title: A novel solubility-modulated granules through porosity osmotic pump for controlled carvedilol delivery.
abstract: A method for the preparation of porosity osmotic pump granules was obtained by modulating carvedilol solubility with tartaric acid. Controlled porosity of the membrane was accomplished by the use of pore-forming agent in the coating. In this study, carvedilol was chosen as a model drug with an aim to develop a zero-order release system; tartaric acid was used as the solubility promoter; NaCl was used as the osmotic agent; cellulose acetate (CA) was used as the materials of semipermeable membrane; and PEG-400 was used as the pore-forming agent in the semipermeable membrane. The influence of different factors or levels on the in vitro release was studied. In order to simulate the gastrointestinal tract environments, two kinds of pH media (pH 1.5 and 6.8) on drug release were studied in this research, respectively. This porosity osmotic pump was optimized by single factor design experiments, and it was found to deliver carvedilol at a zero-order rate within 12 h and controlled release for 24 h. We drew a conclusion that the solubility-modulated porosity osmotic pump system is simple to prepare and might be used for the preparation of osmotic pump system of other poorly water-soluble drugs with alkaline or acid groups.
authors.affiliation: Lanzhou University Second Hospital, Lanzhou, P.R. China.
authors.forename: Qun-Li
authors.initials: QL
authors.lastname: Song
authors.forename: Ping
authors.initials: P
authors.lastname: Li
authors.forename: Yu-Min
authors.initials: YM
authors.lastname: Li
mesh_terms: D002227:Carbazoles / Q000737:chemistry*; D000077261:Carvedilol; D002482:Cellulose / Q000031:analogs & derivatives / Q000737:chemistry; D002626:Chemistry, Pharmaceutical / Q000379:methods; D003692:Delayed-Action Preparations / Q000737:chemistry*; D004337:Drug Carriers / Q000737:chemistry; D016503:Drug Delivery Systems / Q000379:methods; D005079:Excipients / Q000737:chemistry; D006863:Hydrogen-Ion Concentration; D015918:Infusion Pumps, Implantable; D009995:Osmosis; D004364:Pharmaceutical Preparations / Q000737:chemistry*; D011092:Polyethylene Glycols / Q000737:chemistry; D016062:Porosity; D011412:Propanolamines / Q000737:chemistry*; D012965:Sodium Chloride / Q000737:chemistry; D012995:Solubility; D013644:Tartrates / Q000737:chemistry; D014867:Water / Q000737:chemistry
chemical_list: D002227:Carbazoles; D003692:Delayed-Action Preparations; D004337:Drug Carriers; D005079:Excipients; D004364:Pharmaceutical Preparations; D011412:Propanolamines; D013644:Tartrates; D014867:Water; D000077261:Carvedilol; C005062:acetylcellulose; D011092:Polyethylene Glycols; D012965:Sodium Chloride; D002482:Cellulose; C029768:tartaric acid