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Arbutin/hydroxypropyl-beta-cyclodextrin inclusion compound and preparation method thereof

A cyclodextrin inclusion complex, hydroxypropyl technology, applied in the chemical field, can solve the problems of skin irritation, allergic reaction, poor water solubility and stability of arbutin, improve thermal stability, widen the scope of application, The effect of improving water solubility and thermal stability

Active Publication Date: 2015-05-20
WUHAN POLYTECHNIC UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Among them, although hydroquinone has a strong inhibitory effect on the formation of melanin, it is irritating to the skin and can cause allergic reactions; at the same time, hydroquinone is easily oxidized when exposed to light, producing reddish-brown substances , which produces tan spots on the surface of the skin
Due to the poor water solubility and stability of arbutin, the application of arbutin in the field of cosmetics is limited.

Method used

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  • Arbutin/hydroxypropyl-beta-cyclodextrin inclusion compound and preparation method thereof
  • Arbutin/hydroxypropyl-beta-cyclodextrin inclusion compound and preparation method thereof
  • Arbutin/hydroxypropyl-beta-cyclodextrin inclusion compound and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] A preparation method of arbutin / hydroxypropyl-β-cyclodextrin inclusion compound, which comprises the following steps:

[0033] (1) Weigh 2.920g (2mmol) of hydroxypropyl-β-cyclodextrin (HP-β-CD) and dissolve it in 100mL of distilled water to prepare a 0.02mol / L hydroxypropyl-β-cyclodextrin solution;

[0034] (2) According to the ratio of the amount of hydroxypropyl-β-cyclodextrin to arbutin as 2:1, weigh 0.272g (1mmol) of arbutin;

[0035] (3) Add the arbutin weighed in step (2) to the hydroxypropyl-β-cyclodextrin solution prepared in step (1) and mix to prepare a mixed solution A;

[0036] (4) Place the mixed solution A in step (3) in a sealed Erlenmeyer flask and shake in a 60°C water bath for 24 hours to obtain a clear solution B;

[0037] (5) Pour the clear solution B in step (4) into a fresh-keeping box and freeze-dry to obtain a white solid, which is an arbutin / hydroxypropyl-β-cyclodextrin inclusion compound.

Embodiment 2

[0039] A preparation method of arbutin / hydroxypropyl-β-cyclodextrin inclusion compound, which comprises the following steps:

[0040] (1) Weigh 2.920g (2mmol) of hydroxypropyl-β-cyclodextrin (HP-β-CD) and dissolve it in 100mL of distilled water to prepare a 0.02mol / L hydroxypropyl-β-cyclodextrin solution;

[0041] (2) According to the ratio of the amount of hydroxypropyl-β-cyclodextrin to arbutin as 1:1, weigh 0.554g (2mmol) of arbutin;

[0042] (3) Add the arbutin weighed in step (2) to the hydroxypropyl-β-cyclodextrin solution prepared in step (1) and mix to prepare a mixed solution A;

[0043] (4) Place the mixed solution A in step (3) in a sealed Erlenmeyer flask and shake in a 60°C water bath for 24 hours to obtain a clear solution B;

[0044] (5) Pour the clear solution B in step (4) into a fresh-keeping box and freeze-dry to obtain a white solid, which is an arbutin / hydroxypropyl-β-cyclodextrin inclusion compound.

Embodiment 3

[0046] A preparation method of arbutin / hydroxypropyl-β-cyclodextrin inclusion compound, which comprises the following steps:

[0047] (1) Weigh 2.920g (2mmol) of hydroxypropyl-β-cyclodextrin (HP-β-CD) and dissolve it in 100mL of distilled water to prepare a 0.02mol / L hydroxypropyl-β-cyclodextrin solution;

[0048] (2) According to the ratio of the amount of hydroxypropyl-β-cyclodextrin to arbutin as 2:3, weigh 0.816g (3mmol) of arbutin;

[0049] (3) Add the arbutin weighed in step (2) to the hydroxypropyl-β-cyclodextrin solution prepared in step (1) and mix to prepare a mixed solution A;

[0050] (4) Place the mixed solution A in step (3) in a sealed Erlenmeyer flask and shake in a 60°C water bath for 24 hours to obtain a clear solution B;

[0051] (5) Pour the clear solution B in step (4) into a fresh-keeping box and freeze-dry to obtain a white solid, which is an arbutin / hydroxypropyl-β-cyclodextrin inclusion compound.

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Abstract

The invention discloses an arbutin / hydroxypropyl-beta-cyclodextrin inclusion compound and a preparation method thereof. The arbutin / hydroxypropyl-beta-cyclodextrin inclusion compound is prepared by inclusion of hydroxypropyl-beta-cyclodextrin and arbutin at the mass ratio of (2:1) to (2:3). According to the arbutin / hydroxypropyl-beta-cyclodextrin inclusion compound prepared by the method disclosed by the invention, the phase of the arbutin is greatly changed; the arbutin exists in the inclusion compound in an amorphous state, and is completely dispersed into the hydroxypropyl-beta-cyclodextrin; the water solubility of the arbutin is increased; the arbutin is combined with the hydroxypropyl-beta-cyclodextrin in the inclusion process in a non-covalent bond form; and the heat stability of the arbutin is significantly improved, so that the application range of the arbutin in cosmetics industry is expanded.

Description

Technical field [0001] The invention relates to the technology of the chemical industry, in particular to an arbutin / hydroxypropyl-β-cyclodextrin inclusion compound and a preparation method thereof. Background technique [0002] Arbutin (Arb), also known as arbutin, arbutin, arbutin, its chemical name is p-hydroxyphenyl-β-D-glucopyranoside. It is originally derived from natural green plants and has anti-inflammatory, antibacterial, antitussive, expectorant and antiasthmatic effects. It is widely used in clinical practice and is also a natural whitening active substance. Drugs containing arbutin are often used to treat tracheitis, infectious urinary system diseases, skin diseases, allergies and inflammatory diseases. At the same time, it can quickly penetrate into the skin, without affecting the proliferation concentration of skin cells, effectively inhibiting the activity of tyrosinase in the skin, blocking the formation of melanin, and accelerating the production of melanin thr...

Claims

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Application Information

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IPC IPC(8): A61K8/60A61K8/73A61K8/02A61Q19/02A61Q19/00
Inventor 沈汪洋孙威李芳陈轩
Owner WUHAN POLYTECHNIC UNIVERSITY
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