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Docetaxel lyophilization dry emulsion for injections and method for preparing the same

A freeze-dried emulsion and docetaxel technology, which is applied in the direction of freeze-dried delivery, emulsion delivery, powder delivery, etc., can solve the problems that do not meet the requirements of drug safety and industrial production, so as to facilitate industrial production and extend the validity period , improve the effect of therapeutic index

Inactive Publication Date: 2008-01-02
SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, most of them do not meet the requirements of drug safety and industrialized production, and there have been no reports of clinical application and marketing.

Method used

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Examples

Experimental program
Comparison scheme
Effect test

preparation Embodiment 1

[0042] 20 mg of docetaxel and 500 mg of lecithin were dissolved in 5 ml of a mixed solvent of ethyl acetate and ethanol to form an organic phase. Weigh 6 mg of poloxamer and 3 mg of α-tocopherol and dissolve in 30 ml of water for injection as the water phase. Stir the organic phase and the water phase under the condition of 1500rpm magnetic stirring for 10 minutes to obtain colostrum, and then homogenize the colostrum through a high-pressure homogenizer to obtain a finely dispersed emulsion; remove the organic solvent under reduced pressure, add 2 g of mannitol, and freeze Dry to remove water, obtain dry docetaxel lyophilized emulsion.

preparation Embodiment 2

[0044] Dissolve 8 mg of docetaxel and 200 mg of monoglyceride acetate in a mixed solvent of 5 ml of dichloromethane and ethanol to form an organic phase. Weigh 5 mg of poloxamer 108 and 2 mg of sodium deoxycholate dissolved in 50 ml of water for injection as the water phase. Stir the organic phase and the water phase under the condition of 1000rpm magnetic stirring for 30 minutes to obtain colostrum, and then homogenize the colostrum with a high-pressure homogenizer to obtain a finely dispersed emulsion; add 1.5g of sucrose, stir to dissolve it, and remove it under reduced pressure organic solvent, and then freeze-dried to obtain the freeze-dried emulsion of docetaxel of the present invention.

preparation Embodiment 3

[0046]10 mg of docetaxel, 200 mg of soybean lecithin, and 200 mg of cholesterol were dissolved in 6 ml of a mixed solvent of acetone and ethanol to form an organic phase. Weigh 5g of sodium cholate and 3mg of glycerol and dissolve in 50ml of water for injection as the water phase. Stir the organic phase and the water phase at 50°C and 3000rpm for 3 minutes to obtain colostrum, then homogenize the colostrum with a high-pressure homogenizer to obtain a finely dispersed emulsion; add 1.2g of mannitol, stir to dissolve it, and remove it under reduced pressure organic solvent, and then freeze-dried to obtain the freeze-dried emulsion of docetaxel of the present invention.

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PUM

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Abstract

The invention relates to pharmacology field, which in detail provides a frozen died emulsion that contains docetaxel and findings, with the weight proportion being 1-50 and 3-1000, respectively. The invention also relates to the preparation method. Said method comprises following steps: (1)mixing docetaxel, emulsifier and solvent top prepare dispersed docetaxel emulsion; (2)adding frozen dried protecting agent into dispersed emulsion; (3)removing water through freeze drying and preparing dried docetaxel emulsion. The invention is characterized by low-toxic frozen dried emulsion, increased medicine safety and body durability, improved medicine treatment index and stability for storage and transportation, prolonged medicine effective date and increased medicine quality.

Description

technical field [0001] The invention relates to the field of pharmaceutical preparations. Specifically, the present invention relates to a docetaxel freeze-dried emulsion and a preparation method thereof. Background technique [0002] Docetaxel (DOCETAXEL) is a taxane drug, which is an anticancer drug that can inhibit the mitosis and proliferation of cancer cells. The pharmacological effect of docetaxel is stronger than paclitaxel, and its antitumor activity is higher than that of paclitaxel, and it is effective for advanced breast cancer, non-small cell lung cancer, ovarian cancer, prostate cancer, pancreatic cancer, liver cancer, head and neck cancer and gastric cancer . [0003] Due to the poor water solubility of docetaxel, the currently commercially available docetaxel injection (40g L -1 ) uses Tween-80 (tween-80) as a solvent, and is equipped with a diluent containing 13% ethanol. Because Tween-80 is hemolytic, it will cause allergic reactions when used for intrav...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K9/19A61K9/107A61K31/337A61P35/00
Inventor 李亚平陈伶俐顾王文
Owner SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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