申请人:Merck & Co., Inc.
公开号:EP0314206A1
公开(公告)日:1989-05-03
The instant invention is directed to a drug-delivery device for the controlled release of a therapeutically active ingredient into an environment of use which comprises:
(A) a core composition comprising
(a) a solubility modulating agent which is either (i) surrounded by a water insoluble coat containing at least one pore forming additive dispersed throughout said coat, or (ii) dispersed in a matrix substrate, and
(b) a diffusible water soluble therapeutically active ingredient;
and
(B) a water insoluble wall surrounding said core composition and prepared from
(i) a polymer material that is permeable to water but substantially impermeable to solute and
(ii) 0.1 to 75% by weight, based on the total weight of (i) and (ii), of at least one water leachable pore forming additive dispersed throughout said wall; or
(C) a substantially imperforate water insoluble wall surrounding said core composition and prepared from a semipermeable material substantially impermeable to core composition and permeable to the passage of an external fluid in the environment of use, with said wall having a means for release of the therapeutic agent through the water insoluble wall.
本发明涉及一种将治疗活性成分控制释放到使用环境中的给药装置,该装置包括
(A) 核心成分,包括
(a) 溶解度调节剂,其(i)被不溶于水的外衣包围,该外衣至少含有一种分散在所述外衣中的孔形成添加剂,或(ii)分散在基质基材中,以及
(b) 可扩散的水溶性治疗活性成分;
和
(B) 围绕所述核心成分的水不溶壁,由以下材料制备而成
(i) 可渗透水但基本上不渗透溶质的聚合物材料,以及
(ii) 分散在整个所述壁中的至少一种可渗透水的孔隙形成添加剂,按重量计,占(i)和(ii)总重量的 0.1%至 75%;或
(C) 围绕所述核心成分的基本上不穿孔的不溶于水的壁,由基本上不渗透核心成分并可渗透使用环境中的外部流体的半渗透材料制备而成,所述壁具有通过不溶于水的壁释放治疗剂的装置。