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Pharmaceutical composition containing dabigatran etexilate mesylate and preparation method thereof

A technology for dabigatran etexilate mesylate and a composition is applied in the field of dabigatran etexilate mesylate pharmaceutical composition and preparation thereof, and can solve the problem of large variability of bioavailability, excessive residual solvent environment, and active ingredients. Degradation and other problems to achieve the effect of reducing gastric irritation, improving bioavailability in vivo, and reducing variability

Inactive Publication Date: 2021-06-11
南京海辰药业股份有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0010] The technical problem to be solved in the present invention is that on the one hand dabigatran etexilate mesylate pharmaceutical preparations are easy to contact with water in the preparation process, and the use of organic solvents will cause problems such as degradation of active components, excessive residual solvents and environmental pollution; On the one hand, the dissolution of dabigatran etexilate mesylate is pH-dependent, poor solubility, low dissolution rate, and large variability in bioavailability between different individuals

Method used

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  • Pharmaceutical composition containing dabigatran etexilate mesylate and preparation method thereof
  • Pharmaceutical composition containing dabigatran etexilate mesylate and preparation method thereof
  • Pharmaceutical composition containing dabigatran etexilate mesylate and preparation method thereof

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Embodiment 1

[0025] This embodiment provides the preparation method of the dabigatran etexilate mesylate pharmaceutical composition. The prescription is as follows:

[0026] composition Dosage (mg) Dabigatran etexilate mesylate 126.83 macrogol glyceride laurate 89.40 polyethylene glycol 4000 135.50 microcrystalline cellulose 69.66 Carboxymethyl Starch Sodium 19.50 talcum powder 2.00 Micropowder silica gel 2.00

[0027] Preparation Process:

[0028] Mix polyethylene glycol 4000 and dabigatran etexilate mesylate, melt at 60-70°C, stir and granulate, cool and sizing to obtain Granule 1. Mix granule 1 with macrogolglycerol laurate, melt at 45-55°C, stir and granulate, cool, and granulate to obtain granule 2. Mix granule 2 with microcrystalline cellulose, sodium starch glycolate, talcum powder, and micropowder silica gel evenly, fill capsules, and obtain the product.

Embodiment 2

[0030] This embodiment provides the preparation method of the dabigatran etexilate mesylate pharmaceutical composition. The prescription is as follows:

[0031] composition Dosage (mg) Dabigatran etexilate mesylate 126.83 Ethylene glycol stearate 86.30 polyethylene glycol 6000 123.90 microcrystalline cellulose 42.70 Calcium hydrogen phosphate anhydrous 31.15 Croscarmellose Sodium 21.60 Magnesium stearate 2.60

[0032] Preparation Process:

[0033] Mix polyethylene glycol 6000 and dabigatran etexilate mesylate, melt at 60-70°C, stir and granulate, cool and sizing to obtain Granule 1. Mix granule 1 with ethylene glycol stearate, melt at 50-60°C, stir and granulate, cool, and granulate to obtain granule 2. Then mix the above granule 2 with microcrystalline cellulose, anhydrous calcium hydrogen phosphate, croscarmellose sodium and magnesium stearate, and press into tablets to obtain the product.

Embodiment 3

[0035] This embodiment provides the preparation method of the dabigatran etexilate mesylate pharmaceutical composition. The prescription is as follows:

[0036] composition Dosage (mg) Dabigatran etexilate mesylate 126.83 Propylene Glycol Monolaurate 95.60 polyethylene glycol 4000 142.32 Spray Dried Lactose 61.4 Low-substituted hydroxypropyl cellulose 38.24 Sodium stearate fumarate 5.00

[0037] Preparation Process:

[0038] Mix polyethylene glycol 4000 and dabigatran etexilate mesylate, melt at 60-70°C, stir and granulate, cool, and granulate to obtain Granule 1. Mix granule 1 with propylene glycol monolaurate, melt at 50-60°C, stir and granulate, cool, and granulate to obtain granule 2. Then the above granules 2 are mixed with spray-dried lactose, low-substituted hydroxypropyl cellulose and sodium stearate fumarate, and filled into capsules to obtain the product.

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Abstract

The invention discloses a pharmaceutical composition containing dabigatran etexilate mesylate and a preparation method of the pharmaceutical composition. The dabigatran etexilate mesylate composition is prepared from an active substance dabigatran etexilate mesylate, a water dispersible surfactant, a hydrophilic polymer and other pharmaceutically acceptable auxiliary materials. Wherein the melting temperature of the water dispersible surfactant is 40-80 DEG C, and the content of the water dispersible surfactant is 15-25%; and the melting temperature of the hydrophilic polymer is 60-100 DEG C, and the content of the hydrophilic polymer is 25-35%. The pharmaceutical composition prepared by the invention avoids the use of organic acid, reduces the stimulation to the stomach of a patient with excessive gastric acid secretion, and improves the compliance of the patient. According to the invention, the dissolution rate of the pharmaceutical composition in an acetate medium with the pH value of 4.5 is improved by using the solubilization effect of the water dispersible surfactant, and the dissolution amount in 30 minutes can reach 80% or more, so that the solubility of dabigatran etexilate mesylate in the stomach of a patient with gastric acid deficiency in a relatively high pH value environment is effectively solved, the in-vivo bioavailability is improved, and the variability among individuals is reduced; and the low hygroscopicity of hydrophilic polymerization is utilized to improve the stability problem of the pharmaceutical composition in the production and storage processes. The pharmaceutical composition is prepared by adopting a hot-melting stirring granulation process, water is not contacted and an organic solvent is not used in the process, the degradation of active substances is effectively reduced, the stability of the pharmaceutical composition is improved, meanwhile, the production process is simple, the period is short, the cost is low, the pharmaceutical composition is green and environment-friendly, and industrial mass production is easy to realize.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, in particular to a dabigatran etexilate mesylate pharmaceutical composition and a preparation method thereof. Background technique [0002] Dabigatran etexilate (Dabigatran Etexilate) of the present invention, its chemical name is: 3-(2-{[(4-{N'-[(hexyloxy)carbonyl]amidino}phenyl )amino]methyl}-1-methyl-N-(pyridin-2-yl)-1H-benzo[d]imidazole-5-carboxamido)ethyl propionate methanesulfonate, molecular formula: C 34 h 41 N 7 o 5 ·CH 4 o 3 S, molecular weight: 723.86, structure as follows: [0003] [0004] Dabigatran etexilate mesylate, as a new type of oral anticoagulant drug, can specifically block a key link in the blood coagulation cascade, significantly reduce the risk of bleeding while ensuring the anticoagulant effect, and is an effective treatment for thromboembolic complications in patients with atrial fibrillation. Prevention offers a safe and effective new opt...

Claims

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Application Information

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IPC IPC(8): A61K9/14A61K9/16A61K9/48A61K9/20A61K47/14A61K47/10A61K47/32A61K31/4439A61P7/02A61P9/10
CPCA61K9/146A61K9/145A61K9/1641A61K9/1617A61K9/1635A61K9/1682A61K9/4866A61K9/4858A61K9/2031A61K9/2013A61K9/2027A61K9/2095A61K31/4439A61P7/02A61P9/10
Inventor 徐云郭进冯明声姚晓敏曹于平
Owner 南京海辰药业股份有限公司
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