| Docetaxel interferences the microtubule network, which are necessary for mitotic and interkinesis cells, give rise to anti-tumor effect. It can bind free tubulin and promote tubulin assembly into stable microtubules while inhibiting their disaggregation, resulting in the loss of normal micro-bundle forming and fixing, thereby inhibiting cell mitosis. Docetaxel chemotherapy for early failure of advanced or metastatic breast cancer treatment, as well as the use of cisplatin-based chemotherapy for advanced or metastatic failure in non-small cell lung cancer treatment. As a new generation of highly effective anticancer drug, docetaxel currently in our country there is no patent and administrative protection, the market outlook remains positive for imitation.In this paper, based on production process of freeze-dried formulations, docetaxel prescription, preparation, filtration sterilization, in addition to the original heat, freeze-drying of the eutectic point, vacuum, temperature, time etc., were studied. As a result, 8% mannitol as shaped excipients was selected, forming good preparation structure. Stability of prescription was also studied. The entire preparation process, the filling process should be completed within six hours. By comparing pyrogen elimination through activated carbon and ultrafiltration, we selected ultrafiltration as a means of pyrogen elimination. Applying 0.22u selected aperture PVDF membrane filter for sterilization, the sample was bottled in 100 degree zone. Vials were washed by using ultrasound, furthur were exposed in 300℃for drying and sterilization. Rubber plug were rinsed for injection usage, than exposed in heat steam for sterilization and dried by hot air. Eutectic point was determined by electical resistance method, the measured eutectic point was about -13 ~ -15℃. Freeze-dried curve was carried out on 2m2 freeze dryers in the tests; in order to achieve the sublimation of the surface vapor pressure and obtain large pressure difference between the vapor pressure and freeze drier, the vacuum degree of vacuum drier was controlled on 20±4Pa. By adjusting shelf temperature, in a drying process to ensure that the product temperature does not exceed the temperature of eutectic point, as far as possible to raise the shelf temperature, to improve the efficiency of sublimation. After the completion of drying, residual moisture was about 10%, increasing shelf temperature to 25℃for a second drying, maintaining eight hours, detected the pressure difference during three minutes, ending freeze-drying when the difference was less than 2Pa. Vials were bottled in the freeze-dried equipment, then for packaging. Finally, samples were obtaind.Quality analysis: shape, identification, acidity, particulate matter, weight differences and pyrogen were investigated on three batches of samples. The results were mmet the quality requirements. We verified the methodology of aseptic testing methods, and used high-performance liquid chromatography for content determination, the method was free of influence of excipents and solvents, has good precision, durability, recovery rate and accurate, showed it is suitable for content determination. Employing high-performance liquid chromatography system for separating the relative materials, self-controled method to determine the amount of related substances, test results meet the quality requirements. Also we used gas chromatography to measure residual ethanol, results were in line with quality requirements.Through the above-mentioned work, the preparation was to be a viable production process. The analysis of injection lyophilized docetaxel preparation process and the quality were accomplished.
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