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Composition containing dronedarone

A composition and drug technology, applied in the field of compositions containing dronedarone, can solve problems such as insignificant influence, inability to dissolve drugs well, enter the intestinal tract, etc., to improve dissolution rate, increase drug dissolution, and enhance The effect of speed and degree of absorption

Active Publication Date: 2012-02-15
JILIN BODA PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The results of the patent pharmacokinetic test show that: under fasting conditions, the Cmax and AUC of the prescription containing poloxamer 407 are significantly greater than those without poloxamer 407; The effect of poloxamer 407 on Cmax and AUC was not obvious; however, the Cmax and AUC of the prescription containing poloxamer 407 administered under fasting conditions were significantly lower than those under fed conditions
[0007] Dronedarone is taken by almost all elderly patients. Although the instructions of the marketed preparation clearly indicate that this product must be taken after meals, for people with excessive or low gastric acid secretion, the gastric environment after meals still cannot dissolve the drug well. Most dronedarone enters the intestinal tract with food

Method used

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  • Composition containing dronedarone
  • Composition containing dronedarone
  • Composition containing dronedarone

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] Samples were prepared according to the above prescription, and the process was as follows:

[0033] Step 1: Mix citric acid with low-substituted hydroxypropyl cellulose, then mix with copovidone S630, microcrystalline cellulose, and lactose, then add dronedarone hydrochloride and mix;

[0034] Step 2: dissolve or disperse egg yolk lecithin in four times the amount of 95% ethanol, add the material obtained in step 1, and mix evenly;

[0035] Step 3: use purified water as a wetting agent, wet granulate, and dry;

[0036] Step 4: Add silicon dioxide and magnesium stearate to step 4, and mix well;

[0037] Step 5: the material obtained in step 4 is filled into hard capsules.

Embodiment 2

[0040] Samples were prepared according to the above prescription, and the process was as follows:

[0041] Step 1: Mix 50% of the prescription amount of croscarmellose sodium, citric acid, microcrystalline cellulose, and hypromellose, and then add dronedarone hydrochloride;

[0042] Step 2: add 30% recipe quantity magnesium stearate in the material gained in step 1;

[0043] Step 3: egg yolk lecithin is dissolved or dispersed in four times the amount of 95% ethanol, added to the material obtained in step 2, and mixed evenly;

[0044] Step 4: Dry granulate the material obtained in Step 3 with a granulation screen of 24 mesh. The prepared granules are passed through a 80 mesh sieve, and the fine powder under the sieve is dry granulated again

[0045] Step 5: Add silicon dioxide, 50% of the prescription amount of low-substituted hydroxypropyl cellulose, and 70% of the prescription amount of magnesium stearate into the dry granules;

[0046] Step 6: Tablet pressing.

Embodiment 3

[0049] Samples were prepared according to the above prescription, and the process was as follows:

[0050] Step 1: mix microcrystalline cellulose, lactose, tartaric acid, hypromellose, and 50% prescription amount of crospovidone, and add dronedarone hydrochloride;

[0051] Step 2: Soybean lecithin is dissolved or dispersed in four times the amount of 95% ethanol, added to the material obtained in Step 1, and mixed evenly;

[0052] Step 3: wet granulation with 5% hypromellose aqueous solution binder;

[0053] Step 4: dry, granulate, add 50% prescription amount of crospovidone, silicon dioxide, magnesium stearate

[0054] Step 5: Compression

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PUM

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Abstract

The invention relates to a pharmaceutical composition which comprises dronedarone or pharmaceutically acceptable salt thereof used as a preparation active ingredient, a phosphatide, an acidity regulator and one or more crystallization inhibitors. The composition is suitable for any oral drug forms, such as tablets, capsules or granules. The composition has the advantages that: the drug dissolution can be effectively increased, thereby increasing the in-vivo absorption rate and degree of the active ingredients; and more importantly, the areas below the in-vivo blood concentration-time curves of the Beagle dog under drug feeding / fasting conditions have no difference almost.

Description

technical field [0001] The invention belongs to the field of medicines, in particular to a composition containing dronedarone. Background technique [0002] Dronedarone hydrochloride (Dronedarone) is an analogue of amiodarone, a new class III antiarrhythmic drug, which has blocking effects on calcium, potassium, and sodium channels, and has anti-adrenergic effects. Dronedarone is similar to amiodarone in chemical structure, but does not contain iodine, and its lipophilicity is weaker than amiodarone. After taking it, phospholipids will not be deposited in the lungs, so the adverse reactions outside the cardiovascular system are less than that of amiodarone. , clinically well tolerated. Dronedarone is currently the only antiarrhythmic drug that has been shown to significantly reduce the morbidity and mortality of patients with atrial fibrillation / atrial flutter. [0003] The chemical structural formula of dronedarone hydrochloride is as follows, the molecular weight is 593,...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/343A61K47/24A61K47/12A61P9/06
Inventor 张翠霞孙蕴哲李晓强
Owner JILIN BODA PHARMA
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