Diltiazem hydrochloride control release capsule and its preparing method

Abstract

The present invention relates to controlled releasing diltiazem hydrochloride capsule as a kind of organic coated pill medicine preparation and its preparation process. Each capsule contains diltiazem hydrochloride pill in 90-180 mg. The medicine pill consists of: medicine pill containing 50-75 wt% of the medicine; one release controlling film layer, which is outside the pill, water insoluble and medicine permeable, comprises polymer, enteric soluble material, plasticizer and lubricant, and is in the amount of 5-20 wt% of the pills; and one fast releasing medicine layer, which is outside the release controlling film layer, comprises diltiazem hydrochloride and water soluble adhesive, and is in the amount of 5-35 wt% of the coated pill. The medicine preparation can maintain the concentration of diltiazem hydrochloride in blood plasma within the treating window for 24 hr.

Description

Technical field [0001] The invention relates to a pharmaceutical formulation characterized by a pellet shape that uses an organic coating layer to continuously release a drug and a preparation method thereof, in particular to a capsule prepared from a controlled release coated pellet containing the antihypertensive drug diltiazem hydrochloride and the same Preparation. Background technique [0002] Diltiazem hydrochloride is a calcium channel blocker for the treatment of angina pectoris and hypertension. In most sustained-release drug formulations, the drug is released from the membrane-controlled coating layer after taking the drug. The release rate obeys Fick's law of diffusion. The release rate is proportional to the amount of drug remaining in the formulation and proportional to the porosity of the film. For membrane-controlled pellets with fixed porosity, the drug release rate must be a decelerating process, which is faster at the beginning and slows down continuously. This ...

AI Technical Summary

Problems solved by technology

Existing diltiazem hydrochloride sustained-release preparations have capsules made from sustained-release tablets and sustained-release pellets: as disclosed in U.S. Patent No. 4894240, a diltiazem hydrochloride controlled-release pellet preparation that is taken orally once a day, the preparation In addition to the drug ingredient diltiazem hydrochloride in the controlled release film layer of the medium controlled release pellet, an organic acid must be added to regulate the release of the drug at a set speed. Another controlled release hydrochloric acid diltiazem disclosed in U.S. Patent No.4917899 Diltiazem pellet preparation, which is composed of a slow-release pellet and a quick-release pellet filled in the same hard capsule; CN1185104A also discloses a product and preparation method of diltiazem hydrochloride controlled-release preparation, in order to achieve It is taken once within 24 hours, and the drug release is close to constant rate or zero-order release. The drug is also made into two kinds of pellets with different drug release rates, which are mixed and packed in a single dosage system. Such preparations exist The disadvantage is that two kinds of small pills with different drug release rates need to be manufactured separately, the process is complicated and cumbersome, and the two kinds of small pills are different in size, specific gravity and proportion, which will cause uneven mixing, so that the expected drug effect cannot be achieved.