Benita S, Zouai O, Benoit J P
J Pharm Sci. 1986 Sep;75(9):847-51. doi: 10.1002/jps.2600750905.
5-Fluorouracil:carnauba wax microspheres were prepared using a meltable dispersion process with the aid of a surfactant as a wetting agent. It was noted that only hydrophilic surfactants were able to wet the 5-fluorouracil and substantially increased its content in the microspheres. No marked effect was observed in the particle size distribution of the solid microspheres as a function of the nature of the surfactant. Increasing the stirring rate in the preparation process decreased, first, the mean droplet size of the emulsified melted dispersion in the vehicle during the heating process, and, consequently, the mean particle size of the solidified microspheres during the cooling process. 5-Fluorouracil cumulative release from the microspheres followed first-order kinetics, as shown by nonlinear regression analysis. Although the kinetic results were not indicative of the true release mechanism from a single microsphere, it was believed that 5-fluorouracil release from the microspheres was probably governed by a dissolution process, rather than by a leaching process through the carnauba wax microspheres.
5-氟尿嘧啶：巴西棕榈蜡微球采用可熔分散法制备，借助一种表面活性剂作为润湿剂。注意到只有亲水性表面活性剂能够润湿5-氟尿嘧啶，并显著提高其在微球中的含量。未观察到固体微球的粒径分布随表面活性剂性质有明显变化。在制备过程中提高搅拌速率，首先会降低加热过程中载体中乳化熔融分散体的平均液滴尺寸，进而降低冷却过程中固化微球的平均粒径。非线性回归分析表明，5-氟尿嘧啶从微球中的累积释放遵循一级动力学。尽管动力学结果并不表明单个微球的真实释放机制，但据信5-氟尿嘧啶从微球中的释放可能受溶解过程控制，而非通过巴西棕榈蜡微球的浸出过程。
