GRANULAR COMPLEX KETONE ETHER OF GINKGO BILOBA AND METHOD FOR ITS PREPARATION Russian patent published in 2022 - IPC A61K36/16 A61K9/14 A61K9/16 A61K127/00 B01D11/02 

FIELD: pharmaceutical industry.

SUBSTANCE: group of inventions relates to the pharmaceutical industry, namely to the granular composition of ginkgo biloba leaf extract, the method for its preparation and its application. A method for obtaining a granular composition from ginkgo biloba leaf extract, includes the following steps: A) mixing and stirring of ginkgo biloba leaf extract, dextrin, sucrose powder, starch, low-substituted hydroxypropyl cellulose and aspartame in accordance with the ratio in the composition and adding at the same time an aqueous solution of ethanol to obtain a soft material; B) obtaining wet granules from soft material, followed by drying of wet granules; and C) sieving and straightening of dried granules, mixing, releasing and packaging into bags to obtain a granular composition from ginkgo biloba leaf extract; where the ratio in the composition in weight parts includes the following: 35-45 parts of ginkgo biloba leaf extract; 450-500 parts of dextrin; 420-450 parts sucrose powder; 10-30 parts starch; 10-30 parts low-substituted hydroxypropyl cellulose; and 5-10 parts aspartame; moreover, extraction to obtain ginkgo biloba leaf extract includes the following stages: a) crushing of ginkgo biloba leaves to obtain crushed ginkgo biloba leaves; b) adding an aqueous ethanol solution to crushed ginkgo biloba leaves, conducting a double extraction by heating with a reverse refrigerator and obtaining the first filtrate by filtering; c) adding water to the filtered residue of the drug remaining after filtration, conducting a single extraction by heating with a reverse refrigerator, and then obtaining a second filtrate by filtration; d) combining and concentrating the second filtrate and the first filtrate into a thick paste, dissolving in purified water, cooling and filtering to obtain a filtrate; e) loading the filtrate into a column with a macroporous resin, sequential elution with 18% aqueous ethanol solution, 30% aqueous ethanol solution and 50% aqueous ethanol solution to obtain 18% ethanol eluent, 30% ethanol eluent and 50% ethanol eluent, respectively, which are the first eluents; in the first eluents, 50% ethanol eluent it is the first eluent with a high concentration of solvent, and the combined solution of 18% ethanol eluent and 30% ethanol eluent is the first eluent with a low concentration of solvent; f) concentration of the first eluent with a low concentration of solvent so that there is no smell of alcohol, loading the first eluent with a low concentration of solvent into a polyamide column, and then elution with ethanol to obtain ethanol eluate, which is the second eluate; g) combining and concentrating the second eluent and the first eluent with a high concentration of solvent until the smell of alcohol disappears; h) extraction of concentrate with cyclohexane, discarding cyclohexane extract, spray drying of concentrated solution or concentration of concentrated solution into a thick paste and vacuum drying of thick paste; grinding of dried products to obtain ginkgo biloba leaf extract; and where the granular composition of ginkgo biloba leaf extract, based on the loading weight of each package of 1 g, satisfies the following conditions: 1) the content of rutin is less than or equal to 1.60 mg/bag; 2) the content of quercetin is less than or equal to 0.160 mg/bag; 3) the content of bilobalide is 1.04-2.08 mg/bag; 4) the content of ginkgolide J is 0.04-0.20 mg/bag; 5) the residual ethanol content is less than or equal to 0.2 mg/bag; 6) the content of biflavonoids is less than or equal to 0.008 mg/bag, and these biflavonoids include amentoflavone, bilobetin and ginkgetin; 7) the content of genistin is 0, and the content of ginkgolide M is 0; 8) the content of terpene lactones is 2.4-4.8 mg/bag; 9) the content of total flavonoids is 14.08-26.40 mg/bag; and 10) the content of total flavonol glycosides is 9.6-14.0 mg/bag. Granular composition of ginkgo biloba leaf extract, providing anti-PAF (platelet activation factor) effect and nerve nutrition obtained by the above method, where the content of total ginkgolic acids in the granular composition of ginkgo biloba leaf extract is less than or equal to 2 mcg/bag; where total ginkgolic acids in the granular composition of ginkgo biloba leaf extract is calculated based on the total content of ginkgolic acid C13:0, ginkgolic acid C15:1 and ginkgolic acid C17:1. A granular composition from ginkgo biloba leaf extract, providing an anti-PAF effect and nerve nutrition, obtained by the above method, where the ratio of the areas of chromatographic peaks of quercetin to kaempferide in the granular composition of ginkgo biloba leaf extract is 0.8-1.2, and the ratio of the areas of chromatographic peaks of isoramnetin to quercetin in the granular composition of ginkgo biloba leaf extract is greater than 0.15. The above method can be used to obtain a granular composition from ginkgo biloba leaf extract, which provides an anti-PAF effect and nerve nutrition.

EFFECT: above-described granular composition has a high therapeutic activity, providing an anti-PAF effect and nerve nutrition, excellent taste sensation.

7 cl, 1 dwg, 5 tbl, 3 ex