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Method for preparing ultrafine particles of poorly water-soluble or insoluble drugs

A technology for ultra-fine particles and drugs, which is applied in powder delivery, antifungal agents, etc., can solve problems such as precise control of drug particles, and achieve the effects of low cost, simple process, uniform and stable ultra-fine particles

Active Publication Date: 2016-12-14
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 poorly water-soluble or insoluble drugs
  • Method for preparing ultrafine particles of poorly water-soluble or insoluble drugs
  • Method for preparing ultrafine particles of poorly water-soluble or insoluble drugs

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 is far...

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Abstract

The invention discloses a method for preparing ultrafine particles of water-insoluble or insoluble drugs. The method mainly includes: dissolving the water-insoluble or insoluble drugs in other solvents to obtain a drug solution; the drug solution passes through a dispersion membrane and enters the An aqueous solution in which a stabilizer is dissolved to form a solution in which ultrafine drug particles are suspended, and the solution in which ultrafine drug particles are suspended is dried to obtain the product. The invention also discloses the application of the ultrafine drug particles prepared by the above method in the indication of the drug. Using the above method to prepare ultrafine particles of drugs can achieve more precise control of the particle size range of drug particles, and this method also has the characteristics of simple process, low cost, and environmental friendliness, which is very suitable for industrial 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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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/14A61K31/496A61P31/10
Inventor 袁建栋
Owner BRIGHTGENE BIO MEDICAL TECH (SUZHOU) CO LTD
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