Departamento de Farmacia, Facultad de Ciencias Químicas, Universidad Nacional de Córdoba, Ciudad Universitaria, X5000HUA Córdoba, Argentina.
Expert Opin Drug Deliv. 2010 Aug;7(8):943-53. doi: 10.1517/17425247.2010.497536.
Acetazolamide (ACZ), a carbonic anhydrase inhibitor (CAI), and other oral CAIs have been an integral part of antiglaucoma therapy for > 40 years. ACZ is used orally for the reduction of intraocular pressure in patients suffering from glaucoma. However, this treatment leads to unpleasant systemic side effects. The answer to the undesirable effects of ACZ is the topical delivery of this drug into the eye, where it could elicit its physiological action. However, the development of a topical formulation of ACZ is limited by its poor ocular bioavailability, which can be largely attributed to its poor penetration coefficient and poor biphasic solubility.
This review offers an overview of different approaches to delivering ACZ to the eye, highlighting the potential of the ternary system ACZ:HP-beta-CD:TEA as a tool for formulating aqueous ACZ eye drop solutions.
A critical analysis is provided to highlight the key issues to design formulations containing hydrophilic cyclodextrins.
The ACZ:HP-beta-CD:TEA complex is an important new approach to improve the ocular bioavailability of this drug. This approach may be applied to other CAIs in the future.
乙酰唑胺 (ACZ)，一种碳酸酐酶抑制剂 (CAI)，和其他口服 CAI 已经成为抗青光眼治疗的一个组成部分>40 年。ACZ 被口服用于降低青光眼患者的眼内压。然而，这种治疗会导致不愉快的全身副作用。ACZ 的副作用的答案是将这种药物局部递送到眼睛，在那里它可以发挥其生理作用。然而，ACZ 的局部制剂的开发受到其较差的眼部生物利用度的限制，这主要归因于其较差的渗透系数和较差的双相溶解度。
本篇综述提供了一种将 ACZ 递送到眼睛的不同方法的概述，重点介绍了 ACZ：HP-β-CD：TEA 三元系统作为配制水性 ACZ 滴眼溶液的工具的潜力。
提供了批判性分析，突出了设计含有亲水性环糊精的制剂的关键问题。
ACZ：HP-β-CD：TEA 络合物是提高这种药物眼部生物利用度的一种重要新方法。该方法将来可应用于其他 CAI。
