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Voriconazole freeze-drying powder injection and its preparation process

A voriconazole and freeze-drying technology, applied in the field of pharmaceutical preparations, can solve the problems of low solubility, difficult to achieve therapeutic effect, toxicity, etc., and achieve the effect of easy clinical use, plump appearance and loose texture

Inactive Publication Date: 2006-06-21
大道隆达(北京)医药科技发展有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

It is undoubtedly a good solution to make freeze-dried powder injection, but its low solubility is difficult to achieve the concentration of therapeutic effect without solubilization
Chinese patent CN1261287 discloses a method in which voriconazole is made into freeze-dried powder injection through cyclodextrin inclusion solubilization, but the cyclodextrin used is dibutyl ether sulfur-β-cyclodextrin, which has harmful effects on the body. certain toxicity

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0012] Prescription: Voriconazole 10g

[0013] Hydroxypropyl-β-cyclodextrin 200g

[0014] Appropriate amount of water for injection

[0015] Make a total of 1000ml

[0016] Preparation method:

[0017] 1. Treat rubber stoppers, aluminum caps, and vials for later use;

[0018] 2. Weigh hydroxypropyl-β-cyclodextrin and dissolve it in about 700ml water for injection, set aside;

[0019] 3. Weigh voriconazole and add it to the above solution, stir to dissolve. (about 5 hours)

[0020] 4. Adsorb with 0.1% activated carbon at 80° C. for 15 minutes, decarbonize and filter, filter with a 0.22 μm microporous membrane, and check the obtained clear filtrate.

[0021] 5. Dilute the qualified medicinal solution to the full amount, and fill each 20ml into a 30ml vial;

[0022] 6. Vacuum drying:

[0023] 1) Pre-freezing: Put the subpackaged medicines on the inner shelf of the freeze-drying box and pre-freeze at -40°C for 4 hours;

[0024] 2) Sublimation drying: Low...

Embodiment 2

[0029] Prescription: Voriconazole 10g

[0030] Hydroxypropyl-β-cyclodextrin 50g

[0031] Mannitol 100g

[0032] Appropriate amount of water for injection

[0033] Make a total of 1000ml

[0034] Preparation method:

[0035] 1. Treat rubber stoppers, aluminum caps, and vials for later use;

[0036] 2. Weigh hydroxypropyl-β-cyclodextrin and dissolve it in about 700ml of water for injection, and set aside;

[0037] 3. Weigh voriconazole and add it to the above solution, stir to dissolve (about 5 hours), add mannitol to dissolve.

[0038] 4. Adsorb with 0.1% activated carbon at 80° C. for 15 minutes, decarbonize and filter, filter with a 0.22 μm microporous membrane, and check the obtained clear filtrate.

[0039] 5. Dilute the qualified medicinal solution to the full amount, and fill each 20ml into a 30ml vial;

[0040] 6. Vacuum drying:

[0041] 1) Pre-freezing: Put the subpackaged medicines on the inner shelf of the freeze-drying box and pre-free...

Embodiment 3

[0047] Prescription: Voriconazole 10g

[0048] Hydroxypropyl-β-cyclodextrin 400g

[0049] Appropriate amount of water for injection

[0050] Make a total of 1000ml

[0051] Preparation method:

[0052] 1. Treat rubber stoppers, aluminum caps, and vials for later use;

[0053] 2. Weigh hydroxypropyl-β-cyclodextrin and dissolve it in about 700ml of water for injection, and set aside;

[0054] 3. Weigh voriconazole and add it to the above solution, stir to dissolve. (about 5 hours)

[0055] 4. Adsorb with 0.1% activated carbon at 80° C. for 15 minutes, decarbonize and filter, filter with a 0.22 μm microporous membrane, and check the obtained clear filtrate.

[0056] 5. Dilute the qualified medicinal solution to the full amount, and fill each 20ml into a 30ml vial;

[0057] 6. Vacuum drying:

[0058] 1) Pre-freezing: Put the subpackaged medicines on the inner shelf of the freeze-drying box and pre-freeze at -40°C for 4 hours;

[0059] 2) Sublimation dryi...

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Abstract

The present invention relates to one kind of freeze dried voriconazole composition including voriconazole in effectively treating amount and hydroxypropyl-beta-cyclodextrin. Each of the preparation unit contains voriconazole in 50-400 mg, pregreably 200 mg and hydroxypropyl-beta-cyclodextrin of 5-40 time, preferably 15-25 times, weight of voriconazole.

Description

technical field [0001] The invention relates to a pharmaceutical preparation, in particular to voriconazole freeze-dried powder injection and a preparation method. Background technique [0002] Voriconazole is a synthetic triazole drug, which is the second generation of synthetic fluconazole derivatives. As a new type of antifungal drug, it has the characteristics of broad antibacterial spectrum and strong antibacterial efficacy. Pfizer company discovered this product in the 1980s, which can be used for the treatment of severe fungal infections with high mortality. Voriconazole has a low solubility in water of about 0.2mg / ml, pH3) and is unstable and easily hydrolyzed. It is undoubtedly a good solution to make freeze-dried powder injection, but it is difficult to reach the concentration of therapeutic effect without solubilization due to its low solubility. Chinese patent CN1261287 discloses a method in which voriconazole is made into freeze-dried powder injection through...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/4196A61P31/04A61P31/10
Inventor 张金成张成飞
Owner 大道隆达(北京)医药科技发展有限公司
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