DOI: 10.36347/sajp.2021.v10i04.003

Pages: 71-76

The present study involved in-vivo pharmacokinetic evaluation of sintered matrix tablets of Atenolol in comparison to Atenolol pure drug and unsintered matrix tablets of Atenolol. The objective of the present investigation was to study the effect of sintering technique in development of controlled release dosage form. The Atenolol pure drug solution, both formulated unsintered and sintered controlled release matrix tablets of Atenolol were tested for in-vivo pharmacokinetic study in healthy male New Zealand rabbits (n=3). The plasma concentrations of Atenolol drug were determined by a validated HPLC method. From the time versus plasma drug concentration data, various pharmacokinetic parameters (Cmax, Tmax, AUC, KE and t1/2) were estimated. Tmax for pure drug, unsintered and sintered tablets was found to be 2h, 3hr and 4h with Cmax values of 751.00 ± 10.53 ng/ml, 639.33± 10.40 ng/ml and 518.00 ± 8.54 ng/ml respectively. Increase of Tmax values in sintered tablets as compared to the of pure drug and unsintered tablets suggested slow absorption of drug from the formulated sintered tablets and the availability of drug at a controlled manner. An increase of the elimination half- life (T1/2) and decrease in elimination rate constant (KE) of drug in sintered matrix tablet in comparison to the that of unsintered tablets and pure drug was also observed, indicating the prolonged and controlled systemic availability of drug in biological system. The investigated sintered matrix tablets exhibited a remarkable increase in bioavailability due to prolonged plasma residence and could maintain constant plasma level of atenolol up to 24 hr in rabbits.