Two topical carbonic anhydrase inhibitors sezolamide and dorzolamide in Gelrite vehicle: A multiple-dose efficacy study

Abstract

The ocular hypotensive activities of the two potent topical carbonic anhydrase inhibitors sezolamide (previously known as MK-417) and dorzolamide (previously known as MK-507 and L-671,152) were compared formulated in Gelrite vehicle, a novel ophthalmic drug delivery system. This was a four-center, double-blind, randomized, placebo-controlled, parallel study in 73 patients with a diagnosis of bilateral primary open-angle glaucoma or ocular hypertension and a morning intraocular pressure (IOP) of greater than 23 mmHg in both eyes following washout of ocular hypotensive medications. Parallel 12-h modified diurnal curves were performed prestudy and on day 6, with a 4-h IOP curve on day 1. On day 6 the peak mean percentage decrease in IOP from baseline occurred 4 h after the dose of dorzolamide (22.1%) and 6 h after the dose of sezolamide (21.3%). There were no significant differences between 2% dorzolamide and 1.8% sezolamide at any time point, although the decrease in IOP for sezolamide tended to be slightly greater than that for dorzolamide. Duration of action of both compounds was, at most, slightly prolonged by the use of Gelrite vehicle when compared with former studies on sezolamide and dorzolamide.

In situ gelling systems of ofloxacin: Comparative performance of in vivo precorneal drainage and pharmacokinetic study

“…[21] Reports of superficial cornea1 haze/opacity have been noted in 20% of patients after 8 weeks of administration with gellan based systems. [22,23] A similar corneal change has been noticed with carbomer, contained in ophthalmic gel after the same period of time. [24] Looking toward the data supported, further study was conducted on thermosensitive in situ gelling medicated formulation.…”

Review of Ocular Drug Delivery

“…There were no significant differences between 2% dorzolamide and 1.8% sezolamide at any time point, although the decrease in IOP for sezolamide tended to be slightly greater than that for dorzolamide [26].…”

“…Hence, there is a need for development of effective drug delivery strategies for the eye. New drug delivery systems (NDDS), for the anterior segment of the eye includes (a) Ocular inserts (1)(2)(3)(4)(5)(6)(7)(8)(9)(10)(11)(12)(13), corneal shields (14)(15)(16) and contact lenses (17)(18), which provides controlled delivery of drug to the eye, (b) In situ gelling systems (19)(20)(21)(22)(23)(24)(25)(26)(27)(28)(29), which provides ease of administration as drops and gets converted to gel form in the eye, thereby providing some sustained effect of drug in the eye, (c) Vesicular systems (30)(31)(32)(33)(34)(35), offers advantages of targeted delivery, bio-*Address correspondence to this author at the Department of Pharmaceutics, Faculty of Pharmacy, Hamdard University, New Delhi 110062. India; Tel: 91-9811660105; E-mail: yas2312003@yahoo.com; ysultana@jamiahamdard.ac.in compatibility and freedom from blurring of vision, (d) Mucoadhesive systems (36)(37)(38)(39)(40)(41) provides better retention in the eye, (e) Prodrugs (42)…”

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“…Duration of action of both the compounds was slightly prolonged by the use of Gelrite® vehicle, when compared to earlier studies 37 .…”