Solid-state interactions and drug release of teicoplanin in binary combinations with peracetylated α-, β-, and γ-cyclodextrins |
| |
Authors: | Giampiero Bettinetti Milena Sorrenti Laura Catenacci Franca Ferrari Silvia Rossi Ilaria Salvadeo Paolo Carraro |
| |
Institution: | (1) Department of Pharmaceutical Chemistry, University of Pavia, Via Taramelli 12, 27100 Pavia, Italy;(2) Wacker-Chemie Italia srl, Via Einaudi 6-8, 20068 Peschiera Borromeo, MI, Italy |
| |
Abstract: | Triacetyl α-cyclodextrin, triacetyl β-cyclodextrin and triacetyl γ-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 α-cyclodextrin by evaporative
crystallization and kneading and with triacetyl β-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 γ-cyclodextrin combinations at 0.5 mass fraction of carrier. |
| |
Keywords: | Differential scanning calorimetry Intrinsic dissolution rate Peracetylated α - β - and γ -cyclodextrins Teicoplanin Thermogravimetric analysis |
本文献已被 SpringerLink 等数据库收录! |
|