• Bulletin of the Korean Chemical Society
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• 제25권1호
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• pp.109-114
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• 2004

A sensitive method for quantitation of glimepiride in human plasma has been established using liquid chromatography-electrospray ionization tandem mass spectrometry (LC-ESI/MS/MS). Glipizide was used as an internal standard. Glimepiride and internal standard in plasma sample was extracted using diethyl etherethyl acetate (1 : 1). A centrifuged upper layer was then evaporated and reconstituted with the mobile phase of acetonitrile-5 mM ammonium acetate (60:40, pH 3.0). The reconstituted samples were injected into a $C_{18}$ reversed-phase column. Using MS/MS in the multiple reaction monitoring (MRM) mode, glimepiride and glipizide were detected without severe interference from human plasma matrix. Glimepiride produced a protonated precursor ion ([M+H]$^+$) at m/z 491 and a corresponding product ion at m/z 352. And the internal standard produced a protonated precursor ion ([M+H]]$^+$) at m/z 446 and a corresponding product ion at m/z 321. Detection of glimepiride in human plasma by the LC-ESI/MS/MS method was accurate and precise with a quantitation limit of 0.1 ng/mL. The validation, reproducibility, stability, and recovery of the method were evaluated. The method has been successfully applied to pharmacokinetic studies of glimepiride in human plasma.

• Journal of Pharmaceutical Investigation
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• 제37권2호
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• pp.79-84
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• 2007

This study was aimed to establish analytical method of Bi to develop a guideline of the bioequivalence test of tripotassium dicitrato bismuthate (TDB). For this purpose, a simple, specific and sensitive inductively coupled plasma-mass spectrometry (ICP/MS) method were developed and validated in human plasma. Various concentrations of bismuth standard solution (0-25ng/mL) were prepared with distilled water and human blank plasma. To 10mL of the volumetric flasks, 2mL of blank plasma was added with 8ml of distilled water. Bi standard solution was added to prepare the calibration samples and injected into ICP-MS. The plasma samples obtained from volunteers given 3 tablets of bismuth (total 900mg as TDB) were analyzed as described above. As a result, the coefficients of variation were <20% in quantitation limit (0.2 ng/mL) and <15% at the rest of concentrations. The stability test by repeated freezing-thawing cycles showed that the samples were stable only for 24hr. The stability tested for samples with a short-term period of storage at room temperature and pre-treatment prior to the analysis showed very stable over 24hr. In 8 healthy Korean subjects received Denol tablets at the dose of 900mg bismuth, AUC, $C_{max},\;T_{max}$ and half-life $(t_{1/2})$ were determined to be $198.33{\pm}173.78 ng{\cdot}hr/mL,\;64.48{\pm}27.06 ng/mL,\;0.52{\pm}0.21 hr,\;and\;5.15{\pm}2.67 hr$, respectively, from the plasma bismuth concentration-time curves. In conclusion, the method was suitable for the determination of bismuth in human plasma samples and could be applied to bioequivalence test of bismuth tablet.

• 한국독성학회:학술대회논문집
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• 한국독성학회 2002년도 Current Trends in Toxicological Sciences
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• pp.93-93
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• 2002

Oxidative stress has been associated with a number of diseases in humans. Among the sources that can generate oxidative stress, it has been reported that iron can generate reactive oxygen species (ROS) with thiol. In iron overload state, increased thiol levels in plasma appeared to be associated with human mortality.(omitted)

• 대한약학회:학술대회논문집
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• 대한약학회 2003년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.1
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• pp.281.1-281.1
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• 2003

Purpose. The purpose of this study was to develop and validate sensitive and specific analytical method for determinination of simvastatin in human plasma by the column-switching high-performance liquid chromatography (HPLC) system with UV detection. Methods. Simvastatin and internal standard were extracted into diethyl ether from plasma. (omitted)

• 대한약학회:학술대회논문집
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• 대한약학회 2003년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.1
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• pp.283.2-283.2
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• 2003

This study established a highly sensitive novel quantification method for detecting felodipine in human plasma using LC-MS/MS. The mobile phase used after degassing was composed of 1 mM ammonium acetate and acetonitrile (20:80, pH 6.0), with flow rate of 200 uL/min. One mL plasma were pipetted into glass tubes and spiked with 0.1 mL of internal standard solution. (omitted)

• 대한약학회:학술대회논문집
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• 대한약학회 2003년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.1
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• pp.282.1-282.1
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• 2003

This study established a sensitive novel Quantification method for detecting glimepiride in human plasma using LC-MS/MS for pharmacokinetic studies. The mobile phase used after degassing was composed of 10 mM ammonium acetate and acetonitrile (20:80, pH 3.0), with flow rate of 200uL/min. One mL plasma were pipetted into glass tubes and spiked with 0.1 mL of internal standard solution. (omitted)

• 대한약학회:학술대회논문집
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• 대한약학회 2003년도 Proceedings of the Convention of the Pharmaceutical Society of Korea Vol.1
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• pp.284.2-284.2
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• 2003

Using a column-switching technique. highly sensitive and selective semi-micro high-performance liquid chromatographic (HPLC) method has been developed for the determination of baclofen in human plasma. Following precipitation of plasma sample containing baclofen with zinc sulfate-acetonitrile, samples were directly injected on to the system. (omitted)

• Biomolecules & Therapeutics
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• 제4권2호
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• pp.122-126
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• 1996

In vitro inhibitory effect of aspalatone ((3-(2-methyl-4-pyronyl)]-2-acetyloxybenzoate) on collagen-, ADP-, and epinephrine-induced platelet aggregation in human platelet rich plasma (PRP) was compared with the effects of reference drugs (acetylsalicylic acid, cilostazol and ticlopidine). Aspalatone inhibited time and dose dependently human platelet aggregation induced by collagen; relative potency was in the order of cilostazol>acetylsalicylic acid>aspalatone>ticlopidine. Aspalatone, like acetylsalicylic acid, potently inhibited only the secondary phase of ADP-and epinephrine-induced aggregation. Thromboxane $B^2$ production evoked by collagen in human PRP was inhibited significantly and concentration-dependently by aspalatone and acetylsalicylic acid. These results were in agreement with the earlier studies in which the antiplatelet action of aspalatone was indicated to be due to the inhibition of platelet cyclooxygenase activity (Han et al., Arzneim. Forsch./Drug Res. 44(II), 1122, 1994; Suh and Han, Yakhak Hoeji 39, 565, 1995). In addition, the inhibitory activity of aspalatone on the platelet aggregation appears to be inversely related to the rate of nonspecific deacetylation of the drug in plasma.

• 분석과학
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• 제25권1호
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• pp.19-24
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• 2012

LC-MS/MS를 이용하여 혈장과 소변 중 에르타페넴의 신속하고 정확한 분석법을 개발하고 이 분석법에 대한 검증을 수행하였다. 혈장과 소변 분석을 위하여 내부 표준 물질인 세프타지딤을 첨가한 후 메탄올로 단백질을 침전시키고, 그 상층액을 취하여 메탄올로 희석하여 LC-MS/MS로 분석하였다. MS/MS의 MRM (multiple reaction monitoring) 방법을 이용하여 혈장과 소변 중의 에르타페넴을 어떠한 분석의 방해물 없이 선택적으로 검출할 수 있었다. 혈장 중 에르타페넴의 표준 검량선은 1~100 ${\mu}g/mL$의 농도 범위에서 우수한 직선성($r^2$ = 0.9996)을 보였으며, 일내, 일간 재현성은 변동계수 8.9% 이하, 정확성은 97.2~106.2% 이었다. 또한 소변 중 에르타페넴의 분석 결과는 좋은 상관관계($r^2$ = 0.9992)를 보였고, 일내, 일간 재현성이 변동계수 7.2% 이하, 정확성이 97.9~111.6% 이었다. 결과적으로 에르타페넴의 약동학 연구에 적용되기에 충분한 감도와 특이성, 직선성, 정밀성 및 정확성을 가지고 있음을 확인하였다.

• IMMUNE NETWORK
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• 제4권3호
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• pp.176-183
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• 2004

Background: Human seminal plasma (HSP)-induced hypersensitivity is one of the serious complications with sexual intercourse. The clinical manifestations of HSP-induced hypersensitivity may be related to the release of vasoactive mediators from mast cell induced by HSP. It has recently been reported that HSP modulates immune systems and induces mast cell degranulation and histamine release from rat peritoneal mast cells (RPMC). Ketotifen and disodium cromoglycate (DSCG), anti-asthmatic and anti-allergic drugs, have a role of mast cell stabilization and inhibit mast cell-induced leukocyte rolling and adhesion. But the inhibitory agents of HSP-induced mast cell activation are unknown. This study was performed to investigate the effects of DSCG and ketotifen on the HSP-induced mast cell activation. Methods: For this, influences of DSCG and ketotifen on the human seminal plasma-induced degranulation, histamine release and morphological changes of RPMC were observed. Results: The mast cell degranulation and histamine release of RPMC by HSP were induced in a dose-dependent fashion. The HSP-induced cytomorphological changes such as swelling, intracellular vacoules, and interrupted cell boundary were significantly inhibited by pretreatment with DSCG or ketotifen. DSCG and Ketotifen inhibited the HSP-induced degranulation and histamine release from RPMC. Conclusion: From the above results, it is suggested that DSCG and ketotifen have a inhibitory effect of the HSP-induced mast cell activation. DSCG and ketotifen may be used for treatment of HSP-induced hypersensitivity.