• Title/Summary/Keyword: P-C-T curve

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Bioavailability of Ranitidine Tablets in Rats (흰쥐에서 라니티딘제제의 생체이용률)

  • 이미숙;구영순
    • YAKHAK HOEJI
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    • v.39 no.6
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    • pp.636-644
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    • 1995
  • Comparison of bioavailabflity (BA) of three brands of ranitidine (RT) tablets has been studied m rats. The purpose of this study was to characterize the pharniacolunetics of RT tablets in the rat and to coinpare phannacolunetic parameters of three brands of RT tablets. In addition, it was investigated whether plasma RT concentrations m humans can be predicted from pharmacokinetic parameters obtained in rats. RT was administered intravenously in dose of RT.HCI 10mg/kg and orally in dose of RT.HCI 50mg/kg as solution or crushed sample of thablets. Plasma RT concentrations were determned by HPLC. Plasma RT concentrations as a function of time were fitted to two compartment model. Plasma RT concentrations declined with a terminal half life ($t_{{1}/2{\betha}}$) of 40.9 min. The plasma RT concentration-time curve showed two peak plasma concentrations following an oral administration of solution or crushed sample in rats like humans. No significant difference among pharmacokinetic parameters was observed except $T_{max2}$ (p<0.05). The BA for crushed sample A, B and C were found to be 54.6 40.7 and 40.0%, respectively. Equivalence of $C_{max1}$ and $T_{max2}$ were guaranteed in this study. However, it was concluded that three brands of RT tablets are bioequivalent, taking the following characteristics of RT into consideration;(1) rapid onset of the effect is not required, (2) $C_{max1}$ and $T_{max2}$ do not seem to influence the effectiveness of the drug during a long-term treatment by the usual administration of twice a day. Results from this study were combined with plarmacokinetic data for RT in dogs and humans to develop a basis for interspecies scale-up of the disposition characteristics of the drug. there were similarities in the general disposition of the drug. Allometric relationships were sought between pharmacokinetic parameters nd species body weight. Significant interspecies correlations were found for total body clearance($Cl_{t}$) and steady state volume of distribution ($Bd_{ss}$). Thus, plasma RT concentrations in humans can be predicted from pharmacokinetic parameters obtained in rats.

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Age and Growth of the Asian Clam Potamocorbula ustulata ustulata (Reeve, 1844) on the West Coast of Korea (한국 서해산 쇄방사늑조개, Potamocorbula ustulata ustulata (Reeve, 1844) 의 연령과 성장)

  • Ryu, Dong-Ki;Kim, Yeong-Hye
    • The Korean Journal of Malacology
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    • v.23 no.1
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    • pp.17-23
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    • 2007
  • Samples of Potamocorbula ustulata ustulata were collected monthly from October 2004 to November 2005 in the Jujin estuary of Gochang, Chollabuk-do, west coast of Korean peninsula. Age of P. ustulata ustulata was determined by the rings on the shell. The relationship between the shell length and the ring diameter in each ring group was expressed as a regression line. Therefore, there is a correspondence in each ring formation. Based on the monthly variation of the marginal index (MI') of the shell, it is assumed that the ring of this species was formed once a year during October to December. The relationship between the shell length (SL) and the shell height (SH; mm) was highly correlated with shell height as the following equation: SH = 0.6438 SL + 0.5642 ($r^2\;=\;0.978$). The shell length (SL) - shell width (SW) relation was also expressed by the following equation: SW = 0.4352 SL - 0.5675 ($r^2\;=\;0.957$). Shell length (SL; mm) and the total weight (TW; g) followed: $TW\;=\;6.999\;{\times}\;10^{-5}\;SL^{3.2542}(r^2\;=\;0.975)$. Growth curves for the shell length and the total weight fitted to the von Bertalanffy's growth curve were expressed respectively as: $$SL_t=30.77[1-e^{-0.4572(t+0.7371)}],\;TW_t=4.87[1-e^{-0.4572(t+0.7371)}]^{3.2542}.$$

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Revisit on Experimental Conditions in Determination of Stress Intensity Factor and the J-Integral Using the Methods of Caustics (응력확대계수와 J-적분 결정을 위한 코스틱스방법의 실험조건에 관한 연구)

  • 이억섭;조종두;홍성경
    • Transactions of the Korean Society of Mechanical Engineers
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    • v.18 no.9
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    • pp.2331-2338
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    • 1994
  • Experimental conditions of the optical shadow methods of caustics for measurement of the stress intensity factor and the J-integral in various materials(polycarbonate, PMMA, Al 5586D) are investigated. The necessary experimental requirements toe determine accurate values of the stress intensity factors and the J-integrals are described. The ratio of $r_o$ (radius of initial curve) to $r_p$ (plastic zone size) is selected as a parameter to verify the experimental limitation of the method of caustics in determination of fracture parameters. In this study, transmission caustics method was used for compact tension specimens made of polycarbonate and PMMA. while reflection caustics method was applied to c-shaped tension specimen made of Al 5586D. The appropriate ranges of $r_o/r_p$ tp determine accurate values of stress intensity factors were found to be 1.5~1.8. Existing experimental results have been obtained mainly by changing $r_p$ with different loads in $r_o/r_p$. However, in this study we could obtain varying $K_{caus}/K_{th}$ over the wide range of $r_o/r_p$ at fixed load conditions with newly designed optical arrangement. Thus, we could find the range in which theoretical and experimental results agree well each other by changing $r_o$ values only. In Al 5586D specimen, experimental caustics were located inside of the plastic zone, and $K_{caus}/K_{th}$ were found to be not unity in this range. It is found that $J_{caus}/J_{th}=1{\;}with{\;}r_o/t{\geq}0.8$ and the experimental plastic zone includes the contours of caustics.

A Study on the Electrical Conductivity of $Na_2O-Fe2O_3-B_2O_3-P_2O_5$ System Glass ($Na_2O-Fe2O_3-B_2O_3-P_2O_5$ 계 유리의 도전성에 관한 연구)

  • 박용원;이경태
    • Journal of the Korean Ceramic Society
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    • v.22 no.3
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    • pp.35-40
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    • 1985
  • The composition of the base glass was determined to be $Na_2O$ 15, $Fe_2O_3$ 35, $B_2O_3$ 0~20, $P_2O_5$ 30~50 by mole percent. The heating temperature for nucleation was determined by means of thermal expansion curve. Crystalline phases were investigated by X-ray diffraction method and I.R Spectra. Electrical conductivities of glass spec-imens were observed in the temperature range 25~20$0^{\circ}C$ The activation energies of these specimens were caculated. The results obtained were as follows : 1) The limit composition of the melts 15mol% $Na_2O$ 35mole% $Fe_2O_5$ 20mole% $B_2O_3$ 30mole% $P_2O_5$ was able to be formed into desired shapes during cooling, . 2) In the measurement of d. c conductivity($\delta$) on the glasses in the system $15Na_2O-35Fe_2O_3$-$B_2O_3$-(50-x) $P_2O_5$ the values decreased by replacing 5 mole% $P_2O_5$ with $B_2O_3$ 3) The d. c conducties of heat treated samples were increased by replacing $P_2O_5$ with $B_2O_3$ 4) $B_2O_3$ contributed to precipitate crystals such as${\gamma}$-$Fe_2O_3$ $Fe_3O_4$ which had the advantage of electronic conduction in heat treated samples. 5) The slope plotted Log($\delta$) versus 1/T in this glass system was linear in the measured temperature range.

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Effect of Naringin on the Pharmacokinetics of Nifedipine in Rabbits (토끼에서 나린진이 니페디핀의 약물동태에 미치는 영향)

  • Na, Chong-Hak;Choi, Jun-Shik
    • Journal of Pharmaceutical Investigation
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    • v.35 no.2
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    • pp.101-106
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    • 2005
  • The pharmacokinetics of oral nifedipine (5 mg/kg) was studied in rabbits given after or simultaneously with naringin (1.5, 7.5 and 15 mg/kg, respectively). The area under the plasma concentration-time curve (AUC) and the peak concentration $(C_{max})$ of nifedipine coadministered or pretreated with naringin were significantly increased (p < 0.05, coad.; p < 0.01, pret.) compared with the control group. The absolute bioavailability (AB%) of nifedipine was significantly (p < 0.05, coad.; p < 0.01, pret.) higher by 22.3 - 28.1 % compared to the control (17.9%). The relative bioavailability (RB%) of nifedipine was higher by 1.24 - 1.43 times (coad.) and 1.32 -1.57 times (pret.) than those of the control, showing that preatreatrnent of naringin was more effective than that of the coadministration of naringin. Naringin did not show significant effect on the Tmax and $t_{1/2}$ of nifedipine. It is suggested that naringin may alter pharmacokinetic paramiters of nifedipine by inhibition of P-glycoprotein efflux pump and its first-pass metabolism. The dosage of nifedipine should be adjusted when it is administered with naringin in a clinical situation.

Drug Interaction Between Verapamil and Pioglitazone Long-term Administered to Rats (흰쥐에서 베라파밀과 장기투여된 피오그리타존과의 약물상호작용)

  • Choi, Dong-Hyun;Kim, Hyun-Yong;Choi, Jun-Shik
    • Korean Journal of Clinical Pharmacy
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    • v.18 no.1
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    • pp.6-10
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    • 2008
  • This study investigated the effect of long-term administration of pioglitazone on the pharmacokinetics of verapamil in rats. Pharmacokinetic parameters of verapamil were determined after oral administration of verapamil (9 mg/kg) in rats coadministered pioglitazone (0.5 mg/kg) or pretreated with pioglitazone (0.5 mg/kg) for 3 and 9 days. Compared to oral control group, the presence of pioglitazone significantly (p<0.05) increased the area under the plasma concentration-time curve (AUC) of verapamil by 48.6% (coad), 61.1% (3 days) and 56.5% (9 days), and the peak concentration($C_{max}$) by 65.1% (coad), 76.8% (3 days) and 66.4% (9 days). The absolute bioavailability (AB%) of verapamil was significantly (p<0.05) higher by 6.2% (coad), 6.7% (3 days), 6.5% (9 days) compared to control (4.2%), and presence of pioglitazone was no significant change in the terminal half-life ($t_{1/2}$) and the time to reach the peak concentration($T_{max}$) of verapamil. Our results indicate that pioglitazone significantly enhanced oral bioavailability of verapamil in rats, implying that presence of pioglitazone could be effective to inhibit the CYP3A4-mediated metabolism of verapamil in the intestine. Drug interactions should be considered in the clinical setting when verapamil is coadministrated with pioglitazone.

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Bioavailability of Digoxin Tablets in Healthy Volunteers

  • Lee, Chi-Ho;Park, Yun-Ju;Charies-D. Sands;Daniel-W. Jones;John-M. Trang
    • Archives of Pharmacal Research
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    • v.17 no.2
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    • pp.80-86
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    • 1994
  • The bioavailability of digoxin generic tablets manufactures in Korea (formulations A & B) wwere compared to a standard (formulation C; Lanoxin brand digoxin, Burroughs Wellcome, USA) in 12 healthy Korean male volunteers (mean age 31.4 years) in a single dose, randomized, complete block crossover study. Using a latin square design, each of the subjects was randomized to the order number and allocated to each of the three treatments of 0.5mg oral digoxin. Digoxin conc4ntrations in serum and urine samples collected for 48 hours after dosing were measured by fluoprescence polarization immunoassy and radioimmunoassy, respectively. Treatments were compared by using nonlinear least squares regession analysis to evaluate the following pharmacokinetic parameters : maximum serum concentation $(C_{max})$; time of maximum serum concentation $(T_{max})$; area under the serum concentration-time curve $AUC_{0-12}$, $C_{max}$\;and\;(AUC_{0-12})$; and cummulative urinary excretion for 0-48 hours $(CLE_{0-48}.\;Mean\;AUC_{0-12},\;C_{max},\;and\;CUE_{0-48}$ values for formulations B and C were significantly different from formulation A (P<0.001), but not significantly diffeerent form each other. Basede on $AUL_{0-12}\;and\;CUE_{0-48}$ respectively, the relative availability of formulation B was 87.5% and 89.6% and the relative availability of formultation A was 43% and 35% when compared to formulation C(the standard).

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A Comparison between Asia-Pacific Region Criteria and Entropy Model Criteria about Body Mass Index of Elderly Females Using Morbidity of Chronic Disease (만성질환 이환율을 이용한 여자노인의 체질량지수에 대한 아시아-태평양지역 기준과 Entropy모델 기준 비교)

  • Jeong, Gu-Beom;Park, Jin-Yong;Kwon, Se-Young;Park, Kyung-Ok;Park, Pil-Sook;Park, Mi-Yeon
    • Korean Journal of Community Nutrition
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    • v.19 no.5
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    • pp.490-498
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    • 2014
  • Objectives: This study was conducted to propose the need of re-establishing the criteria of the body weight classification in the elderly. We compared the Asia-Pacific Region Criteria (APR-C) with Entropy Model Criteria (ENT-C) using Morbidity rate of chronic diseases which correlates significantly with Body Mass Index (BMI). Methods: Subjects were 886 elderly female participating in the 2007-2009 Korea National Health and Nutrition Examination Survey (KNHANES). We compared APR-C with those of ENT-C using Receiver Operating Characteristics (ROC) curve and logistic regression analysis. Results: In the case of the morbidity of hypertension, the results were as follows: Where it was in the T-off point of APR-C, sensitivity was 67.5%, specificity was 43.1%, and Youden's index was 10.6. While in the cut-off point of ENT-C, it was 56.7%, 56.6%, and 13.3 respectively. In the case of the morbidity of diabetes, the results were as follows: In the cut-off point of APR-C, Youden's index was 14.2. While in the cut-off point of ENT-C, it was 17.2 respectively. The Area Under the ROC Curve (AUC) of the subjects who had more than 2 diseases among hypertension, diabetes, and dyslipidemia was 0.615 (95% CI: 0.578-0.652). Compared to the normal group, the odds ratio of the hypertension group which will belong to the overweight or obesity was 1.79 (95% CI: 1.30-2.47) in the APR-C, and 2.04 (95% CI: 1.49-2.80) in the ENT-C (p < 0.001). Conclusions: We conclude that the optimal cut-off point of BMI to distinguish between normal weight and overweight was $24kg/m^2$ (ENT-C) rather than $23kg/m^2$ (APR-C).

Weathering Characteristics of Rock under Natural Environment and Strength Evaluation of Weathered Rock (자연환경하에서 암석의 풍화특성과 풍화암석의 강도평가)

  • Kang, Dae-Wan;Obara, Yuzo;Hirata, Atsuo;Kang, Seong-Seong
    • Tunnel and Underground Space
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    • v.21 no.6
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    • pp.460-470
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    • 2011
  • Wave velocity was measured to define the weathering characteristics of rock and the strength evaluation of weathered rock on a target of the Aso gravestones with various sizes under the natural environment. As a result, the size correction method which was changed sample of the different size to one of the same size for evaluating wave velocity was proposed, and also suggested the NET (Normalized Elapsed Time) as a new weathering index of rock. In addition, the strength of the weathered rock was estimated from the weathering classification of rock using the NET. Wave velocity of welded tuff was high and didn't show velocity degradation, on the other hand, one of andesite was low and showed velocity degradation. The degree of weathering between rocks of the different size is considered to be comparable, applying the NET based on the on the $V_p/V_o$-NET curve. Furthermore, the classification of rock weathering stages using the NET based on the $S_c/S_o$-NET curve was available, and the estimation of strength for the weathered rock was also possible.

Effects of Resveratrol on the Pharmacokinetics of Nifedipine in Rats (레스베라트롤이 니페디핀의 약물동태에 미치는 영향)

  • Choi, Byung-Chul;Choi, Jun-Shik
    • YAKHAK HOEJI
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    • v.54 no.4
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    • pp.252-257
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    • 2010
  • The aim of this study was to investigate the effect of resveratrol on the pharmacokinetics of nifedipine in rats. The pharmacokinetic parameters of nifedipine were measured after the oral administration of nifenipine (6 mg/kg) in the presence or absence of resveratrol (0.5, 2.5 and 10 mg/kg, respectively). The effect of resveratrol on the P-glycoprotein (Pgp), CYP 3A4 activity was also evaluated. Resveratrol inhibited CYP3A4 enzyme activity in a concentration-dependent manner with 50% inhibition concentration ($IC_{50}$) of 0.94 ${\mu}M$. In addition, resveratrol significantly enhanced the cellular accumulation of rhodamine 123 in MCF-7/ADR cells overexpressing P-gp. Compared to the control groups, the presence of 2.5 mg/kg and 10 mg/kg of resveratrol significantly (p<0.05, p<0.01) increased the area under the plasma concentrationtime curve (AUC) of nifedipine by 49~75%, and the peak concentration ($C_{max}$) of nifedipine by 48~66%. The absolute bioavailability (AB%) of nifedipine was significantly (p<0.05) increased by 22.9-34.8% compared to the control (19.8%). The terminal half-life ($T_{1/2}$) of nifedipine was significantly (p<0.05) increased compared to the control. While there was no significant change in the time to reach the peak plasma concentration ($T_{max}$) of nifedipine in the presence of resveratrol. It might be suggested that resveratrol altered disposition of nifedipine by inhibition of both the CYP3A and P-glycoprotein efflux pump in the small intestine of rats. In conclusion, the presence of resveratrol significantly enhanced the oral bioavailability of nifedipine, suggesting that concurrent use of resveratrol or resveratrol-containing dietary supplenment with nifedipine should require close monitoring for potential drug interation.