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首页> 美国卫生研究院文献>Wiley-Blackwell Online Open >Selection of 12‐Hour Sustained‐Release Acetaminophen (Paracetamol) Formulation Through Comparison of Pharmacokinetic Profiles of 4 Sustained‐Release Prototype Formulations and Standard Acetaminophen Formulation: An Open‐Label Randomized Proof‐of‐Principle Pharmacokinetic Study
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Selection of 12‐Hour Sustained‐Release Acetaminophen (Paracetamol) Formulation Through Comparison of Pharmacokinetic Profiles of 4 Sustained‐Release Prototype Formulations and Standard Acetaminophen Formulation: An Open‐Label Randomized Proof‐of‐Principle Pharmacokinetic Study

机译：通过比较4种持续释放原型制剂和标准对乙酰氨基酚制剂的药代动力学曲线选择12小时持续释放对乙酰氨基酚（对乙酰氨基酚）制剂：一项开放标签随机原理证明药代动力学研究

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摘要

Acetaminophen (APAP; paracetamol), a widely used analgesic and antipyretic, is available in modified‐release and immediate‐release (IR) formulations requiring 3‐ or 4‐times‐daily dosing. This phase 1 open‐label crossover study compared pharmacokinetic profiles of single 2000‐mg doses of 4 different sustained‐release (SR) formulations of APAP (designed to allow twice‐daily dosing) against two 1000‐mg doses (taken 6 hours apart) of standard IR APAP in 14 healthy volunteers. The primary end point was duration of time that plasma APAP concentration exceeded a plasma concentration (TC) of 4 μg/mL. Of the 4 SR APAP formulations studied, a single 2000‐mg dose of a bilayer SR formulation had the longest mean TC>4μg/mL (8.1 hours), similar to that of 2 doses of IR APAP (8.3 hours). Mean TC>4μg/mL was 7.3 hours with a single‐layer SR APAP, 7.5 hours with another single‐layer SR APAP formulation using a different excipient, and 7.1 hours with an enteric‐coated SR APAP coupled with a fast‐dissolving IR APAP. Secondary pharmacokinetic analyses showed a similar extent of absorption and lower peak concentration for the bilayer SR formulation compared with IR APAP. Adverse events were all mild. Based on these results, the bilayer SR APAP formulation was selected for further development.
机译：对乙酰氨基酚（APAP;对乙酰氨基酚）是一种广泛使用的镇痛药和解热药，可用于调释和速释（IR）制剂中，需要每天3或4次给药。这项1期开放标签交叉研究比较了4种不同APAP缓释（SR）制剂的单次2000 mg剂量（设计为允许每天两次给药）与两种1000 mg剂量（间隔6小时）的药代动力学特征。 14位健康志愿者的标准IR APAP评估。主要终点是血浆APAP浓度超过4μg/ mL血浆浓度（TC）的持续时间。在研究的4种SR APAP配方中，单剂量2000 mg双层SR配方的平均TC最长，>4μg/ mL（8.1小时），类似于2剂IR APAP（8.3小时）。单层SR APAP的平均TC>4μg/ mL为7.3小时，另一种单层SR APAP制剂（使用不同的赋形剂）为7.5小时，肠溶性SR APAP结合速溶IR APAP为7.1小时。二级药代动力学分析表明，与IR APAP相比，双层SR制剂的吸收程度相似，峰浓度更低。不良事件都很轻微。基于这些结果，选择了双层SR APAP配方进行进一步开发。

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