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Epilepsia. 2000 Jul;41(7):850-3.

Rectal absorption of lamotrigine compressed tablets.

Author information

1
Experimental and Clinical Pharmacology and Medicinal Chemistry, Epilepsy Research and Education Program, College of Pharmacy, University of Minnesota, Minneapolis, Minnesota 55455, USA. birnb002@tc.umn.edu

Abstract

PURPOSE:

Interruption of oral drug administration poses a significant clinical problem for antiepileptic drugs that have no parenteral formulation. If a drug is absorbed rectally, rectal administration can be a useful alternative when the oral route of administration is not possible. The purpose of this study was to compare the single-dose pharmacokinetics of lamotrigine (LTG) compressed tablets after rectal and oral administration in healthy volunteers.

METHODS:

A single LTG compressed tablet (100 mg) was administered orally and rectally to 12 volunteers in this single-dose, two-period, crossover study with a 2-week washout between doses. For rectal administration, tablets were crushed and suspended in 10 mL of water. Plasma samples were collected from 0 to 120 hr after each dose and analyzed for LTG by an HPLC method developed for this investigation.

RESULTS:

LTG plasma concentrations were lower after rectal administration versus oral administration. The average area under the curve was 28.90 +/- 9.5 microg/mL/hr after rectal administration and 51.71 +/- 19.2 microg/mL/hr after oral administration. The average maximum LTG concentration was 0.53 +/- 0.14 microg/mL after rectal administration and 1.45 +/- 0.35 microg/mL after oral administration. The relative bioavailability for LTG compressed tablets was 0.63 +/- 0.33 for rectal administration. There were no drug-related rashes or serious side effects.

CONCLUSIONS:

LTG suspension prepared from LTG compressed tablets is absorbed rectally, although not to the same extent or rate as when given orally.

PMID:
10897156
[Indexed for MEDLINE]
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