| Title | Triprotic acid-base microequilibria and pharmacokinetic sequelae of cetirizine. | | Author(s) | Marosi A, Kovács Z, Béni S, Kökösi J, Noszál B | | Institution | Department of Pharmaceutical Chemistry, Semmelweis University, Research Group of Drugs of Abuse and Doping Agents, Hungarian Academy of Sciences, Budapest H-1092, Hogyes Endre u. 9, Hungary. | | Source | Eur J Pharm Sci 2009 Jun 28; 37(3-4):321-8. | | Abstract | (1)H NMR-pH titrations of cetirizine, the widely used antihistamine and four related compounds were carried out and the related 11 macroscopic protonation constants were determined. The interactivity parameter between the two piperazine amine groups was obtained from two symmetric piperazine derivatives. Combining these two types of datasets, all the 12 microconstants and derived tautomeric constants of cetirizine were calculated. Upon this basis, the conflicting literature data of cetirizine microspeciation were clarified, and the pharmacokinetic absorption-distribution properties could be interpreted. The pH-dependent distribution of the microspecies is provided. | | Language | eng | | Pub Type(s) | Journal Article
Research Support, Non-U.S. Gov't
| | PubMed ID | 19491022 |
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