Source: http://ubphj.nuph.edu.ua/article/view/ubphj.18.169
Timestamp: 2019-04-19 00:57:34+00:00

Document:
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.
Kolychev, I.O., Koshovyi, O. M., Zahaiko, A. L., Krasnikova, T. O., Kovalova, A. M. (2016). Farmakom, 1, 67–73.
Ruban, E. A., Kolisnyk, T. E., Slipchenko, G. D. (2015). Annals of Mechnikov Institute, 4, 17–24.
Koshovyi, O. M., Zahaiko, A. L., Kolychev, I.O., Fylymonenko, V. P., Komisarenko, A. M. (2016). Sposib oderzhannia likuvalno–profilaktychnoho zasobu iz hipohlikemichnoiu diieiu z lystia chornytsi zvychainoi. Pat. 111134 Ukraine, MPK A61K 36/45, A61K 31/195, A61K 31/05, A61P 3/10; declared 30.06.2015, published 25.03.2016, № 26.
14. Derzhavna Farmakopeia Ukrainy : v 3 tomakh. (2015). Kharkiv: Ukrainskyi naukovyi farmakopeinyi tsentr yakosti likarskykh zasobiv, 1, 1128.
16. European convention for the protection of vertebrate animals used for experimental and other scientific purposes. (1986).Strasbourg : Council ofEurope, 52.
Higa, T. S., Spinola, A. V., Fonseca–Alaniz, M. H., Evangelista, F. S. (2014). Comparison between cafeteria and high–fat diets in the induction of metabolic dysfunction in mice. Int J Physiol Pathophysiol Pharmacol, 6 (1), 47–54.
5. Перспективи створення нового гіпоглікемічного лікарського засобу на основі біологічно активних речовин листя чорниці звичайної / І. О. Количев, О. М. Кошовий, А. Л. Загайко та ін. // Фармаком. – 2016. – № 1. – С. 67–73.
8. Рубан, Е. А. Перспективы создания противодиабетических препаратов на основе полифенолов : механизмы гипогликемического действия и фармакокинетика / Е. А. Рубан, Т. Е. Колиснык, Г. Д. Слипченко // Annals of Mechnikov Institute. – 2015. – № 4. – С. 17–24.
13. Пат. 111134 Україна, МПК A 61 K 36/45, A 61 K 31/195, A 61 K 31/05, A 61 P 3/10. Спосіб одержання лікувально–профілактичного засобу із гіпоглікемічною дією з листя чорниці звичайної / Кошовий О. М., Загайко А. Л., Количев І. О., Филимоненко В. П., Комісаренко А. М. – Заявл.: 30.06.2015; опубл.: 25.03.2016. – Бюл. № 26.
14. Державна фармакопея України : в 3-х т. / Державне підприємство «Український науковий фармакопейний центр якості лікарських засобів». – 2–е вид. – Х. : Український науковий фармакопейний центр якості лікарських засобів, 2015. – Т. 1. – 1128 с.
15. Guide for the care and use of laboratory animals. – 8-th ed. –Washington: The National Academies Press, 2011. – 246 p.
16. European convention for the protection of vertebrate animals used for experimental and other scientific purpose. –Strasbourg: Council ofEurope, 1986. – 52 p.
19. Comparison between cafeteria and high–fat diets in the induction of metabolic dysfunction in mice / T. S. Higa, A. V. Spinola, M. H. Fonseca–Alaniz, F. S. Evangelista // Int. J. Physiol. Pathophysiol. Pharmacol. – 2014. – Vol. 6. – P. 47–54.

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