Applications of Cellulose and Cellulose Derivatives in Immediate Release Solid Dosage

Abstract

In this paper, the use of cellulose crystallites and cellulose derivatives in manufacturing immediate release dosage forms is reviewed from three aspects: tablet binder, tablet disintegrant and wet granulation binder. Cellulose crystallites such as microcrystalline cellulose (MCC) are typically derived from pure cellulose via a hydrolysis process. As a tablet binder, cellulose crystallites exhibit plastic deformation under compression owing to their crystalline and hydrogen bonded structure. The compressibility of cellulose crystallites (MCC) and the effect of their physical properties such as density and particle size on the compressibility and tablet hardness have been summarized. Some new developments in tablet binder using cellulosic materials are also reviewed. Secondly, cellulose crystallites and cellulose derivatives such as croscarmellose as tablet disintegrants have been compared with other disintegrants from a polymer chemistry point of view. Croscarmellose has been shown to have certain advantages when used in a small quantity. The disintegration mechanism and other affecting factors are discussed. Thirdly, cellulose derivatives such as hydroxypropylmethylcellulose (HPMC), hydroxypropylcellulose (HPC), methylcellulose (MC), sodium carboxymethylcellulose (Na-CMC) and ethylcellulose (EC) have been extensively used as wet granulation binders. The theory of wet granulation and in particular the effect of binder characteristics on the physical properties of dry granules has been reviewed. Under certain circumstances cellulose derivatives are better binders than other binders such as povidone. For instance, HPC, which has low surface tension, serves as a good binder for wet granulating poorly water-soluble compounds.