Enhancement of solubility, dissolution and bioavailability of ibuprofen in solid dispersion systems.
To improve its solubility, dissolution, and bioavailability; Ibuprofen-polyethylene glycol 8000 (PEG 8000) solid dispersions (SDs) with different drug loadings were prepared, characterized by scanning electron microscopy (SEM) and differential scanning calorimetry (DSC), and evaluated for solubility, in-vitro release, and oral bioavailability of ibuprofen in rats. Loss of 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 drug-polymer interactions. 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. Preliminary results of this study suggested that the preparation of ibuprofen SDs using PEG 8000 as a meltable hydrophilic polymer carrier could be a promising approach to improve solubility, dissolution and bioavailability of ibuprofen.
Newa
Madhuri
M
College of Pharmacy, Yeungnam University, Kyungsan, Kyungbuk, South Korea.
Bhandari
Krishna Hari
KH
Kim
Jong Oh
JO
Im
Jong Seob
JS
Kim
Jung Ae
JA
Yoo
Bong Kyu
BK
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; D001682:Biological Availability; D002152:Calorimetry, Differential Scanning; D002626:Chemistry, Pharmaceutical; D005079:Excipients; D007052:Ibuprofen / Q000008:administration & dosage* / Q000737:chemistry / Q000493:pharmacokinetics; D008297:Male; D008855:Microscopy, Electron, Scanning; D011092:Polyethylene Glycols; D051381:Rats; D017207:Rats, Sprague-Dawley; D012995:Solubility; D013501:Surface-Active Agents
D000894:Anti-Inflammatory Agents, Non-Steroidal; D005079:Excipients; D013501:Surface-Active Agents; D011092:Polyethylene Glycols; D007052:Ibuprofen