Disposition of Morphine after Oral Administration of Morphine Hydrochloride Tablets and Solution in Preoperative Cancer Patients.

Accession number;03A0109471
Title;Disposition of Morphine after Oral Administration of Morphine Hydrochloride Tablets and Solution in Preoperative Cancer Patients.
Author; MIZUGUCHI TADANOBU (San'obyoin Kanwakeaka)
Journal Title;Clinical Pharmacology and Therapy
Journal Code:L1701A
ISSN:0917-3994
VOL.13;NO.1;PAGE.15-24(2003)
Figure&Table&Reference;FIG.2, TBL.2, REF.21
Pub. Country;Japan
Language;Japanese
Abstract;Disposition of morphine after oral administration of morphine hydrochloride tablets and solution to preoperative patients with cancer was investigated and following results were obtained. 1) Although morphine from tablets showed somewhat delayed absorption behavior compared with solution, no significant difference in the plasma concentration at any time was observed. There was also no significant difference in the areas under the plasma concentration-time curve (AUC) between tablets and solution. 2) There was no difference in the plasma concentration-time curve of morphine metabolites, morphine-3-glucuronide (M-3-G) and morphine-6-glucuronide (M-6-G), between tablets and solution. Maximum plasma concentrations (Cmax) of M-3-G and M-6-G were 9.6-52.0 and 2.2-10.7 folds higher than that of morphine, respectively. The molar ratio between AUC for M-3-G and morphine was the range of 8.6 to 28.0. In the case of M-6-G, the corresponding value was the range of 1.8 to 5.0. These results indicate that morphine is remarkably metabolized to M-3-G and M-6-G with large intersubject variation when orally received, although there is no essential difference in the bioavailability between tablets and solution. (author abst.)