Freeze-dried voriconazole micelle preparation and preparation method thereof

A technology of voriconazole and freeze-dried gel, which is applied in the field of voriconazole freeze-dried micellar preparations and its preparation, can solve the problems of no clinical application value, large freeze-dried volume, long production cycle, etc., and achieve avoidance of toxic effects and biocompatibility Good performance and fast reconstitution

Inactive Publication Date: 2012-02-01
JINAN KANGHE MEDICAL TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

This solution uses a large amount of auxiliary materials such as oily ingredients, emulsifiers, and freeze-drying support agents. Based on a single dose of 200 mg, the amount of auxiliary materials is about 12-40 g. Not only the freeze-dried volume is too large, the production cycle is long, and a large number of auxiliary materials are used There is a relatively large safety risk to the human body and does not have clinical application value

Method used

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  • Freeze-dried voriconazole micelle preparation and preparation method thereof
  • Freeze-dried voriconazole micelle preparation and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] The preparation of embodiment 1 voriconazole lyophilized micellar preparation

[0035] Weigh voriconazole 200mg, sodium glycocholate 300mg, sodium taurodeoxycholate 150mg, hydrogenated soybean lecithin 150mg, disalmitate lecithin 150mg, put them in a round bottom flask, add 15ml of ethanol to dissolve, 40~50℃ water bath, Rotary evaporation under reduced pressure, evaporate ethanol to form voriconazole mixed micelle film, then add 1600mg lactose and appropriate amount of water for injection to disperse, get voriconazole mixed micelle solution, filter with 0.22 micron microporous membrane, dilute to 10ml, fill in In a vial, press half stopper, freeze-dry, press stopper, press aluminum cap to make voriconazole freeze-dried micelles, each containing voriconazole 200mg. The prepared sample was completely redissolved within 2 minutes, and became a colorless clear liquid with an average particle size of 40nm.

Embodiment 2

[0036] The preparation of embodiment 2 voriconazole lyophilized micellar preparation

[0037]Weigh voriconazole 200mg, sodium glycocholate 500mg, sodium taurodeoxycholate 250mg, hydrogenated soybean lecithin 250mg, disalmitate lecithin 250mg, put them in a round bottom flask, dissolve them in 30ml ethanol, bathe in water at 40-50℃, reduce Press rotary evaporation, evaporate ethanol to form voriconazole mixed micelle film, then add 1050mg dextran and appropriate amount of water for injection to disperse to obtain voriconazole mixed micelle solution, filter with 0.22 micron microporous membrane, dilute to 10ml, fill in cillin In the bottle, press half stopper, freeze-dry, press stopper, press aluminum cap to make voriconazole freeze-dried micelles, each containing voriconazole 200mg. The prepared sample was completely redissolved within 1 minute, and was a colorless clear liquid with an average particle size of 25nm.

Embodiment 3

[0038] The preparation of embodiment 3 voriconazole lyophilized micellar preparation

[0039] Weigh voriconazole 200mg, sodium glycocholate 600mg, sodium taurodeoxycholate 300mg, hydrogenated soybean lecithin 200mg, disalmitate lecithin 200mg, put them in a round bottom flask, add 40ml of ethanol to dissolve, 40~50℃ water bath, Rotary evaporation under reduced pressure, evaporate ethanol, form voriconazole mixed micelle film, add 1000mg mannitol and appropriate amount of water for injection to disperse, get voriconazole mixed micelle solution, filter with 0.22 micron microporous membrane filter, dilute to 10ml, fill in In a vial, press half stopper, freeze-dry, press stopper, press aluminum cap to make voriconazole freeze-dried micelles, each containing voriconazole 200mg. The prepared sample was completely redissolved within 1 minute, and became a colorless clear liquid with an average particle size of 20nm.

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Abstract

The invention discloses a freeze-dried voriconazole micelle preparation and a preparation method thereof. The freeze-dried voriconazole micelle preparation consists of the following components in part by weight: 1 part of voriconazole, 2 to 10 parts of cholate, 1.5 to 5 parts of phospholipid, and 1 to 10 parts of freeze-drying supporting agent. According to the preparation, the dissolubility of the voriconazole is increased, and the dissolution degree of the voriconazole in water is improved; and the preparation can be diluted into intravenous injection by using injection water for clinical use. The particle diameter of the prepared voriconazole micelles is between 10 and 100 nanometers, the particle diameter of most micelles is about 20 nanometers, the particle size is uniform, the frozen and dried voriconazole micelles are high in re-dissolution speed, a transparent and colorless solution is formed after the voriconazole micelles are re-dissolved, and the particle diameter has no obvious change, so the safety of clinical application is enhanced. According to the prepared freeze-dried voriconazole micelle preparation, because the voriconazole is wrapped inside by the mixed micelles, influence of light, heat and moisture is avoided, and the stability of the voriconazole in a long-term storage process is improved.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and relates to a voriconazole freeze-dried micellar preparation and a preparation method thereof. Background technique [0002] Voriconazole is a second-generation triazole antifungal drug synthesized by Pfizer, which was launched in the United States in May 2002. The product has antibacterial effect on Candida and bactericidal effect on Aspergillus. In vitro test results show that voriconazole also has bactericidal effect on other pathogenic fungi such as Actinomyces and Fusarium. As a new type of antifungal drug, voriconazole has the characteristics of broad antibacterial spectrum and strong antibacterial efficacy, especially for invasive Aspergillus infiltrating infection. Voriconazole is currently available in the following dosage forms: tablets, dry suspensions, and freeze-dried powder for oral and intravenous administration. In the ICU ward, especially in oncology, hem...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/00A61K31/506A61K47/28A61K47/32A61K47/36A61P31/10
Inventor 刘真豪
Owner JINAN KANGHE MEDICAL TECH
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