Powder Technology, Vol.305, 546-552, 2017
Large-scale preparation of stable irbesartan nanoparticles by high-gravity liquid antisolvent precipitation technique
Irbesartan (IBS), an angiotensin II receptor antagonist mainly used for the treatment of hypertension, is a poorly water-soluble drug. To enhance its solubility and dissolution rate, and thus potentially improve the Oral bioavailability, stable amorphous IBS nanoparticles were prepared via high-gravity liquid antisolvent precipitation (HGLAP) technique, without requiring any additives. The effect of various operating parameters on particle size was investigated in detail. IBS nanoparticles with an average size of 295 nm were successfully prepared. Compared to the raw drug, the saturation solubility of IBS nanoparticles was dramatically increased from 3.6 mu g/mL to 13.7 mu g/mL. The prepared nanoparticles exhibited a good stability and were capable of generating a maximum supersaturation level, reaching up to similar to 13.5 times of raw drug's saturation solubility. In vitro dissolution test, IBS nanoparticles showed a significantly enhanced dissolution rate and 100% of the drug dissolved within 30 min, while the raw drug did not dissolve completely even after 120 min. HGLAP technique offers a great opportunity for the massive production of drug nanoparticles with improved solubility and dissolution rate. (C) 2016 Elsevier B.V. All rights reserved.
Keywords:Irbesartan;Amorphous nanopartides;Dissolution rate;High-gravity;Liquid antisolvent precipitation