24 Journal of Applied Biopharmaceutics and Pharmacokinetics, 2013, 1, 24-30 E-ISSN: 2309-4435/13 © 2013 Pharma Professional Services Disposition Kinetic of Cloxacillin in Healthy and Nephropathic Goats with Immunological and Residual Level in Blood and Tissues Sanjib Khargharia 1,* , Animesh K. Chakraborty 1 , Anjan Bhattacharyya 2 and Tapan K. Mandal 1 1 Department of Pharmacology & Toxicology, West-Bengal University of Animal and Fishery Sciences, Mohanpur, Nadia-741252, West-Bengal, India 2 Department of Agricultural Chemicals, Bidhan Chandra KrishiViswavidyalaya, Mohanpur, Nadia-741252, West-Bengal, India Abstract: In the present investigation, we evaluated the efficacy of pharmacokinetic profile in healthy as well as nephropathic black-Bengal goats (n=6) of either sex through single intravenous route along with metabolism aspects in all vital organs as well as urine. Nephropathic goats resulted higher B (41.03 ± 3.87 gmL -1 ), t1/2(1.17 ± 0.06hr) and low (0.59 ± 0.03 hr -1 ) and ClB (25.70 ± 2.86 mlh -1 kg -1 ) compared to healthy goats. Continuous administration via intramuscular route up to 60 days revealed biochemical, hematological, histopatholocial changes in therapeutic (TP) as well as below therapeutic dosage (HTP) level in black-Bengal goats. Present study also revealed immunosuppressive effect during 60 days continuous intramuscular administration and confirmed stimulatory effect on hepatic microsomal enzyme system. Keywords: Cloxacillin, pharmacokinetic, hematological, biochemical, immunological studies. INTRODUCTION Antibiotic treatment of patients remains a significant challenge for all nations with persisting high mortality and morbidity rates. The importance of effective therapy continues to grow with increasing numbers of patients with increasing levels of sickness. Compelling evidence suggests that in patients, source control of the pathogen is appropriate antibiotic therapy which remains the most important intervention that the clinician can implement at early. Therefore, optimizing antibiotic therapy should be a priority in the management for patients. Some of these antibiotics are encountered by the organism over long period of time. Continuous low level exposure to such antibiotics may increase the susceptibility of the host to various diseases due to immunity breakdown. It has therefore, become important to screen antibiotic at therapeutic dose level with respect to their immunotoxic, biochemical and hematological potential. Cloxacillin, semi synthetic amino penicillin which has activity against penicillin-sensitive gram positive as well as some gram negative bacteria continues to be a useful antimicrobial drug for its low index of toxicity and reliable absorption which continues to make it an attractive agent in the treatment of variety of infections. Pharmacokinetic is concerned with study and *Address correspondence to this author at the MNPC, University of Iowa, Iowa City, IA-52246, USA; Mobile: 3194008179; E-mail: sanjibkharghoria@yahoo.com characterization of time course of drug absorption, distribution, metabolism and excretion [1]. Disease states alter the pharmacokinetic parameters of many drugs. It has been reported that the kinetic behavior of many drugs were altered following administration by different routes in experimentally induced diseased models of goats and dogs [2-4]. The routine use of conventional dosage regimen in patients suffering from liver and/or renal diseases may result in excessive accumulation of drug in the body and consequently may expose the patient to an excessive risk of serious side effects and toxicity. So in the present investigation, we evaluated disposition kinetics of cloxacillin after single intravenous (IV) administration in healthy as well as nephropathic black-Bengal goats. Accumulation of this antibiotic after long term exposure in vital organs and urine were evaluated after repeated therapeutic (TP) and one half of therapeutic dose (HTP) consecutively for 60 days through intramuscular (IM) administration and investigated its role in blood biochemistry and liver cytochrome P 450 component to screen for immunotoxic, biochemical and hematological potential. MATERIALS AND METHODS Materials Cloxacillin was obtained as gift from M/S Alembic Ltd, Mumbai, India. The purity of the compound was 98%.