Effects of the centrifugal coating and centrifugal fluidized bed coating methods on the physicochemical properties of sustained-release microparticles using a multi-functional rotor processor

摘要

The purpose of the present study was to examine the effect of coating processes on the physicochemical properties of sustained-release microparticles prepared by centrifugal coating (CC)and centrifugal fluidized bed coating (CFC) using a multi-functional rotor processor. Acetaminophen (APAP)-loaded microparticles (DP) were coated with 30% w/w aqueous polymer dispersion of Eudragit~R RS (RS) by CC or CFC methods with the apparatus until a dry polymer weight gain of 30%, 60%, 150% and 200% w/w was achieved, and these coated microparticles were abbreviated as CC-DP-RS and CFC-DP-RS, respectively. Both coated microparticles had similar physicochemical properties, but some differences in the drug dissolution behaviors of CC-DP-RS and CFC-DP-RS at lower coating levels were observed. That is, the coated microparticles prepared by CC showed faster release than that by CFC. As a result of dissolution study using Talc seal-coated microparticles and thermal study using differential scanning calorimeter, the rapid dissolution behaviors from CC-DP-RS at the lower coating levels of RS might be due to APAP migration to the coating film during coating due to the weak drying efficacy of the CC method. These findings suggest for the first time that CFC is a suitable method for the coating of functional polymers at lower polymer coating levels, whereas, for the CC method, adjustment of operational conditions (e.g., product temperature, inlet air volume and liquid flow rate) would be required.