Etoposide lipidosome and preparation method thereof

A technology of etoposide and posideside, which is applied in liposome delivery, pharmaceutical formulations, medical preparations of non-active ingredients, etc., can solve the problems of non-compliance with drug safety and industrial production, and improve the chemical stability of drugs Sexuality, increasing curative effect, increasing water solubility and stability

Inactive Publication Date: 2009-11-25
SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although great progress has been made in the research of etoposide preparations, most of these new dosage forms are currently in the laboratory research stage, and most of them do not meet the requirements of drug safety and industrial production. So far, there have been no clinical and market reports

Method used

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  • Etoposide lipidosome and preparation method thereof
  • Etoposide lipidosome and preparation method thereof
  • Etoposide lipidosome and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0046] Take 100 mg of etoposide, 500 mg of lecithin, and 40 mg of cholesterol in a 50 ml eggplant-shaped bottle, add 20 ml of ethanol: acetone (2: 1) and ultrasonically dissolve it fully. Put the eggplant-shaped bottle in a 40°C constant temperature water bath to remove the organic solvent by rotary evaporation under reduced pressure, and form a layer of lipid film on the inner wall of the bottle, slowly add 10ml of phosphate buffer (pH7.0), hydrate, vortex, and make the eggplant The lipid film on the vial was completely dissolved. The mixture was ultrasonically dispersed at room temperature (ultrasonic power 600W) for 30 minutes to obtain etoposide liposomes. Its average particle size is 179nm, all particles are below 300nm, and the particle size distribution is narrow, indicating that the liposome size is relatively uniform; the liposome can be stable at room temperature for several days and at 4°C for at least 3 months, storage No precipitation or degradation of etoposide ...

Embodiment 2

[0048] Accurately weigh 100 mg of etoposide, 400 mg of soybean lecithin, 40 mg of cephalin, 30 mg of soybean steryl glucoside, and 20 mg of vitamin E, and dissolve them with 10 ml of ether. Then slowly inject this solution into 30ml of physiological saline (40°C) containing 0.5% sodium cholate with a syringe, stir with an electronic constant speed stirrer at a speed of 2000r / min until the ether is completely removed, and the mixed solution is homogenized under high pressure (homogeneous Pressure 10000psi) 5 times to obtain etoposide liposomes, which were stored in a refrigerator at 4°C for later use.

Embodiment 3

[0050] Accurately weigh 100mg of etoposide, 2000mg of hydrogenated lecithin, 800mg of soybean sterol, 50mg of cardiolipin, and 50mg of stearylamine in a Erlenmeyer flask, heat to melt, and place in a 75°C water bath for later use. Dissolve 100mg of poloxamer 188, 400mg of glycerin, and 100mg of vitamin C in 20ml of 5% glucose solution, heat to 75°C, add to the lipid melt, mix at high speed, and homogenize under high pressure (homogenization pressure 15000psi) 3 times to obtain etoposide liposomes.

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Abstract

The invention provides an etoposide lipidosome used for injection or oral administration. The etoposide lipidosome is characterized in that etoposide is enveloped with phospholipid type substance, and the etoposide lipidosome with small grain size, high entrapment efficiency, good stability and low toxic side effect is prepared. The prepared etoposide lipidosome enhances the solubility and the stability of the etoposide, reduces the toxicity of the etoposide and prolongs the cycling time of the medicine in the blood, thereby improving the therapeutic effect of the medicine; and the preparation prepared by the etoposide lipidosome has the characteristics of low toxicity, low sensitivity and high efficiency on the clinical application. The invention also relates to a preparation method of the etoposide lipidosome, which has simple preparation process and low cost and is suitable for the industrial production.

Description

technical field [0001] The invention belongs to the field of pharmacy, and specifically relates to liposomes containing etoposide, an antitumor active ingredient, and a preparation method of the liposomes. Background technique [0002] Tumor is a common and frequently-occurring disease, which poses a great threat to people's life and health. It is a research topic that has received more and more attention in the medical field. More than 7 million people die from cancer every year all over the world, and now there are about 37 million cancer patients. In my country, about 1.3 million people die of cancer every year, and the estimated incidence rate is between 1.8 million and 2 million. The overall incidence rate is constantly rising. In many large cities in my country, malignant tumors have surpassed cardiovascular and cerebrovascular diseases, ranking first among all causes of death, and in the 35-59 age group, tumors have always been the number one killer. In the past, ma...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K31/7048A61K47/24A61P35/00
Inventor 李亚平陈伶俐顾王文
Owner SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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