Enhanced dissolution of ibuprofen using solid dispersion with poloxamer 407.
To improve its dissolution, ibuprofen solid dispersions (SDs) were prepared, characterized by scanning electron microscopy (SEM), differential scanning calorimetry (DSC), and Fourier transform infrared spectroscopy (FTIR), and evaluated for solubility, and in-vitro ibuprofen release. Loss of individual surface properties during melting and re-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 drug-polymer interactions. FTIR spectra showed the presence of drug crystalline in SDs. The effect of improved dissolution on the oral absorption of ibuprofen in rats was also studied. Quicker release of ibuprofen from SDs in rat intestine resulted in a significant increase in AUC and C(max), and a significant decrease in T(max) over pure ibuprofen. Comparison of the enhanced solubility, dissolution, AUC, and C(max) of ibuprofen from different poloxamers suggested that the preparation of ibuprofen SDs using P 407 as a meltable hydrophilic polymer carrier could be a promising approach to improve its solubility, dissolution and absorption rate.
Newa
Madhuri
M
College of Pharmacy, Yeungnam University, Gyongsan 712-749, Korea.
Bhandari
Krishna Hari
KH
Oh
Dong Hoon
DH
Kim
Young Ran
YR
Sung
Joon Ho
JH
Kim
Jong Oh
JO
Woo
Jong Soo
JS
Choi
Han Gon
HG
Yong
Chul Soon
CS
D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000008:administration & dosage / Q000737:chemistry* / Q000493:pharmacokinetics; D002152:Calorimetry, Differential Scanning; D002626:Chemistry, Pharmaceutical; D005079:Excipients; D007052:Ibuprofen / Q000008:administration & dosage / Q000737:chemistry* / Q000493:pharmacokinetics; D008297:Male; D008855:Microscopy, Electron, Scanning; D010316:Particle Size; D020442:Poloxamer / Q000737:chemistry*; D051381:Rats; D017207:Rats, Sprague-Dawley; D012995:Solubility; D017550:Spectroscopy, Fourier Transform Infrared
D000894:Anti-Inflammatory Agents, Non-Steroidal; D005079:Excipients; D020442:Poloxamer; D007052:Ibuprofen