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Titolo:
Pharmacokinetics of midazolam: comparison of sublingual and intravenous routes in rabbit
Autore:
Odou, P; Barthelemy, C; Chatelier, D; Luyckx, M; Brunet, C; Dine, T; Gressier, B; Cazin, M; Cazin, JC; Robert, H;
Indirizzi:
Fac06harmaceut & Biol Sci, Dept Clin Pharm Pharmacokinet & Pharmacol, F-590 Fac Pharmaceut & Biol Sci Lille France F-59006 okinet & Pharmacol, F-590
Titolo Testata:
EUROPEAN JOURNAL OF DRUG METABOLISM AND PHARMACOKINETICS
fascicolo: 1, volume: 24, anno: 1999,
pagine: 1 - 7
SICI:
0378-7966(199901/03)24:1<1:POMCOS>2.0.ZU;2-F
Fonte:
ISI
Lingua:
ENG
Soggetto:
CHILDREN; INFUSION;
Keywords:
midazolam; 9 hydroxy-midazolam; sublingual route; HPLC; radio-receptor assay;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Life Sciences
Citazioni:
28
Recensione:
Indirizzi per estratti:
Indirizzo: Odou, P Fac Pharmaceut & Biol Sci, Dept Clin Pharm Pharmacokinet & Pharmacol, 3 Rue Fac Pharmaceut & Biol Sci 3 Rue Prof Laguesse,BP 83 Lille FranceF-59006
Citazione:
P. Odou et al., "Pharmacokinetics of midazolam: comparison of sublingual and intravenous routes in rabbit", EUR J DRUG, 24(1), 1999, pp. 1-7

Abstract

In France, the legal routes used to administer midazolam to a patient are intravenously and intramuscularly. For anaesthetists, these routes are not well adapted to paediatric use; they lead to pain at injection site and stress on children. The sublingual route should be a good compromise between stress and quick efficiency. We have developed a sublingual tablet of midazolam. The aim of the present investigation is to compare the pharmacokineticparameters of midazolam tablets administered by the sublingual and intravenous routes in 6 rabbits to determine the bioequivalence between these routes. We have estimated the 1-hydroxy-midazolam serum level by difference between RRA and HPLC values. By the sublingual route, midazolam absorption is substantial and fast. Thestatistical analysis, on data obtained with HPLC dosage, shows no significant difference between pharmacokinetic parameter values calculated after intravenous and sublingual administration (0.5 mg). The absolute bioavailability was close to 100%. With RRA dosage, however, AUCs were greater than those obtained by HPLC dosage (174%). 1-hydroxy-midazolam seems to have a great importance in BZD activity. To estimate the bioequivalence between intravenous and sublingual midazolam administration, it is necessary to take intoaccount the active metabolites.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 25/01/20 alle ore 09:47:29