公开(公告)号：US5962012A

公开(公告)日：1999-10-05

申请号：US22308

申请日：1998-02-11

Applicant: Wan-Yan Lin ,  Shu-Juan Chen ,  Chao-Wei Liao ,  Chien-Hsin D. Cheng

Inventor： Wan-Yan Lin ,  Shu-Juan Chen ,  Chao-Wei Liao ,  Chien-Hsin D. Cheng

IPC: A61K9/70 ,  A61K31/439 ,  A61K31/46 ,  A61K47/14 ,  A61K47/18 ,  A61F13/02

CPC classification number: A61K9/7061 ,  A61K31/439 ,  A61K31/46 ,  A61K47/18 ,  A61K9/0014 ,  Y10S514/946 ,  Y10S514/947

Abstract: Scopolamine is a folksy cholinergic antagonist, and is used by parasympathetic nerves in autonomic nervous neurons as an anti-motion sickness drug or an anti-emesis drug. Since the human body most effectively absorbs this drug through the postauricular skin, the drug is administered by postauricular transdermal resorption patch. The penetrability of drug is increase by adding a dermal penetrative enhancer, because the penetration ability of patch-administered drugs is usually decreased by the penetrative blockade at dermal horny layers. The present invention discloses a penetration enhancer to increase dermal absorption and penetration of the cholinergic antagonist. The present invention finds that polyethylene and amide enhance penetration, about 2.2-2.8 fold. In accordance with the present invention, a penetration enhancer is added to the formulations of transdermal patch to increase the human body's absorption of scopolamine.

Abstract translation: 东莨菪碱是一种民族胆碱能拮抗剂，由自主神经神经元中的副交感神经用作抗运动疾病药物或抗呕吐药物。 由于人体最有效地通过耳后皮肤吸收该药物，所以该药物通过耳后皮肤吸收贴片施用。 通过添加皮肤渗透性增强剂，药物的渗透性增加，因为补片施用药物的穿透能力通常通过在真皮角质层上的穿透性阻断而降低。 本发明公开了一种增加胆碱能拮抗剂的皮肤吸收和渗透的渗透促进剂。 本发明发现聚乙烯和酰胺增强渗透性，约2.2-2.8倍。 根据本发明，将渗透增强剂加入透皮贴剂的制剂中以增加人体对东莨菪碱的吸收。