Imparting abuse-deterrent properties
Eastman BioSustane™ SAIB NF is a novel excipient for imparting abuse-deterrent properties to the dosage form. Studies show formulations with BioSustane resist tampering methods such as crushing and dissolving in liquids.
Table 1. Experimental matrix using pseudoephedrine hydrochloride (due to its similarity to an opioid)
Ingredients |
Formulations | ||||||
|---|---|---|---|---|---|---|---|
| F1-Control | F5-Control | F1 | F2 | F3 | F4 | F5 | |
| Pseudoephedrine HCI |
30 | 30 | 30 | 30 | 30 | 30 | 30 |
| BioSustane SAIB NF |
— | — | 16.78 | 25.17 |
33.56 | 41.95 | 50.34 |
| Polyethylene oxide |
151.02 | 117.46 | 151.02 | 142.63 | 134.24 | 125.85 | 117.46 |
| Tocopherol acetate |
0.2 | 0.2 | 0.2 | 0.2 | 0.2 | 0.2 | 0.2 |
| Microcrystalline cellulose | 30 | 30 | 30 | 30 | 30 | 30 | 30 |
| Magnesium stearate | 2 | 2 | 2 | 2 | 2 | 2 | 2 |
| Colloidal silicon dioxide | 6 | 6 | 6 | 6 | 6 | 6 | 6 |
| Total | 219 | 186 | 236 | 236 | 236 | 236 | 236 |
Figure 1. Nasal abuse assessment shows that BioSustane increases the particle size. Up to 47% of the ground powder is > 1 mm.
Figure 2. Solvent extraction assessments
Figure 3. Solvent extraction assessments
BioSustane decreases the amount of extracted drug 41.3%–42.5%, 24.8%–26.1%, and 37.4%–50.6% in water, 0.1 N HCl, and 0.1 N NaOH solvents, respectively, compared with control formulations.
Extraction with organic solvents yields sticky residues that are difficult to abuse by various routes (e.g., injection, ingestion, nasal).
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