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Method for preparing tween-free docetaxel injection

A technology for docetaxel and injections, which is applied in the field of medicine and chemical industry, can solve the problems of undiscovered technical methods such as publicity or reporting, achieve good biocompatibility, mild preparation conditions, and increase solubility

Inactive Publication Date: 2012-11-28
邓世明
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] The preparation methods of polymer micelles that use block copolymers to solubilize insoluble drugs are commonly used in chemical reaction methods, dialysis methods, solvent evaporation methods, freeze-drying methods, etc. There are many related researches in domestic published patents and literature Report, which includes the research report of poloxamer for solubilizing docetaxel, such as the invention patent applied by Shandong University (CN 101732234 A, preparation method of block polymer micellar lyophilized preparation loaded with docetaxel) , Chen Ge and other research papers (solid dispersion technology improves the in vitro dissolution characteristics of docetaxel, Chinese Journal of Hospital Pharmacy, P1186, (30) 4, 2010), etc., but have not yet found that the same technical method as the present invention is disclosed or reported

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0015] Weigh 400mg of Poloxamer 407, heat and melt at 65-75°C, stir gently to make the bubbles disappear, add 10mg of docetaxel powder, stir to fully mix and dissolve to obtain a clear molten liquid; The poloxamer 407 melt was poured into a metal tray, placed in a refrigerator for rapid cooling and solidification, and then dried in a vacuum desiccator for 48 hours; the dried poloxamer 407 blocks loaded with docetaxel were collected, Crushed, sterilized by irradiation, subpackaged, each bottle contains 2mg of docetaxel. Before use, add 0.9% physiological saline for injection as required for hydration to obtain a clear micellar solution.

Embodiment 2

[0017] Weigh 400mg of poloxamer 407, heat and melt at 65-75°C, stir gently to make bubbles disappear, add 15mg of docetaxel powder, stir to fully mix and dissolve to obtain a clear molten liquid; The poloxamer 407 melt was poured into a metal plate, placed in a refrigerator to rapidly cool and solidify, and then dried in a vacuum desiccator for 24 hours; the dried poloxamer 407 blocks loaded with docetaxel were collected, Pulverize, then add 3ml of water for injection to hydrate to obtain a clear solution, pass through a 0.22 micron microporous membrane, and divide the filtrate to obtain 5 mg / ml docetaxel injection. Before use, add 0.9% physiological saline for injection to dilute as required to obtain a clear micellar solution.

Embodiment 3

[0019] Weigh 400mg of Poloxamer 407, heat and melt at 65-75°C, stir gently to make the bubbles disappear; take 20mg of docetaxel powder, add 0.3ml of absolute ethanol to dissolve, and then add to the melt of Poloxamer 407 Mix and stir in the medium to make the absolute ethanol volatilize completely to obtain a clear molten liquid; pour the poloxamer 407 molten liquid dissolved in docetaxel into a metal plate, put it in the refrigerator to cool and solidify rapidly, and then dry it in a desiccator 48 hours; crush the dried poloxamer 407 block loaded with docetaxel, add 4ml of water for injection to hydrate, then add 400mg of mannitol to dissolve, pass through a 0.22 micron microporous membrane, and freeze-dry the filtrate , to obtain 5 mg / docetaxel freeze-dried powder injection. Before use, add 0.9% physiological saline for injection and redissolve as required to obtain a clear micellar solution.

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PUM

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Abstract

The invention relates to a method for preparing a changed formulation of an antitumor medicine sold on the market, in particular to a method for preparing a tween-free docetaxel injection, and belongs to the technical field of medicines and chemical industry. According to the method, poloxamer 407 is used as a carrier of docetaxel, precursor polymer micelles are prepared by a melting method, a powder injection or an injection is prepared, and a stable and clarified docetaxel polymer micelle solution can be obtained by melting the powder injection in water or diluting the injection before the powder injection and the injection are used, so that the solubility of docetaxel is improved, the in-vivo detention time is prolonged, and the adverse reaction caused by using tween-80 is avoided.

Description

technical field [0001] The invention relates to a preparation method of Tween-free docetaxel injection, which belongs to the technical field of medicine and chemical industry. Background technique [0002] Docetaxel (Docetaxel) is a semi-synthetic second-generation taxane anti-tumor drug, its mechanism of action is to play an anti-tumor effect by interfering with the microtubule network necessary for cell mitosis and interphase cell functions, and is used for the treatment of Solid tumors such as prostate cancer, breast cancer, ovarian cancer, non-small cell lung cancer, pancreatic cancer, head and neck cancer, gastric cancer, etc., have significant curative effects when used alone or in combination, and have become the first-line drugs for the treatment of solid tumors. However, docetaxel is insoluble in water, has a short half-life and high toxicity. Currently, the clinically used preparation uses Tween-80 as a solubilizer, and is equipped with a solvent containing 13% eth...

Claims

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Application Information

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IPC IPC(8): A61K9/19A61K9/08A61K31/337A61K47/34A61P35/00A61K47/10
Inventor 邓世明杨先会李晓凤汤丽昌王宁
Owner 邓世明
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