Microencapsulation of active ingredient

U farmaceutskoj industriji se velika pozornost počela obraćati na odgođeno otpuštanje lijeka. Većina aktivnih tvari se otpušta odmah iz lijeka te je njihovo djelovanje trenutno, zbog toga se nastoji pronaći formulacija koja će kontrolirano otpuštati aktivnu tvar i tako djelovati kroz duže vrijeme u tijelu. Bitno je i da je lijek stabilan i otpušta aktivnu tvar na točno određenom području. U ovom radu je ispitana djelotvornost mikroinkapsuliranja dronedaron hidroklorida s arapskom gumom kao i njegovo nanošenje na nosač, mikrokristalnu celulozu. Dronedaron hidroklorid je lijek za regulaciju srčane aritmije koji svoju komercijalnu primjenu pronalazi u tabletama Multaq 400 mg. Eksperimenti su provedeni u laboratorijskom sušioniku s raspršivanjem, Büchi B-290. Mijenjani su protoci zraka za raspršivanje od 30 do 60 %. Morfologija dobivenih uzoraka ispitana je pomoću pretražnog elektronskog mikroskopa (SEM). Kinetika otpuštanja je opisana pomoću matematičkih modela. Rezultati su pokazali da je iskorištenje dronedarona veće kod mikroinkapsuliranja arapskom gumom nego kod nanošenja na nosač. Najveće iskorištenje dronedarona dobiveno je za uzorke GA 40 i MCC 50. SEM mikrografije su potvrdile da su dobivene mikrokapsule dronedarona s arapskom gumom, a na uzorcima MCC vidljive su čestice dronedarona deponirane na površini. Otpuštanje dronedarona je vrlo brzo i neujednačeno u odnosu na komercijalnu tabletu. Najbolje rezultate daje uzorak s arapskom gumom koji je pripremljen pri protoku od 60 %. Za taj uzorak su dobivene vrlo sitne i sferične mikrokapsule.In recent years, pharmaceutical industry pays a great attention to the delayed drug release from different dosage forms. Most of the active substances are released immediately from the dosage form; therefore it is challenging to find a formulation for the controlled release as well as prolonged effectiveness in the body. It is important that the drug is stable and releases the active substance to a targeting area. This paper deals with microencapsulation efficiency of dronedarone hydrochloride with gum arabic, as well as the efficiency of his imobilization onto drug carrier, microcrystal cellulose. Dronedarone hydrochloride is a drug for regulation of cardiac arrhythmia, which finds its commercial application in Multaq 400 mg tablets. The experiments were performed in the laboratory spray-dryer, Büchi B-290. Flow rates of atomizing air were changed from 30 to 60 %. Scanning electron microscopy was used to characterize the morphology of prepared samples. Release kinetics is described by mathematical models. From the results it is evident that utilization is much higher in microencapsulation then in deposition onto carrier. Best results were obtained for GA 40 and MCC 50 samples. SEM micrographs confirmed that microcapsules of dronedarone and gum arabic were prepared. It was also confirmed that dronedarone was successfully deposited onto the surface of cellulose carrier. The release of the drug is very fast and uneven compared to the commercial tablet Multaq. Best results are obtained with microcapsules which have been prepared at an air flow of 60 %. Microcapsules obtained at those process conditions are very small and mostly spherical