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Three (3) formulations, each containing the most stable of the 3 identified forms of the potassium salt of XX (Form C), were evaluated in the development program. These included:〔1〕 a rapidly disintegrating tablet used for the initial Phase I studies (Phase I lactose formulation); (2) an erodible tablet containing 30% aa 207, used for Further Phase I studies (Phase I aa formulation); and (3) an erodible tablet containing 15% aa 207, used for Phase II and III studies, as well as late Phase I studies (Phase II/III/FMI aa formulation). The initial Phase I lactose formulation was developed as a probe, fit-for-purpose, formulation to initiate clinical studies with the intent to continue with formulation development. Consequently, the Phase I aa (30%) formulation was developed, which possessed improved PK and physical properties, including a lower peak-to-trough ratio and the advantage of increasing drug loading from 15% (Phase 1 lactose) to 60% allowing a 300-mg potency tablet. However, manufacturing and scale-up difficulties associated with the highly plastic nature and strain-rate sensitivity of this formulation necessitated slight modifications leading to the development of the Phase II/III FMI formulation containing 15% aa. The FMI formulation, consisting of the 300-mg potency Phase II/III/FMI aa formulation with an Opadry II film coat, was used in the Phase III studies. |
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