Resveratrol-sulfobutyl ether-beta-cyclodextrin inclusion compound and preparing method thereof

A technology of cyclodextrin inclusion compound and resveratrol, which is applied in the direction of active ingredients of hydroxyl compounds, drug combinations, pharmaceutical formulations, etc., can solve the problem of resveratrol’s instability to light and heat, insignificant increase in water solubility, Problems such as low bioavailability, to achieve the effect of improving water solubility and stability, satisfactory inclusion rate, and low adverse reactions

Inactive Publication Date: 2016-08-31
CHONGQING MEDICAL UNIVERSITY
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Problems solved by technology

[0008] In view of this, the technical problem to be solved by the present invention is that resveratrol is unstable to light, heat, etc., has little water solubility, and low bioavailability, while existing β-CD and other β-CD derivatives have no effect on resveratrol. Inclusion and inclusion rate is not high, water solubility increase is not obvious, providing a resveratrol-SBE-β-CD inclusion compound and its preparation method

Method used

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  • Resveratrol-sulfobutyl ether-beta-cyclodextrin inclusion compound and preparing method thereof
  • Resveratrol-sulfobutyl ether-beta-cyclodextrin inclusion compound and preparing method thereof
  • Resveratrol-sulfobutyl ether-beta-cyclodextrin inclusion compound and preparing method thereof

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Embodiment

[0035] 1. Determination method of inclusion rate

[0036] 1.1 Chromatographic conditions

[0037] Chromatographic column: Agilent Eclipse XDB-C18 column (4.6mm×250mm, 5um); mobile phase: methanol-water (55:45); flow rate: 1.0mL / min; column temperature: 30°C; injection volume: 10μL; detection Wavelength: 307nm.

[0038] 1.2 Standard curve

[0039] Precisely weigh 10 mg of the resveratrol reference substance, dilute it to a 10 mL brown volumetric flask with methanol, and prepare a stock solution with a concentration of 1 mg / mL; draw up 20, 30, 40, 50, 60 and 70 μL of the stock solution precisely, and use Dilute methanol to 10mL and shake well. Filter with a 0.45um microporous membrane. Draw 10 μL into the liquid chromatograph respectively. Take the chromatographic peak area A as the ordinate, and the resveratrol concentration C as the abscissa to draw a standard curve to obtain the regression equation A=85086C+8933.6, R 2 =09993, n=6. It can be seen that the resveratrol c...

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Abstract

The invention discloses a resveratrol-sulfobutyl ether-beta-cyclodextrin inclusion compound and a preparing method thereof. In the resveratrol-sulfobutyl ether-beta-cyclodextrin inclusion compound, the molar ratio of resveratrol to sulfobutyl ether-beta-cyclodextrin is 1:2. The resveratrol-SBE-beta-CD inclusion compound belongs to a new dosage form. By using the SBE-beta-CD as an auxiliary material, water solubility and stability of resveratrol are improved, and the application range is broadened. Beta-CD or hydroxypropyl-beta-CD is adopted in the prior art mostly, by comparison, as SBE-beta-CD is adopted as the auxiliary material, all the properties of the inclusion compound are remarkably improved, the inclusion compound has better water solubility and a higher inclusion rate, the side effect is small, and adverse reactions such as renal toxicity and hemolysis can be reduced to the lowest degree. By means of the method, the satisfied inclusion rate can be obtained, the problem that resveratrol can not be dissolved into water easily and is poor in stability is solved, and the method can be applied to production and clinical needs.

Description

technical field [0001] The invention belongs to the technical field of traditional Chinese medicine preparations, and in particular relates to a resveratrol-sulfobutyl ether-beta-cyclodextrin inclusion compound and a preparation method thereof. Background technique [0002] In recent years, the application of active ingredients of traditional Chinese medicine in the anticancer effect has attracted widespread attention, making the research on the anticancer effect of active ingredients of traditional Chinese medicine a hot spot. Relevant experts believe that there will be a broad market for health care medicines that prevent heart and cerebrovascular diseases, cancer, arteriosclerosis, and delay aging. And resveratrol is the natural chemopreventive agent of this heart, cerebrovascular disease and cancer. Resveratrol has a variety of pharmacological activities, such as antibacterial, anti-oxidation, heart disease prevention, anti-cancer, anti-platelet aggregation, liver prote...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/48A61K31/05A61K9/19A61P35/00
CPCA61K9/19A61K31/05
Inventor 尚京川王靖雯李晶文瑶
Owner CHONGQING MEDICAL UNIVERSITY
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