Pharmacokinetics of a Novel Formulation, Lopinavir/ritonavir Sprinkles meant for children in Healthy Human Subjects: A Pilot Study
Jaideep Gogtay*1, M Gole1, A Khanna1, R Naidu2, G Malhotra1, and S Purandare1
1Cipla Ltd, Mumbai, India and 2Sitec Labs, Mumbai, India
Background: Developing appropriate ARV formulations for children represents a significant challenge particularly for the protease inhibitors. The present study has evaluated the pharmacokinetics of a novel sprinkle formulation of the Lopinavir/ritonavir (40/10 mg) and compared it to LPV/r oral solution. The sprinkle formulation consists of a finite number of minitablets in a capsule. The capsule is opened and sprinkled over soft food.
Methods: 14 healthy subjects were enrolled in the study after informed consent and permission from the Ethics committee. All received a single dose of sprinkles from 10 capsules of LPV/r (each capsule containing 40 mg Lopinavir sprinkles and 10 mg ritonavir sprinkles sprinkled over soft food) and a single dose of 5 ml Kaletra oral solution (each ml containing Lopinavir 80 mg and ritonavir 20 mg) in a randomized crossover fashion. 25 blood samples were collected pre-dose and serially upto 36 hours and were anlalyzed using a validated LCMS/MS method. A non compartmental method was used to calculate the pharmacokinetic parameters
Results: 12 subjects completed the study. The PK values were as follows
Conclusions: The two products showed similar extent of absorption in Lopinavir while there were minor differences in the absorption of Ritonavir. This suggests that the sprinkle formulation could be tested in HIV infected children