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Teniposide liposome and preparation method thereof

A technology of niposide and teniposide, which is applied in the field of pharmacy, can solve problems such as not meeting the requirements of drug safety and industrial production, and achieve the effects of facilitating industrial production, improving anti-tumor activity, and good stability

Inactive Publication Date: 2013-04-10
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

However, most of these new dosage forms are currently in the research stage of the laboratory, and most of them do not meet the requirements of drug safety and industrial production. So far, there have been no clinical or market reports

Method used

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  • Teniposide liposome and preparation method thereof
  • Teniposide liposome and preparation method thereof
  • Teniposide liposome and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0044] Take 50 mg of teniposide, 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 prepare teniposide liposomes. Its average particle size is 257nm, all particles are below 500nm, and the particle size distribution is narrow, indicating that the liposome size is relatively uniform; the liposome can be stable for several days at room temperature and at least 3 months at 4°C. No precipitation was observed during this time.

Embodiment 2

[0046] Accurately weigh 50 mg teniposide, 200 mg soybean lecithin, 50 mg cephalin, 20 mg soybean steryl glucoside, and 10 mg vitamin E, and dissolve them with 10 ml 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 teniposide liposomes, which were stored in a refrigerator at 4°C for later use.

Embodiment 3

[0048] Accurately weigh 100mg of teniposide, 2000mg of hydrogenated lecithin, 800mg of soybean sterol, 50mg of cardiolipin, and 50mg of stearylamine in an Erlenmeyer flask, heat and 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 get teniposide liposome.

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Abstract

The invention provides teniposide liposome capable of being used for injection or oral administration, which is characterized in that teniposide is encapsulated by phospholipids, and the teniposide liposome with small grain diameter, high encapsulation rate, good stability and low toxic and side effect is prepared. The teniposide liposome prepared by the method improves the solubility and the stability of the teniposide, lowers the toxicity and prolongs the circulation time of drug in blood, thereby improving the treatment effect of the drug, and leading the preparation prepared by the liposome to have the characteristics of low toxicity, low hypersensitivity and high efficiency. The invention also relates to a preparation method of the teniposide liposome, which has simple process and lowcost and is suitable to industrial production.

Description

technical field [0001] The invention belongs to the field of pharmacy, and in particular relates to liposomes containing teniposide, 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, ...

Claims

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Application Information

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Patent Type & Authority Patents(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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