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Mais Fadhel Mohammed , Zainab Ahmed Sadeq , Omar Saeb Salih

Abstract

The study is related to the formulation and evaluation of mucoadhesive buccal tablets of Anastrozole to enhance its bioavailability by avoiding 1st pass effect. The study succeeded in developing mucoadhesive buccal tablets containing two layers (mucoadhesive and backing layer) in a design that permits the unidirectional release of the drug. Tablets of Anastrozole were prepared by double direct compression method using (carbopol 934) as a primary mucoadhesive polymer, Sod.alginate, Na CMC, and HPMC as secondary polymers, Ethyl Cellulose as a backing layer. The tablets are determined for Weight variation, Hardness, Swelling index, Friability, Surface pH, Content Uniformity, Ex vivo Residence time, Mucoadhesive Strength Study, and in-vitro Release Study and Differential Scanning Calorimetry (DSC) studies revealed no evidence of any interaction between drugs, polymers, and additives. Six formulations were prepared to study different factors (different concentrations of primary polymer, different secondary polymers, different methods of formulation, and the effect of adding a Co-binder). The optimum formula (F1) was chosen due to its reasonable results, the cumulative percentage of release (93%), mucoadhesive strength (81.5gm), ex vivo Residence time exceeds the dissolution time (8.1hr), Surface pH is compatible with oral pH (6.1), good mechanical strength with acceptable values for content uniformity, weight variation, and swelling index. These gathered results make a formula that may avoid the 1st pass effect of Anastrozole and improve its bioavailability and consequently may reduce its dose and dosing frequency leading to decrease its side effects and increase compliance of patient‎.

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