Malhotra Manjusha, Majumdar D K
Department of Pharmaceutics, College of Pharmacy ( University of Delhi ), Pushp Vihar, Sector-III, New Delhi 110 017, India.
Indian J Exp Biol. 2002 May;40(5):555-9.
The influence of formulation additives, e.g. preservative, antioxidant and viscolizing agents on in vitro transcorneal permeation of ketorolac tromethamine from 0.5%(w/v) aqueous drop was studied using goat cornea. Permeation characteristics of drug, from selected formulations, through excised rabbit cornea were also evaluated. Aqueous solution of ketorolac tromethamine (0.5% w/v), pH 6.5 or 7.0 having ionic strength 0.2, was prepared. To this solution perservatives either alone or in combination with other additives were added to have drops of various composition. Permeation studies with goat cornea showed maximum permeation of ketorolac tromethamine from formulation containing benzalkonium chloride and disodium edetate. Increase in viscosity of drop resulted in decreased permeation of drug. Formulation containing benzalkonium chloride and disodium edetate also increased permeation of drug through rabbit cornea. Cumulative permeation of drug through rabbit cornea was found to be 2.3-2.4 fold higher than that observed with goat cornea.
采用山羊角膜研究了制剂添加剂（如防腐剂、抗氧化剂和增粘剂）对0.5%（w/v）酮咯酸氨丁三醇滴眼液体外角膜透过性的影响。还评估了选定制剂中药物通过离体兔角膜的渗透特性。制备了pH值为6.5或7.0、离子强度为0.2的酮咯酸氨丁三醇水溶液（0.5% w/v）。向该溶液中单独或与其他添加剂组合添加防腐剂，以制成不同成分的滴眼液。用山羊角膜进行的渗透研究表明，含苯扎氯铵和依地酸二钠的制剂中酮咯酸氨丁三醇的渗透率最高。滴眼液粘度增加导致药物渗透率降低。含苯扎氯铵和依地酸二钠的制剂也增加了药物通过兔角膜的渗透率。发现药物通过兔角膜的累积渗透率比山羊角膜高2.3 - 2.4倍。
