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Flavonoid polyphenol drug self-emulsifying composition, preparation method thereof, pharmaceutical composition and application of pharmaceutical composition

A technology of polyphenols and compositions is applied in the field of flavonoid polyphenols drug self-emulsifying compositions, and can solve the problems of difficulty in further increasing the drug loading of baicalein, drug precipitation, and stability defects, and achieve good self-emulsifying ability, High bioavailability and high drug loading effect

Pending Publication Date: 2020-10-20
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
The results showed that phospholipids had no significant effect on the bioavailability of fenofibrate SEDDS

Method used

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  • Flavonoid polyphenol drug self-emulsifying composition, preparation method thereof, pharmaceutical composition and application of pharmaceutical composition
  • Flavonoid polyphenol drug self-emulsifying composition, preparation method thereof, pharmaceutical composition and application of pharmaceutical composition
  • Flavonoid polyphenol drug self-emulsifying composition, preparation method thereof, pharmaceutical composition and application of pharmaceutical composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0059] Example 1: Preparation of baicalein self-emulsifying composition with different oil phases

[0060] Use Tween 80 as emulsifier, transcutol HP as co-emulsifier, use different oil phases as shown in Table 1 below, and accurately weigh the oil phase, emulsifier and co-emulsifier in a suitable container at a ratio of 2:5:3 , Mix well to obtain blank self-emulsifying concentrate, and then weigh an appropriate amount of baicalein raw material (according to the loading amount of 20mg / g) and soybean phospholipids according to the drug-to-lipid ratio of 1:3.5, and put it in the blank self-emulsifying concentrate. Place it in an air bath shaker at a temperature of 25°C and a rotation speed of 210 rpm. After the baicalein and soybean phospholipids were completely dissolved, the baicalein self-emulsifying composition was obtained, and the drug loading and emulsified particle size were measured at the same time (as shown in Table 2).

[0061] Table 1

[0062]

[0063]

Embodiment 2

[0064] Example 2: Preparation of baicalein self-emulsifying composition with different emulsifiers

[0065] Use ethyl oleate as the oil phase, transcutol HP as the co-emulsifier, use the different emulsifiers shown in Table 2 below, and accurately weigh the oil phase, emulsifier and co-emulsifier in a suitable container at a ratio of 2:5:3 Inside, mix well to obtain a blank self-emulsifying concentrate, and then weigh an appropriate amount of baicalein API (feeding at 20mg / g drug loading) and soybean phospholipids according to the drug-to-lipid ratio of 1:3.5. It is placed in an air bath shaker with a temperature of 25°C and a rotation speed of 210 rpm. After the baicalein and phospholipids were completely dissolved, the baicalein self-emulsifying composition was obtained, and its drug loading and emulsified particle size were measured at the same time (as shown in Table 2).

[0066] Table 2

[0067]

Embodiment 3

[0068] Example 3: Preparation of baicalein self-emulsifying composition with different co-emulsifiers

[0069] Using ethyl oleate as the oil phase, Tween 80 as the emulsifier, using different emulsifiers as shown in Table 3 below, according to the ratio of 2:5:3, accurately weigh the oil phase, emulsifier and emulsifier In a suitable container, mix evenly to obtain a blank self-emulsifying concentrate, and then weigh an appropriate amount of baicalein API (20mg / g feed) and soybean phospholipids in the blank self-emulsifying concentrate at a ratio of 1:3.5. Place it in an air bath shaker at a temperature of 25°C and a rotation speed of 210 rpm. After the baicalein and soybean phospholipids were completely dissolved, the baicalein self-emulsifying composition was obtained, and the drug loading and emulsified particle size were measured at the same time (as shown in Table 3).

[0070] table 3

[0071]

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Abstract

The invention discloses a phospholipid-containing flavonoid polyphenol drug self-emulsifying composition. The composition comprises a flavonoid polyphenol drug, free phospholipid, an oil phase, an emulsifier and a co-emulsifier, and the flavonoid polyphenol drug comprises one or more materials selected from baicalein, procyanidine, quercetin, curcumin and resveratrol. The composition has the beneficial effects of good stability, high drug loading capacity, higher bioavailability and the like.

Description

Technical field [0001] The invention relates to a phospholipid-containing flavonoid polyphenol drug self-emulsifying composition, its preparation method, pharmaceutical composition and use belong to the field of medicine. Background technique [0002] Flavonoid polyphenol compounds are generally divided into three categories: (1) Small molecules of phenolic acids, such as salicylic acid, cinnamic acid, caffeic acid, ferulic acid, chlorogenic acid, etc.; (2) ) Tannin, a polymer of polyphenols, is divided into condensed tannins and hydrolyzed tannins. The former are polyphenols 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 gallic acid or ellagic acid with hydroxyl groups on sugars such as glucose; (3) Polyhydroxyflavonoids, a type of anthocyanin, which is one of plant pigments Glycosides), the other is the narrow sense of flavonoids and their glycosides. Aglycones ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/107A61K31/352A61K31/353A61K31/12A61K31/05A61K47/24A61P31/00A61P29/00A61P37/08A61P37/02A61P35/00A61P39/06A61P17/18A61P5/00A61P9/12A61P3/06A61P9/10A61P25/28A61P17/02A61P19/10A61P1/16
CPCA61K9/107A61K47/24A61K31/352A61K31/353A61K31/12A61K31/05A61P31/00A61P29/00A61P37/08A61P37/02A61P35/00A61P39/06A61P17/18A61P5/00A61P9/12A61P3/06A61P9/10A61P25/28A61P17/02A61P19/10A61P1/16
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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