DEVELOPMENT OF HYDROPHILIC MATRIX TABLET OF CARBAMAZEPINE USING 33 FULL FACTORIAL EXPERIMENTAL DESIGNS
Keywords:
Design of experiment, Hydroxypropyl methycellulose, Full factorial design, Design space, Targeted dissolution profileAbstract
Objective: The study aims at developing the hydrophilic matrix tablet of carbamazepine (CBZ) using an optimization technique. The purpose of the study was to develop the hydrophilic matrix dosage form using the combination of different viscosity grades of hydroxypropyl methylcellulose (HPMC) to get the release within the desired target dissolution profile (TDP).
Methods: A full factorial design was employed to develop once a day matrix tablet using hydrophilic matrix polymers like HPMC K4M (X1), HPMC K15M (X2) and HPMC K100M (X3) as independent variables and the percent drug release at 1h (Y1), 8h (Y2) and 20h (Y3) was considered as dependent variables. The optimization and the design space were obtained using response surface methodology and multiple response optimization using the polynomial equation.
Results: The result indicates that concentration of all the three polymers plays an important role in the release of the drug for 24h. The formulated tablets have good physical properties and the optimized formulation prepared using design space showed the release within the target dissolution profile and followed zero order release pattern.
Conclusion: The results demonstrated that design of an experiment can be used to develop hydrophilic matrix dosage form with the desired drug release properties.
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References
Alderman DA. A review of cellulose ethers in hydrophilic matrices for oral controlled-release dosage forms. Int J Pharm Tech Prod Mfr 1984;5:1-9.
Colombo P. Swelling-controlled release in hydrogel matrices for oral route. Adv Drug Deliv Rev 1993;11:37–57.
Siepmann J, Peppas NA. Modelling of drug release from delivery systems based on hydroxylpropyl methylcellulose (HPMC). Adv Drug Deliv Rev 2001;48:139-57.
Jamzad S, Fassihi R. Development of a controlled release low dose class II drug-Glipizide. Int J Pharm 2006;312:24-32.
Ford JL, Rubinstein MH, McCaul F, Hogan JE, Edgar PJ. Importance of drug type, tablet shape and added diluents on drug release kinetics from hydroxylpropyl methylcellulose matrix tablets. Int J Pharm 1987;40:223-34.
Rao KVR, Padmalatha DK, Buri P. Influence of molecular size and water solubility of the solute on its release from swelling and erosion controlled polymeric matrices. J Control Rel 1990;12:133-41.
Badshah A, Subhan F, Rauf K. Controlled release matrix tablets of olanzapine: influence of polymers on the in vitro release and bioavailability. AAPS Pharm sci Tech 2010;11:1397-04.
Kranz H, Wagner T. Effects of formulation and process variables on the release of a weakly basic drug from single unit extended release formulations. Eur J Pharm Biopharm 2006;62:70-6.
Streubel A, Siepmann J, Dashevsky A, Bodmeier R. pH-independent release of a weakly basic drug from water-insoluble and soluble matrix tablets. J Control Release 2000;67:101-10.
Reynolds JEF. Martindale, The extra pharmacopoeia. London, The Royal Pharmaceutical Society of Great Britain; 1993. p. 295.
Löbenberg R, Amidon GL. Modern bioavailability, bioequivalence and biopharmaceutics classification system; new scientific approaches to international regulatory standards. Eur J Pharm Biopharm 2000;50:3-12.
Rinaki E, Valsami G, Macheras P. Quantitative biopharmaceutics classification system: The central role of dose/solubility ratio. Pharm Res 2003;20:1917-25.
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 April 2009;8(2):145-52.
Sivenius J, Heinonen E, Lehto H, Jaarvensivu P, Anttila M, Ylinen A, et al. Reduction of dosing frequency of carbamazepine with a slow release preparation. Epilepsy Res 1988;2:32-6.
Mohammed FA, Aarunachalam A, Reddy VG, Pallavi V, Sk Moulali, Rama Raju TVT. Formulation and evaluation of carbamazepine extended release tablets USP 200 mg. IJBPR 2012;3(1):145-53.
Aziz SH, Abdulrasool AA, Hussein AA. Factors affecting the formulation of carbamazepine extended release tablet. Iraqi J Pharm Sci 2008;17(1):55-63.
Barakat NS, Elbagory IM, Almurshedi AS. Controlled-release carbamazepine matrix granules and tablets comprising lipophilic and hydrophilic components. Drug Delivery 2009;16(1):57–65.
Lee PI. Novel zero order drug delivery via immobilized nonuniformed drug distribution in glassy hydrogels. J Pharm Sci 1984;7:1344-7.
Korsmeyer RW, Doelker GEP, Peppas NA. Mechanisms of potassium chloride from compressed hydrophilic polymeric matrices: Effect of entrapped air. J Pharm Sci 1983;72:1189-91.
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.
Moneghini M, Voinovich D, Perissutti B, Princivalle F. Action of carriers on carbamazepine dissolution. Pharm Dev Technol 2002;7:289-96.
Katzhendler I, Azoury R, Friedman M. Crystalline properties of carbamazepine in sustained release hydrophilic matrix tablets based on hydroxypropyl methylcellulose. J Control Release 1998;54(1):69-85.
Pani NR, Nath LK. Development of controlled release tablet by optimizing HPMC: Consideration of theoretical release and RSM. Carbohydr Polym 2014;104:238–45.