Compound docetaxel ester microsphere injection and preparation method thereof

A technology of compound docetaxel and injection, which is applied in the field of compound docetaxel lipid microsphere injection and preparation, can solve the problems such as the decrease of drug content, and achieve the effects of improving solubility, improving drug distribution, and increasing sensitivity

Active Publication Date: 2011-04-13
SHENYANG WANJIA INST OF BIOLOGICAL TECH RES
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] The technical problem to be solved by the present invention is to provide a compound docetaxel lipid microsphere injection, which can achieve the effect of small particle diameter below 100nm, has better physical stability, is difficult for drug loading to leak, and can be sterilized by filtration. Problems with decreased drug content in formulations due to autoclaving

Method used

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  • Compound docetaxel ester microsphere injection and preparation method thereof
  • Compound docetaxel ester microsphere injection and preparation method thereof
  • Compound docetaxel ester microsphere injection and preparation method thereof

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Experimental program
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Effect test

Embodiment 1

[0031] The compound docetaxel lipid microsphere injection of the present invention is prepared by the following raw materials by weight and number ratio, docetaxel: Brucea javanica oil: medium chain oil: egg yolk lecithin: polyethylene glycol-12-hydroxyl Stearic acid ester: glycerin: sterile water for injection = 0.5: 30: 30: 10: 10: 20: 700.

[0032] 10g refined egg yolk lecithin (Germany Lipoid company) and polyethylene glycol-12-hydroxystearate of 10g are dispersed in the composite oil phase that 30g injection grade Brucea javanica oil and 30g medium chain oil form, by the above weight Precisely weigh 0.5g of docetaxel and add it to the above oil phase to dissolve, add 700g of sterilized water for injection at about 55-65°C and 20g of glycerin, homogenize at 20000rpm for 5 minutes to form colostrum, add colostrum In the high-pressure homogenizer (Niro-Soavi, Italy), pass N 2 Protection, the initial pressure is 20-30MPa, cycle for 2 minutes, then rise to 80-100Mpa, cycle 6 ...

Embodiment 2

[0034] The compound docetaxel lipid microsphere injection of the present invention is prepared by the following raw materials according to the ratio of weight and number, docetaxel: Brucea javanica oil: medium chain oil: soybean lecithin: polyethylene glycol-12-hydroxy hard Fatty acid ester: glycerin: sterile water for injection = 5: 150: 150: 30: 60: 35: 950.

[0035] 30g of refined soybean lecithin (Germany Lipoid company) and 60g of polyethylene glycol-12-hydroxystearate are dispersed in the composite oil phase composed of 150g of injection-grade javanica javanica oil and 150g of medium chain oil according to the above-mentioned weight ratio. Weigh 5g of docetaxel and add it to the above oil phase to dissolve, add 950g of sterilized water for injection at about 60°C and 35g of glycerin, and homogenize at 20000rpm for 2-4 minutes to form colostrum, and add the colostrum to the high-pressure homogenization Quality machine (Niro-Soavi, Italy), through N 2 Protection, the init...

Embodiment 3

[0038] The compound docetaxel lipid microsphere injection of the present invention is prepared from the following raw materials by weight and number: docetaxel: Brucea javanica oil: medium chain oil: lecithin: polyethylene glycol-12-hydroxystearin Ester: polyethylene glycol 1000 vitamin E succinate: glycerin: sterile water for injection = 2: 50: 50: 15: 7: 8: 20: 800.

[0039] Its preparation method is as follows:

[0040] Disperse 15g lecithin (German lipoid company) with 7g macrogol-12-hydroxystearate and 8g macrogol 1000 vitamin E succinate: dispersed in 50g injection grade Brucea javanica oil with 50 medium chain In the composite oil phase composed of oil, accurately weigh 2 g of docetaxel according to the above weight ratio and add it to the above oil phase to dissolve, add 800 g of sterilized water for injection at about 60 ° C and 20 g of glycerin, and homogenize at 20,000 rpm for 2-4 minutes , to form colostrum, the colostrum is added to the high-pressure homogenizer ...

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Abstract

The invention discloses a compound docetaxel ester microsphere injection and a preparation method thereof, belonging to the technical field of medicines. The compound docetaxel ester microsphere injection is characterized by being prepared from the following raw materials in weight parts: 0.5 to 5 parts of docetaxel, 30-150 parts of Brucea javanica oil, 30-150 parts of middle-chain triglyceride, 10-30 parts of lecithin, 10-60 parts of polyethylene glycol surface active agents, 20-35 parts of glycerine and 700-950 parts of sterilized water for injection. The compound docetaxel ester microsphere injection of the invention is oil in water type microsphere preparation. The docetaxel as a main drug is coated in the Brucea javanica and middle-chain triglyceride compound oil phase of the oil in water type microsphere. The microsphere has a smaller grain diameter (which is lower than 100nm), and the preparation has better stability. The compound oil phase compositions play a cooperative anticancer role, and reduce the stimulation reaction of the injection and the side reactions such as hemolysis, allergy and the like. The invention has targeting function and increases the medicine effect.

Description

technical field [0001] The invention relates to a compound docetaxel lipid microsphere injection and a preparation method. The preparation has good anticancer effect and belongs to the technical field of medicines. Background technique [0002] Docetaxel is a derivative of paclitaxel, also known as docetaxel, the English name is Docetaxel, and the chemical name is {2aR-[2aα, 4β, 4aβ, 6β, 9α(αR * , βs * ), 11α, 12α, 12aα, 12bα]}-β-{[(1,1-dimethylethoxy)carbonyl]amino}-α-carbonylphenylpropanoic acid [12b-acetoxy-12-benzoyl Oxy-2a, 3, 4, 4a, 5, 6, 9, 10, 11, 12, 12a, 12b-dodecahydro-4, 6, 11-trihydroxy-4a, 8, 13, 13-tetramethyl -5-Oxo-7,11-methylene-1H-cyclodecapenta[3,4]benzo[1,2-b]oxetan-9-yl]ester. Paclitaxel has a unique anti-cancer mechanism. It prevents the growth of tumor cells by inducing and promoting tubulin polymerization, assembly and stabilizing microtubules. Significant curative effect in prostate cancer. Since it was launched in the United States in 1993, it...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/10A61K31/337A61K36/185A61K47/46A61P35/00
Inventor 董英杰艾莉李乐邹小峰
Owner SHENYANG WANJIA INST OF BIOLOGICAL TECH RES
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