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Etoposide preparations and preparation thereof

A technology of etoposide and preparation, applied in the field of medicine, can solve the problems of low bioavailability and poor lipid solubility, and achieve the effects of reducing dosage, enhancing absorption and reducing adverse drug reactions

Inactive Publication Date: 2008-09-10
SECOND MILITARY MEDICAL UNIV OF THE PEOPLES LIBERATION ARMY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Because etoposide is almost insoluble in water and its fat solubility is poor, the existing oral preparations such as tablets and soft capsules all have the disadvantage of low bioavailability to varying degrees, which has become a problem that restricts the efficacy of these drugs. main factor

Method used

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  • Etoposide preparations and preparation thereof
  • Etoposide preparations and preparation thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0045] Weigh 5.9g of etoposide and 12.0g of soybean lecithin, add them to tetrahydrofuran, and react with magnetic stirring in a constant temperature water bath for 90 minutes at 35°C until the solution is clear, and remove tetrahydrofuran by volatilization with a rotating thin film solvent method to obtain light yellow Phospholipid complex, spare.

Embodiment 2

[0047] Weigh 5.9g of etoposide and 7.5g of soybean lecithin, add them into tetrahydrofuran, and heat under reflux for 30 minutes at 30°C until the solution is clear, add 16.8g of caprylic triglyceride, polyoxyethylene (35) 29.0 g of sesame oil and 20.8 g of polyethylene glycol (400) were used to volatilize and remove tetrahydrofuran by the method of rotating thin film volatilization solvent, filling and sealing were prepared into hard capsules.

Embodiment 3

[0049] Weigh 36.0g of etoposide and 54.0g of egg yolk lecithin, add them into acetone, heat and reflux at 45°C for 60 minutes, until the solution is clear, add 120.0g of caprylic triglyceride, polysorbate 80 to 180.0 G, polyethylene glycol (400) 120.0g, acetone is volatilized and removed with the method of rotating thin film volatilization solvent, filling, sealing is prepared into hard capsule.

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Abstract

The invention relates to a medicine technical field. Etoposide has broad-spectrum anticancer activity and rather high therapeutic index, however, the etoposide hardly can be dissolved in water and the fat-soluble property is rather poor, the shortcoming of low bioavailability exists to different extent in oral preparations for present clinical use, tablet and soft capsule, for example. The invention aims at improving the hydrophilic property and the lipotropy of the etoposide, promoting the bioavailability of the etoposide and providing an etoposide preparation which has a simple preparation technique and is easily taken. Main medicine of the preparation of the invention is phospholipid compound of etoposide. The invention also provides a self-emulsifying agent and a preparation method thereof. The zooperies is a primary indication that the ACU of the self-emulsifying agent of the phospholipid compound of etoposide is 1.3 to 1.7 times of that of the soft capsules on sale.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to an etoposide preparation and a preparation method thereof. Background technique [0002] Cancer is one of the most difficult and common diseases of human beings. It is an extremely urgent and major issue in the world to conquer this stubborn fortress of cancer and benefit mankind. At present, the number of cancer patients is increasing year by year, and the mortality rate of cancer is constantly rising. According to statistics in recent years, about 800,000 people die of cancer every year, and an average of 1.5 people die of cancer every minute in the country. A large number of facts prove that the progress of cancer treatment is very little, and cancer is more and more serious threat to human life. Therefore, it is urgent to find new anti-cancer drugs, change their formulations to improve their anti-cancer efficacy and reduce their side effects. [0003] Etoposide (etoposide,...

Claims

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Application Information

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IPC IPC(8): A61K9/107A61K9/48A61K31/7048A61K47/24A61P35/00
Inventor 陈建明吴忠斌郭丹熊阳邓莉郑肖莉张悦李莹张扬
Owner SECOND MILITARY MEDICAL UNIV OF THE PEOPLES LIBERATION ARMY
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