Azelnidipine composition

Abstract

The invention discloses an Azelnidipine composition, which consist of Azelnidipine and beta-cyclodextrin, wherein the dosage by weight of the beta-cyclodextrin is 3 to 15 times of that of the Azelnidipine, and the Azelnidipine is enveloped in a hydrophobic cavity of the cyclodextrin. The bioavailability of the Azelnidipine composition is obviously improved compared with a common preparation of the Azelnidipine, which lays a foundation for further development of a new oral preparation of the Azelnidipine.

Description

technical field [0001] The invention relates to a pharmaceutical composition of a dihydropyridine calcium ion antagonist, in particular to an azedipine composition, a preparation method and a preparation application thereof. Background technique [0002] The morbidity and mortality of cardiovascular, cerebrovascular and renal vascular diseases in my country are increasing year by year, and there is a trend of gradually getting younger. Azedipine is a dihydropyridine calcium ion antagonist, which can specifically inhibit the membrane potential-dependent L-type calcium channel of vascular smooth muscle cells. lead to a hypotensive effect. Can control blood pressure smoothly, increase cardiac output, have little effect on heart rate, and do not cause reflex tachycardia. Azedipine is therefore particularly suitable for the long-term treatment of hypertensive patients with underlying cardiac ischemia. [0003] [0004] Azedipine [0005] However, in the research and applic...

AI Technical Summary

Problems solved by technology

[0005] However, in the research and application of oral preparations of azedipine, it is found that its bioavailability is relatively low, and ordinary preparations need to add surfactants such as Tween-80 to improve bioavailability

Since Tween is an oily compound, it brings difficulties to the production of solid preparations of Azedipine

Images