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Itraconazole freeze-dried powder injection and preparing method

A technology for itraconazole and injection, which is applied in the field of itraconazole freeze-dried powder injection and preparation, can solve the problem that the prescription quantity of hydroxypropyl-β-cyclodextrin cannot be inferred, and achieves plump appearance and convenient Clinical use, fast redissolving effect

Inactive Publication Date: 2005-05-18
BEIJING BOERDA BIO TECH DEV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] According to the introduction of itraconazole injection instructions in the US PDR, the injection uses 40% hydroxypropyl-β-cyclodextrin as the solubilizer of itraconazole, but the proportion of hydroxypropyl-β-cyclodextrin The freeze-dried injection of itraconazole prepared by -cyclodextrin as a solubilizer precipitated when mixed with sodium chloride injection. The inventor found a surprising phenomenon through further extensive experiments, increasing the hydroxypropyl- When the amount of β-cyclodextrin reaches 40% to 60%, the freeze-dried product is clear and free of precipitation when diluted with sodium chloride injection. Such a phenomenon has no similar teaching and explanation in pharmacy textbooks and related documents. Technicians cannot infer the prescription amount of hydroxypropyl-β-cyclodextrin for itraconazole lyophilized needle for injection according to the injection formula in the itraconazole injection instructions in the US PDR

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0016] Prescription: Itraconazole 250g

[0017] Hydroxypropyl-β-cyclodextrin 10000g

[0018] Propylene glycol 625ml

[0019] Hydrochloric acid 95ml

[0020] Mannitol 1000g

[0021] Add water for injection to 25000ml

[0022] A total of 1000 pieces were made

[0023] Preparation method: Stir itraconazole with hydrochloric acid to form a paste, add propylene glycol, and ultrasonically dissolve to form a clear solution. Add another amount of hydroxypropyl-β-cyclodextrin into the appropriate amount of water for injection and stir to dissolve, pour the itraconazole propylene glycol solution into the hydroxypropyl-β-cyclodextrin solution, stir until clear, add mannitol, and stir Dissolve, adjust the pH to 4.5 with sodium hydroxide to make up the amount of water, ultrafilter, subpackage, and freeze-dry. Vacuum freeze-drying conditions:

[0024] 1) Pre-freezing: Put the subpackaged medicines on the inner shelf of the f...

Embodiment 2

[0028] Prescription: Itraconazole 250g

[0029] Hydroxypropyl-β-cyclodextrin 12500g

[0030] Propylene glycol 625ml

[0031] Hydrochloric acid 95ml

[0032] Add water for injection to 25000ml

[0033] A total of 1000 pieces were made

[0034] Preparation method: Stir itraconazole with hydrochloric acid to form a paste, add propylene glycol, stir and dissolve to form a clear solution. Add another amount of hydroxypropyl-β-cyclodextrin to an appropriate amount of water for injection and stir to dissolve it. Pour the itraconazole propylene glycol solution into the hydroxypropyl-β-cyclodextrin solution, stir until clear, and adjust with sodium hydroxide. pH to 4.5 to make up the amount of water ultrafiltration, sub-packaging, freeze-drying. Vacuum freeze-drying conditions:

[0035] 1) Pre-freezing: Put the subpackaged medicines on the inner shelf of the freeze-drying box for pre-freezing. The temperature of the product drops ...

Embodiment 3

[0039] Prescription: Itraconazole 250g

[0040] Hydroxypropyl-β-cyclodextrin 15000g

[0041] Propylene glycol 625ml

[0042] Hydrochloric acid 95ml

[0043] Add water for injection to 25000ml

[0044]A total of 1000 pieces were made

[0045] Preparation method: Stir itraconazole with hydrochloric acid to form a paste, add propylene glycol, stir and dissolve to form a clear solution. Add another amount of hydroxypropyl-β-cyclodextrin to an appropriate amount of water for injection and stir to dissolve it. Pour the itraconazole propylene glycol solution into the hydroxypropyl-β-cyclodextrin solution, stir until clear, and adjust with sodium hydroxide. pH to 4.5 to make up the amount of water ultrafiltration, sub-packaging, freeze-drying. Vacuum freeze-drying conditions:

[0046] 1) Pre-freezing: Put the subpackaged medicines on the inner shelf of the freeze-drying box for pre-freezing. The temperature of the product drops to -45°C, a...

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PUM

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Abstract

The freeze-dried Itraconazole powder for injection is prepared through preparing solution with Itraconazole, hydroxypropyl-beta-cyclodextrin, propylene glycol, hydrochloric acid and sodium hydroxide; adding proper amount of diluent and freeze drying. Compared with Itraconazole injection, the present invention has the advantages of raised physical stability, no high temperature decomposing degradation of Itraconazole, loose product and fast recovering of the original solution characteristic after adding water, low water content and drying in vacuum resulting in less oxidation and high stability for long term storing, and less pollution and particle matter introduced during production.

Description

technical field [0001] The invention relates to a pharmaceutical preparation, specifically itraconazole freeze-dried powder injection and a preparation method. Background technique [0002] There are three types of human fungal infections: superficial, subcutaneous, and systemic fungal infections. The first two types have been well controlled, but systemic fungal infections are still difficult. Systemic fungal infections are characterized by difficult diagnosis, rapid disease progression, high mortality, and few effective drugs. Therefore, antifungal drugs with high efficiency, low toxicity, and rapid action are urgently needed in clinic. Abbott of the United States launched itraconazole injection, which solved the long-awaited formulation problem, and can be administered by intravenous infusion. Security and flexibility of use. However, the stability of the injection is relatively poor, and the main drug is easily separated out. It is not heat-resistant, easy to freeze, a...

Claims

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Application Information

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IPC IPC(8): A61K9/16A61K31/496A61P31/10
Inventor 张金成肖云彩
Owner BEIJING BOERDA BIO TECH DEV
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