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Composition for vectorizing an anti-cancer agent

A technology of composition and medicament, applied in the field of compositions carrying anti-cancer medicaments, can solve problems such as ineffectiveness

Active Publication Date: 2016-12-21
GUERBET SA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Therefore, they are not sufficiently potent after injection, since a substantial part of the amount of anticancer agents injected intra-arterially does not reach the target lesion (Raoul et al., 1992)

Method used

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  • Composition for vectorizing an anti-cancer agent
  • Composition for vectorizing an anti-cancer agent
  • Composition for vectorizing an anti-cancer agent

Examples

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example 1

[0181] 1. Preparation of the composition in the form of an emulsion according to the invention

[0182] 1.1. Lipiodol Emulsions with anthracyclines

[0183] 50mg doxorubicin (Amycin injection ) in 2.5ml of the third generation 250 (250mg iodine / ml). After 30 seconds of manual stirring for good dissolution, the resulting solution was removed with a 20 ml Luer lock syringe. The syringe is then placed on the three-way stopcock.

[0184] PGPR (1% w / v total solution, 100 mg - Interchim) was dissolved in 7.5 ml lipiodol by manual stirring middle.

[0185] The resulting oil was removed with a 20 ml luer lock syringe also placed on a three-way stopcock at 90°C. Start with water and oil, and perform 34 back and forth with medium strength, that is, 17 backward and forward movements.

[0186] For these emulsions, the volume of the aqueous phase and the selected lipid phase were 2.5 ml (ie 25% v / v) and 7.5 ml (ie 75% v / v) respectively. The aqueous phase / lipid ratio is 1 / 3. ...

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Abstract

The invention relates to a stable water-in-oil emulsion composition containing: 20% to 40% (v / v) aqueous phase in the form of droplets and containing an anti-cancer agent; and 60% to 80% (v / v) lipid phase containing an iodized oil and at least one surfactant, having Formula (I), in a proportion, of surfactant mass relative to the total volume of the composition, of 0.3% to 5%, formula (I) for said surfactant being the following in which: s has a value of 0 or 1; m is a whole number from 2 to 30; R1 is a Formula (II) grouping wherein n is a whole number from 4 to 10, o is a whole number from 1 to 4, p is a whole number from 3 to 7; q is a whole number from 2 to 10, and r has a value of 0 or 1; R2 is a hydrogen atom or is identical to R1; and each R3 is, separately, a hydrogen atom or is identical to R1. The invention also relates to an emulsion obtained from said composition, to the preparing method thereof, and to the use thereof for treating cancer and the metastases thereof.

Description

technical field [0001] The present invention relates to a composition for the delivery of an anticancer agent comprising lipiodolized oil and a surfactant useful for preparing a composition in the form of a water-in-oil emulsion comprising an anticancer agent, Lipiodol and the surfactant. Background technique [0002] For more than a century, iodized oils (such as the product lipiodol ) has been used as a contrast product in radiological examinations such as lymphography or for the diagnosis of liver lesions. Lipiodol Mainly composed of ethyl esters of iodinated fatty acids of poppy oil. [0003] These iodized oils have been used in interventional radiology for over thirty years. Lipiodol is characterized by its tendency to be selectively taken up by liver tumors. Therefore, it has been suggested as a carrier of anticancer agents for the treatment of hepatocellular carcinoma in a technique called transarterial chemoembolization (TACE) (Nakamura et al., Radiology, 19...

Claims

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Application Information

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IPC IPC(8): A61K31/704A61K9/00A61K47/14A61K9/107A61K47/44A61P35/00A61K49/00A61K51/12
CPCA61K9/0019A61K47/14A61K47/44A61K31/704A61K49/0461A61K9/107A61P35/00A61P35/04A61K49/0447A61K31/407A61K33/26A61K51/1217
Inventor 卡罗琳·罗比克让-费朗索瓦·迈耶
Owner GUERBET SA
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