Bioavailability of Coformulated ART Dispersible Tablet Comparable to Standard Formulation

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Further development of the dispersible tablet for future use in pediatric patients for whom swallowing tablets may be difficult.
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.

Reference

Singh RP, Shaik JSB, Skoura N, Joshi S, Shreeves T, Casillas L, Buchanan AM. Effects of low-and high-mineral content water on the relative bioavailability of a coformulated abacavir/dolutegravir/lamivudine dispersible tablet in healthy adults [published online September 14, 2018]. J Acquir Immune Defic Syndr. doi: 10.1097/QAI.0000000000001859

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