Pectin/anhydrous dibasic calcium phosphate matrix tablets for in vitro controlled release of water-soluble drug.
Different pectin/anhydrous dibasic calcium phosphate (ADCP) matrix tablets have been developed in order to obtain controlled release of a water-soluble drug (theophylline). Swelling, buoyancy and dissolution studies have been carried out in different aqueous media (demineralized water, progressive pH medium, simulated gastric fluid, simulated intestinal fluid and simulated colonic fluid), to characterize the matrix tablets. When the pectin/ADCP ratio was ≥0.26 (P1, P2, P3 and P4 tablets) a continuous swelling and low theophylline dissolution rate from the matrices were observed. So, pectin gel forming feature predominated over the ADCP properties, yielding pH-independent drug release behavior from these matrices. On the contrary, pectin/ADCP ratios ≤0.11 (P5 and P6 tablets) allowed to achieve drug dissolution pH dependent. Consequently, the suitable selection of the pectin/ADCP ratio will allow to tailor matrix tablets for controlled release of water-soluble drugs in a specific manner in the gastrointestinal tract.
Departamento de Farmacia y Tecnología Farmacéutica, Facultad de Farmacia, Universidad Complutense de Madrid, Plaza Ramón y Cajal s/n, 28040 Madrid, Spain. Electronic address: nicte_1906@yahoo.es.
Pseidy Luz
PL
Mamani
Departamento de Farmacia y Tecnología Farmacéutica, Facultad de Farmacia, Universidad Complutense de Madrid, Plaza Ramón y Cajal s/n, 28040 Madrid, Spain; Biotransformations Group, Departamento de Farmacia y Tecnología Farmacéutica, Facultad de Farmacia, Universidad Complutense de Madrid, Plaza Ramón y Cajal s/n, 28040 Madrid, Spain. Electronic address: rruizcar@ucm.es.
Roberto
R
Ruiz-Caro
Departamento de Farmacia y Tecnología Farmacéutica, Facultad de Farmacia, Universidad Complutense de Madrid, Plaza Ramón y Cajal s/n, 28040 Madrid, Spain; Biotransformations Group, Departamento de Farmacia y Tecnología Farmacéutica, Facultad de Farmacia, Universidad Complutense de Madrid, Plaza Ramón y Cajal s/n, 28040 Madrid, Spain. Electronic address: mdveiga@ucm.es.
María Dolores
MD
Veiga
D001826:Body Fluids / Q000737:chemistry; D002130:Calcium Phosphates / Q000737:chemistry*; D002626:Chemistry, Pharmaceutical / Q000379:methods*; D003692:Delayed-Action Preparations / Q000737:chemistry*; D065546:Drug Liberation; D006863:Hydrogen-Ion Concentration; D010368:Pectins / Q000737:chemistry*; D012995:Solubility; D013607:Tablets / Q000737:chemistry*; D013806:Theophylline / Q000737:chemistry
D002130:Calcium Phosphates; D003692:Delayed-Action Preparations; D013607:Tablets; D010368:Pectins; D013806:Theophylline; C485829:calcium phosphate, dibasic, anhydrous
Biodegradable polymers; Colonic drug delivery; Controlled release; Mathematical models; Polymeric drug delivery systems; Tableting; Water sorption