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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 other
conventional types of drug delivery systems. Within the oral mucosal
cavity, the buccal region has rich blood supply and relative
permeability that offers an attractive route for drug administration into
the systemic circulation. This study involved formulation of
metoclopramide HCl as bilayer mucoadheive buccal patch composed
of medicated layer and backing layer to prevent undesirable drug
release by utilizing solvent casting technique. The medicated layer was
prepared by using hydroxyl propyl methyl cellulose as primary
polymer and different secondary polymers including poly vinyl
pyrolidone, Carpabol and sodium carboxy methyl cellulose in order to
optimize the final formula. The backing layer was prepared by using
ethyl cellulose and dibutyl phthalate as plasticizer. The results revealed that formula F4
containing hydroxyl propyl methyl cellulose (75mg) as primary polymer and poly vinyl
pyrolidone (18.75 mg) as secondary polymer, propylene glycol as plasticizer (30% of total
polymer weight), sodium saccharine as sweetening agent (4 mg) was chosen as selected
formula in accordance to the surface pH (6.82), tensile strength (15.34), percentage
elongation 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 residence
time (6.23hrs) which is satisfactory to give invitro release (92.34%) of metoclopramide HCl
after 6 hrs. The research showed invivo drug release of 69.54% for selected formula, with
invitro- invivo correlation equal to (0.9822) suggesting successful formulation that can be
used 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.


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