오메프라졸 함유 직장좌제의 약물속도론적 연구

Pharmacokinetics of Omeprazole from Rectal Suppositories

The pharmacokinetics and relationship between in vitro dissolution and in vivo fraction absorbed were investigated after intravenous(iv) injection of omeprazole(OMZ), oral administration of OMZ capsules and rectal administration of 8 types of suppositories. The plasma concentration of OMZ (Cp)-time (t) curve after iv. administration fitted a two-compartment open model and the equation which best fitted the p kinetics of OMZ was Cp = 13.936 e-8.78t + 2.973 e-0.716t. The bioavailabilities of OMZ in Witepsol H15 base (Supp-2) and PEG 4000 base (Supp-6) suppositories were 40.7% and 33.4%, respectively, which are higher(p<0.001) than 13% of oral administration of capsule. The avoidance fractions of the first-pass metabolism for Supp-2 and Supp-6 suppositiories were 31.8% and 23.4%, respectively, suggesting that the rectal application of OMZ may be a more adequate route of administration than oral one.