Preparation method of composite carrier applied to drug solubilization

A composite carrier and drug technology, applied in the field of medicine, can solve the problems of easy aging of solid dispersions, low drug loading of liposomes, and reduced solubility, and achieves inhibition of insoluble drug crystallization, improvement of drug bioavailability, and good bacteriostasis. active effect

Pending Publication Date: 2022-07-15
ZHEJIANG UNIV OF TECH
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] The insoluble drug carriers used in the above-mentioned drug solubilization system and technology still have limitations in terms of the solubility of insoluble drugs in water, the stability of the solubilization system, and bacteriostasis. will still be limited in the preparation of
For example, nanocrystals have poor thermal stability, which will increase particle size and reduce solubility; liposomes have low drug loading and poor carrier stability, and their structures are easily destroyed under external influences; solid dispersions are prone to aging and poor stability ; When preparing cyclodextrin inclusion complexes, the solubility of natural cyclodextrins in water and organic solvents is small, which limits the size of molecules that can be included, and shows certain nephrotoxicity

Method used

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  • Preparation method of composite carrier applied to drug solubilization
  • Preparation method of composite carrier applied to drug solubilization
  • Preparation method of composite carrier applied to drug solubilization

Examples

Experimental program
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Effect test

Embodiment 1

[0017] Select 0.3g of poloxamer polymer, 0.3g of liquidambar, and 0.3g of terpineol, and heat poloxamer, liquidambar, and terpineol in an oil bath at 75°C and vigorously stir for 1.5h , to obtain a homogeneous and stable hot melt, then add 15% silymarin of the total mass of the system, continue to stir vigorously for 30 minutes to obtain a homogeneous system, cool to obtain a solubilization system in a colloidal state.

[0018] Set the temperature of the intelligent dissolution tester to 37±0.5°C, the rotation speed to 100r / min, add 900ml of ultrasonically degassed distilled water to the dissolution vessel, accurately weigh 1g of the solubilization system of silymarin, put it into the dissolution vessel, and start to rotate Timing, at 5min, 10min, 20min, 40min, 60min respectively, use a syringe to extract 10ml of the dissolution solution, and immediately add isothermal distilled water to make up 900ml. After sampling, continue to rotate the stirring rod until the water solubil...

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Abstract

The invention discloses a preparation method of a composite carrier applied to drug solubilization, sweetgum, poloxamer and terpilenol are used as the composite carrier, the mass ratio of sweetgum to poloxamer is 1: (1-6), the mass ratio of sweetgum to terpilenol is 1: (1-6), and the mass ratio of insoluble drugs is 10%-40% of the total mass of the system. The solid dispersion is prepared by taking silymarin as a model drug, adopting a hot melting method and taking sweetgum, poloxamer and terpilenol as composite carriers, the accumulative dissolution rate of the solid dispersion in simulated gastric juice and intestinal juice reaches 91.8% within 40 minutes, and the saturation solubility of the solid dispersion is improved by 42 times.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a preparation method of a composite carrier for drug solubilization. Background technique [0002] Due to the low solubility of water-soluble drugs in water, the absorption and distribution of drugs in the body are affected, and the drugs are difficult to reach the minimum concentration required for treatment, difficult to be absorbed by the body, and low bioavailability, which limits their clinical application. At the same time, due to the low drug content of poorly soluble drugs in water solvents, it is difficult to realize the diversification of their dosage forms. At present, 40% of the drugs on sale and 80-90% of the drugs under research are insoluble drugs. Therefore, the change of the solubility of these drugs has a significant impact on their absorption. At present, there are many methods for improving the solubility of poorly soluble drugs, such as nanocrys...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/26A61K47/10A61K47/44
CPCA61K47/26A61K47/10A61K47/44
Inventor 韩鹤黄灿金博会赵戈阳付媛丽金志敏
Owner ZHEJIANG UNIV OF TECH
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