14.Parenterals.ppt

15. Ophthalmic Solutions and Suspensions Hongxia Guo Ph.D. in Pharmacy Contents Ophthalmic drug delivery Pharmaceutic requirements Packaging ophthalmic solutions and suspensions Proper administration of ophthalmic solutions and suspensions Ophthalmic drug delivery infections allergic or inflammation elevated intraocular pressure dry-eye 现临床应用的剂型中以滴眼液为主,上市产品中62.4 %为溶液型, 8.7 %为混悬型；还有少量的软膏剂,占17.4 %。 滴眼液用药后经泪液冲刷或从鼻泪管流失,药效维持短,生物利用度低(1%～10%左右) 给药频繁；一般药典规定给药3～4 次/d ,但实际临床应用时可多达10～20 次/d ,从而造成诸多的副作用。 由于夜间给药不便,使得药理峰谷现象突出。 药物在眼部的吸收途径 1．角膜吸收途径 大多数药物眼部用药的吸收途径为角膜吸收，水溶性大的药物不易透过角膜，脂溶性大的药物比较容易透过角膜，但却不易从角膜向眼的深层组织透过，所以在水和脂溶性介质中均有一定溶解度的药物，有利于药物的角膜吸收。 角膜吸收是眼局部用药的主要吸收途径。 2．非角膜吸收 非角膜吸收的部位在角膜—结膜处被局部毛细血管吸收进入体循环，非角膜吸收是眼用制剂发挥全身作用的主要吸收途径。 Pharmaceutic requirements Special consideration for ophthalmic preparations: sterility preservation isotonicity buffering viscosity ocular bioavailability and packaging Sterility and Preservation Ophthalmic solutions/suspensions could be sterilized by autoclaving at 121?C for 15 minutes bacterial filters To maintain sterility during patient use, antimicrobial preservatives generally are included in ophthalmic formulations. The preservatives used in ophthalmic solutions/suspensions are benzalkonium chloride（苯扎氯铵） , 0.004-0.01%; benzethonium chloride（氯化苄乙胺）, 0.01%; chlorobutanol（三氯叔丁醇）, 0.5%; phenylmercuric acetate（醋酸苯汞), 0.004%; phenylmercuric nitrite（硝酸苯汞）, 0.004%; thimerosal（硫酸汞）, 0.005-0.01% Isotonicity Value Isotonic solution: a solution that has the same salt concentration as the normal cells of the body and the blood. Hypotonic, solutions with a lower osmotic pressure than body fluids or a 0.9% sodium chloride solution are commonly referred to as hypotonic. Hypertonic, solutions have a greater osmotic pressure are termed hypertonic. 渗透压调节： (1)冰点降低数据法: 血浆的冰点= ?0.52 ?C 溶液的冰点 = ?0.52 ?C，与血浆等渗 例题1：配100ml等渗NaCl溶液，需NaCl多少？（1%NaCl，冰点= ?0.58?C ,血浆，冰点= ?0.52 ?C） 1% ：X = ?0.58 ：?0.52 X = 0.9g 例题2：配100ml的2%盐酸普鲁卡因溶液,需加NaCl多少使成等渗溶液？ （ 血浆，冰点= ?