Hesperetin complex with high oral bioavailability and antioxidant activity and its preparation method and application

An antioxidant activity, hesperetin technology, applied in the direction of organic active ingredients, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc. It can increase the oral bioavailability, enhance the water solubility and prolong the oral bioavailability.

Active Publication Date: 2019-02-05
宁波宁瑞生物科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] The invention provides a hesperetin complex with high oral bioavailability and antioxidant activity and its preparation method and application. The hesperetin complex overcomes the problems of poor water solubility, low oral bioavailability and in vivo The shortcoming of the half-life, the preparation method of the present invention is simple, the prepared hesperetin complex is stable, has better water solubility, antioxidant activity, oral bioavailability and longer half-life in vivo

Method used

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  • Hesperetin complex with high oral bioavailability and antioxidant activity and its preparation method and application
  • Hesperetin complex with high oral bioavailability and antioxidant activity and its preparation method and application
  • Hesperetin complex with high oral bioavailability and antioxidant activity and its preparation method and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0042] Raw materials: hesperetin 10mg, TPGS 60mg.

[0043] Preparation process: Dissolve 10mg of hesperetin and 60mg of TPGS in 10ml of ethanol, ultrasonically promote their complete dissolution, 40°C water bath, magnetic stirring for 30min, evaporate under reduced pressure until the solvent is completely volatilized, then freeze-dry to obtain hesperetin and TPGS Hesperetin complex with a mass ratio of 1:6.

[0044] Solubility of the hesperetin complex: in 10ml of water, 10mg of hesperetin dissolves 19.77%.

[0045] The average particle size of the hesperetin complex in water is 32.29nm.

Embodiment 2

[0047] Raw materials: Hesperetin 10mg, TPGS 90mg.

[0048] Preparation process: Dissolve 10mg hesperetin and 90mg TPGS in 10ml ethanol, ultrasonically promote their complete dissolution, 40°C water bath, magnetic stirring for 30min, evaporate under reduced pressure until the solvent is completely volatilized, then freeze-dry to obtain hesperetin and TPGS Hesperetin complex with a mass ratio of 1:9.

[0049] Solubility of the hesperetin complex: In 10ml of water, 10mg of hesperetin dissolves 71.72%.

[0050]The average particle diameter of the hesperetin complex in water is 28.91 nm.

Embodiment 3

[0052] Raw materials: Hesperetin 10mg, TPGS 120mg.

[0053] Preparation process: Dissolve 10mg hesperetin and 120mg TPGS in 10ml ethanol, ultrasonically promote their complete dissolution, 40°C water bath, magnetic stirring treatment for 30min, evaporate under reduced pressure until the solvent is completely volatilized, then freeze-dry to obtain hesperetin and TPGS Hesperetin complex with a mass ratio of 1:12.

[0054] Solubility of the hesperetin complex: In 10 ml of water, 10 mg of hesperetin dissolves 100%.

[0055] The average particle diameter of this hesperetin complex in water is 26.15nm, and its particle size distribution figure in water is as follows figure 1 shown.

[0056] The hesperetin complex was subjected to differential scanning calorimetry, as figure 2 As shown, the curve of TPGS has a sharp exothermic peak at 40°C, which is the melting point peak, and hesperetin has a sharp exothermic peak at 230°C, which is the melting point peak. After the complex is f...

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Abstract

The invention discloses a hesperetin compound with high oral bioavailability and antioxidant activity, and a preparation method and application of the hesperetin compound. In the hesperetin compound, hesperetin is used as a raw material medicine, and TPGS is used as a carrier auxiliary; the mass ratio of hesperetin to TPGS is 1 to (0.1 to 20). TPGS is an effective P-glycoprotein inhibitor which inhibits the drug efflux function of P-glycoprotein; hesperetin is used as a substrate of P-glycoprotein. The hesperetin compound disclosed by the invention can increase the oral bioavailability through the inhibition effect of TPGS on P-glycoprotein of intestinal epithelial cells.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations, in particular to a hesperetin complex with high oral bioavailability and antioxidant activity, a preparation method and application thereof. Background technique [0002] Hesperetin (hesperetin) is the main medicinal ingredient of Rutaceae citrus fruit, derived from the hydrolysis of hesperidin, belongs to the flavanones in flavonoids, and its molecular formula is C 16 h 14 o 6 , the relative molecular mass is 302.28. [0003] Hesperetin has a wide range of pharmacological activities, such as anti-oxidation and scavenging free radicals, regulating the cardiovascular system, protecting the nervous system, anti-allergy and dermatitis, anti-cancer and genotoxicity, anti-virus and microorganisms. Among them, the most important physiological activity of hesperetin lies in its anti-oxidation and free radical scavenging effect. Oral administration can reduce the oxidation level of tissues a...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/19A61K31/352A61K47/22A61P39/06
CPCA61K9/0053A61K9/19A61K31/352A61K47/22
Inventor 刘祥瑞顾苏芳王砾莹赵炳祥周珠贤唐建斌申有青
Owner 宁波宁瑞生物科技有限公司
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