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首页> 外文期刊>Clinical therapeutics >Comparative Fasting Bioavailability of Dispersible and Conventional Tablets of Risperidone: A Single-Dose, Randomized-Sequence, Open-Label, Two-Period Crossover Study in Healthy Male Chinese Volunteers
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Comparative Fasting Bioavailability of Dispersible and Conventional Tablets of Risperidone: A Single-Dose, Randomized-Sequence, Open-Label, Two-Period Crossover Study in Healthy Male Chinese Volunteers

机译：利培酮分散片和常规片的比较禁食生物利用度：中国男性男性志愿者的单剂量，随机序列，开放标签，两期交叉研究

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Background: Risperidone (RIS), an atypical antipsychotic drug, is used for the treatment of psychoses associated with schizophrenia and other psychiatric disorders in adult and pediatric populations. An oral dispersible tablet formulation of risperidone has been developed. This study was conducted to provide support for marketing authorization of this drug in China. Objective: This study was designed to compare the pharmacokinetic (PK) properties and bioavailability of 2 RIS formulations-the dispersible formulation (test) and a branded formulation (reference) in healthy male Chinese volunteers. Methods: This single-dose, randomized-sequence, open-label, 2-period crossover study involved 22 healthy male Chinese volunteers. Equal numbers of eligible participants were randomly assigned to receive either the test drug (2 mg) or the same dose of the reference formulation, followed by a 2-week washout period and administration of the alternate formulation. The study drugs were administered after a 10-hour overnight fast. Blood samples were collected before dosing and at 0.33, 0.67, 1, 1.5, 2, 3, 4, 5, 6, 8, 10, 12, 15, 24, 36, 48, 72, and 96 hours after dosing. Plasma concentrations of RIS and its active metabolite, 9-hydroxyrisperidone (9-OH-RIS), were measured using LC-MS/MS. The safety profile was evaluated by recording adverse events (AEs), assessed using physical examination including vital signs, spontaneous reporting, and clinical laboratory results. The 2 formulations were considered to have met the requirements for bioequivalence if the 90% CIs for the log-transformed C max and AUC values were within the predetermined ranges of 75% to 133% and 80% to 125%, respectively, according to the guidelines of the State Food and Drug Administration (SFDA) of China. Results: All 22 volunteers (mean [SD] age, 22.2 [1.98] years; weight, 64.07 [5.93] kg; height, 173 [5] cm; and body mass index, 21.2 [1.67] kg/m 2) that were enrolled completed the study. For RIS, the 90% CIs for the ratios of C max, AUC 0-t, and AUC 0-∞ were 93.2% to 116.7%, 97.9% to 111.3%, and 98.0% to 111.6%, respectively. For 9-OH-RIS, the 90% CIs were 95.8% to 113.9%, 100.2% to 109.7%, and 100.5% to 110.3%, respectively. All values were within the predetermined bioequivalence range. Seven AEs were reported somnolence (4 subjects [9.1%]) and dizziness (3 subjects [6.8%]). All AEs were transient and considered mild by physicians. Conclusions: The test (dispersible) and reference tablets met the regulatory criteria for bioequivalence as defined by the SFDA. Both formulations were well tolerated. Chinese Clinical Trials registration number: ChiCTR-TRC-12001996.
机译：背景：利培酮（RIS）是一种非典型的抗精神病药物，用于治疗成人和儿童人群中与精神分裂症和其他精神疾病有关的精神病。已经开发了利培酮的口服分散片剂制剂。这项研究旨在为该药在中国的销售授权提供支持。目的：本研究旨在比较2种RIS制剂（可分散制剂（测试）和品牌制剂（参考））在中国男性健康志愿者中的药代动力学（PK）特性和生物利用度。方法：这项单剂量，随机序列，开放标签，2期交叉研究涉及22位健康的中国男性志愿者。随机分配相等数量的合格参与者以接受测试药物（2 mg）或相同剂量的参考制剂，然后为期2周的洗脱期并使用替代制剂。禁食10小时后，给予研究药物。给药前以及给药后0.33、0.67、1、1.5、2、3、4、5、6、8、10、12、15、24、36、48、72和96小时收集血液样本。使用LC-MS / MS测量RIS及其活性代谢物9-羟基利培酮（9-OH-RIS）的血浆浓度。通过记录不良事件（AE）来评估安全性，并使用包括生命体征，自发报告和临床实验室结果在内的身体检查进行评估。如果对数转换后的C max和AUC值的90％CI分别在75％至133％和80％至125％的预定范围内，则认为这2种制剂已满足生物等效性要求。中国国家食品药品监督管理局（SFDA）的指南。结果：所有22名志愿者（平均[SD]年龄，22.2 [1.98]岁;体重，64.07 [5.93] kg;身高，173 [5] cm;体重指数，21.2 [1.67] kg / m 2）登记完成研究。对于RIS，C max，AUC 0-t和AUC0-∞之比的90％CI分别为93.2％至116.7％，97.9％至111.3％和98.0％至111.6％。对于9-OH-RIS，90％CI分别为95.8％至113.9％，100.2％至109.7％和100.5％至110.3％。所有值均在预定的生物等效性范围内。据报道有7个AE出现嗜睡（4名受试者[9.1％]）和头晕（3名受试者[6.8％]）。所有不良事件都是暂时性的，并被医生认为是轻度的。结论：试验片（分散片）和参比片符合SFDA定义的生物等效性监管标准。两种制剂均耐受良好。中国临床试验注册号：ChiCTR-TRC-12001996。

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