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Multi-layer tablets containing dabigatran etexilate mesylate

A technology of dabigatran etexilate mesylate and dabigatran etexilate is applied in the field of multi-layer tablets to achieve the effects of prolonging storage time, solving disintegration risk and improving drug safety

Active Publication Date: 2014-09-17
ZHEJIANG JINGXIN PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At the same time, the present invention also solves the problem of crystal transformation and other substances appearing in the production and storage process, improves the production quality, and prolongs the storage time

Method used

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  • Multi-layer tablets containing dabigatran etexilate mesylate
  • Multi-layer tablets containing dabigatran etexilate mesylate
  • Multi-layer tablets containing dabigatran etexilate mesylate

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] Embodiment 1: a kind of monolayer tablet containing dabigatran etexilate, tablet core prescription is:

[0023]

[0024] In the table: MCC102 is microcrystalline cellulose 102, CC-Na is croscarmellose sodium, HPMCE5 is hypromellose E5, MS is magnesium stearate.

[0025] Single-layer core preparation method:

[0026] (1) Weigh the prescribed amount of tartaric acid, dabigatran etexilate mesylate, lactose, MCC102, CC-Na, HPMCE5, add the same amount through a 60-mesh sieve and mix three times, add magnesium stearate, and mix by hand for 30 seconds .

[0027] (2) A 14.3x7.5mm shallow arc die is used to press the tablet, and the control pressure is 2000lbs.

[0028] Coating prescription and process:

[0029] The isopropanol solution of hydroxypropyl cellulose (HPC) was used for coating, and the solid content was 5%. Control coating weight gain was 5%. Obtain single-layer coated tablets.

Embodiment 2

[0030] Embodiment 2: the multi-layer tablet containing dabigatran etexilate, this tablet core prescription is:

[0031]

[0032] Double-layer tablet core preparation method:

[0033] (1) Preparation of tartaric acid layer

[0034] Weigh the prescribed amount of tartaric acid, lactose, MCC102, CC-Na, HPMCE5, add the same amount through a 60-mesh sieve and mix three times, add magnesium stearate, and mix by hand for 30 seconds.

[0035] (2) Preparation of drug-containing layer

[0036] Weigh the prescribed amount of dabigatran etexilate mesylate, lactose, MCC102, HPMCE5, CC-Na, add equal amounts through a 60-mesh sieve and mix three times, add magnesium stearate, and mix by hand for 30 seconds.

[0037] (3) A 14.3x7.5mm shallow arc punching die is used to press the tablet, and the control pressure is 2000lbs.

[0038] Coating prescription and process:

[0039] The isopropanol solution of hydroxypropyl cellulose (HPC) was used for coating, and the solid content was 5%. Co...

Embodiment 3

[0041] Embodiment 3: the multi-layer tablet containing dabigatran etexilate, this tablet core prescription is:

[0042]

[0043]

[0044] Three-layer tablet core preparation method:

[0045] (1) Preparation of tartaric acid layer

[0046] Weigh the prescribed amount of tartaric acid, lactose, MCC102, CC-Na, HPMCE5, add the same amount through a 60-mesh sieve and mix three times, add magnesium stearate, and mix by hand for 30 seconds.

[0047] (2) Preparation of drug-containing layer

[0048] Weigh the prescribed amount of dabigatran etexilate mesylate, lactose, MCC102, HPMCE5, CC-Na, add equal amounts through a 60-mesh sieve and mix three times, add magnesium stearate, and mix by hand for 30 seconds.

[0049] (3) Preparation of isolation layer

[0050] Weigh the prescribed amount of HPMCE5 and MCC102 and add them through a 60-mesh sieve and mix three times, add magnesium stearate, and mix by hand for 30 minutes.

[0051] (4) A 14.3x7.5mm shallow arc punching die is use...

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Abstract

The invention discloses a multi-layer tablet containing dabigatran etexilate mesylate. The multi-layer tablet comprises a tablet core and a coating film; the tablet core comprises at least one drug-containing layer containing dabigatran etexilate mesylate and at least one organic acid layer. The multi-layer tablet is capable of increasing the solubility in vivo and the absorption rate in vivo, and also capable of effectively controlling the release time in vivo, and further is low in batch difference, and therefore, the safety of drug use is improved. Meanwhile, the multi-layer tablet is used for solving the problem that other substances are generated due to crystal transformation in the production and storage processes, and the production quality is improved and the storage time is prolonged. In addition, the multi-layer tablet further has the characteristics of convenience for swallowing, simple production process and high reproducibility.

Description

technical field [0001] The invention relates to a multi-layer tablet containing dabigatran etexilate, which belongs to the technical field of pharmacy. Background technique [0002] Dabigatran etexilate is known from the prior art and first disclosed in WO98 / 37075, it is a potent thrombin inhibitor useful for postoperative prophylaxis of deep venous thrombosis and prophylaxis of stroke, in particular for the prophylaxis of Patients with stroke in patients with atrial fibrillation. WO03 / 074056 discloses the mesylate of particularly useful dabigatran etexilate, namely dabigatran etexilate mesylate, and its structural formula is as follows [0003] [0004] The compound is usually administered orally. In particular, so-called pellet formulations may be used, as disclosed in WO 03 / 074056, which formulations are in the form of compositions in which a core material containing a binder and optionally a release agent is surrounded. Then dabigatran etexilate mesylate is wrapped...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/36A61K31/4439A61P7/02A61P9/10
Inventor 潘裕生徐子金张利锋何海萍俞悦王琼洁
Owner ZHEJIANG JINGXIN PHARMA
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