.4]kg/m(2)[范围，20.6-26.0kg/m(2)]）。吡罗昔康 C(max)、AUC(0-无穷大)和 AUC(0-无穷大)的 90%置信区间分别为 89.98%至 101.04%、91.46%至 101.19%和 93.51%至 105.86%。13 名受试者在研究期间共报告了 17 起不良事件。没有任何不良事件被认为是严重的或与给予的制剂有关。最常见的不良事件是局部静脉穿刺后瘀斑，报告了 8 名受试者（28.6%）。
结论：在这项针对健康的墨西哥成年受试者的小型研究中，口服给予的测试制剂的单 20mg 剂量符合吸收速率和程度的监管要求，可假定具有生物等效性。两种制剂均具有良好的耐受性。墨西哥国家注册码：CE-PEC.0875。
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