Pharmacokinetic Studies And Tissue Distribution Of M-nisoldipine Polymorphs In Rats

Among the various drugs currently available for the treatment of systematic hypertension, the calcium channel antagonists (CCAs) continue to receive much attention as a result of their benefits in the prevention of cardiovascular events and other complications. m-nisoldipine (Fig.1), as a new dihydropyridine calcium ion antagonist, was firstly composed in School of Pharmacy, Hebei Medical University. It is stable in the form of solid when exposed to light, while nisoldipine almost lost activity under lighting condition for 30 min. A comparison with nisoldipine showed that m-nisoldipine increased cardiac output and cardiac index significantly, and equally effect on rabbits in decreasing mean arterial blood pressure and increasing regional blood flow. The negative inotropic effect of m-nisoldipine on myocardium was dramatically less potent than that of nisoldipine. As a result, m-nisoldipine has relatively higher selectivity on the thoracic aorta than nisoldipine.Objective: To study physical and chemical properties of m-nisoldipine polymorphs and to identify the two different polymorphs, so as to preparing for pharmacokinetic study of A and B polymorphs. To develop a sensitive and specific liquid...