Malhotra M, Majumdar D K
Department of Pharmaceutics, College of Pharmacy, (University of Delhi), New Delhi, India.
Indian J Exp Biol. 1997 Dec;35(12):1324-30.
Transcorneal permeation of ketorolac from oil based ocular drops and ophthalmic ointments was studied in vitro, using goat cornea. Cumulative (%) permeation of ketorolac through cornea, was found to be maximum with 0.2% (w/v) ketorolac drops in sesame oil followed by formulations in corn oil and soyabean oil. Ketorolac 1% (w/v) drops in castor oil increased the quantity permeated but cumulative (%) permeation was less. Permeation profiles of ketorolac were in consistence with the partition characteristic of drug between oil and aqueous phase. Formulations favouring corneal permeation of ketorolac increased corneal hydration. Addition of benzyl alcohol, a preservative, to oil drops reduced permeation of ketorolac and corneal hydration indicating possible protective effect of benzyl alcohol against corneal damage. Permeation studies on ointment formulations containing either ketorolac acid or ketorolac tromethamine salt indicated better permeation for formulation containing ketorolac tromethamine aqueous solution. Thus for better transcorneal permeation, ketorolac 0.2% (w/v) drops, formulated in sesame oil, containing 0.5% v/v benzyl alcohol and ophthalmic ointment containing 0.5% (w/w) ketorolac tromethamine in dissolved state appear suitable.
采用山羊角膜,在体外研究了酮咯酸从油基眼药水和眼膏中的角膜渗透情况。发现酮咯酸通过角膜的累积(%)渗透率在芝麻油中0.2%(w/v)的酮咯酸滴眼液中最高,其次是玉米油和大豆油中的制剂。蓖麻油中1%(w/v)的酮咯酸滴眼液增加了渗透量,但累积(%)渗透率较低。酮咯酸的渗透曲线与药物在油相和水相之间的分配特性一致。有利于酮咯酸角膜渗透的制剂增加了角膜水合作用。向油滴中添加防腐剂苯甲醇会降低酮咯酸的渗透率和角膜水合作用,表明苯甲醇对角膜损伤可能具有保护作用。对含有酮咯酸或酮咯酸氨丁三醇盐的眼膏制剂的渗透研究表明,含有酮咯酸氨丁三醇水溶液的制剂具有更好的渗透性。因此,为了实现更好的角膜渗透,芝麻油中配制的含0.5% v/v苯甲醇的0.2%(w/v)酮咯酸滴眼液和溶解状态下含0.5%(w/w)酮咯酸氨丁三醇的眼膏似乎是合适的。