Structural Factors Affecting Abuse Performance of Common Pharmaceutical Superdisintegrants

Nova Southeastern University, Davie, Florida, USA

Objective. The objective was to evaluate the abuse deterrence performance of commercial superdisintegrants, carboxymethyl cellulose (AcDiSol) and carboxymethyl starch (Explotab), to entrap cationic drug model (Dextromethorphan HBr, DEX) in solvents commonly used in IV drug abuse. Background. AcDiSol and Explotab (Regular, Low pH, and CLV) are crosslinked substituted cellulose and starch, respectively. We previously found out that both polymers deter drug abuse due to their binding and swelling features. Although both polymers are supplied as sodium salt, they differ in degree of substitution and level of crosslinking, potentially affecting their deterrence performance in extracting solvents. Methods. DEX and CMC/CMS mixtures were prepared in different aqueous solvents. Drug concentration in solution was determined (UV Spectrophotometer). Percent of entrapment was calculated from the mass balance. Same procedure was repeated using washed Explotab CLV. Results. AcDiSol showed highest entrapment compared with non-washed Explotabs in polar solvents (>80% versus ~60%). Comparable results were achieved in less polar solvents or those containing ions ( Conclusion. Higher degree of substitution significantly enhanced the deterrence capacity of cellulose and starch derivatives in polar solvents. Crosslinking had no significant effect on total drug entrapment. Ionic interferences, derived from solvents or polymers, negatively affected the entrapment efficiency. Grants. This study was supported by NSU Grants 335357 & 335829