| Docetaxel is a new anti-tumor drug, especially effective for ovarian cancer, breast cancer, nonsmall-cell lung cancer, esophageal carcinoma etc. The marketed dosage form is injectable concentrated solution, which is unstable and with many kinds of Ads, such as body fluid retention, leukopenia, nausea, diarrhea, etc. We prepared the ODS of docetaxel, which can improve the stability and facilitate its storage and transport, and reduce its Ads. This text showed its preparation of solid dispersion and nanoemulsion and the optimization technology of formula composition and preparation, recomment the two kind of system by the study in vitro.In this study, we first establish HPLC analysis method of docetaxel: Agilent 1100 HPLC instrument, DiamonsilTM ODS column, mobile phase is the mixture of methanol,acetonitrile and water(34:42:24), flow rate was 1.0 mL·min-1, wavelength was at 323 nm, column temperature was at 25℃, and injection volumn was 20μL, the method was suitable for the analysis of docetaxel, the concentration and test results was linear correlation in a concentration range of 1.6～48.0μg·mL-1, the concentration of the daily precision was 0.19,0.20 and 0.40% and its concentration of interval daily precision was 0.67,0.55 and 0.47%; the quantitation concentration and detection concentration are 64.0 ng·mL-1 and 25.6 ng·mL-1; and specificity study showed its specificity was good and the reversed phase HPLC method was suitable for the analysis of the concentration of decetaxel.In this paper, the balance solubility in different medium, apparent oil/water partition coefficient, stability in the solutions with different pH value, and stability of it exposed to high temperature (40℃), high humidity and illumination were studied. The results indicated that balance solubility of docetaxel dissolved in the HC1 solution of 0.1 mol·L-1, distilled water, buffer solution of pH=6.8, 0.9% NaCl solution, mid-chain soybean oil and PEG400 were (2.51±0.08), (3.67±0.27), (3.43±0.09), (3.56±0.13), (1218.0±219.4) and (710.9±104.8)μg·mL-1, the Log P of docetaxel in n-octyl alcohol and cholorform were 3.06 and 1.15. the solubility of docetaxel in weak acid was not good, and which dissolved in alkaline solution and exposed to high temperature and high temperature and illumination was unstable.In the paper the identification of solid dispersion of docetaxel also was studied. The study indicated that the solid dispersion have been changed into mono phase system from double phase system, and the docetaxel present in the carriers with amorphism or molecular, which insured the drug could be dissolved quickly in gastrointestinal tract. The stability study of docetaxel solid dispersion indicated it was unstable when it was exposed to illumination, high temperature and high humidity, so its preparation must be stored protected from light and in cool and dryness. But result of long term stability showed that solid dispersion of doxacel/poloxamer188 was stable during the period of 30 days.In the study of docetaxel nanoemulsion, the mid chain soybean was as oil phase, and chose the RH-40 and PEG 400 as emulsifier and assistant emulsifier through establishing pseudo-ternary phase diagram; and selected the area of nanoemulsion by pseudo-ternary phase diagram, so the optimized formulation of pre-nanoemulsion enriched solution were 35% of MCT, 46.4% of RH-40 and 18.6% of PEG 400, the particle size of prenanoemulsion enriched solution diluted by HCl of 0.1 mol·L-1 , PBS buffer solution of pH=6.8 and distilled water were 59.2, 59.3 and 56.6 nm, but the particle size of prenanoemulsion enriched solution diluted by distilled water would not decrease with addition of distilled water, but PDI was changed from 0.224 into 0.109. The stability of nanoemulsion also be investigated, the results showed that nanoemulsion was stable for 10 days when it was exposed to illumination, high temperature and was stable for 3 months at room temperature.
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