Pradaxa-containing microemulsion preparation

A dabigatran etexilate and microemulsion technology, applied in the field of medicine, can solve the problems of low bioavailability, complex process, poor dissolution of dabigatran etexilate, etc.

Inactive Publication Date: 2015-08-12
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The dispersion preparation can disintegrate rapidly and evenly disperse in water, and it is the same as the commercially available acid-containing pellet capsules containing dabigatran etexilate mesylate, which mainly solves the problem of poor dissolution of dabigatran etexilate in the stomach , improved the dissolution of dabigatran etexilate in the stomach, but still can not change the problem of poor solubility of dabigatran etexilate in the intestine, easy to separate out, and poor absorption, making the bioavailability of dabigatran etexilate low
At the same time, in the production process of dispersible tablets and dispersible granule capsules, the raw materials need to be micronized, which increases the production process and increases the cost.
[0013] Above-mentioned effort has only provided the dabigatran etexilate liposome or the solid dosage form containing dabigatran etexilate of preparation loaded down with trivial details or complex process or poor stability or bioavailability

Method used

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Examples

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Effect test

Embodiment 1

[0054] Embodiment 1 A kind of dabigatran etexilate microemulsion preparation, each raw material proportioning of this microemulsion preparation is as follows:

[0055] Specifications: 100ml

[0056]

[0057] Preparation process: Accurately weigh 0.25 g of dabigatran etexilate according to the prescription ratio, dissolve it in propylene glycol, add medium-carbon chain triglycerides, polyoxyethylene hydrogenated castor oil, and oleic acid, and stir continuously at room temperature until dissolved and mixed evenly. Obtain the drug-containing oil phase of dabigatran etexilate; dissolve poloxamer 188 and povidone K30 in deionized water, and mix uniformly to obtain the water phase; heat the oil phase and the water phase to 60° C. Slowly drop the oil phase into the water phase, stir at high speed for 8 minutes, continue to add sorbic acid, stevioside, and aspartame, and finally add deionized water to make the volume to 100ml to obtain dabigatran etexilate microemulsion.

Embodiment 2

[0058] Embodiment 2 A kind of dabigatran etexilate microemulsion preparation, each raw material proportioning of this microemulsion preparation is as follows:

[0059] Specifications: 100ml

[0060]

[0061] Preparation process: Accurately weigh 0.25 g of dabigatran etexilate according to the prescription ratio, dissolve it in propylene glycol, add medium-carbon chain triglycerides, castor oil, polyoxyethylene hydrogenated castor oil, and oleic acid, and stir continuously at room temperature until dissolved and Mix well to obtain the drug-containing oil phase of dabigatran etexilate; dissolve poloxamer 188 and povidone K30 in deionized water, and mix uniformly to obtain the water phase; heat the oil phase and the water phase to 60°C respectively, Under magnetic stirring, the oil phase was slowly dropped into the water phase, stirred at a high speed for 8 minutes, continued to add sorbic acid, stevioside, and aspartame, and finally added deionized water to settle to 100ml to...

Embodiment 3

[0062] Embodiment 3 A kind of dabigatran etexilate microemulsion preparation, each raw material proportioning of this microemulsion preparation is as follows:

[0063] Specifications: 100ml

[0064]

[0065] Preparation process: Accurately weigh 0.25 g of dabigatran etexilate according to the prescription ratio, dissolve it in propylene glycol, add medium-carbon chain triglycerides, egg yolk lecithin, and oleic acid, and stir continuously at room temperature until dissolved and mixed to obtain Dabigatran etexilate Gatran etexilate containing drug oil phase; Dissolve Poloxamer 188 and Povidone K30 in deionized water, mix well to obtain water phase; heat oil phase and water phase to 60°C respectively, under magnetic stirring, The oil phase was slowly dropped into the water phase, stirred at high speed for 8 minutes, continued to add sorbic acid, stevioside, and aspartame, and finally added deionized water to make the volume to 100ml, and obtained dabigatran etexilate microemu...

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Abstract

The invention relates to the technical field of medicine preparations, and particularly relates to a pradaxa-containing microemulsion preparation and a preparation method thereof. The pradaxa-containing microemulsion preparation is prepared by combination of a certain proportion of a surfactant, a cosurfactant, an oil phase, a water phase and a moderate amount of a stabilizer, a suspension aid, a sweetener and a preservative, the prepared pradaxa-containing microemulsion preparation is oil-in-water type, the particle size is in the range of 200-400 nm, appearance is clear transparent uniform, and stability is good. The microemulsion preparation, compared with an oral solid preparation, has the advantages of low production cost, simple preparation process and the like, after oral administration, dissolution of pradaxa in the gastrointestinal tract is increased, the bioavailability is improved, and the pradaxa-containing microemulsion preparation has the good market prospect.

Description

technical field [0001] The invention relates to a microemulsion preparation containing dabigatran etexilate, a preparation method and application thereof, and belongs to the technical field of medicine. Background technique [0002] Thrombosis is a major killer of human health, but compared with other diseases that attract more attention, ordinary people know little about the harm caused by thrombus. Due to poor diet and living habits, many people have become a high-risk group of thrombotic diseases, making the field of thrombotic diseases in my country present the characteristics of high incidence, high death, high disability, and high recurrence. In the European Union, venous thromboembolism (VTE) alone kills 500,000 people every year, more than twice the combined death toll from AIDS, breast cancer, prostate cancer and traffic accidents in the region. [0003] Currently, warfarin is the only oral antithrombotic drug approved by the FDA for the prevention of postoperative...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/107A61K31/4439A61P7/02
Inventor 郑春丽柴夫娟张雅捷丁亚飞刘建平朱家壁
Owner CHINA PHARM UNIV
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