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Busulfan injection and preparation method thereof

A busulfan injection and a technology for busulfan injection, which are applied in the field of busulfan injection, can solve problems such as the stability of busulfan injection not found, and achieve the effect of improving stability

Active Publication Date: 2015-03-04
SICHUAN CREDIT PHARMA +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Through the search of literature and previous patented technologies, no other methods have been found to effectively improve the stability of busulfan injection.

Method used

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  • Busulfan injection and preparation method thereof
  • Busulfan injection and preparation method thereof
  • Busulfan injection and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] The preparation of embodiment 1 busulfan injection of the present invention

[0030] Take 60 mg of Busulfan crude drug and 1 mg of citric acid (accounting for 0.01% w / v of the total amount of the mixed solvent), add 3.3 ml of N,N-dimethylacetamide, and stir to dissolve. Add 0.3% activated carbon by volume of the solution, stir at room temperature for 30 minutes, and filter with a 0.45 μm microporous membrane. Add 6.7ml of polyethylene glycol 400, stir evenly, filter with a 0.22 μm microporous membrane, and aseptically fill.

Embodiment 2

[0031] The preparation of embodiment 2 busulfan injection of the present invention

[0032] Take 60mg of Busulfan crude drug, 20mg of citric acid / sodium citrate (1:1, m / m) (accounting for 0.2%w / v of the total amount of mixed solvent), add 3.3ml N,N-dimethyl Acetamide, stir to dissolve. Add 0.3% activated carbon by volume of the solution, stir at room temperature for 30 minutes, and filter with a 0.45 μm microporous membrane. Add 6.7ml polyethylene glycol 400 and stir well. 0.22μm microporous membrane filtration, aseptic filling.

Embodiment 3

[0033] The preparation of embodiment 3 busulfan injections of the present invention

[0034] Take 60 mg of Busulfan crude drug and 10 mg of citric acid (accounting for 0.1% w / v of the total amount of the mixed solvent), add 3.3 ml of N,N-dimethylacetamide, and stir to dissolve. Add 0.3% activated carbon by volume of the solution, stir at room temperature for 30 minutes, and filter with a 0.45 μm microporous membrane. Add 6.7ml polyethylene glycol 400 and stir well. 0.22μm microporous membrane filtration, aseptic filling.

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Abstract

The invention provides a busulfan injection. Busulfan is dissolved in a mixed solvent of N,N-dimethyl acetamide with a volume ratio of 33% and polyethylene glycol 400 with a volume ratio of 67%, wherein the concentration of the busulfan is 6mg / ml, and the mixed solvent contains organic acid and alkali metal or alkaline earth metal salt of organic acid, which account for 0.01-5%w / v of the total amount of the mixed solvent; and the organic acid contains more than two carboxyl groups. The stability of main constituents of the busulfan injection provided by the invention can be improved remarkably so that the quality guarantee period of products is prolonged to more than 24 months; and various indices (such as appearance, content of tetrahydrofuran, content of main constituents, content of impurities, endotoxin, sterility test and the like) conform to the requirement of the quality standard. The active constituents and the auxiliary materials of the injection provided by the invention have no injection stimulation, and the injection can be used for clinical injection and can ensure that the medication safety cannot be lowered while the stability of products is improved.

Description

technical field [0001] The invention relates to a busulfan injection, which belongs to the field of pharmaceutical preparations. Background technique [0002] Busulfan injection is mainly used for the treatment of chronic myelogenous leukemia, polycythemia vera, and myelofibrosis. The products currently on the market are only produced by Ben Venue Laboratories, Inc. The clinically used preparations in China are sold on the market in my country after subpackaging by Otsuka Pharmaceutical Company, Ltd. There are two US patents US5430057 and US5559148, one Canadian patent CA2171738 and one EU patent EP 0 725 637 B1 about the preparation of this product. It is proposed to dissolve this product in a mixed solution of a certain proportion of N,N-dimethylacetamide, polyethylene glycol 400 and / or water. From the analysis of the chemical structure of busulfan, the instability of this product is mainly concentrated on the easily hydrolyzed ester bond, so choosing a suitable solvent ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/255A61K9/08A61K47/32A61K47/12A61P35/02
Inventor 陈刚宋庆国
Owner SICHUAN CREDIT PHARMA
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