STUDIES ON THE PHARMACOKINETICS OF MELOXICAM FOLLOWING INTRAVENOUS, INTRAMASCULAR AND ORAL ADMINISTRATION IN DOGS
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Date
2006
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AAU, Anand
Abstract
Meloxicam is a new non-steroidal anti-inflammatory drug of oxicam family. It is having more selectivity towards cyclooxygenase-2 rather than cyclooxygenase-1. In the present study, pharmacokinetics and dosage regimen of meloxicam was determined in mongrel dogs following single dose intravenous, intramuscular and oral administrations of meloxicam (0.4 mg.kg-1 body weight). Following intravenous route, the disposition kinetics of meloxicam was best described by a two-compartment open model. The distribution and elimination half-lives of meloxicam were 0.262 ± 0.04 and 25.94 ± 0.65 h respectively. The values of zero time plasma drug concentration and area under curve of meloxicam were 1.608 ± 0.14 μg.h ml-1 and 35.56 ± 3.62 μg.h ml−1, respectively. The values of area under moment curve were 922.3 ± 81.33. The values of apparent volume of distribution, volume of distribution at steady state, volume of drug in central compartment and volume of drug in peripheral compartment were 0.395 ± 0.05, 0.313 ± 0.04, 0.262 ± 0.01 and 0.14 ± 0.04 L.kg−1, respectively. The first order rate constants from central compartment to peripheral and peripheral to central compartment were 0.853 and 2.08 h- 1, respectively. The values of total body clearance and mean residence time were 0.195 ± 0.02 ml.min−1.kg−1 and 26.13 ± 0.51 h, respectively. On the basis of values of pharmacokinetic variables obtained by intravenous administration of meloxicam (0.4 mg.kg−1 body weight), the optimal intravenous dosage regimens of meloxicam would be 0.33 mg.kg−1 as priming dose followed by 0.28 mg.kg−1 as maintenance dose to be repeated at 72 h interval. In present study, the Pharmacokinetic of meloxicam through intramuscular and oral route of administration were described by non-compartmental analysis in dogs. The elimination half-lives for i.m and oral route of administration was 23.41 ± 0.93 h and 21.18 + 1.22 h, respectively. The values of area under curve were 33.40 ± 2.02 μg.h.ml-1 and 32.62 + 2.14 μg.h.ml-1 for i.m and oral route of administration, respectively. The value of area under first moment of curve were found to be 1259 ± 35.1 μg.h2.ml-1 and 1607.29 + 185 μg.h2.ml-1. The values of MRT were 38.38 ± 2.46 and 48.72 + 3.63 h, respectively. Values of F for i.m. and oral study were 0.96 ± 0.06 and 0.95± 0.07 % respectively. On the basis of observed meloxicam concentration in plasma, the drug can be given intramuscularly or orally at dose rate of 0.4 mg/kg to be repeated at an interval of 48 h.
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VETERINARY PHARMACOLOGY, A Study