挤出造粒、气流包衣法制备包衣微粒剂.Ⅵ.氟尿嘧啶肠溶微粒的制备和药动学研究

Preparation of Micro-granules with Extrusion and Airflow Coating Method .Ⅵ. Preparation and Pharmacokinetics of Enteric Coated Fluorouracil Micro-granules

用挤出造粒、气流包衣技术制备氟尿嘧啶肠溶微粒。体外试验表明,其在0.1mol/L盐酸中2h内不释放,在pH6.8条件下30min释放率大于96%。大鼠体内药物动力学研究表明口服氟尿嘧啶肠溶乳糖微粒后t1/2为(0.63±0.13)h,AUC0→6h为(1215.7±255.3)ng·h-1·ml-1,均优于氟尿嘧啶水溶液[t1/2为(0.35±0.03)h,AUC0→6h为(851.6±84.9)ng·h-1·ml-1]。

Enteric coated fluorouracil micro-granules were prepared with extrusion, spheronization and airflow coating method. The in vitro release of prepared micro-granules containing lactose or sodium chloride showed that fluorouracil was not released in 0.1mol/L hydrochloric acid for 2h, while in pH 6.8 phosphate buffer solution at 30min release was above 96%. The results of pharmacokinetics study in SD rats indicated that tl/2 （0.63±0.13）h and AUC0→6h （1215.7±255.3）ng.h-1.ml-1 of the enteric-coated micro-granules containing lactose were better than those of the fluorouracil solution [tl/2 （0.35±0.03） h, A UC0→6h （851.6±84.9） ng.h-1.ml-1].