Triacetyl alfa-cyclodextrin, triacetyl beta-cyclodextrin and triacetyl gamma-cyclodextrin were tested as possible hydrophobic carriers to prolong the release of hydrophilic teicoplanin (TCP). Physical–chemical characterization of individual components, drug-carrier physical mixtures at 0.5, 0.67 and 0.75 mass fraction of carrier, and the respective interaction products by kneading or evaporative crystallization under microwave irradiation was carried out using differential scanning calorimetry (DSC) and thermogravimetric analysis (TGA). In vitro drug release in pH 7.4 phosphate buffer at 37 °C was determined by intrinsic dissolution rate (IDR) measurements on non disintegrating compressed discs. Solid-state interactions of TCP with triacetyl a-cyclodextrin by evaporative crystallization and kneading and with triacetyl beta-cyclodextrin by evaporative crystallization (probably resulting in carrier amorphization) were demonstrated. The role of carrier hydrophobicity, carrier mass fraction and preparation method of solid drug-carrier combinations on solid-state drug-carrier interactions and slowing down of TCP release was assessed. Modulation of drug release can be achieved using TCP-triacetyl gamma-cyclodextrin combinations at 0.5 mass fraction of carrier.

Solid-state interaction and drug release of teicoplanin in binary combinations with peracetylated alfa-, beta- and gamma-cyclodextrins

BETTINETTI, GIAMPIERO;SORRENTI, MILENA LILLINA;CATENACCI, LAURA;FERRARI, FRANCA;ROSSI, SILVIA STEFANIA;
2007-01-01

Abstract

Triacetyl alfa-cyclodextrin, triacetyl beta-cyclodextrin and triacetyl gamma-cyclodextrin were tested as possible hydrophobic carriers to prolong the release of hydrophilic teicoplanin (TCP). Physical–chemical characterization of individual components, drug-carrier physical mixtures at 0.5, 0.67 and 0.75 mass fraction of carrier, and the respective interaction products by kneading or evaporative crystallization under microwave irradiation was carried out using differential scanning calorimetry (DSC) and thermogravimetric analysis (TGA). In vitro drug release in pH 7.4 phosphate buffer at 37 °C was determined by intrinsic dissolution rate (IDR) measurements on non disintegrating compressed discs. Solid-state interactions of TCP with triacetyl a-cyclodextrin by evaporative crystallization and kneading and with triacetyl beta-cyclodextrin by evaporative crystallization (probably resulting in carrier amorphization) were demonstrated. The role of carrier hydrophobicity, carrier mass fraction and preparation method of solid drug-carrier combinations on solid-state drug-carrier interactions and slowing down of TCP release was assessed. Modulation of drug release can be achieved using TCP-triacetyl gamma-cyclodextrin combinations at 0.5 mass fraction of carrier.
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11571/134460
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