ISSN:
1365-2036
Quelle:
Blackwell Publishing Journal Backfiles 1879-2005
Thema:
Medizin
Notizen:
Background : Targeted drug delivery to the colon is important for topical treatment of inflammatory bowel diseases. Established targeting systems predominantly focus on either pH- or time-dependent release, or bacterial degradation.Aim : To perform a three-phase, crossover design trial evaluating a novel combined pH- and time-based multiunit delivery system.Methods : Twelve healthy male volunteers each received 200 mg of caffeine as either uncoated immediate release tablets, coated pellets with pH-dependent rapid release (EUDRAGIT FS 30D), and pellets with pH- and time-based release (inner layer EUDRAGIT RL/RS 30D; outer layer EUDRAGIT FS 30D). Orocecal transit time was measured using lactose-[13C]ureide. Serum concentrations of caffeine were measured by high-performance liquid chromatography.Results : In contrast to the uncoated tablet, both coated systems reached the ileocecal region almost at the same time (3.19 ± 0.71 and 3.33 ± 0.81 h). Serum caffeine profiles were significantly prolonged for the pH and time delivery system compared with the pH-only based system (median tmax 12.0 vs. 5.5 h; P 〈 0.001). This was further reflected by a lower Cmax value and a lower area under the curve within 24 h after application.Conclusion : Compared with the conventional delivery systems, drug release from the new dosage form may offer a new dimension for the oral treatment of mid to distal ulcerative colitis.
Materialart:
Digitale Medien
URL:
http://dx.doi.org/10.1111/j.1365-2036.2004.02033.x
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