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Bioavailability study of zolmitriptan sublingual tablets on sheep model
2nd World Congress on Bioavailability & Bioequivalence: Pharmaceutical R & D Summit-2011 and International Conference on Pharmaceutics & Novel Drug Delivery Systems
06-08 June 2011, Las Vegas, USA

Ziya BAYRAK, Cetin TAS, Umut TASDEMIR, Halil EROL, Cansel KOSE OZKAN, Ayhan SAVASER and Yalcin OZKAN

Scientific Tracks Abstracts: JBB

Abstract:

S ublingual tablet administration has an important fi eld in therapy because of taking immediate pharmacologic response, bypass of fi rst pass eff ect and so high bioavailability and patient satisfaction. Zolmitriptan is a good candidate as an active pharmaceutical ingredient in sublingual tablet formulations because of its freely soluble in water, exposing fi rst pass eff ect and high potency impact. Sublingual tablet formulations were prepared with diff erent polymers such as hydroxypropyl methyl cellulose (HPMC), chitosan and sodium carboxy methyl cellulose (CMCNa) with direct compression method. Th e eff ect of polymers has been investigated on in vitro and in vivo drug studies. In vitro studies show that all formulations met the pharmacopeial criteria. Th e optimum formulations for diff erent ratios of polymers were chosen for in vivo bioavailability studies on sheep model. A simple solution formulation of zolmitriptan was used for in vivo studies to calculate relative bioavailability of sublingual tablets. Th e results of in vivo studies showed that formulation containing 5% chitosan, has the maximum C max and AUC and minimum t max values (p < 0.05). Increasing the contact time with the sublingual mucosa with a mucoadhesive polymer improve sublingual bioavailability and result in more predictable plasma levels of the drug, leading to better therapeutic effi cacy. As a result sublingual tablet administration of zolmitriptan formulated with appropriate excipients and especially with chitosan seems promising alternative to traditional routes

Biography :

Ziya Bayrak has begun doctoral studies in 2009. He continues doctorate education in Gulhane Military Medical Academy, Department of Pharmaceutical Technology. The main fi elds of research area are tablets, drug absorption and penetration from mucosa and skin