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Preparaton method of anticancer medicine colchicin microsphere freeze dried agent

A technology of colchicine and freeze-dried agent is applied in the field of preparation of anti-cancer drug colchicine microsphere freeze-dried agent, and achieves the effects of no hemolytic reaction, small particle size and low production cost

Inactive Publication Date: 2009-07-29
TSINGHUA UNIV
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

There are no relevant patents or literature reports on the colchicine microsphere freeze-dried agent in China

Method used

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  • Preparaton method of anticancer medicine colchicin microsphere freeze dried agent
  • Preparaton method of anticancer medicine colchicin microsphere freeze dried agent
  • Preparaton method of anticancer medicine colchicin microsphere freeze dried agent

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preparation example Construction

[0055] The preparation method for preparing the anticancer drug colchicine microsphere freeze-dried agent comprises the following steps:

[0056] 1) Prepare the raw materials of the following weight and volume ratios:

[0057] Colchicine 200-800 mg

[0058] Polycyanoacrylate 800 mg

[0059] Polyvinyl alcohol 20mg

[0060] Surfactant 40-80 mg

[0061] Sodium chloride 9000mg

[0062] Lyoprotectant 100—1000 mg

[0063] Organic solvent 500-1000ml

[0064] 1000ml distilled water

[0065] 2) dissolving the polyvinyl alcohol in water first, adding a surfactant and sodium chloride to the water phase to obtain an isotonic aqueous solution with blood plasma;

[0066] 3) Co-dissolve colchicine and cyanoacrylate in an organic solvent, inject it into the above aqueous solution at high speed, and keep stirring, and maintain the solution temperature at 40°C to 50°C;

[0067] 4) The organic phase rapidly diffuses into the water phase to form an O / W or W / O type emulsion, heat, and use ma...

Embodiment 1

[0074] 1), prepare the following weight and volume of raw materials

[0075] Colchicine 250 mg

[0076] Polycyanoacrylate 800 mg

[0077] Polyvinyl alcohol 20mg

[0078] Surfactant 40mg

[0079] Sodium chloride 9000mg

[0080] Glycine 500mg

[0081] Chloroform 500ml

[0082] 1000ml distilled water

[0083] 2) Accurately weigh 20 mg of polyvinyl alcohol, first fully swell with 500 ml of double distilled water, after the polyvinyl alcohol is fully swollen, continue to add another 500 ml of water and 40 mg of surfactant, and then add 9.0 g of sodium chloride to adjust the aqueous solution To isotonic with plasma, stir with a magnetic stirrer at 500rpm, and keep the solution temperature at 20°C;

[0084] 3), prepare 250ml of colchicine chloroform solution of 1.0mg / ml, place it in a 500ml beaker, and set aside;

[0085] 4) Fully dissolve 250ml of chloroform to prepare 800mg of polycyanoacrylate, put it in another 500ml beaker, and set aside;

[0086] 5) Take an equal amoun...

Embodiment 2

[0093] Identical with the step of embodiment 1, difference is that the formula of raw material is as follows:

[0094] Colchicine 400mg

[0095] Polycyanoacrylate 600mg

[0096] Polyvinyl alcohol 40mg

[0097] Surfactant 50mg

[0098] Sodium chloride 9000mg

[0099] Glycine 800mg

[0100] 800ml organic solvent

[0101] 1000ml distilled water

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Abstract

The invention discloses a preparation method of an anticancer drug colchicine microsphere freeze-dried agent which belongs to a pharmaceutical preparation. Dissolve polyvinyl alcohol in distilled water, add sodium chloride to adjust the solution to an aqueous solution that is isotonic with blood plasma; co-dissolve colchicine and cyanoacrylate in a machine solvent, and inject it into the sodium chloride of polyvinyl alcohol at high speed heating and stirring in the aqueous solution, adding a surfactant and a freeze-drying protective agent to the water phase, and performing vacuum freeze-drying to obtain a white, loose, and fluid powder-like solid colchicine microsphere freeze-dried agent. Clinically used to treat cancer, colchicine has obvious inhibitory effect on cell mitosis and can inhibit the growth of cancer cells; it has effects on breast cancer, primary gout, liver injury and fibrosis. The colchicine microsphere freeze-dried agent is a new type of anticancer drug with broad application prospects. The method for producing the colchicine microsphere freeze-dried agent has simple process, does not need special equipment, and thus has low production cost, and is suitable for large-scale industrial production.

Description

technical field [0001] The invention relates to a pharmaceutical preparation, in particular to a preparation method of an anticancer drug colchicine microsphere freeze-dried agent used for preparing a novel anticancer drug preparation. Background technique [0002] Microspheres are closed small spheroids composed of biodegradable polymer materials. According to literature reports, microspheres are a new dosage form of targeted drug delivery systems. After entering the body, microspheres are mainly covered by reticuloendothelial Systemic phagocytosis allows the drug to accumulate in macrophage-rich tissues and organs such as liver, spleen, and bone marrow. The microspheres increase the local drug concentration and improve the efficacy of the drug; at the same time, it reduces the distribution of the drug in the whole body and reduces the side effects of the drug. The microspheres have good biocompatibility, are non-toxic or immunogenic, and are safe and reliable. Microspher...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/165A61K9/50A61K9/14A61K9/19A61P35/00
Inventor 罗国安张奇王义明李德华
Owner TSINGHUA UNIV
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