申请人:MACROCHEM CORPORATION
公开号:EP0552879A1
公开(公告)日:1993-07-28
New and improved method for the transdermal administration of agents is provided utilizing iontophoresis in conjunction with a water-insoluble, stratum corneum-lipid modifier. The lipid modifier may be prior to iontophoresis or simultaneously therewith. The lipid modifier may be selected from a wide variety of moieties of the general formula R-X where R is a C₅ to C₂₈ alkyl or unsaturated alkyl and X is a member of the following: 1,3-dioxane; 1,3-dioxolane; lactam; morpholine; -COOH; -OH; -COOR'; -C-N(R')₂; cyclo ethylene and propylene carbonates; -CONH₂; -(CH₂-CH₂O)nH;
acetals, and hemiacetals; and wherein R' is lower alkyl (e.g., C₁ to C₃) and n is an integer of from 1 to 20. Optionally there may be present a polar, water-soluble chemical compound from the group of alcohols, glycols, lactams, dioxolanes, esters, ureas, morpholine and the like. Compositions and articles useful in the processes of the present invention are also provided.
本发明提供了一种新的、改进的透皮给药方法,利用离子透入法和一种不溶于水的角质层脂质改性剂。脂质修饰剂可以在离子透入之前使用,也可以与离子透入同时使用。脂质改性剂可选自多种通式 R-X 的分子,其中 R 为 C₅ 至 C₂₈ 烷基或不饱和烷基,X 为以下成员:1,3-二氧六环;1,3-二氧戊环;内酰胺;吗啉;-COOH;-OH;-COOR';-C-N(R')₂;环乙烯和环丙烯碳酸盐;-CONH₂;-(CH₂-CH₂O)nH;
其中 R'为低级烷基(如 C₁ 至 C₃),n 为 1 至 20 的整数。可选择加入醇、乙二醇、内酰胺、二氧戊环、酯、脲、吗啉等极性水溶性化合物。还提供了本发明工艺中有用的组合物和物品。