Characterization, dissolution and in vivo evaluation of solid acetazolamide complexes

MARIA JULIA MORA, IGNACIO TÁRTARA, RENÉE ONNAINTY, SANTIAGO D. PALMA, MARCELA R. LONGHI, GLADYS E. GRANERO

CARBOHYDRATE POLYMERS

ELSEVIER SCI LTD

Lugar: Amsterdam; Año: 2013

0144-8617

inary and ternary systems of acetazolamide (ACZ) with hydroxypropyl-ß-cyclodextrin (HP-ß-CD) and/or triethanolamine (TEA) were investigated for solid phase characterization. Freeze-drying affected the marketed ACZ powder, not only the particle morphology but also the polymorphic form of the drug. The starting ACZ was converted to pure form A upon freeze-dried treatment Freeze-drying produced inclusion complexes between ACZ and HP-ß-CD and the conversion of the drug into amorphous state. In contract, no inclusion complex was formed by the physical mixture of ACZ with HP-ß-CD and/or TEA, even though, drug-CD interaction was expressive. ACZ underwent a polymorphic transformation from form B to form A with the physical mixture of ACZ with HP-ß-CD. However, the presence of the TEA, in this binary physical mixture, inhibited the drug polymorphic transformation. It was found that the amount of TEA affected the capability of HP-ß-CD to interact with ACZ efficiently, as well as, the morphology