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Paclitaxel Submicroemulsion Using Lipoplex as Intermediate Carrier

A technology of lipid complex and paclitaxel, which is applied in the direction of drug combination, emulsion delivery, and medical preparations containing active ingredients, etc. It can solve the problems of inability to directly make drug loading, easy demulsification, unstable quality, etc. , to achieve the effects of reducing allergic reactions and toxicity, being easy to industrialized large-scale production, and maintaining stable quality

Active Publication Date: 2011-12-07
BEIJING WEHAND BIO PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Although paclitaxel is more lipophilic than hydrophilic, its solubility in oil is also low, only 0.25 mg / ml, and it cannot be directly made into a submicron emulsion with high drug loading, and it is prone to demulsification during sterilization and storage , Aggregation and precipitation, unstable quality

Method used

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  • Paclitaxel Submicroemulsion Using Lipoplex as Intermediate Carrier
  • Paclitaxel Submicroemulsion Using Lipoplex as Intermediate Carrier

Examples

Experimental program
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Effect test

preparation example 1

[0039] Preparation Example 1: Paclitaxel-egg yolk phospholipid complex

[0040] Take 0.4g of paclitaxel and 2.4g of egg yolk lecithin, add 100ml of tetrahydrofuran, compound at 40°C for 1 hour, remove the tetrahydrofuran by rotary evaporation, and dry in vacuum for more than 12 hours (20-30°C) to obtain the drug-loaded egg yolk phospholipid complex. Pack and store in the refrigerator.

preparation example 2

[0041] Preparation Example 2: Paclitaxel-soybean phospholipid complex

[0042] Take 1g of paclitaxel and 6g of soybean lecithin, add 250ml of acetone preheated to 40°C, compound at 40°C for 1 hour, remove the solvent by rotary evaporation, and dry in vacuum for more than 12 hours (20-30°C), to obtain drug-loaded soybean lecithin compound Items, airtightly packaged, stored in the refrigerator.

preparation example 3

[0043] Preparation Example 3: Paclitaxel-Cholesterol Complex

[0044] Take 2g of paclitaxel and 4g of cholesterol, add 750ml of acetone preheated to 40°C, compound at 40°C for 2 hours, remove the solvent by rotary evaporation, and dry in vacuum for more than 12 hours (20-30°C) to obtain the drug-loaded cholesterol-lipid compound Items, airtightly packaged, stored in the refrigerator.

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Abstract

The invention discloses paclitaxel submicroemulsion with lipoplex as intermediate carrier. If the paclitaxel lipid complex is used as the intermediate carrier, the paclitaxel is dissolved in the oil phase, and the water phase, emulsifier, and co-emulsifier are added. The emulsion droplet size is below 600nm; the ratio of oil phase to water phase is 5:95 to 35:65; calculated as paclitaxel, the drug loading is 0.25mg / ml-5mg / ml. The prepared submicron emulsion has high drug loading capacity, high pressure sterilization resistance and stable quality in long-term storage. It can be directly made into infusion solution for intravenous infusion, and can also be made into dry milk by freeze-drying process, and diluted with physiological saline or glucose before use, and then intravenously infused. The submicron emulsion of the present invention uses non-toxic refined vegetable oil as the oil phase and phospholipid as the emulsifier, wraps the medicine in the oil phase, reduces the irritation and adverse reactions of paclitaxel preparations, and has good safety.

Description

technical field [0001] The invention relates to paclitaxel submicroemulsion with paclitaxel lipid complex as an intermediate carrier, belonging to the technical field of pharmaceutical preparations. Background technique [0002] Paclitaxel (Taxol) has important antitumor activity and is clinically used in the treatment of ovarian cancer, breast cancer, non-small cell lung cancer, head cancer and neck cancer. Because it is almost insoluble in water (0.006μg / ml), paclitaxel injection is now used clinically It was prepared by dissolving 30 mg of paclitaxel in 5 ml of Cremopher EL (polyoxyethyl castor oil) / ethanol (50% each) mixed solution. A few minutes after the prescription is administered, some patients may experience allergic reactions such as drug-induced rash, shortness of breath, bronchospasm, and hypotension. This is mainly due to the release of histamine in the body caused by Cremopher EL in the prescription. At present, antihistamines such as dexamethasone and amin...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K9/107A61K31/337A61P35/00
Inventor 刘玉玲夏学军郭瑞芳汪仁芸王洪亮金笃嘉
Owner BEIJING WEHAND BIO PHARMA CO LTD
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