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Elemene liposome and its preparation method

A technology of elemene lipid and elemene lipid, applied in the field of fat-soluble drug elemene liposome and preparation thereof, can solve the problem of low bioavailability, poor oral absorption of elemene, and stability of elemene injection problems such as poor sex, to achieve a high distribution, beneficial to the effect of treatment

Inactive Publication Date: 2005-08-10
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0012] The purpose of the present invention is to provide a new injection form, oral dosage form, infusion dosage form, aerosol dosage form of elemene, i.e. elemene liposome and its preparation method, to improve the poor oral absorption of elemene and low bioavailability ; The defect of poor stability of elemene injection

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0016] Embodiment 1: get 0.4g soybean lecithin, 0.1g cholesterol, 0.05g elemene, appropriate amount of V E Inject into 10ml of pH 8 Tris buffer solution by ether injection method or ethanol injection method to obtain elemene liposome.

Embodiment 2

[0017] Embodiment 2: get 0.75g soybean lecithin, 0.25g cholesterol, 0.075g elemene, appropriate amount of V E Dissolve it with 40ml of chloroform-ether (1:1), put it in a 500ml flask, form a film under reduced pressure on a rotary thin film evaporator and remove all organic solvents, add 25ml of pH7.4 phosphate buffer for hydration, and obtain Elemi en liposome

Embodiment 3

[0018] Embodiment 3: take by weighing 0.60g soybean lecithin, 0.2g cholesterol, 0.075g elemene, appropriate amount of V E Add 10ml of chloroform to dissolve, place in a 150ml eggplant-shaped bottle, evaporate the chloroform under reduced pressure, and form a layer of lipid film on the inner wall of the bottle. Add 5ml of chloroform, 10ml of ether, and then add 15ml of elemene in phosphate buffer (pH7.4), bath ultrasonic for 3 minutes to form a homogeneous single-phase system, evaporate under reduced pressure to remove chloroform and ether until gel is formed, continue to reduce Evaporate under pressure for 5 to 10 minutes, and vortex until the aqueous suspension, that is, liposomes, is formed.

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Abstract

A novel elemene lipid in the form of oral liquid, injection, perfusion, aerosol, or solid is prepared from the plant extract containing element isomer, phosphoride and cholesterol by alcohol injection method, reverse-phase distilling method, extruding method, or mechanical method. Its advantages are high distribution in liver, low distribution in kidney, high biologic utilization rate, and high target effect.

Description

[0001] Technical field: the present invention belongs to the technical field of medicine, specifically it is fat-soluble drug elemene liposome and its preparation method. Background technique: [0002] Elemene is a sesquiterpene mixture extracted from traditional Chinese medicine or certain plants. Its Latin name is elemenum and its English name is elemene. Elemene is a mixture mainly composed of β-elemene and a small amount of other sesquiterpenes (α-elemene, γ-elemene, δ-elemene). The chemical structure of β-elemene is 1-methyl-1-vinyl-2,4-diisopropenylcyclohexane and the molecular formula is C 15 h 24 , volatile and highly fat-soluble. Elemene is clinically used to treat cancerous chest, ascites, liver cancer, cervical cancer, brain tumor, lung cancer, esophageal cancer and other cancers. When it kills cancer cells, it does not harm normal cells. A large number of clinical studies have shown that its effect is significantly better than cisplatin in the treatment of canc...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K31/015A61P35/00
Inventor 邓英杰王秀敏张修宇
Owner SHENYANG PHARMA UNIVERSITY
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