Drop Size and Initial Dosing Frequency Problems of Topically Applied Ophthalmic Drugs

Chrai, Sukhbir S.; Makoid, Michael C.; Eriksen, Stuart P.; Robinson, Joseph R.

doi:10.1002/jps.2600630304

Cited by 228 publications

(111 citation statements)

References 3 publications

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“…When 2 drugs are required to control the IOP, there are a number of potential advantages in using a fixed combination rather than separate drugs, including no risk of drug washout, 11 reduced exposure to preservatives, and ultimately better patient compliance and quality of life. 12 The first prostaglandin fixed combination available in the market was latanoprost plus timolol followed by the fixed combination of travoprost plus timolol and bimatoprost plus timolol.…”

Section: Owering Intraocular Pressure (Iop) Is Thementioning

confidence: 99%

Comparison of Travoprost and Bimatoprost plus Timolol Fixed Combinations in Open-Angle Glaucoma Patients Previously Treated with Latanoprost plus Timolol Fixed Combination

Centofanti¹,

Oddone²,

Gandolfi³

et al. 2010

American Journal of Ophthalmology

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GIANLUCA MANNI, AND LUCA ROSSETTI• PURPOSE: To compare the ocular hypotensive effect of bimatoprost plus timolol and travoprost plus timolol fixed combinations in glaucoma patients whose disease was controlled but had not reached their target intraocular pressure (IOP) with the fixed combination of latanoprost plus timolol.• DESIGN: A 2 ؋ 3-month, multicenter, prospective, randomized, double-masked, cross-over clinical trial.•

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Section: Owering Intraocular Pressure (Iop) Is Thementioning

confidence: 99%

Comparison of Travoprost and Bimatoprost plus Timolol Fixed Combinations in Open-Angle Glaucoma Patients Previously Treated with Latanoprost plus Timolol Fixed Combination

Centofanti¹,

Oddone²,

Gandolfi³

et al. 2010

American Journal of Ophthalmology

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“…The fixed combinations have several advantages over the unfixed components. First, they eliminate the need to separate dosing as shown by Chrai et al, 34 who indicated at least 5 min was required before instilling a second treatment to avoid washing out the first. Second, the fixed combination simplifies therapy and should help compliance.…”

Section: Eyementioning

confidence: 99%

Twenty-four-hour efficacy of the brimonidine/timolol fixed combination versus therapy with the unfixed components

Konstas

Katsimpris

Kaltsos

et al. 2007

Eye

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Purpose To evaluate the 24-h intraocular pressure (IOP) control of brimonidine/timolol fixed combination (BTFC) versus the unfixed combination of its individual components, each dosed twice daily, in patients with primary open-angle glaucoma or ocular hypertension. Methods An observer-masked, randomized, crossover, active-controlled, two-centre comparison. Following a 6-week medicine-free period, patients were randomized to BTFC or to the unfixed combination of brimonidine and timolol for 3 months. Patients then were crossed over to the opposite treatment for another 3 months. At the end of the medicinefree period, and each treatment period, patients underwent 24-h IOP measurements at 0600, 1000, 1400, 1800, 2200, and 0200 hours. Results Twenty-eight patients completed this study. Both BTFC and the unfixed components showed a significant IOP reduction from untreated baseline (Po0.0001), and were statistically equal when compared directly, for each individual time point and for the 24-h IOP curve (P40.05). The mean 24-h IOP was 24.671.9 for baseline, 19.271.9 for BTFC, and 19.271.6 mmHg for the unfixed components (P ¼ 1.0). Four patients were discontinued due to side effects. The most common ocular adverse event was ocular hyperaemia (n ¼ 3 with BTFC and n ¼ 5 with the unfixed components, P ¼ 0.7) and systemic adverse events were rare. Conclusion This study suggests that both BTFC and the unfixed components of brimonidine and timolol provide a significant 24-h IOP reduction from untreated baseline, and statistically equal control when compared directly, at each time point and for the 24-h pressure curve.

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“…Studies had revealed that fixed dose combinations of both the drugs are well tolerated in patients with glaucoma with least side effects [15][16][17]. Hence, an attempt was done to design ocular inserts that could remain in the cul-de-sac of the eye for a sustained period of time with a vision to maximise the ocular bioavailability.…”

Section: Resultsmentioning

confidence: 99%

Design and Evaluation of Controlled-Release Ocular Inserts of Brimonidine-Tartrate and Timolol Maleate

Preethi

Kunal

2016

Int J Pharm Pharm Sci

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Objective: The current work was attempted to formulate and evaluate a controlled-release matrix-type ocular inserts containing a combination of brimonidine tartrate and timolol maleate, with a view to sustain the drug release in the cul-de-sac of the eye.Methods: Initially, the infrared studies were done to determine the drug-polymer interactions. Sodium alginate-loaded ocuserts were prepared by solvent casting technique. Varying the concentrations of polymer-sodium alginate, plasticizer-glycerine, and cross-linking agent-calcium chloride by keeping the drug concentration constant, made a total of nine formulations. These formulations were evaluated for its appearance, drug content, weight uniformity, thickness uniformity, percentage moisture loss, percentage moisture absorption, and in vitro release profile of the ocuserts. Finally, accelerated stability studies and the release kinetics were performed on the optimised formulation.Results: It was perceived that polymer, plasticizer, and calcium chloride had a significant influence on the drug release. The data obtained from the formulations showed that formulation-F9 was the optimised formulation, which exhibited better drug release. The release data of the optimised formulation tested on the kinetic models revealed that it exhibited first-order release kinetics. Conclusion:It can be concluded that a natural bioadhesive hydrophilic polymer such as sodium alginate can be used as a film former to load water soluble and hydrophilic drugs like brimonidine tartrate and timolol maleate. Among all formulations, F9 with 400 mg sodium alginate, 2% calcium chloride and 60 mg glycerin were found to be the most suitable insert in terms of appearance, ease of handling, thickness, in vitro drug release and stability.

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Drop Size and Initial Dosing Frequency Problems of Topically Applied Ophthalmic Drugs

Cited by 228 publications

References 3 publications

Comparison of Travoprost and Bimatoprost plus Timolol Fixed Combinations in Open-Angle Glaucoma Patients Previously Treated with Latanoprost plus Timolol Fixed Combination

Comparison of Travoprost and Bimatoprost plus Timolol Fixed Combinations in Open-Angle Glaucoma Patients Previously Treated with Latanoprost plus Timolol Fixed Combination

Twenty-four-hour efficacy of the brimonidine/timolol fixed combination versus therapy with the unfixed components

Design and Evaluation of Controlled-Release Ocular Inserts of Brimonidine-Tartrate and Timolol Maleate

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