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Compound fisetin microemulsion gel as well as preparation method and application thereof

A technology of compound fisetin and microemulsion gel, which is applied in the direction of non-active ingredient medical preparations, pharmaceutical formulas, emulsion delivery, etc., can solve problems such as instability and poor solubility, achieve good stability, increase viscosity Adhesion, enhancing the effect of drug transdermal ability

Pending Publication Date: 2020-04-17
中山大学新华学院
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the volatile oils of traditional Chinese medicines such as litsea cubeba oil have poor solubility and are unstable.

Method used

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  • Compound fisetin microemulsion gel as well as preparation method and application thereof
  • Compound fisetin microemulsion gel as well as preparation method and application thereof
  • Compound fisetin microemulsion gel as well as preparation method and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0052] Example 1 Screening of compound fisetin microemulsion formula

[0053] 1. Screening of oil phase, surfactant and co-surfactant

[0054] 1. Experimental method

[0055] Take 0.5g of fisetin and add 5mL of oil phase, surfactant and co-surfactant respectively, stir magnetically evenly at room temperature, dissolve by ultrasonic (100Hz, 30min), vortex mix, and put into constant temperature shaker (37℃, 72h) Then centrifuge (5000Hz, 30min), get supernatant and filter, place in sample tube, add mobile phase methanol to dilute, filter, measure according to above-mentioned chromatographic conditions;

[0056] Wherein, the oil phase is selected from the group consisting of: ethyl oleate (EO): Radix japonica oil, medium chain triglyceride (MCT): Radix japonica oil, isopropyl myristate (IPM): Radix japonica oil;

[0057] The surfactant is selected from: Tween-80 (TW-80), Span-80 (SP-80), Poloxamer 188, Poloxamer 407, polyethylene glycol 15-hydroxystearate ( HS-15), hydrogenated...

Embodiment 2

[0070] Example 2 Star point design-response surface method to optimize the formula of compound fisetin microemulsion

[0071] 1. Experimental method

[0072] According to the pseudo-ternary diagram results obtained in Example 1, determine the relationship between the oil phase (MCT: Radix chinensis oil (9:1)), the mixed surfactant (HS-15: isopropanol=2:1) ​​and the water phase For the maximum and minimum values, a two-factor five-level star point design-effect surface was used, and an expert design CCD was used to design a two-factor five-level experiment. The two-factor five-level water meter is shown in Table 2.

[0073] According to the experimental design in Table 2, MCT was accurately weighed: Radix japonica oil (9:1), HS-15, isopropanol, and then water was added to prepare microemulsions of different proportions, 0.19 g of fisetin was added, and magnetic stirring was carried out at room temperature. Uniform, ultrasonic (100Hz, 30min) to dissolve, vortex to mix, put into...

Embodiment 3

[0090] Example 3 Screening of compound fisetin microemulsion gel prescription

[0091] 1. Screening of Compound Fisetin Microemulsion Gel Matrix

[0092] 1. Experimental method

[0093] Weigh 5g each of Carbomer 940 gel base and Carbomer 941 gel base, add 5g of compound fisetin microemulsion respectively to make 10g of compound fisetin microemulsion gel, stir evenly, adjust pH with triethanolamine 6 to 7.

[0094] 2. Experimental results

[0095] The screening results of the compound fisetin microemulsion gel matrix types are shown in Table 5. It can be seen that when the compound fisetin microemulsion gel matrix is ​​carbomer 941, the appearance of the compound fisetin microemulsion gel It is a yellow gel-like liquid with good viscosity and spreadability. Therefore, carbomer 941 is preferably a compound fisetin microemulsion gel matrix.

[0096] Table 5 Screening results of compound fisetin microemulsion gel matrix types

[0097]

[0098] 2. Screening of compound fise...

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Abstract

The invention discloses compound fisetin microemulsion gel as well as a preparation method and application thereof. The invention provides compound fisetin microemulsion gel comprising fisetin, a compound fisetin microemulsion and a compound fisetin microemulsion gel matrix. The mass ratio of the fisetin to the compound fisetin microemulsion to the compound fisetin microemulsion gel matrix is (2.25-2.7): (50-60): (40-50). According to the invention, natural extracts of fisetin and litsea cubeba oil are used in a compatible manner and the compound fisetin microemulsion gel prepared by combiningthe microemulsion gel preparation technology can synergistically exert the biological activity of fisetin and litsea cubeba oil. The compound fisetin microemulsion gel is non-irritant to skin and mucous membranes and good in stability and has the remarkable effects of inhibiting skin oxidative damage and cell apoptosis and inhibiting melanin formation. Moreover, the preparation process of the microemulsion gel is simple, and the use is convenient. Thereofre, the fisetin microemulsion gel has the broad application prospects in preparation of skin care products with whitening, anti-aging and freckle-removing effects.

Description

technical field [0001] The invention belongs to the technical field of microemulsion gel preparation. More specifically, it relates to a compound fisetin microemulsion gel and its preparation method and application. Background technique [0002] Whitening, freckle removal and anti-aging is a topic that people have been paying close attention to for a long time. People hope to use functional skin care products to reduce pigmentation such as melasma and age spots, and make the skin fair and smooth. Therefore, in order to meet people's pursuit of beauty, the market of skin-whitening, freckle-removing and anti-aging skin care products is becoming increasingly active, and product sales are increasing day by day. With the improvement of people's living standards, higher and higher requirements are put forward for the quality and performance of skin care products. However, in order to highlight the rapid whitening effect of products, manufacturers illegally use mercury, glucocorti...

Claims

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Application Information

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IPC IPC(8): A61K8/49A61K8/92A61K8/37A61K8/86A61K8/34A61K8/81A61K8/04A61K8/06A61Q19/02A61Q19/08A61K31/352A61K36/54A61K9/06A61K9/107A61K47/14A61K47/26A61K47/10A61K47/32A61P17/00A61P17/18
CPCA61K8/498A61K8/922A61K8/37A61K8/86A61K8/4993A61K8/34A61K8/345A61K8/8147A61K8/042A61K8/068A61Q19/02A61Q19/08A61K31/352A61K36/54A61K9/06A61K9/1075A61K9/0014A61K47/14A61K47/26A61K47/10A61K47/32A61P17/00A61P17/18A61K2800/782A61K2800/592A61K2300/00
Inventor 张素中罗兰刘盈陈锐娥姚小丽蔡安妮李慧瑜吴嘉琳钟丽娟
Owner 中山大学新华学院
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