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Paeonol inclusion compound and preparation method thereof

A technology of paeonol and clathrate, applied in the field of paeonol clathrate and its preparation, can solve the problems of poor taste-masking effect, low clathrate rate, poor water solubility, etc., and achieve good taste-masking effect, Good stability and increased water solubility

Active Publication Date: 2014-04-16
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 1000 g of Moutan cortex medicinal material, add 15 L of purified water to infiltrate for 0.5 hour, and then carry out steam distillation. Collect 10L of distillate, add 50g of NaCl and 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 evenly to prepare the inclusion compound. Take paeonol 5 times the molar amount of clathrate agent, add purified water to make a saturated solution in a constant temperature water bath at 60°C; take paeonol, dissolve it in 8 times 95% ethanol, slowly add it to the clathrate solution, and keep the temperature constant After stirring for 2 hours, the heating was stopped, and the stirring was continued to room temperature to obtain a white suspension. Refrigerate in the refrigerator for 12 ...

Embodiment 2

[0031] Take the Moutan Cortex medicinal material, add 10 times the amount of purified water of the Moutan Cortex medicinal material to infiltrate for 0.5 hours, conduct steam distillation, collect 8 times the amount of the medicinal material distillate, add NaCl, stir to dissolve, stand overnight, suction filter, and collect the paeonol cortex Phenol crystals are obtained by drying; wherein, the mass ratio of NaCl to Cortex Moutan is 1:10. The prepared paeonol is dissolved in ethanol, and the mass ratio of paeonol and ethanol is 1:5.

[0032] Take the inclusion agent prepared by mixing β-cyclodextrin and hydroxypropyl β-cyclodextrin, add purified water to make a saturated solution in a constant temperature water bath at 50°C; slowly add the ethanol solution of paeonol under electric stirring , stirred at constant temperature for 1 hour, stopped heating, and continued to stir to room temperature to obtain a white suspension, which was stored in the refrigerator for 10 hours, su...

Embodiment 3

[0039]Take the Moutan Cortex medicinal material, add 15 times the amount of purified water of the Moutan Cortex medicinal material, soak for 2 hours, perform steam distillation, collect 10 times the medicinal material distillate, add NaCl, stir to dissolve, stand overnight, suction filter, and collect the paeonol cortex Phenol crystals are obtained by drying; wherein, the mass ratio of NaCl to Cortex Moutan is 1:20. The prepared paeonol was dissolved in ethanol, and the mass ratio of paeonol to 90% ethanol was 1:10.

[0040] Take the inclusion agent prepared by mixing β-cyclodextrin and hydroxypropyl β-cyclodextrin, add purified water to make a saturated solution in a constant temperature water bath at 80°C; slowly add the ethanol solution of paeonol under electric stirring , stirred at constant temperature for 2 hours, stopped heating, and continued to stir to room temperature to obtain a white suspension, put it in the refrigerator for 15 hours, filter with suction, dry the ...

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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 bark of Paeonia moutan Sim. and the whole plant of Pycnostelma paniculatum K. Schum. Its chemical formula is 2-hydroxy-4-methoxybenzene Ethyl ketone, the molecular formula is C 9 h 10 o 3 , the relative molecular mass is 166.18. Paeonol is white or light yellow crystal or crystalline powder, with specific odor, slightly spicy taste, easily soluble in ethanol and methanol, soluble in hot water, insoluble in cold water, can volatilize with water vapor, melting point 48 ℃ ~ 51 ℃. Paeonol has a wide range of pharmacological activities, and has analgesic, anti-inflammatory, antipyretic and anti-allergic effects, sedative, hypnotic, antibacterial, anti-inflammatory, anti-oxidant, and blood pressure-lowering effects. Immune system and other diseases;...

Claims

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Application Information

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Patent Type & Authority Patents(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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