Timolol maleate

Glaucoma is an optic neuropathy associated with retinal ganglion cell death that results in visual field loss. Elevated intraocular pressure (IOP) is a primary risk factor for the disease. Glaucoma is the second leading cause of blindness worldwide. Primary open angle glaucoma alone accounts for about 75% of all primary glaucoma. Timolol maleate (non selective β adrenergic antagonist) and Latanoprost (prostaglandin analogue) are commonly used drugs. Our aim of study is to compare the ocular hypotensive effect and safety of topical Timolol maleate (0.5%) and Latanoprost (0.005%) in patients of primary open angle glaucoma. A total of 60 patients with primary open angle glaucoma were included and studied for 6 months. One group of patients were given 0.5% timolol maleate eye drops twelve hourly and other group were given 0.005% latanoprost eye drops once a day. In our study both drugs were significantly effective in lowering the intraocular pressure. The mean fall in IOP in Timolol group was 6.69mmHg (26.10%) and in Latanoprost group was 7.20mmHg (28.5%) from pretreatment values. The difference between the values of mean of reduction in IOP from baseline IOP of the two groups was 0.512 mmHg that was statistically insignificant. The systemic and ocular side effects observed in two groups were comparable and both groups were well tolerated. Timolol maleate and Latanoprost both drugs are effective significantly in lowering the IOP, well tolerated and safe with negligible systemic side effects and comparable ocular side effects.

  The aim of the present study was to prepare and characterize twice-daily sustained-release matrix tablets of Timolol maleate (TM) using different concentrations of hydrophilic Hydroxypropylmethylcellulose (HPMC K100M CR) alone and its combination with hydrophobic ethyl cellulose (EC). Formulations prepared by the wet granulation technique and were evaluated for the release of TM over a period of 12 hours using United States Pharmacopoeia (USP) type-II dissolution apparatus. Along with physical properties, the dynamics of water uptake and erosion degree of tablets were also studied. The in-vitro drug release study revealed that formulation F3 (40% wt/wt HPMC K100M) could extend the drug release up to 8 hours. The most successful formulation of the study, F5 (HPMC to EC, 1:1), extended the drug release up to 12 hours, exhibited satisfactory drug release in the initial hours, and the total release pattern was close to the theoretical release profile. The drug release from optimized formulation (F5) followed first-order kinetics via Non-Fickian (anomalous) diffusion. FTIR studies revealed that there was no interaction between the drug and excipients. In conclusion, the results indicated that the prepared sustained-release tablets of TM could perform therapeutically better than conventional tablets with improved efficacy and better patient compliance.   Key words: Timolol maleate; Matrix tablets; Sustained-release; Ethyl cellulose; Hydroxypropylmethylcellulose; In-vitro drug release.

Timolol maleate, an antihypertensive drug has a half-life of 2-3 hours and a bioavailability of about 60%. It undergoes extensive first pass metabolism. The present study aims to formulate and evaluate Transdermal drug delivery for sustained release of Timolol maleate. The partition coefficient in octanol /water system indicates that the drug is suitable for Transdermal drug delivery. The Physicochemical compatibility of the drug and polymers was studied by IR spectroscopy and the results suggested no physicochemical incompatibility between drugs and the polymers. Total 20 formulations were prepared. The transdermal patches were prepared using different polymers like Hydroxy Propyl Methyl Cellulose, Polyvinyl alcohol and Poly vinyl pyrrolidine in varied ratios, plasticizers like propylene glycol and various permeation enhancers. The patches were evaluated for various parameters like Thickness, weight variation, Water-Vapor Permeability, Tensile Strength, Percent Moisture Uptake, Drug Content, Diffusion and Dissolution studies. The interaction among various components of the matrices was studied by performing Differential Scanning Calorimetry. The Optimized formulation containing PVA: PVP (F 19) in the ratio of 3:2 and containing 30 % propylene glycol as a plasticizer and 2 % Hyaluronidase as a permeation enhancer gave a maximum release 51.68 % (4.75 mg) over a period of 8 hours. Stability studies were carried out as per ICH guidelines and formulations were found to be Stable. Key words: Transdermal patches; Timolol maleate; Differential Scanning Calorimetry (DSC); Infrared spectroscopy (IR); Partition co-efficient.