• Title/Summary/Keyword: high performance liquid chromatography

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Pharmacokinetic analysis for the development of new potent anti-HIV-1 agents, the KR-V series (새로운 항HIV-1제, KR-V series의 개발을 위한 약물동태연구)

  • Lee, Young-mi;Kim, Jin-suk;Han, Sang-seop;Shin, Ho-chul
    • Korean Journal of Veterinary Research
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    • v.40 no.3
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    • pp.471-478
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    • 2000
  • The pharmacokinetic properties of KR-V compounds, recently developed as new anti-HIV agents, were studied after i.v. and p.o. administration in rats. The concentrations of the KR-V series were determined in rat plasma using an high-performance liquid chromatography (HPLC)-UV detection system. Of the 19 KR-V compounds investigated in the present study, only KR-V 3, 10, 14, 16 and 18-1 showed oral bioavailability. The plasma concentration-time data could be adequately described by an one-compartment open model. In the i.v. kinetic study (10mg/kg), the CLt of KR-V 3, 10, 14 and 16 (>4L/hr/kg) were significantly higher than that of KR-V 18-1 (1.1 L/hr/kg). The AUC of KR-V 18-1 was greater ($8.97{\mu}g{\cdot}hr/ml$) than that of the other compounds, but the Vd (0.58 L/kg) was lower. In the p.o. kinetic study (50mg/kg), although the t-1/2 of KR-V 18-1 was shorter than that of the other compounds, the AUC ($3.659{\mu}g{\cdot}hr/ml)$ and $C_{max}(1.891{\mu}g/ml$) were markedly higher. In a seperated in vitro experiment, only KR-V 18-1, of the 5 compounds with bioavailibility, exhibits potent activity against HIV-1 mutant strains. Therefore, KR-V 18-1 is expected to become a new potent anti-AIDS drug candidate/lead compound.

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EFFECT OF PHOSPHORIC ACID CONCENTRATION ON THE DIFFUSION OF HEMA THROUGH DENTIN (상아질을 통한 HEMA의 확산에 인산농도가 미치는 영향)

  • Yoon, Mi-Ran;Lee, Kwang-Won;Park, Soo-Joung
    • Restorative Dentistry and Endodontics
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    • v.24 no.1
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    • pp.147-155
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    • 1999
  • The purpose of this study was to investigate the effect of phosphoric acid concentration on the movement of 2-hydroxyethylmethacrylate(HEMA) from bonding resin - resin composite combination through dentin in vitro. Freshly extracted human third molar teeth were divided into four groups each of 10 teeth. A closed chamber with 1 ml distilled water was attached to the CEJ of each tooth. An occlusal cavity of 4mm diameter & remaining dentin thickness of 1.0-1.5mm was prepared in each tooth. Dentin was treated with 10% phosphoric acid gel for 15 seconds. 32% phosphoric acid gel for 15 seconds, or with 35% phosphoric acid gel for 15 seconds. A control group not treated with acid gel was also prepared. The cavities were rinsed, dried and then treated with the HEMA-containing All-Bond 2 primer & bonding resin which was light-cured for 10 seconds. The cavities were then restored with Z100 composite resin(shade:A3.5:3M Dent. Prod. USA) & light cured for 30 seconds. Water samples were retrieved from the chambers over a time course (4.32, 14.4, 43.2, 144 & 432 minutes ; 1, 3 & 10 days) and analyzed by high performance liquid chromatography. The results were as follows. 1. HEMA was detected in the pulp chambers of all teeth from 4.32 minutes after resin placement The highest rate of release was in the first sample period (0-4.32 min) & rate of release declined exponentially thereafter. 2. No significant differences were found for mean release rate for HEMA over a time course among the four groups (p>0.05). 3. The diffusion rate was significantly (p<0.05) less for 10% phosphoric acid gel than 32% phosphoric acid gel at the second sample period(4.32-14.4 min). 4. No significant differences were found for cumulative HEMA diffusion among the four groups at 10 days(p>0.05) and mean total(cumulative) release at 10 days for all groups was in the 9 - 16 nmol range. 5. The cumulative release was significantly (p<0.05) less for 10% phosphoric acid gel than 32% phophoric acid gel at the third(14.4-43.2 min) & fourth(43.2-144 min) sample period.

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Bioequivalence of AmbrectTM Tablet to MucopectTM Tablet (Ambroxol hydrochloride 30 mg) (뮤코펙트 정(염산암브록솔 30 mg)에 대한 암브렉트 정의 생물학적 동등성)

  • Yoo, Jeong-Yeon;Joung, Sun-Koung;Choi, Mee-Hee;Han, Sang-Beom;Lee, Kyung-Ryul;Lee, Hee-Joo
    • Journal of Pharmaceutical Investigation
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    • v.33 no.3
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    • pp.215-221
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    • 2003
  • A bioequivalence study of $Ambrect^{TM}$ tablets (Dong Wha Pharm. Ind. Co., Ltd.) to $Mucopect^{TM}$ tablets (Boehringer Ingelheim Korea, Ltd.) was conducted according to the guideline of Korea Food and Drug Administration (KFDA). Twenty four healthy male Korea volunteers received each medicine at the ambroxol hydrochloride dose of 30 mg in a $2{\times}2$ crossover study. There was a one-week wash out period between the doses. Plasma concentrations of ambroxol were monitored by a high-performance liquid chromatography for over a period of 24 hours after the administration. $AUC_t$ (the area under the plasma concentration-time curve from time zero to 24 hr) was calulated by the linear trapezoidal rule method. $C_{max}$ (maximum plasma drug concentration) and $T_{max}\;(time\;to\;reach\;C_{max})$ were compiled from the plasma concentration-time data. Analysis of variance was carried out using logarithmically transformed $AUC_t\;and\;C_{max}$. No significant sequence effect was found for all of the bioavailability parameters indicating that the crossover design was properly performed. The 90% confidence intervals of the $AUC_t$ ratio and the $C_{max}$ ratio for $Ambrect^{TM}/Mucopect^{TM}$ were 0.89-1.01 and 0.89-1.02, respectively. These values were within the acceptable bioequivalence intervals of 0.80-1.25. Thus, our study demonstrated the bioequivalence of $Ambrect^{TM}\;and\;Mucopect^{TM}$ with respect to the rate and extent of absorption.

Effect of Ginger Fractions for Inhibition of Soybean Oil and Rat Liver Microsomal Lipid Peroxidation (생강 추출획분의 대두유 및 흰쥐 간 마이크로좀 지질 과산화 억제 효과)

  • 백숙은
    • Korean journal of food and cookery science
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    • v.11 no.4
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    • pp.365-369
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    • 1995
  • The content ratios of gingerol in 4 fractions (hexane, ether, ethylacetate and hexane-ether (1:1, v/v) fraction) extracted from ginger (Zingiber officinale Roscoe) were analyzed using high performance liquid chromatography (HPLC). The content ratios of 6-gingerol in 4 fractions were hexane fraction; 49.5%, ether fraction; 20.74%, ethylacetate fraction; 21.43% and hexane-ether (1 : 1, v/v) fraction; 93.70%. Antioxidant activities of soybean oil added 0.2% of each ginger fraction and 0.02% of BHT were determined by peroxide value during storage at 45$^{\circ}C$. And relative antioxidant effectiveness (RAE) was calculated as the ratio of the induction period of a given substrate oil to that of a control oil. RAE of each fraction was hexane fraction; 2.60, ether fraction; 2.33, ethylacetate fraction; 2.07 and hexane-ether (1 : 1, v/v) fraction; 2.75, BHT; 1.74. Inhibition effect of each fraction on the rat liver microsomal lipid peroxidation showed hexane fraction; 93%, ether fraction; 92%, ethylacetate fraction; 86% in 350 g/$m\ell$ and hexane-ether (1 : 1, v/v) fraction; 89% in 20 g/$m\ell$.

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Nutrikinetic study of fermented soybean paste (Cheonggukjang) isoflavones according to the Sasang typology

  • Kim, Min Jung;Lee, Da-Hye;Ahn, Jiyun;Jang, Young-Jin;Ha, Tae-Youl;Do, Eunju;Jung, Chang Hwa
    • Nutrition Research and Practice
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    • v.14 no.2
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    • pp.102-108
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    • 2020
  • BACKGROUND/OBJECTIVES: In Oriental medicine, certain foods may be beneficial or detrimental based on an individual's constitution; however, the scientific basis for this theory is insufficient. The purpose of this study was to investigate the effect of body constitution, based on the Sasang type of Korean traditional medical classification system, on the bioavailability of soy isoflavones of Cheonggukjang, a quick-fermented soybean paste. SUBJECTS/METHODS: A pilot study was conducted on 48 healthy Korean men to evaluate the bioavailability of isoflavone after ingestion of food based on constitution types classified by the Sasang typology. The participants were classified into the Taeeumin (TE; n = 15), Soyangin (SY; n = 15), and Soeumin (SE; n = 18) groups. Each participant ingested 50 g of Cheonggukjang per 60 kg body weight. Thereafter, blood was collected, and the soy isoflavone metabolites were analyzed by ultra-performance liquid chromatography/quadrupole time-of-flight mass spectrometry. Ntrikinetic analysis of individual isoflavone-derived metabolites was performed. RESULTS: Our nutrikinetic analysis identified 21 metabolites derived from isoflavones in the blood samples from 48 healthy Korean men (age range, 21-29 years). Significant differences were observed in the time to maximum concentration (Tmax) and elimination half-life (t1/2) for nine metabolites among the three groups. The Tmax and t1/2 of the nine metabolites were higher in the SE group than in the other groups. Moreover, the absorption rates, as determined by the area under the plasma-level curve (AUC) values of intact isoflavone, were 5.3 and 9.4 times higher in the TE group than in the SY and SE groups, respectively. Additionally, the highest AUC values for phase I and II metabolites were observed in the TE group. CONCLUSIONS: These findings indicate that isoflavone bioavailability, following Cheonggukjang insgestion, is high in individuals with the TE constitution, and relatively lower in those with the SE and SY constitutions.

A Study on Removal of Abietic Acid Using Plasma (플라스마를 이용한 Abietic Acid의 제거에 관한 연구)

  • Kim, Ga-Young;Kim, Da-Seul;Kim, Dong-Hyun
    • Journal of the Korea Academia-Industrial cooperation Society
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    • v.21 no.11
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    • pp.788-794
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    • 2020
  • This study was measured and analyzed from January to November 2019 to confirm the effect that Abietic acid, an asthma-causing substance, which can be exposed to workers in the electronics industry, is removed by plasma treatment. The experiment was carried out using a solder wire and natural rosin. Air at temperatures of 250℃, 300℃, and 350℃ was collected with a glass fiber filter paper using an air sampler for 10 minutes at a flow rate of 2ℓ/min. An analysis of the collected samples was performed by pretreatment with methyl alcohol and quantitative analysis by high performance liquid chromatography (HPLC). This procedure confirmed that abietic acid was generated in both natural rosin and solder wires, and the quantum of abietic acid increased as the treatment temperature increased. The amount of abietic acid was higher in natural rosin than solder wire. As a result of plasma treatment, a removal efficiency of about 92% or more was confirmed in natural rosin. A peak of abietic acid was not detected in the solder wire. Therefore, a removal efficiency of 100% was confirmed. This study, confirmed that abietic acid, an asthma-trigger can be generated in solder wire and natural rosin, and can be removed by plasma treatment.

Changes of Saponin and β-Glucan Content on the Cultured Ginseng with Mushroom Mycelia (버섯균사체로 배양된 인삼 Saponin과 β-Glucan 함량 변화)

  • Joung, Eun-Mi;Hwang, In-Guk;Lee, Hyeon-Yong;Jeong, Jae-Hyun;Yu, Kwang-Won;Jeong, Heon-Sang
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.38 no.8
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    • pp.1084-1089
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    • 2009
  • This study investigated the changes of saponin and $\beta$-glucan content on the cultured ginseng with mushroom mycelia of Phellinus linteus (PL), Ganoderma lucidum (GL), and Hericium erinaceum (HE). Cultured ginsengs with mushroom mycelia were extracted with 80% ethanol, fractionated with n-buthanol, and analysed for ginsenosides by high performance liquid chromatography (HPLC). Crude saponin content of raw ginseng was 4.11% (d.b) but cultured ginseng with mushroom mycelia of PL, GL, and HE were increased to 6.74, 6.77 and 6.23% (d.b), respectively. Ginsenoside-Rd, among the 12 ginsenosides which were available for analysis, was remarkably increased to 13.61, 24.26, and 32.69 mg/g, respectively (raw ginseng: 0.80 mg/g). The $\beta$-glucan content of cultured ginseng with mushroom mycelia of PL, GL, and HE were decreased to 8.85, 5.51 and 5.46% rather than mushroom mycelia of 29.14, 19.44, and 23.39% (d.b), respectively.

Synthesis of Functional Lipid from Glyceryl Monooleate and Conjugated Linoleic Acid by Enzymatic Reaction (Glyceryl Monooleate와 Conjugated Linoleic Acid로부터 효소적 반응을 이용한 기능성 유지 합성)

  • Jeon, Mi-Sun;Lee, Ki-Teak
    • Journal of the Korean Society of Food Science and Nutrition
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    • v.38 no.8
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    • pp.1062-1068
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    • 2009
  • Diacylglycerol (DAG) were synthesized by enzymatic esterification of glyceryl monooleate (GMO) and conjugated linoleic acid (CLA) in a shaking water bath. The reaction was catalyzed by Lipozyme TLIM (immobilized lipase from Thermomyces lanuginosa). Effects of reaction time, molar ratio, enzyme road and molecular sieves were studied. Results of normal-phase high performance liquid chromatography (NP-HPLC) analysis were performed. At 1:1, 2:1 and 3:1 (GMO : CLA) molar ratio and Lipozyme TLIM of 20% amount, DAG were produced in 42.6, 54.4 and 54.6 area% in 1 hr, respectively. When different Lipozyme TLIM amounts (2, 5, 10, 20%) were used with 2:1 (GMO : CLA) molar ratio, DAG were produced 21.4 (24 hr), 51.7 (12 hr), 56.2 (6 hr) and 54.4 (1 hr) area%, respectively. The reaction in the absence of molecular sieves increased DAG contents. The maximum DAG concentration conditions were obtained with molar ratio of 2:1 (GMO : CLA), lipase concentration of 10% (of substrate), 10% molecular sieves and reaction time of 6 hours at 55$^{\circ}C$. Under this reaction condition, produced DAG-rich oil was composed of 69 area% DAG, 7.9 area% TAG, 2 area% FFA, and 21.1 area% MAG.

Simultaneous Analysis of Bangpungtongseong-san and Its Antioxidant Effect (방풍통성산의 동시분석 및 항산화 효능 연구)

  • Seo, Chang-Seob;Kim, Ohn Soon;Shin, Hyeun-Kyoo
    • Herbal Formula Science
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    • v.21 no.2
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    • pp.133-143
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    • 2013
  • Objectives : We carry out the simultaneous quantification for quality control of four components in Bangpungtongseong-san (BPTSS) sample. In addition, we assessed the antioxidant effects of BPTSS sample. Methods : The used column for separation and analysis of four compounds was Luna C18 column and column oven temperature was maintained at $40^{\circ}C$. The mobile phase for simultaneous determination consisted of two solvent systems, 1.0% acetic acid in water and 1.0% acetic acid in acetonitrile. High performance liquid chromatography-photodiode array (HPLC-PDA) method for analysis was performed at a flow rate of 1.0 mL/min with PDA detection at 254 and 280 nm. The injection volume was 10 ${\mu}L$. The antioxidant activities of BPTSS were evaluated by measuring free radical scavenging activities on 2,2'-Azinobis-3-ethyl-benzothiazoline-6-sulfonic acid (ABTS) and 1-1-diphenyl-2-picrylhydrazyl (DPPH). The inhibitory effects on low-density lipoprotein (LDL) oxidation were evaluated by the formation of thiobarbituric acid relative substances (TBARS) and relative electrophoretic mobility (REM). Results : Calibration curves were acquired with $r^2{\geq}0.9999$. The values of limit of detection (LOD) and quantification (LOQ) were 0.06-0.29 ${\mu}g/mL$ and 0.20-0.98 ${\mu}g/mL$, respectively. The amounts of geniposide, liquiritin, baicalin, and glycyrrhizin in BPTSS were 5.06, 7.33, 27.56, and 7.81 mg/g, respectively. The BPTSS showed the radical scavenging activity in a dose-dependent manner. The concentration required for 50% reduction (RC50) against ABTS and DPPH radicals were 72.51 ${\mu}g/mL$ and 128.49 ${\mu}g/mL$. Furthermore, GMGHT reduced the oxidation properties of LDL induced by CuSO4. Conclusions : The established HPLC-PDA method will be helpful to improve quality control of BPTSS. In addition, BPTSS has potentials as therapeutic agent on anti-atherosclerosis.

Comparative study on stability and efficacy of Banhasasim-tang decoction depending on the preservation temperature and periods (반하사심탕 전탕액의 보관 온도 및 기간에 따른 안정성 및 유효성 연구)

  • Jin, Seong Eun;Kim, Ohn Soon;Seo, Chang-Seob;Shin, Hyeun-Kyoo;Jeong, Soo-Jin
    • The Journal of Korean Medicine
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    • v.37 no.1
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    • pp.21-33
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    • 2016
  • This study aimed to investigate the stability and biological activities of BHSST decoction depending on the preservation temperature and periods. Methods: BHSST decoction was preserved at room temperatures (R/T, $23{\pm}1^{\circ}C$) or refrigeration ($4^{\circ}C$) for 0, 30, 60 and 90 days. To evaluate the stability of BHSST decoction, pH and sugar content were estimated. In addition, high-performance liquid chromatography (HPLC) analysis was performed to determine marker compounds of BHSST decoction. To evaluate anti-inflammatory effect, nitric oxide (NO) and prostaglandin $E_2$ ($PGE_2$) productions were measured in LPS-stimulated RAW 264.7 macrophages. Antioxidant activity was examined using the assays for 3-ethyl-benzothiazoline-6-sulfonic acid (ABTS) and 1-1-diphenyl-2-picrylhydrazyl (DPPH) radical scavenging activities. Results: There was no change in pH and sugar content depending on the preservation temperature and periods of BHSST decoction. Among the major components of BHSST, contents of liquiritin, baicalein and wogonin was reduced time-dependently both at R/T and $4^{\circ}C$. Inhibitory effects of BHSST decoction on NO and PGE2 productions were slightly decreased in a time-dependent manner by 90 days of preservation. In addition, BHSST decoction maintained ABTS and DPPH radical scavenging activities by 60 days while significantly reducing the activities in 90 days of preservation at R/T. By contrast, BHSST decoction had no significant change of ABTS and DPPH radical scavenging activities by 90 days at $4^{\circ}C$. Conclusions: Our results suggest that the stability and efficacy of BHSST decoction are maintained for 60 days at $4^{\circ}C$ rather than R/T.