Dabigatran etexilate medicine composition and preparation method thereof

A technology of dabigatran etexilate and composition, applied in the field of dabigatran etexilate pharmaceutical composition and its preparation, capable of solving problems such as poor stability

Inactive Publication Date: 2014-12-24
SICHUAN HAISCO PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, dabigatran etexilate is unstable in acidic environment, and its stability is worse if it encounters moisture in acidic environment

Method used

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  • Dabigatran etexilate medicine composition and preparation method thereof
  • Dabigatran etexilate medicine composition and preparation method thereof
  • Dabigatran etexilate medicine composition and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1-11

[0141] Will prepare pill 1 (as figure 1 , figure 2 and image 3 Shown in A) component, proportioning are listed in table 1, table 2 and table 3, and wherein wetting agent Virahol just uses in the preparation process, will be removed in final ball 1.

[0142]

[0143]

[0144] The preparation method of pill I in the above-mentioned embodiment 1-10 is as follows:

[0145] (a), dissolving polyvinylpyrrolidone k30 in isopropanol, as a binder solution, its binder concentration is about 2%;

[0146] (b), dabigatran etexilate mesylate or dabigatran etexilate butanedisulfonate particle size distribution is controlled at D90 less than 20 microns, mixed with talcum powder;

[0147] (c), suspending Opadry 200 in isopropanol as the isolation material suspension, the solid content of the suspension is about 8%;

[0148] (d), adopt the centrifugal pill making device, make its turntable be the state of horizontal rotation, its rotating speed is 200 revolutions / min, put blank ball ...

Embodiment 12-25

[0161] Components and proportions for preparing pill II are listed in Table 4, Table 5, Table 6 and Table 7, wherein the wetting agent ethanol is only used in the preparation process and will be removed in the final pill II.

[0162]

[0163]

[0164]

[0165] Pill II in the above-mentioned embodiment 12-24 (as figure 1 Shown in B) the preparation method is as follows:

[0166] (a), dissolving polyvinylpyrrolidone k30 in 50% ethanol as a binder solution, the binder concentration is about 2%;

[0167] (b), the particle size distribution of tartaric acid or maleic acid is controlled at D90 and is less than 150 microns, mixes evenly with talcum powder;

[0168] (c), suspending Opadry 200 in 50% ethanol aqueous solution as the isolation material suspension, the solid content of the suspension is about 8%;

[0169] (d), adopt the centrifugal pill making device, make its turntable be the state of horizontal rotation, its rotating speed is 250 revolutions per minute, put t...

Embodiment 26-37

[0191] Containing dabigatran etexilate in the following pharmaceutical composition is 75mg, and the composition of pill I and pill II, proportioning are listed in table 8, table 9 and table 10 in this composition:

[0192]

[0193]

[0194] The preparation method of composition in above-mentioned embodiment 26-37 is as follows:

[0195] According to the content of dabigatran etexilate in pill I and the content of organic acid in pill II, and according to the different mass ratios of dabigatran etexilate and organic acid, pills I and pill II are filled in No. 1 capsule by 2 filling methods Among them, multiple specifications of dabigatran etexilate capsules (such as 75mg, 110mg, and 150mg, different specifications are only different in loading capacity) can be obtained.

[0196]

[0197] The preparation method of composition among the above-mentioned embodiment 38 is as follows:

[0198] According to the content of dabigatran etexilate in pill I, according to the mass...

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Abstract

The invention relates to a dabigatran etexilate medicine composition and a preparation method thereof. The dabigatran etexilate medicine composition consists of a pill I and a pill II, wherein the pill I contains an active ingredient, a blank pill core material, an adhesive, an anti-sticking agent and/or an isolation material, wherein the active ingredient is dabigatran etexilate or a pharmaceutically acceptable salt, hydrate or solvate thereof; and the pill II contains a medicinal organic acid, a pill core material, an adhesive, an anti-sticking agent and/or an isolation material. The discovery shows that the active ingredient and the organic acid are respectively contained in the two different pills, so that the requirement of dissolving out the active ingredient is satisfied, and the active ingredient is more uniformly dissolved out; and in addition, an isolation effect between the active ingredient and the organic acid is enhanced, so that the stability of the dabigatran etexilate medicine composition is improved.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, in particular to a dabigatran etexilate pharmaceutical composition and a preparation method thereof, more specifically to an anticoagulant active ingredient dabigatran etexilate or a pharmaceutically acceptable salt thereof, hydrated Oral pharmaceutical composition of substance or solvate and preparation method thereof. Background technique [0002] The chemical name of Dabigatran etexilate (Dabigatran etexilate) of the present invention is 3-[[[2-[[[4-[[[(hexyloxy)carbonyl]amino]iminomethyl]phenyl] Amino] methyl] -1-methyl-1H-benzimidazol-5-yl] carbonyl] (pyridin-2-yl) amino] ethyl propionate, structural formula such as formula (I), dabigatran etexilate or Its pharmaceutically acceptable salt, hydrate or solvate is hereinafter referred to as "active ingredient". [0003] [0004] Dabigatran etexilate is a new type of synthetic non-peptide oral thrombin inhibitor develope...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/62A61K31/4439A61P7/02
Inventor 向志祥江智勇黄智龙周仕川罗杰李方群徐同利曾琴魏瑶
Owner SICHUAN HAISCO PHARMA CO LTD
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