Voriconazole phosphate ester for injection and preparation method thereof

Abstract

The invention provides voriconazole phosphate ester for injection and a medicinal salt thereof and a preparation method for the voriconazole phosphate ester for injection and the medicinal salt thereof. The preparation method comprises the following steps: adding 5 to 98 percent water for injection in a liquid preparation container; adding 90 to 110 percent of the accurate formula dosage of voriconazole phosphate ester and the medicinal salt thereof in the container; stirring the mixture; slowly dropwise adding a pH value regulator; regulating pH to between 6.0 and 11; supplementing water to the full dosage and then adding 0.01 to 1.0 percent (weight in volume) medicinal carbon into the product; stirring the mixture for 15 to 60 minutes; using a sand filter stick to carry out rough filtration and decarburization on the obtained product, and using a 0.22mum millipore filter to carry out fine filtration on the product until the clarity is qualified; after determining that the content of the midbody is qualified, determining the filling quantity and subpackaging the finished product in the vial; adding the semi-plug; carrying out freezing and drying on the sample; controlling the moisture content between 1 and 8 percent; pressing the plug; and carrying out capping.

Description

Technical field:

[0001] The invention belongs to the technical field of medicine, and relates to voriconazole phosphate for injection or a medicinal salt thereof and a preparation method thereof. technical background:

[0002] Voriconazole is a broad-spectrum triazole antifungal drug indicated for the following: treatment of invasive aspergillosis. Treatment of severe invasive infections caused by fluconazole-resistant Candida species (including Candida krusei). Treatment of serious infections caused by Actinomycetes and Fusarium species. This product should be used primarily for the treatment of progressive, potentially life-threatening infections in immunocompromised patients. The prodrug of voriconazole phosphate voriconazole can be rapidly hydrolyzed into voriconazole in the body to take effect. Since voriconazole has very little water solubility, the method of encapsulating voriconazole with hydroxypropyl β-cyclodextrin is used to solubilize voriconazole for injectio...

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