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首页> 外文期刊>Clinical drug investigation >Tramadol SR Formulations Pharmacokinetic Comparison of a Multiple-Units Dose (Capsule) versus a Single-Unit Dose (Tablet)
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Tramadol SR Formulations Pharmacokinetic Comparison of a Multiple-Units Dose (Capsule) versus a Single-Unit Dose (Tablet)

机译：曲马多SR制剂多单位剂量（胶囊）与单单位剂量（片剂）的药代动力学比较

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Introduction: Different oral sustained-release (SR) formulations of tramadol have been introduced in pain treatment in order to prolong the dosage interval to improve convenience for the patient. The objective of this study was to compare tramadol pharmacokinetics and intra- and intersubject variability after replicate single-dose administrations of a multiple-units SR formulation (capsule) and a single-unit formulation (tablet).Methods: This was a randomised, single-dose, single-centre study with an open-label, four-period, two-sequence, two-formulation, replicate crossover design in healthy subjects under fed conditions. The main outcome measures were the intra- and intersubject variance of the area under the concentration-time curve from 0 to 12 hours (AUC_(12)) and maximum concentration (Cmax), as well as the mean AUC_(12) and C_(max) for tramadol. Study drugs were a tramadol SR multiple-units formulation (capsule) and a tramadol SR single-unit formulation (tablet), each containing tramadol hydrochloride l00mg. The time interval from 0 to 12 hours of AUC_(12) of the single-dose design corresponds to the recommended twice-daily dosage interval for both study drugs during long-term treatment. Results: The two formulations were equivalent in the area under the curve (AUC_(infinity) 2411 vs 2527mug·h/L). However, capsules led to a lower C_(max) (148.6 vs 183.2mug/L), to a later time to reach C_(max) (5.9 vs 4.9 hours), and to a longer half-value duration (13.4 vs 10.4 hours). In addition, intrasubject variability of AUC12 was significantly smaller for capsules than for tablets (p = 0.041). Capsules also produced smaller intra- and intersubject variability in plasma concentrations during the first 2.5 and 3.0 hours after administration, respectively (p < 0.05).Conclusion: Although tramadol SR capsules and tramadol SR tablets led to an equivalent systemic exposure to the drag, capsules provided a smoother and more extended plasma profile. In addition, in the case of capsules, bioavailability was subjected to lower variability in terms of both rate and extent of absorption.
机译：简介：曲马多的不同口服缓释（SR）制剂已被引入疼痛治疗中，以延长给药间隔以提高对患者的便利性。这项研究的目的是比较多单位SR制剂（胶囊）和单单位制剂（片剂）的重复单剂量给药后曲马多的药代动力学以及受试者内部和受试者之间的变异性。高剂量，单中心，开放标签，四周期，两序列，两配方，重复交叉设计的单中心研究。主要结果指标是浓度-时间曲线下从0到12小时的区域内和受试者间方差（AUC_（12））和最大浓度（Cmax），以及平均AUC_（12）和C_（最大值）用于曲马多。研究药物为曲马多SR多单位制剂（胶囊）和曲马多SR单单位制剂（片剂），每种药物均含100mg盐酸曲马多。单剂量设计的AUC_（12）从0到12小时的时间间隔对应于长期治疗期间两种研究药物的建议每日两次剂量间隔。结果：两种制剂在曲线下面积相等（AUC_（无穷大）2411对2527mug·h / L）。然而，胶囊导致较低的C_（max）（148.6 vs 183.2mug / L），导致达到C_（max）的时间较晚（5.9 vs 4.9小时），以及半值持续时间较长（13.4 vs 10.4小时） ）。此外，胶囊的受试者内部AUC12变异性明显小于片剂（p = 0.041）。在给药后的前2.5个小时和3.0个小时内，这些胶囊在受试者体内和受试者之间的血浆浓度变化也较小（p <0.05）。结论：尽管曲马多SR胶囊和曲马多SR片剂导致与药物同等的全身暴露，提供了更平滑，更扩展的血浆轮廓。另外，在胶囊的情况下，就吸收率和吸收程度而言，生物利用度具有较低的可变性。

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