Enhanced bioavailability of morphine after rectal administration in rats

Autor: Tadanori Itakura, Kohji Naora, Kikuo Iwamoto, Yoshihiro Katagiri, Yasuhiro Kanba
Rok vydání: 1988
Předmět:
Zdroj: Journal of Pharmacy and Pharmacology. 40:879-881
ISSN: 2042-7158
0022-3573
Popis: Plasma morphine levels and the area under the plasma concentration-time curve (AUC) after i.v. (10 mg kg−1), p.o. (100 mg kg−1) and rectal (unrestricted or restricted to 1.5 cm from the anus, 10 mg kg−1) administration of morphine hydrochloride were determined in 10 or 11-week-old male Wistar rats to compare bioavailability of morphine after the rectal dosage with that after oral administration. The AUC value after oral administration (15 μg min mL−1), which was normalized by the dose, was only one-tenth of that after i.v. dosing (151 μg min mL−1). In contrast, the AUC after rectal administration (unrestricted, 133 μg min mL−1; restricted, 142 μg min mL−1) was almost comparable with that after i.v. administration. From the comparison of these AUC values, the extent of systemic availability of morphine after rectal (unrestricted or restricted) and p.o. administration was estimated to be approximately 90 and 10%, respectively.
Databáze: OpenAIRE