THE EFFECTS OF FINE LACTOSE AS A THIRD COMPONENT ON AEROSOLIZATION OF CEFOTAXIME SODIUM FROM DRY POWDER FORMULATIONS

Abstract: Dry powder inhaler (DPI) formulations usually contain micronized drug particles and lactose as a carrier. Fine lactose could be used as a ternary component to improve drug delivery from DPIs. The aim of this study was to investigate the deposition profile of a model drug, cefotaxime sodium (CS), using coarse and fine carriers after aerosolization at 60 l/min via a spinhaler® into a twin stage liquid impinger (TSI). Two micronization methods. jet milling and spray drying were used to micronize the active drug and carrier. The particle size of CS and lactose were characterized by laser diffraction, and the morphology of formulations was examined by scanning electron microscopy. X-ray diffraction of jet milled lactose showed crystalline nature, but spray dried lactose exhibited an amorphous state. The results showed the existence of fine lactose in formulations significantly (p<0.05) influenced the deposition profiles of aerosolized jet milled CS. However, no significant (p>0.05) difference was observed between the effect of jet milled and spray dried lactose. On the other hand selection of micronization technique to reduce particle size of CS, was very effective on deposition profile. The highest influence of fine lactose was obtained by formulation containing jet milled CS in ratio of drug/carrier 1/1 and 10% of fine lactose as third component.