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Eye use voriconazole nanocrystal preparation and preparation method thereof

A voriconazole ophthalmic and nanocrystalline technology, which is applied in the field of voriconazole ophthalmic nanocrystalline preparations and its preparation, can solve the problems of limited effect and poor solubility of voriconazole, and achieves the effects of good stability, reduced adverse reactions, and easy industrialized production.

Active Publication Date: 2014-12-10
HUBEI UNIV OF TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] The purpose of the present invention is to provide a voriconazole nano-crystal preparation with high permeability and good stability and its preparation method, so as to solve the limitation of the effect of voriconazole in the treatment of ocular fungal infection due to its poor solubility and the unique physiological barrier of the eye in the prior art. And other issues

Method used

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  • Eye use voriconazole nanocrystal preparation and preparation method thereof
  • Eye use voriconazole nanocrystal preparation and preparation method thereof
  • Eye use voriconazole nanocrystal preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0041] (1) Disperse 5 g of voriconazole and 50 g of fat-soluble stabilizer in 50 ml of organic solvent to obtain drug solution A; wherein, the fat-soluble stabilizer is Eudragit RS100 or EVA, and the organic solvent is an acetone-methanol mixture with a volume ratio of 3:1 ;

[0042] (2) Disperse 10g of water-soluble stabilizer and 20g of penetration enhancer in 600ml of distilled water to obtain an aqueous dispersion medium, and obtain aqueous dispersion medium solution B, wherein the water-soluble stabilizer is PVA or PVP, and the penetration enhancer is N -Methylpyrrolidone (Pharmasolve) and sodium hyaluronate, the ratio of the two penetration enhancers is 9:1;

[0043] (3) Disperse the drug solution A prepared in step (1) in the aqueous dispersion medium B prepared in step (2) under high-speed shear or ultrasonic conditions to obtain suspension C; wherein the high-speed shear condition It is a Fluko-FA25 high-shear dispersing and emulsifying machine, shearing at 13000rpm ...

Embodiment 2

[0048] (1) Disperse 0.5 g of voriconazole and 10 g of glyceryl monooleate in 20 ml of an organic solvent to obtain drug solution A; wherein the organic solvent is an acetone-PEG400 mixture with a volume ratio of 1:1;

[0049] (2) Disperse 40g of water-soluble stabilizer and 20g of penetration enhancer in 800ml of distilled water to obtain aqueous dispersion medium B, wherein the water-soluble stabilizer is Poloxamer 407, and the penetration enhancer is sodium hyaluronate and propylene glycol , the ratio of the two penetration enhancers is 1:4;

[0050] (3) Disperse the drug solution A prepared in step (1) in the aqueous dispersion medium B prepared in step (2) under high-speed shear or ultrasonic conditions to obtain suspension C; wherein the high-speed shear condition It is a Fluko-FA25 high-shear dispersing and emulsifying machine, shearing at 8000rpm for 10 minutes, the ultrasonic conditions are power 400-900W, ultrasonic ratio 2:2, ultrasonic frequency 30 times;

[0051] ...

Embodiment 3

[0055] (1) Disperse 20.0g of voriconazole and 100g of fat-soluble stabilizer in 200ml of organic solvent to obtain drug solution A; wherein the fat-soluble stabilizer is Eudragit RL100 and ethylene-vinyl acetate polymer (EVA), two fat-soluble stabilizers The solvent ratio is 4:1; the organic solvent is an acetone-ethanol mixture with a volume ratio of 2:1;

[0056] (2) Disperse 50g of water-soluble stabilizer and 20g of penetration enhancer in 600ml of distilled water to obtain aqueous dispersion medium B, wherein the water-soluble stabilizer is PVA, and the penetration enhancer is sodium lauryl sulfate and propylene glycol, two The ratio is 3:1; (3) Disperse the drug solution A prepared in step (1) in the aqueous dispersion medium B prepared in step (2) under high-speed shear or ultrasonic conditions to obtain suspension C Wherein the condition of high-speed shearing is Fluko-FA25 high-shear dispersing emulsifier, 13000rpm shearing 15min, the condition of ultrasonic is power ...

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Abstract

The invention provides an eye use voriconazole nanocrystal preparation and a preparation method thereof. The eye use voriconazole nanocrystal preparation is prepared from voriconazole, biodegradable polymer auxiliary material, a penetration enhancer, an osmotic pressure conditioning agent, a pH conditioning agent and distilled water, and is characterized in that the solubility of indissolvable voriconazole is improved by adopting the nanocrystal technique and using the eye use penetration enhancer, so as to enhance the adhesion and permeability between the preparation and the corneas. The voriconazole nanocrystal preparation takes EudragitRS100, PVA, and the like as main carrier materials and the precipitation method is adopted to prepare the voriconazole nanocrystal preparation; the novel eye use penetration enhancer with good safety and small stimulation is used to enhance the permeability of the cornea of the system; the voriconazole nanocrystal preparation can be used for eye administration of fat-soluble voriconazole; the preparation is good in stability, high in permeability and high in bioavailability and has no stimulation.

Description

technical field [0001] The invention relates to an ophthalmic preparation, in particular to a voriconazole ophthalmic nano crystal preparation and a preparation method thereof. Background technique [0002] In recent years, due to the wide application of antibiotics, glucocorticoids, immunosuppressants, etc., as well as the gradual increase in the application of contact lenses and vegetative trauma, the incidence of ocular fungal infections is on the rise. At the same time, due to the characteristics of insidious onset, long course of disease, lack of specific and effective treatment methods, and easy recurrence, the disease has become an infectious eye disease that is difficult to treat clinically and has a high blinding rate. At the same time, clinically, the drugs for ocular fungal infection are very scarce due to their own insoluble characteristics. In addition, the eye’s own barrier-like physiological structure makes it difficult for drugs to reach the lesion through th...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/10A61K9/14A61K31/506A61K47/32A61K47/34A61P31/10A61P27/02
Inventor 祝红达戴助徐瑶蔡萌尚星星
Owner HUBEI UNIV OF TECH
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