ABSTRACT
The study was planned to observe the bioavailability and disposition kinetics of amoxicillin in adult rabbits [irrespective of sex] under healthy and dehydrated conditions. Comparative. Place and duration of. The study was conducted at the department of pharmacology, University of Veterinary and Animal Sciences, Lahore from April 2013 to October 2013. Initially all rabbits were weighed and their packed cell volume [PCV] and other biochemical parameters were observed under normal conditions. Bioavailability and disposition kinetics of amoxicillin [10mg/kg body weight] were studied in normal rabbits following oral and intravenous route of drug administration. After 10 days washout period, these rabbits were made dehydrated by keeping the animals off water but not food. The animals with 10% decrease in body weight were declared dehydrated. Their parameters were again measured. Treated rabbits were administered amoxicillin orally and intravenously [10mg/kg body weight]. Samples were drawn at prescribed time. Amoxicillin was assessed in plasma by using microbiological assay method. Plasma concentration was analyzed using non compartmental method. The water deprived or dehydrated rabbits showed a significant increase in the packed cell volume, blood glucose and plasma globulins as compared to the normal rabbits. However, there was a significant decrease in body weight, total proteins, albumins and albumin globulin ratio of the dehydrated rabbits. The peak plasma concentration, volume of distribution and rate constant of elimination was lower in the dehydrated rabbits as compared to the normal rabbits. The plasma concentration of amoxicillin after intravenous administration in dehydrated rabbits had a significant larger area under curve, area under 1[st] moment curve, a longer half life and a larger mean residence time. The study in the dehydrated rabbits indicated the need of modification of dosage regimen
ABSTRACT
Carvedilol is an anti-hypertensive agent capable of blocking both alph [a] and beta [p] receptors used to preclude cardiac arrhythmias and angina
The study was designed to evaluate the Pharmacokinetics of carvedilol in human male and female volunteers
Healthy male and female [twenty each] volunteers were finalized for the study after preliminarily clinical examination. Blood samples were collected at specific time intervals after giving an oral dose of 12.5mg carvedilol, separated the plasma and placed at -80°C until analysis. Estimation of carvedilol in human plasma was accomplished by High performance liquid chromatographic [HPLC] method using fluorescent detector
Plasma concentration-time curve was used for calculation of pharmacokinetic parameters using two-compartment open model
Mean [SD] values of AUC and C[max] 0.076+/-0.021microg.h/ml and 0.024+/-0.005microg/mL, respectively] in male differ significantly [P<0.05] from the female 0.197+/-0.042jug.h/ml and 0.048+/-0.02microg/mL, respectively]
Overall, bioavailability of carvedilol was somewhat higher in females than in males, but these differences could be expounded by the lower body weight of female
Conversely, no significant differences were found for tmax, clearance and half-life in male and female
Moreover the ethnicity had significant impact on the Pharmacokinetics of carvedilol in human
ABSTRACT
Montelukast is a leukotrien receptor antagonist used for asthma treatment. Objective of this study was to evaluate the bioequivalence of two montelukast 10mg tablets, Innovator drug [Singulair] as reference and other locally manufactured drug [Montiget] in 12 healthy volunteers. It was randomized, single dose, two-period crossover study with 1 week washout period. Blood samples [4-5 ml] were collected before and after drug administration and plasma was separated for analysis. Concentrations of montelukast at different time intervals were determined by validated UV-HPLC method at 345nm wavelength. Bioequivalence was assessed by using non compartmental approach and also calculated the 90% confidence interval of the least-squared pharmacokinetic parameters [C[max], AUC[0-t] and AUC[0-infinity]]. On average, C[max], AUC[0-t], AUC[0-inf], was 2.35 micro g/ml, 1.28 micro g.h./ml, 1.67 micro g.h./ml, for innovator drug and 2.53 micro g/ml, 1.53 micro g.h./ml, 1.96 micro g.h./ml, for test drug, respectively. Confidence interval [90%] for C[max], AUC[0-t] and AUC[0-inf] was 89-97%, 85-91% and 81-98% respectively. No statistical difference was found between the C[max] and AUC values of test and reference drugs. The confidence intervals for C[max], AUC[0-t] and AUC[0-infinity] are fully laid within the acceptable range of FDA [80-125%], thus two formulations are considered to be bioequivalent
ABSTRACT
The fluoroquinolones are currently enjoying extensive worldwide clinical applications because of their good bioavailability and pharmacokinetic profile. Investigation into several aspects of the pharmacokinetic of all clinically relevant fluoroquinolones, have been carried out notably in Europe, USA and Japan. In view of the 'geonetical' [geographical influences on genetics-pharmacogenetics] differences, it is important that for the optimal therapeutic outcome, biodisposition studies on drugs are better conducted in the population and environments where wide and extensive use of the drug is anticipated. The Objectives of study were to see the pharmacokinetic parameters in healthy young male and female volunteers. This comparative study was conducted King Edward Medical University, Lahore, Pakistan, from July 2005 to December 2005. In Pakistan where the use of antibiotics is more frequent by the general practitioners it is important to elucidate certain dose parameters it is also noticed that side effects are more in females than males so present study is conducted to calculate any differences in bioavailability on the basis of sex. The pharmacokinetic parameters of ofloxacin were determined in each of the clinically health eight young girls and boys [mean age 23.9 and 25.1 years, respectively] following a single oral dose of 400 mg tablet. The method adopted was microbiological assay. The blood samples collected at predetermined time intervals after drug administration revealed almost twice as high concentration of the drug in plasma of the girls than that in the boys. The pharmacokinetic parameters revealed significantly [p<0.01] higher values for area under curve [AUC] and C[max], and lower total body clearance [TBC] and volume of distribution in the girls than in the boys. The gender differences in pharmacokinetic parameters indicate that the dose adjustment should be considered in male and female