The Impact of Disintegrant Type, Surfactant, and API Properties on the Processability and Performance of Roller Compacted Formulations of Acetaminophen and Aspirin

Abstract

In formulation development, certain excipients, even though used in small quantities, can have a significant impact on the processability and performance of the dosage form. In this study, three common disintegrants, croscarmellose sodium (CCS), crospovidone (xPVP), and sodium starch glycolate (SSG) as well as the surfactant sodium lauryl sulfate (SLS) were evaluated for their impact on the processability and performance of a typical dry granulation formulation. Two model compounds, the mechanically brittle and chemically inert acetaminophen and the mechanically ductile carboxylic acid aspirin, were used for the evaluation. It was found that the disintegrants were generally identical in their impact on the processability and little difference was observed in the granulation and compression processes. The exception is that when xPVP was used in the formulation of the brittle acetaminophen, lower compression forces were needed to reach the same tablet hardness, suggesting a binding effect of xPVP for such systems. In general, CCS and xPVP tend to provide slightly better disintegration than SSG. However, in the case of aspirin, a strong hydrogen bonding interaction between the carboxylic acid group of aspirin and the carbonyl group of xPVP was observed, resulting in slower release of the drug after fast disintegration. SLS was found to have a significant impact on the processability due to its lubricating effect, resulting in higher compression forces needed to achieve the target tablet hardness. Due to the higher degree of compression, the disintegration and dissolution of both drugs became slower despite the wetting effect of SLS.

Quality-by-Design Approach and Optimization of Risk Factors by Box-Behnken Design in Formulation Development of Aspirin and Glycine Orally Disintegrating Tablet

“…Disintegrating property does vary depending upon the API characteristics. Zhao and Augsburger carried out an experiment to prove that croscarmellose sodium (CCS) was most effective for reducing disintegration and improving dissolution of ASP among the three super-disintegrants [31,32]. Consequently, CCS was considered as the superdisintegrant in the current study.…”

Formulation and In Vivo Evaluation of a Solid Self-Emulsifying Drug Delivery System Using Oily Liquid Tocotrienols as Model Active Substance

“…Highly hydrophobic compounds such as the TRF and silica carriers were not wetted easily by physiological fluids. Croscarmellose sodium has good hydrophilicity and facilitates fast water-wicking action [59]. SLS has frequently been used as a wetting agent to accelerate drug release and dissolution [59,60].…”

Mechanism for the Reduced Dissolution of Ritonavir Tablets by Sodium Lauryl Sulfate

“…[5][6][7] It has been used as an emulsifier, solubilizer, tablet lubricant, and wetting agent. 5,[8][9][10][11] When applied as a wetting agent, SLS could reduce the surface tension between hydrophobic drugs and aqueous media to prevent the self-aggregation of drug particles, thus increase the effective surface area of dissolution. 8 Above the critical micelle concentration (CMC), SLS monomers aggregate to form micelles that can solubilize hydrophobic drugs.…”