The influence of excipients on drug release from hydroxypropyl methylcellulose matrices.
The influence of commonly used excipients, spray-dried lactose (SDL), microcrystalline cellulose (MCC), and partially pregelatinized maize starch (Starch 1500) on drug release from hydroxypropyl methylcellulose (HPMC, hypromellose) matrix system has been investigated. A model formulation contained 30%w/w drug, 20%w/w HPMC, 0.5%w/w fumed silica, 0.25%w/w magnesium stearate, and 49.25%w/w filler. Chlorpheniramine maleate and theophylline were used as freely (1 in 4) and slightly (1 in 120) water-soluble drugs, respectively. It was found that for both drugs, addition of 20 to 49.25%w/w Starch 1500 resulted in a significant reduction in drug release rates compared to when MCC or SDL was used. The study showed that using lactose or microcrystalline cellulose in the formulations resulted in faster drug release profiles. Partially pregelatinized maize starch contributed to retardation of both soluble and slightly soluble drugs. This effect may be imparted through synergistic interactions between Starch 1500 and HPMC and the filler actively forming an integral part within the HPMC gel structure.
Levina
Marina
M
Colorcon Limited, Flagship House, Victory Way, Crossways, Dartford, Kent DA2 6QD, UK. mlevina@colorcon.co.uk
Rajabi-Siahboomi
Ali R
AR
D002626:Chemistry, Pharmaceutical; D019245:Compressive Strength; D005079:Excipients / Q000737:chemistry / Q000493:pharmacokinetics*; D065347:Hypromellose Derivatives; D008747:Methylcellulose / Q000031:analogs & derivatives* / Q000737:chemistry / Q000493:pharmacokinetics*; D004364:Pharmaceutical Preparations / Q000737:chemistry / Q000378:metabolism*
D005079:Excipients; D004364:Pharmaceutical Preparations; D065347:Hypromellose Derivatives; D008747:Methylcellulose