Nifedipine controlled-releasing tablet and preparation method thereof

Abstract

The invention discloses nifedipine controlled release medicament, which contains a pastille layer and a boosting layer with the proportion of 1: 0.5-3 by weight, wherein the pastille layer contains nifedipine and carrying agent which is the homopolymer of vinylpyrrohdone and / or copolymer of vinylpyrrohdone and is 40-99% of the pastille layer, the boosting layer includes infiltration promoting polymer which is 10-80% of the boosting layer by weight, insoluble polymer which is 10-80% of the boosting layer by weight, and the other component is osmotic pressure accelerant The rate of medicament releasing controlled by nifedipine can make the medicament release the nifedipine in 24 hours by administering drug once a day.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to an osmotic pump drug delivery preparation containing the active drug nifedipine and a preparation method thereof. Dipine is capable of being released in a manner that controls the release of the active ingredient. Background technique [0002] Nifedipine is a dihydropyridine antihypertensive drug, the chemical name is 2,6-dimethyl-4(2-nitrophenyl)-1,4-dihydro-3,5-pyridinedicarboxylic acid Dimethyl ester is mainly used in the treatment of cardiovascular diseases such as angina pectoris and hypertension. The main mechanism of action of nifedipine in the human body is to reduce the entry of calcium ions into cells through slow calcium channels, and it specifically acts on smooth muscle cells of cardiomyocytes, coronary arteries and peripheral resistance vessels, showing a significant antihypertensive effect. The common preparation of nifedipine has low bioavailability, i...

AI Technical Summary

Problems solved by technology

However, osmotic pump controlled-release tablets with PEO as the main auxiliary material have some inherent disadvantages: the water absorption rate and hydration rate of polyoxyethylene are slow, so the drug release time lag is long, resulting in the drug not taking effect quickly after taking; The typical glass transition temperature of polyoxyethylene ranges from 65°C to 67°C. Therefore, PEO does not have ideal thermal stability. It has the following problems in the process of preparation and storage in industrial production: it is difficult to dry the solvent in the granulation process, Since the drying temperature should generally not exceed 40°C, it is easy to cause a high residual amount of organic solvents. If the drying is to be relatively complete, a relatively long drying time is required; the storage temperature of the tablet should not be too high. The physical and chemical properties of ethylene oxide change, which affects the release behavior of the tablet; in the process of high-speed tablet compression, if the die generates heat after repeated use and the temperature reaches about 50°C, adverse phenomena such as sticking and punching are prone to occur, so it is necessary to Special cooling facilities to control the temperature of the die

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