Morphological control by the Supercritical Antisolvent Technique (SAS). |
Paper ID : 1057-ISCHU |
Authors |
Fouad Zahran * Chemistry department, Faculty of Science, Helwan University |
Abstract |
Ciprofloxacin (CIP) is a broad-spectrum antibiotic which is currently used to treat different infections. Here we propose the use of supercritical CO2 (ScCO2) as a green solvent for the micronization of ciprofloxacin hydrochloride (CipHCl) to prepare a drug for inhalation. The recommended particle size for inhalation is ≤ 5 μm, to allow a deeper distribution in the airways. Reduction of the drug particle size improves its bioavailability, reducing the adverse effects. The addition of excipients (PVP K30, PVP K10 and lactose) is assessed to control the particle shape and size of the precipitates. CipHCl has two anhydrous polymorphs. During SAS precipitation, Ciprofloxacin loses its water of crystallization forming the anhydrous form as shown by TGA. SAS CipHCl is the metastable anhydrous form AH1 that undergoes a solid-solid transition to AH2 by heating. CipHCl keeps its polymorphism when coprecipitated with PVP K-10 as AH1. Anhydrous form AH1 is more water soluble than hydrated CipHCl |
Keywords |
Supercritical antisolvent, morphology control, supercritical carbón dioxide,Ciprofloxacin |
Status: Abstract Accepted (Oral Presentation) |