First pass hepatic metabolism

Lignocaine Hydrochloride (LH) is a local anesthetic agent used in the treatment of periodontal and various other dental diseases. It undergoes extensive first pass metabolism with a consequent low bioavailability. Keeping this into account the research work was focused to formulate buccal tablets of LH in an effort to achieve prolonged relief from pain. Buccal tablets were prepared by direct compression method using different bio-adhesive polymers such as chitosan with methocel K15, sodium alginate and methocel K4. Ethyl cellulose (EC) was used as an impermeable backing layer. The optimized formula (F9) was evaluated for in vitro drug release (99.51%±0.59) in phosphate buffer for 6 hrs and bio adhesion strength was found to be 22 gr. The amount of drug permeated through the buccal membrane was found to be 85.03 ±0.21.Stability studies of the F9 indicated no significant changes with respect to drug content, in-vitro release and ex-vivo permeation. Key Words: Lignocaine hydrochloride, Buccal drug delivery system, First pass hepatic metabolism, Ex vivo permeation studies.