• Mass Spectrometry Letters
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• 제13권1호
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• pp.20-25
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• 2022

Fargesin, a tetrahydrofurofuranoid lignan isolated from Flos Magnoliae, shows anti-inflammatory, anti-oxidative, anti-allergic, and anti-hypertensive activities. To evaluate the pharmacokinetics of fargesin in mice, a sensitive, simple, and selective liquid chromatography-high resolution mass spectrometric method using electrospray ionization and parallel reaction monitoring mode was developed and validated for the quantification of fargesin in mouse plasma. Protein precipitation of 6 µL mouse plasma with methanol was used as sample clean-up procedure. The standard curve was linear over the range of 0.2-500 ng/mL in mouse plasma with the lower limit of quantification level at 0.2 ng/mL. The intra- and inter-day coefficient variations and accuracies for fargesin at four quality control concentrations including were 3.6-11.3% and 90.0-106.6%, respectively. Intravenously injected fargesin disappeared rapidly from the plasma with high clearance values (53.2-55.5 mL/min/kg) at 1, 2, and 4 mg/kg doses. Absolute bioavailability of fargesin was 4.1-9.6% after oral administration of fargesin at doses of 1, 2, and 4 mg/kg to mice.

• Journal of Ginseng Research
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• 제46권2호
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• pp.206-213
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• 2022

Ginsenoside Rb2 is an active protopanaxadiol-type saponin, widely existing in the stem and leave of ginseng. Rb2 has recently been the focus of studies for pharmaceutical properties. This paper provides an overview of the preclinical and clinical pharmacokinetics for Rb2, which exhibit poor absorption, rapid tissue distribution and slow excretion through urine. Pharmacological studies indicate a beneficial role of Rb2 in the prevention and treatment of diabetes, obesity, tumor, photoaging, virus infection and cardiovascular problems. The underlying mechanism is involved in an inhibition of oxidative stress, ROS generation, inflammation and apoptosis via regulation of various cellular signaling pathways and molecules, including AKT/SHP, MAPK, EGFR/SOX2, TGF-β1/Smad, SIRT1, GPR120/AMPK/HO-1 and NF-κB. This work would provide a new insight into the understanding and application of Rb2. However, its therapeutic effects have not been clinically evaluated. Further studies should be aimed at the clinical treatment of Rb2.

• 대한방사성의약품학회지
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• 제6권2호
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• pp.155-164
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• 2020

Polyethylene glycol (PEG) has been the most commonly used polymer for the past few decades in the field of biomedical applications due to its gold standard stealth effect. PEGylation of antibody-drug conjugates, liposomes, peptides, nanoparticles, and proteins is done to improve their pharmaceutical efficacy and pharmacokinetic properties. PEGylation of antibodies with various PEG linkers improves targeting ability by increasing the blood circulation time and thus enhances the biodistribution profiles. It also assists in minimizing the immediate capture by the reticuloendothelial system. In this review, we summarize the effect of PEG linkers in an antibody conjugation and their pharmacokinetics in the field of biomedical imaging.

• 대한수의학회지
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• 제51권4호
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• pp.253-257
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• 2011

Amikacin is a semisynthetic derivative of kanamycin and primarily active against aerobic Gram-negative-pathogens with limited activity against Gram-positive bacteria. Meager study was reported on pharmacokinetic data on multi-days administration of amikacin. Hence, pharmacokinetics study was done in five clinically healthy goats (n = 5), after intravenous bolus injection of amikacin sulfate at the dose rate of 10 mg/kg body weight daily for three consecutive days. The amikacin concentrations in plasma and pharmacokinetics-parameters were analyzed by using microbiological assay technique and noncompartmental open-model, respectively. The mean peak plasma concentrations (Mean ${\pm}$ SD) of amikacin at time zero ($Cp^{0}$) was $114.19{\pm}20.78$ and $128.67{\pm}14.37{\mu}g/mL$, on day 1st and 3rd, respectively. The mean elimination half-life ($t_{1/2}ke$) was $1.00{\pm}0.28h$ on day 1st and $1.22{\pm}0.29h$ on day 3rd. Mean of area under concentration-time curve ($AUC_{0{\rightarrow}{\infty}}$) was $158.26{\pm}60.10$ and $159.70{\pm}22.74{\mu}g.h/mL$, on day 1st and 3rd respectively. The total body clearance ($Cl_{B}$) and volume of distribution at steady state (Vdss) on day 1st and 3rd were $Cl_{B}=0.07{\pm}0.02$ and $0.06{\pm}0.01L/h.kg$ and $Vdss=0.10{\pm}0.03$ and $0.11{\pm}0.05L/kg$, respectively. No-significant difference was noted in both drug-plasma concentration and pharmacokinetics-parameters, respectively. Amikacin concentration in plasma was found higher up-to 4 h and 6 h onward on down-ward trends favour to reduce toxicity. Which also support the pharmacokinetic-pharmacodynamic way of dosing of aminoglycosides and hence, amikacin may be administered 10 mg/kg intravenously daily to treat principally Gram-negative pathogens and limitedly Gram-positive-pathogens.

• 약학회지
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• 제34권6호
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• pp.375-383
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• 1990

The pharmacokinetics of haloperidol were determined after single oral and intravenous doses in 13 male schizophrenic patients. Plasma concentrations of haloperidol(HP) and reduced haloperidol(RH) were measured by high performance liquid chromatography. Plasma concentration data obtained were analyzed by obth model dependent (one-or two exponential decay models using nonlinear regression) and model independent (AUC and first moment curve) approaches. The two methods were found to be in close results. After intravenous injections of HP in 8 patients (10 mg/man), the mean central and peripheral volume of distributions were $2.85\;{\pm}\;1.70$ and $8.09\;{\pm}\;2.10\;l/kg$, respectively, and mean steady state volume of distribution was $11.87\;{\pm}\;3.21\;l/kg$. Mean clearance, MRT and elimination half life were $12.39\;{\pm}\;3.25\;ml/min/kg$, $925.10\;{\pm}\;166.79\;min$ and $676.35\;{\pm}\;126.45\;min$, respectively. After oral administrations of HP in 5 patients, mean peak time and peak concentration were $217.63\;{\pm}\;61.60\;min$ and $9.77\;{\pm}\;2.92\;ng/ml$, respectively. Mean MRT and elimination half life were $1112.23\;{\pm}\;131.73\;min$ and $724.02\;{\pm}\;120.03\;min$, respectively, and these parameters were not significantly different from those of intravenous injection of HP. Absolute bioavailability of HP oral product was found to be about 44%. The profiles of plasma RH concentration-time curves after oral or intravenous doses of HP were similar. Also it was found that the elimination rate of RH was solwer than that of HP by comparing the slopes of plasma concentration-time curves of HP and RH.

• 생명과학회지
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• 제26권1호
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• pp.123-128
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• 2016

본 연구의 최종 목표는 한방제제인 심적환과 심혈관계 양방 치료제인 cilostazol과 병용 투여 효과에 대한 포괄적이고 통합의학 측면에서 정확한 정보를 얻는 것이다. Cilostazol은 말초 동맥질환 치료제로 개발 된 항 혈소판 및 혈관확장제이다. 사이클릭 AMP protein kinase A를 활성 시켜 세포내 사이클릭 AMP (cAMP) 증가를 통하여 내피세포의 NO생산을 활성화 시킨다. 심적환을 단 회 또는 반복 투여 후 cilostazol의 약물 동태학적 효과를 평가하기 위하여 순수한 증류수 단회 용량과 증류수에 심적환 콜로이드 현탁액을 각각 대조군과 시험군에 투여 하여 30분 후, 두 그룹에 cilostazol를 투여하였다. 혈청은 cilostazol 약물 투여 30분 전에 수집 하였으며, cilostazol 약물 처리 후 0.25, 0.5, 0.45 및 1, 2, 4, 6, 8, 24시간 후에 각각 수집 하였다. 그 다음 실험군과 및 테스트 그룹 사이에 실로 스타 졸에서 관찰 된 약동학 적 변화를 평가 하였다. 통계적으로 유의 한 차이는 심적관 단독 투여와 반복투여군 그룹의 약물 동태 학에서 관찰되지 않았다. 이러한 연구 결과는 만성 질환 환자에서 한약제인 심적환의 투여는 cilostazol의 약동학에 영향을 미치지 않았음을 보여 주었다. 본 연구에서 얻어진 결과는 만성 혈관질환 환자에서 심적환과 cilostazol의 병용 투여를 제안하며 두 약물간의 잠재적 인 약물 상호 작용에 대한 cilostazol의 생체 이용률에 영향을 미치지 않을 것이라 판단된다.

• 한국미생물생명공학회소식지:생물산업
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• 제15권3호
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• pp.16-19
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• 2002

• 한국독성학회:학술대회논문집
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• 한국독성학회 2006년도 춘계학술대회
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• pp.93-102
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• 2006

• 생약학회지
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• 제2권1호
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• pp.49-51
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• 1971

• Journal of Pharmaceutical Investigation
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• 제17권4호
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• pp.217-232
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• 1987