• 약학회지
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• 제59권3호
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• pp.92-97
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• 2015

KIOM-MA128 is a novel Korean herbal medicine with anti-atopic, anti-inflammatory and anti-asthmatic effects. This article presents the first pharmacokinetic study on KIOM-MA128. The purpose of this study was to characterize a pharmacokinetic characteristic of matrine, a potential marker of KIOM-MA128, in rats using population pharmacokinetic model. 1, 2 and 8 g/kg of KIOM-MA128 were administered to rats orally and plasma concentrations of matrine was determined by HPLC-MS/MS. Non-compartmental analysis (NCA) was performed using Phoenix$^{(R)}$ and pharmacokinetic model was built using NONMEM$^{(R)}$. This model was validated with internal validation which is visual predictive check (VPC) and bootstrap. The NCA result of matrine showed that $C_{max}$ was 294.24, 552.22 and 868.65 ng/ml, $AUC_{inf}$ was 1273.05, 2724.76 and $9743.25ng{\cdot}hr/ml$ and $T_{max}$ was 1, 1.3 and 2.3 hr for the doses of 1, 2, and 8 g/kg, respectively. The rat plasma concentrations were described very well with one-compartment model. Pharmacokinetic model for matrine was successfully developed and evaluated. Finally, our model is helpful to understand pharmacokinetic characteristic of KIOM-MA128.

• 한국임상수의학회지
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• 제23권2호
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• pp.114-118
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• 2006

본 연구는 플로르페니콜을 체중당 20mg 용량으로 경구 및 정맥내로 투여한 후 플로르페니콜 및 그 대사체인 플로르페니콜 아민의 생체이용율 및 약물동태학적 분석을 육계에서 실시하였다. 혈청내의 플로르페니콜 및 플로르페니콜 아민의 정량은 액체크로마토그래프/질량분석기를 사용하였으며, 경구 및 정맥내 투여후 혈청 농도-시간 자료는 non-compartmental analysis를 이용하여 분석하였다. 플로르페니콜의 정맥주사 후 청소율 및 소실반감기는 각각 $0.74{\pm}0.25L/kg/h$와 $1.15{\pm}1.06h$로 나타났으며, 정상상태 분포용적은 $1.16{\pm}0.19L/kg$으로 정맥주사후 빠른 체내 분포와 소실을 나타냈다. 플로르페니콜의 경구투여 후 혈중최고농도 ($8.18{\pm}0.97{\mu}g/mL$)는 $1.33{\pm}0.29h$에 나타났다. 소실반감기는 $1.24{\pm}0.64h$이었으며, 경구생체이용율은 약 75.46%로 나타났다. 플로르페니콜의 주요 대사체인 플로르페니콜 아민은 정맥 및 경구투여한 모든 육계에서 검출되었다. 플로르페니콜 아민의 혈중최고농도는 정맥 및 경구투여 후 각각 $1.88{\pm}0.39{\mu}g/mL$과 $2.64{\pm}1.39{\mu}g/mL$로 $0.16{\pm}0.19h$ 및 $1.61{\pm}1.02h$에 관찰되었다. 플로르페니콜 아민은 정맥 및 경구 투여후 각각 $1.88{\pm}0.39$ and $2.64{\pm}1.39h$로 그 모약인 플로프페니콜보다 다소 느리게 소실되었다.

• 한국임상약학회지
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• 제12권2호
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• pp.71-75
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• 2002

This study was carried out to compare the bioavailability of $Ceclex^{(R)}$ (test drug, cefaclor 250 mg/capsule) with that of $Ceclor^{(R)}$ (reference drug) and to estimate the pharmacokinetic parameters of cefaclor in healthy Korean adult. The bioavailability was examined on 20 healthy volunteers who received a single dose (250 mg) of each drug in the fasting state in a randomized balanced 2-way crossover design. After dosing, blood samples were collected for a period of 6hours. Plasma concentrations of cefaclor were determined using HPLC with UV detection. The pharmacokinetic parameters $(AUC_{0-6hr},\;C_{max},\;T_{max},\;AUC_{int},\;K_e,\;t_{1/2},\;Vd)$ F, and CL/F) were calculated with non-compartmental pharmacokinetic analysis. The ANOVA test was utilized for the statistical analysis of the $T_{max},\;log-transformed\;AUC_{0-6hr}\;log-transformed\;C_{max},\;t_{l/2},\;V_d/F$, and CL/F. The ratios of geometric means of AUC0-6hr and $C_{max}$ between test drug and reference drug were $103.2\%\;(6.74\;{\mu}g{\cdot}hr/ml\;vs\;6.53{\pm}g{\cdot}hr/ml)\;and\;100.4\%\;(4.85\;{\mu}g\ml\;vs\;4.82\;{\mu}g/ml)$, respectively. The $T_{max}$ of test drug and reference drug were $0.9\pm0.38\;hr\;and\;0.83\pm0.34$ hrs, respectively. The $90\%$ confidence intervals of mean difference of logarithmic transformed $AUC_{0-6h},\;and\;C_{max}$ were log $0.98{\sim}log$ 1.08 and log $0.88{\sim}log1.15$, respectively. It shows that the bioavailability of test drug is equivalent with that of reference drug. The estimated half-life of this study was longer $(1.21\pm0.27\;hrs\;vs\;0.5-1\;hr)$, the Vd/F was larger $(68.89\pm25.72L$ vs 24.9L), and the CL/F was higher $(38.62\pm7.09\;L/hr$ vs 24.9 L/hr) than the previously reported values.

• Translational and Clinical Pharmacology
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• 제25권3호
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• pp.153-156
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• 2017

UI14SDF100CW is a chewable tablet of sildenafil citrate, which was developed to improve compliance through convenience of administration. The purpose of this study was to compare the pharmacokinetic (PK) properties of sildenafil citrate chewable tablets (UI14SDF100CW) and conventional sildenafil citrate film-coated tablets ($Viagra^{(R)}$, Pfizer). A randomized, open-label, single dose, two-treatment, two-period, two-way crossover study was conducted in 60 healthy male volunteers. In each period, the subjects received a single oral dose of UI14SDF100CW or $Viagra^{(R)}$ (both tablets contain 140.45 mg of sildenafil citrate, which is equivalent to 100 mg of sildenafil). Serial blood samples were collected up to 24 h post-dose for PK analysis. The plasma concentration of sildenafil was determined using a validated HPLC-MS/MS assay. PK parameters of sildenafil were calculated using non-compartmental methods. The plasma concentration-time profiles of sildenafil in both formulations were similar. For UI14SDF100CW, the $C_{max}$ and $AUC_{last}$ of sildenafil were $1068.69{\pm}458.25$ (mean${\pm}$standard deviation) mg/L and $3580.59{\pm}1680.29h{\cdot}mg/L$, and the corresponding values for $Viagra^{(R)}$ were $1146.84{\pm}501.70mg/L$ and $3406.35{\pm}1452.31h{\cdot}mg/L$, respectively. The geometric mean ratios (90% confidence intervals) of UI14SDF100CW to $Viagra^{(R)}$ for $C_{max}$ and $AUC_{last}$ were 0.933 (0.853-1.021) and 1.034 (0.969-1.108), respectively, which met the bioequivalence criteria of Korean regulatory agency. In conclusion, UI14SDF100CW and $Viagra^{(R)}$ showed similar PK properties. Therefore, UI14SDF100CW can be an alternative to sildenafil for the treatment of erectile dysfunction, providing better compliance.