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Posaconazole oral solution and preparation method thereof

A technology of posaconazole oral liquid and posaconazole, applied in the field of posaconazole oral liquid preparations, can solve the problems of poorly water-soluble drugs and low oral bioavailability

Inactive Publication Date: 2016-08-24
CENTAURUS BIOPHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Posaconazole is a weakly basic, poorly water-soluble drug with low oral bioavailability

Method used

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  • Posaconazole oral solution and preparation method thereof
  • Posaconazole oral solution and preparation method thereof
  • Posaconazole oral solution and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] components

[0029] The preparation method is as follows: add the initial volume of purified water to the container, add disodium edetate (EDTA), mix until dissolved, add hydroxypropyl-β-cyclodextrin (Hp-β-CD), mix until dissolved. Add 0.1N hydrochloric acid to the vessel to acidify the solution to a pH of approximately 1.2, then add pre-wetted posaconazole, mix until posaconazole is completely dissolved and form a clear solution, continue adding sodium benzoate, sodium saccharin and margarine Essence, add 1N sodium hydroxide to adjust the pH value of the solution to about 4.0, add pure water to a sufficient amount, and filter through a 0.22 μm microporous membrane to obtain the product. The prepared posaconazole oral solution is a colorless and transparent solution.

Embodiment 2

[0031] components

[0032] Prepared according to the method of Example 1, the pH value is 2.0.

Embodiment 3

[0034] components

[0035] The preparation method is as follows: add the initial volume of purified water to the container, add EDTA, mix until dissolved, add sulfobutyl ether-β-cyclodextrin (SBE-β-CD), mix until dissolved. Add 0.1N hydrochloric acid to the vessel to acidify the solution to a pH of approximately 1.2, then add pre-wetted posaconazole, mix until posaconazole is completely dissolved and form a clear solution, continue adding sodium benzoate, sodium saccharin and margarine Essence, add 1N sodium hydroxide to adjust the pH value of the solution to about 2.8, add pure water to a sufficient amount, and filter through a 0.22 μm microporous membrane to obtain the product. The prepared posaconazole oral solution is a yellow transparent solution.

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Abstract

The invention discloses a posaconazole oral solution capable of improving bioavailability, wherein the posaconazole oral solution contains posaconazole or a pharmaceutically acceptable salt thereof, modified beta-cyclodextrin, a preservative, a chelating agent, a sweetener, an aromatic agent and a pH regulator.

Description

technical field [0001] The present invention relates to oral liquid formulations of posaconazole. The oral solution adopts cyclodextrin inclusion technology to improve the solubility and bioavailability of posaconazole. Background technique [0002] Posaconazole is a new generation of antifungal drugs, it is a derivative of itraconazole, can be used for the treatment of oropharyngeal candida infection and aspergillus infection, can also be used for preventive treatment, its structural formula is as follows: [0003] [0004] Posaconazole is a weakly basic, poorly water-soluble drug with low oral bioavailability. Usually, it needs to be micronized before being prepared into a preparation. Posaconazole is currently available in three dosage forms: oral suspension, sustained-release tablets, and intravenous injection. Posaconazole Oral Suspension (trade name: ), developed and produced by Schering / MSD, was approved for import registration by the China State Food and Drug...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/48A61K31/496A61K9/08A61P31/10
Inventor 殷静王再全马秋平张德富刘玲冀冲杨利民韩永信
Owner CENTAURUS BIOPHARMA
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