Influence of Carbopol 71G-NF on the release of dextromethorphan hydrobromide from extended-release matrix tablets

The objective of this study was to evaluate the potential of Carbopol® 71G-NF on the release of dextromethorphan hydrobromide (DM) from matrix tablets in comparison with hydroxypropyl methylcellulose (HPMC® K15M) and Eudragit® L100-55 polymers. Controlled release DM matrix tablets were prepared using Carbopol 71G-NF, HPMC K15M, and Eudragit L100-55 at different drug to polymer ratios by direct compression technique. The mechanical properties of the tablets as tested by crushing strength and friability tests were improved as the concentration of Carbopol, HPMC, and Eudragit increased. However, Carbopol-based tablets showed a significantly (P < 0.05) higher crushing strength and a lower friability than HPMC and Eudragit tablets. No significant differences in weight uniformity and thickness values were observed between the different formulations. It was also found that Carbopol significantly (P < 0.05) delayed the release of DM in comparison with HPMC K15M and Eudragit L100-55. A combination of HPMC K15M and Eudragit L100-55 in a 1:1 ratio at 20 and 30% significantly (P < 0.05) delayed the release of DM than Eudragit L100-55 alone. Moreover, blends of Carbopol and HPMC at a 1:1 ratio at the 10, 20, and 30% total polymer concentration were investigated. The blend of Carbopol and HPMC at 10% level significantly (P < 0.05) slowed the release of DM than Carbopol or HPMC alone, whereas blends at 20 and 30% level significantly (P < 0.05) delayed the release of DM compared with HPMC or Carbopol alone. The results with these polymer blends showed that it was possible to reduce the total amount of polymers when used as a combination in formulation.

[1]  G. Khan,et al.  Studies on drug release kinetics from ibuprofen-carbomer hydrophilic matrix tablets: influence of co-excipients on release rate of the drug. , 1999, Journal of controlled release : official journal of the Controlled Release Society.

[2]  K. Rao,et al.  Swelling controlled-release systems: recent developments and applications , 1988 .

[3]  E. Touitou,et al.  Influence of additives on (hydroxyethyl) methylcellulose properties: relation between gelation temperature change, compressed matrix integrity and drug release profile , 1982 .

[4]  Donald L. Wise,et al.  Handbook of Pharmaceutical Controlled Release Technology , 2000 .

[5]  Ho-Wah Hui,et al.  Design and Fabrication of Oral Controlled Release Drug Delivery Systems , 1987 .

[6]  O. Güven,et al.  Formulation and in Vitro–in Vivo Evaluation of Buccoadhesive Morphine Sulfate Tablets , 1994, Pharmaceutical Research.

[7]  N A Peppas,et al.  Modeling of drug release from delivery systems based on hydroxypropyl methylcellulose (HPMC). , 2001, Advanced drug delivery reviews.

[8]  S. Samani,et al.  The effect of polymer blends on release profiles of diclofenac sodium from matrices. , 2003, European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V.

[9]  Sanjay Garg,et al.  Factors affecting mechanism and kinetics of drug release from matrix-based oral controlled drug delivery systems , 2004 .

[10]  G. Jayasagar,,et al.  Formulation and Evaluation of Diclofenac Sodium Using Hydrophilic Matrices , 2001, Drug development and industrial pharmacy.

[11]  S. Neau,et al.  Fabrication and characterization of extruded and spheronized beads containing carbopol® 974P, NF resin , 1996 .

[12]  U. Rungsardthong,et al.  Characteristics and in vitro release of dextromethorphan resinates , 2005 .

[13]  J. Robinson,et al.  Bioadhesive polymers as platforms for oral controlled drug delivery II: synthesis and evaluation of some swelling, water-insoluble bioadhesive polymers. , 1985, Journal of pharmaceutical sciences.

[14]  Koichiro Tahara,et al.  Overall mechanism behind matrix sustained release (SR) tablets prepared with hydroxypropyl methylcellulose 2910 , 1995 .

[15]  N. Peppas,et al.  Mechanisms of solute release from porous hydrophilic polymers , 1983 .

[16]  G. Khan,et al.  Formulation and in vitro evaluation of ibuprofen-Carbopol 974P-NF controlled release matrix tablets. III: Influence of co-excipients on release rate of the drug. , 1998, Journal of controlled release : official journal of the Controlled Release Society.

[17]  A. Sakr,et al.  Influence of methacrylic acid and hydroxypropylmethyl cellulose on the tablet properties and in vitro release of dextromethorphan hydrobromide. , 2003, Die Pharmazie.

[18]  A. Moes [Research and development of oral controlled-release dosage forms]. , 1989 .