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Paclitaxel mixed composition and water-in-oil type emulsion formulation for chemoembolization and preparation method thereof

A composition, paclitaxel technology, applied in the direction of drug combination, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc., can solve problems such as toxicity and side effects

Inactive Publication Date: 2004-11-17
DAE HWA PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, it is known that Taxol  The solubilizers used in the

Method used

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  • Paclitaxel mixed composition and water-in-oil type emulsion formulation for chemoembolization and preparation method thereof
  • Paclitaxel mixed composition and water-in-oil type emulsion formulation for chemoembolization and preparation method thereof
  • Paclitaxel mixed composition and water-in-oil type emulsion formulation for chemoembolization and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0049] Embodiment 1. the manufacture of super liquefied lipiodol / iobemol / paclitaxel emulsion

[0050] 800 μl of lipiodol Ultra-fluid (Lipiodol Ultra-fluid, Laboratoire Guerbet, France, iodine content of 38% by weight) was used as an oily contrast medium. Add the paclitaxel (Samyang Genex, Korea) of 8mg in the described super liquefied lipiodol, pack into test tube (micro test tube with safety plug, polyethylene system, 1.5ml, Eppendorf, Germany AG), stirred at room temperature to dissolve. It was heated to 40°C for rapid dissolution. To this oily mixture was added 200 μl of Iopexol (Bracco s.p.a. Italy). As a control mixture, a mixture of 0.8 ml of paclitaxel and 0.2 ml of iopexol was used. Photographs of these two mixtures after they were made are shown in figure 1 (upstream). Using a vortex mixer, each mixture was vortexed at maximum setting (120V, 0.65A, 60Hz) for 10 minutes. At the end of the vortexing, the lipiodol / iobiram / paclitaxel formulation did not phase-separa...

Embodiment 2

[0051] Embodiment 2. the manufacture of super liquefied lipiodol / iobix / paclitaxel / doxorubicin emulsion

[0052]800 μl of lipiodol Ultra-fluid (Lipiodol Ultra-fluid, Laboratoire Guerbet, France, iodine content of 38% by weight) was used as an oily contrast medium. Add the paclitaxel (Samyang Genex, Korea) of 8mg in the described super liquefied lipiodol, pack into test tube (micro test tube with safety plug, polyethylene system, 1.5ml, Eppendorf, Germany AG), stirred at room temperature to dissolve. For rapid dissolution, sonicate with a tank sonicator. To this oily mixture was added 200 μl of iopexate (Bracco s.p.a. Italy) containing 4 mg of doxorubicin (Sigma Chemicals). As a control mixture, a mixture consisting of 0.8 ml of paclitaxel and 0.2 ml of iopexate containing 4 mg of doxorubicin was used. Photographs of these two mixtures after they were made are shown in figure 2 (upstream). Using a vortex mixer, each mixture was vortexed at maximum setting (120V, 0.65A, 60H...

Embodiment 3

[0053] Embodiment 3. the manufacture of super liquefied lipiodol / iobix / paclitaxel / carboplatin composition

[0054] Compositions and controls were produced as in Example 2, except that 4 mg of carboplatin was used instead of doxorubicin. Photographs of these two mixtures after they were made are shown in image 3 (upstream). Using a vortex mixer, each mixture was vortexed for 10 minutes at maximum setting (120R, 0.65A, 60Hz). At the end of the vortexing, the lipiodol / iopix / paclitaxel / carboplatin formulation did not phase-separate to form an emulsion, while phase separation was observed in the lipiodol / iobix / carboplatin composition (BOC) . After 3 hours from the end of vortexing, the emulsion of the lipiodol / iopix / paclitaxel / carboplatin composition was stable, while the lipiodol / iobix / carboplatin composition was almost completely phase-separated (downstream). In the manufactured super liquefied lipiodol / iobixate / paclitaxel / carboplatin composition, only small water droplets (...

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Abstract

The present invention relates to the paclitaxel mixed composition and water-in-oil type emulsion formulation for chemoembolization and preparation method thereof. The combinatory formulation of anticancer drugs can be easily prepared since the emulsion formulation of the present invention can include other hydrophilic or lipophilic drugs.

Description

technical field [0001] The present invention relates to an oily paclitaxel composition and preparation for transcatheter arterial chemoembolization (TACE) obtained by solubilizing paclitaxel, and their production methods. Arterial chemoembolization (TACE) is a method of treating cancer by injecting anticancer agents and embolic substances into the nutrient arteries of the tumor while using a contrast agent to visualize the surgical procedure, thereby blocking the flow of blood to the cancer tissue. Provide nutrition. Background technique [0002] The most widely used arterial chemoembolization is hepatic arterial chemoembolization for the treatment of liver cancer. Contrast agents are used during or after surgery as an imaging tool and to induce embolism within the tumor. Anticancer agents such as doxorubicin (adriamycin), cisplatin, and carboplatin are dissolved or dispersed in oily contrast media. [0003] One of the most frequently used contrast agents in arterial chem...

Claims

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Application Information

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IPC IPC(8): A61K9/113A61K9/00A61K9/10A61K31/337A61K31/4164A61K31/4745A61K31/475A61K31/513A61K31/555A61K31/565A61K31/7048A61K33/24A61K47/16A61K47/18A61K47/22A61K47/24A61K47/28A61K47/34A61K47/44A61K49/04A61P35/00
CPCA61K9/0019A61K47/44A61K49/0452A61K31/337A61P35/00A61K9/10
Inventor 郑蕙婵郑曙荣权翊赞朴在亨郑镇旭金盈万李仁铉
Owner DAE HWA PHARMA
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