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Research Article

<i>In vitro</i> Modified Release Studies on Melatoninergic Fluorinated Phenylalkylamides: Circumventing their Lipophilicity for Oral Administration

[ Vol. 30 , Issue. 18 ]

Author(s):

Marilena Vlachou*, Angeliki Siamidi, Chrystalla Protopapa, Michalis Vlachos, Sophia Kloutsou, Chrysoula-Christina Dreliozi and Ioannis P. Papanastasiou   Pages 1433 - 1441 ( 9 )

Abstract:


Introduction: In an attempt to circumvent the lipophilicity burden for the oral administration of new potent synthetic melatoninergic fluorine-substituted methoxyphenylalkyl amides, we conducted in vitro modified release studies using carefully selected matrix tablets’ biopolymeric materials in different ratios.

Method: 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®.

Result: It was found that some of these systems, albeit being more lipophilic than MLT, mimic the in vitro release patterns of melatonin and Circadin®.

Conclusion: 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.

Keywords:

Melatonin, synthetic melatoninergic analogues, lipophilicity, matrix tablets, <i>in vitro</i> dissolution studies, oral administration.

Affiliation:



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