Propafenone hydrochloride sustained-release capsule and preparation method thereof

Abstract

The invention relates to a propafenone hydrochloride sustained-release capsule and a preparation method thereof. The propafenone hydrochloride sustained-release capsule is prepared by filling sustained-release micro-tablets with the diameter of 2-3 mm, and has good dosage dispersion and uniformity. The micro tablets are composed of propafenone hydrochloride, a framework material, a lubricant and a diluent. The framework material is one or more of methyl cellulose, ethyl cellulose, hydroxypropyl methylcellulose and povidone; and a usage amount of the framework material is 1%-10%. The lubricant is one or more of sodium stearyl fumarate, magnesium stearate, micro-powder silica gel, talcum powder, calcium stearate and polyethylene glycol; and a usage amount of the lubricant is 0.1%-1.5%. The diluent is one or more of sucrose, mannitol, microcrystalline cellulose, lactose and polyethylene glycol; and a usage amount of the diluent is 2%-12%. According to the propafenone hydrochloride sustained-release capsule, the usage amount of a main drug is 77%-98%; and propafenone level in blood plasma reaches the maximum value 3-8 hours after drug delivery. The propafenone hydrochloride sustained-release capsule is stable in drug release and has a good sustained-release effect. An object of the invention is to provide a preparation method of the propafenone hydrochloride sustained-release capsule. The preparation method is simple in process, high in yield, good in stability and suitable for large-scale production.

Description

technical field [0001] The invention relates to a propafenone hydrochloride preparation, especially a slow-release preparation and a preparation method thereof. Background technique [0002] Propafenone hydrochloride (C 21 h 27 NO 3 HCl) is a class Ic antiarrhythmic drug with local anesthetic effect, and its main function is to block the sodium ion channel of cardiomyocytes. Clinically used for the treatment of ventricular, sinus, supraventricular tachycardia and pre-excitation syndrome. It was synthesized for the first time by German Hxlppharm company in 1975, and successfully imitated in my country in 1982. Commonly used oral preparations start to act 0.5 to 1 hour after taking them, reach the peak plasma concentration in 2 to 3 hours, and last for 4 to 8 hours. Therefore, the therapeutic dose of ordinary tablets is taken 3 to 6 times a day, which brings a lot of inconvenience. Moreover, the adverse reactions mostly appear at the peak time after administration, so the...

AI Technical Summary

Problems solved by technology

[0005] In 2003, the Propafenone Hydrochloride Sustained-release Capsules (12-hour sustained release) developed and produced by Abbott Laboratories of the U.S. went on the market. It is a kind of 2×2mm micro-tablets packed into capsules, and each capsule contains about 50-60 micro-tablets. The technical solution is disclosed in the PCT patent Chinese document CN1120312A, which is characterized in that propafenone hydrochloride and its auxiliary substances are prepared into micro-tablets. Sustained release of propafenone, its preparation process is complicated, and there are many types of excipients, which is not conducive to human body absorption and metabolism, and the clinical safety of the drug needs to be improved

[0011] The above domestic propafenone hydrochloride sustained-release preparations prepared by coating / skeleton and other sustained-release technologies have achieved sustained-release effects to a certain extent, but there are disadvantages: (1) The tablet volume is relatively large and the bioavailability is low At the same time, it is not popular with patients; (2) The homogeneity of the drug is relatively poor, and the coating effect is very high. Once there is a slight damage to the coating, the content of all active components will be released suddenly, resulting in side effects; (3) ) The bioefficiency of sustained-release pellets is greatly affected by food intake, with large inter-individual and intra-individual variability

Images