Paclitaxel lipid composite

A technology of lipid complex and paclitaxel, which is applied in the directions of liposome delivery, drug combination, medical preparations with inactive ingredients, etc., can solve the problems of high submicron emulsion, low solubility, aggregation and precipitation, etc., and achieves high drug loading capacity. , high safety, low allergic effect

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 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 lipid composite
  • Paclitaxel lipid composite

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0030] Embodiment 1: paclitaxel-egg yolk phospholipid complex

[0031] 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.

Embodiment 2

[0032] Embodiment 2: paclitaxel-soybean phospholipid complex

[0033] 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.

Embodiment 3

[0034] Example 3: Paclitaxel-Cholesterol Complex

[0035] 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 lipid complex. The paclitaxel lipid complex consists of paclitaxel and lipid material. The weight proportion of the paclitaxel and the lipid material is 1 to 1 - 19, the preferential proportion is 1 to 2 - 10, and the more preferential proportion is 1 to 3 - 6. The lipid material is selected from natural lipid and synthetic lipid or the mixture thereof. The paclitaxel lipid complex can also contain antioxidation stabilizer. The invention also discloses a preparation method of the paclitaxel lipid complex and the application in the preparation of injection submicron emulsion and dry emulsion. The paclitaxel lipid complex has high solubility in oil, and the prepared submicron emulsion has the advantages of high drug loading quantity, high stability, high safety and low irritability.

Description

technical field [0001] The invention relates to a paclitaxel lipid complex, which belongs 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 aminophylline are often taken before administration to pre...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/127A61K31/337A61K47/24A61P35/00
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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