41 results about "Dronedarone hydrochloride" patented technology

The invention discloses a medicine composition of dronedarone hydrochloride, which is a dispersible tablet. The medicine composition is a tablet which is prepared from dronedarone hydrochloride micronized by a solid dispersion technology and an auxiliary material. According to the medicine composition, the dissolubility of the primary medicine is improved, rapid disintegration of the medicine is facilitated, the absorbability of the medicine in the blood is increased, and the bioavailability of the primary medicine is improved. Moreover, the medicine composition has a favorable treatment effect on symptoms such as arrhythmia, atrial fibrillation and the like.

The invention discloses a preparation method of an intermediate of dronedarone hydrochloride, which comprises the step of reacting 2-butyl-5-amino benzofuran hydrochloride serving as a starting material with methylsulfonyl chloride in the presence of a basic catalyst and an organic solvent to produce the intermediate of dronedarone hydrochloride, wherein the intermediate is 2-butyl-5-((N, N-dimethyl sulfonyl) amido) benzofuran. The invention also discloses a method for preparing dronedarone hydrochloride by using the intermediate. The preparation of the intermediate is simple and easy to operate; amino is protected by methylsulfonyl, so that the side reaction possibly generated in the reaction for preparing the dronedarone hydrochloride at the later period can be avoided, and the difficulty in purification at the later period can be simplified; the dronedarone hydrochloride yield is high; the problems in the prior art that the preparation of dronedarone hydrochloride is complicated with high cost, the intermediate is difficult to purify and aftertreatment is complicated can be solved; and the preparation difficulty of dronedarone hydrochloride is greatly reduced.

The invention discloses a preparation method of dronedarone hydrochloride tablets. The preparation method includes the steps that firstly, poloxamer and Kollicoat IR are dissolved in ethanol, ethanol is removed through drying, screening is performed, and a poloxamer mixture (1) wrapped by Kollicoat IR is obtained; secondly, dronedarone hydrochloride, a disintegrating agent and a filling agent are evenly mixed, granulation is performed, drying is performed, and a mixture (2) is obtained; thirdly, the mixture (1) and the mixture (2) are evenly mixed, a proper amount of magnesium stearate is added, and the dronedarone hydrochloride tablets are obtained through mixing and tabletting.

The invention provides a dronedarone hydrochloride pharmaceutical composition which is suitable for the sublingual administration, can quickly run, and can greatly improve the bioavailability and the curative effect. The pharmaceutical composition consists of 5-65 parts of dronedarone hydrochloride, 1-10 parts of a disintegrating agent, 10-80 parts of filler, 0.5-3 parts of antacid, 0-5 parts of corrigent, 1-10 parts of an adhesive and 0.3-2 parts of a lubricating agent. The invention further provides a preparation method suitable for the industrial production. The dronedarone hydrochloride pharmaceutical composition provided by the invention is directly absorbed by the sublingual mucosa, and the first-pass effect of oral medicaments can be avoided, and the gastrointestinal digestion, acidolysis and the like can be avoided, so that the bioavailability can be greatly improved. The epithelium of the sublingual mucosa is not cornified, so that the dronedarone hydrochloride pharmaceutical composition is large in superficial area, and high in infiltration capacity. The medicament can be quickly absorbed after being administrated, so that the dronedarone hydrochloride pharmaceutical composition is quick to run, and convenient to use; and compared with the other administrated preparations, the dronedarone hydrochloride pharmaceutical composition is convenient to administrate, and good in patient compliance.

The invention provides a method for detecting N-(2-butyl-3-(4-(3-(dibutylamino)propoxy)benzoyl)benzofuran-5-yl)Methanesulfonamide hydrochloride (dronedarone hydrochloride). N-(2-Butyl-3-(4-(3-(dibutylaMino)propoxy)benzoyl)benzofuran-5-yl)MethanesulfonaMide hydrochloride is detected by employing high performance liquid chromatography. Under the high performance liquid chromatography conditions provided by the invention, N-(2-butyl-3-(4-(3-(dibutylamino)propoxy)benzoyl)benzofuran-5-yl)Methanesulfonamide hydrochloride can be relatively well isolated from concomitant impurities, and all impurities can be relatively well separated. The provided method has relatively high sensitivity, and therefore the provided method is capable of relatively accurately determining N-(2-butyl-3-(4-(3-(dibutylamino)propoxy)benzoyl)benzofuran-5-yl)Methanesulfonamide hydrochloride.

The invention belongs to the field of pharmaceutical preparations, in particular to a surfactant-free dronedarone hydrochloride tablet. Contains the following components by mass: 400 parts of dronedarone hydrochloride, 100-1200 parts of hydroxypropyl methylcellulose, 20-640 parts of disintegrant, 7-10 parts of lubricant, excluding Surfactant. The technical scheme of the present invention does not add any surfactant, which not only increases the safety, but also avoids the problem of low melting point of the surfactant and easy sticking during the production process of the preparation, and at the same time significantly improves the dissolution rate of dronedarone hydrochloride . During the preparation process, dronedarone hydrochloride and hydroxypropyl methylcellulose are pulverized together until the particle size is not greater than 1 μm, and then made into tablets with other suitable auxiliary materials. The process is relatively simple, the operation is convenient, and it is suitable for large-scale industrial production.

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.

The invention relates to a preparation method for dronedarone hydrochloride. The preparation method includes utilizing 1,4-cyclohexanedione as a raw material to generate dihalogenated-1,4-cyclohexanedione through halogenation reaction with chlorine or bromine; generating a compound V and a compound V' through nucleophilic substitution reaction, elimination reaction and dehydration annulation with1-[4-(3-di-n-butylamino-propoxy)-phenyl]-heptane-1,3-dione; and obtaining a product through the ammonification of ammonia gas to generate dronedarone through the mesylation of methanesulfonyl chloride, and generating dronedarone hydrochloride by salting with hydrochloric acid. The preparation method is simple in process flow, less in operation step, low in production cost, high in yield and purity, less in waste water generation amount and green and environmentally friendly, and therefore, the industrial production and application of the dronedarone hydrochloride can be realized.

The invention relates to an oral solid medicinal composition, which is characterized by comprising pelletized dronedarone hydrochloride and hydrophilic gel matrix type slow release material hydroxypropyl methyl cellulose, wherein the pelletized dronedarone hydrochloride and hydrophilic gel matrix type slow release material hydroxypropyl methyl cellulose are selectively combined with one or more medicinal excipients. The oral solid medicinal composition is mainly used for treating arrhythmia.