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Flavone polyphenol drug self-emulsifying composition, preparation method of flavonoid polyphenol drug self-emulsifying composition, drug composition and application

A technology of polyphenols and compositions, which is applied in the field of self-emulsifying compositions of flavonoids and polyphenols, can solve problems such as drug precipitation, difficulty in further increasing the drug loading of baicalein, and inability to meet the requirements of drug loading, etc.

Active Publication Date: 2020-10-23
BEIJING WEHAND BIO PHARMA CO LTD +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0010] Proanthocyanidins, quercetin, curcumin, and resveratrol self-microemulsions were prepared according to the methods described in literature 2 to 5, and they were placed at 4°C and room temperature for 5 days, 1 month, and 2 months, respectively, and the changes in appearance were observed , to investigate its physical stability, the results show that the self-microemulsion mixtures of flavonoids and polyphenols prepared according to the prescriptions of literature 2-5 have obvious stability defects: they are easy to form semi-solid or precipitate after being placed at 4 ° C, and they are placed at room temperature for a period of time. drug leaching
[0015] (2) Under the conditions of given oil phase, emulsifier, and co-emulsifier, it is difficult to further increase the drug loading of baicalein, which cannot meet the requirements of clinical treatment dosage for drug loading;
[0016] (3) Compared with baicalein raw material drug, Cmax and AUC increase range is limited

Method used

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  • Flavone polyphenol drug self-emulsifying composition, preparation method of flavonoid polyphenol drug self-emulsifying composition, drug composition and application
  • Flavone polyphenol drug self-emulsifying composition, preparation method of flavonoid polyphenol drug self-emulsifying composition, drug composition and application
  • Flavone polyphenol drug self-emulsifying composition, preparation method of flavonoid polyphenol drug self-emulsifying composition, drug composition and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0066] Embodiment 1 adopts different medicine lipid ratio (baicalein crude drug and soybean phospholipid mass ratio) to prepare baicalein-phospholipid compound compound.

[0067] Precisely weigh the baicalein raw material drug and soybean lecithin according to the drug-to-lipid ratio in Table 1, place them in a 1000ml rotary steamer, add an appropriate amount of tetrahydrofuran, mix and shake well, and wait until the baicalein raw material drug and phospholipid are completely dissolved and the compound solution is clarified, place

[0068] After 15-30 minutes, place it on a rotary evaporator, and evaporate the solvent at 40°C. After the object in the rotary steaming bottle foams and becomes honeycomb, continue rotary steaming for 1 to 2 hours. After the preparation is completed, put it in a drying oven and dry it for 3 days. Gently scrape off the solid baicalein-phospholipid complex and place it in the drying oven Save it for later use.

[0069] Table 1 Prescriptions of b...

Embodiment 2

[0071] Embodiment 2 adopts different organic solvents to prepare baicalein-phospholipid complex

[0072] Using the same method as in Example 1, the difference is: the mass ratio (w / w) of baicalein crude drug to soybean lecithin is 1:3.5, and ethyl acetate, methyl alcohol, acetone, ethanol, and dehydrated alcohol are respectively used , n-propanol, isopropanol, n-butanol, isobutanol, tert-butanol, ethyl ether, methyl ethyl ether, dioxane, butanone, petroleum ether, hexane, cyclohexane, dichloromethane , chloroform, carbon tetrachloride, DMSO, and DMF were used as reaction solvents to prepare baicalein-phospholipid complexes, and the complex rate was investigated.

[0073] The results show that when the above-mentioned organic solvent is used as the reaction solvent, the recombination rates of all the obtained baicalein-phospholipid complexes are greater than 80%.

Embodiment 3

[0074] Embodiment 3 adopts different phospholipids to prepare baicalein-phospholipid complex

[0075] Using the same method as in Example 1, the difference is: the mass ratio (w / w) of baicalein crude drug to phospholipids is 1:3.5, and natural phospholipids are respectively adopted: egg yolk phospholipids or soybean phospholipids, etc., or synthetic phospholipids: Phosphoglycerides, sphingomyelin, phosphatidylcholine, phosphatidylethanolamine, phosphatidylserine, phosphatidylinositol, phosphatidylglycerol, glycerol phosphatidic acid, distearoylphosphatidylcholine, dipalmitoylphosphatidylcholine, Dipalmitoylphosphatidylethanolamine or dimyristoylphosphatidylcholine were used as lipid materials to prepare baicalein-phospholipid complexes, and the complex rates were investigated respectively.

[0076] The results show that the recombination rates of all baicalein-phospholipid complexes prepared by using the above-mentioned phospholipids are above 80%.

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Abstract

The invention discloses a flavone polyphenol drug self-emulsifying composition based on a flavone polyphenol drug-phospholipid complex as an intermediate. The self-emulsifying composition comprises the flavone polyphenol drug-phospholipid complex, an oil phase, an emulsifier and a co-emulsifier. Flavone polyphenol drugs include one or more selected from baicalein, procyanidine, quercetin, curcuminand resveratrol. The self-emulsifying composition has the beneficial effects of good stability, high drug loading capacity, high bioavailability and the like.

Description

technical field [0001] The invention relates to a flavonoid polyphenol drug self-emulsifying composition, its preparation method, pharmaceutical composition and application, and belongs to the field of medicine. Background technique [0002] Flavonoid polyphenols are currently generally divided into three categories: (1) small molecule phenolic acids, such as salicylic acid, cinnamic acid, p-hydroxycinnamic acid, caffeic acid, ferulic acid, chlorogenic acid, etc.; (2) ) Tannin, which is a polymer of polyphenols, is divided into condensed tannin and hydrolyzed tannin. The former is a polyphenol with different degrees of polymerization connected by flavanols through C4-C6 or C4-C8 bonds. Known as proanthocyanidins, the latter is formed by esterification of hydroxyl groups on sugars such as gallic acid or ellagic acid and glucose; (3) polyhydroxy flavonoids, a class of anthocyanins (anthocyanins) that are one of plant pigments glycosides), and the other category is flavones an...

Claims

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Application Information

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IPC IPC(8): A61K45/00A61K9/107A61K47/24A61K47/44A61K31/352A61K31/12A61K31/05A61P3/06A61P9/10A61P9/12A61P1/16A61P31/00A61P35/00A61P39/06
CPCA61K45/00A61K47/24A61K47/44A61K31/352A61K31/12A61K31/05A61P3/06A61P9/10A61P9/12A61P1/16A61P35/00A61P39/06A61K9/107A61K47/14A61K47/10A61P37/02A61P17/16A61P31/04A61P31/12A61P29/00A61P37/08A61P25/28A61P31/14A61P19/10A61P31/00A61K36/539A61K9/1075A61K31/353A61K9/145A61K47/544A61K47/22
Inventor 刘玉玲廖恒锋高越董武军刘志华王邦源张运冯遇周君卓刘璐叶军杨艳芳夏学军
Owner BEIJING WEHAND BIO PHARMA CO LTD
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