呋喃妥因缓释微丸的人体内药物动力学研究

Pharmacokinetic Study on the Nitrofurantoin Sustained-release Pellets in Healthy Volunteers

采用高效液相色谱法测定单剂量口服呋喃妥因缓释微丸 (NF PE)和市售肠溶包衣片(NF TA)后的尿药浓度 ,研究该药缓释微丸的药动学参数和生物利用度 ,并考察其体内外相关性 .结果表明 :呋喃妥因缓释微丸相对于肠溶包衣片的生物利度为 130 2 5 % ;供试品呋喃妥因缓释微丸和对照品肠溶包衣片的消除速率常数分别为 0 44 98h-1、0 82 0 2h-1,前者的消除半衰期(t1/ 2 )及平均滞留时间 (MRT)均较后者有所延长 ;该药体内吸收率与体外溶出度相关性显著 (r =0 972 4) .

To study the pharmacokinetics and relative bioavailability of nitrofurantoin sustained-release pellets(NF-PE),NF-PE the market enteric coated tablets(NF-TA) were given according to a crossover design.The concentration in urine was determined by HPLC.The elemination rate constants of NF-PE and NF-TA were 0 449 8 and 0 820 2 respectively.Compared with the market tablets(NF-TA),the bioavailability of NF-PE was enhanced to 135 02%, and T 1/2 and MRT were prolonged.The in vivo and in vitro correlation of NF-PE is marked( r = 0 972 4 ).