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Oleanolic acid polycystic lipidosome and preparation method and application thereof

A multivesicular liposome and oleanolic acid technology, which is applied in the field of medicine, can solve the problems of obvious liver first-pass effect, reduced bioavailability, and poor absorption

Inactive Publication Date: 2015-10-21
钟志容
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

At present, the relevant preparations of oleanolic acid are mainly oleanolic acid tablets, but oleanolic acid is a fat-soluble drug, which has the disadvantages of low dissolution rate in the gastrointestinal tract, poor absorption, and obvious first-pass effect in the liver. Its bioavailability is greatly reduced, therefore, it is necessary to research and develop new formulations of oleanolic acid

Method used

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  • Oleanolic acid polycystic lipidosome and preparation method and application thereof
  • Oleanolic acid polycystic lipidosome and preparation method and application thereof
  • Oleanolic acid polycystic lipidosome and preparation method and application thereof

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Effect test

Embodiment 1

[0035] A preparation method of oleanolic acid multivesicular liposomes, comprising the following steps:

[0036] 1), take by weighing soybean lecithin, cholesterol, glyceryl triolein, oleanolic acid, stearic acid and dissolve in organic solvent, dissolve and form oily phase; Wherein, described soybean lecithin, cholesterol, glycerol triolein The mass ratio of ester and oleanolic acid is: 1:0.57:0.38:0.2; the concentration of stearic acid in the oil phase is: 1mg / ml;

[0037] 2) Take 1ml of the oil phase and add it to 1ml of the inner water phase, and use an emulsifier to shear and disperse to form colostrum; the shear speed is 13500rpm, and the shear time is 150s;

[0038] 3) Take 0.3ml of colostrum and add it to 1ml of the external water phase, vortex to form double milk; the time of vortex is 25s;

[0039] 4), quickly transfer the double emulsion to a round-bottomed flask, and remove the organic solvent by rotary evaporation to obtain oleanolic acid multivesicular liposomes...

Embodiment 2

[0041] 1), take by weighing soybean lecithin, cholesterol, glyceryl triolein, oleanolic acid, stearic acid and dissolve in organic solvent, dissolve and form oily phase; Wherein, described soybean lecithin, cholesterol, glycerol triolein The mass ratio of ester and oleanolic acid is: 1:0.57:0.38:0.2; the concentration of stearic acid in the oil phase is: 1mg / ml;

[0042] 2) Take 1.5ml of the oil phase and add it to 1ml of the inner water phase, and use an emulsifier to shear and disperse to form colostrum; the shear speed is 13500rpm, and the shear time is 150s;

[0043] 3) Take 0.5ml of colostrum and add it to 1ml of the external water phase, vortex to form double milk; the time of vortex is 25s;

[0044] 4), quickly transfer the double emulsion to a round-bottomed flask, and remove the organic solvent by rotary evaporation to obtain oleanolic acid multivesicular liposomes.

[0045] In the above embodiments, the internal aqueous phase includes, by mass percentage: 5% glucose...

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Abstract

The invention provides oleanolic acid polycystic lipidosome and a preparation method and application thereof. The method comprises the following steps: 1 weighing granulesten, cholesterol, olein, oleanolic acid and stearic acid by mass, and dissolving the ingredients into organic solvent, wherein oil phase is formed through the dissolution; 2 taking and adding a specified amount of oil phase into internal water phase, and using an emulsifying machine for conducting shearing and dispersing for forming primary emulsion; 3 taking and adding a specified amount of primary emulsion into external water phase, and conducting vortex oscillation for forming compound emulsion; 4 transferring the compound emulsion rapidly into a round-bottom flask, conducting rotary evaporation for removing the organic solvent, and obtaining the oleanolic acid polycystic lipidosome. According to the oleanolic acid polycystic lipidosome and the preparation method and application thereof, the oleanolic acid is loaded into a lipoid layer of polycystic lipidosome for preparing the oleanolic acid polycystic lipidosome (OA-MVLs), and it is expected to improve the bioavailability and achieve the purposes of releasing medicine slowly, reducing administration times and improving the adaptability of a patient.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to an oleanolic acid multivesicular liposome, a preparation method, and an application thereof. Background technique [0002] Oleanolic acid (OA for short), also known as soil angelica acid, alias Qingsisu, chemical name (3β)-3-Hy-droxyolean-12-en-28-oic-acid, white cluster Crystalline powder, odorless, tasteless, insoluble in water, soluble in methanol, ethanol, chloroform and acetone. OA is a pentacyclic triterpenoid compound, mainly present in plants such as Prunella vulgaris, forsythia, olive, privet and papaya in the form of free or saponins. In 1908, OA was first isolated from the leaves of Oleaeuro-peae L by FB Powers, and its structure was determined by Ruzicka in 1946. In 1975, the Hunan Institute of Pharmaceutical Industry in my country isolated and identified the OA monomer in the chemical and pharmacological research on the anti-hepatitis active ingredients of Folium ...

Claims

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Application Information

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IPC IPC(8): A61K9/127A61K31/56A61P35/00
Inventor 钟志容刘中兵柯发敏唐灿李劲薇罗玉玲熊丹景沛肖双礼刘丽
Owner 钟志容
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