Evaluation of emulsifiable glasses for the oral administration of cyclosporin in beagle dogs

作者: Christopher J.H. Porter , Susan A. Charman , Rachel D. Williams , Margarita V. Bakalova , William N. Charman

DOI: 10.1016/0378-5173(96)04641-8

关键词: Dosage formBeagleDrugChemistryPharmacologyChromatographyEmulsionPulmonary surfactantBioavailabilityOral administrationPharmacokinetics

摘要: Abstract Solid state emulsifiable glasses have been proposed as delivery systems for poorly water soluble drugs. This study assessed the utility of glass (EG) technology oral cyclosporin. EG formulations were prepared, evaluated in vitro, and bioavailability beagle dogs. Although standard (i.e. containing no surfactant) produced a dispersed phase upon reconstitution, significant quantities residual oil present within these systems. The absolute cyclosporin after administration an formulation (12.5 mg dose) was compared with 25 Sandimmun ® capsule surfactant-based self-emulsifying lipid (SEDDS) randomized cross-over conducted four major pharmacokinetic parameters similar three formulations. Subsequently, surfactant enhanced (SEEG) formulated which offered following advantages over systems: (i) rapid, efficient complete emulsification, (ii) four-fold increase drug loading capacity, (iii) two-fold decrease processing time. relative characteristics SEEG to two-way crossover There differences either or two Comparing studies, there significantly less variability blood profiles than formulation. These studies demonstrate cyclosporin, develop include offer improved characteristics.

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