FORMULATION AND TECHNOLOGY OF ORODISPERSIBLE TABLETS OF APIGENIN WITH POTENTIAL ANTIHYPERTENSIVE ACTION

Abstract

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.