Oth M, Franz M, Timmermans J, Möes A
Searle European Development Centre, Mont-Saint-Guibert, Belgium.
Pharm Res. 1992 Mar;9(3):298-302. doi: 10.1023/a:1015870314340.
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. gamma-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.
提出了一种双层漂浮剂型单位，以实现在胃黏膜水平局部递送米索前列醇（一种前列腺素E1类似物）。该系统是一种胶囊，由使剂型单位在胃内容物上保持漂浮的漂浮层和配制为持续释放系统的药物层组成。两层的差异设计允许优化漂浮能力和药物释放曲线。两层均由基于羟丙基甲基纤维素（HPMC）的亲水性基质组成。描述了影响释放曲线的参数。使用大胶囊会增加胃滞留时间（GRT），因为它会阻碍通过幽门开口。进行了γ闪烁扫描研究，以在体内观察两层的黏附情况，并确定GRT作为进餐方案的函数。单次进餐（早餐）后的平均GRT为199±69分钟，连续进餐之后为618±208分钟。
