Bioavailability of Coformulated ART Dispersible Tablet Comparable to Standard Formulation
Further development of the dispersible tablet for future use in pediatric patients for whom swallowing tablets may be difficult.
A dispersible fixed-dose combination tablet formulation of abacavir/dolutegravir/lamivudine for the treatment of HIV-1 had higher bioavailability of dolutegravir compared to the nondispersible film-coated tablet formulation, according to results from a study published in Journal of Acquired Immune Deficiency Syndromes. However, there was no difference in the bioequivalence for abacavir and lamivudine.
Treatment for children living with HIV-1 infection has improved but there remains a need for alternative drug formulations and dosing strategies, particularly for individuals who experience problems swallowing tablets or capsules. In this phase 1, open-label, randomized study, the relative bioavailability of a novel, strawberry-cream flavored, dispersible fixed-dose combination tablet consisting of abacavir 150 mg/dolutegravir 10 mg/lamivudine 75 mg and 1.2 mg/mL was compared with dolutegravir plus abacavir/lamivudine nondispersible, film-coated tablets. The tablet was dispersed in either 40 mL of high-mineral content water or purified, zero-mineral content water. The cohort included 20 adults who were randomly assigned to 1 of 5 treatment groups over 5 dosing periods.
The relative bioavailability for dolutegravir after it was administered as a dispersible tablet ranged from 53% to 59% higher in all treatment groups vs the nondispersible tablet. The relative bioavailability of lamivudine and abacavir as a dispersible formulation was within the bioequivalence range of 80% to 125% and comparable to the nondispersible formulation. These results indicate that the formulations are interchangeable. In addition, 76% of participants rated its palatability as “neutral/acceptable.”
These data support “further development of the dispersible tablet for future use in pediatric patients for whom swallowing tablets may be difficult,” the authors concluded.