Abstract
A bilayer floating dosage unit is proposed to achieve local delivery of misoprostol, a prostaglandin E1 analogue, at the gastric mucosa level. The system is a capsule consisting of a floating layer maintaining the dosage unit buoyant upon the gastric content and a drug layer formulated to act as a sustained-delivery system. The differential design of the two layers allows the optimization of both floating capability and drug release profile. The layers are both composed of a hydrophilic matrix based upon hydroxypropylmethyl cellulose (HPMC). Parameters influencing the release profiles are described. The use of a large capsule increases the gastric residence time (GRT), as it impedes passage through the pylorus opening. γ-Scintigraphic studies were performed to visualize cohesion of the two layers in vivo and to determine GRT as a function of meal regimen. The average GRTs were 199 ± 69 min after a single meal (breakfast) and 618 ± 208 min after a succession of meals.
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Oth, M., Franz, M., Timmermans, J. et al. The Bilayer Floating Capsule: A Stomach-Directed Drug Delivery System for Misoprostol. Pharm Res 9, 298–302 (1992). https://doi.org/10.1023/A:1015870314340
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DOI: https://doi.org/10.1023/A:1015870314340