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Preparation of indissoluble medicament nano granule

A technology of insoluble drugs and nanoparticles, applied in the field of medicine, can solve the problems of low solubility, high toxicity and side effects, and low bioavailability of insoluble drugs, so as to improve bioavailability, good stability of preparations, and increase saturation solubility Effect

Inactive Publication Date: 2008-12-17
KANGYA OF NINGXIA PHARMA +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The purpose of the present invention is to provide a simple, rapid, less energy-consuming, and easy-to-scale method for preparing insoluble drug nanoparticles, thereby providing a solution to the problems of low solubility, high toxicity and side effects, and low bioavailability of insoluble drugs. Formulation method and a new dosage form for developing poorly soluble drugs

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] The preparation of embodiment 1 itraconazole nanosuspension

[0028] The present invention contains the following components in every 100ml itraconazole nanosuspension:

[0029] Itraconazole 1g, N-methylpyrrolidone 6ml, stabilizer 0.2g, co-stabilizer 0.05g, isotonic regulator 2.2g, and the rest is water. The stabilizer is poloxamer 188, the co-stabilizer is sodium deoxycholate, and the isotonic regulator is glycerol.

[0030] Preparation:

[0031] 1. Preparation of drug solution Add itraconazole to N-methylpyrrolidone, heat and stir (60°C, 500rpm) until the drug is completely dissolved, continue to stir for 15min, let cool, filter through a 0.22μm membrane, and set aside.

[0032] 2. Preparation of stabilizer solution Add glycerin to water, stir to dissolve, then add poloxamer 188, stir or sonicate until dissolved, finally add sodium deoxycholate, and sonicate to dissolve. 0.22μm membrane filtration, spare.

[0033] 3. The preparation method of stabilizer replacemen...

Embodiment 2

[0038] The preparation of embodiment 2 paclitaxel nanosuspension

[0039] The present invention contains the following components in every 100ml paclitaxel nanosuspension:

[0040] Paclitaxel 0.17g, dimethylformamide 7ml, stabilizer 0.85g, co-stabilizer 0.05g, isotonic regulator 2.0g, and the rest is water. The stabilizer is PE-PEG2000, the co-stabilizer is Transcutol, and the isotonic regulator is glycerin.

[0041] Preparation:

[0042] 1. Preparation of drug solution Add PE-PEG2000 to dimethylformamide, stir to dissolve, then add paclitaxel, heat and stir (60°C, 500rpm) until the drug is completely dissolved, continue to stir for 15min, let cool, 0.22μm Membrane filtration, spare.

[0043] 2. Preparation of stabilizer solution Add glycerin to water, stir to dissolve, then add Transcutol, stir or sonicate until dissolved. 0.22μm membrane filtration, spare.

[0044] 3. Preparation of stabilizer replacement solution Add PE-PEG2000 and glycerin to water, and the rest are t...

Embodiment 3

[0051] The preparation of embodiment 3 hydroxycamptothecin nanosuspension

[0052] The present invention contains the following components in every 100ml hydroxycamptothecin nano suspension:

[0053] Hydroxycamptothecin 0.1g, dimethylimide 10ml, stabilizer 1.0g, co-stabilizer 0.05g, isotonic regulator 2.0g, and the rest is water. The stabilizer is PVP K30, the co-stabilizer is mPEG-DSPE, and the isotonic regulator is mannitol.

[0054] 1. Preparation of drug solution Add hydroxycamptothecin to dimethylimide, heat and stir (70°C, 500rpm) until the drug is completely dissolved, continue stirring for 15min, let cool, filter through a 0.22μm membrane, and set aside.

[0055] 2. Preparation of stabilizer solution Add mannitol into water, stir to dissolve, then add PVP K30 188, stir or sonicate until dissolved, finally add mPEG-DSPE, and sonicate to dissolve. 0.22μm membrane filtration, spare.

[0056] 3. The preparation method of stabilizer replacement solution is the same as "P...

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Abstract

The invention relates to the technical field of medicine, in particular to a preparation method of nano-particles of insoluble drugs. The method includes the following steps: (1) dissolving the drugs in a first solvent (good solvent) to form solution, (2) blending the solution with a second solvent (poor solvent) to form premixed suspension, (3) applying energy on the premixed suspension to form the nano-particles, the average effective grain diameter of which is less than 2Mum. By adopting the technology combining micro-deposition and homogenization, the invention suspends the drugs in poor solvent (usually water) in a form of pure nano-crystal, thus solving the problem that solution is difficult to be prepared since the drugs are difficult to be dissolved in water and oil; compared with the corresponding injection for intravenous infusion and the oral preparations such as tablets, capsules, and the like, the preparation method of the invention can lower adverse reaction, reduce toxic and side effect, improve bioavailability, has sustained-release effect and is convenient to be used by patients.

Description

technical field [0001] The invention relates to the technical field of medicine, and relates to a preparation method of insoluble drug nanoparticles. Background technique [0002] In the past 10 years, high-throughput drug screening technology has been widely used, but most of the active compounds screened out have high molecular weight and strong hydrophobicity. According to statistics, at least 40% of drugs are currently restricted due to water solubility, and some drugs are even difficult to dissolve in organic solvents. In the preparation process, the use of cyclodextrin inclusion technology, surfactant solubilization, emulsion, microemulsion, inclusion compound, solid dispersion technology, polymer nanoparticles and lipid system can solve the low biological Utilization problem, but there are problems such as low drug loading, complex preparation process and poor stability. However, the nanoparticles mentioned in the present invention provide these drugs with the oppor...

Claims

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Application Information

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IPC IPC(8): A61K9/00A61K9/14A61K47/30A61K47/24
Inventor 何仲贵蒲晓辉孙进王永军刘锋刘晓红
Owner KANGYA OF NINGXIA PHARMA
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