The systemic availability of meptazinol in man after oral and rectal doses |
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| Authors: | G. R. Murray O. Petitjean R. A. Franklin D. F. Graham J. H. Trouvin C. Jacquot |
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| Affiliation: | (1) Wyeth Laboratories, Taplow, Maidenhead, Berkshire, UK;(2) Hospital Avicenne, Bobigny, France;(3) Laboratoire de Pharmacodynamie et Pharmacocinetique, Université de Paris-Sud, Chatenay-Malabry, France;(4) Present address: Syntex Research Centre, Heriott-Watt University, Riccarton, Edinburgh, UK;(5) Present address: Sterling Research Group-Europe, Guildford Research Centre, Guildford, Surrey, UK;(6) Present address: Sterling Research Group-Europe, Alnwick Research Centre, Alnwick, Northumberland, UK |
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| Abstract: | Summary We have studied the pharmacokinetics of the centrally-acting analgesic meptazinol after oral and rectal administration to 15 healthy men. Each subject took a standard 200 mg tablet orally and Witepsol H12 suppositories containing 75, 100, and 150 mg of the drug in a cross-over design.Meptazinol plasma concentrations were measured by HPLC using fluorescence detection and the pharmacokinetics determined.The tmax values for the 100 mg and 150 mg suppositories (median =0.5 h) were statistically significantly shorter than for the tablet (median =1.13 h), suggesting that meptazinol was more rapidly absorbed via the rectal route.Despite substantial intersubject variation in Cmax the plasma concentrations after rectal dosage were higher than after oral administration. There was a statistically significant (p<0.001) improvement in systemic availability for each of the suppository doses (mean approximately 15.5% compared with the oral tablet (mean approximately 4.5%). |
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| Keywords: | meptazinol rectal and oral administration pharmacokinetics first-pass metabolism |
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