Timolol maleate

• CAS: 26921-17-5
• Catalog Number: ACM26921175
• Category: Main Products
• Molecular Weight: 432.49
• Molecular Formula: C17H28N4O7S
• Synonyms: (2S)-1-[(1,1-Dimethylethyl)amino]-3-[[4-(4-morpholinyl)-1,2,5-thiadiazol-3-yl]oxy]-2-propanol (2Z)-2-Butenedioate Salt; (S)-(-)-3-Morpholino-4-(3-tert-butylamino-2-hydroxypropoxy)-1,2,5-thiadiazole Hydrogen Maleate
• Melting Point: >196 °C
• Appearance: White Solid

Case Study

Timolol Maleate for Intraocular Pressure Reduction in Horses

Ziadi A, et al. Journal of Equine Veterinary Science, 2022, 111, 103886.

Timolol maleate has been widely utilized for lowering intraocular pressure (IOP) in both human and veterinary ophthalmology. A comparative study evaluated the efficacy of 0.5% timolol maleate versus 0.5% apraclonidine in reducing IOP in healthy horses.
The study involved 20 thoroughbred horses divided into two groups. One group received a single topical application of 0.5% timolol maleate in one eye, while the contralateral eye was treated with placebo (artificial tears). IOP measurements were taken at multiple time points post-instillation using a rebound tonometer. The results demonstrated that timolol maleate significantly reduced IOP, with the most pronounced effect observed at 360 minutes post-application, achieving a 14.7% reduction. However, compared to apraclonidine, which exhibited a faster and more substantial IOP-lowering effect (29.7% at 120 minutes), timolol required a longer duration to exert its peak effect.
Although the study confirmed timolol maleate's efficacy in reducing IOP in equine eyes, its slower onset and lower magnitude of reduction compared to apraclonidine suggest that it may be more suitable for long-term IOP management rather than rapid pressure relief.

Timolol Maleate-Loaded Interpenetrating Polymer Network (IPN) Sponges for Ophthalmic Drug Delivery

Balla E, et al. International Journal of Pharmaceutics, 2023, 646, 123439.

A novel interpenetrating polymer network (IPN) sponge system was developed for the controlled delivery of timolol maleate (TIM). TIM was incorporated at concentrations of 10, 20, and 30 wt% by dissolving the drug in an aqueous medium, followed by homogenization and freeze-drying at -60°C under reduced pressure. The resulting porous sponges exhibited enhanced drug loading capacity and stability under ambient conditions. Furthermore, a co-encapsulation strategy integrating TIM with dorzolamide hydrochloride (DORZ), a carbonic anhydrase inhibitor, at a 1:1 ratio (20 wt% per drug) was successfully implemented, offering a synergistic approach for dual-action glaucoma therapy. The study underscores the potential of IPN-based sponges as an advanced ocular drug delivery system, enabling prolonged drug release and improved patient compliance.

Timolol Maleate 0.5% Microdrops for Intraocular Pressure Reduction in Open-Angle Glaucoma and Ocular Hypertension

Jennifer S. Steger, et al. Ophthalmology, 2024, 131(9), 1045-1055.

A recent randomized, active-controlled clinical trial evaluated the efficacy and safety of Timolol Maleate 0.5% microdrops administered using the Nanodropper Adaptor for patients with open-angle glaucoma (OAG) and ocular hypertension (OHT). This prospective, multicenter study assessed whether a 12.5 μl microdrop formulation provides noninferior intraocular pressure (IOP) reduction compared to conventional 28 μl drops.
Results demonstrated that both conventional and microdrop formulations significantly lowered IOP at all measured timepoints. Noninferiority was established at three out of four timepoints, confirming that Timolol Maleate 0.5% microdrops effectively reduce IOP while utilizing a lower drug volume. Additionally, the microdrop formulation exhibited a slightly reduced systemic impact, with a 3 beats per minute (bpm) lower heart rate reduction than conventional drops.
These findings suggest that Timolol Maleate 0.5% microdrops offer a clinically effective and potentially safer alternative to traditional formulations, minimizing systemic β-blocker effects while maintaining ocular hypotensive efficacy in glaucoma and OHT management.

Timolol Maleate in Coloaded Liposomal Formulation for Ocular Drug Delivery

Verma P, et al. International Journal of Pharmaceutics, 2024, 664, 124566.

Timolol maleate is widely used in ophthalmic applications for lowering intraocular pressure (IOP) in glaucoma treatment. In a study utilizing the thin-film hydration method, timolol maleate and dorzolamide HCl were coloaded into liposomes to enhance ocular bioavailability and therapeutic efficacy. The formulation incorporated LECIVA-S75 and cholesterol, dissolved in a chloroform-methanol mixture (2:1), followed by solvent evaporation via rotary evaporation at 60 °C under reduced pressure. Hydration of the lipid film was performed using phosphate-buffered saline (pH 7.4) under bath sonication, and particle size reduction was achieved through high-pressure homogenization.
To ensure sterility, the process was conducted aseptically with all glassware autoclaved prior to use. Gamma irradiation (5 kGy) was employed for final sterilization, with post-irradiation characterization confirming formulation stability. This liposomal delivery system offers a promising approach to enhance drug retention, reduce systemic absorption, and improve patient compliance in glaucoma therapy.