A dronedarone hydrochloride tablet and preparation method thereof

Abstract

The invention discloses a dronedarone hydrochloride tablet and a preparation method thereof; the tablet contains citric acid and is prepared by the following method: mixing dronedarone hydrochloride, citric acid and pharmaceutically common auxiliary materials evenly, adding an aqueous solution, granulating, drying, adding a lubricant, mixing, and tabletting to obtain the product. Compared with the prior art, the dronedarone hydrochloride tablet has the dissolution rate of dronedarone hydrochloride in tap water significantly improved, and the in-vivo environment is better simulated; micronization, dispersion preparation and other complex operations are not needed, the preparation process is relatively simple, operations are convenient, addition of poloxamer and other surfactants are not needed, and the tablet is rapidly dissolved in a gastric juice.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and in particular relates to a dronedarone hydrochloride tablet and a preparation method thereof. Background technique [0002] The chemical name of dronedarone is 2-n-butyl-3-[4-(3-di-n-butyl-aminopropoxy)benzoyl]-5-methylsulfonamide benzofuran, which is Sanox The latest drug developed by Felix-Zendibel for the treatment of cardiac arrhythmia. [0003] Dronedarone hydrochloride has very low solubility in aqueous media, especially its solubility is pH-dependent at room temperature, and has a maximum solubility in the range of pH 3 to 5, which is about 1-2 mg / ml, and is about 6 to 7 at pH The solubility becomes very low at pH=7, the solubility is only 10μg / ml at pH=7. [0004] Because of its dissolution characteristics, the solubility of dronedarone hydrochloride gradually decreases during the process of gradually increasing pH from the stomach to the intestinal tract, which ...

AI Technical Summary

Problems solved by technology

[0008] The inventor considers that the prior art uses pH4.5 phosphate buffer as the dissolution medium, which cannot fully simulate the human body environment. Because dronedarone hydrochloride has the best solubility in the medium of pH4.5, the inventor intends to use water as the dissolution medium. Dissolution medium, preparation of rapidly dissolving dronedarone hydrochloride tablets in water

In order to improve the dissolution rate of dronedarone hydrochloride tablets, a large number of experiments have been carried out, and it was unexpectedly found that if a small amount of tap water remains in the dissolution cup during the dissolution test, the liquid medicine will become cloudy rapidly. In order to further confirm this phenomenon, the inventors mixed hydrochloric acid A small amount of tap water is added to the solution of dronedarone, the liquid becomes mixed, and the absorbance is significantly reduced. No solution has been proposed in the prior art

Images