Kinetic modeling in pharmaceutical industry

In vitro ispitivanje oslobađanja djelatne tvari nalazi sve veću primjenu u farmaceutskoj industriji pri razvitku kako inovativnih, tako i generičkih lijekova. Djelatna tvar može se oslobađati difuzijskim mehanizmom ili erozijom, te može imati trenutni, produženi ili kontrolirani učinak. Ispitivanje se provodi propisanim metodama, specifičnim za svaku djelatnu tvar. Rezultati se opisuju statističkim metodama, metodama neovisnima o modelu te metodama ovisnima o modelima. U ovom radu ispitano je otpuštanje lijeka za reguliranje srčane aritmije, dronedaron hidroklorida, iz dva različita pripravka: mikrokapsula dobivenih sušenjem raspršivanjem u kojima je dronedaron obložen arapskom gumom, te peletama pripremljenim od mikrokristalne celuloze na koje je dronedaron nanesen impregnacijom u vakuumu. Prema rezultatima ispitivanja, otpuštanje dronedarona s obje vrste pripravka može se prikladno opisati Weibullovim modelom. Također, profil otpuštanja dronedarona iz mikrokapsula serije GA 60 pokazao se najsličniji profilu otpuštanja dronedarona iz komercijalnih Multaq tableta što pokazuje njihov potencijal kao nosača dronedaron hidroklorida.In vitro release of the active substance is commonly used in the pharmaceutical industry in the development of both, innovative and generic drug. The active substance can be released by a diffusion mechanism or erosion mechanism and can have immediate, delayed or controlled release. Dissolution test are carried out according to prescribed methods, specific for each active substance and described in the pharmacopoeia. The results are described using statistical methods, model independent methods and model dependent methods. In this study the release of dronedarone hydrochloride, drug for regulation of cardiac arrhythmia, was investigated using two different formulations: microcapsules obtained by spray-drying were coated with gum arabic, and the pellets prepared from microcrystalline cellulose and impregnated in vacuum with dronedarone. According to test results, the release profiles of the drug, for both formulations, can be described using the Weibull model. Also, the release profile of the microcapsules GA 60 proved to be most similar to the release profile of the commercial Multaq tablets which shows their potential as dronedarone carrier