Background and Objective: Upon oral administration domeperidone is rapidly absorbed, but
subjected to the first pass effect which lowers systemic bioavailability to 15%. Mucoadhesive tablet
can remain attached to buccal mucosa and becomes capable of bypassing hepatic first-pass metabolism
to improve absorption directly into systemic circulation. The present research work was carried with an
aim to develop, evaluate and optimize mucoadhesive tablet containing domperidone (DOME) for buccal
delivery using different bio-adhesive polymeric combinations.
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Methods: The buccal tablets were formulated by wet granulation method using isopropyl alcohol. The
preliminary formulations were prepared using combinations of HPMC K4, HPMC K15, HPMC K100,
HPMC E5 as mucoadhesive polymers. 32 full factorial design was applied to determine the effect of
independent variables like concentration of mucoadhesive polymers (HPMC K15 and HPMC K100)
over dependent variables like mucoadhesive properties (swelling index, bioadhesive strength and in vitro
drug release). The prepared mucoadhesive tablets were evaluated for their tablet properties and mucoadhesive
properties. The interactions between drug and polymers were studied by Fourier Transform
Infrared Spectroscopy (FTIR) and Differential Scanning Calorimetry (DSC).
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Results: All formulations of factorial design showed satisfactory physicochemical, mechanical and
bioadhesive characteristics. The formulation F9 exhibited maximum cumulative drug release, mucoadhesive
strength and swelling index.
Conclusion:
The developed buccal tablet of domperidone might prove alternative to bypass the hepatic
first pass metabolism and to avoid degradation which in turn may result in reducing the frequency of
administration. Thus, mucoadhesive tablet of domeperidone may become viable alternative overcoming
the side effects; achieving greater therapeutic effectiveness and improving the patient compliance.
Stereoselective first-pass metabolism of highly cleared drugs: studies of the bioavailability of L- and D-verapamil examined with a stable isotope technique.
