COMPARATIVE IN VIVO STUDY OF MARKETED SR AND PULSATILE FORMULATIONS OF BUDESONIDE
A. Prameela Rani*, M. Rama Krishna and V. Saikishore
ABSTRACT
Chronotherapeutics refers to a treatment method in which in vivo drug availability is timed to match rhythms of disease, in order to optimise therapeutic outcomes and minimise side effects. It is based on the observation that there is an interdependent relationship between the peak-to-trough rhythmic activity in disease symptoms, pharmacologic sensitivity, and pharmacokinetics of many drugs. The objective of this study was to investigate differences in the pharmacokinetic patterns between an optimized pulsatile formulation and an exisisting marketed sustained formulation of Montelukast sodium. The formulations were administered to 2 groups of white New Zealand rabbits (n=6) following cross over design pattern and the plasma levels were measured using LC-MS/MS method. Pharmacokinetic parameters were determined for each formulation. The comparison of the plasma time curves of the dosage forms showed that each dosage form caused significant differences in the drug plasma levels. The pulsatile capsular formulation prepared in the laboratory managed to show some lag phase initially before releasing the drug. The mean residence timemean residence time mean residence timemean residence timemean residence timemean residence time mean residence time mean residence time mean residence timemean residence time mean residence timemean residence time of pulsatile formulationspulsatile formulationspulsatile formulationspulsatile formulationspulsatile formulations pulsatile formulationspulsatile formulationspulsatile formulationspulsatile formulationspulsatile formulationspulsatile formulations pulsatile formulationspulsatile formulations administration (22.6 22.6 22.6 22.6 22.6 ± 0.110.110.110.11hrs) was found to be more than marketed sustained formulation (17.1 17.1 17.1 17.1 17.1 ± 0.090.090.090.09 hrs). Implications for the use of a pulsatile drug delivery device for chronopharmacotheraphy are discussed. Pulsatile drug delivery offers a promising way for chronopharmacotheraphy if the time of administration and pulse time are adjusted to the circadian pattern.
Keywords: LC-MS/MS, Budesonide, Pulsatile, In-vivo studies, pharmacokinetic parameters.
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