41 results about "Dronedarone hydrochloride" patented technology

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 relates to a method for preparing dronedarone hydrochloride, comprising the following concrete steps of: (1) carrying out etherification reaction on 2-butyl-3-(4-hydroxy benzoyl)-5-nitro benzofuran and 1-bromine-3-chloropropane in an organic solvent so as to obtain 2-n-butyl-3-[4-(3-chlorine propoxy) benzoyl]-5-nitro benzofuran; (2) reducing to 2-n-butyl-3-[4-(3-chlorine propoxy) benzoyl]-5-amido benzofuran by utilizing a reductant; (3) carrying out sulfamide reaction with methyl sulfonyl chloride in the organic solvent so as to obtain 2-n-butyl-3-[4-(3-chlorine propoxy) benzoyl]-5-methyl sulfonamide benzofuran; (4) carrying out N-hydrocarbon reaction with di-n-butylamine so as to obtain the dronedarone; and (5) salifying the dronedarone hydrochloride and obtaining the dronedarone hydrochloride. The method provided by the invention has the advantages that the reaction route is simple, the raw material is cheap and easy to obtain and the reaction condition is mild and easy to control and is suitable for industrialized production.

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 belongs to the field of pharmaceutical preparations, and specifically relates to a surfactant-free dronedarone hydrochloride tablet. The dronedarone hydrochloride tablet comprises the following components in parts by weight: 400 parts of dronedarone hydrochloride, 100-1200 parts of hydroxypropyl methyl cellulose, 20-640 parts of disintegrating agent, 7-10 parts of lubricant, and zero surfactant. The technical scheme of the dronedarone hydrochloride tablet is characterized in that no surfactant is added, so that the safety is improved, and the problems of low melting point and easy sticking of the surfactant in the production process of the preparation are also avoided; and simultaneously, the dissolution rate of dronedarone hydrochloride is obviously improved. In the preparation process, the dronedarone hydrochloride and hydroxypropyl methyl cellulose are together ground until the particle size thereof is not greater than 1 micron, and then the obtained powder is formed into tablets with other suitable accessories; the process is quite simple, convenient to operate and suitable for industrial large-scale production.

The present invention relates to a process for preparation of Dronedarone or pharmaceutically acceptable salts thereof. More particularly, the present invention provides a process for preparation of Dronedarone hydrochloride, without the isolation of Dronedarone base.

The invention discloses an application of combination of dronedarone hydrochloride and 5-fluorouracil in preparation of antitumor drugs. Pharmacodynamic experiments prove that the combination of dronedarone hydrochloride and 5-fluorouracil can effectively inhibit proliferation of human hepatoma cell lines HepG2, PLC/PRF/5 and Hep3B. The single use of dronedarone hydrochloride can effectively inhibit the proliferation of human hepatoma cell lines HepG2, PLC/PRF/5 and Hep3B, and the single use of dronedarone hydrochloride can effectively inhibit the proliferation of human lung cancer cell lines SPC-A1 and A549 and mouse lung cancer cell lines Lewis. In addition, dronedarone hydrochloride is combined with 5-fluorouracil, so that growth of tumors in a mouse liver cancer transplantation tumor model can be inhibited. The dronedarone hydrochloride combined antitumor drug has the characteristics of safety, effectiveness and the like when being used for treating liver cancer and lung cancer, can be used for preparing the drug for treating liver cancer and lung cancer, and provides a new treatment strategy for clinical treatment of liver cancer and lung cancer.

The invention discloses a dronedarone hydrochloride self-microemulsion preparation and a preparing method thereof. A liquid self-microemulsion preparation is prepared from dronedarone hydrochloride, an oil phase, an emulsifier and a co-emulsifier, or a solid self-microemulsion preparation is further prepared from the obtained liquid self-microemulsion preparation and an excipient.

The invention relates to a solid preparation composition containing a benzofurane derivative and a preparation method thereof and belongs to the technical field of medicines. The technical scheme is that a dronedarone hydrochloride composition is characterized in that dronedarone hydrochloride and a surfactant undergo co-micronization to D90 5-10[mu]m. Through a co-micronization technology of dronedarone hydrochloride and the surfactant, a rational formula and a preparation method, a stable tablet is obtained. The tablet which is moderate in weight and convenient to transport and store is provided clinically.

The invention provides a composition for a dronedarone hydrochloride tablet and a preparation method thereof. The dronedarone hydrochloride tablet is prepared from an active component, a surfactant, lauryl sodium sulfate and other pharmaceutically acceptable components, wherein the active component is dronedarone hydrochloride, and the surfactant is polyethylene glycol. The dronedarone hydrochloride tablet has high dissolution rate and is suitable for industrial production, and the preparation process of the dronedarone hydrochloride tablet is simple.

The invention provides a novel dronedarone hydrochloride osmotic pump-type controlled-release tablet, which adopts cellulose acetate and polycarbonate as semipermeable membrane film-forming materials, which can overcome the semipermeable membrane aging phenomenon, obtain a stable release rate, and Reduce drug residues. The dronedarone oral osmotic pump preparation provided by the present invention has excellent release performance and high stability, and there is no obvious aging phenomenon after being placed for a long time, which meets the market demand.

The invention belongs to the field of medicine preparations and discloses dronedarone hydrochloride slow-release tablets and a preparation method thereof. The slow-release tablets are prepared from, in percentage by mass, 10%-35% of dronedarone hydrochloride, 50%-90% of a hydrophobic framework material, 1%-5% of a binder and 0.5%-5% of a lubricant. The slow-release tables are prepared from the hydrophobic framework material and the like, medicine release can be well controlled, the process is simple, and expanded production is facilitated.

The invention relates to the field of medicine preparation, in particular to a method for preparing dronedarone hydrochloride tablets. The method for preparing the dronedarone hydrochloride tablets comprises the following specific steps: S1, carrying out compatibility test on raw materials and auxiliary materials of dronedarone hydrochloride; S2, preliminarily selecting preparation auxiliary materials; S3, processing raw materials and auxiliary materials; S4, mixing raw materials and auxiliary materials; S5, pelletizing; S6, drying granules; S7, granulating; S8, total mixing; S9, tabletting; S10, coating; S11, internal coating; and S12, external coating. The feasibility and reproducibility of the production process determined in the invention can be reflected well; the tablets can be effectively prepared, intermediate products in different stages can be accurately understood and controlled in time in a processing and preparation process, the quality of the intermediate products in thewhole production process is guaranteed, and thus, it can be ensured that the final product meets the processing requirement.