New bilobalide B compound and preparation method thereof

Abstract

The invention relates to a new bilobalide B compound. The bilobalide B compound is extracted from ginkgo leaf; and the bilobalide B content in the bilobalide B compound is greater than 99%. The bilobalide B compound contains bilobalide A of which the content is lower than 0.4%. The invention also relates to a preparation method of the bilobalide B compound, which comprises the following steps: under stirring conditions, adding kieselguhr and ginkgo leaf extract, heating under reflux at 78-85 DEG C for 0.5-1.5 hours, filtering and concentrating; adding distilled water, removing impurities, separating out the ethyl acetate layer, passing the ethyl acetate layer through an peracidic aluminum oxide column, eluting with water saturated ethyl acetate, and collecting the eluate; concentrating the eluate under reduced pressure until no ethyl acetate smell is emitted, adding a proper amount of ethanol to dissolve the concentrated eluate, adding water until the ethanol content is 60-70%, standing, precipitating coarse crystal, filtering, taking the coarse crystal, and drying; and recrystallizing the coarse crystal sequentially with ethanol and ethyl acetate to obtain the finished product bilobalide B compound.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a novel ginkgolide B compound and a preparation method thereof. Background technique [0002] Ginkgolide B, English name Ginkgolide B; molecular formula: C 20 h 24 o 10 ;Molecular weight: 424.40. [0003] Ginkgolide B is a highly active platelet activating factor (PAF) antagonist, which can competitively bind to the PAF receptor and inhibit the action of PAF; therefore, any diseases related to PAF, such as: thrombosis, cerebral Ginkgolide B has a certain curative effect on tissue damage, organ transplant rejection, acute inflammation, cardiac allergy, cellular endotoxin and shock caused by IgG. [0004] But so far, there are no preparations with a single component of ginkgolide B as a raw material on the market both at home and abroad. According to the chemical drug registration classification in my country's "Measures for the Administration of Drug Registration...

AI Technical Summary

Problems solved by technology

[0008] At present, the medicinal ginkgolide B is mainly extracted from Ginkgo biloba, but because the content of Ginkgolide B in Ginkgo leaves is extremely low, and Ginkgolide B and Ginkgolide A, ginkgolic acid and bilobalide co-exist , the structure of ginkgolide B and ginkgolide A is very similar, and the polarity difference is very small, it is difficult to extract high-purity ginkgolide B monomer from ginkgo leaves, especially the combination of ginkgolide B and ginkgolide The separation of A is more difficult

The purity of ginkgolide B extracted in the above-mentioned patents and the prior art is not high enough, and the solubility of ginkgolide B is poor, so it can only be used as a raw material for oral administration and not as a raw material for injections, and the bioavailability of oral administration is relatively low. Low, can not give full play to the efficacy of ginkgolide B, the use of injections can greatly improve its bioavailability, and the clinically applicable population - patients with ischemic encephalopathy, including patients with acute ischemic stroke and cerebral infarction, the treatment time window is narrow , and needs to take effect quickly. Generally, oral preparations have a slower onset of action than injections, but the onset of administration is rapid after being made into injections. In addition, patients with ischemic encephalopathy may have difficulty swallowing oral drugs, but injections do not. difficult question

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