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The effect of food on ritonavir bioavailability following administration of ritonavir 100 mg film-coated tablet in healthy adult subjects

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Journal of the International AIDS Society200811 (Suppl 1) :P247

https://doi.org/10.1186/1758-2652-11-S1-P247

  • Published:

Keywords

  • Gastric Emptying
  • Ritonavir
  • Fasting Condition
  • Maximum Plasma Concentration
  • Tablet Formulation

Purpose of the study

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.

Methods

This 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.

Summary of results

Table 1 presents the food effect results of the ritonavir pharmacokinetic parameters following administration of the ritonavir tablet.

Table 1

  

Arithmetic Mean ± SD

 

Relative Bioavailability

 
 

Pharmacokinetic Parameter

Test (Meal)

Reference (Fasting)

Point Estimate #

90% CI

 

Ritonavir Dosed Under Moderate Fat Meal Condition (20–30% Fat, N = 26)

    

Moderate Fat vs. Fasting

Cmax (mg/mL)

0.47 ± 0.27

0.60 ± 0.31

0.784

0.675 – 0.910

 

Tmax (h)

4.2 ± 1.2

3.2 ± 1.2

  
 

AUCt (mg*h/mL)

3.8 ± 2.0

4.6 ± 2.0

0.791

0.719 – 0.870

 

AUCinf (mg*h/mL)

3.9 ± 2.1

4.7 ± 2.0

0.798

0.726 – 0.877

 

Ritonavir Dosed Under High Fat Meal Condition (50% Fat, N = 25)

    

High Fat vs. Fasting

Cmax (mg/mL)

0.44 ± 0.21

0.60 ± 0.31

0.765

0.657 – 0.892

 

Tmax (h)

4.8 ± 1.1

3.2 ± 1.2

  
 

AUCt (mg*h/mL)

3.5 ± 1.6

4.6 ± 2.0

0.763

0.692 – 0.841

 

AUCinf (mg*h/mL)

3.6 ± 1.7

4.7 ± 2.0

0.773

0.702 – 0.851

#Antilogarithm of the difference (test minus reference) of the least square means for logarithms.

Ritonavir 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.

Conclusion

Overall, ritonavir pharmacokinetics after administration of the tablet are slightly affected by meal content (with moderate or high fat).

Authors’ Affiliations

(1)
Abbott, Abbott Park, USA

Copyright

© Ng et al; licensee BioMed Central Ltd. 2008

This article is published under license to BioMed Central Ltd.

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