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1-Substd. azacycloalkan-2-one penetrants for topical compsns. - esp. for application of antibacterials, antifungals steroids, iododeoxyuridine and 5-fluorouracil
1-Substd. azacycloalkan-2-one penetrants for topical compsns. - esp. for application of antibacterials, antifungals steroids, iododeoxyuridine and 5-fluorouracil
Compsns. contain a physiologically-active agent and a sufficient but non-toxic amt. of a cpd. of formula (I) to provide effective penetration; (where R'=H or 1-4C alkyl; m=3-7; n=0-17; R=CH3; phenyl, opt. substd. byhalo; or the gp. provided that when m = 3 and R is CH3, then n is not = 0-4). (I) is esp. used for topical application to humans or animals of antibacterials (esp. lincomycin, clindamycin, erythromycin or their salts); steroids, antifungals (esp. griseofulvin); iododeoxyuridine (for treating herpes simplex) and 5-fluorouracil, but also in skin-protecting compsns. (e.g. sun-screens), and cosmetics. The active cpds. are carried across body membranes by (I) and retained in the tissues, and (partic. in the case of griseofulvin) can be given without the side-effects apparent on oral administration.
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机译:Compsns。包含生理活性剂和足够但无毒的amt。 cpd。式(I)的化合物以提供有效的渗透; (其中R'= H或1-4C烷基; m = 3-7; n = 0-17; R = CH3;苯基,优选取代为卤代;或gp。条件是当m = 3且R为CH3 ,则n不等于0-4)。 (I)是。用于对人或动物局部使用抗菌剂(尤其是林可霉素,克林霉素,红霉素或其盐);类固醇,抗真菌药(尤其是灰黄霉素);碘脱氧尿苷(用于治疗单纯性疱疹)和5-氟尿嘧啶,也可用于皮肤保护药。 (例如防晒霜)和化妆品。活动的cpds。通过(I)将它们通过体膜携带并保留在组织中,并且(特别是灰黄霉素)可以给予而口服给药没有明显的副作用。
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