Abstract
Purpose. This study was performed to examine the use of guar gum to sustain the release of diltiazem under in vitro and in vivo conditions.
Methods. Guar gum tablet formulations were prepared and evaluated under a variety of in vitro dissolution conditions. The formulations, along with Dilacor XR®, were administered to a group of eight fasted, healthy volunteers in a four period crossover study.
Results. Varying the lot of guar gum as well as using guar from different suppliers had little effect on diltiazem dissolution. Also, dissolution of diltiazem from guar gum tablets was essentially independent of stir speed under normal conditions (USP Apparatus II). The stability of guar-based formulations under stressed conditions (40°C/75% relative humidity for 3 months) was also established. All four formulations gave similar plasma concentrations over time in the healthy volunteers pharmacokinetic study.
Conclusions. Guar gum-based matrix tablets represent a simple and economical alternative to existing diltiazem sustained release dosage forms.
Similar content being viewed by others
REFERENCES
A. M. Sakr and H. M. Elsabbagh. Correlation of water absorption with the disintegration effectiveness of guar gum. Pharm. Ind. 37:457-459 (1975).
E. M. Rudnic, C. T. Rhodes, J. F. Bavitz, and J. B. Schwartz. Some effects of relatively low levels of eight tablet disintegrants on a direct compression system. Drug Dev. Ind. Pharm. 7:347-358 (1981).
M. Z. Iqbal, M. Amin, and N. A. Muzaffar. Comparative evaluation of guar gum as disintegrating agent. J. Pharmacy 1:17-34 (1979).
L. E. Eatherton, P. E. Platz, and F. P. Cosgrove. Drug Standards 23:42-47 (1955).
W. Feinstein and A. J. Bartilucci. Comparative study of selected disintegrating agents. J. Pharm. Sci. 55:332-334 (1966).
H. M. Elsabbagh, A. M. Sakr, and S. E. Abd-Elhadi. Effect of guar gum on the dissolution rate of ephedrine hydrochloride and sulphadimidine tablets. Pharmazie 33:730-731 (1978).
P. J. Waaler, M. Anderson, C. Graffner, and B. W. Muller. Optimization of a matrix tablet formulation using a mixture design. Acta Pharm. Nord. 4:167-170 (1992).
H. E. Huber and G. L. Christenson. Utilization of hydrophilic gums for the control of drug substance release from tablet formulations II. Influence of tablet hardness and density on dissolution behavior. J. Pharm. Sci. 57:164-166 (1968).
H. L. Bhalla and Y. D. Sanzgiri. An improved controlled release tablet of salbutamol sulphate. Indian J. Pharm. Sci. 49:22-25 (1987).
S. K. Baveja, K. V. Ranga Rao, and J. Arora. Chemical investigations of some galactomannan gums as matrix tablets for sustained drug delivery. Ind. J. Pharm. Sci. 30B:133-137 (1991).
H. L. Bhalla and S. O. Gulati. Sustained release theophylline tablets. Indian Drugs 24:338-342 (1987).
P. J. Waaler, C. Graffner, and B. W. Muller. Optimization of a matrix tablet formulation using a mixture design. Acta Pharm. Nord. 4:9-16 (1992).
P.J. Waaler, K. Arnesen, C. Graffner, and B. W. Muller. Optimization of the amount of xanthan gum and guar gum in a matrix tablet formulation using a central composite design. Acta Pharm. Nord. 4:291-296 (1992).
P. J. Waaler, C. Graffner, and B. W. Muller. Biopharmaceutical studies of naftidrofuryl in hydrocolloid matrix tablets. Int. J. Pharm. 87:229-237 (1992).
K. Yu, D. Wong, J. Parasrampuria, and D. R. Friend. Guar Gum. In: Analytical Profiles of Drug Substances and Excipients, Vol. 24, H. G. Brittain, Ed., Academic Press, Orlando, Florida, pp. 397-442 (1996).
A. M. Goldstein, E. Alter, and J. K. Seamam. Guar gum In: Industrial gums, polysaccharides and their derivatives, 2nd ed. New York, NY: Academic Press.: pp. 303-321, (1973).
D. R. Friend, S. A. Altaf, K. L. Yu, and M. S. Gebert. Development of a zero-order nifedipine dosage form using COSRx technology. Proc. Int. Sym. Control. Rel. Bioact. Mat. 24:311-312 (1997).
M. S. Gebert and D. R. Friend. Purified guar galactomannan as an improved pharmaceutical excipient. Pharm. Develop. Tech.(1998) in press.
M. S. Gebert, J. Parasrampuria, and D. R. Friend. Purified galactomannan as an improved pharmaceutical excipient. Pharm. Res. 13:S180 (1996).
F. Langenbucher. Parametric representation of dissolution-rate curves by the RRBSW distribution. Pharm. Ind. 38:472-477 (1976).
S. Bolton. Statistical Inference: Estimation and Hypothesis Testing, Pharmaceutical Biostatistics, Marcel Dekker, USA, pp. 105-161 (1984).
R. Bodmeier, X. Guo, R. E. Sarabia, and P. F. Skultety. The Influence of Buffer Species and Strength on Diltiazem HCl Release from Beads Coated with the Aqueous Cationic Polymer Dispersions, Eudragit RS. RL 30D. Pharm. Res. 13:52-56 (1996).
G. A. McClelland, S. Sutton, K. Engle, and G. M. Zentner. The solubility-modulated osmotic pump: in vitro/in vivo release. Pharm. Res. 8:88-92 (1991).
Author information
Authors and Affiliations
Rights and permissions
About this article
Cite this article
Altaf, S.A., Yu, K., Parasrampuria, J. et al. Guar Gum-Based Sustained Release Diltiazem. Pharm Res 15, 1196–1201 (1998). https://doi.org/10.1023/A:1011931622536
Issue Date:
DOI: https://doi.org/10.1023/A:1011931622536