Gastrointestinal mucoadhesive patch system (GI-MAPS) for oral administration of G-CSF, a model protein.

摘要: A new gastrointestinal mucoadhesive patch system (GI-MAPS) has been designed for the oral delivery of protein drugs. The consists four layered films, 3.0 x mm2, contained in an enteric capsule. 40 microm backing layer is made a water-insoluble polymer, ethyl cellulose (EC). surface pH-sensitive polymer such as hydroxypropylmethylcellulose phthalate (HP-55), Eudragit L100 or S100 and was coated with adhesive layer. middle layer, drug-containing membrane attached to EC by heating press method. Both drug pharmaceutical additives including organic acid, citric non-ionic surfactant, polyoxyethylated castor oil derivative (HCO-60), were formulated carboxyvinyl (Hiviswako 103). Fluorescein (FL), 30mg, first used model administration GI-MAPS having different layers beagle dogs. plasma FL concentration vs. time profiles demonstrated that targeting systems obtained, because Tmax, when concentrations reaches its maximum lelev, 2.33+/-0.82 h HP-55 system, 3.33+/-0.41 5.00+/-0.00 system. same three kinds GI-MAPSs containing 125 microg recombinant human granulocyte colony-stimulating factor (G-CSF) prepared orally administered dogs increase total white blood cell (WBC) counts measured pharmacological index G-CSF. Comparison WBCs after iv injection amount G-CSF (125 microg) indicated availabilities (PA) 23%, 5.5% 6.0% L100, systems. By decreasing HCO-60 PA decreased. These results suggest usefulness proteins.