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Dronedarone hydrochloride pharmaceutical composition and preparation method thereof

A technique for dronedarone hydrochloride and its composition, which is applied in the field of dronedarone hydrochloride pharmaceutical composition and preparation, can solve the problems of high cost, complicated manufacturing process, poor stability, etc., and achieve rapid onset of effect and improved bioavailability , strong penetration effect

Active Publication Date: 2013-04-24
CSPC ZHONGQI PHARM TECH (SHIJIAZHUANG) CO LTD +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

But this method for improving the solubility of dronedarone hydrochloride has complicated manufacturing process, high cost and poor stability

Method used

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  • Dronedarone hydrochloride pharmaceutical composition and preparation method thereof
  • Dronedarone hydrochloride pharmaceutical composition and preparation method thereof
  • Dronedarone hydrochloride pharmaceutical composition and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0043] Preparation prescription: dronedarone hydrochloride 5g, lactose 40g, mannitol 40g, cross-linked polyvinylpyrrolidone 5g, lactic acid 0.5g, stevioside 5g, polyethylene glycol 4000 lg, polyvinylpyrrolidone 2g.

[0044] The specific preparation method is as follows: dry, pulverize and sieve the main drug, filler lactose and mannitol, disintegrant cross-linked polyvinylpyrrolidone, flavoring agent stevioside and lubricant polyethylene glycol 4000; Dissolve the binder polyvinylpyrrolidone and the antacid agent lactic acid in an appropriate amount of water to make a binder solution; mix the pretreated main drug with fillers, flavoring agents and disintegrants, and use the prepared binder Soft material made from solvent solution, granulated with a 20-mesh sieve; dried at 40°C until moisture content ≤ 2%; added lubricant to the obtained dry granules, blended, and finally compressed to obtain Dronedarone Hydrochloride Sublingual Tablets .

Embodiment 2

[0046] Preparation prescription: dronedarone hydrochloride 40g, microcrystalline cellulose-mannitol 40g, cross-linked polyvinylpyrrolidone 5g, citric acid 2g, stevioside 2g, polyethylene glycol 4000 0.5g, polyvinylpyrrolidone 5g.

[0047] The specific preparation method is as follows: dry the main drug, fill microcrystalline cellulose-mannitol, disintegrant cross-linked polyvinylpyrrolidone, corrective agent stevioside and lubricant polyethylene glycol 4000, dry, pulverize, and sieve. Treatment; dissolve the binder polyvinylpyrrolidone and the antacid agent citric acid in an appropriate amount of water to make a binder solution; mix the pretreated main ingredient with fillers, flavoring agents and disintegrants, and use the prepared Soft material made from a good binder solution, granulated with a 20-mesh sieve; dried at 50°C until moisture content ≤ 2%; added lubricant to the obtained dry granules, blended, and finally compressed to obtain dronedar hydrochloride Sublingual au...

Embodiment 4

[0052] Preparation prescription: dronedarone hydrochloride 20g, microcrystalline cellulose-mannitol 30g, cross-linked polyvinylpyrrolidone 1g, citric acid 1.5g, stevioside 1g, polyethylene glycol 4000 0.3g, polyvinylpyrrolidone 1g.

[0053] The specific preparation method is as follows: dry, pulverize and sieve the main ingredient, filler sugar powder, mannitol, sodium carboxymethyl starch, flavoring agent steviol glycoside and lubricant magnesium stearate; The agent polyvinylpyrrolidone and the antacid agent citric acid are dissolved in an appropriate amount of water to prepare an adhesive solution; the pretreated main drug is mixed with fillers, flavoring agents and disintegrants, and the prepared adhesive solution is used The soft material is granulated with a 20-mesh sieve; dried at 60°C until the moisture content is ≤2%; the lubricant is added to the obtained dry granules for total blending, and finally compressed to obtain dronedarone hydrochloride sublingual tablets.

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Abstract

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.

Description

technical field [0001] The invention belongs to the field of medicine, in particular to a dronedarone hydrochloride pharmaceutical composition and a preparation method. Background technique [0002] The chemical name of Dronedarone is N-[2-butyl-3-[4-[3-(dibutylamino)propoxy]benzoyl]-5-benzofuryl]methanesulfonyl Amidobenzofuran, formula C 31 h 44 N 2 o 5 S, molecular weight 593.22. The chemical formula is as follows: [0003] [0004] Dronedarone hydrochloride is an arrhythmia drug developed by Sanofi-Aventis. This product is a benzofuran derivative that does not contain iodine. Its structure and characteristics are similar to iodamine, but it does not contain iodine and has low lipophilicity. After taking it, phospholipids will not be deposited in the lungs, so the adverse reactions outside the cardiovascular system Iodoamine is less and clinically well tolerated. The half-life of this product is 1-2 days, which is more conducive to adjusting the dosage of the dru...

Claims

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Application Information

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IPC IPC(8): A61K9/20A61K31/343A61P9/06
Inventor 刘翠艳樊俊红王彦刘峰耿佳容彦华刘媛媛赵曦郭文敏王丙林胡永亮郭小丰于普
Owner CSPC ZHONGQI PHARM TECH (SHIJIAZHUANG) CO LTD
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