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Method for preparing ultrafine particles of water-insoluble or insoluble medicine

A technology of ultra-fine particles and drugs, which is applied in the direction of pharmaceutical formulations, medical preparations containing active ingredients, organic active ingredients, etc., can solve the problems of precise control of drug particles, and achieve low cost, uniform and stable ultra-fine particles, Effect of improving solubility and bioavailability

Active Publication Date: 2012-12-26
BRIGHTGENE BIO MEDICAL TECH (SUZHOU) CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although the liquid phase precipitation method has the characteristics of simple process, large operating flexibility and small investment in equipment, the process of preparing nano-microstructure drug particles cannot achieve more precise control of the particle size of the drug particles. Increased bioavailability and potency exert adverse effects

Method used

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  • Method for preparing ultrafine particles of water-insoluble or insoluble medicine
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  • Method for preparing ultrafine particles of water-insoluble or insoluble medicine

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0039] Example 1 Preparation of ultrafine particles of itraconazole (ITA) by dispersing itraconazole (ITA) in hydroxypropylmethylcellulose (HPMC)

[0040] First, dissolve 0.5g of itraconazole (ITA) in 50ml of methanol / tetrahydrofuran (1:1) mixed solvent, and shake it for about 10 minutes to completely dissolve it to obtain solution A 1 ; Then prepare the 8.0mg / ml HPMC aqueous solution of 750ml, stir and make it mix homogeneously, get solution B 1 ; Then, at a stirring rate of 500rpm, the raw material solution A 1 Press into solution B through a single-channel PTFE membrane with an average pore size of 100 nm (POREFLON series from Sumitomo Electric, model: FP-010-60) 1 In the process, a white suspension of ultrafine particles is generated, and the stirring is continued for 2 minutes to make the reaction uniform; then the precipitate obtained is filtered with a 1.0 μm filter membrane to remove larger particles; finally, the slurry that produces ultrafine particles is freeze-d...

Embodiment 2

[0043] Example 2 Polyvinylpyrrolidone (PVP) disperses itraconazole (ITA) to prepare its ultrafine particles

[0044] First, dissolve 0.5g of itraconazole (ITA) in 50ml of methanol / tetrahydrofuran (1:1) mixed solvent, and shake it for about 10 minutes to completely dissolve it to obtain solution A 2 ; Then prepare the PVP aqueous solution of 8.0mg / ml of 750ml, stir and make it mix homogeneously, obtain solution B 2 ; Again, at a stirring rate of 500rpm, the raw material solution A 2 , pressed into solution B through a single-channel PTFE membrane with an average pore size of 100 nm (POREFLON series from Sumitomo Electric, model: FP-010-60) 2 In the process, a white ultrafine particle suspension is generated, and the stirring is continued for 2 minutes to make the reaction uniform; then the precipitate obtained is filtered with a 1.0 μm filter membrane to remove larger particles; finally, the slurry that produces particles is subjected to freeze-drying treatment or Spray dry...

Embodiment 3

[0047] Example 3 GC Headspace Sampling Method to Detect Residues of THF and Methanol in ITA Composite Nanoparticles

[0048] Use the GC headspace sampling method to detect the solvent residue in the ITA composite nanoparticles obtained in Implementation 1 and Example 2. The results show that the THF content is about 11ppm in ITA / HPMC, and the THF content in ITA / PVP is about 23.7ppm. Methanol was not detected.

[0049] Using GC headspace sampling method to detect the residues of tetrahydrofuran and methanol after ITA / HPMC were dried by different methods, the methanol peak represented 1000ppm, and the tetrahydrofuran peak represented 500ppm. The results showed that the residues of the two solvents were far lower than the pharmacopoeia upper limit concentration.

[0050] Through the comparison of the above experimental results, it can be seen that it is more appropriate to choose HPMC as the dispersant and freeze-drying as the condition, and the residual organic solvent...

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Abstract

The invention discloses a method for preparing ultrafine particles of a water-insoluble or insoluble medicine. The method mainly comprises the following steps: dissolving the water-insoluble or insoluble medicine into other solvents to prepare a medicine solution; allowing the medicine solution to enter an aqueous solution, into which a stabilizing agent is dissolved, through a dispersing film to form a solution on which ultrafine medicine particles are suspended; and drying the solution on which ultrafine medicine particles are suspended to obtain the product. The invention also discloses the ultrafine medicine particles prepared by the method. By the method, the particle size range of the medicine particles can be controlled precisely. The method has the characteristics of simple process, low cost and environmental friendliness and meets the requirement of industrialized production.

Description

technical field [0001] The invention relates to the field of micronization of medicines, more specifically, to the field of ultrafine granulation, especially nanometerization, of water-insoluble medicines. Background technique [0002] According to statistics: more than one-third of the drugs in the United States Pharmacopoeia are poorly soluble drugs, and more than 40% of the workload in the development of new drugs is to improve the solubility and bioavailability of poorly soluble drugs. Currently, at least 40% of the drugs Its use is limited due to solubility problems. Therefore, improving the solubility and bioavailability of poorly soluble drugs has always been one of the main tasks in pharmaceutical research. It has been reported in the literature that the classic method of using mixed solvents or adding surfactants such as solubilizers and co-solvents can improve the solubility of drugs to a certain extent, but the addition of some surfactants will affect the absorpt...

Claims

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Application Information

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IPC IPC(8): A61K9/14A61K31/496A61P31/10
Inventor 袁建栋
Owner BRIGHTGENE BIO MEDICAL TECH (SUZHOU) CO LTD
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