Bioavailability of Ampicillin in Sera Healthy Volunteers

Abstract

III the staff for giving me the chance to get and finish my A.M degree. I would like to express my whole-hearted gratitude and sincere love to (my father and mother) who are considered as the secrete behind my success. I would like to express many words of thanks to my wifewho supported me all the time and shared me all the difficulties that I have faced during the qualifying year. My great gratitude due to my uncle's nice family, for their help, support and patience. I extend my true thankfulness to the employees of the Technology Sciences Ministry, College of Baghdad; all those who support and help me in everything, my brothers and sisters, Dr.Abass Shebeeb, Al- Haj Saadon, Mr. Dhafer, Dr. Thaka'a, Russul younis, Abu- Dyar, Maryam A.Hmed, Mr. Saad Saleem, my colleagues; Ahmed Mudhafar, Noor Jassim, Noor Qasim and for all those who advised and presented me sincere help and advice. The researcher... IV Abstract Ampicillin is an antibiotic of β-lactam group compounds which are widely used in the treatment of infectious diseases. The bioavailability of ampicillin (500 mg) after a single dose orally administrated is investigated in twenty Iraqi healthy volunteers for both genders with different ages, weights and heights with their consents. Sera concentrations of ampicillin are determined at various times after dose administration, by High Performance Liquid Chromatography (HPLC). The new method was carried out by using [fast column C-18, (50 × 4.6 mm I.D, 3 􀁐m particle size],sensitive (detection limit =0.02 μg.ml-1),linearity (R2=0.9999), retention time=3.307 min and can be applied to determine the drug concentration in sera and study on pharmacokinetics. In this study ampicillin is well absorbed rapidly after single dose administration (maximum time Tmax 1.0 hr) and without clinically adverse effects on volunteers. Absorption rate of ampicillin in males almost slightly higher than absorbed in females, but the elimination rate equal to both genders, depending upon pharmacokinetic parameters: Area under curve concertation AUC0-8(19.18 ±0.51, 18.68 ±0.89)μg.ml-1.hr, maximum concentration Cmax (7.37±0.46, 6.87±0.72) μg.ml-1, elimination rate constant ke(0.52±0.03, 0.53±0.03) hr-1, T1/2(1.35±0.08, 1.31±0.08) hr, and absorption rate constant ka (1.75±0.07, 1.69±0.06)hr-1 for males and females respectively The pharmacokinetic parameters for all healthy volunteers (Cmax) is found to be 7.15±0.63 μg.ml-1 occurring Tmax of 1.0 hr, T1/2, AUC0-8 , ka and ke values are found to be 1.33±0.08 hr, 18.96±0.75 μg. ml-1 hr, 1.73±0.07 hr -1 and 0.52±0.03 hr -1, respectively. The effect of volunteers characteristics on bioavailability ampicillin, the results studied show there is no clear effect for weight and height but there is slight effect for age and gender for drug absorption.