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Preparation method of voriconazole for injection

A technology for voriconazole and injection is applied in the field of preparation of voriconazole for injection, and can solve the problems of uneven stability of voriconazole-hydroxypropyl beta cyclodextrin inclusion complex, low effective components of voriconazole, instability of voriconazole in the presence of alkali, etc.

Pending Publication Date: 2022-05-06
ZHUHAI EBANG PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the voriconazole-hydroxypropylbeta-cyclodextrin inclusion complex formed by magnetic stirring is not uniform and stable
Since voriconazole is unstable when it encounters alkali, if the inclusion is uneven and stable, the uncoated voriconazole will decompose when it encounters alkali during the process of adjusting the pH value of the liquid, resulting in low active ingredients and high impurity content in voriconazole for injection

Method used

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  • Preparation method of voriconazole for injection
  • Preparation method of voriconazole for injection
  • Preparation method of voriconazole for injection

Examples

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preparation example Construction

[0048] The invention provides a preparation method of voriconazole for injection, comprising the following steps:

[0049] A preparation method of voriconazole for injection, comprising the following steps:

[0050] (1) Under the stirring condition of the stirring blade, hydroxypropyl beta-cyclodextrin is dissolved in water for injection to obtain an aqueous solution of hydroxypropyl-beta-cyclodextrin; the mass concentration of the aqueous solution of hydroxypropyl-beta-cyclodextrin 10.47-27.18%;

[0051] (2) under the stirring condition of stirring paddle, hydrochloric acid solution is mixed with voriconazole, obtains the hydrochloric acid solution of voriconazole;

[0052] (3) under the condition of stirring with a stirring blade, the hydrochloric acid solution of voriconazole is added to the aqueous solution of hydroxypropyl beta-cyclodextrin to obtain the voriconazole-hydroxypropyl-beta-cyclodextrin solution;

[0053](4) Under the condition of stirring with a stirring pa...

Embodiment 1

[0091] The prescribed amount of voriconazole for injection is as follows:

[0092]

[0093] The preparation method of voriconazole for injection comprises the following steps:

[0094] (1) Slowly add 800g of hydroxypropyl beta-cyclodextrin into 3300mL of water for injection with 80% of the prescription quantity, control the temperature between 50°C and 60°C, stir with a stirring paddle until the material is completely dissolved, and the stirring frequency is 30Hz .

[0095] (2) Add 200mL of 2mol / L hydrochloric acid solution to the prescribed amount of voriconazole, and stir while adding to completely dissolve the voriconazole, and the solution is clear.

[0096](3) Slowly add the completely dissolved voriconazole-hydrochloric acid solution into the dissolved hydroxypropyl beta-cyclodextrin aqueous solution, between 50°C and 60°C, stir with a stirring paddle at a stirring frequency of 30Hz, and complete the addition Stirring was then continued for 30 minutes.

[0097] (4)...

Embodiment 2

[0101] The amount of raw materials and the preparation method are the same as those in Example 1, except that the batches are different. The obtained voriconazole product for injection is recorded as batch 20190102.

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Abstract

The invention provides a preparation method of voriconazole for injection, and belongs to the technical field of pharmacy. According to the invention, the stirring paddle is adopted for stirring, and the stirring frequency of the stirring paddle is controlled, so that the flowability of the mixed liquid is accelerated, the liquid medicine reaches a uniform state instantly, and stable and uniform coating of the voriconazole by the hydroxypropyl-beta-cyclodextrin is realized; meanwhile, due to the adoption of a stirring mode of a stirring paddle, in the process of adjusting the pH value of the sodium hydroxide solution, the sodium hydroxide solution is instantly and uniformly dispersed after being added into the voriconazole-hydroxypropyl-beta-cyclodextrin-mannitol solution, so that the decomposition of voriconazole caused by local overhigh pH value is avoided, and the stability of effective components in the medicine is improved.

Description

technical field [0001] The invention relates to the technical field of pharmacy, in particular to a preparation method of voriconazole for injection. Background technique [0002] Voriconazole is a new type of third-generation triazole broad-spectrum antifungal drug. Compared with fluconazole, it has a wider antibacterial spectrum and stronger antibacterial efficacy. Its preparations are widely used clinically to treat invasive Aspergillus albicans, severe invasive infections caused by fluconazole-resistant Candida albicans, and severe infections caused by actinomycetes and Fusarium species. [0003] The solubility of voriconazole in water is 0.2 mg / mL (pH=3), and it is unstable, and its hydrolyzed retro aldol product will recombine into an inactive enantiomer. In view of the low solubility and poor stability of voriconazole in water, how to effectively increase the solubility of voriconazole in water and maintain the stability of the drug when it is prepared into a lyophil...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/19A61K31/506A61K47/26A61K47/69A61P31/10
CPCA61K47/6951A61K31/506A61K9/19A61K9/0019A61K47/26A61P31/10
Inventor 吴浩山钟桂雄吴集程陈小梅陈柳颖卢金娜
Owner ZHUHAI EBANG PHARMA
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