Event Title

COMPLEXATION EFFICIENCY OF CROSCARMELLOSE SODIUM (CCS) AS AN EFFECTIVE ABUSE-DETERRENT AGENT

Location

POSTER PRESENTATIONS

Start Date

12-2-2016 12:00 AM

Description

Objective. To determine solution state drug complexation and physical entrapment characteristics of CCS using five model drugs. Background. CCS is a common inactive ingredient used in tablet formulations. However, CCS is known to bind with certain drugs in solution through ionic interactions to form insoluble drug-CCS complexes. These complexes prevent the drug from being easily released and absorbed. Furthermore, CCS is capable of rapidly swelling and entrapping aqueous solutions. These properties make CCS an ideal candidate in the development of medications which can resist abuse via intravenous injection. Methods. Aqueous drug solutions containing low (200 μg/mL) and high (1000 μg/mL) concentrations of either acetaminophen, diclofenac sodium, dextromethorphan hydrobromide, lidocaine hydrochloride, and verapamil hydrochloride were prepared. To simulate extraction conditions, increasing amounts of CCS (25, 50,100 mg) were then added to 10 mL of each drug solution. After 1 min, the solutions were centrifuged, the supernatant filtered, and drug concentration measured using UV-Vis spectroscopy at corresponding of 248, 275, 276, 263, and 278 nm, respectively. The amount of drug bound to CCS was determined indirectly from the amount of free drug remaining in the supernatant. Results. The percent of drug bound to CCS from solution greatly varied from 2.6% to 93% depending on the nature of the drug and starting concentration of drug and CCS. Overall, acetaminophen showed the least tendency to binding, whereas verapamil hydrochloride showed highest binding percentage over all concentrations. Conclusion. Owing to its anionic charge, CCS preferentially forms complexes with drugs that are cationic, resulting in highly selective drug binding property for cationic weak bases Grants. #PFRDG 335867

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Feb 12th, 12:00 AM

COMPLEXATION EFFICIENCY OF CROSCARMELLOSE SODIUM (CCS) AS AN EFFECTIVE ABUSE-DETERRENT AGENT

POSTER PRESENTATIONS

Objective. To determine solution state drug complexation and physical entrapment characteristics of CCS using five model drugs. Background. CCS is a common inactive ingredient used in tablet formulations. However, CCS is known to bind with certain drugs in solution through ionic interactions to form insoluble drug-CCS complexes. These complexes prevent the drug from being easily released and absorbed. Furthermore, CCS is capable of rapidly swelling and entrapping aqueous solutions. These properties make CCS an ideal candidate in the development of medications which can resist abuse via intravenous injection. Methods. Aqueous drug solutions containing low (200 μg/mL) and high (1000 μg/mL) concentrations of either acetaminophen, diclofenac sodium, dextromethorphan hydrobromide, lidocaine hydrochloride, and verapamil hydrochloride were prepared. To simulate extraction conditions, increasing amounts of CCS (25, 50,100 mg) were then added to 10 mL of each drug solution. After 1 min, the solutions were centrifuged, the supernatant filtered, and drug concentration measured using UV-Vis spectroscopy at corresponding of 248, 275, 276, 263, and 278 nm, respectively. The amount of drug bound to CCS was determined indirectly from the amount of free drug remaining in the supernatant. Results. The percent of drug bound to CCS from solution greatly varied from 2.6% to 93% depending on the nature of the drug and starting concentration of drug and CCS. Overall, acetaminophen showed the least tendency to binding, whereas verapamil hydrochloride showed highest binding percentage over all concentrations. Conclusion. Owing to its anionic charge, CCS preferentially forms complexes with drugs that are cationic, resulting in highly selective drug binding property for cationic weak bases Grants. #PFRDG 335867