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Paeonol inclusion compound and preparation method thereof

A technology of paeonol and inclusion compound, applied in the field of inclusion compound of paeonol and preparation thereof, can solve the problems of poor taste masking effect, low inclusion rate, poor water solubility and the like, and achieves good taste masking effect, Good stability and increased water solubility

Active Publication Date: 2012-11-21
HUBEI TIANSHENG PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, due to the formation of intramolecular hydrogen bonds between the C-2 and C-3 hydroxyl groups in the β-cyclodextrin molecule, its water solubility is poor (25°C, 1.85g / 100ml), which limits its use in many applications
The currently prepared paeonol inclusion compound still has problems such as poor taste-masking effect, low inclusion rate, instability, and poor water solubility.

Method used

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  • Paeonol inclusion compound and preparation method thereof
  • Paeonol inclusion compound and preparation method thereof
  • Paeonol inclusion compound and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0019] (1) Extraction of Paeonol: Take 1000g of Paeonia Suffruticosa medicinal material, add 15L of purified water to soak for 0.5 hour, and perform steam distillation. Collect 10L of distillate, add 50g of NaCl, stir to dissolve, stand overnight, filter with suction, collect paeonol crystals, dry in a desiccator and weigh to obtain 22g of paeonol.

[0020] (2) Preparation of paeonol inclusion compound: take a 10:1 mixture of β-cyclodextrin and hydroxypropyl β-cyclodextrin and stir to make an inclusion agent. Take 5 times the molar amount of paeonol clathrate, add purified water in a 60℃ constant temperature water bath to make a saturated solution; take paeonol, dissolve it in 8 times 95% ethanol, slowly add it to the clathrate solution, keep constant temperature After stirring for 2 hours, the heating was stopped, and the stirring was continued to room temperature to obtain a white suspension. Put it in a refrigerator for 12 hours, filter with suction, dry the precipitate at 50...

Embodiment 2

[0031] Take the medicinal material of Paeonia suffruticosa, add 10 times the amount of purified water of Paeonia suffruticosa herb to soak for 0.5 hours, then perform steam distillation, collect the distillate of 8 times the amount of the medicinal material, add NaCl, stir to dissolve, stand overnight, suction filter, and collect the peony cortex Phenol crystals are dried and prepared; wherein the mass ratio of the NaCl to the medicinal materials of Paeonia Suffruticosa is 1:10. The prepared paeonol is dissolved in ethanol, and the mass ratio of paeonol to ethanol is 1:5.

[0032] Take the inclusion agent prepared by mixing β-cyclodextrin and hydroxypropyl β-cyclodextrin, add purified water in a 50℃ constant temperature water bath to make a saturated solution; under electric stirring, slowly add the ethanol solution of paeonol , Stir at constant temperature for 1 hour, stop heating, continue to stir to room temperature to obtain a white suspension, put it in the refrigerator for ...

Embodiment 3

[0039] Take the medicinal material of Paeonia suffruticosa, add 15 times the amount of purified water of Paeonia suffruticosa medicinal material for 2 hours, then perform steam distillation, collect the distillate of 10 times the amount of the medicinal material, add NaCl, stir to dissolve, stand overnight, suction filter, and collect the peony cortex Phenol crystals are dried and prepared; wherein the mass ratio of the NaCl to the medicinal materials of Paeonia Suffruticosa is 1:20. The prepared paeonol is dissolved in ethanol, and the mass ratio of paeonol and 90% ethanol is 1:10.

[0040] Take the inclusion agent prepared by mixing β-cyclodextrin and hydroxypropyl β-cyclodextrin, add purified water and make a saturated solution in a constant temperature water bath at 80°C; slowly add paeonol ethanol solution under electric stirring , Stir at constant temperature for 2 hours, stop heating, continue stirring to room temperature to obtain a white suspension, put it in the refrige...

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Abstract

The invention provides a paeonol inclusion compound. A compound agent is a mixture of beta-cyclodextrin and hydroxypropyl beta-cyclodextrin; the molar ratio of the beta-cyclodextrin to the hydroxypropyl beta-cyclodextrin is (10:1)-(1:1); and the molar ratio of paeonol to the compound agent is (1:12)-(1:10). The paeonol inclusion compound has greatly increased water-solubility, good stability, difficulty in separation, and an excellent taste masking effect; and the compound rate can reach to more than 80 percent.

Description

Technical field: [0001] The invention belongs to the field of medicine and relates to an inclusion compound of paeonol and a preparation method thereof. technical background: [0002] Paeonol is the main active ingredient in the whole plant of the skin of Paeonia moutan Sim. and Pycnostelma paniculatum K. Schum. Its chemical formula is 2-hydroxy-4-methoxybenzene. Ethyl ketone, molecular formula is C 9 H 10 O 3 , The relative molecular mass is 166.18. Paeonol is a white or slightly yellow crystal or crystalline powder with a peculiar smell and a slightly spicy taste. It is easily soluble in ethanol and methanol, soluble in hot water, insoluble in cold water, and can be volatilized with water vapor. The melting point is 48℃~51. ℃. Paeonol has a wide range of pharmacological activities. It has analgesic, anti-inflammatory, antipyretic and allergic inhibition, sedative, hypnotic, antibacterial, anti-inflammatory, anti-oxidant, and hypotensive effects. It is clinically used for card...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/12A61K9/06A61K47/40A61K8/35A61K8/73A61P29/00A61P37/08A61P31/04A61P31/12A61P25/20A61P17/00A61Q19/02A61Q11/00A61K47/69
Inventor 谈宗华刘群丁月旭吴统选李达富张聪
Owner HUBEI TIANSHENG PHARMA
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