Paclitaxel submicron emulsion using lipid composite as middle carrier

A technology of lipid complexes and intermediate carriers, which is applied in the fields of drug combination, emulsion delivery, and medical preparations containing active ingredients, etc. problems, to achieve the effect of reducing allergic reactions and toxicity, easy industrialized large-scale production, and stable storage quality

Active Publication Date: 2009-04-01
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 submicr

Method used

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  • Paclitaxel submicron emulsion using lipid composite as middle carrier
  • Paclitaxel submicron emulsion using lipid composite as middle 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 a paclitaxel submicron emulsion with a lipid compound as an intermediate carrier. With the paclitaxel lipid compound as the intermediate carrier, the paclitaxel is solved in oil phase, and water phase, emulsifier and auxiliary emulsifier are added. Emulsion droplet grain diameter is less than 600nm; the proportion of the oil phase and the water phase is 5 to 95 to 35 to 65; and the drug loading quantity is 0.25mg/ml to 5mg/ml if counted according to the paclitaxel. The prepared submicron emulsion has high drug loading quantity, is resistant for autoclaving and has stable quality after long time storage. The submicron emulsion can be made into intravenous drip transfusion directly, as well as into dry emulsion by a freeze drying technology, and when being used, the submicron emulsion is added with physiological saline or glucose to be diluted into intravenous drip.. The submicron emulsion uses nontoxic refined plant oil as the oil phase and phospholipid as the emulsifier, drug is coated in the oil phase, and thereby the submicron emulsion reduces the irritation and the adverse reaction of the paclitaxel preparation 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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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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