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聚氨酯作为睾酮经皮给药的自粘性基质。

Polyurethanes as self adhesive matrix for the transdermal drug delivery of testosterone.

机构信息

Otto Bock Kunststoff Holding GmbH, Duderstadt, Germany.

出版信息

Drug Dev Ind Pharm. 2012 May;38(5):597-602. doi: 10.3109/03639045.2011.620965. Epub 2011 Oct 19.

Abstract

The new technology to manufacture transdermal active patches without solvents or increased temperatures described here is based on polyol and isocyanate reacting to polyurethane (PU) in the presence of the drug. The technology was proven using testosterone (T) as the drug and N,N-Diethyl-m-toluamide (DEET) and Limonene (L) as enhancers for skin permeation. The experimental patches varied in drug content and enhancer concentration. The patches were evaluated regarding adhesion to stainless steel or leather, in vitro drug release and T permeation across human cadaver skin using Franz cell. Comparing the results with those of a parallel investigation of the commercial product, Testopatch(®), adhesion to leather and in vitro drug release of the experimental patches were found to be higher. The steady-state flux (J(SS)) of T from the experimental patches was found lower than Testopatch(®). The flux of the experimental patch P3, which had the highest concentration of DEET and a low concentration of L was comparable to J(SS) of the commercial product, Testopatch(®).

摘要

此处描述的无溶剂和升温制造透皮活性贴片的新技术基于多元醇和异氰酸酯在药物存在的情况下反应生成聚氨酯(PU)。该技术已使用睾酮(T)作为药物,使用 N,N-二乙基间甲苯酰胺(DEET)和柠檬烯(L)作为皮肤渗透增强剂进行了验证。实验贴片的药物含量和增强剂浓度各不相同。使用 Franz 细胞评估了贴片对不锈钢或皮革的粘附性、体外药物释放以及 T 经人体尸体皮肤渗透的情况。将结果与商业产品 Testopatch(®)的平行研究进行比较,发现实验贴片对皮革的粘附性和体外药物释放均高于 Testopatch(®)。实验贴片 P3 的稳态通量(J(SS))低于 Testopatch(®)。具有最高 DEET 浓度和低 L 浓度的实验贴片 P3 的通量与商业产品 Testopatch(®)的 J(SS)相当。

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