Characterization, dissolution and in vivo evaluation of solid acetazolamide complexes

MARÍA J. MORA, LUIS I. TÁRTARA, RENÉE ONNAINTY, SANTIAGO D. PALMA, MARCELA R. LONGHI, GLADYS E. GRANERO

ELSEVIER SCI LTD

Lugar: Amsterdam; Año: 2013 vol. 98 p. 380 - 380

he effects of binary and ternary systems of acetazolamide (ACZ) with hydroxypropyl-b-cyclodextrin (HP-b-CD) alone or with triethanolamine (TEA) on the crystalline properties, dissolution and intraocular pressure (IOP)-lowering effect were investigated. It was found that the crystal structure of ACZ powder could be modified by the processing conditions. Freeze-drying ACZ powder affected not only the particle morphology but also its polymorphic form and the starting ACZ was converted to pure form A upon freeze-drying treatment. Results provided by DSC/TGA, XRPD, SEM and FT-IR suggested the formation of inclusion complexes between ACZ with HP-b-CD alone or with TEA, obtained by the freeze-drying method and the conversion of the drug into the amorphous state. Binary and ternary systems of ACZ obtained by freeze-drying exhibited significantly enhanced ACZ dissolution rates. The IOP-lowering effects of ACZ and its complexes with HP-b-CD alone or with TEA were studied in normotensive rabb