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首页> 外文期刊>Journal of Clinical Pharmacy and Therapeutics >The effects of food on the pharmacokinetics of mitiglinide tablets in healthy volunteers and a novel mass-spectrometric (UPLC-MS/MS) method for such studies
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The effects of food on the pharmacokinetics of mitiglinide tablets in healthy volunteers and a novel mass-spectrometric (UPLC-MS/MS) method for such studies

机译：食物对健康志愿者米格列奈片药代动力学的影响，以及用于此类研究的新型质谱（UPLC-MS / MS）方法

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What is known and Objective: Mitiglinide (MGN) is a new insulinotropic agent of the glinide class with rapid onset. The effects of food intake on the pharmacokinetic (PK) profile of mitiglinide tablets after single oral administration have not yet been reported in healthy adults. We aimed to assess the effects of food intake on the PK properties of mitiglinide (MGN) tablets, using a novel analytical method, after single escalating oral doses in healthy Chinese volunteers. Methods: In this open-label, randomized, single-dose (three distinct doses), two-way crossover PK study, three doses of MGN 5, 10 or 20 mg were administered to healthy adult volunteers after an overnight fast (fasted condition) or low-fat breakfast (fed condition) (period 1). After 7 days, the participants received the same dose under the opposite fed/fasted condition (period 2). Serial blood samples were obtained before and through 8 h after study drug administration. Concentrations of MGN in plasma were determined using UPLC-MS/MS. Adverse events (AEs) were monitored and recorded on each in-clinic day. Results and Discussion: Twenty-four Chinese volunteers (eight [four men, four women] volunteers per group) were enrolled in the study. The extent of absorption of MGN was similar in both fed and fasted conditions at single doses in the range 5-20 mg. Food intake was associated with decreases in C max by 60·4% to 65·2% in the three dose groups and greatly delayed T max [0·36(Standard deviation 0·16) vs. 1·75(0·92) hours with 5 mg, 0·29(0·19) vs. 1·97(0·81) hours with 10 mg and 0·30(0·10) vs. 1·18(0·68) hours with 20 mg; all, P 0·05]. t 1/2, CL/F and V/F (P 0·05) were unaffected. MRT 0-8 at the 5 and 10-mg doses, but not at the 20-mg dose, were markedly lower in fasted volunteers than fed volunteers (P 0·05). What is new and Conclusions: Using a novel UPLC-MS/MS method, we showed that food intake affected the rate but not the extent of absorption of MGN within the 5- to 20-mg dose range. Gender did not appear to affect the PK properties of MGN in either fasted or fed states. MGN should be preferably taken before food.
机译：已知和目的：米格列奈（MGN）是一种新型的格列奈特促胰岛素药物，起效迅速。在健康成年人中，单次口服给药后食物摄入量对米格列奈片药代动力学（PK）的影响尚未见报道。我们旨在通过一种新颖的分析方法，在健康的中国志愿者中单次增加口服剂量后，评估食物摄入量对米格列奈（MGN）片的PK特性的影响。方法：在这项开放标签，随机，单剂量（三个不同剂量）的双向交叉PK研究中，禁食过夜（禁食）后，向健康成人志愿者服用三剂MGN 5、10或20 mg或低脂早餐（进食状态）（时间段1）。 7天后，参与者在相反的进食/禁食条件下接受相同剂量（第二阶段）。在服用研究药物之前和之后的8小时内获得了连续的血液样本。使用UPLC-MS / MS测定血浆中MGN的浓度。在每个诊所的一天监测并记录不良事件（AE）。结果与讨论：24名中国志愿者（每组八名[四名男性，四名女性]志愿者）被纳入研究。在进食和禁食条件下，单剂量5-20 mg的MGN吸收程度相似。在三个剂量组中，食物摄入可使C max降低60·4％至65·2％，并且Tmax大大延迟[0·36（标准差0·16）与1·75（0·92） 5毫克时，0·29（0·19）小时与10毫克时1·97（0·81）小时和20毫克时0·30（0·10）小时1·18（0·68）小时;全部，P <0·05]。 t 1/2，CL / F和V / F（P> 0·05）不受影响。禁食志愿者在5和10毫克剂量下的MRT 0-8，而不是20毫克剂量下，显着低于进食志愿者（P <0·05）。新内容和结论：使用新颖的UPLC-MS / MS方法，我们发现食物摄入量在5至20 mg剂量范围内影响MGN的吸收速率，但不影响其吸收程度。在禁食或进食状态下，性别似乎均未影响MGN的PK特性。 MGN应优先在食物前服用。

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