Summary:
Oral mucoadhesive tablets belong to modern dosage forms, which allow controlled drug release
after buccal application. They are used for the treatment of oral cavity disorders or for systemic
administration of drugs with high first-pass effect or drugs instable in gastrointestinal tract. This study
reports the development of oral mucoadhesive tablets containing antimycotic drug ciclopiroxolamine.
Mucoadhesive properties of placebo tablets containing different ratios of carbomer and hydroxypropylmethylcellulose
were evaluated in vivo in healthy human volunteers. The longest
mucoadhesion for 9 hours was achieved in matrices containing 60 % (w/w) of carbomer. When optimum
combination of the two mucoadhesive polymers was selected, tablets containing ciclopiroxolamine
were prepared and one tablet side was film-coated to make the application procedure easier.
Tablet quality parameters were determined and drug dissolution profile was evaluated under different
pH conditions. In vitro release of ciclopiroxolamine was slower than the desintegration of prepared
mucoadhesive tablets in vivo. Nevertheless, tablets containing 25 mg of ciclopiroxolamine
performed prolonged drug release with oral mucosa concentrations higher than its MIC of relevant
pathogens.
Key words:
mucoadhesion – tablet – carbomer – controlled release – ciclopiroxolamine
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