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Teniposide medicinal composition and preparation method thereof

The technology of teniposide and composition is applied in the field of pharmaceutical compositions containing teniposide, an active anti-tumor component, and can solve the problems such as the lack of teniposide cyclodextrin, so as to improve the bioavailability and improve the therapeutic effect

Inactive Publication Date: 2010-01-27
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

Judging from the current retrieval data, there is no published relevant report on the composition of teniposide cyclodextrin or its derivatives

Method used

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  • Teniposide medicinal composition and preparation method thereof
  • Teniposide medicinal composition and preparation method thereof
  • Teniposide medicinal composition and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] Weigh teniposide 50mg, dissolve in 5ml acetone; weigh 2g β-cyclodextrin, dissolve in 50ml water for injection, add the teniposide acetone solution dropwise into the β-cyclodextrin solution, at room temperature Magnetic stirring was performed at 1000 rpm for 6 hours to obtain a clear and transparent solution, acetone was removed under reduced pressure, and a white loose powder teniposide β-cyclodextrin pharmaceutical composition was obtained by freeze-drying.

[0036] Get the teniposide β-cyclodextrin pharmaceutical composition 2g (equivalent to teniposide 0.0488mg) and teniposide 0.0488mg obtained by this method, add water 10ml respectively, shake and dissolve respectively and filter, get the filtrate for use UV spectrophotometer to measure its absorbance, and calculate its solubility.

[0037] Results: The solubility of teniposide β-cyclodextrin pharmaceutical composition is 0.04g / 100ml, and the solubility of teniposide raw material is 0.001g / 100ml. The solubility has...

Embodiment 2

[0039] Weigh 4g of α-cyclodextrin, add 40ml of distilled water, and ultrasonically dissolve it; weigh 50mg of teniposide, dissolve it with 5ml of dimethylformamide, and drop it into the α-cyclodextrin solution, and put it under 600W power Under ultrasonication for 30 minutes, the resulting solution was vacuum-dried at 30° C. to obtain a solid teniposide α-cyclodextrin pharmaceutical composition.

Embodiment 3

[0041] Weigh 4g of hydroxypropyl-β-cyclodextrin, add 40ml of distilled water, and ultrasonically dissolve it; weigh 50mg of teniposide, dissolve it in 5ml of dimethylacetamide, and drop it into hydroxypropyl-β-cyclodextrin The cyclodextrin solution was sonicated for 30 minutes at a power of 600W, and the obtained solution was vacuum-dried at 30° C. to obtain a solid teniposide hydroxypropyl-β-cyclodextrin pharmaceutical composition.

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Abstract

The invention relates to a teniposide medicinal composition and a preparation method thereof. The teniposide medicinal composition comprises active component teniposide, cyclodextrin, and derivatives or mixture thereof, and unnecessary excipient, wherein the teniposide is included by the cyclodextrin and / or the derivatives of the cyclodextrin. The medicinal composition improves the water solubility and stability of the teniposide, reduces toxic and side effects of the teniposide, and can be used as an initial material or a component for preparing injection or an oral preparation of the teniposide.

Description

technical field [0001] The invention belongs to the field of pharmacy, and in particular relates to a pharmaceutical composition containing teniposide, an antitumor active ingredient, and a preparation method of the composition. 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 k...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/7048A61K47/40A61K47/48A61P35/00
Inventor 李亚平陈伶俐顾王文
Owner SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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