申请人:Sucampo AG
公开号:US11534404B2
公开(公告)日:2022-12-27
Multilayer beads for pharmaceutical use having a drug-in-polymer layer are disclosed. The disclosed multilayer beads for pharmaceutical use have (a) a core particle; (b) an optional barrier layer coated on the surface of the core particle; (c) a drug-in-polymer layer coated on the surface of the core or the barrier layer, (d) an optional sealant layer coated on the surface of the drug-in-polymer layer; and (e) optionally one or more outer layers external to the drug-in-polymer layer or the sealant layer. The drug-in-polymer layer consists essentially of (i) a drug selected from the group consisting of a 15-keto prostaglandin drug, a 13,14-dihydro prostaglandin drug, and a 13,14-dihydro-15-keto prostaglandin drug; and (ii) a polymer selected from the group consisting of polyvinylpyrrolidone, vinylpyrrolidone-vinylacetate copolymer or a mixture thereof. The drug-in-polymer layer may be solid dispersion of the drug in the polymer. Pharmaceutical compositions comprising a plurality of multilayer beads and a pharmaceutically acceptable excipient and methods of treating a gastrointestinal disorder are also disclosed.
本发明公开了具有聚合体药物层的药用多层微珠。所公开的药用多层微珠具有:(a) 核心颗粒;(b) 涂在核心颗粒表面的任选阻隔层;(c) 涂在核心或阻隔层表面的聚合体药物层;(d) 涂在聚合体药物层表面的任选密封剂层;(e) 聚合体药物层或密封剂层外部的一个或多个外层。药包聚合物层主要包括:(i) 选自 15-酮前列腺素药物、13,14-二氢前列腺素药物和 13,14-二氢-15-酮前列腺素药物组的药物;(ii) 选自聚乙烯基吡咯烷酮、乙烯基吡咯烷酮-乙酸乙烯酯共聚物或其混合物组的聚合物。药物聚合物层可以是药物在聚合物中的固体分散体。还公开了包含多个多层微珠和药学上可接受的赋形剂的药物组合物以及治疗胃肠道疾病的方法。