Design and Optimization of Novel Sugar Alcohol Based Extended Release Tablets Prepared by Melt Dispersion Technique Sugar alcohol as controlled release carrier
Iranian Journal of Pharmaceutical Sciences,
Vol. 8 No. 2 (2012),
1 April 2012
,
Page 83-98
https://doi.org/10.22037/ijps.v8.40975
Abstract
The aim of this study is to prepare novel sorbitol based extended release tablets by melt dispersion method using carbamazepine as a model drug. Carbamazepine was melted along with sugar alcohol to get melt dispersion granules (MGDs) and was characterized by differential scanning calorimetry (DSC), powder X-ray diffractometry (XRD) and solubility study. The physical and chemical parameters of MDGs and tablets were measured while drug release was studied using USP II dissolution apparatus. The release data were subjected to different models to evaluate their release kinetics and mechanisms. Evaluation of MDGs using XRD and DSC indicated that melt dispersion process converted crystalline carbamazepine and sugar alcohol into lower crystallinity with no significant improvement in solubility. The drug release rate was found to be affected by sugar alcohol concentration, particle size of MDGs, the nature of co-excipients, agitation rate and hardness. The kinetics of carbamazepine release from formulation (F3) showed best fit to Higuchi and super case II transport mechanism. It can be concluded that sorbitol is a suitable matrix-forming agent to sustain the release of low soluble drug carbamazepine. Melt dispersion technique using sorbitol is proved to be a promising technique for controlled drug delivery.
Keywords:
- Carbamazepine
- Extended release tablets
- Melt dispersion
- Sorbitol
- Sugar alcohol
How to Cite
Balamurugan Jeganathan, & Vijayalakshmi Prakya. (2012). Design and Optimization of Novel Sugar Alcohol Based Extended Release Tablets Prepared by Melt Dispersion Technique: Sugar alcohol as controlled release carrier. Iranian Journal of Pharmaceutical Sciences, 8(2), 83–98. https://doi.org/10.22037/ijps.v8.40975
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[36] Kincl M, Meleh M, Veber M. Study of physiochemical parameters affecting the release of diclofenac sodium from the lipophilic matrix tablets. Acta chim Slov 2004;1: 409-25.
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[38] Ritger PL and Peppas NA. A simple equation for description of solute release. I. Fickian and nonfickian release from non-swellable devices in form of slabs, spheres, cylinders or discs. J Control Release 1987;5: 23–36.
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[40] El-shanawany S. Sustained-release of nitrofurantoin from inert wax matrixes. J Control Release 1993;26:11-9.
[2] Gines JM, Veiga MD, Arias MJ, Rabasco AM. Elaboration and thermal study of interactions between cinnarizine and gelucire® 53/10 physical mixtures and solid dispersions. Int J Pharm 1995; 126: 287-91.
[3] Liu C, Wu J, Shri B, Zhang Y, Gao T, Pei Y. Enhancing the bioavailability of cyclosporin a solid dispersion containing polyoxyethylene(40) stearate. Drug Dev Ind Pharm 2006; 22: 110-22.
[4] Sahoo J, Murthy PN, Biswal S, Manik. Formulation of sustained-release dosage form of verapamil hydrochloride by solid dispersion technique using eudragit rlpo or kollidon®sr. AAPS Pharm Sci Tech 2009; 10: 27-33.
[5] Jagdale S, Ghorpade S, Bhavsar D, Kuchekar B, Chabukswar A. Effect of wax on the release pattern of drugs from the sustained release fatty matrix tablet. J Chem Pharm Res 2010; 2: 330-8.
[6] Deore RK, Kavitha K, Tamizhmani TG. Preparation and evaluation of sustained release matrix tablets of tramadol hydrochloride using glyceryl palmitostearate. Trop J Pharm Res 2010; 9: 275-81.
[7] Kavitha K, Deore RK, Tamizhmani TG. Preparation and evaluation of sustained release matrix tablets of tramadol hydrochloride using compritol 888 ATO by melt granulation technique. Res J Pharm Biol Chem Sci 2010; 1: 431-40.
[8] Vaz CM,van Doeveren PF, Reis RL, Cunha AM. Soy matrix drug delivery systems obtained by melt-processing techniques. Biomacromolecules 2003; 4: 1520-9.
[9] Elzoghby AO, El-Fotoh WS, Elgindy NA. Caseinbased formulations as promising controlled release drug delivery systems. J Control Release 2011; 153: 206-16.
[10] Szuts A, Makai Z, Rajkob R, Revesz PS. Study of the effects of drugs on the structures of sucrose esters and the effects of solid-state interactions on drug release. Eur J Pharm Biopharm 2008; 48:1136-42.
[11] Goyanes A, Souto C, Pacheco RM. Control of drug release by incorporation of sorbitol or mannitol in microcrystalline-cellulose-based pellets prepared by extrusion-spheronization. Pharm Dev Tech 2010; 15:626-35.
[12] Van Drooge DJ, Hinrichs WLJ, Frijlink HW. Anomalous dissolution behavior of tablets prepared from sugar glass-based solid dispersions. J Control Release 2004; 97: 44-52.
[13] Ochoa L, Igartua M, Hernandez RM, GasconAR, Solinis MA, Pedraz JL. Novel extended-release formulation of lovastatin by one-step melt granulation: in vitro and in vivo evaluation. Eur J Pharm Biopharm 2011; 77: 306-12.
[14] Fukuda M, Peppas NA, McGinity JW. Properties of sustained release hot-melt extruded tablets containing chitosan and xanthan gum. Int J Pharm 2006; 310: 90-100.
[15] Korsmeyer RW, Gurny R, Docler E, Buri P and Peppas NA .Mechanism of solute release from porous hydrophilic polymers. Int J Pharm 1983;15:25–35.
[16] Costa P and Lobo JMS. Modeling and comparison of dissolution profiles. Eur J Pharm Sci 2001; 13:123–33.
[17] Berger CM, Tsinman O, Voloboy D, Lipp D, Stones S and Avedeef A. Miniaturized intrinsic dissolution rate (mini-idr) measurement of griseofulvin and carbamazepine. Disso Tech 2007;11:39-41.
[18] Abdou H.M. Dissolution, Bioavailability and Bioequivalence. Mack Publishing Company, Easton, Pennsylvania 1989;53–72.
[19] Nokhodchi A, Bolourtchian N and Dinarvand R. Dissolution and mechanical behaviors of recrystallized carbamazepine from alcohol solution in the presence of additives. J Crystal Growth 2005;274: 573–84.
[20] Bolourtchian N, Nokhodchi A and Dinarvand R.The effect of solvent and crystallization conditions on habit modification of carbamazepine. Daru 2001;9:12–22.
[21] Grzesiak AL, Lang M, Kim K and Matzger AJ.Comparison of the four anhydrous polymorphs of carbamazepine and the crystal structure of form Int. J Pharm Sci 2003;92: 2260–71.
[22] Sztatisz J, Fodor GI and Pungor E. Thermal investigations on the crystallization of sorbitol. J Therm Anal 1977;12: 351-60.
[23] Kavanagh N and Corrigan OI. Swelling and erosion properties of hydroxypropylmethylcellulose (Hypromellose) matrices- influence of agitation rate and dissolution medium composition. Int J Pharm 2004;279:141–52.
[24] Raghuram RK, Srinivas M and Srinivas R. Once daily sustained release matrix tablets of nicorandil:formulation and in vitro evaluation. AAPS Pharm Sci Tech 2003;4 (4): Article 61.
[25] Amaral MH, Sousa JM and Ferreira DC. Effect of hydroxypropyl methylcellulose and hydrogenated castor oil on naproxen release from sustained release tablets. AAPS Pharm Sci Tech 2001;2(2): Article 6.
[26] Reza MS, Quadir M A and 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.
[27] Quadir MA, Rahman MS, Karim MZ, Akter S, Awakt MT and Reza MS. Evaluation of hydrophobic materials as matrices for controlledrelease drug delivery. Pak J Pharm Sci 2003;16:17-28.
[28] Abdelkader H, Abdalla O Y and Salem H.Formulation of controlled- release baclofen matrix tablets ii: influence of some hydrophobic excipients on the release rate and in vitro evaluation. AAPS Pharm Sci Tech 2008;9: 675-83.
[29] Chris HO and Chi Hwang GW. Development of extended-release solid dispersions of nonsteroidal anti-inflammatory drugs with aqueous polymeric dispersions: optimization of drug release via a curvefitting
technique. Pharm Res 1992;9: 206-10.
[30] Tiwari G, Srivastava B and Rai AK. Development and optimization of multi-unit solid dispersion systems of poorly water soluble drug. Res J Pharm Tech 2008;1: 444-9.
[31] Dahl TC, Calderwood T, Bormeth A, Trimble K and Piepmeir E. Influence of physico-chemical properties of hydroxypropyl methylcellulose in naproxen release from sustained release matrix tablets. J Control Release 1990;14:1-10.
[32] Crowley MM, Schroeder B, Fredersdorf A, Obara S, Talarico M, Kucera S, McGinity JW. Physicochemical properties and mechanism of drug release from ethyl cellulose matrix tablets prepared by direct compression and hot-melt extrusion. Int J Pharm 2004;269:509–22.
[33] Ravi PR, Ganga S and Saha RN. Design and study of lamivudine oral controlled release tablets. AAPS Pharm Sci Tech 2007;8 (4): Article 101.
[34] Tiong N and Elkodry AA. Effects of liquisolid formulations on dissolution of naproxen. Eur J Pharm Biopharm 2009;73: 373-84.
[35] Lee H, Park SAe, Sah H. Surfactants effects of Carbamazepine immediate release tablet. Arch Pharm Res 2005;28:120-6.
[36] Kincl M, Meleh M, Veber M. Study of physiochemical parameters affecting the release of diclofenac sodium from the lipophilic matrix tablets. Acta chim Slov 2004;1: 409-25.
[37] Ravi PR, Kotreka UK and Saha RN. Controlled release matrix tablets of zidovudine: effect of formulation variables on the in vitro drug release kinetics. AAPS Pharm Sci Tech 2008;9: 302-13.
[38] Ritger PL and Peppas NA. A simple equation for description of solute release. I. Fickian and nonfickian release from non-swellable devices in form of slabs, spheres, cylinders or discs. J Control Release 1987;5: 23–36.
[39] Liu J, Zhang F and McGinity JW. Properties of lipophilic matrix tablets containing phenylpropanolamine hydrochloride prepared by hot-melt extrusion. Eur J Pharm Biopharm 2001;52:181-90.
[40] El-shanawany S. Sustained-release of nitrofurantoin from inert wax matrixes. J Control Release 1993;26:11-9.
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