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Oral drug composition of dabigatran etexilate and preparation method thereof

A composition and drug technology, applied in the directions of drug combination, drug delivery, pharmaceutical formulation, etc., can solve the problems of difficult quality control of multi-component pellets, many process steps, and high production cost, and achieves simplified human processing and simplified process. , the effect of reducing the influence of excipients

Inactive Publication Date: 2018-07-10
QILU PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

This method involves multi-step micropellet preparation and isolation process, the process is complicated, and there are many process steps, which makes the quality control of multi-component micropills more difficult and the production cost is higher.

Method used

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  • Oral drug composition of dabigatran etexilate and preparation method thereof
  • Oral drug composition of dabigatran etexilate and preparation method thereof
  • Oral drug composition of dabigatran etexilate and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0040]

[0041] a) Preparation of drug-containing granules

[0042] composition:

[0043]

[0044]Add the prescribed amount of active substances, hydroxypropyl cellulose, and low-substituted hydroxypropyl cellulose into the mixing granulator, and mix for 5 minutes. After mixing, continue stirring, add the prescribed amount of isopropanol, and stir for 2 minutes to obtain The granules are added to the fluidized bed and dried until the water content is below 0.7%. Pass through a 30-mesh sieve or granulate with a granulator.

[0045] Add colloidal silicon dioxide and mix well.

[0046] b) Isolation of tartaric acid crystals

[0047] composition:

[0048] 129.9 parts by weight of tartaric acid

[0049] Gelatin Empty Capsule No. 4 Capsule

[0050] Fill the prescribed amount of tartrate crystals into a size 4 capsule.

[0051] c) Capsule filling

[0052] Pack the drug-containing granules and tartaric acid-containing gelatin capsules into No. 1 hypromellose hollow capsu...

Embodiment 2

[0054]

[0055] a) Preparation of drug-containing granules

[0056] composition:

[0057]

[0058] Add the prescribed amount of active substances, hydroxypropyl cellulose, and low-substituted hydroxypropyl cellulose into the mixing granulator, and mix for 5 minutes. After mixing, continue stirring, add the prescribed amount of isopropanol, and stir for 2 minutes to obtain The granules are added to the fluidized bed and dried until the water content is below 0.7%. Pass through a 30-mesh sieve or granulate with a granulator.

[0059] Add colloidal silicon dioxide and mix well.

[0060] b) Isolation of tartaric acid crystals

[0061] composition:

[0062] 110 parts by weight of tartaric acid

[0063] Gelatin empty capsule No. 5 capsule

[0064] Fill the prescribed amount of tartaric acid crystals into a size 5 capsule.

[0065] c) Capsule filling

[0066] Pack the drug-containing granules and tartaric acid-containing gelatin capsules into No. 1 hypromellose hollow c...

Embodiment 3

[0068]

[0069] a) Preparation of drug-containing granules

[0070] composition:

[0071]

[0072] Add the prescribed amount of active substances, hydroxypropyl cellulose, and low-substituted hydroxypropyl cellulose into the hopper mixer, and mix for 10 minutes at 15 rpm. After mixing, add them to the dry granulator for granulation. The pore size of the granulation screen is selected. 2.0mm, and then use a granulator with a pore size of 1.2mm for granulation.

[0073] Add colloidal silicon dioxide and mix well.

[0074] b) Isolation of citric acid crystals

[0075] composition:

[0076] 110 parts by weight of tartaric acid

[0077] Gelatin empty capsule No. 5 capsule

[0078] Fill the prescribed amount of citric acid crystals into a size 5 capsule.

[0079] c) Capsule filling

[0080] Pack the drug-containing granules and the gelatin capsule containing citric acid into No. 1 hypromellose hollow capsules.

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Abstract

The invention provides an oral drug composition of dabigatran etexilate and a preparation method thereof, belongs to the field of pharmaceutic preparation, aims at providing oral preparation of the dabigatran etexilate which has the advantages of simple technology, easy implementation, lower cost, better active material dissolution and easy absorption and a preparation method for the oral preparation. The oral drug composition comprises (a) medicated particles composed of active material ingredients, adhesive, disintegrating agent and flow aid, wherein the active material ingredients are dabigatran etexilate or acceptable salt in pharmacy; (b) isolated organic acid crystals, wherein an isolating layer is made from an empty capsule I or an isolating material of acceptable cellulose-based auxiliary materials in pharmacy; a preferred isolating layer is made from the empty capsule I; and the medicated particles and the isolated organic acid crystals are evenly mixed in proportion and filled into an empty capsule II.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and relates to an active substance of N-[2-[4-[N-(hexyloxycarbonyl)amidino]anilinomethyl]-1-methyl-1Hbenzimidazole-5- An oral pharmaceutical composition of ethyl carbonyl]-N-(2-pyridyl)-β-alanine (ie: dabigatran etexilate) or a pharmaceutically acceptable salt thereof. The invention also relates to a preparation method of the pharmaceutical composition. Background technique [0002] Dabigatran etexilate, the chemical name is N-[2-[4-[N-(hexyloxycarbonyl)amidino]anilinomethyl]-1-methyl-1Hbenzimidazol-5-ylcarbonyl]- N-(2-pyridyl)-beta-alanine ethyl ester, the chemical structural formula of its mesylate is as follows: [0003] [0004] Dabigatran etexilate was first disclosed in WO 98 / 37075 and was developed by Boehringer Ingelheim (BoehringerIngelheim) in Germany. It is a new type of direct thrombin inhibitor with oral, potent, no need for special drug monitoring, drug interaction L...

Claims

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Application Information

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IPC IPC(8): A61K9/50A61K47/12A61K31/4439A61P7/02
CPCA61K9/5047A61K9/5084A61K31/4439A61K47/12
Inventor 刘星宇杨清敏郑晓清
Owner QILU PHARMA
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