Citation: Chandan Mohanty & KV Subrahmanyam. In-Vivo Pharmacokinetic Study of Matrix Tablets of Atenolol Prepared by
Sintering Technique. Sch Acad J Pharm, 2021 Apr 10(4): 71-76.
71
Scholars Academic Journal of Pharmacy
Abbreviated Key Title: Sch Acad J Pharm
ISSN 2347-9531 (Print) | ISSN 2320-4206 (Online)
Journal homepage: http://saspublishers.com
In-vivo Pharmacokinetic Study of Matrix Tablets of Atenolol Prepared
by Sintering Technique
Chandan Mohanty
1*
, KV Subrahmanyam
2
1
Guru Nanak Institutions Technical Campus-School of pharmacy, Ibrahimpatnam, Hyderabad-501506, Telangana, India
2
Siddhartha Institutions of Pharmacy, Narapally (V), Ghatkesar (M), Hyderabad-501506, Telangana, India
DOI: 10.36347/sajp.2021.v10i04.003 | Received: 21.02.2021 | Accepted: 10.04.2021 | Published: 13.04.2021
*Corresponding author: Chandan Mohanty
Abstract Original Research Article
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 (C
max
, T
max
, AUC, K
E
and t
1/2
) were estimated. T
max
for pure drug, unsintered and sintered
tablets was found to be 2h, 3hr and 4h with C
max
values of 751.00 ± 10.53 ng/ml, 639.33± 10.40 ng/ml and 518.00 ±
8.54 ng/ml respectively. Increase of T
max
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 (T
1/2
) and decrease in elimination rate constant (K
E
) 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.
Key words: In-vivo, Sintering, Pharmacokinetic Parameters, Controlled release, Matrix Tablet, Atenolol.
Copyright © 2021 The Author(s): This is an open-access article distributed under the terms of the Creative Commons Attribution 4.0 International
License (CC BY-NC 4.0) which permits unrestricted use, distribution, and reproduction in any medium for non-commercial use provided the original
author and source are credited.
INTRODUCTION
Atenolol (2-(4-{2-hydroxy-3-[(propan-2-yl)
amino] propoxy} phenyl) acetamide) is a selective β1
receptor blocker, widely prescribed in hypertension,
arrhythmias, angina pectoris, and myocardial infraction.
Atenolol is included in class III category of BCS
(biopharmaceutics classification system), that is high
aqueous solubility and low gastrointestinal permeability
[1]. The absorption of Atenolol after oral administration
is rapid (peak plasma levels reaches in 2-4 hr) and
consistent but incomplete [2]. Moreover, Atenolol has
been reported to undergo extensive hepatic first-pass
metabolism. Hence, oral bioavailability of Atenolol is
only 50-60% and left behind being excreted unchanged
in feces. In antihypertensive treatment, the oral dose of
Atenolol is 50 mg in conventional release system, twice
a daily. But administration of conventional release
tablets of Atenolol has been reported to exhibit
fluctuations in plasma concentration of the drug,
resulting either in adverse effects due to systemic
accumulation of drug like nausea, ischemic colitis,
diarrhoea and mesenteric thrombosis or decrease in
concentration of drug at the receptor site. This
combined with low oral bioavailability of atenolol make
it suitable drug for the design of sustained release
formulation to maintain a proper blood level of drug for
a long time without fluctuation [1, 3].
The concept of sintering in pharmaceutical
sciences is relatively new, but the research interests
related to this process have been growing continuously.
In powder metallurgy, sintering is defined as bonding of
adjacent particle surfaces in a mass of powder or in
compact, by the application of heat. Conventional
sintering technique involves the heating of compact at a
temperature below the melting point of the solid
constituent in controlled environment under
atmospheric pressure [4, 5]. In the pharmaceutical
science, sintering has been described as the mechanism
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