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Dabigatran etexilate mesylate inclusion compound, preparation method and application

A dabigatran etexilate mesylate and inclusion compound technology, which is applied in the field of dabigatran etexilate mesylate inclusion compound, can solve the problems of low bioavailability, low drug solubility, and gastrointestinal irritation of organic acids In order to avoid the problems of large drug resistance and other problems, it can achieve the effect of reducing the dosage, having a good market prospect and improving the bioavailability

Pending Publication Date: 2022-01-07
SHANGHAI BOCIMED PHARMA CO LTD +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0008] The technical problem to be solved by the present invention is to provide a kind of methanesulfonic acid in order to solve the defects of the prior art, such as low drug solubility, low bioavailability, and the need to use organic acids, which are highly irritating to the gastrointestinal tract of dabigatran preparations. Dabigatran etexilate inclusion compound, preparation method and application

Method used

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  • Dabigatran etexilate mesylate inclusion compound, preparation method and application
  • Dabigatran etexilate mesylate inclusion compound, preparation method and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0046]Dabigatran etexilate mesylate: hydroxypropyl-β-cyclodextrin=1:1 (molar ratio of substances)

[0047] Weigh 0.050 g of dabigatran etexilate mesylate and 0.104 g of hydroxypropyl-β-cyclodextrin respectively, and prepare clathrates according to the following method.

[0048] After dabigatran etexilate mesylate was dissolved with 1ml methanol, it was added dropwise to 9% hydroxypropyl-beta-cyclodextrin aqueous solution (the mass percentage refers to hydroxypropyl-beta-cyclodextrin aqueous solution). The mass of cyclodextrin and the percentage of the mass of hydroxypropyl-β-cyclodextrin aqueous solution), in a magnetic stirrer, 60 ° C (water bath) inclusion for 7 hours, let cool to room temperature (20 ° C ~ 25 ° C), rotary evaporation , filtered, and freeze-dried to obtain dabigatran etexilate mesylate hydroxypropyl-β-cyclodextrin inclusion compound.

Embodiment 2

[0050] Dabigatran etexilate mesylate: hydroxypropyl-β-cyclodextrin=1:2 (molar ratio of substances)

[0051] Weigh 0.200 g of dabigatran etexilate mesylate and 0.832 g of hydroxypropyl-β-cyclodextrin respectively, and prepare clathrates according to the following method.

[0052] After dabigatran etexilate mesylate was dissolved with 4ml methanol, it was added dropwise to 9% hydroxypropyl-beta-cyclodextrin aqueous solution (the mass percentage refers to hydroxypropyl-beta-cyclodextrin aqueous solution). The mass of cyclodextrin and the percentage of the mass of hydroxypropyl-β-cyclodextrin aqueous solution), in a magnetic stirrer, 60 ° C (water bath) inclusion for 7 hours, let cool to room temperature (20 ° C ~ 25 ° C), rotary evaporation , filtered, and freeze-dried to obtain dabigatran etexilate mesylate hydroxypropyl-β-cyclodextrin inclusion compound.

Embodiment 3

[0054] Dabigatran etexilate mesylate: sulfobutyl-β-cyclodextrin=1:1 (molar ratio of substances)

[0055] Weigh 0.200 g of dabigatran etexilate mesylate and 0.328 g of sulfobutyl-β-cyclodextrin respectively to prepare clathrates according to the following method.

[0056] After dabigatran etexilate mesylate was dissolved with 4ml of methanol, it was added dropwise to 9% sulfobutyl-β-cyclodextrin aqueous solution (the mass percentage refers to sulfobutyl-β-cyclodextrin aqueous solution). The mass of cyclodextrin and the percentage of the mass of sulfobutyl-β-cyclodextrin aqueous solution), in a magnetic stirrer, 60 ° C (water bath) inclusion for 7 hours, let cool to room temperature (20 ° C ~ 25 ° C), rotary evaporation , filtered, and freeze-dried to obtain dabigatran etexilate mesylate hydroxypropyl-β-cyclodextrin inclusion compound.

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Abstract

The invention provides a dabigatran etexilate mesylate inclusion compound, a preparation method and application. The dabigatran etexilate mesylate inclusion compound provided by the invention comprises dabigatran etexilate mesylate and cyclodextrin. The dabigatran etexilate mesylate inclusion compound provided by the invention can effectively improve the solubility of a drug, the solubility is improved by 2-5 times compared with the solubility of the dabigatran etexilate mesylate, the bioavailability is improved, and the use of organic acid is avoided, so that the gastrointestinal irritation is small. The method can realize continuous processing, and is high in production efficiency, good in process reproducibility and good in market prospect.

Description

[0001] This application claims to enjoy the priority rights of the following earlier applications: the application number submitted to the State Intellectual Property Office of China on November 27, 2020 is 202011363686.2, and the name is "dabigatran etexilate mesylate inclusion compound, preparation method and application ” Chinese invention patent application. The entirety of the aforementioned prior application is incorporated herein by reference. technical field [0002] The invention relates to dabigatran etexilate mesylate inclusion compound, preparation method and application. Background technique [0003] Dabigatran etexilate is a novel oral anticoagulant drug, and its structural formula is shown in Formula I. After oral 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...

Claims

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Application Information

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IPC IPC(8): A61K47/69A61K31/4439A61P7/02
CPCA61K31/4439A61K47/6951A61P7/02
Inventor 郭桢应述欢覃伟何新怡王婷婷
Owner SHANGHAI BOCIMED PHARMA CO LTD
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