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Multilayer tablet containing dabigatran etexilate mesylate

A dabigatran etexilate mesylate and methanesulfonic acid-containing technology, applied in the field of multi-layer tablets, to achieve the effects of improving solubility, increasing absorption rate, and increasing bioavailability

Active Publication Date: 2016-05-11
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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  • Multilayer tablet containing dabigatran etexilate mesylate
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  • Multilayer tablet containing dabigatran etexilate mesylate

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] Example 1: A single-layer tablet containing dabigatran etexilate mesylate, the 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 prescription amount of tartaric acid, dabigatran etexilate mesylate, lactose, MCC102, CC-Na, HPMCE5, add the same amount through a 60 mesh screen and mix three times, add magnesium stearate, and mix by hand for 30S .

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

[0028] Coating prescription and process:

[0029] The coating is carried out with a solution of hydroxypropyl cellulose (HPC) in isopropanol with a solid content of 5%. The weight gain of the control coating is 5%. A single-layer coated tablet is obtained.

Embodiment 2

[0030] Example 2: Multi-layer tablets containing dabigatran etexilate mesylate, the tablet core prescription is:

[0031]

[0032] Preparation method of double layer core:

[0033] (1) Preparation of tartaric acid layer

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

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

[0036] Weigh the prescription amount of dabigatran etexilate mesylate, lactose, MCC102, HPMCE5, CC-Na, and add the same amount through a 60 mesh screen and mix three times, add magnesium stearate, and mix by hand for 30S.

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

[0038] Coating prescription and process:

[0039] The coating is carried out with a solution of hydroxypropyl cellulose (HPC) in isopropanol with a solid content of 5%. The weight gain of...

Embodiment 3

[0041] Example 3: Multi-layer tablets containing dabigatran etexilate mesylate, the tablet core prescription is:

[0042]

[0043]

[0044] Three-layer core preparation method:

[0045] (1) Preparation of tartaric acid layer

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

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

[0048] Weigh the prescription amount of dabigatran etexilate mesylate, lactose, MCC102, HPMCE5, CC-Na, and add the same amount through a 60-mesh screen and mix three times, add magnesium stearate, and mix by hand for 30S.

[0049] (3) Preparation of isolation layer

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

[0051] (4) A 14.3x7.5mm shallow arc die is used to press the tablet, an...

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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 mesylate and belongs to the technical field of pharmacy. Background technique [0002] Dabigatran etexilate can be known from the prior art and first disclosed in WO98 / 37075. It is a potent thrombin inhibitor that can be used to prevent deep vein thrombosis and stroke after surgery, especially for prevention The patient had a stroke in a patient with atrial fibrillation. WO03 / 074056 discloses a particularly useful mesylate of dabigatran etexilate, which is dabigatran etexilate mesylate, and its structural formula is as follows [0003] [0004] The compound is usually administered orally. Specifically, a so-called pellet formulation can be used, as disclosed in WO03 / 074056, which is in the form of a composition in which a binder and optionally a release agent are surrounded by the core material The dabigatran etexilate mesylate is wrapped on the release agent, and the core materi...

Claims

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Application Information

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Patent Type & Authority Patents(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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