Section of Pharmaceutical Technology, Department of Pharmacy, School of Health Sciences, National and Kapodistrian University of Athens, Panepistimioupoli-Zografou, Athens 15784, Greece.
Section of Pharmaceutical Chemistry, Department of Pharmacy, School of Health Sciences, National and Kapodistrian University of Athens, Panepistimioupoli-Zografou, Athens 15784, Greece.
Curr Pharm Des. 2024;30(18):1433-1441. doi: 10.2174/0113816128304967240328065809.
In an attempt to circumvent the lipophilicity burden for the oral administration of new potent synthetic melatoninergic fluorine-substituted methoxyphenylalkyl amides, we conducted modified release studies using carefully selected matrix tablets' biopolymeric materials in different ratios.
In particular, we sought to attain release profiles of these analogues similar to that of the parent compound, the chronobiotic hormone Melatonin (MLT), and also of the commercially available drug, Circadin.
It was found that some of these systems, albeit being more lipophilic than MLT, mimic the release patterns of melatonin and Circadin.
Moreover, a number of these derivatives were proven suitable for dealing with sleep onset problems, whilst others for dealing with combined sleep onset/sleep maintenance dysfunctions.
为了规避新型强效合成褪黑素类氟取代甲氧基苯烷基酰胺经口服给药的亲脂性负担，我们使用经过精心挑选的基质片剂中的生物聚合物材料以不同比例进行了改良释放研究。
特别是，我们试图使这些类似物的释放曲线与母体化合物、生物钟激素褪黑素（MLT）以及市售药物 Circadin 的释放曲线相似。
结果发现，尽管这些系统比 MLT 更亲脂，但它们模拟了褪黑素和 Circadin 的释放模式。
此外，这些衍生物中的一些被证明适合于处理睡眠起始问题，而另一些则适合于处理睡眠起始/维持功能障碍。
