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A dabigatran etexilate mesylate capsule pharmaceutical composition and a preparing method thereof

A technology of dabigatran etexilate mesylate and composition, which is applied in the field of pharmaceutical preparations, can solve the problems of long time consumption, poor patient compliance, complicated process, etc., and achieve the effects of good dissolution effect, improved compliance, and simple process

Active Publication Date: 2015-07-22
CHENGDU EASTON BIOPHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Since the patented preparation process prepares the active substance into a ball core, a large amount of fillers and / or binders need to be added, which makes the volume and weight of the granules larger, and larger-sized capsules need to be used for filling, resulting in the pain of the patient when taking it. Poor compliance
Moreover, the preparation of active substances into pellet cores also has the disadvantage that it is not easy to dissolve completely. At the same time, the preparation process also has difficulties in controlling the amount of organic acid, uneven organic acid layer, poor reproducibility between batches, and low yield of finished products. And other issues
[0005] Both of the above two patents need to be coated layer by layer, resulting in complex processes and long time-consuming. Therefore, this area still needs a simple preparation process that can fully ensure the dissolution of dabigatran etexilate mesylate. new prescription and preparation process, and the present invention meets such demand

Method used

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  • A dabigatran etexilate mesylate capsule pharmaceutical composition and a preparing method thereof
  • A dabigatran etexilate mesylate capsule pharmaceutical composition and a preparing method thereof
  • A dabigatran etexilate mesylate capsule pharmaceutical composition and a preparing method thereof

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Experimental program
Comparison scheme
Effect test

Embodiment 1～3

[0028] The preparation of embodiment 1~3 dabigatran etexilate mesylate capsules

[0029] Prescription: a prescription for preparing 1000 dabigatran etexilate mesylate capsules

[0030]

[0031] Preparation Process:

[0032] The first part: the preparation of dabigatran etexilate mesylate coated granules

[0033] (1) Granulation: get the hypromellose of prescription quantity 40%, add appropriate amount of isopropanol and be mixed with 2% solution, standby as binder; Add binder in the dabigatran etexilate mesylate , granulation; dry the wet granules and granulate;

[0034] (2) Coating: get the remaining hypromellose, add appropriate amount of isopropanol to be mixed with 2% solution, add the talcum powder of 2.2% of the total amount of the first part of the prescription, stir well, set aside; The sized granules are placed in a fluidized bed and coated to obtain the finished product.

[0035] Part II: Preparation of Tartaric Acid Coated Granules

[0036] (1) Granulation: ...

Embodiment 4～6

[0039] The preparation of embodiment 4~6 dabigatran etexilate mesylate capsules

[0040] Prescription: a prescription for preparing 1000 dabigatran etexilate mesylate capsules

[0041]

[0042] Preparation Process:

[0043] The first part: the preparation of dabigatran etexilate mesylate coated granules

[0044] (1) Granulation: get 40% polyvinylpyrrolidone of prescription quantity, add appropriate amount of isopropanol and be mixed with 3% solution, standby as binder; Add binder in dabigatran etexilate mesylate, prepare Granules; dry the wet granules and then granulate;

[0045] (2) Coating: take the remaining polyvinylpyrrolidone, add appropriate amount of isopropanol to prepare a 3% solution, add 2.2% talcum powder in the first part of the prescription, stir well, and set aside; The final granules are placed in a fluidized bed and coated to obtain the finished product.

[0046] Part II: Preparation of Tartaric Acid Coated Granules

[0047] (1) Granulation: Take 10% ...

Embodiment 7

[0050] The preparation of embodiment 7 dabigatran etexilate mesylate capsules

[0051] Prescription: a prescription for preparing 1000 dabigatran etexilate mesylate capsules

[0052]

[0053] Preparation Process:

[0054] The first part: the preparation of dabigatran etexilate mesylate coated granules

[0055] (1) Granulation: get 2.8g hydroxypropyl cellulose, add appropriate amount of isopropanol and be mixed with 3% solution, standby as binder; Add binder in dabigatran etexilate, granulate; After the wet granules are dried, the granules are sized;

[0056] (2) Coating: take the remaining hydroxypropyl cellulose, add appropriate amount of isopropanol to prepare a 3% solution, add 2.2g talcum powder, stir evenly, and set aside; put the granules sized in step (1) in In a fluidized bed, coating is carried out.

[0057] Part II: Preparation of Tartaric Acid Coated Granules

[0058] (1) Granulation: get 0.9g hydroxypropyl cellulose, add appropriate amount of water and be m...

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Abstract

A dabigatran etexilate mesylate capsule pharmaceutical composition is provided. The composition comprises following two parts: coated granules of dabigatran etexilate mesylate and coated granules of tartaric acid. The granules of the two parts are mixed uniformly and filled into capsules. Capsules prepared by a prescription and a process are small in size and low in weight, have dissolution effects superior to that of the prior art, and have advantages of less related compounds, better stability and better quality.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, in particular to a dabigatran etexilate mesylate capsule pharmaceutical composition and a preparation method thereof. Background technique [0002] Dabigatran etexilate is a new type IIa factor direct thrombin inhibitor, which is the prodrug of dabigatran, mainly used for the prevention and treatment of acute and chronic thromboembolic diseases. After oral administration and gastrointestinal absorption, it is transformed into dabigatran with direct anticoagulant activity in the body. Dabigatran binds to the fibrin-specific binding site of thrombin, preventing fibrinogen from being cleaved into fibrin, thereby blocking the final step of the coagulation cascade network and thrombus formation. [0003] Patent No. ZL03805473.6 discloses a pharmaceutical composition for oral administration of dabigatran etexilate mesylate, wherein the composition can be prepared into capsules, and each part...

Claims

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Application Information

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IPC IPC(8): A61K9/48A61K31/4439A61K47/38A61K47/32A61P7/02
Inventor 王颖伍熹聂昱
Owner CHENGDU EASTON BIOPHARM CO LTD
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