NOVEL PERORAL DOSAGE FORMS WITH PROTEASE INHIBITORY ACTIVITIES .1. DESIGN OF CAPSULES WITH FAST GEL-FORMING AND FAST DRUG-RELEASING PROPERTIES

Capsules, containing the poly(acrylic acid) derivative Carbopol(R) 934 P (C934P) with the aim of inhibiting intestinal proteolytic activities after swelling with water into a hydrated state, were designed. Eryth rosin was used as a hydrophillic model drug to characterize the releas e properties of the dosage forms, Capsule formulations which rapidly d isintegrated and released the drug quickly, were prepared because both rapid disintegration and rapid swelling of C934P and simultaneous dru g release are prerequisites for the enzyme inactivating properties of the system. The capsules containing freeze-dried, neutralized C934P (F NaC934P) disintegrated quicker than the capsules containing C934P. Cap sules which contained poly(glycerol ester of fatty acid) microparticle s with FNaC934P released erythrosin quicker than capsules containing m ixtures of FNaC934P, erythrosin and a disintegrant.