Azelnidipine composition
A technology of azeldipine and its composition, which is applied in the field of azeldipine composition and its preparation, can solve the problems of difficult production of azelnidipine solid preparations and low bioavailability, and improve bioavailability and bioavailability , The effect of bioavailability improvement
Active Publication Date: 2011-03-30
QINGDAO HUANGHAI PHARM CO LTD
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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
Method used
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Experimental program
Comparison scheme
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Embodiment 1
[0028] Preparation of Azedipine Composition
[0029] Azedipine 8g, ethyl acetate 50ml, stir to dissolve, add β-cyclodextrin 40g, stir until paste, remove ethyl acetate under 50Pa to obtain azedipine composition.
Embodiment 2
[0031] Preparation of Azedipine Composition
[0032] Azedipine 8g, ethyl acetate 65ml, stir to dissolve, add β-cyclodextrin 56g, stir until paste, remove ethyl acetate under 50Pa to obtain azedipine composition.
Embodiment 3
[0034] Preparation of Azedipine Composition
[0035] Azedipine 8g, ethyl acetate 100ml, stir to dissolve, add β-cyclodextrin 120g, stir until paste, remove ethyl acetate under 50Pa to obtain azedipine composition.
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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...
Claims
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IPC IPC(8): A61K31/4427A61K47/48A61P9/10A61P9/12A61K47/40A61K47/61
Inventor 孙桂荣吴立明
Owner QINGDAO HUANGHAI PHARM CO LTD
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