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Stable preparation method of decitabine freeze-dry preparation

A technology for decitabine and freeze-dried preparations, which is applied in the field of preparation of decitabine freeze-dried preparations, can solve problems such as increasing the toxic and side effects of drugs, and achieve the effects of reducing toxic and side effects, avoiding a large amount of degradation, and slowing down the degradation speed.

Inactive Publication Date: 2009-02-11
深圳万乐药业有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The above-mentioned organic solvents are injected into the blood as injections, which undoubtedly increases the toxic and side effects of the drug

Method used

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  • Stable preparation method of decitabine freeze-dry preparation
  • Stable preparation method of decitabine freeze-dry preparation
  • Stable preparation method of decitabine freeze-dry preparation

Examples

Experimental program
Comparison scheme
Effect test

preparation Embodiment 1

[0020] Disperse 50g of decitabine evenly in 6L of tert-butanol, add sodium hydroxide and sodium dihydrogen phosphate buffered saline solution with a pH of 6.5 to 7.5 to 10L for miscibility, and control the miscibility temperature at -10°C to obtain Citabine clear solution. 0.22um membrane filter, filled into vials and freeze-dried to remove tert-butanol-water mixture. Related substances of decitabine after dissolution ≤ 1%, almost no degradation occurs, after freeze-drying product decitabine related substances ≤ 3%, residual organic solvent is 0.31%, and is still stable through the test of influencing factors, related substances Still < 3%.

preparation Embodiment 2

[0022] Evenly disperse 60 g of decitabine in 5 L of ethanol, add water to 10 L for miscibility, and control the miscibility temperature at 0° C. to obtain a clear solution of decitabine. 0.22um membrane filter, filled into vials and freeze-dried to remove ethanol-water mixture. Related substances of decitabine after dissolution ≤ 1%, almost no degradation occurs, after freeze-drying, related substances of decitabine ≤ 3%, residual organic solvent is 0.12%, and it is still stable through the test of influencing factors, related substances Still < 3%.

preparation Embodiment 3

[0024] Disperse 70 g of decitabine evenly in 3 L of methanol, add a mixed solution of lactose and potassium dihydrogen phosphate with a pH of 5.5 to 6.5 to 10 L for miscibility, and control the miscibility temperature at 10° C. to obtain a clear solution of decitabine. 0.22um membrane filter, filled into vials and freeze-dried to remove tert-butanol-water mixture. The related substances of decitabine after dissolution are ≤1%, almost no degradation occurs, the related substances of decitabine after lyophilization are ≤3%, and the residual organic solvent is 0.09%, and it is still stable through the test of influencing factors. Still < 3%.

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Abstract

The invention discloses a method for preparing a stable Decitabine freeze-dried preparation, which comprises the following steps: Decitabine is uniformly dispersed in at least one of organic solvents including tertiary butyl alcohol, ethanol and methanol or dissolved in the organic solvent dimethyl sulfoxide; and then the mixed solution is mixed with water for injection or the water for injection with freeze-dried propping agents and / or pH regulators dissolved, thus obtaining a new mixed solution and the organic solvent accounting for 5-80 percent of the mixed solution in volume; and organic solution is removed after filtration and freeze drying. The method can prepare a stable Decitabine freeze-dried preparation, in which the residual quantity of organic solvent is not more than 1 percent.

Description

technical field [0001] The invention relates to a preparation method of a stable decitabine freeze-dried preparation. Background technique [0002] Decitabine is a cytosine analog, which belongs to DNA methyltransferase inhibitors. After phosphorylation, it directly binds to DNA to inhibit DNA methyltransferase, causing DNA hypomethylation and cell differentiation and apoptosis. [0003] Because decitabine is extremely unstable in aqueous solution, the water molecules in the aqueous environment carry out nucleophilic attack on its 5-azacytosine ring, which causes the 5-azacytosine ring to break and degrade to its α-inactive form. Isomers. Therefore, routinely use water as a solvent to prepare a stable and qualified freeze-dried preparation. [0004] In order to solve the above problems, the US patent application US20060128653 discloses that decitabine and cyclodextrin are combined into a compound, and the cyclodextrin encapsulates the drug inside so as to avoid the degrada...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/19A61K31/706A61P43/00
Inventor 吴静曾嘉铨张汉利宝玉荣
Owner 深圳万乐药业有限公司
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