DEVELOPMENT OF ORODISPERSIBLE FILMS PRODUCED BY HOT-MELT EXTRUSION FOR POORLY WATER SOLUBLE DRUGS

Abstract

THE ORODISPERSIBLE FILM (ODF) IS A MEDICATED SHEET THAT DISPERSES UPON CONTACT WITH THE ORAL CAVITY AND RELEASES THE DRUG FOR OROMUCOSAL ABSORPTION. IT CAN BE MANUFACTURED AS SELF-CONTAINING AMORPHOUS SOLID DISPERSION (ASD) SYSTEMS WITH SOLUBILISING POLYMERS TO AFFORD HIGH DRUG LOADING AND ENHANCE THE DISSOLUTION OF POORLY WATER SOLUBLE DRUGS. THE EFFECT OF SOL OR KOL IN COMBINATION WITH A FILM-FORMING POLYMER ON THE MECHANICAL PROPERTIES AND DRUG RELEASE RATES OF INDOMETHACIN (IDM) ODFS PREPARED BY HOT MELT EXTRUSION (ME) IN COMPARISON TO SOLVENT-CASTING WAS INVESTIGATED. THE FILM-POLYMER SYSTEM OF HPC:KOLLIDON/SOLUPLUS AT 3:1 ENABLED DESIRABLE MECHANICAL PROPERTIES AND WAS ROBUST TO ACCOMMODATE UP TO 30% (W/W) DRUG LOAD OF IDM AS A STABLE ASD WITH 4-WEEK STABILITY. WITH THIS OPTIMISED FORMULATION, A DRUG LOADING OF 50% (W/W) WAS ACHIEVED WITH HPC FORMULATIONS WITH STABLE SUPERSATURATION SOLUBILITY COMPARED TO PURE AMORPHOUS IDM AND WAS STABLE OVER 4 WEEKS.