Investigation of the effect of tablet surface area/volume on drug release from hydroxypropylmethylcellulose controlled-release matrix tablets.
The purpose of this study was to investigate the influence of tablet surface area/volume (SA/Vol) on drug release from controlled-release matrix tablets containing hydroxypropylmethylcellulose (HPMC). Soluble drugs (promethazine HCl, diphenhydramine HCl, and propranolol HCl) were utilized in this study to give predominantly diffusion-controlled release. Drug release from HPMC matrix tablets with similar values of SA/Vol was comparable within the same tablet shape (i.e., flat-faced round tablets) and among different shapes (i.e., oval, round concave, flat-faced beveled-edge, and flat-faced round tablets). Tablets having the same surface area but different SA/Vol values did not result in similar drug release; tablets with larger SA/Vol values hadfaster release profiles. Utility of SA/Vol to affect drug release was demonstrated by changing drug doses, and altering tablet shape to adjust SA/Vol. When SA/Vol was held constant, similar release profiles were obtained with f2 metric values greater than 70. Thus, surface area/volume is one of the key variables in controlling drug release from HPMC matrix tablets. Proper use of this variable has practical application by formulators who may need to duplicate drug release profiles from tablets of different sizes and different shapes.
Reynolds
Thomas D
TD
The Dow Chemical Company, Midland, Michigan 48674, USA. tdreynolds@dow.com
Mitchell
Shawn A
SA
Balwinski
Karen M
KM
D003692:Delayed-Action Preparations / Q000737:chemistry*; D004058:Diffusion; D004155:Diphenhydramine / Q000737:chemistry; D004337:Drug Carriers / Q000737:chemistry; D065347:Hypromellose Derivatives; D008747:Methylcellulose / Q000031:analogs & derivatives* / Q000737:chemistry*; D011398:Promethazine / Q000737:chemistry; D011433:Propranolol / Q000737:chemistry; D013499:Surface Properties / Q000187:drug effects; D013607:Tablets
D003692:Delayed-Action Preparations; D004337:Drug Carriers; D013607:Tablets; D065347:Hypromellose Derivatives; D004155:Diphenhydramine; D008747:Methylcellulose; D011433:Propranolol; D011398:Promethazine