Enteric controlled-release pantoprazole-loaded microparticles prepared by using Eudragit S100 and poly(epsilon-caprolactone) blend.
Microparticles of poly(epsilon-caprolactone) and of its blend with Eudragit S100 were prepared by emulsion/solvent evaporation technique to provide controlled release and gastro-resistance for an acid labile drug. This drug was sodium pantoprazole, a proton pump inhibitor. Both formulations were successfully prepared, but only the microparticles prepared with the blend were capable of stabilizing the drug in the acid medium. Furthermore, this formulation showed in vivo protection of stomachs against ulceration caused by ethanol in rats. These microparticles were tabletted, and the tablets demonstrated slower drug release and higher acid protection than the microparticles before tabletting.
Raffin
Renata Platcheck
RP
Faculdade de Farmácia - Universidade Federal do Rio Grande do Sul, Brazil.
Colomé
Leticia Marques
LM
Guterres
Silvia Stanisçuaski
SS
Pohlmann
Adriana Raffin
AR
D053799:2-Pyridinylmethylsulfinylbenzimidazoles / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics*; D000096:Acetone / Q000737:chemistry; D000284:Administration, Oral; D000818:Animals; D000897:Anti-Ulcer Agents / Q000008:administration & dosage / Q000737:chemistry / Q000493:pharmacokinetics; D001682:Biological Availability; D002152:Calorimetry, Differential Scanning; D006863:Hydrogen-Ion Concentration; D008297:Male; D008855:Microscopy, Electron, Scanning; D008899:Mineral Oil / Q000737:chemistry; D000077402:Pantoprazole; D010316:Particle Size; D011091:Polyesters / Q000737:chemistry*; D011109:Polymethacrylic Acids / Q000737:chemistry*; D051381:Rats; D017208:Rats, Wistar; D013276:Stomach Ulcer / Q000517:prevention & control; D013499:Surface Properties; D013608:Tablets, Enteric-Coated
D053799:2-Pyridinylmethylsulfinylbenzimidazoles; D000897:Anti-Ulcer Agents; D011091:Polyesters; D011109:Polymethacrylic Acids; D013608:Tablets, Enteric-Coated; D000096:Acetone; C016240:polycaprolactone; C038300:methylmethacrylate-methacrylic acid copolymer; D008899:Mineral Oil; D000077402:Pantoprazole