• Title/Summary/Keyword: $C_{}$ max/

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Studies on Triterpenoid Corticomimetics (I) Inhibition of Corticoid-$5{\beta}$-reductase by 11-Oxo-oleanolic Acid and 11-Oxo-hederagenin (Corticoid 활성물질의 개발을 위한 기초연구(I) 11-Oxo-oleanolic Acid 및 11-Oxo-hederagenin의 Corticoid-$5{\beta}$-reductase에 대한 조해효과)

  • 한병훈;이혜정;한대석
    • YAKHAK HOEJI
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    • v.26 no.1
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    • pp.1-8
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    • 1982
  • Derivation of triterpenoids and then the screening for corticomimetics among them is our primary interest. $C_{11}$-oxo-triterprenoids except glycyrrhetinic acid are rarely found in the plant kingdom. Based on the facts that $C_{3}$ and $C_{11}$-Oxo-group are essential for the corticoid-like-activity through its competitive inhibition on the corticoid-5.betha.-reductase, it was attempted to produce artificial inhibitor on the enzyme by introducing $C_{11}$-oxo group to the triterpenoids of oleanene series such as oleanolic acid and hederagenin. We could obtain the $C_{11}$-oxo-oleanolic acid m.p. $264-6^{\circ}$, uv ${\lambda}max$ 249 and $C_{11}$-oxo-hederagenin amorp. uv ${\lambda}max$ 251 by acetylation, $CrO_{3}$-oxid., and deacetylation. Glycyrrhetinic acid, a natural 11-oxo-compound and the other 11-oxo-derivatives of oleanolic acid and hederagenin were compared in their inhibitory activity on the corticoid-5.betha.-reductase. The inhibitory activity of those compound were decreased in the order of $C_{11}$-oxo-oleanolic acid, $C_{11}$-oxo- hederagenin, glycyrrhetinic acid. This suggests more strong corticomimetic activity of those artificially derived $C_{11}$-oxo-oleanolic acid and $C_{11}$-oxa-hederagenin. Their Ki value were $4.6{\times}10^{-4}M$ and $5.8{\times}10^{-4}M$ respectively.

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A STUDY ON dmf & PREDILECTION SITES OF PRESCHOOL CHILDREN IN SEOUL. (서울시(市) 미취학아동(未就學兒童)의 dmf 및 치아우식(齒牙齲蝕) 호발부위(好發部位)에 대(對)한 연구(硏究))

  • Ko, Sung-Hee
    • Journal of the korean academy of Pediatric Dentistry
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    • v.8 no.1
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    • pp.103-117
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    • 1981
  • The data about dental caries obtained from 1438 preschool children (male 797, female 641) in Seoul aged from 3 to 6 were analyzed by their sexes, ages, jaws and teeth surfaces. The results were as follows. 1. dmf rate : 92.63% 2. dmft index : 6.06 dmft rate 30.81 % dmfs index : 11.82 dmfs rate 12.02 % 3. d,m & f rate d rate: 79.45% m rate: 8.15% f rate : 12.40 % 4. dft index : 5.94 5. The order of caries susceptible tooth 1. Lower deciduous 2nd molar 2. Lower deciduous 1st molar 3. Upper deciduous 2nd molar 4. Upper deciduous lateral incisor 5. Upper deciduous cental incisor 6. Upper deciduous lateral incisor 7. Lower deciduous canine 8. Upper deciduous canine 9. Lower deciduous central incisor 10. Lower deciduous lateral incisor 6. Predilection sites of each tooth A) Deciduous central incisor ; Max. : Mesial cavity Mand. : Mesio-distal cavity B) Decidous lateral incisor ; Max. : Mesial cavity Mand. : Distal cavity=Mesial cavity C) Deciduous canine; Max. : Labial cavity Mand. : Distal cavity D) Decidous 1st molar ; Max. : Disto-occlusal cavity Mand.: Disto-occlusal cavity E) Deciduous 2nd molar ; Max. : Linguo-occlusal cavity Mand.: Occlusal cavity 7. All the values in caries criteria in 1981 were somewhat lower than in 1968, but m & f rate were increased.

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Effect on the Externally Stained IPS e.max Press Porcelain Due to Tooth Brushing (칫솔질이 IPS e.max Press 도재의 외부 stain에 미치는 영향)

  • Park, Chan;Lee, Gyeong-Je;Kim, Hee-Jung
    • Journal of Dental Rehabilitation and Applied Science
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    • v.28 no.2
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    • pp.213-221
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    • 2012
  • The purpose of this study was to evaluate the stability of external stain that long term attrition caused by tooth brushing affected the color variation of external stain of IPS e.max Press Porcelain. The specimen was made by IPS e.max Press LT ingots, and treated the shade of external staning as Orange, A, B, C, D After conducting horizontal toothbrush strokes about 11,000 / 22,000 / 44,000 / 66,000 / 88,000, Color changers of the external stained layer was measured with SpectroShade$^{tm}$ MICRO(MHT, Italy). The result of this study was obtained as follows: 1. After 11,000 strokes, the color changes of shade were greater in Orange shade than the other 4 shade groups. And even though toothbrush strokes were increased until 88,000, there were no statistical significant color changes about the external stain shade variation. 2. The amount of color variation about increasing of toothbrushing strokes was irregular(no consistent increasing, or decreasing), and it was no statistical significant changes According to these results, the long term tooth-brushing doesn't affect the changes of external stain about IPS e.max press porcelain. And it doesn't reduce the stability of external stain clinically. Later, it will be needed to study other factors affecting the external stain.

Comparison of voice range profiles of modal and falsetto register in dysphonic and non-dysphonic adult women (음성장애 성인 여성과 정상음성 성인 여성 간 진성구와 가성구의 음성범위프로파일 비교)

  • Jaeock Kim;Seung Jin Lee
    • Phonetics and Speech Sciences
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    • v.14 no.4
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    • pp.67-75
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    • 2022
  • This study compared voice range profiles (VRPs) of modal and falsetto register in 53 dysphonic and 53 non-dysphonic adult women with gliding vowel /a/'. The results shows that maximum fundamental frequency (F0MAX), maximum intensity (IMAX), F0 range (F0RANGE), and intensity range (IRANGE) are lower in the dysphonic group than in the non-dysphonic group. F0MAX and F0RANGE are significantly higher in falsetto register than modal register in both groups. IMAX and IRANGE are significantly higher in falsetto register in the non-dysphonic group, but those are not different between two registers in the dysphonic group. There was no statistically significant difference in minimum F0 (F0MIN) and minimum intensity (IMIN) between the two groups. Modal-falsetto register transition occurred at 378.86 Hz (F4#) in the dysphonic group and 557.79 Hz (C5#) in the non-dysphonic group, which was significantly lower in the dysphonic group. It can be seen that both modal and falsetto registers in dysphonic adult women are reduced compared to non-dysphoinc adult women, indicating that the vocal folds of dysphonic adult women are not easy to vibrate in high pitches. The results of this study would be the basic data for understanding the acoustic features of voice disorders.

Bioequivalence Assessment of DM Tablet to Motilium-$M^{(R)}$ Tablet (모티리움엠정(말레인산 돔페리돈 12.72 mg)에 대한 디엠정의 생물학적동등성 평가)

  • Cho, Seong-Wan;Kim, Young-Il;Lee, Jong-Oh;Bang, Joon-Seok;Jeong, Ji-Hoon
    • Korean Journal of Clinical Pharmacy
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    • v.18 no.2
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    • pp.106-113
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    • 2008
  • The aim of this study was to evaluate the bioequivalence of two domperidone preparations. Bioequivalence assessment was conducted on 34 healthy volunteers who received two tablets (Domperidone Maleate, 12.72 mg/tablet) in the fasting state, in a randomized balanced $2{\times}2$ cross-over study design. This whole study was performed according to the implementation guidelines of the Korea Food Drug Administration. After dosing of two tablets, blood samples were collected serially for a period of 36 hours. Plasma was analyzed for domperidone by using LC/MS/MS assay method. The analysis system was validated in specificity, accuracy, precision, and linearity. $AUC_t$, (the area under the plasma concentration-time curve from the zero-time to 36 hr) was calculated through the trapezoidal rule. $C_{max}$ (maximum plasma drug concentration) and $T_{max}$ (time to reach $C_{max}$) were compiled from the plasma domperidone concentration-time data of each volunteer. No significant sequence effect was found for the bioavailability parameters indicating that the cross-over design was properly performed. The 90%-Confidence intervals of the $AUC_t$ ratio and the $C_{max}$ were from log 0.8007 to log 1.1240 and log 0.8645- log 1.2483, respectively. These values were within the acceptable bioequivalence intervals between 0.80 and 1.25. Therefore, this study demonstrated that two formulations have bioequivalence with respect to the rate and extent of absorption.

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Determination of Hydrochlorothiazide in Human Plasma by HPLC and Applicability to Oral Bioavailability in Korean Healthy Male Volunteers (HPLC를 이용한 혈중 히드로클로로티아지드의 분석 및 이를 이용한 한국인 성인남성에 대한 생체이용률 평가)

  • Park, Ah-Yeon;Kim, Jin-Hee;Kim, Sung-Yong;Chi, Sang-Cheol;Bok, Hae-Sook;Kim, Ho-Jung;Youm, Jeong-Rok;Han, Sang-Beom
    • YAKHAK HOEJI
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    • v.50 no.5
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    • pp.301-307
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    • 2006
  • A simple and sensitive high-performance liquid chromatographic method for quantitation of hydrochlorothiazide in human plasma was developed and bioavailability parameters of hydrochlorothiazide were assessed in Korean healthy male volunteers. Caffeine was used as an internal standard. Hydrochlorothiazide and internal standard in plasma sample were extracted using tert-butylmethylether (TBME). A centrifuged upper layer was then evaporated and reconstituted with mobile phase of acetonitrile-25 mM phosphate buffer (20/80, pH 2.5). The reconstituted samples were injected into a Luna C18 column $(250{\times}4.6\;mm,\;5{\mu}m)$ at a flow-rate of 1.0 ml/min. The wavelength was set at 230 nm and no endogenous substances were found to interfere, A linear relationship for hydrochlorothiazide was found in the range of $10{\sim}300\;ng/ml$. The lower limit of quantitation (LLOQ) was 10 ng/ml with acceptable precision and accuracy. Assayed in plasma, the intra- and inter-day validation for all coefficients of variation (R.S.D.%) were found less than 15%. Main pharmacokinetic parameters of 50mg of hydrochlorothiazide were revealed as follows: $AUC_t\;1761{\pm}509.0\;ng{\cdot} hr\;ml,\;C_{max}\;296.5{\pm}95.5\;ng/ml,\;T_{max}\;1.94{\pm}0.85hr,\;K_{el}\;0.12{\pm}0.04\;hr^{-1}\;and T_{12}\;6.81{\pm}2.92\;hr.\;C_{max}\;and\;T_{max}$ were in accordance with the values $(270{\sim}350\;ng/ml\;and\;1.9{\sim}2.7\;hr)$ of Caucasian.

Bioequivalence Study of Hydrocortisone Tablets while Secretion of Endogenous Cortisol Suppressed

  • Ok, Tae-Suk;Lee, Kyoung-Jin;Shin, Young-Hee
    • Biomolecules & Therapeutics
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    • v.16 no.3
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    • pp.255-260
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    • 2008
  • The purpose of this study was to evaluate the bioequivalence of the test (Daewoo Hydrocortisone 10 mg, Daewoo Pharm. Co., Busan, Korea) and reference (Jenapharm Hydrocortisone 10 mg, JayTech Biogen, Seoul, Korea) hydrocortisone tablets. Twenty-four healthy male Korean volunteers were divided into two groups with a randomized $2{\times}2$ cross-over design. In order to suppress the endogenous cortisol secretion, a single oral dose of Dexamethasone (4 mg) was administered 10 hr prior to hydrocortisone administration. Blood samples were withdrawn for 10 hr at the predetermined intervals after a single oral dose of hydrocortisone (20 mg). The serum concentration of hydrocortisone was analyzed by HPLC/UV using a column switching method after liquid-liquid extraction process. The pharmacokinetic parameters ($AUC_{0{\sim}10hr}$, $C_{max}$, and $T_{max}$) of the test and reference hydrocortisone tablets were determined while the secretion of endogenous cortisol was being suppressed. The pharmacokinetic parameters of the test tablet were not statistically different from those of the reference tablet at ex value was 0.05. The 90% confidence intervals for the average ratio (test/reference) of $AUC_{0{\sim}10hr}$ and $C_{max}$ were within the Korea Food and Drug Administration acceptance range of 0.80-1.25 ($0.89{\sim}0.99$ and $0.86{\sim}0.99$ for $AUC_{0{\sim}10hr}$ and $C_{max}$, respectively). Therefore it was concluded that the test tablet, Daewoo Hydrocortisone tablet was bioequivalent to the reference tablet, Jenapharm Hydrocortisone tablet.

Preparation and Pharmacokinetic Evaluation of Ipriflavone Sustained Release Tablet (이프리플라본 서방정 제조 및 약동학적 평가)

  • Park, Kyoung-Ho
    • Journal of Pharmaceutical Investigation
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    • v.27 no.4
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    • pp.323-329
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    • 1997
  • Ipriflavone is non-hormonal antiosteoporotic drug which inhibits bone resorption by reducing recruitment and/or differentiation of osteoclasts, and stimulates proliferation and differentiation of osteoblast, and also enhances calcitonin secretion in the presence of estrogen. Although some kinds of immediately-released preparation of ipriflavone are available in commercial market, in present study, we tried to formulate sustained-release tablet using coating method with hydrophobic and hydrophilic coating materials. In vitro dissolution test was applied to evaluate sustained-release patterns of several test preparations (Test tablet A, B and C) designed using different preparation method or different compositions. From the results of dissolution test, test tablet A which showed suitable dissolution profile was selected as the candidate of new product. Pharmacokinetic evaluation of test drug, ipriflavone sustained-release tablets, was conducted in 6 beagle dogs weighing $11.5{\pm}0.5\;Kg$ compared with $Theobon^{\circledR}$ tablet, immediately-released tablet (Kukjae Pharm. Co.) as reference drug. Two products were randomly administered to 6 beagle dogs, and after 1 week, cross-over study was conducted. From the present study, AUC and $T_{max}$ of test product were significantly different from those of reference product (p<0.05), respectively$(AUC\;:\;3646.28{\pm}472.56\;vs\;3646.28{\pm}472.56\;ng{\cdot}hr/ml,\;T_{max}\;:\;4.33{\pm}1.03\;vs\;1.42{\pm}0.38\;hr)$. But $C_{max}$ was not significantly different between two products (p>0.05) $(\;512.52{\pm}48.18\;vs\;443.97{\pm}140.53\;ng/ml)$. From the results of pharmacokinetic evaluations, it was noted that absorption amount of test product was increased, but absorption rate was delayed and $C_{max}$ of two products were not changed. And it was concluded that redesign of the sustained-release preparation which has a lower content of iprifavone rather than test tablet A must be considered.

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Bioequivalence of Taepyungyang Baclofen Tablet to BaclanTM Tablet (Baclofen 10 mg) (바클란 정(바클로펜 10 mg)에 대한 태평양바클로펜 정의 생물학적동등성)

  • Kang, Il-Mo;Ryu, Ju-Hee;Lee, Heon-Woo;Seo, Ji-Hyung;Lee, Hyun-Soo;Lee, Myung-Jae;Choi, Sang-Jun;Kang, Jin-Yang;Lee, Kyung-Tae
    • Journal of Pharmaceutical Investigation
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    • v.37 no.4
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    • pp.249-254
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    • 2007
  • The purpose of the present study was to evaluate the bioequivalence of two baclofen tablets, $Baclan^{TM}$ tablet (Yooyoung Pharm. Co., Ltd., Seoul, Korea, reference drug) and Taepyungyang Baclofen tablet (Pacificpharma Corporation, Seoul, Korea, test drug), according to the guidelines of Korea Food and Drug Administration (KFDA). Twenty-four healthy male Korean volunteers received three tablets containing baclofen 10 mg in a $2{\times}2$ crossover study. There was a one-week washout period between the doses. Plasma concentrations of baclofen were monitored for over a period of 24 hr after the administration by using an LC-MS/MS. $AUC_t,\;C_{max}\;and\;T_{max}$ were compiled from the plasma concentration-time data. Analysis of variance (ANOVA) test was utilized for the statistical analysis of the parameters using logarithmically transformed $AUC_t\;and\;C_{max}$. The 90% confidence intervals of the $AUC_t$ and the $C_{max}$ for Taepyungyang $Baclofen/Baclan^{TM}$ were $log0.92{\sim}log1.06\;and\;log1.03{\sim}log1.22$, respectively. These values were within the acceptable bioequivalence intervals of $log0.80{\sim}log1.25$. It was concluded that Taepyungyang Baclofen tablet was bioequivalent to $Baclan^{TM}$ tablet, in terms of both rate and extent of absorption.

Proteomic Analysis of Fructophilic Properties of Osmotolerant Candida magnoliae

  • Yu, Ji-Hee;Lee, Dae-Hee;Park, Yong-Cheol;Lee, Mi-Gi;Kim, Dae-Ok;Ryu, Yeon-Woo;Seo, Jin-Ho
    • Journal of Microbiology and Biotechnology
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    • v.18 no.2
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    • pp.248-254
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    • 2008
  • Candida magnoliae, an osmotolerant and erythritol producing yeast, prefers D-fructose to D-glucose as carbon sources. For the investigation of the fructophilic characteristics with respect to sugar transportation, a sequential extraction method using various detergents and ultracentrifugation was developed to isolate cellular membrane proteins in C. magnoliae. Immunoblot analysis with the Pma1 antibody and two-dimensional electrophoresis analysis coupled with MS showed that the fraction II was enriched with membrane proteins. Eighteen proteins out of 36 spots were identified as membrane or membrane-associated proteins involved in sugar uptake, stress response, carbon metabolism, and so on. Among them, three proteins were significantly upregulated under the fructose supplying conditions. The hexose transporter was highly homologous to Ght6p in Schizosaccharomyces pombe, which was known as a predominant transporter for the fructose uptake of S. pombe because it exhibited higher affinity to D-fructose than D-glucose. The physicochemical properties of the ATP-binding cassette transporter and inorganic transporter explained their direct or indirect associations with the fructophilic behavior of C. magnoliae. The identification and characterization of membrane proteins involved in sugar uptake might contribute to the elucidation of the selective utilization of fructose to glucose by C. magnoliae at a molecular level.