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흰쥐에서 이부프로펜 리신염의 물리화학적 특성 및 약물동태에 관한 평가
신대환(Dae Hwan Shin),김시현(Si Hyun Kim),박승혁(Seong Hyeok Park),김태성(Tai Sung Kim),한건(Kun Han),정연복(Youn Bok Chung),조한준(Han Jun Jo) 大韓藥學會 2011 약학회지 Vol.55 No.3
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 (CLt) 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 (Cmax) significantly ealier and higher than IB. Time to reach peak concentration (Tmax) 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 (ka) 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.
박승혁, 정성우, 정연복 충북대학교 약품자원개발연구소 2013 약학논문집 Vol.28 No.-
The purpose of the present study was to evaluate the dissolution of the enteric-coated tablets of acetyl-L-carnitine, and to investigate its pharmacokinetics at the dose of 500 mg/kg in human subjects. For this purpose, we developed convenient HPLC method to measure the acetyl-L-carnitine concentration in the biological fluids. The low detection limit was 0.1 ug/mL using a HPLC system of UV detection. The linearity of the assay was determined over the concentration range of 0.1-0.8 ug/mL. Precision, exprssed as cv%, was less than 3.3% for the endogeneous acetyl-L-carnitine in the plasma. Dissolution rate of acetyl-L-carnitine tablets in pH 1.2 buffer was almost 0%, whereas that in pH 6.8 buffer after 90 min was over 98.5%. The parmacokinetic parameters such as AUC, Cmax and Tmax of acetyl-L-carnitin were claculated after its oral administration at the dose of 500 mg/kg. In conclusion, the tablets prepared in the present study was useful for the enteric-coated tablets of acetyl-L-carnitine.
박승혁, 정성우, 정연복 충북대학교 약품자원개발연구소 2013 약학논문집 Vol.28 No.-
The purpose of the present study was to investigate the pharmacokinetics of DIOS-1, a potential antidote of dioxins, in rats. We also investigated the administration routes such as oral, intramuscular and subcutaneous route. For this purpose, HPLC analysis method usig UV detector was developed. the plasma concentration of DIOS-1 was disappeared by 20 min after its i.v. administration at a dose of 10 mg/kg. The half lives at α-phase and β-phase were 6.47 min and 29.6 min, respectively. The plasma peak concentration (Cmax) of DIOS-1 after its i.m. ofr s.c. administration at the dose 10mg/kg was 10 ug/ml (tmax=10 min). The absorption rate constant was comparable between i.m. and s.c. route. The bioavailability (79.0%) of DIOS-1 after s.c. administration was significantly larger than that (58.9%) of i.m. route. Thus, s.c. route was considered to be useful compared with i.m. route for the DIOS-1 administration. On the other hand, the plasm concentration of DIOS-1 was not detected after its oral administration at the dose of 100 mg/kg, suggesting that DIOS-1 may not be absorbed in oral route. On the basis of the simulation results, the accumulation in the body was not demonstrated with DIOS-1 s.c administration at the dose of 10 mg/kg for the dosing interval of 24 hr. In conclusion, s.c. route was considered to be useful for the DIOS-1 administration.