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Oleanolic acid liposome preparation, freeze dried powder injecta thereof and its preparation

A technology for liposome preparation and freeze-dried powder injection, which is applied in the field of oleanolic acid liposome and freeze-dried powder for injection and preparation, can solve the problems of affecting drug dissolution and absorption, low drug bioavailability, affecting curative effect, etc. problem, to achieve good biocompatibility, solve the problem of water insolubility, and the preparation method is simple and easy to implement.

Inactive Publication Date: 2007-03-07
HENAN UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Due to the strong hydrophobicity of the drug, the dissolution and absorption of the drug in the gastrointestinal tract is affected, and the bioavailability of the drug is low, which greatly affects the full play of its curative effect

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0025] Weigh 10mg oleanolic acid, 300mg soybean lecithin (purity>90% phosphatidylcholine), 10mg cholesterol, 100mg Tween 80, place in a pear-shaped glass bottle, and use 20ml chloroform / methanol (1:2) mixed solvent In 37°C constant temperature water bath, the organic solvent was removed under reduced pressure with a rotary evaporator, so that a uniform lipid film was formed on the wall of the glass bottle, placed in a vacuum desiccator, and placed overnight at room temperature for later use. Take 10ml of pH6.8 phosphate buffer solution, add it to the above-mentioned glass bottle, rotate and wash the membrane with a rotary evaporator under the condition of an ice bath, until the lipid film is hydrated and becomes a milky white liposome suspension, and press evenly Reduce the particle size to a smaller size (5000psi, 10 times). 300 mg of mannitol was dissolved in liposomes, and after aseptic filtration (the pore size of the membrane filter was 0.22 μm), the final dispersion was ...

Embodiment 2

[0027] Weigh 10 mg of oleanolic acid, 500 mg of soybean lecithin (purity > 80% phosphatidylcholine), and 5 mg of cholesterol, place them in a pear-shaped glass bottle, and put them in a mixed solvent of 20 ml of chloroform / methanol (1:1) at 37 ° C. Use a rotary evaporator on a constant temperature water bath to remove the organic solvent under reduced pressure to form a uniform lipid film on the glass bottle wall, place it in a vacuum desiccator, and place it overnight at room temperature for later use. Take 10ml of glucose injection dissolved with 150mg of poloxamer 188, add it to the above-mentioned glass bottle, and use a rotary evaporator to wash the membrane under the condition of an ice bath until the lipid film is hydrated and becomes a milky white liposome mixture. Suspension, obtained by high-pressure homogenization with smaller particle size (5000psi, 5 times). 300 mg of lactose was dissolved in liposomes, and after aseptic filtration (membrane filter pore size 0.22 ...

Embodiment 3

[0029] Weigh 10mg of oleanolic acid and 300mg of lecithin and dissolve in 5ml of ether, then dissolve 200mg of polyoxyethylene castor oil in 10ml of 0.9% sodium chloride injection, then add the phospholipid ether solution to the chloride solution containing EL In sodium injection, the two are mixed for emulsification, and then the organic solvent is removed under reduced pressure, and probe ultrasonication is enough for 1 min. 1000 mg trehalose was dissolved in liposomes, after sterile filtration (membrane filter pore size 0.22 μm), the final dispersion was divided into vials, and then freeze-dried. The measured encapsulation efficiency is 72.8%, and the average particle diameter is 265nm.

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PUM

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Abstract

The invention relates to the liposome with oleanolic acid, relative freeze dried. Wherein, the liposome comprises oleanolic acid, phosphatide, cholesterol and surface activator, while their ratios are 1:10-80:0-20:0-50; the freeze dried is formed by oleanolic acid agent, dextran, monosaccharide, diose and / or polysaccharide, while their amounts are based on the mass of phosphatide, that one deal of phosphatide takes 0.2-5.0 deals of them; when the oleanolic acid is made into liposome, it can be inactively targeted into liver, to improve the drug density and reduce side effect; the drug will be slowly released in human body, to prolong the effective time; and its package rate is higher than 75%, particle diameter is 100-800cm.

Description

technical field [0001] The invention belongs to the technical field of pharmaceutical preparations, and in particular relates to an oleanolic acid liposome, a freeze-dried powder injection thereof and a preparation method thereof. Background technique [0002] Oleanolic acid (oleanolic acid, OA) is a pentacyclic triterpenoid compound, which is an effective active monomer extracted from natural plants. It exists in the free form or in the form of glycosides, and is widely distributed in nature. Oleanolic acid exists in 160 kinds of plants, such as cornel, privet fruit, ginseng, etc. Oleanolic acid can improve the structure and function of liver cells, inhibit the formation of mitochondrial lipid peroxide in liver cells, protect the liver cell membrane, reduce the elevated serum alanine aminotransferase, promote liver cell regeneration, and accelerate the repair of necrotic tissue . Clinically, it is mainly used to treat acute jaundice hepatitis and chronic toxic hepatitis, ...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K31/56A61K47/24A61K47/28A61P1/16A61P31/12
Inventor 陈洪轩陈志鹏肖衍宇牛江秀王艳丽邢磊
Owner HENAN UNIVERSITY
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