Formulation and in vitro evaluation of nifedipine- controlled release tablet: Influence of combination of hydrophylic and hydrophobic matrix forms

Katayoun Derakhshandeh, Marzieh Soleymani

Abstract


The aim of the present work was to develop controlled release matrix formulation of nifedipine and investigate the effects of both hydrophilic and hydrophobic polymers on in vitro drug release. Matrix tablets were prepared by wet granulation
technique using different concentration of hydroxy propyl methyl cellulose (HPMC), ethyl cellulose (EC), compressible Eudragits (RSpo and RLpo) and their combination in different ratios to examine their influence on tablet properties and
drug release profile.Tablets were evaluated by measurement of hardness, friability, content uniformity, weight variation and drug release pattern. Release studies were carried out using USP type II apparatus in 900 ml of sodium phosphate buffer (pH 7.4) with 0.5% (w/v) SDS. The amount of drug released was determined at 238 nm by UV-visible spectrophotometer.
In vitro dissolution studies indicated that hydrophobic polymers significantly reduced the rate of drug release compared to hydrophilic ones in 12 hrs and combination of both polymers exhibited the best release profile to sustain the drug release for prolong period of time. As a result, the tablet containing HPMC:EC in ratio of 0.75:1 showed better controlled release pattern over a period of 12 hrs. In selected formulation, the calculated regression coefficients for release models fitted best to zero-order models


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Apu AS, Pathan AH, Shrestha D, Kibria G, Jalil R. Investigation of In vitro

Release Kinetics of Carbamazepine from Eudragit® RS PO and RL PO

Matrix Tablets. Trop J Pharm Res 2009;8:145-52.

gastrointestinal therapeutic system (GITS), evaluation of pharmaceutical, pharmacokinetic and pharmacological properties. Clin Pharmacokin 1996;30:28-51.

Eur J Pharmacol 1996;50:195-201.

as a major determinant of its haemodynamic effects in humans. Clin

Pharmacol Ther 1987;41:26-30.

PDR (Physicians’ Desk Reference). 54th ed. Montvale, NJ: Medical

Economics Company Inc; 2000. p. 331: 2363.

Kohri N, Mori KI, Miyazaki K, Arita T. Sustained release of nifedipine

from granules. J Pharm Sci 1986;75:57-61.

Barkai A, Pathak YV, Benita S. Polyacrylate (Eudragit retard)

microspheres for oral controlled release of nifedipine. Drug Dev Ind

Pharm 1990;16:2057-75.

Chowdary KR, Ramesh KS. Controlled nifedipine release from

microcapsules of its dispersions in PVP–MCC and HPC–MCC. Drug Dev

Ind Pharm 1995;21:1183-92.

Maggi L, Torre ML, Giunchedi P, Conte U. Supramicellar solutions of

sodium dodecyl sulphate as dissolution media to study in vitro release

characteristics of sustained release formulations containing an insoluble

drug: Nifedipine. Int J Pharm 1996;135:73-9.

Mehrgan H, Mortazavi SA. The release behavior and kinetic evaluation

of diltiazem HCL from various hydrophilic and plastic based matrices.

Iran. J Pharm Res 2005;3:137-46.

Colombo P. Swelling-controlled release in hydrogel matrices for oral

route. Adv Drug Deliv Rev 1993;11:37-57.

Bravo SA, Lamas MC, Salomon CJ. Swellable matrices for the controlled-release of diclofenac sodium: Formulation and in-vitro studies. Pharm Dev Technol 2004;9:75-83

Reza MS, Quadir MA, Haider SS. Comparative evaluation of plastic,

hydrophobic and hydrophilic polymers as matrices for controlled-

release drug delivery. J Pharm Pharmaceut Sci 2003;6:282-91.

Rowe RC. Molecular weight dependence of the properties of ethyl

cellulose and hydroxypropyl methylcellulose films. Int J Pharm

;88:405-8.

Akbuga J. Furosemide-loaded ethyl cellulose microspheres prepared

by spherical crystallization technique: Morphology and release

characterization. Int J Pharm 1991;76:193-8.

Janselijak I, Nicolaidou CF, Nixon JR. Dissolution from tablets prepared

using ethylcellulose microcapsules. J Pharm Pharmacol 1977;29:169-72.

Shaikh NA, Abidi SE, Block LH. Evaluation of ethyl cellulose as a

matrix for prolonged release formulations. Part 1. Water-soluble

drugsacetaminophen theophylline. Drug Dev Ind Pharm 1987;13:1345-69.

Kibbe AH. Handbook of pharmaceutical excipients. Washington, D.C.:

USA, American Pharmaceutical Association; 2000. p. 401-6.

Garg R. Pre-formulation: A need for dosage form design. Pharmainfo

Net 2008. vol.6. Banker G, Rhodes CT. Modern Pharmaceutics. New York: Marcel Dekker, Inc.; 2000.

Pharmacopoeia of India. Ministry of health and family welfare. New Delhi:

Government of India controller of publications; 2007. p. 663,183, 662.

Najib N, Suleiman M. The kinetics of drug release from ethyl cellulose

solid dispersions. Drug Dev Ind Pharm 1985;11:2169-81.

Desai SJ, Singh P, Simonelli AP, Higuchi WI. Investigation of factors

influencing release of solid drug dispersed in wax matrices III.

Quantitative studies involving polyethylene plastic matrix. J Pharm

Sci 1966;55:1230-4.

Higuchi T. Mechanism of sustained action medication. Theoretical

analysis of rate of release of solid drugs dispersed in solid matrices. J

Pharm Sci 1963;52:1145-9.

Korsmeyer RW, Gurny R, Doelker E, Buri P, Peppas NA. Mechanisms

of solute release from porous hydrophilic polymers. Int J Pharm

;15:25-35.

Banker GS, Anderson LR. Tablets. In: Lachman L, Liberman HA, Kanig

JL, editors, The theory and practice of industrial pharmacy. Mumbai,

India: Varghese Publishing House; 1987. p. 293-345.

Akubuga J. Preparation and evaluation of controlled release furosemide

microspheres by spherical crystallization. Int J Pharm 1989;53:99-105.

Patra C, Kumar AB, Pandit HK, Singh SP, Devi MV. Design and evaluation

of sustained release bilayer tablets of propranolol hydrochloride. Acta

Pharm 2007;57:479-89.

Kuksal A, Tiwary AK, Jain N, Jain S. Formulation and In vitro, In vivo

evaluation of extended- release matrix tablet of zidovudine: Influence

of combination of hydrophilic and hydrophobic matrix formers. AAPS

PharmSci Tech 2006;7:E1.

Khandai M, Chakraborty S, Sharma A, Panda D, Khanam N, Panda

SK. Development of propranolol hydrochloride matrix tablets: An

investigation of effects of combination of hydrophilic and hydrophobic

matrix forms using multiple comparison analysis. Int J Pharm Sci

;1:1-7.

Rajabi-Siabhoomi AR, Melia CD, Davies MC, Bowtell RW, Mcjury M,

Sharp JC. Imaging the internal structure of the gel layer in hydrophilic

matrix systems by NMR microscopy. J Pharm Pharmacol 1992;

:1062.

Sarfraz M, Rehamn NU, Mohsin S. Naproxen release from sustained

release matrix system and effect of cellulose derivations. Pak J Pharm

Sci 2006;19:251-5.




DOI: http://dx.doi.org/10.22377/ajp.v4i4.227

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