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Icaritin liposome and preparation method thereof

A technology of icariin and liposome preparation, which is applied in the field of medicine, can solve the problems of poor therapeutic effect, stability of curative effect, lower therapeutic index, and poor curative effect, so as to reduce the dosage of drugs and toxic and side effects, and repair liver acute disease. Damage and toxicity reduction effects

Inactive Publication Date: 2011-07-27
SECOND MILITARY MEDICAL UNIV OF THE PEOPLES LIBERATION ARMY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Because the compound is extremely poorly soluble in water, most in vivo studies have been limited to oral or gavage administration
Although this method is simple and easy to operate, there are still many disadvantages that cannot be ignored, such as: the drug entering the gastrointestinal tract is inevitably interfered by the first-pass elimination effect of the liver, greatly reducing the therapeutic index; gastrointestinal function and Gastrointestinal contents can greatly affect the efficacy of drug therapy or show poor efficacy stability; oral administration is usually absorbed slowly, and the effect on acute damage to organs or tissues is not good

Method used

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  • Icaritin liposome and preparation method thereof
  • Icaritin liposome and preparation method thereof
  • Icaritin liposome and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] Embodiment 1: the preparation of icariin liposome injection

[0033] Step 1: Weigh 1 g of epimeditin, 20 g of soybean lecithin and 2.5 g of cholesterol and put them in a round bottom flask;

[0034] Step 2: Add an appropriate amount of a mixed solution consisting of 8ml of ethanol and 4ml of chloroform to the above mixture to completely dissolve into a clear solution, and dry under reduced pressure at 65°C for about 4 hours by rotary thin film evaporation to completely evaporate the organic solvent;

[0035] Step 3: Add 800ml of water for injection, and continue to rotate under normal pressure until the film is completely hydrated;

[0036] Step 4: emulsify with a shear emulsifier for 5 minutes (rotating speed 2000 rpm) to obtain colostrum, homogenize the colostrum with a micro-jet high-pressure homogenizer (pressure 9000 psi) three times, and dilute the volume to 1000 ml with water for injection;

[0037] Step 5: adjust the pH to 5.0 with potassium dihydrogen phosphat...

Embodiment 2

[0038] Embodiment 2: the preparation of icariin liposome injection

[0039] Step 1: Weigh 1g of epimeditin, 30g of egg yolk lecithin, 30g of cholesterol and 5g of polysorbate 80 and place in a round bottom flask;

[0040] Step 2: Add 30ml of chloroform to the above mixture to completely dissolve into a clear solution, and dry under reduced pressure at 70°C for about 2 hours by rotary thin film evaporation to completely evaporate the organic solvent;

[0041] Step 3: Add 600ml of water for injection, and continue to rotate under normal pressure until the film is completely hydrated;

[0042] Step 4: emulsify with a shear emulsifier for 3 minutes (3000 rpm) to obtain colostrum, homogenize the colostrum with a micro-fluid high-pressure homogenizer (pressure 8000 psi) three times, and dilute the volume to 1000 ml with water for injection;

[0043] Step 5: adjust the pH to 6.0 with sodium dihydrogen phosphate buffer solution, pack in ampoules (or vials), and sterilize to obtain ic...

Embodiment 3

[0044] Embodiment 3: the preparation of icariin liposome injection

[0045] Step 1: Weigh 4g of epimeditin and 10g of soybean lecithin into a round bottom flask;

[0046] Step 2: Add 15ml of chloroform to the above mixture to completely dissolve into a clear solution, and dry under reduced pressure at 75°C for about 3 hours by rotary thin film evaporation to completely evaporate the organic solvent;

[0047] Step 3: Add 200ml of water for injection, and continue to rotate under normal pressure until the film is completely hydrated;

[0048] Step 4: Use a shear emulsifier to emulsify for 4 minutes (1000 rpm) to obtain colostrum, sonicate the colostrum with an ultrasonic instrument for 10 minutes, and dilute the volume to 1000ml with water for injection;

[0049] Step 5: adjust the pH to 4.5 with glacial acetic acid, pack in ampoules (or vials), and sterilize to obtain icariin liposomes for injection.

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Abstract

The invention provides icaritin liposome and a preparation method thereof. The lcaritin liposome mainly contains the following raw materials according to mass ratio: 0.01-5% of icaritin, 0.05-88% of phospholipid, 0-8% of plastification materials, 0-20% of propping agent and the balance of injection water. The preparation method comprises the following steps: completely dissolving the icaritin and the phospholipid in a organic solvent, then adopting a rotating film evaporation method for volatilizing the organic solvent completely; adding the injection water, continuously rotating a film under the normal pressure until the film is hydrated completely; emulsifying the mixture so as to obtain colostrum, conducting ultrasonic and homogenate on the colostrum, and then adopting the injection water for constant volume; and adjusting the PH value to be 4-8, then obtaining injecta preparation of the icaritin liposome, and further conducting vacuum cooling and drying on the icaritin liposome, then obtaining icaritin liposome powder preparation. Due to the icaritin liposome preparation, the icaritin treatment has better liver target property, and the stability and the bioavailability of a medicine are improved.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to an icariin liposome and a preparation method thereof. Background technique [0002] Icaritin, such as figure 1 As shown, the molecular formula C 21 h 20 o 6 , with a molecular weight of 368, is a flavonoid monomer compound extracted from the natural plant Epimedium (Epmedium). In recent years, a large number of studies have shown that icariin has various functions such as inducing cell proliferation and differentiation, expanding cardiovascular and cerebrovascular, anti-tumor, estrogen-like, improving sexual function, protecting neurodegenerative damage, and anti-osteoporosis. Especially in the article "Studies on Icaritin Alleviating Acute Liver Injury and Its Molecular Mechanism" (Liu Peng, Medical and Health Science and Technology, 2009), the author used a variety of methods to confirm the anti-free radical oxidation of icariin and the inhibition of liver dama...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K31/352A61P1/16
Inventor 李君严以群殷正丰郑肖利熊俊峰李娟晏建军黄亮
Owner SECOND MILITARY MEDICAL UNIV OF THE PEOPLES LIBERATION ARMY
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