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Pharmaceutical composition containing posaconazole

A technology of posaconazole and composition, applied in the field of saconazole pharmaceutical composition, to achieve the effect of low MIC value

Inactive Publication Date: 2020-08-11
山西振东泰盛制药有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] However, the minimum inhibitory concentrations (minimal inhibitory concentration, MIC) of posaconazole on the market are greater than 16 μg / ml for Mucor circinosa, Scedosporium sterica, and Fusarium solani

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] 1) Preparation of posaconazole crystal I: Add 2 g of posaconazole into a mixed solvent of 18 mL of ethyl acetate and 5 mL of ethanol, heat up to 80° C. to dissolve and clarify, then cool down to 20° C. within 1.5 hours, and crystallize , 1.4g was obtained after insulated at 20°C and filtered, with a yield of 70%, and the crystal form was Form I as detected by XRD.

[0032] 2) Microcrystallization treatment of posaconazole crystals I: The posaconazole crystals I prepared above were ground for 20 min to obtain microcrystallized posaconazole crystals I with an average particle size of 7.3 μm.

[0033] 3) Preparation of posaconazole crystal Y: take 2 g of posaconazole crystal I and heat treatment at a heating temperature of 175° C. for 10 min, so that all posaconazole crystal I is converted into posaconazole crystal Y , the crystal form was detected as Form Y by XRD. The posaconazole crystal Y has an average particle size of 9.6 μm and a median particle size of 7.9 μm.

...

Embodiment 2

[0036] 1) Preparation of posaconazole crystal I: Add 3 g of posaconazole into a mixed solvent of 27 mL of ethyl acetate and 12 mL of methanol, heat up to 75° C. to dissolve and clarify, then cool down to 25° C. within 2 hours, and crystallize , 2.4g was obtained after insulated at 25°C and filtered, with a yield of 80%, and the crystal form was detected as crystal form I by XRD.

[0037] 2) Microcrystallization treatment of posaconazole crystals I: The posaconazole crystals I prepared above were ground for 31 min to obtain microcrystallized posaconazole crystals I with an average particle size of 6.6 μm.

[0038] 3) Preparation of posaconazole crystal Y: take 8g of posaconazole crystal II and heat treatment at 180°C for 15 minutes, so that posaconazole crystal II is completely converted into posaconazole crystal Y , the crystal form was detected as Form Y by XRD. The posaconazole crystal Y has an average particle size of 8.7 μm and a median particle size of 7.6 μm.

[0039] ...

Embodiment 3

[0041] 1) Preparation of posaconazole crystal I: Add 8 g of posaconazole into a mixed solvent of 72 mL of methyl acetate and 30 mL of methanol, heat up to 80° C. to dissolve and clarify, then cool down to 20° C. within 1.5 hours, and crystallize , 7.3g was obtained after being incubated at 20°C and filtered, with a yield of 91%, and the crystal form was Form I as detected by XRD.

[0042] 2) Microcrystallization treatment of posaconazole crystals I: Grinding the posaconazole crystals I prepared above for 40 min to obtain microcrystallized posaconazole crystals I with an average particle size of 6.0 μm.

[0043] 3) Preparation of posaconazole crystal Y: take 20 g of posaconazole crystal I and heat treatment at a heating temperature of 175° C. for 19 minutes, so that posaconazole crystal I is completely converted into posaconazole crystal Y , the crystal form was detected as crystal form Y by XRD, the average particle size of the posaconazole crystal Y was 9 μm, and the median p...

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Abstract

The invention discloses a pharmaceutical composition containing posaconazole. The pharmaceutical composition comprises posaconazole crystal I and posaconazole crystal Y, wherein the weight ratio of the posaconazole crystal I to the posaconazole crystal Y is 1: 1-1: 1.5; the posaconazole crystal I is micronized; the posaconazole crystal Y is not micronized; the average particle size of the micronized posaconazole crystal I is 6-8 microns, and the median particle size is 2-4 microns; the average particle size of the non-micronized posaconazole crystal Y is 8.5-1.2 microns, and the median particle size is 4.5-8 microns. The in-vitro antibacterial test results of the pharmaceutical composition containing posaconazole on mucor circinelloides, polyspora tococcus and fusarium solani are higher than the antibacterial effect of the posaconazole independently used in the market, and the MIC value is lower.

Description

technical field [0001] The invention relates to the field of medicine, in particular to a pharmaceutical composition containing posaconazole as an active pharmaceutical ingredient. Background technique [0002] Posaconazole (posaconazole) is a derivative of itraconazole, which belongs to broad-spectrum triazole antifungal drugs, developed and produced by Merck; its oral suspension was approved by the European Agency for Medicines Evaluation ( EMEA) and the US Food and Drug Administration (FDA) approved for the treatment of fungal infections, and in 2013 obtained the import registration approval of China's State Food and Drug Administration, mainly for the prevention of invasive Aspergillus and Candida infections including In patients with graft-versus-host disease (GVHD) after hematopoietic stem cell transplantation (HSCT) or in patients with hematological malignancies with prolonged neutropenia caused by chemotherapy, the treatment of oropharyngeal candidiasis includes itra...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/496A61P31/10C07D405/14
CPCA61K31/496A61P31/10C07B2200/13C07D405/14
Inventor 高治华叶飞王旭峰赵永军沈达
Owner 山西振东泰盛制药有限公司
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