Voriconazole nano-micro composite powder and preparation method thereof

A voriconazole micro-, voriconazole-based technology, applied in the field of voriconazole micro-composite powder and its preparation, can solve the problems of not being widely used, toxic and side effects of organic solvents, unsuitable injections, etc., to achieve no toxic and side effects, avoid side effects, and be safe sex high effect

Active Publication Date: 2013-06-05
BEIJING WINSUNNY PHARMA CO LTD +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, sulfonbutane-β-cyclodextrin has certain physiological toxicity
In order to solve the above problems, there are mainly three types of methods in the current public literature: the first type uses auxiliary materials such as cyclodextrin or Tween as a solubilizer, such as CN200410098736, which uses hydroxypropyl-β-cyclodextrin as an auxiliary material to prepare freeze-dried powder Injections; CN200510068033 added auxiliary materials such as cyclodextrin and Tween; CN200510095595 disclosed a method for preparing voriconazole injections with cyclodextrin as auxiliary materials and using organic solvents; the voriconazole inclusion compound prepared by CN200710143810 and CN200910019770 also added cyclodextrin Dextrin au

Method used

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  • Voriconazole nano-micro composite powder and preparation method thereof
  • Voriconazole nano-micro composite powder and preparation method thereof
  • Voriconazole nano-micro composite powder and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] A: Weigh 250mg voriconazole crude drug and dissolve it in 25mL tetrahydrofuran; weigh 5g mannitol, 500mg sodium oleate, 1g polyethylene glycol 400, 1g polyethylene glycol stearate, dissolve it in 250mL water, and mix the drug solution with The aqueous solution is mixed and stirred to obtain a drug slurry;

[0033] B: freeze-dry the above slurry to obtain voriconazole composite powder. Take an appropriate amount of composite powder, disperse it in water, and prepare a transparent dispersion liquid of 5 mg / mL, and the average particle size of the drug particles is 80 nm. After the composite powder is sterilized, the powder for injection can be obtained.

Embodiment 2

[0035] A: Weigh 500mg of voriconazole crude drug and dissolve it in 25mL of methanol; weigh 5g of mannitol, 80mg of sodium oleate, 2g of polyethylene glycol 400, and 2g of polyethylene glycol stearate, dissolve it in 100mL of water, and mix the drug solution with The aqueous solution is mixed and stirred to obtain a drug slurry;

[0036] B: Voriconazole composite powder can be obtained by freeze-drying the above slurry. Take an appropriate amount of composite powder, disperse it in water, and prepare a transparent dispersion liquid of 2 mg / mL, and the average particle size of the drug particles is 120 nm. The composite powder is mixed with an appropriate amount of tablet auxiliary materials sodium carboxymethyl starch and magnesium stearate, granulated, and made into tablets after passing the tablet compression test.

Embodiment 3

[0038] A: Weigh 500mg voriconazole crude drug and dissolve it in a mixed solvent of 10mL methanol and 10mL tetrahydrofuran; weigh 10g mannitol, 100mg sodium oleate, 600mg polyethylene glycol 400, 1g polyethylene glycol stearate, 100mg egg The phospholipids were dissolved in 750mL of water, and the drug solution was mixed with the aqueous solution and stirred to obtain a drug slurry;

[0039] B: Spray-dry the above slurry at an inlet temperature of 90°C to obtain voriconazole composite powder. Take an appropriate amount of composite powder, disperse it in water, and make a transparent dispersion liquid of 8mg / mL, and the average particle size of the drug particles is 50nm. The above composite powder is mixed with an appropriate amount of tablet auxiliary materials microcrystalline cellulose, croscarmellose sodium and talcum powder, granulated and passed the test to make capsules.

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Abstract

The invention discloses voriconazole nano-micro composite powder, wherein a safe and reliable pharmaceutical auxiliary material is adopted to replace cyclodextrin, tween and other auxiliary materials generally-used in the current voriconazole preparations or physiologically toxic organic solvents as a solvent so as to improve product safety, the composite powder can be dispersed in water so as to obtain a transparent dispersion, and the drug has characteristics of high concentration, small particle size and easy absorption by human body. The present invention provides a voriconazole nano-micro composite powder preparation method, which has characteristics of simple operation, easy enlargement and industrial production, and good application prospect.

Description

technical field [0001] The invention relates to a voriconazole micro-composite powder and a preparation method thereof, belonging to the field of pharmaceutical preparations. Background technique [0002] Voriconazole, chemical name: (2R,3S)-2-(2,4-difluorophenyl)-3-(5-fluoro-4-pyrimidine)-1-(1H-1,2,4 -Triazol-1-yl)-2-butanol, which is a second-generation triazole broad-spectrum antifungal new drug developed by Pfizer Pharmaceutical Company of the United States, was listed in 2002. Voriconazole is a derivative of fluconazole. Its chemical structure is to add a methyl group to the fluconazole structure and replace the triazole ring with a fluoropyrimidine ring. Its molecular structure is as follows: [0003] [0004] As a new type of broad-spectrum antifungal drug, voriconazole has strong antifungal activity in vivo and in vitro, and is active against a wide range of pathogenic yeasts, filamentous fungi, and dimorphic fungi, and is also effective against drug-resistant fu...

Claims

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Application Information

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IPC IPC(8): A61K9/14A61K31/506A61K47/44A61P31/10
Inventor 陈建峰张智亮乐园王洁欣黄河耿玉先张志兵朱文珍
Owner BEIJING WINSUNNY PHARMA CO LTD
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