Gwak Hye Sun, Oh Ik Sang, Chun In Koo
College of Pharmacy, Dongduk Women's University, Seoul 136-714, Korea.
Arch Pharm Res. 2003 Aug;26(8):644-8. doi: 10.1007/BF02976714.
To investigate the feasibility of developing a new ondansetron transdermal system, the effects of vehicles and penetration enhancers on the in vitro permeation of ondansetron hydrochloride (OS) from a pressure-sensitive adhesive (PSA) matrices across dorsal hairless mouse skin were studied. Vehicles employed in this study consisted of various ratios of propylene glycol monocaprylate (PGMC)-diethylene glycol monoethyl ether (DGME) co-solvents and PGMC-propylene glycol (PG) co-solvents with 3% oleic acid. Duro-Tak 87-2100 and Duro-Tak 87-2196 were used as PSAs. The concentration of DGME in PGMC-DGME co-solvent system affected the release rate; as the concentration of DGME increased, the release rate decreased. The cumulative release amount of OS increased as the ratio of PSA to drug solution decreased. The permeation flux was also primarily affected by the amount of PSAs; as the amount decreased, the permeation flux increased. The overall fluxes from matrix formulations were significantly lower when compared to those obtained from solution formulations. The ratio of PG to PGMC did not affect permeation flux, while the lag time decreased significantly from 5.14 +/- 3.31 to 0.31 +/- 0.12 h as the PG increased from 40% to 60%.
为研究开发一种新型昂丹司琼透皮给药系统的可行性，研究了载体和渗透促进剂对盐酸昂丹司琼（OS）从压敏胶（PSA）基质经背部无毛小鼠皮肤的体外渗透的影响。本研究中使用的载体由不同比例的单辛酸丙二醇酯（PGMC）-二甘醇单乙醚（DGME）共溶剂和含3%油酸的PGMC-丙二醇（PG）共溶剂组成。Duro-Tak 87-2100和Duro-Tak 87-2196用作压敏胶。PGMC-DGME共溶剂体系中DGME的浓度影响释放速率；随着DGME浓度的增加，释放速率降低。OS的累积释放量随着压敏胶与药物溶液比例的降低而增加。渗透通量也主要受压敏胶用量的影响；随着用量的减少，渗透通量增加。与溶液制剂相比，基质制剂的总通量显著更低。PG与PGMC的比例不影响渗透通量，而随着PG从40%增加到60%，滞后时间从5.14±3.31小时显著缩短至0.31±0.12小时。
