Method for realizing dispersion of indissolvable drug in water

A poorly soluble drug and dispersion technology, which is applied in pharmaceutical formulations, drug delivery, medical preparations with inactive ingredients, etc., can solve the problems that chitosan cannot be directly dissolved, limit the application range of chitosan, etc., and achieve good dispersibility. , easy to operate, to achieve the effect of dispersion

Pending Publication Date: 2020-04-17
INST OF BIOMEDICAL ENG CHINESE ACAD OF MEDICAL SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, chitosan cannot be directly dissolved in water, which limits the scope of application of chitosan

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] A method for realizing the dispersion of poorly soluble drugs in water according to the present embodiment includes steps:

[0029] 30 mg of chitosan with a molecular weight of 310,000 to 375,000 Da was dissolved in 1 mL of 1-ethyl-3-methylimidazole acetate (EMIMAc) ionic liquid at 125° C. and a stirring speed of 650 rpm to obtain 2.65 wt % of chitosan- ionic liquid system.

[0030] 5 mg of paclitaxel was dissolved in 1 mL of 2.65 wt % chitosan-ionic liquid system with stirring at room temperature. Place 0.1 mL of the obtained product in 5 mL of water for dialysis and stir to obtain a dispersed aqueous solution of a poorly soluble drug.

Embodiment 2

[0032] A method for realizing the dispersion of poorly soluble drugs in water according to the present embodiment includes steps:

[0033] 25 mg of chitosan with a molecular weight of 200,000 Da was dissolved in 1 mL of 1-ethyl-3-methylimidazolium acetate (EMIMAc) ionic liquid at 120 ° C and a stirring speed of 700 rpm to obtain 2.22 wt % chitosan-ion liquid system.

[0034] 4 mg paclitaxel was stirred and dissolved in 1 mL of 2.22 wt % chitosan-ionic liquid system at 37°C. 0.05 mL of the obtained product was dropped into 6 mL of water to obtain a poorly soluble drug dispersed aqueous solution.

Embodiment 3

[0036] A method for realizing the dispersion of poorly soluble drugs in water according to the present embodiment includes steps:

[0037] 20 mg of chitosan with a molecular weight of 310,000 to 375,000 Da was dissolved in 1 mL of 1-ethyl-3-methylimidazolium acetate (EMIMAc) ionic liquid at 140° C. under vortex conditions to obtain 1.78 wt % chitosan- ionic liquid system.

[0038] 6mg of camptothecin was stirred and dissolved in 1mL of 1.78wt% chitosan-ionic liquid system at room temperature. 0.1 mL of the obtained product was dropped into 5 mL of water to obtain a poorly soluble drug dispersed aqueous solution.

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Abstract

The invention discloses a method for realizing dispersion of an indissolvable drug in water. The method comprises the following steps: dissolving chitosan in ionic liquid to obtain a chitosan-ionic liquid system and then dissolving an indissolvable drug in the chitosan-ionic liquid system; and then putting the chitosan-ionic liquid system dissolved with the indissolvable drug into water to realizedispersion of the indissolvable drug in the water. The ionic liquid is 1, 3-dialkyl substituted imidazolium ionic liquid; the indissolvable drug comprises paclitaxel or a derivative thereof, and camptothecin or a derivative thereof. According to the method, a chitosan-ionic liquid system is used as a medium of the indissolvable drug, effective dispersion of the indissolvable drug in water can berealized, the steps are simple, and operation is easy and convenient. In addition, dispersion of insoluble drugs in water can be adjusted by designing and adjusting conditions such as the type of theionic liquid and the molecular weight of chitosan, so that targeted biological medicine application is realized.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and in particular relates to a method for dispersing insoluble drugs in water by using a chitosan-ionic liquid system as a medium. Background technique [0002] The poor water solubility of drugs limits its practical use to a large extent. Therefore, people have been working on how to effectively disperse insoluble drugs in water, improve their solubility in water, and improve their bioavailability. Get effective treatment. [0003] At present, chemical modification into salt, physical micronization, and polymer nano-embedding can improve the problem of insoluble drugs being difficult to be effectively used in water to a certain extent. However, the implementation of these methods is mostly complicated. Therefore, it is of great significance to develop new and simple methods for dispersing insoluble drugs in water. [0004] As a new type of solvent, ionic liquid has the adva...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/08A61K47/36A61K47/22A61L27/44
CPCA61K9/08A61K47/22A61K47/36A61L27/44
Inventor 李博轩朱敦皖张琳华冷希岗
Owner INST OF BIOMEDICAL ENG CHINESE ACAD OF MEDICAL SCI
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