Serum morphine concentrations after buccal and intramuscular morphine administration.

Abstract

1. This study compared serum concentrations of morphine after administration of a buccal tablet (25mg) with those after intramuscular injection (10mg). 2. Buccal morphine was administered to eleven healthy volunteers and intramuscular morphine was given to five preoperative surgical patients. Serum morphine concentrations were assayed by high performance liquid chromatography (h.p.l.c.) in samples taken up to 8 h after drug administration. 3. Mean maximum morphine concentrations were eight times lower after buccal administration than after intramuscular injection and occurred at a mean of 4 h later. Individual morphine concentration‐time profiles showed marked interindividual variability after administration of the buccal tablet, consistent with considerable variation in tablet persistence time on the buccal mucosa.

Clinical Pharmacokinetics of Drugs Administered Buccally and Sublingually

“…A sustained release buccal tablet formulation of morphine was previously claimed to result in a marked increase in bioavailability compared with other methods of delivery (Bell et al 1985). This has not been substantiated by recent work (Fisher et al 1987;Osborne et al 1990), in that the overall bioavailability is similar to that from other nonparenteral routes (27.0 ± 11.2%; Osborne et al 1990). Furthermore, the sustained release buccal formulation yields very low plasma morphine concentrations with a lag time of 30 min to 4h, due to the extremely prolonged dissolution of the tablet (Osborne et al 1990).…”

Noninvasive drug delivery

“…Buccal and sublingual morphine administration has been extensively utilized because of the need for nonparenteral methods of morphine administration in patients with cancer. 35,[38][39][40][41][42][43][44][45] Buccal and sublingual morphine are useful when oral morphine is impractical (patient with nausea and vomiting, difficulty swallowing, or GI problems) and parenteral injections are difficult and painful (patients with bleeding disorders, inaccessible veins, or muscle wasting). Concentrated concentrations of morphine solution (10-20 mg/mL) are now available for sublingual administration.…”

“…OTFC bioavailability is similar to buprenorphine (55%), 48 but much greater than buccal morphine and other opioids with low lipid solubility. 35,40 OTFC was initially developed because of the need for less painful and frightening methods of obtaining analgesia in children. Procedure pain remains an enormous source of distress for children with cancer.…”

Review: The Application of Liquid Chromatography Electrochemical Detection for the Determination of Drugs of Abuse

“…Table 2 summaries reported LC ED application for the determination of alkaloids. Fisher et al [62] have compared the serum concentrations of morphine after administration of a buccal tablet (25 mg) with those obtained after intramuscular injection (10 mg). Buccal morphine was administered to eleven healthy volunteers and intramuscular morphine was given to five preoperative surgical patients.…”