Hesperetin emulsion and preparation method thereof

A technology of hesperetin and emulsion, applied in the directions of anti-inflammatory agent, antitoxic agent, antifungal agent, etc., can solve the problems of low drug loading and fast oral metabolism of hesperetin

Active Publication Date: 2021-07-30
GUANGZHOU HANFANG PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The object of the present invention is to overcome the problems of low hesperetin drug loading and fast oral metabolism in the prior art, and provide a hesperetin emulsion and its Preparation

Method used

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  • Hesperetin emulsion and preparation method thereof
  • Hesperetin emulsion and preparation method thereof
  • Hesperetin emulsion and preparation method thereof

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Embodiment 1

[0041] In the hesperetin emulsion of the present embodiment, every 100mL emulsion contains: hesperetin (structural formula such as figure 1 ) 0.3g, soybean oil 10g, refined egg yolk lecithin 3.0g, sodium oleate 0.03g, glycerin 2.25g, lysine 0.3g, absolute ethanol 1mL, water for injection to 100mL. Wherein the proportion of oil phase is 10%, and the consumption of hesperetin solubilizer is 1.3%.

[0042] The preparation method of the hesperetin emulsion of the present embodiment is:

[0043] 1) Weigh the prescribed amount of refined egg yolk lecithin and add it to the prescribed amount of soybean oil, heat and stir at 60°C to dissolve; weigh the prescribed amount of lysine, dissolve it with absolute ethanol, add it to soybean oil, and heat at 60°C Stir and mix evenly, add hesperetin to the above soybean oil, continue heating and stirring at 60°C to fully dissolve, and use it as the oil phase for later use;

[0044] 2) Concentrate the above oil phase under reduced pressure to re...

Embodiment 2

[0051] In the hesperetin emulsion of the present embodiment, every 100mL emulsion contains: hesperetin (structural formula such as figure 1 ) 1.0g, soybean oil 10g, glyceryl caprate 10g, refined egg yolk lecithin 12.0g, sodium oleate 0.06g, Tween 80 0.5g, glycerin 5.0g, arginine 0.6g, methanol 3.4mL, water for injection Dilute to 100mL. Wherein the proportion of oil phase is 20%, and the consumption of hesperetin solubilizer is 4%.

[0052] The preparation method of the hesperetin emulsion of the present embodiment is:

[0053] 1) Weigh the prescribed quantity of refined egg yolk lecithin and add it to the prescribed quantity of soybean oil and caprylic glyceride, heat and stir at 70°C to dissolve; weigh the prescribed quantity of arginine, dissolve it in methanol, add it to soybean oil and In the caprylic acid glyceride, heat and stir at 70 ° C to mix evenly, add hesperetin to the above soybean oil and caprylic capric acid glycerin, continue heating and stirring at 70 ° C t...

Embodiment 3

[0061] In the hesperetin emulsion of the present embodiment, every 200mL emulsion contains: hesperetin (structural formula such as figure 1 ) 1.0g, soybean oil 10g, olive oil 10g, refined egg yolk lecithin 10.0g, sodium oleate 0.1g, glycerol 5.0g, triethanolamine 0.6g, methanol 4.4mL, water for injection to 200mL. Wherein the proportion of oil phase is 20%, and the consumption of hesperetin solubilizer is 5%.

[0062] The preparation method of the hesperetin emulsion of the present embodiment is:

[0063] 1) Weigh the refined egg yolk lecithin of the prescribed amount and add it to the soybean oil and olive oil of the prescribed amount, heat and stir at 65°C to dissolve; weigh the triethanolamine of the prescribed amount, dissolve it with methanol, and add it to the soybean oil and olive oil, Heat and stir at 65°C and mix evenly, add hesperetin to the above soybean oil and olive oil, continue heating and stirring at 65°C to fully dissolve, and use it as the oil phase for late...

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Abstract

The invention relates to a hesperetin emulsion and a preparation method thereof, and belongs to the technical field of pharmaceutics. The hesperetin emulsion comprises the following components in percentage by mass: 0.3-3% of hesperetin, 10-30% of an oil phase solvent, 3.0-20% of an emulsifier, 0.03-0.6% of a stabilizer and 1-5% of an isoosmotic adjusting agent. The injection emulsion further comprises a pH regulator, a hesperetin solubilizer and the balance of water for injection, the pH value of the injection emulsion is 7.0-8.5, the hesperetin drug loading capacity is greatly improved, and the problem of rapid metabolism due to oral absorption is solved.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, and in particular relates to a hesperetin emulsion and a preparation method thereof. Background technique [0002] Hesperetin is mainly found in the fruits of citrus plants of Rutaceae, and belongs to dihydroflavonoids, with a structural formula such as figure 1 shown. It has been confirmed that hesperetin has a variety of pharmacological activities, including antibacterial, anti-inflammatory, anti-oxidation, anti-virus, anti-allergic, regulating blood lipids and enhancing immunity. In recent years, studies have reported that hesperetin and its derivatives also have anti-Alzheimer's disease, anti-Parkinson's disease, hypoglycemic, anti-snake venom hemocoagulase, anti-fibrosis and other effects. However, hesperetin is easily metabolized in the body, and it is difficult to maintain the blood concentration. Therefore, oral administration or traditional injection administration cannot gua...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/107A61K31/352A61K47/10A61K47/18A61P31/04A61P31/10A61P29/00A61P39/06A61P31/12A61P37/08A61P3/06A61P37/04A61P25/28A61P25/16A61P3/10
CPCA61K9/107A61K9/0019A61K31/352A61K47/10A61K47/183A61K47/18A61P31/04A61P31/10A61P29/00A61P39/06A61P31/12A61P37/08A61P3/06A61P37/04A61P25/28A61P25/16A61P3/10Y02A50/30
Inventor 牛亚伟袁诚许文东唐顺之傅玉萍杨阳彭万才满兴战李遥李继荣牟肖男杨玉琼魏劭恒
Owner GUANGZHOU HANFANG PHARMA
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