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Temozolomide freeze-dried preparation

A technology for temozolomide and freeze-dried preparations, which is applied in the field of temozolomide freeze-dried preparations, and can solve the problems of long dissolution and preparation process, difficulty in industrial production, waste of main ingredients, etc.

Active Publication Date: 2013-08-14
重庆世森医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] US6251886 discloses a temozolomide injection administered in the form of a micronized suspension, but it can cause blood vessel blockage, which is not ideal
[0007] Chinese patent CN200510014962.3 discloses a temozolomide freeze-dried powder injection, which dissolves temozolomide by adjusting the pH and heating ultrasonically, but the entire dissolving process takes a long time, the temozolomide solution is unstable, and the use of the injection has hidden dangers in quality and safety
This freeze-dried preparation method shortens the dissolution time of temozolomide and increases the stability of the solution, but the solution formed after dissolution in this preparation method is still easy to precipitate solids. The patent uses a secondary filtration method to solve this problem, but this method There are many shortcomings such as long production time, cumbersome operation, and waste of main ingredients, so it is difficult to realize industrial production

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] Preparation composition:

[0021]

[0022] Preparation:

[0023] Weigh N(2)-L-alanyl-L-glutamine, polysorbate 80, mannitol, sodium citrate, and hydrochloric acid of the above weight, add them to 8000ml of water for injection, stir until the solids are all dissolved and clear, Add the prescribed amount of temozolomide, stir until the solids are completely dissolved and clear, adjust the pH to 5.0 with hydrochloric acid solution or sodium hydroxide solution; add water for injection to make up the volume to 10,000ml, filter through a 0.22μm microporous membrane for sterilization, and dispense into 30ml of penicillin In the bottle, each bottle is filled with 10ml of the solution, placed in a freeze-drying box, and freeze-dried to form a freeze-dried preparation.

Embodiment 2

[0025] Preparation composition:

[0026]

[0027] Preparation:

[0028] Weigh the above weight of glycyl glutamine, polysorbate 80, mannitol, sodium citrate, hydrochloric acid, add to 8000ml water for injection, stir until the solids are completely dissolved and clear, add the prescribed amount of temozolomide, stir until the solids are all Dissolve and clarify, adjust the pH to 5.0 with hydrochloric acid solution or sodium hydroxide solution; add water for injection to make up the volume to 10,000ml, pass through a 0.22μm microporous membrane filter to sterilize, and dispense into 30ml vials, each containing 10ml of solution, Put it in a freeze-drying box and freeze-dry to form a freeze-dried preparation.

Embodiment 3

[0030] Preparation composition:

[0031]

[0032] Preparation:

[0033] Weigh the above-mentioned weight of glycyltyrosine, polysorbate 80, mannitol, sodium citrate, hydrochloric acid, add to 8000ml water for injection, stir until the solids are all dissolved and clear, add the prescribed amount of temozolomide, and stir until the solids are all Dissolve and clarify, adjust the pH to 5.0 with hydrochloric acid solution or sodium hydroxide solution; add water for injection to make up the volume to 10,000ml, pass through a 0.22μm microporous membrane filter to sterilize, and dispense into 30ml vials, each containing 10ml of solution, Put it in a freeze-drying box and freeze-dry to form a freeze-dried preparation.

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Abstract

The invention relates to a temozolomide freeze-dried preparation, which contains a temozolomide active ingredient and at least one solubilizer which can dissolve the temozolomide. The solubilizer used in the preparation may be N(2)-L-Alanyl-L-glutamine, glycyl-L-glutamine monohydrate, glycyl-l-tyrosine, ornithine aspartate or a mixture of the four. The temozolomide preparation prepared by using the technology provided by the invention has the advantages that the solubility of the temozolomide and the stability of the solution are improved; the quality of the solution is stable; the use of thepreparation is convenient; and the preparation method is simple and suitable for large-scale preparation.

Description

technical field [0001] The invention relates to a temozolomide freeze-dried preparation, belonging to the technical field of pharmaceutical preparations. Background technique [0002] Temozolomide (Temozolomide, trade name Temodar) chemical name 3,4-dihydro-3-methyl-4-oxoimidazo[5,1-d]-1,2,3,5-tetrazine-8-amide , developed by the Schering-Plough Company. In 1999, the FDA approved its oral capsule formulation for the treatment of adult glioblastoma and melanoma, especially the first-line treatment of glioblastoma multiforme or anaplastic astrocytoma. The emergence of temozolomide is a great progress in the treatment of malignant glioma. [0003] At present, only temozolomide capsules are taken orally in clinical practice. Although they are completely absorbed after oral administration, have high bioavailability, good tissue distribution, and can pass through the blood-brain barrier, the incidence of side effects such as nausea, vomiting, headache and burnout is very high, a...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/19A61K31/4188A61K47/18A61P35/00
Inventor 崔东冬吴宜艳赵玉佳赵君嫦韩瑞亭蔡威任玉兰徐春霖
Owner 重庆世森医药科技有限公司
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