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Intravenous injection microemulsion preparation of teniposide

A technology of teniposide and emulsion, which is applied in the field of new microemulsion preparations for intravenous injection of teniposide, which can solve the problems of high cost, liposome instability, and easy leakage

Inactive Publication Date: 2007-08-15
PEKING UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, most of these new preparations are still in the research stage of the laboratory, and the liposomes used as injections still have problems such as instability, easy leakage, high cost, and difficulty in large-scale production.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033] prescription:

[0034] Teniposide 0.24g

[0035] Absolute ethanol 6.4g

[0036] Lecithin 4.5g

[0037] soybean oil 0.64g

[0038] CremophorEL 6.32g

[0039] 5% glucose solution 500ml

[0040] Preparation method:

[0041]Dissolve 0.24 g of teniposide in 6.4 g of absolute ethanol, then add 4.5 g of lecithin, 0.64 g of soybean oil and 6.32 g of CremophorEL, and mix them uniformly to form a pre-concentrate. Add the preconcentrate into 500ml of 5% glucose solution and shake to form a microemulsion.

Embodiment 2

[0043] prescription:

[0044] Teniposide 0.24g

[0045] Absolute ethanol 8g

[0046] Lecithin 4g

[0047] Corn Oil 0.8g

[0048] CremophorEL 8g

[0049] 5% glucose solution 500ml

[0050] Preparation method:

[0051] Mix 0.24 g of teniposide, 8 g of absolute ethanol, 4 g of lecithin, 0.8 g of soybean oil and 8 g of CremophorEL to form a preconcentrate. Add the preconcentrate into 500ml of 5% glucose solution and shake to form a microemulsion.

Embodiment 3

[0053] prescription:

[0054] Teniposide 0.24g

[0055] Lecithin 10g

[0056] soybean oil 1.1g

[0057] Cremophor EL 6.4g

[0058] Absolute ethanol 24g

[0059] 5% glucose solution 500ml

[0060] Preparation method:

[0061] Mix 0.24 g of teniposide with 10 g of lecithin, 1.1 g of soybean oil, 6.4 g of Cremophor EL and 24 g of absolute ethanol to form a pre-concentrate. When preparing the emulsion, inject the preconcentrate into 500 ml of 5% glucose injection to form a microemulsion.

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PUM

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Abstract

This invention relates to a formulation and preparation method of micro emulsion of Teniposide for intravenous injection. The micro emulsion comprises active components and auxiliary materials, wherein the active components are Teniposide or mixture of Teniposide, paclitaxel, and etoposide; and auxiliary materials is composed of vegetable oil, emulsifying agent or assistant emulsifier, and organic solvent. The micro emulsion for intravenous injection is obtained by preparing active components and auxiliary materials to pre-concentration liquid and adding to 5% glucose solution for clinical use. The invention has the advatages of convenient adminstration, high bioavailability, and reduced toxic anaphylaxis.

Description

technical field [0001] The invention relates to the formulation and preparation of a new microemulsion preparation for intravenous injection of teniposide. Background technique [0002] Teniposide (VM-26) is a semi-synthetic derivative of podophyllotoxin, which belongs to plant-derived antineoplastic drugs. It is a cycle-specific cytotoxic drug that inhibits DNA topoisomerase II, resulting in double-strand or single-strand damage, causing cell mitosis to stop in late S or early G2, thereby hindering tumor cell division and inhibiting tumor growth. Teniposide has a remarkable curative effect, and its biological activity is 5-10 times that of the same type of drug etoposide, and clinical data show that teniposide has few side effects, less toxicity, and has no effect on liver and kidney functions. Due to its extensive anti-tumor activity in clinical practice, teniposide is now widely used in the clinical treatment of children with acute lymphoblastic leukemia, small cell lung...

Claims

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Application Information

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IPC IPC(8): A61K31/7048A61K9/107A61K47/44A61P35/00A61K31/337
Inventor 张烜朱静吴科春曹轶刘祥瑞孙葭北张强
Owner PEKING UNIV
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