In VitroStudies of Controlled Release Alfuzosin Matrix TabletsPrepared with Ethylcellulose and Hydroxypropyl Methylcellulose Controlled release alfuzosin matrix tablets
Iranian Journal of Pharmaceutical Sciences,
Vol. 5 No. 2 (2009),
1 April 2009
,
Page 59-68
https://doi.org/10.22037/ijps.v5.41187
Abstract
Extended release formulation of alfuzosin, an α-antagonist used for prostatic hypertrophy, is available in market. It is convenient for older patients to take only one tablet a day. Marketed alfuzosin formulation is three layered geomatrix tablet that requires special facilities, high cost, more time and complex operation than normal direct compression formulation. Therefore, a less complicated formulation is desired which can be prepared by conventional tools. The aim of the study was the development and in vitroevaluation of a controlled release dosage form of a freely soluble weakly basic drug (alfuzosin hydrochloride). Binary mixer of one hydrophilic polymer (hydroxypropyl methylcellulose) and one hydrophobic polymer (ethyl cellulose) was used in tablets prepared by direct compression, 32factorial design was chosen and the amount of two polymers were taken as independent variables.The percent drug released at 1, 6, 12, and 20 h were selected as response. The main effect and interaction terms were quantitatively evaluated using mathematical model. Dissolution data were fitted to zero order, first order, and Higuchi’s releasekinetics to evaluate kinetic data. According to Korsmeyer's equation drug release followed both diffusion and erosion mechanism in all cases. Drug release was different from three fillers (microcrystalline cellulose, lactose and dibasic calcium phosphate).
Keywords:
- Alfuzosin
- Ethyl cellulose
- Hydroxypropyl methylcellulose
- Releasekinetics
How to Cite
Monzurul Amin Roni, Golam Kibria, & Reza-ul Jalil. (2009). In VitroStudies of Controlled Release Alfuzosin Matrix TabletsPrepared with Ethylcellulose and Hydroxypropyl Methylcellulose: Controlled release alfuzosin matrix tablets. Iranian Journal of Pharmaceutical Sciences, 5(2), 59–68. https://doi.org/10.22037/ijps.v5.41187
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[35]Gao P, Nixon P, Skoug J. Diffusion in HPMC gels.II. Prediction of drug release rates from hydrophilic matrix extended-release dosage forms.Pharm Res1995; 12: 965-71.
[36]Katzhendler I, Hoffman A, Goldbergern A,Friedman M. Modeling of drug release from erodible tablets. J Pharm Sci 1997; 86: 110-5.
[37]Mitchell K, Ford JL, Armstrong DJ, Elliott PNC,Hogan JE, Rostron C. The influence of drugs on the properties of gels and swelling characteristics of matrices containing methylcellulose or hydrox-ypropylmethycellulose. Internat J Pharm1993;100: 165-73.
[38]Huang YB, Tsai YH, Yang WC, Chang JS, Wu PC. Optimization of sustained release propranolol dosage form using factorial design and response surface methodology. Biol Pharm Bull2004; 27:1626-9.
[2]Guay DR. Extended-release alfuzosin hydrochloride: Anew alpha-adrenergic receptor antagonist for symptomatic benign prostatic hyperplasia. Am J Geriatr Pharmacother2004;2: 14-23.
[3]Foglar R, Shibata K, Horie K, Hirasawa A,Tsujimoto G. Use of recombinant a1-adrenorecep-tors to characterize subtype selectivity of drugs for the treatment of prostatic hypertrophy. Eur J Pharmacol1995; 288: 201-7.
[4]British Pharmacopoeia.London: HSMO, 2005.
[5]Uroxatral [package insert]. New York: Sanofi-Synthelabo Inc., 2003.
[6]Jardin A, Bensadoun H, Delauche-Cavallier MC,Attali P. Long-term treatment of benign prostatic hyperplasia with alfuzosin: A12-18 month assessment. BPHALF Group. Br J Urol 1993; 72:615-20.
[7]Jardin A, Bensadoun H, Delauche-Cavallier MC,Stalla-Bourdillon A, Attali P. Long-term treatment of benign prostatic hyperplasia with alfuzosin:A24-30 month survey. BPHALF group. Br J Urol1994; 74: 579-84.[8]Lukacs B, Grange JC, McCarthy C, Comet D.Clinical uroselectivity: A3-year follow-up in general practice. BPAGroup in General Practice.Eur Urol1998; 33(suppl 2): 28-33.
[9]Kerrebroeck VP, Jardin A, Laval KU, Cangh,VP.Efficacy and safety of a new prolonged release formulation of alfuzosin 10 mg once daily versus alfuzosin 2.5 mg thrice daily and placebo in patients with symptomatic benign prostatic hyperplasia. Eur Urol 2000; 37: 306-13.
[10]Viswanathan, Narayanan B, Ramakrishnan,Sankar, Raghuvanshi, Rajeev S, Rampal A.Sustained release compositions containing alfuzosin. US Patent2003; 20060147530.
[11]Cameron CG, McGinity JW. Controlled release theophylline tablet formulations containing acrylic resins, II. Combination resin formulations. Drug Dev Ind Pharm 1987; 13: 1409-27.
[12]Rekhi GS, Nellore RV, Hussain AS, Tillman LG,Malinowski HJ, Augsburger LL. Identification of critical formulation and processing variables for metoprolol tartrate extended-release (ER) matrix tablets. J Control Release1999; 59: 327-42.
[13]Hjärtstam J, Hjertberg T. Swelling of pellets coated with a composite film containing ethyl cellulose and hydroxypropyl methylcellulose.Internat J Pharm 1998; 161: 23-8.
[14]Sakellariou P, Rowe RC. The morphology of blends of ethylcellulose with hydroxypropyl methylcellulose as used in film coating. Internat J Pharm 1995; 125: 289-96.
[15]Dabbagha MA, Forda,JL, Rubinsteina MH,Hogan JE. Effects of polymer particle size,compaction pressure and hydrophilic polymers on drug release from matrices containing ethylcellulose. Internat J Pharm1996; 140: 85-95.
[16]Traconis N, Rodríguez R, Campos ME, Villafuerte L. Influence of admixed polymers on the metronidazole release from hydroxypropyl methylcellulose matrix tablets. Pharmaceutica Acta Helv 1997; 72: 131-8
[17]Sandip B, Tiwari T, Murthy K, Pai MR, Mehta PR, Chowdary PB. Controlled release formulation of tramadol hydrochloride using hydro-philic and hydrophobic matrix system. AAPS Pharm Sci Tech2003; 4: Article 31.
[18]Colombo P. Swelling-controlled release in hydrogel matrices for oral route. Adv Drug Delivery Rev1993; 11: 37-57.
[19]Vyas SP, Jain NK, Khana S. Formulation and performance evaluation of controlled-release diclofenac sodiumtablets.J Control Release1989;10: 219-23.
[20]Silvina AB, Maria CL, Claudio JS.In vitro studies of diclofenac sodium controlled-release from biopolymeric hydrophilic matrices. J Pharm Pharm Sci 2002; 5: 213-9.
[21]Lee JW, Park JH, Robinson JR. Bioadhesive-based dosage forms: The next generation. J Pharm Sci2000; 89: 850-63.
[22]Biju SS, Saisivam S, Rajan NS, Mishra PR. Dual coated erodible microcapsules for modified release of diclofenac sodium. Eur J Pharm Biopharm2004; 58: 61-7.
[23]Pearnchob N, Bodmeier R. Dry polymer powder coating and comparison with conventional liquid-based coatings for Eudragit RS, ethylcellulose and shellac. Eur J Pharm Biopharm2003; 5: 363-9.
[24]Sajeev C, Vinay G, Archna R, Saha RN. Oral controlled release formulation of diclofenac sodium by microencapsulation with ethyl cellulose. J Microencapsul2002; 19: 53-60.
[25]Iqbal Z, Babar A, Ashraf M. Controlled release naproxen using micronized ethyl cellulose by wet granulation and solid dispersion method.Drug Dev Ind Pharm2002; 28: 129-34.
[26]Pruthvipathy RK. Sathyanarayara MU, Steven HN, Amit KM. Ethyl cellulose matrix controlled release tablets of water soluble drug. Internat JPharm1995; 123: 119- 25.
[27]Liu Q, Fassihi R. Zero-order delivery of a highly soluble, low dose drug alfuzosin hydrochloride via gastro-retentive system. Internat J Pharm2008;348: 27-34.
[28]Nair A, Gupta R, Vasanti S. In vitrocontrolled release of alfuzosin hydrochloride using HPMC-based matrix tablets and its comparison with marketed product. Pharm Development Technol 2007; 12: 621-5.[29]Aulton ME. Pharmaceutics, the science of dosage form design. Oxford: Churchill Livingstone, 2005;pp. 133-4.
[30]Dissolution methods for drug products, US FDA.Available at: http://www.accessdata.fda.gov/scripts/cder/dissolution/dsp
[31]Ritger PL, Peppas NS. Asimple equation for description of solute release II. Fickian and anomalous release from swellable devices. J Control Release1987; 5: 37-42.
[32]Korsmeyer RW, Gurny R, Doelker E, Buri P,Peppas NA. Mechanisms of solute release from porous hydrophilic polymers. Internat J Pharm1983; 15: 25-35.
[33]Siepmann J, Peppas NA. Modeling of drug release from delivery systems based on hydroxypropyl methylcellulose (HPMC). Adv Drug Deliv Rev2001; 48: 139-57.
[34]Möckel J, Lippold BC. Zero-order drug release from hydrocolloid matrices. Pharm Research 1993; 10: 1066-70.
[35]Gao P, Nixon P, Skoug J. Diffusion in HPMC gels.II. Prediction of drug release rates from hydrophilic matrix extended-release dosage forms.Pharm Res1995; 12: 965-71.
[36]Katzhendler I, Hoffman A, Goldbergern A,Friedman M. Modeling of drug release from erodible tablets. J Pharm Sci 1997; 86: 110-5.
[37]Mitchell K, Ford JL, Armstrong DJ, Elliott PNC,Hogan JE, Rostron C. The influence of drugs on the properties of gels and swelling characteristics of matrices containing methylcellulose or hydrox-ypropylmethycellulose. Internat J Pharm1993;100: 165-73.
[38]Huang YB, Tsai YH, Yang WC, Chang JS, Wu PC. Optimization of sustained release propranolol dosage form using factorial design and response surface methodology. Biol Pharm Bull2004; 27:1626-9.
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