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Etoposide venous emulsion and preparation method thereof

A technology of etoposide and emulsion, which is applied in the field of intravenous emulsion, and can solve the problems of poor water solubility, low bioavailability and low solubility of oral preparations, etc.

Inactive Publication Date: 2008-02-13
大道隆达(北京)医药科技发展有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the absolute bioavailability of etoposide oral preparations is only 25% to 75%. The poor water solubility of etoposide and its decomposition into inactive products in acidic medium are the main reasons for the low bioavailability of its oral preparations.
[0005] Its main toxicity is severe reduction of bone marrow suppressed neutrophils, nausea, vomiting and other gastrointestinal toxicity, allergic reaction chills, fever, tachycardia, bronchospasm, dyspnea and / or hypotension, etc., and its solubility in water is extremely low. Small, need to improve the dosage form

Method used

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  • Etoposide venous emulsion and preparation method thereof

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Experimental program
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Effect test

Embodiment 1

[0018] First, dissolve 0.8 etoposide in methyl benzoate, heat in a constant temperature water bath at 80 degrees Celsius, add 12 g of soy lecithin, stir thoroughly for 3 minutes to disperse the soy lecithin evenly, add 100 g of soybean oil preheated to 80 degrees to the above liquid, and use The colostrum is produced by a high-speed emulsifier, and the preheated water for injection is added to the colostrum to a sufficient amount, and the volume is adjusted to 1000ml, transferred to a homogenizer for homogenization, and then filtered, potted and sterilized.

Embodiment 2

[0020] First, dissolve 1.0 etoposide in methyl benzoate, heat in a constant temperature water bath at 80 degrees Celsius, add 12 g of egg yolk lecithin, and stir for 3 minutes to make the soybean lecithin evenly dispersed, add 100 g of soybean oil preheated to 80 degrees Celsius to the above liquid, Use a high-speed emulsifier to make colostrum, add preheated water for injection to the colostrum to a sufficient amount, set the volume to 1000ml, transfer to a homogenizer for homogenization, and then filter, pot and sterilize.

Embodiment 3

[0022] First, dissolve 1.2 etoposide in methyl benzoate, heat in a constant temperature water bath at 80 degrees Celsius, add 12 g of soy lecithin, and stir for 3 minutes to make the soy lecithin evenly dispersed, add 100 g of soybean oil preheated to 80 degrees Celsius to the above liquid, and use The colostrum is produced by a high-speed emulsifier, and the preheated water for injection is added to the colostrum to a sufficient amount, and the volume is adjusted to 1000ml, transferred to a homogenizer for homogenization, and then filtered, potted and sterilized.

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Abstract

The present invention relates to a compound with etoposide stable emulsion for intravenous injection, which is characterized in that the present invention comprises the etoposide, the plant oil, the emulsifier, the antioxidant and the organic solvent. The present invention can not only provide high energy nutrition, but also work as vector for a plurality of oiliness or lipid soluble drug; therefore high dispersion and high bioavailability are obtained. In addition, the present invention relates to the preparation of the compound with topside stable emulsion for intravenous injection.

Description

technical field [0001] The invention relates to a pharmaceutical composition for intravenous injection, in particular to an intravenous emulsion of etoposide. Background technique [0002] The antineoplastic drug etoposide is the sugar metabolite of podophyllotoxin, which is extracted and separated from plants such as podophyllum and podophyllum in Tibet, China. [0003] [0004] Using podophyllotoxin as raw material, semi-synthesized under certain conditions to obtain etoposide, exerts anti-tumor effect by inhibiting the activity of DNA topoisomerase II in mammals, has broad-spectrum anti-cancer activity and quite high therapeutic index, It is mainly used for the treatment of lung cancer, lymphoma, acute leukemia, testicular cancer and small cell lung cancer. However, the absolute bioavailability of etoposide oral preparations is only 25% to 75%. The poor water solubility of etoposide and its decomposition into inactive products in acidic medium are the main reasons for...

Claims

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Application Information

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IPC IPC(8): A61K9/107A61K31/7048A61P35/00
Inventor 周英
Owner 大道隆达(北京)医药科技发展有限公司
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