FORMULATION AND TECHNOLOGY OF ORODISPERSIBLE TABLETS OF APIGENIN WITH POTENTIAL ANTIHYPERTENSIVE ACTION
Keywords:Arterial hypertension, Apigenin, Orodispersible tablets
Arterial hypertension is the most common chronic disorder in economically developed countries leading to chronic disability and lethal outcome. During the recent years the attention of the researchers was focused on identifying new endogenous substances involved in vasoconstriction and vasodilation mechanisms. In this direction special attention is paid to vasodilating products of epoxygenic metabolism such as epoxyeicosatrienoic acids (EETs), whose rapid conversion in the body into less active metabolites such as dihydroxyeicosatrienoic acids (DHETs) is promoted by enzymatic epoxide hydrolase (sHE). According literature sources biologically active substance of plant origin – apigenin has the ability to inhibit sEH action, promoting the prolongation of EETs vasodilating activity. In the treatment of arterial hypertension, special attention is paid to the ability of the patient to use the drug independently, without any additional materials (water, syringe, etc.) and rapid action. Based on pharmacological studies plant origin phenolic compound sEH inhibitor-Apigenin by enhancing EETs vasodilatory activity provide beneficial effect on hemodynamic parameters and baroreflex sensitivity in hypertensive state being promising agent for improvement of different cardiovascular disorders. Based on artificial intelligence and biopharmaceutical studies, the formulation of apigenin orodispersible tablets and its technology was developed by sublimation method. As it was shown ODT of apigenin meet standard requirements in terms of quality. The use of sodium starch glycolate as disintegrant ensures the accelerated absorption of water into the tablets, which reduces the binding force between the particles and causes the tablets disintegration.
Ankit A., Kiran Kumar G.B., Madhu B.K. Formulation and evaluation of orodispersible tablets of Dimenhydrinate by using co-processed superdisintegrants/Journal of Science, Engineering and Technology. June 2016; 12(1):23-33.
Anupam Roy, Orodispersible tablets: a Review, Asian J Pharm Clin Res, 2016; 9(1):19-26.
Bellien J, Joannidis R. Epoxyeicosatrienoic acid pathway in human health and diseases. J. of Cardiovasc. Pharmacol. 2013; 61:188-96.
Blasco Alejandro, Torrado Guillermo and Peña M Ángeles. Formulation and Evaluation of Loperamide HCl Oro Dispersible Tablets. - Pharmaceuticals 2020, 13, 100; doi:¬10.3390¬/ph-13050100.
Campbel W.B. Imig J.D. Schmitz J.M., Falck J.R. Orally Active Epoxyeicosatrienoic Acid Analogs. Journal of Cardiovascular Pharmacology. 2017; 70:211-224.
Capdevila J, Wang W. Role of cytochrome p-450 epoxygenase in regulating renal membrane transport and hypertension. Curr. Opin. Nephrol. Hypertens. 2013; 22:163–169.
Kezeli T, Gongadze N, Sukoyan G, Shikhashvili M, Chapichadze Z, Okujava M, Dolidze N. Circadian Variation in Vasoconstriction and Vasodilation Mediators and Baroreflex Sensitivity in Hypertensive Rats. J Circadian Rhythms. 2019 Oct 14;17:10. doi: 10.5334/jcr.185.
Darshana Pravinchandra Panhale, Rishikesh Shankar Bachhav, Sheetal Bhaskar Gondkar. Formulation and Evaluation of Orodispersible Tablets of Apremilast by Inclusion Complexa¬tion using β-Cyclodextrin. - Indian J of Pharmaceutical Education and Research. 2021; 55(1s): s112-s121.
Ettehad D. et al. Blood pressure lowering for prevention of cardiovascular disease and death: A systematic review and meta-analysis. Lancet. 2016; 387(10022):957-967.
Fan F, Muroya Y, Roman R. J. Cytochrome P-450 eicosanoids in hypertension and renal disease. Curr. Opin. Nephrol. Hypertens. 2015; 24(1): 37-46.
Fleming J. The pharmacology of the cytochrome P-450 epoxygenase/soluble epoxide hydrolase axis in the vasculature and cardiovascular disease. Pharmacol. Rev. 2014; 66: 1106-1140.
Imig J.D. Epoxyeicosanoids in Hypertension. Physiol. Res. 2019; 68: 695–704.
Imig J.D. Prospective for cytochrome P-450 epoxygenase cardiovascular and renal therapeutics. Pharmacol. Ther. 2018; 192: 1-19.
Jiang H, Quilley J, Doumad A.B, Zhu A. B., Falck J.R., et al. Increases in plasma trans-EETs and blood pressure reduction in spontaneously hypertensive rats. Am. J. Physiol. Heart Circ. Physiol. 2011; 300(6): H1990-H1996.
K Kareemuddin Ansari, Neeraj Sharma. Formulation and evaluation of orodispersible tablets of lornoxicam. - Journal of Drug Delivery & Therapeutics. 2018; 8(6):225-228.
Khan A.H, Pavlov T.S, Christian S.V, et al. Epoxyeicosatrienoic acid analogue lowers blood pressure through vasodilation and sodium channel inhibition. Clin. Sci. 2014; 127: 463-474.
Mills K.T, Bundy J.D, Kelly T.N, et al. Global Disparities of Hypertension Prevalence and Control: A Systematic Analysis of Population-Based Studies From 90 countries. Circulation. 2016; 134:441-450.
Papiashvili N, Gongadze N, Bakuridze A, Bakuridze K. Antihypertensive and cardioprotective effect of epoxyeicosatrienoic acid analog and soluble epoxide hydrolase inhibitors. Georgian Medical News, 2021, 3(312): 125-131.
Papiashvili N. Bakuridze K. Ghongadze M. Bakuridze A. Ghongadze N. Influence of plant origin soluble epoxide hydrolase inhibitors on hemodynamic parameters in hypertensive rats. European J. of clinical pharmacology, 2022; 78 (1):38-38.
Redina O.E, Abramova T.O, Klimov L.O, Ryazanova M.A, et al. Soluble epoxide hydrolase (sEH) as a potential target for arterial hypertension therapy. Russian J. of Genetics; 2017; 53: 972-981.
Rewar S, Singh C J, Bansal B K, Pareek R, Sharma A K. Oral dispersible tablets: an overview; development, technologies and evaluation - International Journal of Research and Development in Pharmacy and Life Sciences - 2014, Vol.3, No.6, No.4, 1223-1235.
Tacconelli S, Partignani P. Inside epoxyeicosatrienoic acids and cardiovascular disease. Frontiers in pharmacology. 2014; 5; 239.
Vishali T, Damodharan N. Orodispersible Tablets: A Review - Research J. Pharm. And Tech. 2020; 13(5); 2522-2529.
Vivek D., Renu BY., Richa A., Atul KS. Formulation and evaluation of orally dispersible tablets of Chlorpheniramine maleate by fusion method, J. of Marmara Pharmaceutical. 2017; 21:67-77.
Wang C.Y, Lee S, Jang H.J, Su X.D. et al. Inhibition potential of phenolic constituents from the aerial parts of Tetrastigma hemsleyanum against soluble epoxide hydrolase and nitric oxide synthase. J. of Enzyme Inhibition and Medicinal Chemistry. 2019; 34(1): 753-760.