シスプラチン坐剤の調製とその薬剤学的性質

Abstract

Cisplatin suppositories were prepared with polyethylene glycol bases (PEG 1500, PEG 4000). The suppository released swiftly almost 100% of cisplatin within 90 minutes. On single intravenous administration to rabbits, blood levels of platinum decreased in a bi-exponential manner; the half lives of the α-and β-phase were 0.31 hours and 43.86 hours, respectively. On rectal administration of cisplatin suppository, the plasma concentration curve of platinum showed twocompartment model including the first-order absorption proccess.The absolute bioavailability of cisplatin suppository (AUC 0→48 suppo/AUC 0→48 i.v.×100%) was 24.5%.