Bragagni Marco, Bozdag Murat, Carta Fabrizio, Scozzafava Andrea, Lanzi Cecilia, Masini Emanuela, Mura Paola, Supuran Claudiu T
Università degli Studi di Firenze, Dipartimento di Chimica, Via Ugo Schiff 6, 50019 Sesto Fiorentino (Firenze), Italy.
Università degli Studi di Firenze, Dipartimento di Chimica, Laboratorio di Chimica Bioinorganica, Rm. 188, Via della Lastruccia 3, I-50019 Sesto Fiorentino (Firenze), Italy.
Bioorg Med Chem. 2015 Sep 15;23(18):6223-7. doi: 10.1016/j.bmc.2015.07.047. Epub 2015 Jul 29.
Two new sulfonamides incorporating arylsulfonylureido moieties were complexed with gamma cyclodextrin (γ-CD), hydroxypropyl-gamma cyclodextrin (HPγ-CD), hydroxypropyl-beta cyclodextrin (HPβ-CD) and hydroxyethyl-beta cyclodextrin (HEβ-CD) in order to obtain drug formulations with effective topical intraocular pressure (IOP) lowering effects, in an animal model of glaucoma. The HPγ-CD was the best solubilizing agent for the two sulfonamides and its complexes were characterized in detail and administered to rabbits with eye hypertension of 45-50 mmHg. The peak IOP lowering was observed after 1h post-administration and was of 36-37 mmHg. A low IOP pressure (of around-35 mmHg) was then maintained for the next 24h post-administration, which has not been observed before with any IOP lowering drug.
为了在青光眼动物模型中获得具有有效降低眼压（IOP）效果的药物制剂，将两种含有芳基磺酰脲基部分的新型磺胺与γ-环糊精（γ-CD）、羟丙基-γ-环糊精（HPγ-CD）、羟丙基-β-环糊精（HPβ-CD）和羟乙基-β-环糊精（HEβ-CD）进行络合。HPγ-CD是这两种磺胺的最佳增溶剂，对其络合物进行了详细表征，并给予眼压为45-50 mmHg的兔。给药后1小时观察到眼压降低峰值，为36-37 mmHg。给药后接下来的24小时内眼压维持在低水平（约-35 mmHg），这是以往任何降低眼压药物都未观察到的。
