OBJECTIVE: The purpose of this investigation was to introduce a new concept of admixing coated pellets with excipients to obtain a segregation-free combination of pellet-containing granules and cushioning granules during mixing and compression. METHODS: Acrylic polymeric-coated pellets were granulated by centrifugal granulation method with excipients; then, the pellet-containing granules were compacted into tablets with the cushioning granules, which were prepared in mixer or fluidized bed-granulator. Tablets were also made in a traditional method by directly compressing the mixtures of coated pellets and cushioning granules for control. Drug-release profiles, weights and drug content of tables were tested to compare this new method with the traditional method. RESULTS: The granulation process changed the surface morphology of coated pellets from smooth to rough and increased the angle of repose of pellets to close to that of the cushioning granules. Weight and drug content RSD values of tablets prepared by pellet-containing granules were much lower than those of tablets prepared by coated pellets. The similarity factor f(2) values for drug-release profiles of tablets prepared from pellet-containing granules and the original coated pellets were above 50 when microcrystalline cellulose (MCC), Polyplasdone(R) XL (PVPP), and lactose were used as granulating excipients. CONCLUSIONS: The granulation process could roughen the surface of coated pellets and increase the angle of repose and uniformity of the mixture with cushioning granules. Compared with the tablets directly compressed from coated pellets, the tablets prepared by pellet-containing granules showed improved uniformity in both weight and drug content. The granulation and compression processes did not significantly influence the drug-release behavior of coated pellets, and the enteric dissolution was retained.
OBJECTIVE: The purpose of this investigation was to introduce a new concept of admixing coated pellets with excipients to obtain a segregation-free combination of pellet-containing granules and cushioning granules during mixing and compression. METHODS: Acrylic polymeric-coated pellets were granulated by centrifugal granulation method with excipients; then, the pellet-containing granules were compacted into tablets with the cushioning granules, which were prepared in mixer or fluidized bed-granulator. Tablets were also made in a traditional method by directly compressing the mixtures of coated pellets and cushioning granules for control. Drug-release profiles, weights and drug content of tables were tested to compare this new method with the traditional method. RESULTS: The granulation process changed the surface morphology of coated pellets from smooth to rough and increased the angle of repose of pellets to close to that of the cushioning granules. Weight and drug content RSD values of tablets prepared by pellet-containing granules were much lower than those of tablets prepared by coated pellets. The similarity factor f(2) values for drug-release profiles of tablets prepared from pellet-containing granules and the original coated pellets were above 50 when microcrystalline cellulose (MCC), Polyplasdone(R) XL (PVPP), and lactose were used as granulating excipients. CONCLUSIONS: The granulation process could roughen the surface of coated pellets and increase the angle of repose and uniformity of the mixture with cushioning granules. Compared with the tablets directly compressed from coated pellets, the tablets prepared by pellet-containing granules showed improved uniformity in both weight and drug content. The granulation and compression processes did not significantly influence the drug-release behavior of coated pellets, and the enteric dissolution was retained.
Authors: Konrád Sántha; Nikolett Kállai-Szabó; Viktor Fülöp; Géza Jakab; Péter Gordon; Barnabás Kállai-Szabó; Emese Balogh; István Antal Journal: AAPS PharmSciTech Date: 2020-12-29 Impact factor: 3.246