Design and In vivo evaluation of Metoprolol Tartrate bilayer floating tablets in healthy human volunteers
Keywords:
Metoprolol tartrate, superdisintigrants, HPMC, bilayer floating tablets, bioavailabilityAbstract
The aim of the present investigation was to prepare bilayer floating tablets of metoprolol tartrate using the combination of superdisintigrants, HPMC K grade polymers and natural polymers like xanthan gum and guar gum by direct compression method. Bilayer floating tablets were prepared using optimized immediate release layer and floating layer as sustained release layer. The physicochemical characteristics of the prepared tablets were evaluated and found to be satisfactory. All the prepared batches showed in vitro buoyancy. It was observed that the tablets remained buoyant for more than 12 h. Formulation F7 was selected as best formulation based on the in vitro characteristics and used in vivo radiographic studies by adding barium sulphate. These studies revealed that the tablets remained in the stomach for 210μ5.4 min (n=3) in fasting human volunteers. Based on the in vivo performance in healthy subjects, the developed bilayer floating tablets showed superior bioavailability than the marketed tablets, the drug release was up to 12 h in controlled manner. The systemic availability of the best formulation was high after administration to obtain immediate action due to the immediate release layer, from sustained release layer the drug was released in controlled manner. It can be concluded that the best formulation F7 by choosing biphasic drug release pattern in a single dosage form could improve patient compliance and ensure better disease management.
References
. Priti T, Nidhi J, Pathak AK.
Formulation and evaluation of bilayer
floating tablets of Metoprolol tartrate.
Int J Biomed Adv Res. 2012; 03(02):
-128.
. Patel N, Nagesh C, Patel J,
Chandrasekhar S, Jani D. Formulation
and evaluation of floating tablet
containing Glipizide. Asian J. Pharm.
Tech. 2012; 2(4): 135-140.
. Harshal PG, Manohar VP, Bharat WT,
Vinod MT, Patil VR. Formulation and
in vitro evaluation of trifluoperazine
hydrochloride bilayer floating tablet. Int
J Pharm Bio. 2012; 2 (1): 166-172.
. Nayak AK, Maji R, Das B.
Gastroretentive drug delivery systems:
a review. Asian J of Pharm and Clin
Res. 2010; 3 (1): 2-10.
. Chein YW. Novel Drug Delivery
System, 2nd ed. Marcel Dekker Inc,
New York, 1992; p. 1-3.
. Fonner DE, Buck JR, Banker GS.
Mathematical optimization techniques
in drug product design and process
analysis. J. Pharm. Sci. 1970; 59:
-1596.
. Aqil M, Ali A, Ahad A, Sultana Y,
Najmi AK, Saha N. A validated HPLC
method for estimation of metoprolol in
human plasma. Acta Chromatograph.
; 19: 130-140.
. Hirtz J. The GIT absorption of drugs in
man: a review of current concepts and
methods of investigation. Br J Clin
Pharmacol. 1985; 19: 77S-83S.
. Baumgartner S, Kristl J, Vrecer F,
Vodopivec P, Zorko B. Optimization of
floating matrix tablets and evaluation
of their gastric residence time. Int J
Pharm. 2000; 195:125-135.
. USP 27/NF 22, Asian edition, General
test procedures, U.S. Pharmacopoeial
convention, Rockville MD. 2004:1204.
. Sharma D. Formulation development
and evaluation of fast disintegrating
tablets of salbutamol sulphate for
respiratory disorders, ISRN
Pharmaceu. 2013; 2013: 1-8.
. Moiz Md, Prathima Srinivas M,
Sadanandam M. Formulation and
evaluation of bilayered tablets of
montelukast and levocetrizine
dihydrochloride using natural and
synthetic polymers. Int J D Del. 2011;
: 597-618.
. Nerurkar J, Jun HW, Prince JC, Park
MO. Controlled release matrix tablets
of ibuprofen using cellulose ethers and
carrageenans: effect of formulation
factors on dissolution rate. Eur J
Pharm Biopharm. 2005; 61: 56-68.
. Puneeth KP, Kavitha K, Tamizh MT.
Development and evaluation of
rosiglitazone maleate floating tablets.
Int J Appl Pharm. 2010; 2(2): 6-10.
. Mohsin AA, Nimbalkar NE, Sanaullah
S, Aejaz A. Formulation and
evaluation of mouth dissolving tablets
of amitryptyline hydrochloride by direct
compression technique. Int J Pharm
Sci. 2010; 2(1): 204-210.
. Higuchi T. Rate of release of
medicaments from ointment bases
containing drugs in suspensions. J
Pharm Sci. 1961; 50: 874-875.
. Siepmann J, Peppas NA. Modelling of
drug release from delivery systems
based on hydroxypropyl
methylcellulose (HPMC). Adv D Del
Rev. 2001; 48: 139-157.
. Raghavendrarao NG, Sagar G, Tarun
P. Formulation and evaluation of
sustained release matrix tablets of
tramadol hydrochloride. Int J Phar
Pharmaceu Sci. 2009; 1: 60-70.
. Sekar V, Chellan VR. Immediate
release tablets of telmisartan using
superdisintegrant-formulation,
evaluation and stability studies. Chem.
Pharm. Bull. 2008; 56(4): 575-577.
. Mohan G, Ramesh B, Kishan V.
Development of sustained release
floating drug delivery system for
norfloxacin: In vitro and in vivo
evaluation. PDA J Pharm Sci Tech.
; 65(3): 198-206.
