在禁食健康成年人中,持续释放与立即释放的黑激素囊的比较药理动力学:一个随机的,开放的,交叉研究
Shefali Thanawala1, R Abiraamasundari2, Rajat Shah1
1Nutriventia Limited, Mumbai 400069, Maharashtra, India.
Pharmaceutics
|October 26, 2024
概括
与立即释放的黑激素相比,新的持续释放的黑激素 (Melatonin-SR) 提供了更好的药理动力学特征. 这种新型配方提供更长时间的血度,可能增强睡眠周期调节.
科学领域:
- 药理学 药理学是指药理学的学科.
- 营养学科学 营养学科学
- 睡眠医学 睡眠医学
背景情况:
- 外源性黑激素由于生物可用性差和半衰期短,需要高,频繁的剂量,影响睡眠障碍管理.
- 开发持续释放的黑激素配方对于实现长时间的治疗效果和一致的血度至关重要.
- 新的5毫克持续释放的黑激素囊 (Melatonin-SR) 是为了解决这些局限性而开发的.
研究的目的:
- 为了比较Melatonin-SR与立即释放的黑色素 (Melatonin-IR) 的药理动力学和安全性.
- 评估关键的药理动力学参数,包括Cmax,Tmax,AUC和消除半衰期 (t1/2).
- 在健康的成年人中评估黑色素-SR的耐受性.
主要方法:
- 一项开放标签,随机化,交叉研究,涉及16名健康成年人 (18-45岁).
- 参与者接受了单次口服剂量5毫克 Melatonin-SR和5毫克 Melatonin-IR在两个单独的时间段与7天的洗.
- 监测了药理动力学参数和不良事件.
主要成果:
- 与梅拉托尼-IR (1.01小时) 相比,梅拉托尼-SR的平均清除半衰期 (5.10小时) 显著更长,增加了五倍.
- 黑色素SR的Cmax (11,446.87 pg/mL) 比黑色素IR的Cmax (22,786.30 pg/mL) 低,这表明峰值度降低.
- 黑素-SR (1.26小时) 与黑素-IR (0.87小时) 的平均Tmax略长. 只有一个不良事件 (吐) 发生在 Melatonin-IR.
结论:
- 黑色素-SR在长时间内表现出持续的血黑色素度,这表明药物动力学特性得到改善.
- 健康参与者能很好地容忍梅拉素-SR配方.
- 持续释放的黑激素为支持健康睡眠模式和管理睡眠障碍提供了一个有前途的营养药物选择.
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