Abstract

OPTIMIZATION AND EVALUATION OF METOCLOPRAMIDE HCl AS MUCOADHESIVE BUCCAL PATCH

Nora Zawar Yousif* and Nidhal Khazaal Maraie

Abstract

Buccal drug delivery appeared as an innovative substitute to otherconventional types of drug delivery systems. Within the oral mucosalcavity, the buccal region has rich blood supply and relativepermeability that offers an attractive route for drug administration intothe systemic circulation. This study involved formulation ofmetoclopramide HCl as bilayer mucoadheive buccal patch composedof medicated layer and backing layer to prevent undesirable drugrelease by utilizing solvent casting technique. The medicated layer wasprepared by using hydroxyl propyl methyl cellulose as primarypolymer and different secondary polymers including poly vinylpyrolidone, Carpabol and sodium carboxy methyl cellulose in order tooptimize the final formula. The backing layer was prepared by usingethyl cellulose and dibutyl phthalate as plasticizer. The results revealed that formula F4containing hydroxyl propyl methyl cellulose (75mg) as primary polymer and poly vinylpyrolidone (18.75 mg) as secondary polymer, propylene glycol as plasticizer (30% of totalpolymer weight), sodium saccharine as sweetening agent (4 mg) was chosen as selectedformula in accordance to the surface pH (6.82), tensile strength (15.34), percentageelongation at break (26.75), swelling index (18.64), mucoadhesive strength (19.23gm),percentage moisture absorption (5.35), percentage moisture loss (4.81) and Ex-Vivo residencetime (6.23hrs) which is satisfactory to give invitro release (92.34%) of metoclopramide HClafter 6 hrs. The research showed invivo drug release of 69.54% for selected formula, withinvitro- invivo correlation equal to (0.9822) suggesting successful formulation that can beused mainly for patients having difficulties in swallowing, patients with nausea or vomiting,patients with upper gastrointestinal disease or surgery. Furthermore, to reduce first pass effect with possible reduction in overall dosing, dose dependent side effect and frequency of administration.

Keywords: Metoclopramide HCl, antiemetic, transmucosal, mucoadhesion, buccal patch.