Enhancing the bioavailability of cyclosporine a using solid dispersion containing polyoxyethylene (40) stearate.
Solid dispersion containing polyoxyethylene (40) stearate and cyclosporine A was prepared by solvent-melt method and characterized using differential scanning calorimetry, powder X-ray diffraction, and Infrared Fourier Transform Spectroscopy (FTIR). Dissolution of the drug from solid dispersion was dramatically enhanced compared to that from the drug powder alone and physical mixture. In vivo oral bioavailability of cyclosporine A from the solid dispersion in Wistar rats was comparable to that from a commercial product, Sandimmun Neoral (P>0.05). The formulation is stable up to six months under 30 degrees C/RH60% and one year at 25 degrees C/RH 60% when packed in aluminum-polyethylene laminated bags.
Liu
Chen
C
Department of Pharmaceutics, School of pharmacy, Fudan University, Shanghai, 200032, People's Republic of China.
Wu
Junhua
J
Shi
Bin
B
Zhang
Yuanxing
Y
Gao
Tiankun
T
Pei
Yuanying
Y
D000818:Animals; D001682:Biological Availability; D002152:Calorimetry, Differential Scanning; D016572:Cyclosporine / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics*; D004355:Drug Stability; D008297:Male; D011092:Polyethylene Glycols / Q000008:administration & dosage*; D051381:Rats; D017208:Rats, Wistar; D012995:Solubility; D017550:Spectroscopy, Fourier Transform Infrared; D013678:Technology, Pharmaceutical; D014961:X-Ray Diffraction
D011092:Polyethylene Glycols; D016572:Cyclosporine