Etoposide freeze-dry powder preparation for injection and preparation method thereof

A technology of etoposide and freeze-dried powder for injection, which is applied in the field of medicine and can solve the problems of low bioavailability and poor fat solubility.

Inactive Publication Date: 2009-05-06
李铁军
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0002] Etoposide (etoposide, 4-desmethyl epipodophyllotoxin-β-D-ethyl glucopyranoside) is a sugar metabolite of podophyllotoxin, which belongs to cell cycle specific antineoplastic drugs and has broad-spectrum anticancer activity , clinically commonly used dosage forms are injections and oral soft capsules. Since etoposide is almost insoluble in water and has poor fat solubility, the currently used clinical dosage forms have the disadvantage of low bioavailability to varying degrees. Because etoposide Glycosides are difficult to dissolve in water, and the existing injections are not very stable. Therefore, it is urgent to invent a stable, high bioavailability, and cheap etoposide freeze-dried powder preparation that is convenient for industrialized large-scale production to provide clinical needs.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment Construction

[0037] According to the above method, the following preparations of the present invention are prepared:

[0038] Formulation 1:

[0039] Etoposide or its pharmaceutically acceptable salt 50mg

[0040] Mannitol 150mg

[0041] Sodium bicarbonate amount

[0042] Formulation 2:

[0043] Etoposide or its pharmaceutically acceptable salt 100mg

[0044] Dextran 200mg

[0045] Sodium bicarbonate amount

[0046] Formulation 3:

[0047] Etoposide or its pharmaceutically acceptable salt 50mg

[0048] Glucose 200mg

[0049] Sodium bicarbonate amount

[0050] Formulation 4:

[0051] Etoposide or its pharmaceutically acceptable salt 50mg

[0052] Polyethylene Glycol 150mg

[0053] Sodium bicarbonate amount

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PUM

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Abstract

The invention relates to the technical field of medicament and discloses an etoposide freeze-dried powder preparation used for injection, which is convenient to be used in clinic, is high in bioavailability, is low in cost and can cure solid tumors. The medicament can quickly achieve effective curing concentration in a body when being directly injected through vein or muscle; moreover, the first-pass effect of the medicament to a liver is reduced, the bioavailability of the medicament in the body is improved, and the freeze-dried powder preparation used for injection is more convenient to be transported and can be stored for a longer time. The etoposide freeze-dried powder preparation used for injection contains the etoposide or the pharmaceutically acceptable salt thereof and pharmaceutically acceptable accessories used as active components; wherein, the weight percentage of the etoposide or the pharmaceutically acceptable salt thereof can be 1 to 80 percent, preferably be 30 to 70 percent and more preferably be 40 to 60 percent; the content range thereof in the preparation is generally 1 to 1000mg and preferably be 10 to 500mg.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to an etoposide freeze-dried powder injection preparation for injection that can treat solid tumors. Background of the Invention [0002] Etoposide (4-desmethylepipodophyllotoxin-β-D-ethyl glucopyranoside) is a sugar metabolite of podophyllotoxin, a cell cycle specific antitumor drug with broad-spectrum anticancer activity , The commonly used clinical dosage forms are injections and oral soft capsules. Since etoposide is almost insoluble in water and has poor lipid solubility, the currently used clinical dosage forms have the disadvantage of low bioavailability to varying degrees. The glycoside is not easily soluble in water, and the existing injection is not very stable. Therefore, there is an urgent need to invent a stable, high bioavailability and low price etoposide lyophilized powder injection preparation for industrialized large-scale production to provide clinical needs. S...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/19A61K31/7048A61P35/00
Inventor 李铁军王宏
Owner 李铁军
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