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Preparation method of oily fluconazole injection for pets

A technology of fluconazole oil and injections, which is applied in the field of preparation of drug injections, and can solve problems such as functional destruction, lack of ergosterol synthesis, and changes in the activity of membrane-permeable enzymes

Inactive Publication Date: 2015-05-20
QINGDAO UNIV OF SCI & TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Fluconazole functions by inhibiting cytochrome P450-dependent 14α-demethylase (P45014DM). The antifungal mechanism of fluconazole and other azoles has been elucidated at the molecular level: the nitrogen on the azole ring The lone pair of electrons on the atom forms a coordination bond with the Fe atom of the P45014DM heme prosthetic group, which makes the hemoglobin lose the opportunity to combine with the oxygen atom, and the function of P45014DM is destroyed, thereby inhibiting the demethylation reaction of the 14α position of lanosterol, resulting in fungal The accumulation of lanosterol in the body and the lack of ergosterol synthesis lead to changes in membrane permeability and many enzyme activities on the membrane, thereby inhibiting the growth of fungi

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0015] First, dry heat sterilize 8L of castor oil for injection at 150°C for 2 hours, cool to 50°C, dissolve 1kg of fluconazole and 150g of butylhydroxyanisole in a mixed solution of 2L of triacetin and 3L of absolute ethanol , then add 2L of 1,2-propanediol to mix, slowly add the above-mentioned sterilized castor oil for injection, stir evenly, divide the prepared solution into sterilized vials after filtering through a microporous membrane, and obtain Stabilized oily injection for pets containing fluconazole 6.7%.

Embodiment 2

[0017] First, dry heat sterilize 8L of castor oil for injection at 150°C for 2 hours, cool to 50°C, dissolve 0.75kg of fluconazole and 150g of butylated hydroxyanisole in a mixed solution of 2L triacetin and 3L absolute ethanol Add 1,2-propanediol 2L and mix, slowly add the above-mentioned sterilized castor oil for injection, stir evenly, filter the prepared solution through a microporous membrane, and then pack it into sterilized vials, namely A stable oily injection containing fluconazole 5% was obtained for pets.

Embodiment 3

[0019] First, 75L of castor oil for injection was sterilized by dry heat at 150°C for 2 hours, cooled to 50°C, and 15kg of fluconazole and 1.5kg of butylated hydroxyanisole were dissolved in a mixed solution of 30L of triacetin and 20L of absolute ethanol Add 25L of 1,2-propanediol to mix, slowly add the above-mentioned sterilized castor oil for injection, stir evenly, filter the prepared solution through a microporous membrane, and then pack it into sterilized vials, i.e. Obtained a stable oily injection containing fluconazole 10% for pets.

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PUM

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Abstract

The invention relates to a preparation method of oily fluconazole injection for pets. The preparation method comprises the following steps: at first, carrying out dry heat sterilization on injection castor oil at 150 DEG C for 2 hours, cooling to 50 DEG C, dissolving fluconazole and butyl hydroxy anisd in a mixed solution of glyceryl triacetate and absolute ethyl alcohol, adding 1,2-propylene glycol for mixing, slowly adding the sterilized injection castor oil, stirring uniformly, filtering the prepared solution via a microfiltration membrane, and packaging the product in a sterilized penicillin bottle to obtain stable oily fluconazole injection for pets. The preparation process is simple and the cost is low, so that the commercialization prospect is good.

Description

technical field [0001] The invention relates to a preparation method of a drug injection, in particular to a preparation method of a fluconazole oily injection for pets. Background technique [0002] Fluconazole is a triazole antifungal drug. Its antifungal mechanism is the same as that of other nitrogen azole antifungal drugs. It works by competitively inhibiting fungal ergosterol biosynthesis. Ergosterol is a unique lipid in fungal cell membranes and is an important structural component. It plays an important role in ensuring the integrity of membrane structure, activity of membrane-bound enzymes, membrane fluidity, cell viability, and material transport. . Fluconazole functions by inhibiting cytochrome P450-dependent 14α-demethylase (P45014DM). The antifungal mechanism of fluconazole and other azoles has been elucidated at the molecular level: the nitrogen on the azole ring The lone pair of electrons on the atom forms a coordination bond with the Fe atom of the P45014D...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/10A61K31/4196A61P31/10
Inventor 吴汝林王凡业
Owner QINGDAO UNIV OF SCI & TECH
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