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1. 发明授权

US06444234B1 Compositions for rapid and non-irritating transdermal delivery of pharmaceutically active agents and methods for formulating such compositions and delivery thereof 有权
标题翻译：用于药物活性剂的快速和无刺激性透皮递送的组合物和用于配制这种组合物的方法和其递送
公开(公告)号：US06444234B1
公开(公告)日：2002-09-03
申请号：US09381095
申请日：2000-05-11
申请人： Kenneth B Kirby , Berno I. R. Pettersson, Jr.
发明人： Kenneth B Kirby , Berno I. R. Pettersson, Jr.
IPC分类号： A01N3578
CPC分类号： A61K9/0014 , A61K36/232 , A61K36/324 , A61K36/53 , A61K36/74 , A61K36/752 , A61K47/10 , A61K47/12 , Y10S514/946 , Y10S514/947 , A61K2300/00
摘要： Pharmaceutical compositions for the transdermal administration of a medicament or other active agent by topical application of the composition to the skin of humans or other animals are described. Methodology for formulating such compositions which provide for very rapid uptake of the medicament and transmigration into and through the skin to either fatty tissues or the vascular system, while minimizing irritation to the skin and/or immunological response, is based on a transdermal delivery system (TDS) wherein the medicament is modified to form a true solution in a complex formed from particular solvents and solvent and solute modifiers in combination with skin stabilizers. Uptake of the medicament is further facilitated and made more rapid by including Forskolin or other source of cellular energy, namely induction of cAMP or cGMP. Selection of specific solvents and solvent and solute modifiers and other functional ingredients and the amounts thereof are chosen such that there is a balance between the sum of the mole-moments [(molar amount of each individual ingredient)×(dipole moment of that ingredient)] of the delivery system and the sum of the moler moments of the composition in which the medicament is dissolved. Preferably, the van der Waals forces of the delivery system is also similarly matched to the van der Waals forces of the total composition, namely, delivery system plus active agent.
摘要翻译：描述了通过将组合物局部施用于人或其他动物的皮肤来透皮施用药物或其它活性剂的药物组合物。用于配制这样的组合物的方法，其基于透皮递送系统（其对皮肤和/或免疫应答的最小化）最小化地吸收药物并向皮肤递送进入脂肪组织或血管系统， TDS），其中药物被修饰以在由特定溶剂和溶剂和溶质改性剂与皮肤稳定剂组合形成的络合物中形成真正的溶液。通过包括福斯科林或其他细胞能源，即诱导cAMP或cGMP，进一步促进和促进药物的摄取。选择特定溶剂和溶剂以及溶质改性剂和其它功能成分及其用量选择为使得摩尔矩[（各个成分的摩尔量）×（该成分的偶极矩）之和之和之间存在平衡， ]和药物溶解的组合物的分散器力矩的总和。优选地，输送系统的范德华力也类似地与总组合物的范德华力，即递送系统加活性剂匹配。

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