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Solid dispersion (SD) of radix salviae miltiorrhizae and radix puerariae extracts and preparation method of SD

A technology of solid dispersion and kudzu root extract, which is applied in the field of solid dispersion of salvia miltiorrhiza and kudzu root extract and its preparation, can solve the problems of low absorption efficiency, low solubility, and affecting drug efficacy, and achieve improved dissolution rate and good Prevention and control effect, reduction of production cost and dosage

Active Publication Date: 2021-02-05
SICHUAN ACAD OF CHINESE MEDICINE SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Among the above active ingredients, total tanshinone is a fat-soluble component with low solubility in water and is an insoluble drug. If the total tanshinone is directly administered orally, the absorption efficiency is low, thereby affecting its medicinal effect.

Method used

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  • Solid dispersion (SD) of radix salviae miltiorrhizae and radix puerariae extracts and preparation method of SD

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0027] Salvia miltiorrhiza is crushed through a 10-mesh sieve, 10 kg is taken, and 80% ethanol (both volume content, the same below) is used as a solvent, soaked for about 3 hours, percolated at a speed of about 4ml / kg per minute, and collected 10 times the volume of percolated The eluting liquid (based on the weight-volume ratio of Salvia miltiorrhiza, the same below), i.e. 100L, recovered ethanol under reduced pressure, diluted with water to about 0.5g crude drug / ml, adjusted the pH value to about 3.0 with hydrochloric acid, allowed to stand for precipitation, filtered, and obtained the total Tanshinone precipitation, set aside. The filtered aqueous solution is applied to a HPD100 macroporous adsorption resin column. After washing with water of 2 times of the column bed volume, the water washing solution is discarded, and then eluted with 50% ethanol, and the ethanol eluent of 3 times of the column bed volume is collected, and the Press to recover ethanol, concentrate to the...

Embodiment 2

[0031] Grind Danshen through a 20-mesh sieve, take 10 kg, moisten with an appropriate amount of 80% ethanol, seal it for about 3 hours, put it into a percolator, add 80% ethanol to soak for about 5 hours, and percolate at a speed of about 4ml / kg per minute. Collect 8 times the volume of percolation liquid, recover ethanol under reduced pressure, add water to dilute to about 1.0 g crude drug / ml, adjust pH value to about 3.0 with hydrochloric acid, let stand for precipitation, and centrifuge to obtain total tanshinone precipitate, which is set aside. Put the centrifuged aqueous solution on a D101 macroporous adsorption resin column, wash it with 3 times the column bed volume of water, and then elute with 40% ethanol, collect the ethanol eluate with 2 times the column bed volume, recover the ethanol under reduced pressure, and concentrate When the relative density is about 1.05 (50°C), the total phenolic acid extract of Salvia miltiorrhiza is obtained.

[0032] Take 20kg of kudzu...

Embodiment 3

[0035] Grind Salvia miltiorrhiza through a 10-mesh sieve, take 10kg, use 85% ethanol as a solvent, soak for about 4 hours, permeate at a speed of about 4ml / kg per minute, collect 4 times the volume of the initial liquid, and then continue to collect 4 times the volume Volume of continuous distillate. Recover the ethanol from the salvia miltiorrhiza under reduced pressure, concentrate it to about 7 times (for example, if 1000ml is concentrated to about 150ml, that is about 7 times), add water to dilute to about 1g crude drug / ml, stir well, let it stand for precipitation, and filter to obtain tanshinone precipitate (I) and the first water precipitation solution (I); after the salvia miltiorrhiza is decompressed to recover ethanol, add the first water precipitation solution (I), recover and concentrate to remove ethanol, add water to dilute to about 0.5g crude drug / ml , adjust the pH value to about 3.0 with hydrochloric acid, let the precipitation stand, and filter to obtain the ...

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Abstract

The invention discloses a solid dispersion (SD) of radix salviae miltiorrhizae and radix puerariae extracts and a preparation method of the SD. The SD takes total salvianolic acid, total flavonoids ofradix puerariae and total tanshinone as effective medicinal components, takes the contained total salvianolic acid and total flavonoids of radix puerariae as a combined carrier of the total tanshinone, and does not contain other solid dispersion carrier materials except the total salvianolic acid and the total flavonoids of radix puerariae. When the SD is prepared, the total salvianolic acid andthe total flavonoids of radix puerariae are mixed and concentrated into the combined carrier, and then the total tanshinone is loaded, and concentration and drying are carried out to form the SD. Thedissolution rate of tanshinone is effectively improved, and the 90 min cumulative dissolution rate of tanshinone IIA in the total tanshinone is larger than 60%.

Description

technical field [0001] The invention relates to a solid dispersion of salvia miltiorrhiza and kudzu root extract (total phenolic acids of salvia miltiorrhiza, total tanshinone and total flavonoids of kudzu root) and a preparation method thereof. Prepared into a solid dispersion, significantly improving the dissolution rate and bioavailability of tanshinone. Background technique [0002] Solid dispersion (SD) refers to a dispersion system in solid form formed by highly dispersing drugs in solid carriers, and is mainly used to accelerate and increase the dissolution of insoluble drugs and improve their bioavailability. Commonly used solid dispersion carrier materials can be divided into three categories: water-soluble carrier materials, including polyethylene glycol (PEG), povidone (PVP), surfactants, organic acids, sugars and alcohols, etc.; insoluble carrier materials Materials, including cellulose, polyacrylic resin, etc.; enteric carrier materials, including cellulose and...

Claims

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Application Information

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IPC IPC(8): A61K36/537A61K9/14A61K9/48A61P9/10A61P3/10A61P25/28A61P9/00A61K36/488
CPCA61K36/537A61K36/488A61K9/14A61K9/4808A61P9/10A61P3/10A61P25/28A61P9/00A61K2236/333A61K2236/55A61K2300/00
Inventor 易进海刘云华黄志芳陈燕刘玉红
Owner SICHUAN ACAD OF CHINESE MEDICINE SCI
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