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2. Formulation and in vitro evaluation of mucoadhesive buccal tablets of Timolol maleate

Author(s): Satyabrata Bhanja | P. Ellaiah | Sujit Kumar Martha | Pratit Kanchan Sahu | Sandip Prasad Tiwari | Bibhuti Bhusan Panigrahi | Debajyoti Das

Journal: International Journal of Pharmaceutical and Biomedical Research (IJPBR)
ISSN 0976-0350

Volume: 01;
Issue: 04;
Start page: 129;
Date: 2010;
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Keywords: Timolol maleate | mucoadhesive buccal tablet | Carbopol 934 | Bioadhesive strength | In vitro drug release | Release kinetics

The present investigation is concerned with formulation and evaluation of mucoadhesive buccal tablets containing antihypertensive drug, Timolol maleate to circumvent the first pass effect and to improve its bioavailability with reduction indosing frequency and dose related side effects. The tablets were prepared by direct compression method. Eight formulations were developed with varying concentrations of polymers like Carbopol 934, Polyethylene oxide and Hydroxy Propyl Methyl Cellulose. The tablets were tested for weight variation, hardness, surface pH, drug Content uniformity, swelling index, and bioadhesive strength and in-vitro drug dissolution study. FTIR studies showed no evidence on interactions between drug, polymers, and excipients. The in vitro release of Timolol maleate was performed under sink conditions (Phosphate buffer PH 6.8, 37±0.5ºC, rpm 50) using USP-XXIV dissolution apparatus type II. The best in-vitro drug release profile was achieved with the formulation F5 which contains the drug, Carbopol 934p and HPMC K4M in the ratio of 1:2.5:10. The surface pH, bioadhesive strength and swelling index of formulation F5 was found to be 6.34, 36.5 g and 80.3 %, respectively. The formulation F5, containing 10 mg of Timolol maleate exhibited 7 h sustained drug release i.e. 98.18 % with desired therapeutic concentration. The in vitro release kinetics studies reveal that all formulations fits well with zero order kinetics followed by Korsmeyer-Peppas, first order and then Higuchi’s model and the mechanism of drug release is non-Fickian diffusion.
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