Generation of high drug loading amorphous solid dispersions by Spray Drying

Bhianca Lins de Azevedo Costa (1) , Martial Sauceau (1) , Romain Sescousse (1) , Maria-Inês Ré (1)

1 RAPSODEE - Centre de recherche d'Albi en génie des procédés des solides divisés, de l'énergie et de l'environnement

Amorphous solid dispersions (ASDs) refers to drug - carrier systems, where the drug is dispersed in the carrier at a molecular level. In this work, ASDs were formulated by spray drying. The aim was to achieve high drug loads of an amorphous hydrophobic drug (Efavirenz - EFV) in the carrier Soluplus (R). Solid state characterizations (mDSC, XRPD, DVS, Raman, SEM, stability and solubility studies) were done. EFV amorphisation in ASDs (20 to 85% EFV loads) resulted in improved drug solubility compared to unprocessed EFV crystals and tendency of properties evolution over time for ASDs with EFV loads higher than 70 wt%.

Mots clés: efavirenz; amorphous solid dispersion; high drug loading; soluplus; spray drying

Domaines: Pharmacie galénique; Génie des procédés

Bhianca Lins de Azevedo Costa, Martial Sauceau, Romain Sescousse, Maria-Inês Ré. Generation of high drug loading amorphous solid dispersions by Spray Drying. IDS 2018 - 21st International Drying Symposium, Sep 2018, Valence, Spain. pp.1123-1130, ⟨10.4995/ids2018.2018.7871⟩. ⟨hal-02267499⟩