Pakistan Journal of Pharmaceutical Sciences

Abstract: Ciprofloxacin (CFX) belongs to the second-generation broad-spectrum fluoroquinolone antibiotic and it has been targeted for the development of new moiety against resistant microbes by the alteration at position C3 (carboxylic group) and C7 (piperazine moiety). Seven ciprofloxacin derivatives were developed, out of them three were found to be potent against resistant microbes. In current research study, we present the pharmacokinetics parameters of CFX and derivatives using animal model. Fifteen rabbits were fasted for 12 h before given single oral dose of 40mg/kg CFX and analogues. The blood sample of rabbits were collected over the period of 0 to 24 h. The parameters of pharmacokinetics of CFX and analogues were evaluated by validated high performance liquid chromatography (HPLC) method. The results unveiled that, the CFX and analogues were quickly absorbed, distributed, and moderately eliminated for the animal body. The volume of distribution was large with (Vdss) value of 263.51-1068.89 (mg)/(?g/ml). The total body clearance (CL) of ciprofloxacin and its 3 mentioned analogues were in the range of 42.35 to 200.16 mg/(?g/ml) in each hour. The peak plasma concentration (Cmax) of 1.04-5.66 ?g/mL was attained at 0.5 h which is showing its time for achieving maximum plasma concentration (Tmax). The elimination half-life (T1/2) was 4.055-10.14 h. The preclinical pharmacokinetics study revealed that all analogues of CFX indicates that the analogues have better pharmacokinetics than the parent compound, Ciprofloxacin, after oral administration.