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Emulsion containing dicaffeoyl quinic acid and its preparing method

A technology of caffeoylquinic acid and emulsion, which is applied in the field of medicine and can solve the problems of inconvenience and inconvenience for patients

Inactive Publication Date: 2005-05-18
INST OF RADIATION MEDICINE ACAD OF MILITARY MEDICAL SCI OF THE PLA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Ordinary tablets or other solid preparations are taken by taking a large amount of solid preparations (such as tablets or capsules) with an appropriate amount of water every day, which not only brings some inconvenience to ordinary patients, but also brings inconvenience to children, the elderly and patients with dysphagia. great inconvenience

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 2

[0036] Embodiment 2. Two of dicaffeoylquinic acid emulsion

[0037] 3,5-Di-O-caffeoylquinic acid 1g

[0038] Poloxamer P188 1.8g

[0039] Propylene Glycol 8ml

[0040] Vitamin C 0.1g

[0041] water 50ml

[0042] Take 3,5-di-O-caffeoylquinic acid, poloxamer P188 and propylene glycol, heat to dissolve, and slowly drop into the stirred aqueous solution containing vitamin C to obtain an emulsion. The emulsion is circulated and emulsified by a homogenizer for 3 times to obtain an emulsion with an emulsion droplet size less than 1 micron. The emulsion was sealed in an ampoule and heated at 100°C for 30 minutes. Sampling and observation showed that the particle size of most emulsion droplets was less than 5 microns. The emulsion is stable for a long time at room temperature. The emulsion can be used intravenously, intramuscularly, or orally.

Embodiment 3

[0043] Embodiment 3. The third of dicaffeoylquinic acid emulsion

[0044] 1,5-Di-O-caffeoylquinic acid 1g

[0045] Tween 80 4g

[0046] Macrogol 400 10ml

[0047] Vitamin C 0.1g

[0048] Sorbic acid 0.05g

[0049] Aspartame 0.1g

[0050] water 50ml

[0051] Take 1,5-di-O-caffeoylquinic acid, Tween 80 and polyethylene glycol 400, heat to dissolve, slowly drop into the stirred aqueous solution containing vitamin C, sorbic acid and aspartame to obtain Homogeneous emulsion. The particle size range of the emulsion droplets in the emulsion is mostly less than 5 microns. The emulsion remained stable after standing at room temperature for a long time. This emulsion can be used orally.

Embodiment 4

[0052] Embodiment 4. The fourth of dicaffeoylquinic acid emulsion

[0053] 1,5-Di-O-caffeoylquinic acid 1g

[0054] Tween 80 4g

[0055] Ethanol 10ml

[0056] Vitamin C 0.5g

[0057] Stevioside 0.2g

[0058] Benzoic acid 0.02g

[0059] water 50ml

[0060] Take 1,5-di-O-caffeoylquinic acid, Tween 80, and ethanol, ultrasonically dissolve them completely, and slowly drop the solution into the stirred aqueous solution containing vitamin C, stevioside, and benzoic acid to obtain a uniform emulsion. The emulsion was evaporated under reduced pressure on a rotary evaporator to evaporate almost all the ethanol. The particle size range of the emulsion droplets in the emulsion is mostly less than 5 microns. The emulsion remained stable after standing at room temperature for a long time. This emulsion can be used orally.

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Abstract

The present invention discloses emulsion containing dicaffeoyl quinic acid and its preparation process. The emulsion has high stability and small particle size, and may be used in intravenous injection, intramuscular injection or oral taking. The emulsion may be obtained directly via dispersing the organic solution of dicaffeoyl quinic acid and emulsifier directly into water phase component.

Description

technical field [0001] The invention relates to the field of medicine, in particular to an emulsion containing dicaffeoylquinic acid and a preparation method thereof. Background technique [0002] Dicaffeoylquinic acid (DCQA), also known as dicaffeoylquinic acid. It is the dicaffeic acid ester of quinic acid, depending on the caffeoyl substitution position, there can be 1,5-di-O-caffeoylquinic acid, 1,3-di-O-caffeoylquinic acid, 1, 4-di-O-caffeoylquinic acid, 3,5-di-O-caffeoylquinic acid, 3,4-di-O-caffeoylquinic acid, 4,5-di-O-caffeoylquinic acid Quinic acid, among which 1,5-di-O-caffeoylquinic acid has been reported more. The chemical name of 1,5-di-O-caffeoylquinic acid is (1s,1α,3β,4α,5α)1,3-bis[[3-(3,4-dihydroxyphenyl)-1- Oxo-2-propenyl]oxy]4,5-dihydroxy-cyclohexane acid, formula C 25 h 24 o 12 . As a pharmacological active ingredient, dicaffeoylquinic acid has a wide range of actions, and has antiviral (CN1087608; EP1008344; US6331565; US20020111382), antioxidant...

Claims

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Application Information

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IPC IPC(8): A61K9/107A61K31/216A61P1/16A61P31/12
Inventor 金义光李淼董俊兴
Owner INST OF RADIATION MEDICINE ACAD OF MILITARY MEDICAL SCI OF THE PLA
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