The Study of Spray-Freeze-Drying Technique for Development of Novel Combination pMDIs, Part II: In Vitro and In Vivo Evaluations

Abstract The mometasone furoate (MF) and formoterol fumarate dihydrate (FF) inhalable microparticles prepared by different methods, such as micronized active pharmaceutical ingredients (APIs), of APIs spray-freeze drying technique (SFD APIs), phospholipid SFD Lip-APIs), showed inhaled drug delivery characteristics. Study on the physicochemical characteristics those effect matrix excipients pharmacokinetic (PK) behaviors is helpful for development new methods with excellent performance inhalation In this study, crystal state was investigated powder X-ray diffraction differential scanning calorimetry. density a bulk method. suspension dispersion were determined observing its in hydrofluoroalkane (HFA). Meanwhile, PK Lip-APIs beagle dogs also airway administration to evaluate phospholipids release. results indicated that presence prevents formation solid bridges bonding each other during pure solutions. comparison conventional microparticles, drug–phospholipid easily dispersed suspended HFA. embedded drugs endowed better physical stability, most interestingly, have similar behavior control (a mixed solution MF/FF), suggesting phospholipids, excipients, had no absorption. Given above, our designed may represent an efficient carrier pulmonary MF FF further clinical treatment.