Method for lowering osmotic pressure of boron-carrying agent injection

Abstract

The invention relates to a method for lowering osmotic pressure of a boron-carrying agent injection. The method comprises the step of adopting a nanofiltration technology. The method is simple and easy to implement, good in osmotic pressure lowering effect, good in stability, high in safety and applicable to industrial production.

Description

technical field [0001] The invention relates to a method for reducing the osmotic pressure of a boron carrier injection, in particular to a method for reducing the osmotic pressure of a boron carrier injection by using nanofiltration technology, and belongs to the technical field of pharmacy. Background technique [0002] The chemical name of L-BPA is 4-dihydroxyboryl-L-phenylalanine, and its structural formula is as follows: [0003] [0004] L-BPA is a boron carrier for boron neutron capture therapy, which requires tumor cells to reach 10 9 However, due to the low boron loading capacity of L-BPA and the limited targeting, the dosage is very large, reaching 100-500mg / kg. Due to the poor water solubility of L-BPA, it is necessary to use a large amount of sodium hydroxide to dissolve it during the preparation process, and then use polyhydroxy sugar to form a complex with it, and use hydrochloric acid to adjust the pH to an acceptable range. A large amount of excess sodiu...

AI Technical Summary

Problems solved by technology

Due to the poor water solubility of L-BPA, it is necessary to use a large amount of sodium hydroxide to dissolve it during the preparation process, and then use polyhydroxy sugar to form a complex with it, and use hydrochloric acid to adjust the pH to an acceptable range. A large amount of excess sodium chloride will be produced under the process conditions, which will cause the osmotic pressure of the preparation to be high, and the risk of use is greater

[0005] The US6169076B1 patent provides a method for reducing the osmotic pressure, that is, after the L-BPA-saccharide complex is prepared, hydrochloric acid is not used for callback, and H + A type of cation exchange resin that exchanges Na in the solution + , reduce the pH of the solution at the same time, but the amount of resin used in this method is large, the concentration of the L-BPA solution obtained is low, and it is difficult to control the end point at the same time, the pH needs to be monitored in real time. Once the pH is too low, it will cause precipitation. of limited utility

[0006] When using L-BPA preparation clinically at present, all adopt the mode of preparing and using now, the main reason is that L-BPA-fructose solution is sensitive to temperature and is not easy to store; patent CN103100094B provides a kind of freeze-drying method, but this method only Suitable for low concentration and small batch, not suitable for large production

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