Preparation, characterization and in vivo evaluation of ibuprofen binary solid dispersions with poloxamer 188.
Ibuprofen-Poloxamer 188 (P 188) binary solid dispersions (SD) with different drug loadings were prepared, characterized by scanning electron microscopy (SEM), differential scanning calorimetry (DSC) and Fourier transform infrared spectroscopy (FTIR), and evaluated for solubility, in vitro release, and oral bioavailability of ibuprofen in rats. Loss of their individual surface properties during melting and solidification as revealed by SEM micrographs indicated the formation of effective SDs. Absence or shifting towards the lower melting temperature of the drug peak in SDs and physical mixtures in DSC study indicated the possibilities of its interactions with P 188. However, no such interactions in the solid state were confirmed by FTIR spectra which showed the presence of drug crystalline in SDs. Immediate and complete release of ibuprofen from SDs might be because of the reduction in the drug crystalline due to eutectic formation, and their dosing to fasted rats resulted in a significant increase in the area under curve (AUC) of the plasma concentration versus time curve and the maximum plasma concentration (Cmax), and a significant decrease in the time to reach Cmax (Tmax) over ibuprofen and physical mixtures.
Newa
Madhuri
M
College of Pharmacy, Yeungnam University, Gyongsan 712-749, South Korea.
Bhandari
Krishna Hari
KH
Li
Dong Xun
DX
Kwon
Tae-Hyub
TH
Kim
Jung Ae
JA
Yoo
Bong Kyu
BK
Woo
Jong Soo
JS
Lyoo
Won Seok
WS
Yong
Chul Soon
CS
Choi
Han Gon
HG
D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000097:blood / Q000737:chemistry / Q000493:pharmacokinetics; D001682:Biological Availability; D002152:Calorimetry, Differential Scanning; D004339:Drug Compounding; D005079:Excipients / Q000737:chemistry* / Q000493:pharmacokinetics; D007052:Ibuprofen / Q000097:blood / Q000737:chemistry* / Q000493:pharmacokinetics; D008855:Microscopy, Electron, Scanning; D020442:Poloxamer / Q000737:chemistry* / Q000493:pharmacokinetics; D051381:Rats; D012995:Solubility; D017550:Spectroscopy, Fourier Transform Infrared
D000894:Anti-Inflammatory Agents, Non-Steroidal; D005079:Excipients; D020442:Poloxamer; D007052:Ibuprofen