复合制剂新进展PPT.ppt

* 4.Cosopt（ 0.5%timolol + 2% dorzolamide ） 降眼压作用比单用timolol或dorzolamide显著 Yeh J,et al. Rational use of the fixed combination of dorzolamide - timolol in the management of raised intraocular pressure and glaucoma. Clin Ophthalmol. 2008 Jun;2(2):389-99. * Cosopt与非固定配方联合用药比较 与timolol和dorzolamide的非固定配方联合用药对比 Yeh J,et al. Rational use of the fixed combination of dorzolamide - timolol in the management of raised intraocular pressure and glaucoma. Clin Ophthalmol. 2008 Jun;2(2):389-99. * Cosopt增加视网膜血流作用 24例（12例POAG/12例正常对照）临床研究 Cosopt降眼压作用显著优于timolol (p 0.039) Cosopt能显著减少视网膜零流量像点 (zero-flow pixels)，增加视网膜血流 下方视网膜零流量像点减少量 POAG组 -51.44%，p 0.008 正常对照组 -55.38%，p 0.006 Siesky B, et al. Ocular blood flow and oxygen delivery to the retina in primary open-angle glaucoma patients: the addition of dorzolamide to timolol monotherapy. Acta Ophthalmol. 2010 Feb;88(1):142-9. * Cosopt 与单用brimonidine比较 Cosopt (n=23), brimonidine (n=23), control (n=23) 点眼后6小时眼压 Cosopt (16.3+/-2.9 mm Hg)brimonidine (20.6+/-2.9 mm Hg) control (24.6+/-5.4 mm Hg) 点眼后24小时眼压 Cosopt (14.1+/-2.8 mm Hg) brimonidine (17.5+/-2.7 mm Hg) control (19.8+/-4.7 mm Hg) Ozkurt Y, et al. Comparison of the effects of dorzolamide-timolol fixed combination and brimonidine on intraocular pressure after phacoemulsification surgery. Eye Contact Lens. 2008 Jan;34(1):21-3. * 5.Combigan（ 0.2％Brimonidine ＋ 0.5％timolol ） 与两种单药对比，多中心、双盲临床研究 Combigan 385例, brimonidine 382例, timolol 392例 眼压下降幅度 Combigan 4.9-7.6 mmHg timolol 4.3 to 6.2 mmHg brimonidine 3.1 to 5.5 mmHg (P or = 0.026) Craven ER,et al. Brimonidine and timolol fixed-combination therapy versus monotherapy: a 3-month randomized trial in patients with glaucoma or ocular hypertension. J Ocul Pharmacol Ther. 2005 Aug;21(4):337-48. 眼药水的大部分都通过泪道排出 每滴眼药水体积30–50 μL 结膜囊容积大概7 μL 每眨眼1下就有大约2 μL药水从泪囊消除 7 μL 30–50 μL 洗出效应 洗出效应的影响 Chrai SS et al. J Pharm Sci. 1974; 63(3): 333-338 第一药效的流失(%) 眼部短时间内多次虽然可增加角膜前药物的浓度，但同时也增加了药