Formulation design and evaluation of the physicotechnical and hypoglycaemic properties of tablets containing Dioscorea dumetorum fraction in alloxanized diabetic rats

Document Type : Original article

Authors

Department of Pharmaceutics and Pharmaceutical Technology, Faculty of Pharmaceutical Sciences, Nnamdi Azikiwe University, Awka, Anambra State, Nigeria

10.30495/medherb.2021.686193

Abstract

Background & Aim: There is increasing interest in the quest for safe and relatively inexpensive medicines from natural products for the treatment of diabetes mellitus (DM). Thus, the main thrust of this study was to formulate and evaluate the anti-diabetic activity of tablets containing aqueous fraction of Dioscorea dumetorum (bitter yam).
Experimental: D. dumetorum was extracted using ethanol followed by aqueous fractionation. A rational amount (200 mg) of the fraction (drug) was blended used to produce seven batches of granules by wet granulation and their micromeritic profiles were determined. The granules were compressed into seven batches of tablets and quality control tests including weight uniformity, crushing strength, friability, drug content, disintegration, and dissolution profiles were undertaken. Anti-diabetic activity of the tablets was assayed using alloxan-induced diabetic rats.
Results: Results showed that the granules had good flow properties and compressibility. Tablets produced had good uniformity of weight (0.64 ± 0.01 to 0.66 ± 0.01 g), hardness (4.33 to 8.67 kgf), were less friable (0.05 ± 0.03 to 0.31 ± 0.04 %) with high drug content (98.91 ± 0.55 to 101.39 ± 0.92 %), had acceptable disintegration time (6.44 ± 0.46 to 14.05 ± 0.42 min) for normal release tablets, and recorded 70 – 100 % drug release in 60 min. The result of the anti-diabetic activity study showed that the tablets had blood glucose lowering ability similar to metformin tablet, and therefore could be used as an important alternative in the treatment of diabetes. 
Recommended applications/industries: Aqueous fractions of D. dumetorum should be further purified and used in the preparation of tablets for the treatment of diabetes mellitus. Extraction and fractionation methods for the plant should be made reproducible for easier industrial application.

Keywords


Article Title [فارسی]

طراحی فرمولاسیون و ارزیابی خواص فیزیکو تکنیکی و هیپوگلیسمی قرص های حاوی فراکشن Dioscorea dumetorum در موش های صحرایی دیابتی شده با آلوکسان

Authors [فارسی]

  • آزوبیکه اوکولی
  • چوکووبوکا اومیور
  • کالیستوس نواکیله
  • ابره اوکویی
  • توچوکو او ککه
  • امانوئل اوروناچی
گروه داروسازی و فناوری دارویی، دانشکده علوم دارویی، دانشگاه Nnamdi Azikiwe، Awka، ایالت آنامبرا، نیجریه
Abstract [فارسی]

Background & Aim: There is increasing interest in the quest for safe and relatively inexpensive medicines from natural products for the treatment of diabetes mellitus (DM). Thus, the main thrust of this study was to formulate and evaluate the anti-diabetic activity of tablets containing aqueous fraction of Dioscorea dumetorum (bitter yam).
Experimental: D. dumetorum was extracted using ethanol followed by aqueous fractionation. A rational amount (200 mg) of the fraction (drug) was blended used to produce seven batches of granules by wet granulation and their micromeritic profiles were determined. The granules were compressed into seven batches of tablets and quality control tests including weight uniformity, crushing strength, friability, drug content, disintegration, and dissolution profiles were undertaken. Anti-diabetic activity of the tablets was assayed using alloxan-induced diabetic rats.
Results: Results showed that the granules had good flow properties and compressibility. Tablets produced had good uniformity of weight (0.64 ± 0.01 to 0.66 ± 0.01 g), hardness (4.33 to 8.67 kgf), were less friable (0.05 ± 0.03 to 0.31 ± 0.04 %) with high drug content (98.91 ± 0.55 to 101.39 ± 0.92 %), had acceptable disintegration time (6.44 ± 0.46 to 14.05 ± 0.42 min) for normal release tablets, and recorded 70 – 100 % drug release in 60 min. The result of the anti-diabetic activity study showed that the tablets had blood glucose lowering ability similar to metformin tablet, and therefore could be used as an important alternative in the treatment of diabetes. 
Recommended applications/industries: Aqueous fractions of D. dumetorum should be further purified and used in the preparation of tablets for the treatment of diabetes mellitus. Extraction and fractionation methods for the plant should be made reproducible for easier industrial application.

Keywords [فارسی]

  • Diabetes mellitus
  • Dioscorea dumetorum
  • Metformin
  • Micromeritics
  • Physicotechnical
  • Tablets
Ahmed, M.F., Kazim, S.M., Ghori, S.S., Mehjabeen, S.S., Ahmed, S.R., Ali, S.M., and Ibrahim, M. 2010. Antidiabetic activity of Vinca rosea extracts in alloxan-induced diabetic rats. International Journal of Endocrinology, 2010: 841090.
Anioke, I., Okwuosa, C., Uchendu, I., Chijioke, O., Dozie-Nwakile, O., Ikegwuonu, I., Kalu, P., and Okafor, M. 2017. Investigation into hypoglycemic, antihyperlipidemic, and renoprotective potentials of Dennettia tripetala (pepper fruit) seed in a rat model of diabetes. BioMed Research International, 9: 1– 11.
Baviskar, D., Rajput, A., Bare, K., Biranwar, Y., Chaudhari, H., Narkhede, D., and Jain, D. 2014. Development and in vitro characterization of mebendazole delayed release tablet for colonic drug delivery. Pakistan Journal of Pharmaceutical Sciences, 27(2): 249 – 253.
British Pharmacopoiea.. 2012. British Pharmacopoeia Commission, Her Majesty’s Stationary Office, University Press, Cambridge. 2, A326-327
WHO Publication, 2021. Diabetes: Key Facts. Available on internet at https://www.who.int/news-room/fact-sheets/detail/diabetes.
Gadhiya, J., Jaithliya, T., Sehgal, S., and Somani, N. 2018. Herbals and its marketed formulations to treat diabetes mellitus: An overview. International Journal of Trends in Scientific Research and Development, 2(3): 2602– 2613
Hemamalini, K., and Vijusha, M. 2012. Antidiabetic activity of methanolic extracts of leaves of Anogeissus acuminata Roxburgh ex candolle and Solanum pubescens Willd by alloxan induced model in rats. Der Pharmacia Lettre, 4(5): 1445– 1460.
Iwu, M.M., Okunji, C.O., Ohiaeri, G.O., Akah, P., Corley, D., and Tempesta, M.S. 1990. Hypoglycaemic activity of dioscoretine from tubers of Dioscorea dumetorum in normal and alloxan diabetic rabbits. Planta Medica, 56: 264– 267.
Jayakumar, R.V. 2010. Herbal medicines for type-2 diabetes. International Journal of Diabetes in Developing Countries, 30(3): 150 – 152.
Kipo, S.L., Oppong, E.E., and Ofori-Kwakye, K. 2014. Physicochemical evaluation and tablet formulation properties of shea tree gum. Asian Journal of Pharmaceutical and Clinical Research, 7(5): 121–127.
Lorke, D. 1983. A new approach to practical acute toxicity testing. Archives of Toxicology, 54(4): 275– 287.
Malviya, N., Jain, S., and Malviya, S. 2010. Antidiabetic potential of medicinal plants. Acta Poloniae Pharmaceutica-Drug Research, 67(2): 113– 118.
Mahomed, I.M., and Ojewole, J.A. 2003. Hypoglycaemic effect of Hypoxis hemerocallidea corm (African potato) aqueous extract in rats. Methods and Findings in Experimental and Clinical Pharmacology, 25: 617- 623.
Obidiegwu, J.E., Lyons, J.B., and Chilaka, C.A. 2020. The Dioscorea genus (Yam) – An appraisal of nutritional and therapeutic potentials. Foods, 9: 1304.
Obitte, N.C., Ezeiruaku, H., and Onyishi, V.I. 2008. Preliminary studies on two vegetable oil-based self-emulsifying drug delivery system (SEDDS) for the delivery of metronidazole, a poorly water soluble drug. Journal of Applied Sciences, 8(10): 1950- 1955.
Okunlola, A., and Odeku, O.A. 2011. Evaluation of starches obtained from four Dioscorea species as binding agent in chloroquine phosphate tablet formulations. Saudi Pharmaceutical Journal, 19: 95–105.
Okunlola, A. 2015. Design of bilayer tablets using modified Dioscorea starches as novel excipients for immediate and sustained release of aceclofenac sodium. Frontiers in Pharmacology, 5: 294- 301.
Onyegeme-Okerenta, B.M., Onyeike, E.N., and Esialekpe, F.O. 2013. Effect of ethanol leaf extract of Millettia aboensis on selected haematological indices of Wistar albino rats. Global Advanced Research Journal of Medicinal Plants, 2(1): 4 – 11
Onyishi, I.V., Chime, S.A., and Ugwu, J.C. 2013. Evaluation of binder and disintegrant properties of starch derived from Xanthosoma sagittifolium in metronidazole tablets.  African Journal of Biotechnology, 12(20): 3064– 3070.
Pareek, H., Sharma, S., Khajja, B.S., Jain, K., and Jain, G.C. 2009. Evaluation of hypoglycemic and anti-hyperglycemic potential of Tridax procumbens (Linn.). BMC Complementary and Alternative Medicine, 9: 48 54.
Pujari, A.K., and Jadhav, N.R. 2019. Design and development of anti-diabetic tablet formulation containing spray dried extract of mulberry leaves. International Journal of Pharmaceutical Sciences and Research, 10(3): 1501– 1509.
Reginald-Opara, J.N., Attama, A., Ofokansi, K., Umeyor, C., and Kenechukwu, F. 2015. Molecular interaction between glimepiride and Soluplus®-PEG 4000 hybrid based solid dispersions: Characterisation and anti-diabetic studies. International Journal of Pharmaceutics, 496: 741– 750.
Salawu, S.O., Ajiboye, P.B., Akindahunsi, A.A., and Boligon, A.A. 2017. Antioxidant and anticholinesterase potential of two Nigerian bitter yams using a simulated gastrointestinal digestion model and conventional extraction. Preventive Nutrition and Food Science, 22(2): 107– 117.
Sparg, S.G., Light, M.E., and Van-Staden, J. 2004. Biological activities and distribution of plant saponins. Journal of Ethnopharmacology, 94(2-3): 219– 243.
Tiwari, S., Prasad, V., Chauhan, P.S., and Lata, C. 2017. Bacillus amyloliquefaciens confers tolerance to various abiotic stresses and modulates plant response to phytohormones through osmoprotection and gene expression regulation in rice. Frontiers in Plant Science, 8: 1510.
Tripathy, K.D. 2013. Essentials of medical pharmacology, Seventh ed. Jaypee Brothers Medical Publishers (P) Ltd, New Delhi, pp. 258.
Ukwueze, C.O., Onoja, S.O., and Ezeja, M.I. 2015. Experimental evaluation of analgesic and antioxidant effects of hydromethanolic extract of Dioscorea dumetorum tuber. Journal of Advances in Medical and Pharmaceutical Sciences, 3(3): 131– 137
Umeyor, C., Anaka, E., Kenechukwu, F., Agbo, C., and Attama, A. 2016. Development, in vitro and in vivo evaluations of novel lipid drug delivery system of Newbouldia laevis (P. Beauv.). Nanobiomedicine, 3: 1- 17
Umeyor, C.E., Okoye, I., Uronnachi, E., Okeke, T., Kenechukwu, F., and Attama, A. 2021. Repositioning miconazole nitrate for malaria: Formulation of sustained release nanostructured lipid carriers, structure characterization and in vivo antimalarial evaluation. Journal of Drug Delivery Science and Technology, 2021, 61: 102125.
USP 32, 2009. The U.S. Pharmacopioeal Convention, Rockville. 2: 2113- 2116.