Posaconazole solid dispersion and preparation method thereof

A technology of posaconazole solid and posaconazole, which is applied in the direction of medical preparations containing active ingredients, pharmaceutical formulas, organic active ingredients, etc., can solve the problems of low dissolution rate, poor solubility, and low bioavailability, etc. Achieve the effects of continuous operation, stable preparation quality and simple preparation process

Inactive Publication Date: 2015-04-15
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 poor solubility of posaconazole preparations in the small intestine in the prior art, the dissolution rate is low, and the shortcoming of low bi

Method used

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  • Posaconazole solid dispersion and preparation method thereof
  • Posaconazole solid dispersion and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033] Example 1 Preparation of Posaconazole and Soluplus Solid Dispersions by Hot Melt Extrusion

[0034] Co-rotating twin-screw extruder TE-20 (Coperon Keya, Germany) was used to set the temperature from each section to the head. After 20 minutes of equilibrium, the screw speed was set to 25r / min, and posaconazole and Put 200g of the physical mixture of Soluplus 1:6 (mass ratio) into the hopper. After 1min, the die hole of the material machine head is extruded in strips, and the extrudate is placed on a glass plate, cooled to room temperature and placed for 4 hours. , pulverized, and crossed an 80-mesh sieve to obtain a white powder. X-ray powder diffraction showed that posaconazole was dispersed in Soluplus in an amorphous state (as attached figure 1 shown).

Embodiment 2

[0035] Example 2 Preparation of solid dispersions of posaconazole and Soluplus by melting method

[0036] 33 grams of Soluplus and 67 grams of posaconazole are blended together until a uniform blend of posaconazole and Soluplus is made, then heated and melted, stirred, and after posaconazole is fully dispersed in the carrier, placed Stir vigorously on an ice-salt bath, cool rapidly to solidify, then place in a -20°C refrigerator for 2 hours, dry in a desiccator for 2 days, crush, and pass through an 80-mesh sieve for later use.

Embodiment 3

[0037] Example 3 Preparation of solid dispersions of posaconazole and Soluplus by freeze-drying

[0038] Dissolve 10g of posaconazole in a mixed solution of 50ml of methanol and concentrated hydrochloric acid (methanol:concentrated hydrochloric acid=10:1, V / V), stir and mix evenly; dissolve 100g of Soluplus in purified water to prepare a 30% aqueous solution; The above two solutions were mixed and stirred for 2 h to obtain a clear solution; the above clear solution was filtered through a 0.45 μm polytetrafluoroethylene filter (Rezist 30, Whatman, Dassel, Germany); cooled with liquid nitrogen, and finally lyophilized for 56 h to obtain a white solid powder.

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Abstract

The invention belongs to the technical field of pharmacy, and specifically relates to a posaconazole solid dispersion and a preparation method thereof. The invention discloses a posaconazole solid dispersion which is composed of posaconazole and a water-soluble polymer according to a weight ratio of 1:0.5-10, and a pharmaceutical composition comprising the same. The provided posaconazole solid dispersion can prominently improve the dissolution rate of antifungal agent posaconazole, which is hard to dissolve, in small intestines, and is capable of prominently increasing the biological utilization rate of posaconazole. The pharmaceutical dosage forms prepared from the pharmaceutical composition comprising the provided solid dispersion has the advantages of simple preparation technology and stable quality.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to a solid dispersion of posaconazole, a preparation method thereof, 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 infections (such as aspergillosis, tuberculosis and fusarium disease, etc.), the drug was developed and marketed by Schering-Plough in the United States. It is a new chemical molecular entity and is the first drug approved by the FDA 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 inhib...

Claims

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Application Information

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