Loftsson T, Frithriksdóttir H, Stefánsson E, Thórisdóttir S, Guthmundsson O, Sigthórsson T
Department of Pharmacy, Faculty of Medicine, University of Iceland, Reykjavik.
J Pharm Pharmacol. 1994 Jun;46(6):503-4. doi: 10.1111/j.2042-7158.1994.tb03835.x.
The effect of topically active 2-hydroxypropyl-beta-cyclodextrin (HP-beta-CyD) eye-drop formulations containing solutions of acetazolamide, ethoxyzolamide or timolol on the intra-ocular pressure (IOP) was investigated in normotensive conscious rabbits. Both acetazolamide and ethoxyzolamide were active but their IOP-lowering effect was less than that of timolol. The IOP-lowering effects of acetazolamide and ethoxyzolamide and that of timolol appeared to be to some extent additive. Combination of acetazolamide and timolol or ethoxyzolamide and timolol in one HP-beta-CyD formulation resulted in a significant increase in the duration of activity compared with HP-beta-CyD formulations containing only acetazolamide, ethoxyzolamide or timolol. Also, it was possible to increase the IOP-lowering effect of acetazolamide by formulating the drug as a suspension in an aqueous HP-beta-CyD vehicle.
在正常血压的清醒兔中研究了含有乙酰唑胺、乙氧唑胺或噻吗洛尔溶液的局部活性2-羟丙基-β-环糊精（HP-β-CyD）滴眼剂配方对眼压（IOP）的影响。乙酰唑胺和乙氧唑胺均有活性，但它们的降眼压作用小于噻吗洛尔。乙酰唑胺和乙氧唑胺以及噻吗洛尔的降眼压作用在一定程度上似乎具有相加性。与仅含有乙酰唑胺、乙氧唑胺或噻吗洛尔的HP-β-CyD配方相比，在一种HP-β-CyD配方中联合使用乙酰唑胺和噻吗洛尔或乙氧唑胺和噻吗洛尔可使活性持续时间显著延长。此外，将药物制成在水性HP-β-CyD载体中的混悬液，可以提高乙酰唑胺的降眼压作用。
