Abstract
Simvastatin(SMV) is poorly soluble drug classified as belonging to Class II of BiopharmaceuticsClassification System. Common approach to improve apparent solubility of drugsis production of amorphous solid dispersions (ASD) by means of spray drying(SD) or hot-melt extrusion. Spray drying of low-glass transition temperature(Tg) ASDs is challenging due to the risk of material being exposed to SD outlettemperatures close to its Tg which may result in melting of ASD and subsequentcrystallisation of amorphous drug. It was hypothesised that addition ofeasily-crystallising material to ASD will improve its SD processability. Inaddition, it was hypothesised that produced ternary solid dispersions (TSD)composed of amorphous composite of drug and the polymer (PVP K17, 55 and 150) andcrystalline, soluble nanoparticles (NaCl) will improve dissolution of TSDtablets. The dissolution of SMV fromTSDs was faster compared with that of binary solid dispersion in case of SMV-TSDsproduced with PVP K55 and 150. The tabletabilityassessment showed increase in compression led to increase in tensile strengthand decrease in porosities of SDs tablets.
Highlights
SUMMARYSimvastatin (SMV) is a poorly soluble drug classified as belonging to Class II of the Biopharmaceutics Classification System
Transformation of the solid state of a drug from crystalline into the amorphous form is commonly used to improve its apparent solubility
Spray drying of relatively low-Tg amorphous solid dispersions (ASD) is challenging due to the risk of material being exposed to process outlet temperatures close to its Tg, Abdalmaula et al (2019) BJPharm, 4(1), S16-17 which may result in melting of the ASD and subsequent crystallisation of the amorphous drug
Summary
Simvastatin (SMV) is a poorly soluble drug classified as belonging to Class II of the Biopharmaceutics Classification System. A common approach to improve the apparent solubility of drugs is the production of amorphous solid dispersions (ASD) by means of spray drying (SD) or hot-melt extrusion. Spray drying of lowglass transition temperature (Tg) ASDs is challenging due to the risk of material being exposed to SD outlet temperatures close to its Tg which may result in melting of ASD and subsequent crystallisation of amorphous drug. It was hypothesised that addition of an -crystallising material to ASD will improve its SD processability. It was hypothesised that ternary solid dispersions (TSD) composed of an amorphous composite of drug and the polymer (PVP K17, 55 and 150) and crystalline, soluble nanoparticles (NaCl) will improve dissolution of TSD tablets. The dissolution of SMV from TSDs was faster compared with that of binary solid dispersions in the case of SMV-TSDs produced with PVP K55 and 150. The tabletability assessment showed an improvement in compression leading to an increase in tensile strength and decrease in the porosities of SD tablets
Sign-in/Register to view highlights & summary Sign-in/Register to access full text options 
Free) 
Talk to us
Join us for a 30 min session where you can share your feedback and ask us any queries you have
Schedule a call
