Supramolecular elucidation of the quality attributes of microcrystalline cellulose and isomalt composite pellet cores

Quality aspects in the development of pelletized dosage forms

“…Due to its excellent plastic behaviour and cohesiveness when wetted and its capacity to uptake, hold and yield water; MCC parts acceptable shape, size, mechanical resistance and flow properties to pellets. Hence, it is the most preferred aid for pellet formulation [ 18 , 57 ]. Different grades of MCC show significant difference in their physical properties, which influences the water uptake.…”

“…The most preferable processing can be done at temperature above the M.P. of semi-crystalline polymers or [ 50 , 51 , 52 , 53 , 54 , 55 , 56 , 57 , 58 , 59 , 60 , 61 , 62 , 63 , 64 , 65 , 66 , 67 , 68 , 69 , 70 , 71 , 72 , 73 , 74 , 75 , 76 , 77 , 78 , 79 , 80 , 81 , 82 , 83 , 84 , 85 , 86 , 87 , 88 , 89 , 90 , 91 , 92 , 93 , 94 , 95 , 96 , 97 , 98 , 99 , 100 ] °C above the glass transition temperature Tg of amorphous polymers, but below the M. P. of the crystalline API [ 80 , 81 ].…”

Review on Starter Pellets: Inert and Functional Cores

“…Both isomalt and sugar-based pellets develop significant osmotic pressure during dissolution (Figure 12), which promotes drug release [59]. Inert pellet cores made of water-soluble excipients as well as water-insoluble materials, with patent registration pellet cores, containing different proportions of isomalt and MCC, were prepared [132,133]. For composite pellet cores, the release rate of sodium diclofenac depended on the isomalt content of the starter pellet core for the Eudragit RS Inert pellet cores made of water-soluble excipients as well as water-insoluble materials, with patent registration pellet cores, containing different proportions of isomalt and MCC, were prepared [132,133].…”

Amorphous Solid Dispersions

“…Spatial resolution limits the estimation of phaseseparated domain (Antal et al 2013;Bölcskei et al 2011;Chieng et al 2013a, b;Gottnek et al 2013;Szabó et al 2011;Szente et al 2009;Zelkóa et al 2006) Very sensitive analysis of local and global molecular mobility based on free volume change Change in free volume owing to structural cross linking by H-bond formation in ASD Miscibility derived from change in number, size (distribution) of molecular holes as a function of API content in ASD Water-solid interaction Study of miscibility in product with low drug content (0.5-1 %w/w) Estimation of domain size and identification of molecular cluster to dispersion possible Selective Not applicable for high drugloading system as API molecular proximity below FRET distance Fluorescent properties required and FRET should occur Neutron scattering (Bordallo et al 2012;Lerbret et al 2012;Magazù et al 2008;Magazù et al 2010;Qi et al 2013a, b) Molecular dynamics and structural relaxation of multicomponent amorphous systems Small-angle neutron scattering for polymer-surfactant interaction during dissolution of ternary ASD Sample preparation tedious Requires isotope labeling or enrichment USP < 1092 > provides detailed requirements for the development and validation of dissolution methods (USP 2009b). As noted in the guidance, recommendations are made for sink condition to be established for the test whereby sink condition is defined as the volume of medium at least three times that required in order to form a saturated solution of drug substance.…”