The characterization and dissolution performances of spray dried solid dispersion of ketoprofen in hydrophilic carriers

摘要

Abstract Solid dispersion is one of the most promising strategies to improve oral bioavailability of poorly soluble API. However, there are inconsistent dissolution performances of solid dispersion reported which entails further investigation. In this study, solid dispersions of ketoprofen in three hydrophilic carriers, i.e. {PVP} K30, {PVPVA} 6:4 and {PVA} were prepared and characterized. Physical characterization of the physical mixture of ketoprofen and carriers shows certain extent of amorphization of the API. This result is coinciding to evaluation of drug–polymer interaction using ATR-FTIR whereby higher amorphization was seen in samples with higher drug–polymer interaction. {XRPD} scanning confirms that fully amorphous solid dispersion was obtained for {SD} {KTP} {PVP} {K30} and {PVPVA} system whereas partially crystalline system was obtained for {SD} {KTP} PVA. Interestingly, dissolution profiles of the solid dispersion had shown that degree of amorphization of {KTP} was not directly proportional to the dissolution rate enhancement of the solid dispersion system. Thus, it is concluded that complete amorphization does not guarantee dissolution enhancement of an amorphous solid dispersion system.