Development of novel ibuprofen-loaded solid dispersion with improved bioavailability using aqueous solution.
To develop a novel ibuprofen-loaded solid dispersion with enhanced bioavailability, various ibuprofen-loaded solid dispersions were prepared with water, HPMC and poloxamer. The effect of HPMC and poloxamer on aqueous solubility of ibuprofen was investigated. The dissolution and bioavailability of solid dispersion in rats were then evaluated compared to ibuprofen powder. When the amount of carrier increased with a decreased in HPMC/poloxamer ratio, the aqueous solubility of ibuprofen was elevated. The solid dispersion composed of ibuprofen/HPMC/poloxamer at the weight ratio of 10:3:2 improved the drug solubility approximately 4 fold. It gave significantly higher initial plasma concentration, AUC and Cmax of drug than did ibuprofen powder in rats. The solid dispersion improved the bioavailability of drug about 4-fold compared to ibuprofen powder. Thus, this ibuprofen-loaded solid dispersion with water, HPMC and poloxamer was a more effective oral dosage form for improving the bioavailability of poor water-soluble ibuprofen.
Park
Young-Joon
YJ
College of Pharmacy, Yeungnam University, Gyongsan, Korea.
Kwon
Ram
R
Quan
Qi Zhe
QZ
Oh
Dong Hoon
DH
Kim
Jong Oh
JO
Hwang
Ma Ro
MR
Koo
Yoon Bon
YB
Woo
Jong Soo
JS
Yong
Chul Soon
CS
Choi
Han-Gon
HG
D000284:Administration, Oral; D000818:Animals; D000894:Anti-Inflammatory Agents, Non-Steroidal / Q000008:administration & dosage / Q000097:blood / Q000737:chemistry / Q000493:pharmacokinetics*; D001682:Biological Availability; D002626:Chemistry, Pharmaceutical; D004304:Dosage Forms; D004337:Drug Carriers; D065347:Hypromellose Derivatives; D007052:Ibuprofen / Q000008:administration & dosage / Q000097:blood / Q000737:chemistry / Q000493:pharmacokinetics*; D008297:Male; D008747:Methylcellulose / Q000031:analogs & derivatives / Q000737:chemistry; D020442:Poloxamer / Q000737:chemistry; D011208:Powders; D051381:Rats; D017207:Rats, Sprague-Dawley; D012995:Solubility; D014867:Water / Q000737:chemistry
D000894:Anti-Inflammatory Agents, Non-Steroidal; D004304:Dosage Forms; D004337:Drug Carriers; D011208:Powders; D014867:Water; D020442:Poloxamer; D065347:Hypromellose Derivatives; D008747:Methylcellulose; D007052:Ibuprofen