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Self-microemulsion composition, capsule and preparation method of dabigatran etexilate

A technology for dabigatran etexilate and a composition, which is applied in the field of self-microemulsion compositions of dabigatran etexilate, can solve the problems of low dissolution rate of dispersible tablets and the like, so as to improve drug bioavailability, reduce drug cost, reduce Effects of adverse reactions

Active Publication Date: 2022-02-22
HUNAN HUIZE BIO PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The prepared dabigatran etexilate self-emulsifying dispersible tablet can be self-emulsified in vivo to form a microemulsion with a particle size of about 200nm after oral administration, and the prepared self-emulsion is easy to precipitate when placed at room temperature. Ethylene glyceride is used as an emulsifier, which makes the dissolution rate of dispersible tablets low in the body, and there are limitations in the actual application process

Method used

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  • Self-microemulsion composition, capsule and preparation method of dabigatran etexilate
  • Self-microemulsion composition, capsule and preparation method of dabigatran etexilate
  • Self-microemulsion composition, capsule and preparation method of dabigatran etexilate

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0054] The prescription is as follows:

[0055] Dabigatran etexilate: 15mg;

[0056] The total mass of SMEDDS carrier is 600mg: the mass ratio of oil phase: emulsifier: co-emulsifier is: 2.5:5:2.5;

[0057] The oil phase is glycerol monolinoleate; the emulsifier is RH40; and the co-emulsifier is propylene glycol.

[0058] The preparation process refers to Experiments 1 and 2: the drug loading of the obtained dabigatran etexilate self-microemulsion composition is 2.5%.

Embodiment 2

[0060] The prescription is as follows:

[0061] Dabigatran etexilate: 15mg;

[0062] The total mass of SMEDDS carrier is 375mg: the mass ratio of oil phase: emulsifier: co-emulsifier is 2:5:3;

[0063] The oil phase is glycerol monolinoleate; the emulsifier is RH40; and the co-emulsifier is PEG400.

[0064] The preparation process refers to Experiments 1 and 2: the drug loading of the obtained dabigatran etexilate self-microemulsion composition is 4%.

Embodiment 3

[0066] The prescription is as follows:

[0067] Dabigatran etexilate: 15mg;

[0068] The total mass of SMEDDS carrier is 800mg: the mass ratio of oil phase: emulsifier: co-emulsifier is 3:5:2;

[0069] The oil phase is a mixed oil phase of oleic acid and MCT, and the mass ratio of the two is 8:2; the emulsifier is a mixed emulsifier of Labrasol and RH40, and the mass ratio of the two is 3:1; the co-emulsifier for Transcutol P.

[0070] The preparation process refers to Experiments 1 and 2: the drug loading of the obtained dabigatran etexilate self-microemulsion composition is 1.87%.

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Abstract

The invention belongs to the technical field of medicine, and specifically discloses a self-microemulsion composition of dabigatran etexilate, a capsule and a preparation method thereof. Described self-microemulsion composition comprises: dabigatran etexilate and SMEDDS carrier; Described SMEDDS carrier comprises: at least one oily phase, at least one emulsifier, at least one co-emulsifier; Described self-microemulsion composition The particle size of the microemulsion formed by dispersing into the aqueous medium is less than 100nm. The self-microemulsion composition provided by the invention can not only effectively increase the drug loading of dabigatran etexilate in the self-microemulsion composition solution, but also the prepared self-microemulsion composition has a large solubility, exists stably at normal temperature, and can It forms uniform and stable nanoemulsion with water in the gastrointestinal tract, and the self-emulsification time is short during the preparation process, and the preparation process is simple.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a self-microemulsion composition of dabigatran etexilate, a capsule and a preparation method thereof. Background technique [0002] Dabigatran etexilate (English name: Dabigatran etexilate) chemical name is 3-[[[2-[[[4-[[[(hexyloxy)carbonyl]amino]iminomethyl]phenyl]amino]methyl Base]-1-methyl-1H-benzimidazol-5-yl]carbonyl](pyridin-2-yl)amino]ethyl propionate, the structural formula is as shown in formula I, developed by Boehringer Ingelheim, Germany It is a direct thrombin inhibitor with multiple characteristics, which can be used to prevent deep vein thrombosis and prevent stroke after surgery. Dabigatran etexilate capsules (trade name: Pradaxa), which were launched in Germany and the UK in 2008, were approved by the FDA in 2010, and were approved in my country in 2013. They are used for stroke and systemic Embolism prevention. After oral absorption, dabigatran etexilate can ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/107A61K9/48A61K47/44A61K47/14A61K31/4439A61P7/02A61P9/00A61P9/10A61P9/06
CPCA61K9/1075A61K9/4808A61K9/4858A61K47/44A61K47/14A61K31/4439A61P7/02A61P9/00A61P9/10A61P9/06
Inventor 黄建国易木林周群罗熙周旋
Owner HUNAN HUIZE BIO PHARMA CO LTD
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