BioSustane adds abuse-deterrent properties to formulations.

Eastman BioSustane™ SAIB NF is a novel excipient for imparting abuse-deterrent properties to the dosage form. Studies show formulations with BioSustane provide tamper resistance to common forms of tampering, such as crushing and dissolving in liquids. It has been shown that using BioSustane in the formulation makes it difficult to extract the API using commonly available solvents. Crushing the dosage form containing BioSustane results in large-size particles that are difficult to snort. Extraction with alcohol results in a sticky residue that is difficult to handle; even when ingested, there is no observed burst effect.

Experimental matrix using pseudoephedrine hydrochloride (due to its similarity to an opioid)

F1-Control F5-Control F1 F2 F3 F4 F5
    Pseudoephedrine HCI30303030303030
    BioSustane SAIB NF

    Polyethylene oxide 151.02117.46151.02142.63134.24125.85117.46
    Tocopherol acetate
    Microcrystalline cellulose30 303030303030
    Magnesium stearate 2222222
    Colloidal silicon dioxide 6 666666
    Total 219 186 236 236 236 236 236

Nasal abuse assessment shows that BioSustane increases the particle size. Up to 47% of the ground powder is >1 mm.

BioSustane - nasal abuse assessment

Solvent extraction assessments

Solvent extraction assessment 1

Solvent extraction assessment 2

  • 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).