4.4 Article

Design and in vitro characterization of buccoadhesive tablets of timolol maleate

Journal

DRUG DEVELOPMENT AND INDUSTRIAL PHARMACY
Volume 40, Issue 5, Pages 680-690

Publisher

TAYLOR & FRANCIS LTD
DOI: 10.3109/03639045.2014.892955

Keywords

Buccal; compatibility; drug release; DSC; entrapments; FTIR; P-XRD; swelling index

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Objective: The purpose of this work was to develop and evaluate buccoadhesive tablets of timolol maleate (TM) due to its potential to circumvent the first-pass metabolism and to improve its bioavailability. Methods: The tablets were prepared by direct compression using two release modifying polymers, Carbopol 974P (Cp-974p) and sodium alginate (SA). A 3(2) full factorial design was employed to study the effect of independent variables, Cp-974p and SA, in various proportions in percent w/w, which influences the in vitro drug release and bioadhesive strengths. Physicochemical properties of the drug were evaluated by ultraviolet, Fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC) and powder X-ray diffraction (P-XRD). Tablets were evaluated for hardness, thickness, weight variation, drug content, surface pH, swelling index, bioadhesive force and in vitro drug release. Results: The FTIR and DSC studies showed no evidence of interactions between drug, polymers and excipients. The P-XRD study revealed that crystallinity of TM remain unchanged in optimized formulation tablet. Formulation F9 achieves an in vitro drug release of 98.967% +/- 0.28 at 8 h and a bioadhesive force of 0.088 N +/- 0.01211. Conclusion: We successfully developed buccal tablet formulations of TM and describe a non-Fickian-type anomalous transport as the release mechanism.

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