Preparation method for idebenone microcapsule through ultrasonic inclusion by beta-cyclodextrin

A technology of idebenone and cyclodextrin, which is applied in the field of preparing microcapsules, can solve problems such as difficult consumer acceptance, affecting product appearance and texture, and limiting the application of IDBN, achieving good hydrophilicity, suitable for promotion, and reducing color Effect

Inactive Publication Date: 2013-08-21
广州保税区雅兰国际化妆品有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] IDBN is insoluble in water, and when dissolved in organic matter, it presents a golden deep orange color. When it is directly added to cosmetics, the product presents a deep orange color, which seriously affects the appearance and texture of the product and is difficult for consumers to accept.
In addition, the insoluble nature of IDBN makes it difficult to directly add to water-based products, which greatly limits the application of IDBN in the cosmetics industry

Method used

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  • Preparation method for idebenone microcapsule through ultrasonic inclusion by beta-cyclodextrin
  • Preparation method for idebenone microcapsule through ultrasonic inclusion by beta-cyclodextrin
  • Preparation method for idebenone microcapsule through ultrasonic inclusion by beta-cyclodextrin

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0105] Dissolve β-CD in distilled water to make a saturated β-CD solution, heat in a water bath to 50°C and stir at a speed of 400 rpm for 30 minutes, add IDBN with a molar ratio of 1:3 to β-CD under constant temperature stirring Continue to stir for 30 minutes, and after ultrasonication at 80W for 20 minutes, place it at 4°C for 24h, filter it under pressure of -0.06MPa, dry it in an oven at 55°C for 12h, and grind the dried solid powder into The fine powder passed through a 80-mesh sieve to obtain β-CD-IDBN inclusion complex microcapsules, the inclusion rate of inclusion complex was 35.20%, the drug content was 14.77%, and the yield was 30.08%.

Embodiment 2

[0107] Dissolve β-CD in distilled water to make a saturated β-CD solution, heat it in a water bath to 60°C and stir at a speed of 500 rpm for 40 minutes, add IDBN with a molar ratio of 1:3 to β-CD under constant temperature stirring Continue to stir for 30 minutes, and after ultrasonication at 80W for 20 minutes, place it at 4°C for 24h, filter it under pressure of -0.06MPa, dry it in an oven at 55°C for 12h, and grind the dried solid powder into The fine powder was passed through an 80-mesh sieve to obtain β-CD-IDBN inclusion compound microcapsules, the inclusion rate of which was 30.60%, the drug content 12.63%, and the yield 26.52%.

Embodiment 3

[0109] Dissolve β-CD in distilled water to make a saturated β-CD solution, heat in a water bath to 60°C and stir at a speed of 400 rpm for 30 minutes, add IDBN with a molar ratio of 1:2 to β-CD under constant temperature stirring Continue to stir for 30 minutes, ultrasonicate at 80W for 20 minutes, place it at 4°C for 24h, filter it with pressure at -0.06MPa, dry it in an oven at 55°C for 12h, and grind the dried solid powder into fine powder, passed through a 80-mesh sieve to obtain β-CD-IDBN inclusion compound microcapsules, the inclusion compound inclusion rate was 25.80%, the drug content was 12.54%, and the yield was 22.53%.

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Abstract

The invention discloses a preparation method for an idebenone microcapsule through ultrasonic inclusion by beta-cyclodextrin. The preparation method comprises the following steps: dissolving beta-cyclodextrin in distilled water to prepare a saturated solution, heating the saturated solution of beta-cyclodextrin to a temperature of 30 to 80 DEG C in a water bath and carrying out isothermal stirring for 15 to 50 min; adding idebenone under the condition of isothermal stirring, continuing stirring to realize uniform mixing so as to obtain a mixed solution and subjecting the mixed solution to ultrasonic inclusion so as to obtain a beta-cyclodextrin-idebenone inclusion solution; and standing the beta-cyclodextrin-idebenone inclusion solution at a temperature of 0 to 8 DEG C for 24 h, carrying out pumping filtration and drying to obtain solid powder, grinding the solid powder into fine powder and carrying out sieving so as to obtain the beta-cyclodextrin-idebenone microcapsule. The preparation method provided by the invention overcomes the problem of water-solubility of idebenone and substantially weakens the inherent color of idebenone, so idebenone is compatible with other components in a formula for a cosmetic without influencing the appearance of the cosmetic, thereby greatly enlarging the application scope of IDBN.

Description

【Technical field】 [0001] The invention relates to a method for preparing microcapsules, in particular to a method for preparing idebenone microcapsules by ultrasonic inclusion of β-cyclodextrin, belonging to the technical field of microencapsulation of bioactive functional substances to change physical properties and appearance . 【Background technique】 [0002] Idebenone (IDBN) chemical name is 6-(10-hydroxydecyl)-2,3-dimethoxy-5-methyl-1,4-benzoquinone, molecular formula is C 19 h 30 o 5 . Idebenone is orange powder crystal, almost insoluble in water, easily soluble in organic solvents such as ethanol and chloroform, with a melting point of 52-55°C. [0003] Idebenone is an organic synthetic drug with great application value. It is similar in structure to coenzyme Q10. It has good antioxidant activity and is a very effective antioxidant. [0004] Idebenone (IDBN) is a derivative of coenzyme CoQ10, the most important biochemical substance in life, and is a kind of effic...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/50A61K31/122A61K47/40A61P39/06
Inventor 朱杰连程传深梁娟陈意平
Owner 广州保税区雅兰国际化妆品有限公司
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