Opioid Complexation and Abuse Performance of Crosslinked Cellulose and Starch Derivatives

Nova Southeastern University, Davie, Florida, USA

Objective. The objective was to determine the percentage of Dextromethorphan HBr (DEX) that, in the form of complex, could be loaded into two crosslinked anionic polymers, carboxymethyl starch (CMS) and carboxymethyl cellulose (CMC) at low and high ratios, and to determine the extent to which the complexation ratio influences the abuse deterrence capacity. Background. We previously disclosed polymer-drug complexes that can effectively minimize the amounts of extracted drug under abuse conditions. We have also shown that CMS and CMC have great potential to form effective polymer-drug complexes. Methods. CMS/CMC were mixed with DEX in water at 8:1 and 1.3:1 weight ratios. Followed by washing, the complexes were dried and milled. Drug loading was determined in 0.1N HCl. Accordingly, given amounts of the complexes (equivalent to 25 mg DEX) were dispersed in 10mL aqueous solutions. The % drug in solution was determined by UV Spectrophotometer. IR spectroscopy was used to characterize drug loading capacity. Results. At low and high drug/polymer ratios, the amounts of drug loaded onto 1g of polymers were respectively found 99mg and 117mg (for CMS) and 112mg and 602mg (for CMC). IR spectra coefficients were 0.98 and 0.85 for CMS and CMC complexes, respectively. Deterrence performance within the CMS group were comparable (≤ 6% differences), but CMC complexes showed up to 35% difference in their deterrence performance. Conclusion. Higher functionality of CMC offered higher loading capacity. The highloaded complexes were found more sensitive to ions present in the solution. Grants. This study was supported by NSU Grant 335081