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Physicochemical Characteristics and Pharmacokintics of Ibuprofen Lysine Salts  

Shin, Dae-Hwan (CBITRC, College of Pharmacy, Chungbuk National University)
Kim, Tai-Sung (CBITRC, College of Pharmacy, Chungbuk National University)
Park, Seong-Hyeok (CBITRC, College of Pharmacy, Chungbuk National University)
Kim, Si-Hyun (CBITRC, College of Pharmacy, Chungbuk National University)
Jo, Han-Jun (CBITRC, College of Pharmacy, Chungbuk National University)
Han, Kun (CBITRC, College of Pharmacy, Chungbuk National University)
Chung, Youn-Bok (CBITRC, College of Pharmacy, Chungbuk National University)
Publication Information
YAKHAK HOEJI / v.55, no.3, 2011 , pp. 260-266 More about this Journal
Abstract
Two types of water soluble lysine salts of ibuprofen were prepared and evaluated. Physicochemical properties for ibuprofen-l-lysinate (IBL-l), ibuprofen-dl-lysinate (IBL-dl) and ibuprofen (IB) were studied on melting point, specific ratation, UV spectra and $^1H$-NMR spectra. There were not differences between IBL-dl and IBL-l in UV spectra and $^1H$-NMR spectra. The pharmacokinetic parameters of IB were compared to those of its lysine salts (IBL-l and IBL-dl) after i.v. or oral administration at the dose of 50 mg/kg (calculated as IB). Total body clearance ($CL_t$) and area under the plasma concentration-time curve (AUC) were not different between IB group and IBL groups after i.v. administration. On the other hand, IBL-l and IBL-dl produced peak plasma concentrations ($C_{max}$) significantly ealier and higher than IB. Time to reach peak concentration ($T_{max}$) after IBL administration was lower than that after IB administration. There was no difference in AUC across all different groups (IB, IBL-l and IBL-dl) after oral administration. However, absorption rate constant ($k_a$) of IBL-l and IBL-dl were significantly increased than that of IB. These results indicated that the administration of IBL-l and IBL-dl may be advantageous if rapid and reliable onset of pain relief is required.
Keywords
ibuprofen; lysinate; pharmacokinetics; physicochemical properties;
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