Bioavailability in healthy adults of efavirenz capsule contents mixed with a small amount of food.
OBJECTIVE
The effect of mixing the contents of efavirenz capsules (sprinkles) with a small amount of food on the bioavailability and pharmacokinetics of efavirenz in healthy adults was evaluated.


METHODS
In a randomized, three-period, crossover study, 24 healthy adult subjects were divided equally into two groups. Group I received treatments A, B, and C, and those in group II received treatments A, D, and E. Treatment A was three efavirenz 200-mg intact capsules under fasting conditions. Treatments B, C, D, and E were three efavirenz 200-mg capsule contents mixed with two teaspoons of applesauce, grape jelly, yogurt, or infant formula, respectively. A single dose was given on days 1, 21, and 41. The steady-state mean maximum observed concentration, time of maximum observed concentration, area under the concentration-time curve (AUC) half-life, taste, and safety were assessed.


RESULTS
The AUC after administration of a single 600-mg dose of efavirenz sprinkles mixed with two teaspoons of any of the food vehicles to healthy adults was bioequivalent to a 600-mg efavirenz dose given as intact capsules under fasting conditions. Subjects rated efavirenz mixed with grape jelly as the most palatable. Adverse events and laboratory abnormalities were similar for all treatments.


CONCLUSIONS
The AUC of efavirenz 600 mg administered as capsule sprinkles with two teaspoons of applesauce, grape jelly, yogurt, or infant formula was bioequivalent to a single dose of efavirenz 600 mg given as intact capsules under fasting conditions in healthy adults.
Kaul
Sanjeev
S
Discovery Medicine and Clinical Pharmacology, Bristol-Myers Squibb (BMS) Research and Development, Princeton, NJ 08543, USA. sanjeev.kaul@bms.com
Ji
Ping
P
Lu
Michael
M
Nguyen
Kim L
KL
Shangguan
Tong
T
Grasela
Dennis
D
D000284:Administration, Oral; D000328:Adult; D000480:Alkynes; D019540:Area Under Curve; D048588:Benzoxazines / Q000008:administration & dosage* / Q000097:blood / Q000493:pharmacokinetics*; D001682:Biological Availability; D002214:Capsules; D018592:Cross-Over Studies; D003521:Cyclopropanes; D004305:Dose-Response Relationship, Drug; D005215:Fasting; D005260:Female; D018565:Food-Drug Interactions; D006207:Half-Life; D006801:Humans; D008297:Male; D018894:Reverse Transcriptase Inhibitors / Q000008:administration & dosage* / Q000097:blood / Q000493:pharmacokinetics*; D013649:Taste; D013810:Therapeutic Equivalency
D000480:Alkynes; D048588:Benzoxazines; D002214:Capsules; D003521:Cyclopropanes; D018894:Reverse Transcriptase Inhibitors; C098320:efavirenz