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Mitoxantrone or liposome of mitoxantrone hydrochloric acid, and preparation method

A technology of mitoxantrone hydrochloride lipid and mitoxantrone hydrochloride lipid is applied in the field of mitoxantrone or mitoxantrone hydrochloride liposome and preparation thereof, and can solve the problem of inconvenience in drug packaging and clinical use, lipid Complex plastid production process, complex cardiolipin process and other problems, to achieve the effect of convenient clinical use, good stability, improved dispersibility and stability

Active Publication Date: 2007-02-21
NANJING LUYE PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The domestic patent (publication number: CN1602844) about mitoxantrone or mitoxantrone hydrochloride liposomes adopts the "pH gradient method" in the "ion gradient method". Prefabricated liposomes and buffers are prepared and packaged separately, and the two are mixed during clinical use. Therefore, the production process of liposomes using the "pH gradient method" is relatively complicated, and it is extremely inconvenient for pharmaceutical packaging and clinical use.
Abroad, there are new drug companies adopting cardiolipin to wrap the patent (publication number: CN1469735) applied for by mitoxantrone, which prepares the mitoxantrone liposome composition according to the action characteristics of mitoxantrone and cardiolipin, but Cardiolipin is an excipient with few natural sources. The process of synthesizing cardiolipin is complicated and expensive

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0032] Take 3g of phosphatidylinositol, 19.6g of egg yolk lecithin and 4g of cholesterol, mix them and dissolve them in a water bath at 55°C with 900ml of ethyl acetate, add 100ml of ethanol solution in which 100mg of sodium deoxycholate is dissolved, mix well and filter, The filtrate was rotatively evaporated under constant temperature and reduced pressure at 50°C to remove the solvent to form a film; take 500 mg of mitoxantrone hydrochloride and dissolve it in 500 ml of 5% glucose solution, wash the film with the above solution, and after the film is completely dispersed in the solution, use high-pressure Homogenization treatment to obtain mitoxantrone hydrochloride liposome emulsion; Mitoxantrone hydrochloride liposome emulsion is filtered with a filter membrane with a 0.22 micron pore size, and each bottle contains mitoxantrone hydrochloride 2mg, 5mg or 10mg sub-packaged, the finished product can be obtained after freeze-drying.

Embodiment 2

[0034]Take 3g of phosphatidylinositol, 40.6g of egg yolk lecithin and 8g of cholesterol, mix them and dissolve them in a water bath at 30°C with 900ml of ethyl acetate, add 100ml of ethanol solution in which 100mg of sodium deoxycholate is dissolved, mix well and filter, The filtrate was rotatively evaporated under constant temperature and reduced pressure at 30°C to remove the solvent to form a film; take 500 mg of mitoxantrone hydrochloride and dissolve it in 500 ml of 5% sucrose solution, wash the film with the above solution, and wait until the film is completely dispersed in the solution, press high pressure to uniformly slurry treatment to obtain the mitoxantrone hydrochloride liposome emulsion; the mitoxantrone hydrochloride liposome emulsion is filtered with a filter membrane with a pore size of 0.22 micron, and each bottle contains mitoxantrone hydrochloride 2mg, 5mg Or 10mg sub-package, the finished product can be obtained after freeze-drying.

Embodiment 3

[0036] Take 2g of phosphatidylinositol and 24g of egg yolk lecithin, mix them and dissolve them in a water bath at 55°C with 800ml of ethyl acetate, add 100ml of ethanol solution in which 100mg of sodium deoxycholate is dissolved, mix well and filter, and the filtrate is heated at 60°C Remove the solvent by rotary evaporation under constant temperature and reduced pressure to form a film; take 500 mg of mitoxantrone hydrochloride and dissolve it in 500 ml of 5% sucrose solution, add it to the film prepared above to wash the film, and wait until the film is completely dispersed in the solution. Homogenization treatment to obtain mitoxantrone hydrochloride liposome emulsion; Mitoxantrone hydrochloride liposome emulsion is filtered with a filter membrane with a 0.22 micron pore size, and each bottle contains mitoxantrone hydrochloride 2mg, 5mg or 10mg sub-packaged, the finished product can be obtained after freeze-drying.

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PUM

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Abstract

A liposome of mitoxantrone or mitoxantrone hydrochloride is prepared from mitoxantrone or mitoxantrone hydrochloride, negatively charged phosphatide, neutral phosphatide and cholate. Its preparing process is also disclosed.

Description

technical field [0001] The invention relates to a liposome preparation, in particular to mitoxantrone or mitoxantrone hydrochloride liposome and a preparation method thereof. Background technique [0002] Mitoxantrone or mitoxantrone hydrochloride was first synthesized by the laboratories of Murdock and Lederle in the United States in 1979 and its antitumor activity was proved. In December 1981, it was developed into a drug marketed by the British Cyanamid of Great Britain company. In 1987, the US FDA approved the production of mitoxantrone hydrochloride injection, and its trade name was Novantrone. Mitoxantrone or mitoxantrone hydrochloride is an anthracycline antineoplastic drug with a molecular structure similar to that of doxorubicin. It has a planar aromatic ring and is easily embedded in the base pairs of DNA double helices, forcing the two base pairs to separate. DNA grows, causing structural deformation and cell death. This product is a non-specific cell cycle drug...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K31/136A61P35/00
Inventor 张国喜翁帼英程培元荣融陈文忠程光
Owner NANJING LUYE PHARMA
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