Lomustine liposome freeze-drying powder injection and its preparation method

A lomustine and liposome technology, applied in the field of liposome preparations, can solve the problems of lomustine clinical application limitations, large toxic and side effects, bone marrow suppression, etc., achieve stable drug loading, good stability, The effect of reducing toxic side effects

Inactive Publication Date: 2006-10-04
ZHEJIANG UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, after the drug is administered, the side effects are relatively large, and the common ones are gastrointestinal toxicity and liver function damage. In addition, long-term drug use will cause bone marrow suppression, and there is a cumulative
These toxic and side effects have greatly restricted the clinical application of lomustine

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0052]Weigh 10 mg of lomustine, 600 mg of soybean lecithin (purity>76% phosphatidylcholine) and 60 mg of cholesterol, dissolve them in ether, mix well, place the solution in a round-bottomed flask, and keep the temperature at 30-32°C On the water bath, use a rotary evaporator to evaporate the organic solvent under the condition of 100rpm and reduced pressure, so that the film-forming materials such as phospholipids form a uniform lipid film at the bottom of the flask; add 30ml of ether to dissolve the above lipid film, and add 5ml (2 -10ml) PH7.4 phosphate buffer solution, ultrasonically emulsified in a water bath, remove the organic solvent with a rotary evaporator at 30°C until it becomes a milky white liposome suspension, and high-pressure emulsify to reduce the particle size. 0.3 mg of vitamin E and 500 mg of mannitol were dissolved in liposomes, and after aseptic filtration (pore diameter of membrane filter: 0.2 μm), the final dispersion was divided into vials, and then fr...

Embodiment 2

[0055] Weigh 10mg of lomustine, 600mg of soybean lecithin (purity > 93% phosphatidylcholine) and 60mg of cholesterol, dissolve them in ether, mix well, place the solution in a ground-mouthed round bottom flask, and keep the temperature at 30-32°C On the water bath, use a rotary evaporator to evaporate the organic solvent under the condition of 100rpm and reduced pressure, so that the film-forming materials such as phospholipids form a uniform lipid film at the bottom of the flask; add 5ml (2-10ml) pH7.4 to the above lipid film Phosphate buffer solution was rotated with a rotary evaporator at 30°C until the lipid film was hydrated and turned into a milky white liposome suspension, and the particle size was reduced by high-pressure emulsification. 0.3 mg of vitamin E and 500 mg of mannitol were dissolved in liposomes, and after aseptic filtration (pore diameter of membrane filter: 0.2 μm), the final dispersion was divided into vials, and then freeze-dried.

[0056] The lomustine...

Embodiment 3

[0058] Weigh 5 mg of lomustine, 300 mg of soybean lecithin (purity>76% phosphatidylcholine) and 30 mg of cholesterol, dissolve them in ether, mix well, place the solution in a round-bottomed flask, and keep the temperature at 30-32°C On the water bath, use a rotary evaporator to evaporate the organic solvent under the condition of 100rpm and reduced pressure, so that the film-forming materials such as phospholipids form a uniform lipid film at the bottom of the flask; add 30ml of ether to dissolve the above lipid film, and add 5ml (2 -10ml) PH7.4 phosphate buffer solution, ultrasonically emulsified in a water bath, remove the organic solvent with a rotary evaporator at 30°C until it becomes a milky white liposome suspension, and high-pressure emulsify to reduce the particle size. 0.3 mg of vitamin E and 500 mg of mannitol were dissolved in liposomes, and after aseptic filtration (pore diameter of membrane filter: 0.2 μm), the final dispersion was divided into vials, and then fr...

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Abstract

The invention relates to an antineoplastic Lomustine liposome, its freeze-dried powder njection and preparing process, wherein the preparation comprises liposome of Lomustine and pharmaceutically acceptable carrier, the liposome of the anti-cancer Lomustine contains the following constituents: Lomustine, phosphatide, cholesterin and vitamin E, their weight ratio being 1 : 2-100 : 1-15 : 0.01-0.05.

Description

Technical field: [0001] The invention relates to a liposome preparation of antitumor drug lomustine. Background technique: [0002] Lomustine (Cyclohexylnitrosourea), an alkylating agent antineoplastic drug, as a cell cycle non-specific drug, is most sensitive to cells at the G2-S boundary, or early S cells, and is most sensitive to cells in the G2 phase It also has an inhibitory effect. After entering the human body, its molecule is broken from the aminocarboxamide bond into two parts: one is the chloroethylamine part, which dissociates chlorine to form vinyl carbocations, which exerts an alkylation effect and causes DNA strand breaks , RNA and protein are subject to alkylation, which is mainly related to anti-tumor effect; the other is that the carbamoyl part is changed into isocyanate, or converted into carbamic acid to exert carbamylation effect, mainly with protein, especially with it The lysine terminal amino group and other reactions. It is believed that this is mai...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/17A61K9/19A61K9/127A61P35/00
Inventor 金一沈圆圆张宏梅
Owner ZHEJIANG UNIV
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