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Solid dispersion of antifungal agent

A solid dispersion and dispersion technology, applied in antifungal agents, pharmaceutical formulations, organic active ingredients, etc., can solve the problems of poor solubility in the small intestine and low bioavailability, and achieve stable preparation quality, simple preparation process, and improved solubility. Effect

Inactive Publication Date: 2015-04-29
BRIGHTGENE BIO MEDICAL TECH (SUZHOU) CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0011] The purpose of the present invention is to overcome the disadvantages of poor solubility and low bioavailability of the triazole antifungal agent posaconazole preparations in the prior art, and provide a novel posaconazole solid dispersion and its preparation method and medicament application

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0049] Example 1 Preparation of solid dispersion containing posaconazole and HP-β-CD (1:2)

[0050] Dissolve 3 g of posaconazole in 15 ml of methanol and HCl conc (10:1, v / v) mixed solution; Dissolve 6g HP-β-CD in 6ml purified water, then mix the two solvents, stir for 2h to get a clear solution, then pass the clear solution through 0.45μm polytetrafluoroethylene Filtrate with a filter (Rezist 30, Whatman, Dassel, Germany); cool in liquid nitrogen, and finally freeze-dry for 56 hours to obtain a white solid powder.

Embodiment 2

[0051] Example 2 Preparation of solid dispersion containing posaconazole and HBen-β-CD (1:4)

[0052] Dissolve 3 g of posaconazole in 15 ml of methanol and HCl conc (10:1, v / v); Dissolve 12g of HBen-β-CD in 12ml of purified water. Then the two solvents were mixed and stirred for 2 hours to obtain a clear solution, which was spray-dried with a spray dryer, the temperature at the inlet of the dryer was 115°C, and the temperature at the outlet was 65°C. After drying, the powder was collected and cooled to obtain a white solid powder.

Embodiment 3

[0053] Example 3 Preparation of solid dispersion containing posaconazole and SEB-β-CD (1:1)

[0054] Dissolve 3 g of posaconazole in 15 ml of methanol and HCl conc (10:1, v / v) mixed solution; 3g SEB-β-CD was dissolved in purified water to make a 50% SEB-β-CD solution. Then the two solvents were mixed, stirred for 2 hours to obtain a clear solution, and then the clear solution was filtered through a 0.45 μm polytetrafluoroethylene filter; cooled with liquid nitrogen, and finally freeze-dried for 56 hours to obtain a white solid powder.

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Abstract

The invention belongs to the field of a medicinal preparation and specifically relates to a posaconazole solid dispersion and a preparation method of the solid dispersion and drug use. The invention provides a posaconazole solid dispersion and its drug use. The posaconazole solid dispersion contains posaconazole, a cyclodextrin derivative and a water-soluble or enteric carrier material, wherein mass ratio of posaconazole to the cyclodextrin derivative is 1:1-4 or mass ratio of posaconazole to the cyclodextrin derivative to the water-soluble or enteric carrier material is 1:1-4:0.001-3. The posaconazole solid dispersion can remarkably raise dissolution rate of the difficultly-soluble antifungal agent posaconazole in the small intestine and also can significantly enhance bioavailability of posaconazole. By the use of a dosage form prepared from the solid dispersion, the preparation technology is simple, and quality of the dosage form is stable.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to a solid dispersion of posaconazole, a pharmaceutical preparation thereof and an application in the technical field of medicine. Background technique [0002] Posaconazole (trade name Noxafil) is a broad-spectrum triazole antifungal drug approved by the US FDA on September 15, 2006, for refractory diseases or other drug resistance caused by Fungal infection (such as aspergillosis, tuberculosis and fusarium disease, etc.), the drug was developed and marketed by Schering-Plough Company in the United States. It is a new chemical molecular entity and the first FDA-approved drug for the prevention of Antibacterial drugs for invasive Aspergillus-induced lesions, which belong to the second-generation antifungal drugs with high lipophilicity, and are the same as other azole antibacterial drugs. Combined with heme cofactors, it inhibits the biosynthesis of fungal erg...

Claims

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Application Information

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IPC IPC(8): A61K9/14A61K31/496A61K47/40A61P31/10
Inventor 袁建栋
Owner BRIGHTGENE BIO MEDICAL TECH (SUZHOU) CO LTD
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