COMPLEXING AGENTS TO PREVENT INTENTIONAL DRUG ABUSE BY RAPID EXTRACTION
Abstract
Objective. To evaluate the effectiveness of bentonite and crosslinked sodium carboxymethylcellulose (XCMC) to entrap an abusable drug during solution extraction attempts from sample tablets. Background. Organic and inorganic complexing agents were hypothesized to be used in tablet formulations to discourage and prevent drug extraction attempts by abusers attempting to inject medications intravenously. Methods. Tablet compositions containing 25 mg of tramadol HCl, 100 mg of Prosolv SMCC 90, and 200 mg of bentonite clay, XCMC, or crosslinked poly(vinyl pyrrolidone)(crospovidone) were prepared by direct compression on a single station Carver press at a compression force of approximately 1000 pounds using a 7/16’ punch and die. Crospovidone was used as a control while a tablet containing only Prosolv SMCC 90 was used as a negative control. Prepared tablets were crushed and immediately mixed with 10 mL of water. After 2 minutes, the mixture was filtered and the extract solution measured for drug concentration by UV- Visible spectroscopy at 271 nm for the total amount of recovered drug. Results. High drug recovery was obtained from control tablets, while the complexing agents largely prevented fast extraction. XCMC and bentonite respectively captured approximately 73% and 92% of tramadol from being recovered. Additional factors such as entrapment of drug inside swollen particles of the complexing agents could also account for low drug recovery. Conclusion. Bentonite and XCMC were capable of binding tramadol HCl from crushed tablets within 2 minutes of aqueous extraction, and at a level statistically different from control tablets. Grants. N/A
COMPLEXING AGENTS TO PREVENT INTENTIONAL DRUG ABUSE BY RAPID EXTRACTION
POSTER PRESENTATIONS
Objective. To evaluate the effectiveness of bentonite and crosslinked sodium carboxymethylcellulose (XCMC) to entrap an abusable drug during solution extraction attempts from sample tablets. Background. Organic and inorganic complexing agents were hypothesized to be used in tablet formulations to discourage and prevent drug extraction attempts by abusers attempting to inject medications intravenously. Methods. Tablet compositions containing 25 mg of tramadol HCl, 100 mg of Prosolv SMCC 90, and 200 mg of bentonite clay, XCMC, or crosslinked poly(vinyl pyrrolidone)(crospovidone) were prepared by direct compression on a single station Carver press at a compression force of approximately 1000 pounds using a 7/16’ punch and die. Crospovidone was used as a control while a tablet containing only Prosolv SMCC 90 was used as a negative control. Prepared tablets were crushed and immediately mixed with 10 mL of water. After 2 minutes, the mixture was filtered and the extract solution measured for drug concentration by UV- Visible spectroscopy at 271 nm for the total amount of recovered drug. Results. High drug recovery was obtained from control tablets, while the complexing agents largely prevented fast extraction. XCMC and bentonite respectively captured approximately 73% and 92% of tramadol from being recovered. Additional factors such as entrapment of drug inside swollen particles of the complexing agents could also account for low drug recovery. Conclusion. Bentonite and XCMC were capable of binding tramadol HCl from crushed tablets within 2 minutes of aqueous extraction, and at a level statistically different from control tablets. Grants. N/A