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Hydrophobic drug solubilizing method based on cation-pi action

A hydrophobic drug and cationic technology, applied in the field of medicine, can solve the problems of toxicity, poor stability of solid dispersion, drug precipitation and other problems, and achieve the effect of simple method, high solubility and good safety

Pending Publication Date: 2021-07-13
WENZHOU INST UNIV OF CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The application overcomes the toxicity of using a large amount of surfactants or organic solvents in the prior art, and the precipitation of the drug may occur during the combination process with the drug; and the solid dispersion has the technical disadvantage of poor long-term storage stability

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0019] Experimental conditions:

[0020] Normal temperature (25°C) normal pressure (1 standard atmospheric pressure)

[0021] experimental method:

[0022] 1. Prepare an ethanol solution of quercetin with a known and definite concentration.

[0023] 2. Prepare an aqueous solution of quercetin with a saturated unknown concentration.

[0024] 3. ZnCl 2 Dissolve in water, configure ZnCl with a concentration of 0.125mol / l~2mol / l 2 aqueous solution, the AlCl 3 Dissolve in water and prepare AlCl with a concentration of 0.3125mol / l~0.5mol / l 3 Aqueous solution; quercetin concentration is 0.1mg / ml (ethanol), quercetin and ZnCl 2 and AlCl 3 Mix them separately and place them in a lyophilizer to drain the ethanol to obtain an aqueous solution of the mixture. The ultraviolet absorption spectrum of the aqueous solution of the mixture is detected by ultraviolet spectroscopy (U-2900, HITACHI, JAPAN). Solution A is an aqueous solution of quercetin, solution B is Zn 2+ + quercetin; C ...

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PUM

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Abstract

The invention provides a pharmaceutical composition, a solubilizing method of a hydrophobic drug, and application of cations in preparation of the pharmaceutical composition. The pharmaceutical composition comprises the hydrophobic drug and the cations. The cations and the hydrophobic drug form a cation-pi effect. A conjugated chemical system between aromatic rings in a medicine and a hydrophobic effect between the conjugated chemical system and water molecules are destroyed by utilizing a cation-pi effect formed by metal cations and the aromatic rings in the medicine, so that the aim of solubilizing the medicine is fulfilled. The solubility can be increased by 1-100 times.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a pharmaceutical composition, the application of cations in the preparation of the pharmaceutical composition, and a method for solubilizing hydrophobic drugs. Background technique [0002] More and more biologically active substances have been discovered or synthesized, and the resulting new chemical entities often have the problems of low biosolubility and low bioavailability, especially the active ingredients in natural medicines are mostly insoluble ingredients. Therefore, how to improve the solubility of poorly soluble drugs, improve the clinical efficacy of drugs, and improve the solubility and bioavailability of poorly soluble drugs play a very important role in the clinical application of these active substances. The solubilization methods that have been developed so far include: micellar solubilization, adding co-solvent or co-solvent, making solid dispersion, liposome ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/52A61K45/00A61K31/352A61K31/366A61K31/337A61K31/704A61K31/4745A61P35/00A61P31/04A61P31/12A61P29/00A61P7/00A61P13/00A61P5/00A61P37/06
CPCA61K47/52A61K45/00A61K31/352A61K31/366A61K31/337A61K31/704A61K31/4745A61P35/00A61P31/04A61P31/12A61P29/00A61P7/00A61P13/00A61P5/00A61P37/06
Inventor 方海平张峰王莉萍王超群李亚平
Owner WENZHOU INST UNIV OF CHINESE ACAD OF SCI
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