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Inclusion compound of helicid and beta-cyclodextrin and derivatives thereof and preparation method of inclusion compound

A technology of cyclodextrin inclusion complex and tofufuside is applied in the directions of drug combination, medical preparations without active ingredients, and medical preparations containing active ingredients, which can solve the problem of low bioavailability, weak action strength, The problem of slow effect and other problems is achieved, and the effect of the preparation method is simple and easy to implement.

Inactive Publication Date: 2016-05-25
YUNNAN MINZU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

At the same time, it has a good improvement and regulation effect on memory and thinking power, and has broad application prospects. Its disadvantages are small solubility, large dosage, weak action intensity, slow onset, and low bioavailability

Method used

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  • Inclusion compound of helicid and beta-cyclodextrin and derivatives thereof and preparation method of inclusion compound
  • Inclusion compound of helicid and beta-cyclodextrin and derivatives thereof and preparation method of inclusion compound
  • Inclusion compound of helicid and beta-cyclodextrin and derivatives thereof and preparation method of inclusion compound

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preparation example Construction

[0037] Such as figure 1 : a preparation method of the inclusion compound of tofu glucoside and β-cyclodextrin and its derivatives, the preparation method of the inclusion compound of the tofu glucoside and β-cyclodextrin and its derivatives comprises the following steps:

[0038] S101: Dissolve tofu glucoside in a small amount of methanol at room temperature, stir for 1 hour, wait until the sample is completely dissolved, then add β-cyclodextrin and its derivatives, store in the dark, and continue stirring for 10 days;

[0039] S102: After evaporating methanol at 60°C, remove unreacted tofu glucoside by filtration, evaporate the filtrate to dryness to obtain a white solid powder, and dry it in vacuum to obtain tofu glucoside / β-cyclodextrin and its derivatives clathrate.

[0040] An inclusion compound of tofu glucoside and β-cyclodextrin and its derivatives, the inclusion compound of tofu glucoside and β-cyclodextrin and its derivatives includes tofu glucoside / β-cyclodextrin i...

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Abstract

The invention discloses an inclusion compound of helicid and beta-cyclodextrin and derivatives thereof and a preparation method of the inclusion compound. The method includes: dissolving the helicid into a small amount of methanol at the room temperature, stirring for dissolving, adding the beta-cyclodextrin and the derivatives thereof, storing under a light shading condition, and stirring continuously; evaporating for removing the methanol, filtering for removing unreacted helicid, evaporating to dry filtrate to obtain white solid powder, and performing vacuum drying to obtain the inclusion compound of the helicid and the beta-cyclodextrin and the derivatives thereof. After absorbance of the filtrate is measured at 270nm, amounts of the helicid in HEL / beta-CD and HEL / HP-beta-CD inclusion compound are 12.66mg / mL and 14.22mg / mL respectively according to standard curve quantitation of the helicid. Compared with solubility of blank helicid, solubility of the helicid subjected to cyclodextrin inclusion is increased by 2.0-2.3 times.

Description

technical field [0001] The invention belongs to the field of supramolecular inclusion technology and the technical field of preparation of water-soluble drugs, and in particular relates to an inclusion compound of tofu glucoside, β-cyclodextrin and derivatives thereof and a preparation method thereof. Background technique [0002] Tofu fruit glycosides (English name, Helicid, molecular formula, C 19 h 18 o 11 , chemical name, 4-formylphenyl-β-D-alopyranoside, referred to as HEL), also known as Shenshuiguo element, is from the fruit of the radish tree (English name, Heliciaessatica Hook) of Yunnan Longanaceae plant (English name, Heliciaessatica Hook). The active ingredient extracted is a monomeric glycoside, which can restore the imbalance between the excitation and inhibition processes of the cerebral cortex. Pharmacological and clinical studies have found that it has biological activities such as hypnosis, pain relief, sedation, anticonvulsant, and antidepression, and h...

Claims

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Application Information

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IPC IPC(8): A61K47/48A61K31/7034A61P25/20A61P29/00
CPCA61K31/7034
Inventor 杨丽娟赵雪秋杨丽周树娅黄超
Owner YUNNAN MINZU UNIV