High-efficiency stabilizing agent for hard-soluble medicine nanometer system

A technology of insoluble drugs and stabilizers, applied in the field of medicine, can solve the problems of complicated prescription composition and other problems

Inactive Publication Date: 2012-05-16
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The stabilizers currently used in the field of drug delivery systems have great limitations. Generally, ionic surfactants, non-ionic surfactants and high molecular polymers are used in combination to provide charge stabilization effects, steric stability, etc. effect and reduced particle settling velocity, complicating formulation composition

Method used

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  • High-efficiency stabilizing agent for hard-soluble medicine nanometer system
  • High-efficiency stabilizing agent for hard-soluble medicine nanometer system

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0015] Itraconazole Nanosuspension

[0016] Itraconazole 1.0g

[0017] Poloxamer 188 0.5g

[0018] Chitosan 0.2g

[0019] Distilled water 100ml

[0020] Preparation Process:

[0021] Place itraconazole 1% (w / v) in an aqueous solution containing poloxamer 1880.5% and chitosan 0.2%, and ultrasonically disperse to obtain a coarse dispersion system of itraconazole. The chitosan is chitosan with a molecular weight of 50kDa and a deacetylation degree of 86.5%. The obtained coarse dispersion system is pre-circulated twice at 100, 300, 500, 800, 1000 and 1200bar by using a high-pressure homogenizer, and circulated at 1400bar for 20 times to obtain itraconazole nanosuspension, which is diluted with water to an appropriate Concentration, its particle diameter measured by laser particle size analyzer is 342nm, and ξ potential is 26mV, and this system can be stable more than 10 days ( figure 2 ). Compared with the formulation without chitosan, the particle size decreased by 37%. ...

Embodiment 2

[0023] Itraconazole Nanosuspension

[0024] Itraconazole 1.0g

[0025] Poloxamer 188 0.5g

[0026] Trimethyl Chitosan 0.5g

[0027] Distilled water 100ml

[0028] Preparation Process:

[0029] Put itraconazole 1% (w / v) in an aqueous solution containing poloxamer 1880.5% and trimethyl chitosan 0.5%, and ultrasonically disperse to obtain a coarse dispersion system of itraconazole. The trimethyl chitosan is a trimethyl chitosan with a molecular weight of 50kDa and an amino substitution degree of 40%. The obtained coarse dispersion system is pre-circulated twice at 100, 300, 500, 800, 1000 and 1200bar by using a high-pressure homogenizer, and circulated at 1400bar for 20 times to obtain itraconazole nanosuspension, which is diluted with water to an appropriate Concentration, the laser particle size analyzer measures its particle size as 421nm, and the ξ potential is 39mV, and the system can be stable for more than 10 days. Compared with the formulation without trimethyl chit...

Embodiment 3

[0031] Itraconazole Nanosuspension

[0032] Itraconazole 1.0g

[0033] Poloxamer 188 0.5g

[0034] Polyethyleneimine 0.1g

[0035] Distilled water 100ml

[0036] Preparation Process:

[0037] Put itraconazole 1% (w / v) in an aqueous solution containing poloxamer 18880.5% and polyethyleneimine 0.1%, and ultrasonically disperse to prepare a coarse dispersion system of itraconazole. The polyethyleneimine is a branched polyethyleneimine with a molecular weight of 25kDa. The obtained coarse dispersion system is pre-circulated twice at 100, 300, 500, 800, 1000 and 1200bar by using a high-pressure homogenizer, and circulated at 1400bar for 20 times to obtain itraconazole nanosuspension, which is diluted with water to an appropriate Concentration, the laser particle size analyzer measures its particle size as 358nm, and the ξ potential is 32mV. The system can be stable for more than 10 days. Compared with the formulation without polyethyleneimine, the particle size decreased by 3...

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Abstract

The invention belongs to the technical field of medicinal preparations and specifically relates to a cationic polymer stabilizing agent capable of substantially reducing the particle size of nanoparticles of a hard-soluble medicine and improving stability of a system. A cationic polymer used as the stabilizing agent comprises chitosan of different molecular weight and different deacetylation degrees, trimethyl chitosan of different molecular weight and different substitution degrees, polyethyleneimine of different molecular weight, polylysine, etc. When a nanometer suspended system of a hard-soluble medicine is being prepared by using different methods, 0.1 to 0.5% of the cationic polymer is added as a stabilizing agent; through electrostatic repulsion, steric hindrance and increased kinetic stability, aggregation and coalescence of particles are effectively prevented and a particle size is inhibited from increasing, thereby preparing nanometer crystals or nanoparticles with a small particle size and good stability. The nanometer crystals or nanoparticles can be further solidified as needed so as to obtain solid dosage forms, e.g., tablets, capsules, etc.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a class of high-efficiency cationic polymer stabilizers which can significantly reduce the particle diameter of insoluble drug nanoparticles and improve the system stability. Background technique [0002] In drug development, it is found that nearly 40% of the drugs are insoluble in water, and this situation reaches 60% in the drugs obtained by direct synthesis. It is often difficult for poorly soluble drugs to achieve the bioavailability required for treatment after oral administration through traditional preparation methods, or to make preparations for intravenous administration, which greatly limits the application of such drugs. Although the solubility of insoluble drugs can be improved by making liposomes, micronization, solid dispersion, cyclodextrin inclusion and other pharmaceutical methods, these methods all have low drug loading, complicated preparation pro...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/36A61K9/20A61K9/48A61K47/32A61K47/34
Inventor 毛世瑞孙伟
Owner SHENYANG PHARMA UNIVERSITY
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