Freeze dried powder injection of hirudin and its preparation method

Abstract

The invention discloses a freeze dry injection of hirudin and its preparation process. It is characterized in that hirudin is extracted from fresh leech, pharmaceutic adjuvant can be added or not added after purification to prepare freeze dry injection formulation of hirudin, the character also lies in not adopting any organic solvent in the preparation method, but adopting purification methods of ultra filtration, ion exchange column chromatography and reverse osmosis condensation to get hirudin with comparative highly purity. The pharmacody experiment result indicates that the freeze dry injection has a favorable pharmacological action.

Description

Technical field [0001] The invention belongs to the technical field of traditional Chinese medicine pharmacy, and in particular relates to a hirudin freeze-dried powder injection and a preparation method thereof. Background technique [0002] Leech is a traditional Chinese medicine in my country, which was recorded in "Shen Nong's Materia Medica" 1800 years ago. Traditional Chinese medicine believes that it has the effects of breaking blood, expelling blood stasis, and dredging menstrual flow. It is mainly used to treat lumps, lumps, blood stasis, amenorrhea, and bruises. In the West, leeches are also commonly used to suck blood to treat certain diseases. A variety of active ingredients have been extracted from leeches and their salivary glands, among which hirudin is the most active and most researched ingredient. It is a small molecular protein (polypeptide) composed of 65-66 amino acids. Hirudin has a strong inhibitory effect on thrombin, and is the strongest natural sp...

AI Technical Summary

Problems solved by technology

In recent years, there have been more and more studies on recombinant hirudin. However, compared with natural hirudin, recombinant hirudin has two congenital defects: on the one hand, although recombinant hirudin is extremely similar to natural hirudin in amino acid sequence and structure Similar, but the deletion of the sulfate group on the 63-position tyrosine residue makes the inhibitory constant of recombinant hirudin to thrombin 90% lower than that of natural hirudin; on the other hand, an important reason is that hirudin is a good drug The effect is not only the effect of hirudin, but also the participation of other active ingredients in leech saliva.

[0004] The patent application number 03113566 discloses a method for extracting and purifying hirudin, which is to extract hirudin with acetone from the saliva secretion of living leeches, and then purify with column chromatography. The use of organic solvents makes the environmental requirements particularly high, and only anion exchange column chromatography (gel filtration column chromatography is only the effect of molecular sieves) is used for purification, the impurities are not completely separated, the purity of hirudin is not high, and this patent has not been seen Reports on the purity of hirudin; the patent application number 95117701 discloses the use of affinity chromatography to purify hirudin, but in the actual application process, it is only suitable for laboratories and cannot be further scaled up and produced in pilot scales, which is not conducive to industrialization.

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