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Titolo:
DEVELOPMENT OF MIDAZOLAM SUBLINGUAL TABLETS - IN-VITRO STUDY
Autore:
ODOU P; BARTHELEMY C; ROBERT H;
Indirizzi:
FAC PHARMACEUT & BIOL SCI,DEPT CLIN PHARM,3 RUE PROF LAGUESSE,BP 83 F-59006 LILLE FRANCE
Titolo Testata:
European journal of drug metabolism and pharmacokinetics
fascicolo: 2, volume: 23, anno: 1998,
pagine: 87 - 91
SICI:
0378-7966(1998)23:2<87:DOMST->2.0.ZU;2-V
Fonte:
ISI
Lingua:
ENG
Soggetto:
PHARMACOKINETICS;
Keywords:
MIDAZOLAM; SUBLINGUAL TABLETS; PASSIVE DIFFUSION; DISSOLUTION; IN VITRO RELEASE;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Citazioni:
11
Recensione:
Indirizzi per estratti:
Citazione:
P. Odou et al., "DEVELOPMENT OF MIDAZOLAM SUBLINGUAL TABLETS - IN-VITRO STUDY", European journal of drug metabolism and pharmacokinetics, 23(2), 1998, pp. 87-91

Abstract

Midazolam is a benzodiazepine with short elimination half-life, used as induction or continuous agent for general anesthesia. At present, only injectable solution is available from French hospital pharmacies. The aim of the study is the development of 5 mg midazolam sublingual tablets to realize a short general anesthesia without intravenous or intramuscular injection. Incorporation of citric acid in the tablet formulation leads to an increase of dissolution rates of active drug, but a decrease of diffusion through lipid membranes is observed with 10 mgof citric acid when using the Dibbern's Resomat three phases apparatus. One explanation of this result is that midazolam (pKa = 6.1) in presence of 10 mg of citric acid is ionised. The ionised form, more hydrophilic, cannot cross the artificial lipid membrane and therefore the diffusion decreases. On the other hand, the decrease of diffusion's rate, when pH increases, is explained by the precipitation of midazolam at pH higher than 6. A compromise between dissolution and diffusion results leads us to choose the sublingual formulation containing 5 mg of citric acid per tablet.

ASDD Area Sistemi Dipartimentali e Documentali, Università di Bologna, Catalogo delle riviste ed altri periodici
Documento generato il 28/01/20 alle ore 14:54:17