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Intravenous injection emulsion of paclitaxel or polyenic taxusol

A technology of docetaxel and paclitaxel, which is applied in the direction of emulsion delivery, medical preparations with non-active ingredients, medical preparations containing active ingredients, etc., and can solve liposome encapsulation efficiency, drug stability and leakage, etc. Complicated, easily oxidized phospholipids, harmful substances and other problems, to achieve the effect of simple and feasible preparation process, large drug loading capacity and good stability

Inactive Publication Date: 2009-05-20
FUDAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Wherein the emulsifier of the emulsion adopts egg yolk lecithin, Tween 80, PEGylated phospholipids and other emulsifiers, which can improve the solubility of paclitaxel or docetaxel and delay drug release to a certain extent, but the phospholipids are easily oxidized to produce harmful substances; The encapsulation efficiency, drug stability and leakage of plastids are complicated
At present, there is no report on the study of paclitaxel emulsion using polyethylene glycol lauryl hydroxystearate as emulsifier

Method used

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  • Intravenous injection emulsion of paclitaxel or polyenic taxusol
  • Intravenous injection emulsion of paclitaxel or polyenic taxusol
  • Intravenous injection emulsion of paclitaxel or polyenic taxusol

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0033] Example 1 Preparation of Paclitaxel Emulsion Containing 0.01% Paclitaxel

[0034] Weigh 100mg of paclitaxel or docetaxel, 100g of soybean oil, 25g of ethanol, 20g of Solutol 15 and 0.1g of tocopherol, stir and dissolve to obtain the oil phase, add 22.5g of glycerin, add water for injection to 1000ml, mix at 40°C, Emulsify with an emulsifying mixer for 40 minutes (rotating speed 1500 rpm), adjust the pH to 7.0 with sodium hydroxide (0.1mol), use a high-pressure homogenizer to circulate 6 times at 20,000 psi, filter and sterilize, subpackage, and fill with nitrogen to obtain the finished paclitaxel emulsion , the average particle size of the emulsifier is 113.8nm, the paclitaxel content is 0.00965%, and the pH is 7.0.

Embodiment 2

[0035] Example 2 Preparation of Paclitaxel Emulsion Containing 0.05% Paclitaxel

[0036] Weigh paclitaxel or docetaxel 500mg, soybean oil 100g, ethanol 25g, Solutol 15 20g and tocopherol 0.1g, stir and dissolve to obtain the oil phase, add glycerin 22.5g, add water for injection to 1000ml, mix at 40°C, Emulsify with an emulsifying mixer for 60 minutes (rotating speed 2000 rpm), adjust the pH to 6.0 with hydrochloric acid (0.1mol), use a high-pressure homogenizer to circulate 5 times under 20000 psi, filter and sterilize, then subpackage, and fill with nitrogen to obtain the finished paclitaxel emulsion. The average particle diameter of the emulsifier is 119.2nm, the paclitaxel content is 0.00487%, and the pH is 6.17.

Embodiment 3

[0037] Example 3 Preparation of Paclitaxel Emulsion Containing 0.12% Paclitaxel

[0038] Weigh 1.2g of paclitaxel or docetaxel, 100g of medium chain oil, 30g of ethanol, 20g of Solutol 15, and 0.1g of tocopherol, stir and dissolve to obtain the oil phase, add 22.5g of glycerin, add water for injection to 1000ml, mix at 40°C, Emulsify with a shear emulsifying mixer for 40 minutes (rotation speed 2000 rpm), adjust the pH to 7.0 with sodium hydroxide (0.1mol), use a high-pressure homogenizer to circulate 5 times at 15000 psi, filter and sterilize, subpackage, and fill with nitrogen Obtain the paclitaxel emulsion finished product, the average particle diameter of the emulsifier is 120nm, the paclitaxel content is 0.1.1942%, and the pH is 6.89

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Abstract

The invention belongs to the field of traditional Chinese medicine pharmacy, in particular to a novel emulsion for intravenous injection of an anti-cancer drug taxol or polyenic taxusol, and a preparation method thereof. The emulsion consists of the taxol or the polyenic taxusol, and oil for injection, emulsion, in particular to glycol laurylhydroxystearate, and other pharmaceutically necessary auxiliary materials. Results via experiments show that the injection emulsion has excellent stability and haemolysis significantly smaller than a commercial taxol injection, and is helpful for improving administration safety and effectiveness of the taxol. The emulsion for intravenous injection can be directly used for intravenous injection, has the advantages of safe administration and small stimulation, can be easily accepted by patients, and can be used as an energy replenisher. The emulsion has the advantages of good stability, large drug loading, convenient use and simple preparation technology method, and is applicable to mass production.

Description

technical field [0001] The invention belongs to the field of traditional Chinese medicine pharmacy, and in particular relates to an emulsion for intravenous injection of an anticancer drug paclitaxel or docetaxel and a preparation method thereof. In the intravenous injection emulsion of the present invention, the emulsifier polyethylene glycol lauryl hydroxystearate has little irritation and stable properties, and has the effect of reversing drug resistance of tumors. It is expected to realize the anticancer drug paclitaxel or docetaxel good curative effect. Background technique [0002] Paclitaxel and docetaxel are currently one of the broad-spectrum chemotherapeutic drugs in clinical use. They are diterpenoids obtained from the bark or needles of yew or its species in the 1970s, and are effective in ovarian cancer, breast cancer, colon cancer, non-small cell lung cancer, head and neck cancer, and melanoma. It has a good therapeutic effect. Its mechanism of action is to ...

Claims

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Application Information

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IPC IPC(8): A61K31/337A61K9/107A61K47/34A61K47/44A61P35/00A61K47/10A61K47/14A61K47/26
Inventor 陈卫陆伟跃侯惠民
Owner FUDAN UNIV
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