Cyclophosphamide liposome and its preparing method

A technology of cyclophosphamide lipid and cyclophosphamide, which is applied in the field of medicine, can solve the problem of high recurrence rate after surgery, and achieve the effect of improving curative effect and poor oral absorption

Inactive Publication Date: 2006-05-24
胡才忠
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Observation on the Curative Effect of Cyclophosphamide in Postoperative Pterygium Hou Yuanyou Pterygium is one of the common external eye diseases, there are many clinical treatment methods, but the postoperative recurrence rate is high

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0010] Preparation of cyclophosphamide liposomes by ethanol injection method: take soybean phospholipids, cholesterol, VE and dissolve them in absolute ethanol and inject them into cyclophosphamide aqueous solution, stir at constant temperature and high speed, evaporate under reduced pressure to remove ethanol, pass through a microporous membrane for sizing, that is Cyclophosphamide liposomes were obtained, and the encapsulation efficiency could reach 66.8%.

Embodiment 2

[0012] Preparation of cyclophosphamide liposomes by thin film dispersion method: get soybean phospholipids, cholesterol, VE dissolved in 150ml eggplant-shaped bottle with 15ml chloroform, form a film under reduced pressure on a rotary thin film evaporator and remove all organic solvents, add 10ml cyclophosphamide The aqueous solution is hydrated, and the microporous membrane is passed through a microporous membrane to condense the particles to obtain cyclophosphamide liposomes, and the encapsulation efficiency can reach 63.1%.

Embodiment 3

[0014] Preparation of cyclophosphamide liposomes by reverse-phase evaporation method: Weigh soybean phospholipids, cholesterol, VE and add 5ml chloroform to dissolve, then add 10ml ether, then add 15ml cyclophosphamide phosphate buffer, bath ultrasonic to make uniform For single-phase system, remove chloroform ether by vacuum evaporation until gel is formed, continue to evaporate under reduced pressure for 5 to 10 minutes, and vortex until the aqueous suspension, that is, liposome, is formed. The encapsulation efficiency can reach 33.5%.

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Abstract

The present invention relates to a cyclophosphamide liposome and its preparation method. It is a liposome or precursor liposome prepared by using cyclophosphamide and auxiliary materials of phospholipid and cholesterol, in which the auxiliary materials of supporting agent, etc. also can be added. The film material phospholipid can adopt natural phospholipid or synthetic phospholipid, the weight ratio of phospholipid and medicine is 0.1:1-50:1, Its preparation method can adopt ethyl alcohol injection method, film dispersion method, inverted evaporation method, extrusion method and mechanical method. The supporting agent can be sorbitol, mannitol, cane sugar, sodium chloride, water soluble starch, dextran, glucose and lactose, the ratio of supporting agent and phospholipid is 0.01:1-500:1. Said invention can produce action of resisting tumor.

Description

technical field [0001] The invention relates to the technical field of medicine, specifically a cyclophosphamide liposome (including proliposome) and a preparation method thereof. Background technique [0002] Cyclophosvnamide (CTX) is white crystal, odorless, slightly bitter taste. Insoluble in ether, acetone, slightly soluble in water, unstable aqueous solution, slightly soluble in acetic acid. CTX is an alkylating agent, which was first artificially synthesized in 1958. CTX is a latent nitrogen mustard drug, which has no anti-tumor activity in vitro. When it enters the body, it is hydrolyzed by excess phosphoramidase or phosphatase in the liver or tumor tissue, and released Nitrogen mustard base plays an anti-tumor effect. Belonging to the cell cycle non-specific drugs, the anti-tumor spectrum is wider than nitrogen mustard, but the toxicity is lower than nitrogen mustard. It is mainly used for tumor immunity and has obvious inhibitory effect on various tumors. In rece...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/675A61K9/127A61P35/00
Inventor 胡才忠
Owner 胡才忠
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