抽象的

Formulation, In vitro and In vivo Evaluation of Taste Masked Rasagiline Orally Fast Disintegrating Tablets (ODTS)

Tansel Comoglu, Ozge Inal, Asli Kargili and Bilge Pehlivanoglu 

Orally disintegrating tablets (ODTs) have become a rapidly growing area in the pharmaceutical industry during the last decade. Drugs exhibit the advantage of good absorption from the oral mucosa or intending for immediate pharmacological action can be formulated as ODT dosage forms. Rasagiline, a second generation, selective, irreversible inhibitor of mono amine oxidase type B drug, is primarily responsible for inactivation of dopamine in central nervous system (CNS) and has been used to treat long term Parkinson’s disease. As Rasagiline undergoes extensive first-pass metabolism resulting in low bioavailability, ODT dosage form can be a good alternative.

In this study, Rasagiline ODT formulations were developed using Crospovidone, Ac-Di-Sol and Parteck® ODT superdisintegrants in two different concentrations, and also the unpleasant taste of the Rasagiline was improved with using a polymer; Eudragit EPO. ODTs were evaluated by means of in vitro quality control tests and an in vivo animal study was performed to evaluate the bioavailability of the Rasagiline ODT versus conventional tablet.

As a result, precompressional parameters for Rasagiline ODTs indicated fair flow properties. All Rasagiline ODT formulations satisfied the requirements of FDA for rapid dissolving tablets and allowed more than 85% drug to be dissolved within 30 minutes. Among the investigated superdisintegrants; Ac-Di-Sol is found more effective (7.6%) for its enhancing the rate and water uptake effect and dissolution. Thus, it can be concluded that Rasagiline ODTs may be an alternative solution to overcome the low bioavailability problems occurred with conventional therapy.