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ABSTRACT: Cilostazol is frequently used to treat and prevent thrombosis in Korean patients.
We performed the pharmacokinetic and correlation analysis of cilostazol in Korean healthy subjects. A total of male 78 volunteers was subjected to three separate bioequivalence studies in which 100 mg of cilostazol was administered. AUC, t(1/2), and C(max) were 12,100 ± 4,880 ng×h/ ml, 11.1 ± 4.4 hours, and 827 ± 361 ng/ml, respectively.
ALT was positively correlated with age and C(max) was positively correlated with AUC, but negatively correlated with body weight.
We suggest that the unique pharmacokinetic parameters and interrelationship can help to understand the pharmacokinetics of cilostazol in Korean subjects.
International journal of clinical pharmacology and therapeutics 05/2012; 50(5):345-8. · 1.18 Impact Factor
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ABSTRACT: A new controlled-release formulation of aceclofenac 200 mg (Clanza CR®) developed by Korea United Pharm., Inc., South Korea, for once-daily (od) dosing provides biphasic aceclofenac release consisting of immediate release of 85 mg followed by sustained release of 115 mg. Food has been known to affect the rate and extent of absorption of several drugs, in both immediate-release and controlled-release formulations.
The aim of this study was to evaluate the relative bioavailability of a new controlled-release formulation of aceclofenac (200 mg od; Clanza CR®) in comparison with immediate-release aceclofenac (100 mg twice daily [bid], Airtal®) and to assess the effect of food on the pharmacokinetics of the new controlled-release aceclofenac formulation.
This study was designed as a randomized, open-label, three treatment-period, crossover, single-centre study with a 1-week washout in 41 healthy adults. The three treatments consisted of immediate-release aceclofenac 100 mg bid administered under fasting conditions; controlled-release aceclofenac 200 mg od administered under fasting conditions; and controlled-release aceclofenac 200 mg od administered immediately after a standardized high-fat breakfast. Plasma concentrations of aceclofenac were determined using a high-performance liquid chromatography method.
In the fasted state, the 90% confidence intervals (CIs) of the least squares geometric mean ratios (GMRs) for the area under the plasma concentration-time curve from time zero to 24 hours (AUC(24)) and the peak plasma concentration (C(max)) of aceclofenac for the controlled-release and immediate-release formulations of aceclofenac were all within the bioequivalence criteria range of 0.8-1.25. The 90% CIs of the GMRs for the AUC(24) and C(max) of aceclofenac for the controlled-release formulation of aceclofenac in the fed and fasted states were also within the bioequivalence range. Both aceclofenac formulations were well tolerated in all subjects, and no serious adverse effects were observed.
The results demonstrate that controlled-release aceclofenac 200 mg is equivalent to immediate-release aceclofenac 100 mg when administered at the same total daily dose. Additionally, the bioavailability of controlled-release aceclofenac was not affected by high-fat foods.
Clinical Drug Investigation 12/2011; 32(2):111-9. · 1.82 Impact Factor
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ABSTRACT: A method for the determination of carvedilol in human plasma was developed using a high-performance liq-uid chromatography with tandem mass spectrometer (HPLC-MS/MS). Plasma samples were deproteinized using acetonitrile and the supernatant was directly injected onto the HPLC column without any preparative steps. Chromatography was performed on a reversed-phase (C 18) column with isocratic mobile phase for 2 min. The calibration curve was linear over the range of 2 to100 ng/ml (R 2 > 0.9998) and the lower limit of quantitation (LLOQ) was 2 ng/ml. This method showed acceptable precision and accuracy, good recovery from the plasma matrix, and stability during the analytical procedures. When its application to the bio-equivalence test of two carvedilol 25 mg tablet formulations in male healthy 28 volunteers, this validated analysis method was appropriate resulting in the bioequivalence of two formulations: no statistically signifi-cant difference was observed between the logarithmic transformed area under curve (AUC) and maximum plasma concentration (C max) values of the two formulations. The 90% confidence interval for the ratio of the above mentioned two parameters were within the bioequivalence limit of 0.80-1.25. These results suggested that the HPLC-MS/MS analysis method developed was suitable for the carvedilol analysis in human plasma.
American Journal of Analytical Chemistry. 01/2010; 1:135-143.
