Formulation and Evaluation of Theophylline Sustained Release Tablet using Lasianthera africana gum
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Abstract
The aim of this study was to evaluate the potential of Lasianthera africana gum as sustained release matrix for the formulation of theophylline tablet and the effect of this polymer on the physical properties and drug release from the tablets. The polymer was used alone and in binary combination with Guar gum at the concentration level of 20% w/w. The theophylline granules were prepared by the wet granulation method. The micromeritic and flow propert ies of the prepared granules such as bulk density (BD), tapped density (TD), flow rate, Carr’s compressibility index (CI), Hausner’s quotient (HQ) as well as angle of repose (AR) were evaluated using standard methods. The compressed tablets were assessed for weight uniformity, crushing
strength, friability, thickness, diameter and uniformity of content. The dissolution profile of the theophylline sustained release tablets was assessed in simulated gastric fluid without the enzyme for a period of 8 h at an agitation rate of 50 rpm and a temperature of 37 ±0.5ºC. Drug release was analyzed spectrophotometrically at wavelength of 271nm using (UNICO-spectrophotometer, UV-2100PC Shanghai Instrument Co., Ltd., China). In order to investigate the release kinetics the data obtained from the in vitro dissolution studies were fitted into various kinetic models which include Zero order, First order and Higuchi. The mechanism of release was further ascertained by fitting the data of the drug release into the Korsemeyer-Peppas equation. The bulk density, tapped density, flow rate, Carr’s inde x, Hausner’s ratio and angle of repose ranged from 0.37 g/cm3 to 0.40 g/cm3, 0.53 to 0. 58 g/cm3, 4.65 to 6.90 g/s, 25.3 to 33.9 %, 1.35 to 1.52, 33.60 to 42.70, respectively. The
crushing strength ranged from 5.83 kg/f to 7.07 kg/f, friability ranged from 0.768 % to 0.910 %, diameter for all the batches was uniform (12.51mm), thickness ranged from 2.48 mm to 2.51 mm, while values for content uniformity ranged from 99.17 % to 99.26 %. The two gums sustained the release of theophylline up to 8 h. The release of theophylline followed zero order kinetics via non-Fickian transport.
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References
Al-Saidan, S.M., Y.S.R. Krishnaiah, S. Patro, V. Satyanaryana (2005)."In vitro and in vivo evaluation of guar gum matrix tablets for oral controlled release of water- soluble diltiazem hydrochloride." AAPS Pharm Sci Tech 6(1): 14-21.
British Pharmacopoeia (2008). Pharmaceutical press, Cambridge, London. Carr, R.L. Evaluating Flow Properties of Solids. Chem. Eng. 1965, 72, 163–168.
Costa, P., J.M. Sousa Lobo (2001)."Modeling and comparison of dissolution profiles." Eur. J. Pharm. Sci. 13(2): 123-133.
Ebube,N.K.,Hikal,A.,Wyandt,C.M.,Bear,D.C.,Miller,LG.,andJones,A.B.(1997)Sustained release of acetaminophen from heterogenous matrix tablets: influence of polymer ratio, polymer loading and coactive on drug release. Pharm.Dev.Technol .2:161-170.
Ellis, E.F.(2004) Theophylline in: Lieberman, P., Anderson, J.A. (eds) Current clinical practice: allergic diseases diagnosis and treatment. Humanpress, New Jersey. Pp 344-359.
Eric Chiang, (2013): Measuring Tablet Hardness, Pharmaceutical Technology 37(6)46 -59
Guathami,S and Bhat, V. R.(1929) A monograph on gum Karaya.Hyderbad: National Institute of nuitrition. Indian Council of medical Res. p.29
Hausner,H.H.(1967) Friction condition in a mass of metal powder..Intl .J powder metal.3: 7-13.
Hutchinson J, Dalziel J M.(1973).Flora of West tropical Africa.2nd edition. Vol. 1. Crown Agents for Overseas Government and Administration; p. 638. part. 2.
Iqbal,D.N., Hussain,E.A.(2010). Physiochemical and pharmaceutical properties of Guar gum derivatives. J. Report and Opinion; 2(10):77-83.
Kiattisak S, Yanee P., Helmut V., Siriporn O. (2007). Factors Influencing Dissolution Characteristics from Hydrophilic Polymer Matrix Tablet. Sci. Pharm. 75 (1) 147-163.
Korsemeyer R.W, Peppas N.A. (1983) Macromolecular and modeling aspects of swelling – controlled Systems. In: Mansdrofsz, Roseman T.J, ad, Controlled Release Delivery systems. New – York, NY: Marcel Dekker; 77.
Krishnaiah, Y., R. Karthikeyan, V. GouriSankar, V. Satyanarayana (2002). "Three-layer guar gum matrix tablet formulations for oral controlled delivery of highly soluble trimetazidinedihydrochloride." Journal of controlled release 81(1-2): 45-56
Lin, S.Y., Yang,J.C.(1989) In vitro dissolutionbehaviour of some sustained release theophylline dosage forms. Pharm. Acta-helv.64: 236-240.
Nokhodchi,A., Raja, S.,andAddo, K.A(2012). The role of oral controlled release matrix tablets in drug delivery system. Bio.impact 2(4): 176-187.
Ogbuagu, C (2004) New Government policies on pharmaceutical raw materials. Pharma news 26(12): 3
Okokon J E, Antia B S, Essiet G A.(2007); Evaluation of in vivoantiplasmodial activity of ethanolic leaf extract of Lasianthera africana. Res. J.Pharmacol. 1(2):30–33.
Patel, V.I, Patel,H.A. Jani, M. KumarS and Patel, J.A.(2012) Formulation and evaluationof okra fruit mucilage as binderin paracetamoland ibuprofen tablet. J. Pharm. Res. 1:1-4
Pash,I.S.,Murphy,P.A.,Nath,L and Chowdury,P.(2010) Kinetic modeling of drug release from controlled drug delivery systems. Acta Poloniae- Drug Res. 67: 217-223.
Prabaharan,M.(2011) Prospective of Guar gum and its derivatives as controlled release tablets. Intl. J. Bio. Macro 49(2):117-124.
Qureshi J, Ijaz H, Sethi A, Zaman M, Bashir I, Hanif M, Danish Z and Azis M (2014). Formulation and In Vitro Characterization of Sustained Release Matrix Tablets of Metoprolol Tartrate Using Synthetic and Natural Polymers. Lat. Am. J. Pharm., 33: 1533-9.
Samsam Shariat H.(1992): Qualitative and quantitative evaluation of the active constituents and control methods for medicinal plants. Mani publications, Isfahan, Iran, 202.
Stanifort, J.(2002)Powder flow in: Aulton M. E. (Ed). Pharmaceutics the science of dosage form design. Churchill Living Stone, pp197-209.
United States Pharmacopeia (2007). United States Pharmacopeial Convention Inc. Rockville. USP28 (2004). The United States Pharmacopeia 28: The national formulary 23. United States Pharmacopeial Convention.
Varshosaz J, Tavakoli N, Eram SA.(2006). Use of natural gums andcellulose derivatives in production of sustained release Metoprolol tablets. Drug Deliv. 13:113–119.