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Self-emulsifying capsule of docetaxel and its preparation method

A technology of docetaxel and self-emulsification, applied in the field of medicine, can solve the problems of low bioavailability, incomplete absorption, restricted use, etc., and achieve the effect of high bioavailability, convenient administration, and good stability

Inactive Publication Date: 2007-08-08
黄成安
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, docetaxel has a particularly low solubility in water and is a solid drug that is insoluble in water, which seriously limits its clinical use.
Made into oral dosage forms such as ordinary tablets, dropping pills, and solid capsules, there will be problems of low bioavailability and incomplete absorption

Method used

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  • Self-emulsifying capsule of docetaxel and its preparation method

Examples

Experimental program
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Effect test

Embodiment 1

[0026] Weigh 400g of glyceryl caprylate, add 50g of docetaxel, fully dissolve it by ultrasound at 25°C, then add 410g of polyoxyethylene (40) castor oil and 140g of PEG400 and stir at 25°C. It becomes a uniform and transparent solution, using a compression method and an automatic rotary capsule machine to prepare soft capsules with a specification of 0.5 g per capsule, that is, each capsule contains 25 mg of docetaxel. The average particle size of the self-emulsifying soft capsule preparation under the condition of gentle stirring in water at 37° C. in vitro is 74.4 nm, and the distribution range is between 50 nm and 80 nm.

Embodiment 2

[0028] Weigh 200g of safflower seed oil, 52g of caprylic acid triglyceride, 100g of corn oil, and 248g of caprylic monoglyceride, mix well, add 80g of docetaxel, stir to dissolve it at 80℃, and then add lecithin 80g, 200g of Simp's high-efficiency solubilizer HD-508, 40g of polyoxyethylene (35) castor oil, stir at 75℃ to make it a uniform and transparent solution, and use the compression method to prepare specifications with an automatic rotary capsule machine Each soft capsule containing 0.7g of content, that is, each capsule contains 56mg of docetaxel. Measured by the Zetasizer Nano S type nanometer particle size analyzer, the self-emulsifying hard capsule preparation has an average particle size of 92.0nm and a distribution range of 70nm-120nm under the condition of gentle stirring in water at 37°C in vitro.

Embodiment 3

[0030]Weigh 65 g of capric monoglyceride, 67 g of capric diglyceride, 100 g of sunflower oil, 18 g of evening primrose oil, and 95 g of fish oil, mix well, add 5 g of docetaxel, and stir to dissolve it at 60°C. , And then add 300g of Simpu high-efficiency solubilizer HD-608, 150g of polyoxyethylene (40) castor oil, then add 130g of PEG600, 50g of n-propanol, and 20g of glycerol. Stir at 65℃ to make it uniform and transparent The solution is filled, sealed, and prepared into a soft capsule with a content of 0.8g per capsule, that is, each capsule contains 4mg of docetaxel. Measured by the Zetasizer Nano S type nanometer particle size analyzer, the self-emulsifying soft capsule preparation has an average particle size of 201nm and a distribution range of 150nm-284nm under the condition of gentle stirring in water at 37°C in vitro.

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Abstract

The invention relates to a method for preparing doxitasa self-emulsion capsule agent, which comprises doxitasa, oil, emulsifier, and auxiliary emulsifying agent. And the preparation comprises that dissolving the materials into oil via mixing or ultrasonic wave, adding emulsifier and auxiliary emulsifying agent, mixing or using ultrasonic wave to obtain uniform transparent solution; filling into capsule to obtain soft or hard capsule. The invention has simple process, high stability and high utilization.

Description

Technical field [0001] The invention relates to the technical field of medicine, in particular to a self-emulsifying capsule preparation containing docetaxel and a preparation method thereof. Background technique [0002] Docetaxel (Docetaxel, Docetaxel, Taxotere, Taxotere) is a taxane compound with the molecular formula C 43 HN 53 O 14 , Its molecular weight is 807.88, structural formula: [0003] [0004] Docetaxel is a semi-synthetic paclitaxel derivative developed by Rhone-Poulenc Rorer. It is a microtubule depolymerization inhibitor. The product was first launched in Mexico in April 1995 and is now available in the United Kingdom, the United States, and France. , Italy, Germany, Japan and other countries. Docetaxel can speed up the polymerization of tubulin into microtubules and delay the depolymerization of microtubules, leading to the formation of stable non-functional microtubule bundles, thereby disrupting mitosis and cell proliferation. Its cytotoxicity is 1.3 to 12 t...

Claims

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Application Information

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IPC IPC(8): A61K31/337A61K9/48A61K47/34A61K47/44A61P35/00A61K47/10A61K47/14A61K47/24
Inventor 黄成安
Owner 黄成安
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