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Itraconazole composite powder and preparation method thereof

A technology of itraconazole and composite powder, which is applied in the field of itraconazole composite powder and its preparation, can solve the problems affecting the clinical efficacy of drugs and poor dispersibility, and achieve excellent dissolution effect, simple process, and easy The effect of the operation

Active Publication Date: 2010-07-21
BEIJING UNIV OF CHEM TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the surface energy of small particles is high, especially for nano-sized particles, the dispersion is not good, and the agglomeration phenomenon is serious, which affects the clinical efficacy of drugs.

Method used

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  • Itraconazole composite powder and preparation method thereof
  • Itraconazole composite powder and preparation method thereof
  • Itraconazole composite powder and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0038] A: Weigh 0.35g of polyvinylpyrrolidone K30 and dissolve it in 20mL of deionized water. After it is completely dissolved, pour it into a stirring tank;

[0039] B: Weigh again 0.35g of itraconazole bulk drug and dissolve it in 10mL of tetrahydrofuran to obtain a solution of itraconazole bulk drug with a concentration of 3.5g / 100mL;

[0040] C: At a stirring speed of 1000rpm, quickly add the obtained raw drug solution into the stirring tank, so that the itraconazole drug is precipitated at 30°C, and stirred for 30 minutes to obtain a slurry of itraconazole drug particles;

[0041] D: Spray-dry the obtained slurry, select SD-Basic spray dryer, set the inlet temperature of the spray dryer to 140°C, the outlet temperature to 63°C-70°C, the feed rate to 20mL / min, and the pressure to 0.8MPa, Obtain dry itraconazole composite powder.

[0042] Observing with an electron scanning electron microscope, the particle size of the obtained composite powder is 0.5 μm to 15 μm, and the ...

Embodiment 2

[0044] A: Weigh 0.25g of hydroxypropyl methylcellulose and dissolve it in 250mL of deionized water. After it is completely dissolved, pour it into a stirring tank;

[0045]B: Take again 0.25g of itraconazole bulk drug and dissolve it in 25mL of nitrogen methyl pyrrolidone to obtain a solution of itraconazole bulk drug with a concentration of 1g / 100mL;

[0046] C: At a stirring speed of 800rpm, quickly add the obtained raw drug solution into the stirring tank, so that the itraconazole drug is precipitated at 20°C, and stirred for 20 minutes to obtain a slurry of itraconazole drug particles;

[0047] D: Spray-dry the obtained slurry, choose SD-Basic spray dryer, set the inlet temperature of the spray dryer to 100°C, the outlet temperature to 55°C-62°C, the feed rate to 10mL / min, and the pressure to 0.6MPa, Obtain dry itraconazole composite powder.

[0048] Observing with an electron scanning electron microscope, the particle size of the obtained composite powder is 1 μm to 10 μ...

Embodiment 3

[0050] A: Weigh 0.1g of hydroxypropyl methylcellulose and dissolve it in 144mL of deionized water. After it is completely dissolved, pour it into a stirring tank;

[0051] B: Weigh 0.1 g of itraconazole raw material drug and dissolve it in 7.2 mL of methanol / tetrahydrofuran co-solvent with a volume ratio of 1 / 1 to obtain a solution of itraconazole raw material drug with a concentration of 1.38 g / 100 mL;

[0052] C: At a stirring speed of 1000rpm, quickly add the obtained raw drug solution into the stirring tank, so that the itraconazole drug is precipitated at 15°C, and stirred for 10 minutes to obtain a slurry of itraconazole drug particles;

[0053] D: Pour the obtained slurry into liquid nitrogen, and use a CHRiST LT-105 freeze dryer to dry the ice cubes containing itraconazole drug particles to obtain dry itraconazole composite powder.

[0054] Observing with an electron scanning electron microscope, the particle size of the obtained composite powder is 0.5 μm to 1 μm, and...

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Abstract

The invention relates to itraconazole composite powder and a preparation method thereof. The method comprises the following steps: dissolving itraconazole medicine into an organic solvent; adding the mixture of the itraconazole medicine and the organic solvent into a water solution with hydrophilic accessory ingredients for in-situ precipitation to separate out medicine; obtaining the nanometer amorphous itraconazole medicine grain turbid liquor; carrying out spraying drying or freeze drying on the obtained itraconazole medicine turbid liquor to obtain micron level itraconazole high molecular accessory ingredient composite powder; and then, dispersing the powder into water to obtain the uniform nanometer amorphous itraconazole medicine grain turbid liquor. The itraconazole high molecular accessory ingredient composite powder has good water-solubility and high dissolution speed, in addition, the operation is simple, the amplification is easy, the production cost is low, and the invention lays the foundation for the industrial production of the itraconazole medicine and the development and the utilization of novel preparations of the itraconazole medicine.

Description

Technical field: [0001] The invention relates to an itraconazole composite powder and a preparation method thereof, belonging to the field of medicine preparation. Background technique: [0002] Itraconazole is a triazole antifungal drug that is insoluble in water and has antibacterial effects on both deep fungi and superficial fungi. The chemical name is (±)-cis-4-[4-[4-4-[[2-(2,4-dichlorophenyl)-2-(1H-1,2,4-triazole-1 -Methyl)-1,3-dioxolan-4-yl]methoxy]phenyl]-1-piperazine]phenyl]-2,4-dihydro-2-(1-methylpropane Base)-3H-1,2,4-triazol-3-one, its structural formula is as follows: [0003] [0004] Itraconazole is poorly soluble in water and has poor oral absorption, resulting in low bioavailability. The formulations of itraconazole currently on the market include injections, capsules and oral solutions. PCT application WO85 / 02767 and U.S. Patent No. 4,764,604 disclose the inclusion of itraconazole molecules with cyclodextrins to achieve the effect of increasing solubi...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/14A61K31/496A61P31/10
Inventor 陈建峰肖光庭乐园王洁欣
Owner BEIJING UNIV OF CHEM TECH
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