Pharmacological evaluation of sustained release matrix tablets containing Vaccinium myrtillus leaf dry extract as an alpha-glucosidase inhibitory drug
Keywords:Vaccinium myrtillus leaves, herbal extract, matrix tablets, diabetes mellitus, alpha-glucosidase inhibition, hamsters
Vaccinium myrtillus leaves are the source of natural polyphenols known to improve glycemic control in diabetic conditions through different mechanisms including intestinal a-glucosidase inhibition. In order to increase the effectiveness of V. myrtillus leaf dry extract as a-glucosidase inhibitory drug its sustained release matrix tablets have been developed.
Aim. To carry out the pharmacological evaluation of V. myrtillus leaf dry extract and its sustained release matrix tablets as a-glucosidase inhibitory agents.
Materials and methods. The matrix tablets were prepared by te wet granulation method. Experimental alimentary metabolic syndrome with persistent insulin resistance was induced in Syrian hamsters by feeding them with highly palatable fat- and sugar rich diet for 12 weeks. From the tenth week of the diet feeding, the pathological hamsters were treated with V. myrtillus leaf dry extract, its sustained release matrix tablets and voglibose tablets as a reference drug. At the end of the treatment period an oral maltose loading test with the determination of blood glucose and serum insulin concentration dynamics was performed. Vaccinium myrtillus leaf dry extract (VMLDE) was obtained according to the method developed under the supervision of Dr. O. Koshoviy (Department of Pharmacognosy, National University of Pharmacy, Kharkiv, Ukraine) . The excipients used to manufacture sustained release matrix tablets were hypromellose (HPMC) of grades Methocel K4M and Methocel K100LV (Dow Chemical Company, USA), Eudragit L100 (Evonik, Germany), microcrystalline cellulose (MCC) of a grade Avicel PH101 (FMC BioPolymer, USA), Plasdone S-630 (Ashland Inc., USA) and magnesium stearate (S.D. Fine. Chemicals Ltd., India). The tablets containing 0.2 mg of voglibose (“Voksid” produced by Kusum Pharm LLC, Ukraine), a marketed α-glucose inhibitor, were used as a reference drug in this study. Methods used : preparation of sustained release matrix tablets, induction of metabolic syndrome and experimental design, biochemical tests, statistical analysis.
Results and discussion. By all markers studied in this work the effectiveness of matrix tablets containing V. myrtillus leaf dry extract exceeded that one of the pure extract and statistically significantly did not differ from reference drug.
Conclusions. V. myrtillus leaf dry extract and its matrix tablets possess the antidiabetic action through several mechanisms, including, but not only intestinal a-glucosidase inhibition, therefore they can be considered as promising agents in diabetes and metabolic syndrome treatment.
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