Development of an indinavir oral liquid for children

An indinavir oral liquid was developed and studied. Several oral liquids containing indinavir were prepared and taste tested in eight healthy volunteers. Physical and chemical stability over two weeks w ere examined, and a randomized, two-way-crossover, single-dose bioequivalen ce trial was performed in 12 healthy male volunteers. Indinavir 800 mg was given as two 400-mg indinair capsules (Crixivan) on day 1 and as 80 mL of t he indinavir liquid on day 2, or vice versa. A standard breakfast and lunch were given at fixed times, and blood and urine samples were collected at v arious intervals up to eight hours. The log-transformed area under the conc entration-versus-time curve from zero to eight hours (AUC(0-8)) and maximum plasma concentration(C-max) for the liquid versus the capsules were compar ed by using a 90% confidence interval [CI) test (limits, 80-125%), and the time to C-max (t(max)) was compared by using the nonparametric sign test. The liquid selected had an acceptable taste, contained indinavir 10 mg/mL, and was chemically stable for two week, at 4 degrees C. The 90% CI for the AUC ratio (liquid versus capsules) was 92-99% (mean, 95%); for the C-max ra tio it was 95-106% (mean, 100%). There was no significant difference in t(m ax) between the liquid and capsules. An oral liquid formulation of indinavir was developed that had an acceptabl e taste, was chemically stable, and was bioequivalent to the commercially a vailable capsule.