DEVELOPMENT AND EVALUATION OF FLOATING TABLET OF METOPROLOL SUCCINATE FOR INCREASED BIOAVAILABILITY VIA IN VIVO STUDY
DOI:
https://doi.org/10.22159/ajpcr.2019.v12i10.35934Keywords:
Gastroretentive formulation, Metoprolol succinate, Glyceryl behenate, Improved bioavailabilityAbstract
Objective: This study was performed to formulate a floating tablet using hydrophobic glyceryl behenate (GB) and hydrophilic hydroxypropyl methylcellulose polymers, optimization of the same for retention in stomach and sustained drug delivery over a period of 20 h from upper gastrointestinal tract so as to increase its oral bioavailability.
Methods: Granules of GB with the metoprolol succinate (MS) was formulated and compressed with the other ingredients to formulate a floating tablet. Physiochemical parameters of an optimized formulation along with its in vitro buoyancy study, dissolution study, in vivo studies in rabbit, and stability studies were performed.
Results: Differential scanning calorimetry data show no interaction between polymers and the drug MS. A 32 factorial design was applied for optimization purpose, and from ANOVA and surface response plot the best formulation (F3) was obtained. In vitro dissolution study shows sustained drug release for 20 h for all the formulations and in vivo studies using rabbit model show increased bioavailability of an optimized formulation F3 as compared to the marketed sustained release formulation of MS (25 mg). Stability study shows no comparable differences in physical parameters and the drug release of initial formulation and the one which is kept for accelerated stability testing.
Conclusion: Hence, we can conclude that a floating tablet containing a combination of hydrophilic and hydrophobic polymers can be used for gastric retention for more than 20 h which will increase the oral bioavailability of MS.
Downloads
References
2. Dipti P, Ganesh P, Nilesh B, Ashawat MS. Extended release formulation of BCS class i drugs. World J Pharm Pharm Sci 2015;4:1676-88.
3. Kendall MJ, Maxwell SR, Sandberg A, Westergren G. Controlled release metoprolol. Clinical pharmacokinetic and therapeutic implications. Clin Pharmaco Kinet 1991;21:319-30.
4. Hwang SJ, Park H, Park K. Gastric retentive drug-delivery systems. Crit Rev Ther Drug Carrier Syst 1998;15:243-84.
5. Sabahuddin S, Anirbandeep B, Jasmina K. Modulation of drug (metoprolol succinate) release by inclusion of hydrophobic polymer in hydrophilic matrix. Drug Dev Inds Pharm 2011;37:1016-25.
6. Kauser F, Shahi SR. Development and validation of spectrophotometric and rp-hplc method for determination of metoprolol succinate. Int J Chem Tech Res 2018;11:78-88.
7. Audumbar DM, Ritesh SB. Development and evaluation of gastro retentive floating tablets of a quinapril HCL by direct compression technique. Int J Pharm Pharm Sci 2017;9:35-46.
8. Rahi FA, Thomas LM. Formulation and in vitro evaluation of mucoadhesive antimicrobial vaginal tablets of ciprofloxacin hydrochloride. Al-mustansiriyah. J Pharm Sci 2012;12:200-13.
9. Elbary AA, Ramadan AA, Bendas IR, Mostafa DA. Formulation and evaluation of taste masked rapidly disintegration tablet containing flupentixol dihydro chloride. Int J Pharm 2011;2:58-64.
10. Kumar S, Das M, Gupta KS, Kumar R, Chongdar A, Ghosh LK. Design, development, optimisation and evaluation of gastro-retentive floating tablets of atenolol. Scholars Res Library 2013;5:436-56.
11. Singh S, Prajapati K, Pathak AK, Mishra A. Formulation and evaluation of floating tablet of captopril. Int J PharmTech Res 2011;3:333-41.
12. Sharma VK. Meloxicam loaded floating sustained release matrix tablet. J Adv Pharm Educ Res 2012;2:18-24.
13. Kavitha K, Puneeth KP, Mani TT. Development and evaluation of rosiglitazone maleate floating tablets. Int J Appl Pharm 2010;2:6-10.
14. United States Pharmacopoeia Revision Bulletin Official August 1. National Formulary. Rockville: USP Convention; 2012.
15. El-Sayed GM, El-Said Y, Meshali MM, Schwartz JB. Kinetics of theophylline release from different tablet matrices. STP Pharma Sci 1996;6:390-7.
16. Pascal P, Cauture E, Piccerelle PH, Kalantzis G, Joachim J. Evaluation of some protective agents on stability and controlled release of oral pharmaceutical forms by fluid bed technique. Drug Dev Ind Pharm 1997;23:817-26.
17. Achanta AS, Adusumilli PS, James KW, Rhodes CT. Hot-melt coating: Water sorption behavior of excipient films. Drug Dev Ind Pharm 2001;27:241-50.
18. Achanta AS, Adusumilli PS, James KW, Rhodes CT. Thermodynamic analysis of water interaction with excipient films. Drug Dev Ind Pharm 2001;27:227-40.
19. Hariharan M, Wowchuk C, Nkansah P, Gupta VK. Effect of formulation composition on the properties of controlled release tablets prepared by roller compaction. Drug Dev Ind Pharm 2004;30:565-72.
20. Obaidat AA, Obaidat RM. Controlled release of tramadol hydrochloride from matrices prepared using glyceryl behenate. Eur J Pharm Biopharm 2001;52:231-5.
21. Raymond CR, Paul JS, Marian EQ. Handbook of Pharmaceutical Excipients. 6th ed. USA: Pharmaceutical Press and American Pharmacists Association; 2009. p. 286-7.
22. Ahmed AA, Wedad KA, Fouad AA. Formulation and evaluation of prochlorperazine maleate sustained release floating tablet. Int J Pharm Pharm Sci 2017;9:89-98.
Published
How to Cite
Issue
Section
The publication is licensed under CC By and is open access. Copyright is with author and allowed to retain publishing rights without restrictions.
