FORMULATION AND EVALUATION OF TIMOLOL MALEATE MUCOADHESIVE BUCCAL TABLET AS ANTIHYPERTENSIVE
Shubham Singh*
ABSTRACT
Back ground: Bioadhesion is simply defined as an ability of material to adhere to a biological tissue for a longer period of time. Mucoadhesion generates the interest in a sequence to enhance localized drug delivery or the delivery of difficult molecule into the systemic circulation. Objective: The formulation and evaluation of mucoadhesive buccal tablets containing an antihypertensive drug are related to the ongoing examination such as timolol maleate to overcome the first pass effect and to enhance its bio-availability with the help of reducing in dosing frequency and also dose-related side effects. With the help of changing the concentration of polymers such as carbopol 934, polyethylene oxide and sodium carboxy methyl cellulose, eight formulations will be prepared. Methods: Weight variation, hardness, friability, surface pH, drug content uniformity, swelling index, and bioadhesive strength, in-vitro drug dissolution study and kinetic studies of the drug release method were used for the tablets testing. FTIR studies exhibited no evidence of interactions between drug, polymers, and excipients. Under sink condition using USP- XXIV dissolution apparatus type 2, in-vitro drug release study of timolol maleate was performed. Results: The in-vitro drug release achieved with the formulation F1 was efficient, which contain the drug, carbopol 934p and polyethylene oxide in the ratio of 1:3:9.5. The result of formulation F1 was found to be surface pH (6.35), bioadhesive strength (36.5 gm) and (82.2 %) swelling index. Conclusion: The tablets (formulation F1) containing 10 mg of timolol maleate exhibited drug release such as 98.36% with desired therapeutic concentration. The dissolution studies of all formulations data were found to be zero-order drug release kinetics.
Keywords: Timolol maleate, Carbopol 934, Polyethylene oxide, Sodium Carboxy Methyl Cellulose, Mucoadhesive, Antihypertensive.
[Full Text Article]
[Download Certificate]