Pharmaceutical design of a new lactose-free coprocessed excipient: application of hydrochlorothiazide as a low solubility drug model

Abstract

Most co-processed excipients used in direct-compression tablets contain lactose, which prevents lactose-intolerant patients from taking such tablets. Therefore, a novel lactose-free co-processed excipient for direct compression tablets has been prepared. Microcrystalline cellulose and dicalcium phosphate dehydrate were used as primary excipients which underwent a wet granulation process and factorial experiment in order to ascertain the best prototype. Finally, the best two prototypes were added to hydrochlorothiazide, which has chosen as the model drug because of its low solubility. An extensive characterization of the new excipient as well as the drug loaded tablets is reported. Our results show adequate parameters (rheological and compression behavior, uniformity of weight, disintegration, friability, crushing force and cohesion index). Moreover, the biopharmaceutical profile was evaluated; the tablets exhibits a Weibull kinetic function and fast drug release.

A review of emerging technologies enabling improved solid oral dosage form manufacturing and processing

“…Several coprocessing approaches can be employed such as melt extrusion, granulation, spheronization, co-crystallization, co-drying, co-milling, spray drying and co-precipitation [72]. Novel coprocessed excipients include calcium carbonate-MCC, cellulose-lactose (cellactose), silicified MCC, magnesium silicate-maize starch, MCC-dicalcium phosphate dehydrate and α-lactose monohydrate-crosslinked PVP-HPMC E3 [72][73][74][75]. These multifunctional co-processed excipients can serve as potential candidates for continuous manufacturing.…”

Co-processing as a tool to improve aqueous dispersibility of cellulose ethers

“…It is aimed at providing the synergistic benefit of functionality improvements and masking the undesirable properties of individual excipients [70][71][72][73] . Co-processed excipients are prepared by incorporating one excipient into the particle structure of another excipient using processes such as co-drying.…”