Curing mechanism of flexible aqueous polymeric coatings
The objective of this study was to explain curing phenomena for pellets coated with a flexible polymeric coating based on poly(vinyl acetate) (Kollicoat® SR 30D) with regard to the effect of starter cores, thickness of drug layer, adhesion of coating to drug-layered-cores as well as coating properties. In addition, appropriate approaches to eliminate the curing effect were identified. Sugar or MCC cores were layered with the model drugs carbamazepine, theophylline, propranolol HCl, tramadol HCl and metoprolol HCl using HPMC (5 or 25% w/w, based on drug) as a binder. Drug-layered pellets were coated with Kollicoat® SR 30D in a fluidized bed coater using TEC (10% w/w) as plasticizer and talc (35–100% w/w) as anti-tacking agent. Drug release, pellet properties (morphology, water uptake-weight loss and osmolality) and adhesion of the coating to the drug layer were investigated as a function of curing at 60 °C or 60 °C/75% RH for 24 h. The film formation of the aqueous dispersion of Kollicoat® SR 30D was complete, and therefore, a strong curing effect (decrease in drug release) at elevated temperature and humidity (60 °C/75% RH) could not be explained by the well-known hydroplasticization and the further gradual coalescence of the colloidal polymer particles. According to the provided mechanistic explanation, the observed curing effect was associated with (1) high flexibility of coating, (2) adhesion between coating and drug layer, (3) water retaining properties of the drug layer, and (4) osmotically active cores. Unwanted curing effects could be minimized/eliminated by the addition of talc or/and pore-forming water soluble polymers in the coating, increasing binder amount or applying an intermediate coating, by increasing the thickness of drug layer or using non-osmotic cores. A new insight into curing phenomena mainly associated with the adhesion between drug layer and coating was provided. Appropriate approaches to avoid unwanted curing effect were identified.