Abstract
A process to coat particles of active pharmaceutical ingredient (API) onto microcrystalline cellulose (MCC) excipient shows promise as a new way to dosage forms showing enhanced drug release. The process consists of a fluidized bed operated at elevated pressure in which API particles are precipitated from a Supercritical Anti-Solvent process (SAS). MCC particles were used as an excipient in the fluidized bed and collect the SAS-generated API particles. Naringin was selected as the model API to coat onto MCC. A number of operational parameters of the process were investigated: fluidization velocity, coating pressure, temperature, concentration of drug solution, drug solution flow rate, drug mass, organic solvent, MCC mass and size and CO2-to-organic solution ratio. SEM and SPM analyses showed that the MCC particle surfaces were covered with near-spherical nanoparticles with a diameter of approximately 100–200nm, substantially smaller than the as-received API material. XRD showed that naringin changed from crystalline to amorphous during processing. The coated particles resulting from the SAS fluidized bed process have a higher loading of API, gave faster release rates and higher release ratios in comparison with those produced using a conventional fluidized bed coating process. The approach could be transferred to other industries where release is important such as agrochemical, cosmetic and food.
Highlights
Active pharmaceutical ingredients (API) in nanoparticulate form have advantageous properties, such as higher dissolute rate and greater bioavailability than those prepared by conventional⇑ Corresponding author.approaches [1]
Supercritical CO2 was introduced from the bottom of the high pressure vessel (HPV) which acted as an antisolvent, causing precipitation of the naringin from the selected organic solvent solution
The shape was chosen in order to enhance the circulation of the excipient particles, which is usual in fluidized bed coating processes in order to ensure uniform coating and prevent agglomeration
Summary
Active pharmaceutical ingredients (API) in nanoparticulate form have advantageous properties, such as higher dissolute rate and greater bioavailability than those prepared by conventional. Previous studies on a number of poorly soluble drugs have demonstrated that particle size reduction resulted in an increase rate of dissolution and higher oral bioavailability [2]. Until the current work there has been no experimental demonstration of the use of SAS within a pressurized fluidized bed to coat API particles, with proof of their release properties. The work reported here uses naringin as a model drug in a Supercritical Anti-Solvent Fluidized Bed process in order to improve its dissolution properties. A number of parameters were studied in order to optimize the process: the fluidization velocity, coating pressure, temperature, concentration of drug solution, drug solution flow rate, drug mass, organic solvent, MCC mass and size and CO2-to-organic solution ratio. The drug release profiles of the coated composite particles were determined
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