A new 100 mg tablet formulation of ritonavir has been developed that would not require refrigeration. This study compared the single-dose bioavailability of the final ritonavir 100 mg tablet formulation following a moderate-fat or high-fat meal relative to that under fasting conditions.
MethodsThis was a single-dose, open-label, 3-period crossover study with a randomized, crossover design. Healthy male and female subjects (n = 27) participated in the study. Serial blood samples were collected for 36 hours after each dose. Ritonavir AUC from time 0 to the last measurable concentration (AUCt) and from time 0 to infinity (AUCinf), maximum plasma concentration (Cmax), and time of Cmax (Tmax) were determined using noncompartmental methods. The bioavailability of the tablet following a meal relative to the fasting condition was assessed by the two one-sided tests procedure using 90% confidence intervals (CI). Safety was assessed throughout the study. Table 1 presents the food effect results of the ritonavir pharmacokinetic parameters following administration of the ritonavir tablet.
Summary of resultsRitonavir Cmax and AUC were approximately 20-24% lower when dosed following a meal compared to administration under fasting conditions. The slight difference in Tmax is consistent with delayed gastric emptying following a meal. Overall, the tablet formulation was generally safe and well tolerated.
ConclusionOverall, ritonavir pharmacokinetics after administration of the tablet are slightly affected by meal content (with moderate or high fat).
Simplified antiretroviral (ARV) regimens may promote adherence and improve outcomes in HIV-1 infected patients. Clinical studies have previously demonstrated greater adherence with LPV/r SGC when dosed once-daily (QD) compared to twice-daily (BID). The objectives of the current analysis are to compare adherence when LPV/ r tablets and SGC are dosed QD and BID and to assess predictors of early adherence.
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