BINDING ENDURANCE AND DETERRENCE CAPACITY OF CROSCARMELLOSE SODIUM (CCS)IN VARIOUS SOLVENTS
Abstract
Objective. Examine the ability of CCS to resist drug extraction from assorted solvents readily available and commonly used by recreational drug abusers. Background. Tampering with a medication from its original form for the purpose of intravenous abuse can heighten its effects compared to the oral route. To help deter this and other types of abuse, formulations resistant to tampering methods are greatly needed. CSS is a common tableting ingredient having ionic functional groups capable of interacting with cationic drugs. The ability of CCS to bind an abusable medication and reduce its aqueous extraction was therefore investigated. Tramadol HCl was chosen as the model drug. Methods. In glass vials, 200 mg of CCS was added to 10 mL of 2.5 mg/mL tramadol HCl aqueous solutions prepared from 0.1 N HCl, 0.9% NaCl, 40% ethanol (EtOH), and hot water (near boiling). All samples were then vortexed, centrifuged, and the supernatant analyzed for drug concentration by UV-Visible Spectroscopy at 271 nm. Results. Almost 70% of the drug dose was prevented from being extracted in water at room temperature and near boiling. CCS-drug binding also showed good resilience in 40% EtOH, but was poor in saline and at low pH. Furthermore, CCS particles rapidly swelled and viscosified the extraction solvents making filtration and syringeability extremely difficult during testing. Conclusion. Most abused pain medications are formulated as cationic drugs easily extracted for intravenous abuse. CCS prevented tramadol from extraction in water and alcohol, however its binding to tramadol was desirably low at low pH, mimicking the gastric environment. Grants. N/A
BINDING ENDURANCE AND DETERRENCE CAPACITY OF CROSCARMELLOSE SODIUM (CCS)IN VARIOUS SOLVENTS
POSTER PRESENTATIONS
Objective. Examine the ability of CCS to resist drug extraction from assorted solvents readily available and commonly used by recreational drug abusers. Background. Tampering with a medication from its original form for the purpose of intravenous abuse can heighten its effects compared to the oral route. To help deter this and other types of abuse, formulations resistant to tampering methods are greatly needed. CSS is a common tableting ingredient having ionic functional groups capable of interacting with cationic drugs. The ability of CCS to bind an abusable medication and reduce its aqueous extraction was therefore investigated. Tramadol HCl was chosen as the model drug. Methods. In glass vials, 200 mg of CCS was added to 10 mL of 2.5 mg/mL tramadol HCl aqueous solutions prepared from 0.1 N HCl, 0.9% NaCl, 40% ethanol (EtOH), and hot water (near boiling). All samples were then vortexed, centrifuged, and the supernatant analyzed for drug concentration by UV-Visible Spectroscopy at 271 nm. Results. Almost 70% of the drug dose was prevented from being extracted in water at room temperature and near boiling. CCS-drug binding also showed good resilience in 40% EtOH, but was poor in saline and at low pH. Furthermore, CCS particles rapidly swelled and viscosified the extraction solvents making filtration and syringeability extremely difficult during testing. Conclusion. Most abused pain medications are formulated as cationic drugs easily extracted for intravenous abuse. CCS prevented tramadol from extraction in water and alcohol, however its binding to tramadol was desirably low at low pH, mimicking the gastric environment. Grants. N/A