空腹健康成人服用缓释和速释褪黑素胶囊的药代动力学比较:一项随机、开放标签、交叉研究。

IF 4.9 3区 医学 Q1 PHARMACOLOGY & PHARMACY Pharmaceutics Pub Date : 2024-09-25 DOI:10.3390/pharmaceutics16101248
Shefali Thanawala, R Abiraamasundari, Rajat Shah
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引用次数: 0

摘要

背景:外源性褪黑素是一种营养保健品,可用于维持健康的睡眠-觉醒周期和控制睡眠障碍,但由于其生物利用度低、半衰期短,因此需要重复服用大剂量褪黑素。这就需要开发一种半衰期更长、血浆浓度更持久的缓释制剂。因此,我们配制了外源性新型 5 毫克褪黑素缓释胶囊(Melatonin-SR,试验产品)。研究方法这项开放标签交叉研究比较了褪黑素-SR与5毫克速释褪黑素胶囊(褪黑素-IR,参比产品)在健康空腹成年人中单次口服后的药代动力学(最大浓度[Cmax]、达到Cmax的时间[Tmax]、曲线下面积[AUC]和消除半衰期[t1/2])和安全性。结果:16名参与者(18-45岁)被随机(1:1)分两次服用褪黑素-SR或褪黑素-IR,并有7天的冲洗期。与褪黑素-IR(22786.30 pg/mL)相比,褪黑素-SR的Cmax较低(11446.87 pg/mL)。褪黑素-SR和褪黑素-IR的平均Tmax分别为1.26小时和0.87小时。褪黑素-SR的平均t1/2(5.10小时)比褪黑素-IR(1.01小时)延长了5倍。服用褪黑素-IR后出现了一次不良反应(呕吐)。结论褪黑素-SR可使血浆中的褪黑素浓度更高且持续时间更长,并且耐受性良好。因此,Melatonin-SR 可能是一种很有前途的维持健康睡眠的营养保健品。
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Comparative Pharmacokinetics of Sustained-Release versus Immediate-Release Melatonin Capsules in Fasting Healthy Adults: A Randomized, Open-Label, Cross-Over Study.

Background: Exogenous melatonin, a nutraceutical for maintaining a healthy sleep-wake cycle and managing sleep disorders, requires large, repeated doses due to its low bioavailability and short half-life. This necessitates the development of a sustained-release formulation with a longer half-life and sustained plasma concentration. Therefore, exogenous novel 5 mg sustained-release melatonin capsules (Melatonin-SR, test product) were formulated. Methods: This open-label cross-over study compared the pharmacokinetics (maximum concentration [Cmax], time to reach Cmax [Tmax], area under the curve [AUC], and elimination half-life [t1/2]) and the safety of Melatonin-SR with 5 mg immediate-release melatonin capsules (Melatonin-IR, reference product) after single-dose oral administration in healthy fasting adults. Results: Sixteen participants (aged 18-45 years) were randomized (1:1) to receive either Melatonin-SR or Melatonin-IR in two periods with a 7-day washout period. Melatonin-SR reported a lower Cmax (11,446.87 pg/mL) compared to Melatonin-IR (22,786.30 pg/mL). The mean Tmax of Melatonin-SR and Melatonin-IR was 1.26 h and 0.87 h, respectively. The mean t1/2 of Melatonin-SR (5.10 h) was prolonged by five-fold compared to Melatonin-IR (1.01 h). One adverse event (vomiting) was reported following the administration of the Melatonin-IR. Conclusions: Melatonin-SR resulted in higher and sustained plasma melatonin concentrations for an extended period and was well-tolerated. Hence, Melatonin-SR may be a promising nutraceutical for maintaining healthy sleep.

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来源期刊
Pharmaceutics
Pharmaceutics Pharmacology, Toxicology and Pharmaceutics-Pharmaceutical Science
CiteScore
7.90
自引率
11.10%
发文量
2379
审稿时长
16.41 days
期刊介绍: Pharmaceutics (ISSN 1999-4923) is an open access journal which provides an advanced forum for the science and technology of pharmaceutics and biopharmaceutics. It publishes reviews, regular research papers, communications,  and short notes. Covered topics include pharmacokinetics, toxicokinetics, pharmacodynamics, pharmacogenetics and pharmacogenomics, and pharmaceutical formulation. Our aim is to encourage scientists to publish their experimental and theoretical details in as much detail as possible. There is no restriction on the length of the papers. The full experimental details must be provided so that the results can be reproduced.
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