Alizarin liposome and preparation method thereof

A technology of alizarin lipid and alizarin, which is applied in the field of alizarin liposome and its preparation, can solve the problems of short half-life in vivo, low bioavailability, cardiotoxicity and the like

Inactive Publication Date: 2018-01-19
HENAN SOAR VETERINARY PHARMA +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, since rubidin is insoluble in water, its absorption is incomplete, its bioavailability is low, and its half-life in vivo is short. In addition, it has certain toxicity to the heart.

Method used

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  • Alizarin liposome and preparation method thereof

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Experimental program
Comparison scheme
Effect test

Embodiment 1

[0020] A preparation method of rubidin liposome, the steps are as follows:

[0021] (1) In terms of mass ratio, weigh 10 mg of madderin and 350 mg of PEG-modified lipid derivative, the PEG-modified lipid derivative is PEG2000-distearoylphosphatidylethanolamine;

[0022] (2) Preparation of blank liposome suspension by injection method: Dissolve PEG-modified lipid derivatives in absolute ethanol to make a lipid solution, absorb the lipid solution and inject slowly into 5mL pH=4, concentration 300mmol / In the citrate-citrate sodium buffer solution (hydration medium) of L, continue stirring to remove ethanol after injecting, and obtain blank liposome suspension after ultrasonic dispersion;

[0023] (3) Ultrasonically disperse rubikin in 5mL of absolute ethanol to prepare rubikin ethanol dispersion;

[0024] (4), mixing the blank liposome suspension obtained in step (2) and the ethanol dispersion of rubidin obtained in step (3), supercritical CO at 50°C and 8Mpa 2 After 5 minutes...

Embodiment 2

[0026] A preparation method of rubidin liposome, the steps are as follows:

[0027] (1) In terms of mass ratio, weigh 10 mg of madderin and 300 mg of PEG-modified lipid derivative, the PEG-modified lipid derivative is PEG2000-distearoylphosphatidylethanolamine;

[0028] (2) Preparation of blank liposome suspension by reverse evaporation method: dissolve PEG-modified lipid derivatives in absolute ethanol to make a lipid solution, then add 5 mL of citrate with pH=2.7 and a concentration of 200 mmol / L In the acid-citrate sodium buffer solution (hydration medium), high-speed shearing makes it form stable W / O colostrum, and then evaporates the organic solvent under reduced pressure to obtain a blank liposome suspension;

[0029] (3) Ultrasonically disperse rubikin in 3.33mL absolute ethanol to prepare rubikin ethanol dispersion;

[0030] (4), mixing the blank liposome suspension obtained in step (2) and the ethanol dispersion of rubidin obtained in step (3), supercritical CO at 55...

Embodiment 3

[0032] A preparation method of rubidin liposome, the steps are as follows:

[0033] (1) In terms of mass ratio, weigh 10 mg of madderin and 400 mg of PEG-modified lipid derivative, the PEG-modified lipid derivative is PEG5000-distearoylphosphatidylglycerol;

[0034] (2) Preparation of blank liposome suspension by spray drying method: dissolve PEG-modified lipid derivatives in absolute ethanol to make a lipid solution, spray dry the lipid solution to obtain a lipid powder, and use 6 mL pH = 5.2, citrate-citrate sodium buffer solution (hydration medium) with a concentration of 400mmol / L hydrates the lipid powder to prepare a blank liposome suspension;

[0035] (3) Ultrasonically disperse rubikin in 4mL of absolute ethanol to prepare rubikin ethanol dispersion;

[0036] (4), mixing the blank liposome suspension obtained in step (2) and the ethanol dispersion of rubidin obtained in step (3), supercritical CO at 50°C and 10Mpa 2 After 3 minutes of treatment, the rubiacin liposome...

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Abstract

The invention belongs to the field of veterinary medicines, and specifically discloses an alizarin liposome and a preparation method thereof. The preparation method comprises the following steps: weighing alizarin and a PEG (Polyethylene Glycol) modified lipid derivative which are 1 to (30 to 40) in mass ratio, wherein the PEG modified lipid derivative is PEG-distearoyl phosphatidyl ethanolamine or PEG-distearoyl phosphatidyl glycerol; adding ethanol in the PEG modified lipid derivative for dissolving, and preparing a blank liposome suspension solution in which the final concentration of the PEG modified liposome derivative is 50 to 100 mg/mL by taking a citric acid-sodium citrate buffer solution of which the pH (Potential of Hydrogen) is 2.7 to 5.2 and the concentration is 200 to 400 mmol/L; ultrasonically dispersing the alizarin in the ethanol, and preparing an alizarin-ethanol dispersing solution in which the final concentration of the alizarin is 2 to 3 mg/mL; mixing the blank liposome suspension solution with the alizarin-ethanol dispersing solution, carrying out supercritical CO2 treatment for 2 to 5 minutes at 50 to 55 DEG C and 8 to 12Mpa, thus obtaining the alizarin liposome. According to the alizarin liposome and the preparation method thereof, disclosed by the invention, supercritical CO2 is utilized for treating a mixed solution of the blank liposome suspension solution and the alizarin-ethanol dispersing solution, so that the alizarin liposome is successfully prepared.

Description

technical field [0001] The invention belongs to the field of veterinary medicine, and in particular relates to a rubidin liposome and a preparation method thereof. Background technique [0002] Rubia is a substance extracted from the plant Rubia. Rubia is a plant dye with a long history. Rubia is cold in the blood, can cool blood and stop bleeding, and can remove blood stasis. It can be used for any bleeding syndrome caused by blood heat. Cooling blood and promoting blood circulation, blood stasis dispelling, stimulates menstrual flow. For hematemesis, epistaxis, metrorrhagia, traumatic bleeding, amenorrhea stasis, joint arthralgia, tumbling swelling pain. Cooling blood to stop bleeding, promoting blood circulation and removing stasis: This product stops bleeding without leaving stasis, and is used for bleeding due to heat syndrome, abdominal pain due to amenorrhea, and traumatic injuries. [0003] Rubidolin (C 14 h 8 o 4 ) is an orange-red crystal or ochre-yellow powd...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K31/122A61K47/24A61P31/04
Inventor 柴保国孙江宏梁军杜雄伟班曼曼张涛
Owner HENAN SOAR VETERINARY PHARMA
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