Lu Guang Wei
Parenteral Center of Emphasis, Global Research & Development, Pfizer Inc, Groton, CT 06340, USA.
Recent Pat Drug Deliv Formul. 2010 Jan;4(1):49-57. doi: 10.2174/187221110789957246.
In an effort to improve the drug solubility, stability and/or ocular bioavailability of ophthalmic formulations,various approaches have been explored in the recent past. Additionally, different formulations have been investigated in order to seek those preservative systems that are more tolerable to the ocular tissue. Over the past ten years, inventions in ophthalmic formulations directed toward front-of-eye instillations have concentrated in the areas of new excipients' applications, novel and combined use of conventional excipients, and developments of novel dosage forms. Among these areas, applications of polymeric excipients, cyclodextrins and stabilized chloride dioxide (SCD) have been the most actively studied fields. In addition, oil-in-water (O/W) emulsions have been becoming more popular as an ophthalmic dosage form due to the potentials in increasing drug solubility, stabilizing active pharmaceutical ingredients (APIs), improving ocular tolerance, and providing palliative effects. Some of these innovations from the past decade have the capability of leading to new commercial products. This patent review has a useful knowledge in the advancement for treating various ophthalmic diseases.
为了提高眼科制剂的药物溶解度、稳定性和/或眼部生物利用度，近年来人们探索了各种方法。此外，还对不同的制剂进行了研究，以寻找对眼部组织耐受性更强的防腐剂系统。在过去十年中，针对眼前部滴注的眼科制剂发明主要集中在新型辅料的应用、传统辅料的新型和联合使用以及新型剂型的开发等领域。在这些领域中，聚合物辅料、环糊精和稳定二氧化氯（SCD）的应用是研究最为活跃的领域。此外，水包油（O/W）乳剂作为一种眼科剂型越来越受欢迎，因为它具有提高药物溶解度、稳定活性药物成分（API）、提高眼部耐受性和提供缓解作用的潜力。过去十年中的一些创新有能力催生新的商业产品。这篇专利综述对治疗各种眼科疾病的进展具有有益的知识。
