EVALUATION OF THE IMPACT OF THE INLET AIR HUMIDITY DURING COATING STEP ON THE IN VITRO DISSOLUTION OF MODIFIED-RELEASE FILM-COATED PELLETS CONTAINING A BCS CLASS I ACTIVE SUBSTANCE
PAUL ANCU DUMITRAȘCU 1,2#, CRISTIAN FUNIERU 1#, VALENTINA ANUȚA 1*, ALEXANDRU GEORGE COMAN 2, CARMEN ALECSANDRESCU 2, ALINA IVANCENCU 2, LĂCRĂMIOARA POPA 1, MIHAELA VIOLETA GHICA 1, CRISTINA ELENA DINU-PÎRVU 1
1.“Carol Davila” University of Medicine and Pharmacy, Bucharest, Romania
2.Zentiva S.A., Strategy and Investment Department, Bucharest, Romania
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Present study aimed to evaluate the impact of the inlet air humidity during the coating step on the in vitro release profile of modified-release film-coated pellets containing a BCS class I active substance, by assessing the results obtained for 25 experimental batches. In order to ensure both the delayed and the prolonged-release mechanism, the release controlling agent (metacrylic acid - ethyl acrylate copolymer in a 1:1 ratio) was added in both matrix pellets and film-coat. The gastro-resistance of the pellets was evaluated after 2 hours in acidic media according to the in-force EMEA and FDA Guidelines. Based on the results obtained for 22 experimental batches, it can be concluded that the optimum absolute humidity of the inlet air during coating should be above 4.5 g/kg, in order to provide an acidic barrier for the pellets. A lower value for the absolute humidity of the inlet air during the coating process increase the brittleness of the coating and therefore reduces its barrier capability. Three experimental batches were manufactured by reducing the inlet air volume and the inlet temperature and by increasing the spray rate, therefore by reducing the product temperature at which the coating is form. The changes in the manufacturing process reduced the impact of a lower inlet air humidity during, but the dependency was not completely cancelled.