Antifungal drug posaconazole solid dispersion, preparation method and application

A technology for solid dispersions and antifungal drugs, which can be used in antifungal agents, pharmaceutical formulations, medical preparations with inactive ingredients, etc., and can solve the problems of increased content of related substances, low drug loading, and poor stability. The effect of promoting absorption, improving dissolution rate, and improving bioavailability

Inactive Publication Date: 2017-01-04
SHANDONG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The hot-melt extrusion temperature used in the above process should be higher than 110°C, and the content of related substances will easily increase during the preparation process; while the inclusion compound of β-cyclodextrin has low drug loading and poor stability, which is not conducive to use.

Method used

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  • Antifungal drug posaconazole solid dispersion, preparation method and application
  • Antifungal drug posaconazole solid dispersion, preparation method and application
  • Antifungal drug posaconazole solid dispersion, preparation method and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031]

[0032] making process:

[0033] Weigh the prescribed amount of posaconazole and HPMC-AS MF into a flask, add a certain amount of 95% ethanol, dissolve in a water bath at 65°C, and then remove it by rotary evaporation at a vacuum of -0.03~-0.07M Pa at 75-80°C. part of ethanol, and then adjust the vacuum degree to be above -0.1M Pa to remove ethanol, take out the content and dry it in an oven at 40°C overnight to prepare posaconazole solid dispersion (its X-ray diffraction pattern is shown in the attached figure 1 ). Pulverize the posaconazole solid dispersion, pass through a 80-100 mesh sieve, add the prescribed amount of microcrystalline cellulose PH102, hydroxypropyl cellulose-EXF, and croscarmellose sodium, pass through a 80 mesh sieve and mix, and then Add the prescribed amount of MS, mix for 3 to 5 minutes, and use a rotary tablet press to directly compress the tablet.

Embodiment 2

[0035]

[0036] All the other processes are the same as in Example 1.

Embodiment 3

[0038]

[0039]

[0040] All the other processes are the same as in Example 1.

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Abstract

The invention discloses an antifungal drug posaconazole solid dispersion, a preparation method and an application. The solid dispersion comprises posaconazole and an enteric-coating material, wherein the enteric-coating material is hydroxypropyl methylcellulose acetate succinate. A formulated amount of the posaconazole and the hydroxypropyl methylcellulose acetate succinate is weighed, mixed and added into mixed solution with one or two of acetone or ethyl alcohol solution, and spin flash drying is performed after dissolution to obtain the posaconazole solid dispersion. The dissolution rate of the posaconazole can be increased by the hydroxypropyl methylcellulose acetate succinate, absorption of the posaconazole is promoted, and bioavailability of the posaconazole is improved.

Description

technical field [0001] The invention belongs to the field of medicines, and in particular relates to a solid dispersion of an antifungal medicine posaconazole, a preparation method and an application thereof. Background technique [0002] Posaconazole, trade name: Noxafil, chemical name: 4-[4-[4-[4-[[(3R,5R)-5-(2,4-difluorophenyl)tetrahydro- 5-(1H-1,2,4-triazole-1-methyl)-3-furan]methoxy]phenyl]-1-piperazinyl]phenyl]-2-[(1S,2S) -1-Ethyl-2-hydroxypropyl]-2,4-dihydro-3H-1,2,4-triazol-3-one, the structural formula is as follows: [0003] [0004] This product was developed by Schering-Plough, and was approved for marketing by the European Union and the US FDA from 2005 to 2006. It is mainly used to prevent invasive Aspergillus fungal infection, and is suitable for patients with severely compromised immune system, including patients with graft-versus-host disease (GVHD) or hematological malignancy in recipients of hematopoietic stem cell transplantation (HSCT) Neutropenia ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/14A61K9/20A61K9/48A61K31/496A61K47/38A61P31/10
CPCA61K9/146A61K9/2054A61K9/4808A61K9/4866A61K31/496
Inventor 赵忠熙杨民董中华张芳刘娜王凯铭
Owner SHANDONG UNIV
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