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.
CN101361718AInactive Publication Date: 2009-02-11深圳万乐药业有限公司
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
深圳万乐药业有限公司
Publication Date
2009-02-11
Estimated Expiration
Not applicable · inactive patent

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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.
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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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