Pentacyclic triterpenoid cyclodextrin clathrate compound proliposome and preparation method thereof

A technology of cyclodextrin inclusion compound and pentacyclic triterpenoids, which is applied in the field of pentacyclic triterpenoid compound cyclodextrin inclusion compound proliposome and its preparation, and can solve the problem of low encapsulation rate and poor stability and other problems, to achieve the effect of high encapsulation rate, small particle size and convenient use

Active Publication Date: 2013-01-16
西安雅芝生物科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

This patented technology improves how long it takes for certain chemical substances like pentaerythronium bromide (PETB), or other molecules called chromones to penetrate through our skins without causing burning sensations over their entire body. These particles help make them easier to apply onto sensitive areas while also being effective at delivering medicines into deeper layers where we don't want any harmful side effects from traditional methods.

Problems solved by technology

This patented technical problem addressed in this patent relates to reducing harmful chemical reactions that occur when we use certain types of herb extractives (such as beta ester) while also enhancing their activity against wreatherings without causing negative side effects like dryness sensitivity or deteriorated feel caused by excessive swelling during rubbing processes.

Method used

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  • Pentacyclic triterpenoid cyclodextrin clathrate compound proliposome and preparation method thereof
  • Pentacyclic triterpenoid cyclodextrin clathrate compound proliposome and preparation method thereof
  • Pentacyclic triterpenoid cyclodextrin clathrate compound proliposome and preparation method thereof

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Embodiment 1

[0044] Embodiment 1: the preparation of ursolic acid β-cyclodextrin inclusion compound proliposome

[0045] Preparation of ursolic acid β-cyclodextrin inclusion compound: Weigh 3.75g of β-cyclodextrin, add 100ml of distilled water to fully dissolve it, take another 0.50g of ursolic acid, dissolve it with 20ml of 95% ethanol and slowly Add it dropwise to the above aqueous solution of β-cyclodextrin, stir at 30°C for 6 hours, centrifuge the dispersion of the inclusion complex at 70000g for 60 minutes, the supernatant is the aqueous solution of the inclusion compound of ursolic acid β-cyclodextrin. The clear liquid was concentrated in vacuum, and the concentrated liquid was dried in a vacuum oven at 40°C and 0.08 MPa for 6 hours to obtain the inclusion compound of ursolic acid β-cyclodextrin in the form of a white powder, and the inclusion rate reached 82.34% by measurement.

[0046] Determination of ursolic acid content: Determination of ursolic acid by high performance liquid c...

Embodiment 2

[0052] Embodiment 2: Preparation of ursolic acid hydroxypropyl-beta-cyclodextrin inclusion compound proliposome

[0053] Preparation of ursolic acid hydroxypropyl-β-cyclodextrin inclusion complex: Weigh 8.00g of hydroxypropyl-β-cyclodextrin, add 100ml of distilled water to fully dissolve it, and take another ursolic acid 0.38g, Dissolve in 20ml of 95% ethanol and slowly add it dropwise to the above β-cyclodextrin aqueous solution, stir at 20°C for 3 hours, centrifuge the dispersion of inclusion complex at 70000g for 60 minutes, the supernatant is ursolic acid hydroxypropyl-β -Aqueous solution of cyclodextrin inclusion complex, the supernatant is concentrated in vacuum, and the concentrated solution is dried in a vacuum oven at 40°C and 0.08MPa for 6 hours to obtain ursolic acid hydroxypropyl-β-cyclodextrin inclusion compound in the form of white powder The inclusion rate was determined to reach 79.08%.

[0054] 20.00g of hydrogenated soybean lecithin and 5.50g of cholesterol ...

Embodiment 3

[0056] Example 3: Preparation of oleanolic acid β-cyclodextrin inclusion complex proliposome

[0057] Preparation of oleanolic acid β-cyclodextrin inclusion compound: Weigh 4.80g of β-cyclodextrin, add 100ml of distilled water to fully dissolve it, take another 0.70g of oleanolic acid, and dissolve it in 20ml of 95% ethanol Then slowly add it dropwise to the above-mentioned β-cyclodextrin aqueous solution, stir at 60°C for 4 hours, then centrifuge the dispersion of the clathrate at 70000g for 60min, the supernatant is the aqueous solution of the ursolic acid β-cyclodextrin clathrate, The supernatant was concentrated in vacuum, and the concentrated solution was dried in a vacuum drying oven at 40°C and 0.08 MPa for 6 hours to obtain the inclusion compound of ursolic acid β-cyclodextrin in the form of white powder, and the inclusion rate reached 86.27% by measurement.

[0058] Determination of oleanolic acid content: Determination of ursolic acid by high performance liquid chrom...

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Abstract

The invention discloses pentacyclic triterpenoid cyclodextrin clathrate compound proliposome and a preparation method thereof. The main component comprises one or more of pentacyclic triterpenoid compound series, for example, ursolic acid, oleanolic acid, betulonic acid, beta-masticinic acid, cyclodextrin clathrate compound, phospholipid material and cholesterol. According to the pentacyclic triterpenoid cyclodextrin clathrate compound proliposome, the pentacyclic triterpenoid compound is clathrated through cyclodextrin to improve the hydrophilicity; the liposome is used as a carrier to clad, and the proliposome is obtained by freezing and drying. According to the pentacyclic triterpenoid cyclodextrin clathrate compound proliposome, the bioavailability and the stability of the pentacyclic triterpenoid compound can be improved; transdermal absorption is promoted, and the skin irritation is reduced. In addition, the cyclodextrin clathrate compound proliposome is of a powder shape, good in stability and rehydration reconstruction and convenient to use, and can be applied to a plurality of cosmetic dosage forms such as cream, emulsion, gel and essence.

Description

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Claims

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Application Information

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Owner 西安雅芝生物科技有限公司
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