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


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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.

About the authors

Marilena Vlachou

Section of Pharmaceutical Technology, Department of Pharmacy, School of Health Sciences,, National and Kapodistrian University of Athens

Author for correspondence.
Email: info@benthamscience.net

Angeliki Siamidi

Section of Pharmaceutical Technology, Department of Pharmacy, School of Health Sciences, National and Kapodistrian University of Athens

Email: info@benthamscience.net

Chrystalla Protopapa

Section of Pharmaceutical Technology, Department of Pharmacy, School of Health Sciences,, National and Kapodistrian University of Athens

Email: info@benthamscience.net

Michalis Vlachos

Section of Pharmaceutical Chemistry, Department of Pharmacy, School of Health Sciences,, National and Kapodistrian University of Athens

Email: info@benthamscience.net

Sophia Kloutsou

Section of Pharmaceutical Chemistry, Department of Pharmacy, School of Health Sciences, National and Kapodistrian University of Athens

Email: info@benthamscience.net

Chrysoula-Christina Dreliozi

Section of Pharmaceutical Chemistry, Department of Pharmacy, School of Health Sciences,, National and Kapodistrian University of Athens

Email: info@benthamscience.net

Ioannis Papanastasiou

Section of Pharmaceutical Chemistry, Department of Pharmacy, School of Health Sciences, National and Kapodistrian University of Athens

Email: info@benthamscience.net

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