Formulation of azapropazone ophthalmic preparations using cyclodextrins as complexing agents

The effect of cyclodextrins (CyDs)​, hydroxypropyl β-​cyclodextrin (HP-​β-​CyD) and β-​cyclodextrin (β-​CyD) on the soly. and release characteristics of azapropazone (Az) was investigated.  The aq. soly. of azapropazone was significantly increased by the formation of water sol. (1:1) inclusion complexes with CyDs.  Also, the soly. of azapropazone increased linearly as a function of HP-​β-​CyD followed by β-​CyD.  The ophthalmic formulations (drops, gels and ophthalmic inserts) were prepd. using aq. vehicles contg. sodium CM-​cellulose and carbopol 941 mixt. at different concns.  The amts. released of azapropazone front eye drops, gels and ophthalmic inserts contg. the drug complexes with CyDs in (1:1) molar ratio were significantly higher than formulations contg. the drug alone.  In addn., the in vitro availability of the drug from drops was higher than gels or and ophthalmic inserts at different time intervals.