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Dabigatran etexilate nano mixed micelle and preparation method thereof

A technology of dabigatran etexilate and mixed micelles, applied in the field of medicine, can solve the problems of low solubility, unsolved P-gp efflux, restricted application, etc., and achieves high bioavailability, improved bioavailability, and accelerated solubility Effect

Active Publication Date: 2016-10-12
SICHUAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although the problem of its low solubility has been solved, after oral administration of the capsule, its oral bioavailability is still only 6.5%, which limits its clinical application to a certain extent
[0007] The research on dabigatran etexilate preparations in the prior art basically continues the idea of ​​solving the problem of low solubility of the commercially available preparations, but does not solve the technical problem of P-gp efflux

Method used

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  • Dabigatran etexilate nano mixed micelle and preparation method thereof
  • Dabigatran etexilate nano mixed micelle and preparation method thereof
  • Dabigatran etexilate nano mixed micelle and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0053] Take 3 mL of 50 mg / mL Soluplus dichloromethane solution and 1 mL of 25 mg / mL Vitamin E-TPGS dichloromethane solution in a 25 ml round-bottomed flask containing 5 mg of dabigatran etexilate, and sonicate the carrier material and the drug is fully dissolved. The solution was placed in a rotary evaporator at 37 °C for 40 minutes to evaporate the organic solvent to dryness, and placed in a vacuum oven at room temperature overnight to remove a small amount of residual solvent to obtain a dry and transparent drug film skeleton. Then add 2 ml of deionized water for ultrasonic hydration to obtain the dabigatran etexilate Soluplus / Vitamin E-TPGS nano-mixed micellar preparation solution.

Embodiment 2

[0055] Take 2 mL of 50 mg / mL Soluplus dichloromethane solution and 3 mL of 25 mg / mL Vitamin E-TPGS dichloromethane solution in a 25 ml round-bottomed flask containing 5 mg of dabigatran etexilate, and sonicate the carrier Materials and drugs are fully dissolved. The solution was placed in a rotary evaporator at 37 °C for 40 min to evaporate the organic solvent to dryness, and placed in a vacuum oven overnight at room temperature to remove a small amount of residual solvent to obtain a dry and transparent drug film skeleton. Then add 2 ml of deionized water for ultrasonic hydration to obtain the dabigatran etexilate Soluplus / Vitamin E-TPGS nano-mixed micellar preparation solution.

Embodiment 3

[0057] Take 3 mL of 50 mg / mL Soluplus dichloromethane solution and 1 mL of 25 mg / mL Vitamin E-TPGS dichloromethane solution in a 25 ml round-bottomed flask containing 7 mg of dabigatran etexilate, and sonicate the carrier material and the drug is fully dissolved. The solution was placed in a rotary evaporator at 37 °C for 40 min to evaporate the organic solvent to dryness, and placed in a vacuum oven overnight at room temperature to remove a small amount of residual solvent to obtain a dry and transparent drug film skeleton. Then add 2 ml of deionized water for ultrasonic hydration to obtain the dabigatran etexilate Soluplus / Vitamin E-TPGS nano-mixed micellar preparation solution.

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Abstract

The invention provides dabigatran etexilate nano mixed micelle and a preparation method thereof. A film dispersion method is adopted for preparing the soluplus / VitaminE-TPGS nano mixed micelle of the dabigatran etexilate, and the particle size is within 70-100 nm.

Description

technical field [0001] The invention specifically relates to a nano-mixed micelle of dabigatran etexilate and a preparation method and application thereof, belonging to the technical field of medicine. Background technique [0002] Atrial fibrillation is the most common rapid supraventricular arrhythmia, which may lead to a variety of adverse consequences, among which stroke is one of the most serious complications, with severe disability and high risk of death. Half of the patients die within one year. In addition, artificial joint replacement may also cause a series of adverse complications, such as deep vein thrombosis and pulmonary embolism, which may even endanger the life of the patient in severe cases. Anticoagulant therapy is the key to reducing atrial fibrillation-related stroke mortality and preventing systemic embolism. [0003] Dabigatran etexilate is the most cutting-edge new generation of oral anticoagulant direct thrombin inhibitors, which can provide effecti...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/107A61K31/4439A61K47/34A61P7/02
CPCA61K9/1075A61K31/4439A61K47/32
Inventor 龚涛张志荣胡梅符垚孙逊
Owner SICHUAN UNIV
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