• YAKHAK HOEJI
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• v.47 no.2
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• pp.120-124
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• 2003

Due to its profound intestinal first-pass metabolism, oral eperisone hydrochloride produces a very low bioavailability and a very short muscle relaxant activity. To improve the efficacy and compliance of eperisone, we designed a new dosage form, the transdermal patch and evaluated the muscle relaxant effects of this patch in rats. The muscle relaxant activity was assessed by measurement of forelimb grip strength and hanging test in rats. The transdermal patch of eperisone hydrochloride showed significant muscle relaxant activity at 0.5, 1.5 and 3 cm$^2$/200 g rat (1.39, 4.17 and 8.33 mg of eperisone hydrochloride/kg, respectively) in a dose-dependent manner and the effects were lasted over 24 hours. The oral eperisone hydrochloride showed significant activity at 12.5, 25 and 50 mg/kg in a dose-dependent manner but the activity was within 1 or 2 hours after administration. These results suggest that the eperisone hydrochloride is absorbed efficiently from transdermal patch and the patch can exert potent and long-lasting muscle relaxant activity. This transdermal patch will increase the efficacy and compliance in the clinical use of eperisone hydrochloride.

• Archives of Pharmacal Research
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• v.29 no.4
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• pp.333-338
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• 2006

The aim of this study was to investigate the effect of morin on the bioavailability of nimodipine after administering nimodipine (15 mg/kg) orally to rabbits either co-administered or pretreated with morin (2, 10 and 20 mg/kg). The plasma concentrations of nimodipine in the rabbits pretreated with morin were increased significantly (p<0.05 at 10 mg/kg, p<0.01 at 20 mg/kg) compared with the control, but the plasma concentrations of nimodipine co-administered with morin were not significant. The areas under the plasma concentration-time curve (AUC) and the peak concentrations $(C_{max})$ of the nimodipine in the rabbits pretreated with morin were significantly higher (p<0.05 at 10 mg/kg, p<0.01 at 20 mg/kg), but only the $C_{max}$ of nimodipine coadministered with morin 10 mg/kg was increased significantly (p<0.05). The absolute bioavailability $(A.B\%)$ of nimodipine in the rabbits pretreated with morin was significantly (p<0.05 at 10 mg/kg, p<0.01 at 20 mg/kg) higher $(54.1-65.0\%)$ than the control $(36.7\%)$. The increased bioavailability of nimodipine in the rabbits pretreated with morin might have been resulted from the morin, which inhibits the efflux pump P-glycoprotein and the first-pass metabolizing enzyme by cytochrome P-450 3A4 (CYP 3A4).

• Wind and Structures
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• v.32 no.5
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• pp.423-437
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• 2021

Aerodynamic measures have been widely used for improving the flutter stability of long-span bridges, and this paper focuses their windproof ability to improve the wind environment for vehicles. The whole wind environment around a long-span bridge located in high altitude mountainous areas is first studied. The local wind environment above the deck is then focused by two perspectives. One is the windproof effects of aerodynamic measures, and the other is whether the bridge with aerodynamic measures meets the requirement of flutter stability after installing extra wind barriers in the future. Furthermore, the effects of different wind barriers are analyzed. Results show that aerodynamic measures exert potential effects on the local wind environment, as the vertical stabilizer obviously reduces wind velocities behind it while the closed central slot has limited effects. The suggested aerodynamic measures have the ability to offset the adverse effect of the wind barrier on the flutter stability of the bridge. Behind the wind barrier, wind velocities decrease in general, but in some places incoming flow has to pass through the deck with higher velocities due to the increase in blockage ratio. Further comparison shows that the wind barrier with four bars is optimal.

• Structural Monitoring and Maintenance
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• v.6 no.1
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• pp.33-46
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• 2019

In present study, Operational Modal Analysis (OMA) was employed to carry out the dynamic and vibration analysis of the threshing unit of the combine harvester thresher as a mechanical component. The main study is to find the causes of vibration and to decrease it to enhance the lifetime and efficiency of the threshing unit. By utilizing OMA, structural modal parameters such as mode shapes, natural frequencies, and damping ratio was calculated. The combine harvester was excited by engine to vibrate different parts and accelerometer sensor collected acceleration signals at different speeds, and OMA was utilized by nonparametric and frequency analysis methods to obtain modal parameters while vibrating in real working conditions. Afterwards, finite element model was designed from the thresher and updated using the data obtained from the modal analysis. Using the conducted analyses, it was specified that proximity of the thresher pass frequency to one of the natural frequencies (16.64 Hz) was the most important effect of vibration in the thresher. Modification process of the structure was carried out by increasing mass required for changing the natural frequency location of the first mode to 12.4 Hz in order to reduce resonance and vibration of the thresher.

• Journal of Pharmaceutical Investigation
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• v.41 no.5
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• pp.273-278
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• 2011

The aim of this study was to investigate the effect of efonidipine on the pharmacokinetics of warfarin after oral and intravenous administration of warfarin in rats. Warfarin was administered orally (0.2 mg/kg) or intravenously (0.05 mg/kg) without or with oral administration of efonidipine (1 or 3 mg/kg) in rats. The effect of efonidipine on the cytochrome P450 (CYP) 3A4 activity was also evaluated. Efonidipine inhibited CYP3A4 enzyme activity with 50% inhibition concentration ($IC_{50}$) of $0.08{\mu}M$. Compared to those in the oral control group (warfarin without efonidipine), the area under the plasma concentration-time curve (AUC) of warfarin was significantly greater (1 mg/kg, P<0.05; 3 mg/kg, P<0.01) by 25.9-59.0%, and the peak plasma concentration ($C_{max}$) was significantly higher (3 mg/kg, P<0.05) by 26.2% after oral administration of warfarin with efonidipine, respectively. The total body clearance of warfarin was significantly (3 mg/kg, P<0.05) decreased by efonidifine. Consequently, the relative bioavailability of warfarin was increased by 1.26- to 1.59-fold and the absolute bioavailability of warfarin with efonidipine was significantly greater by 59.7-75.4 % compared to that in the control group (47.4%). In contrast, efonidipine had no effect on any pharmacokinetic parameters of warfarin given intravenously. Therefore, the enhanced oral bioavailability of warfarin may be due to inhibition of CYP 3A4-mediated metabolism in the intestine and/or liver and to reduction of total body celarance rather than renal elimination, resulting in reducing first-pass metabolism by efonidipine.

• Journal of the Korean Applied Science and Technology
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• v.28 no.2
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• pp.170-177
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• 2011

Transdermal drug delivery(TDS) offers many important advantages. For instance, it is easy and painless, it protects the active compound from gastric enzymes, and it avoids the hepatic first-pass effect. Also, it is simple to terminate the therapy if any adverse or undesired effect occurs. But skin is a natural barrier, and only a few drugs can penetrate the skin easily and in sufficient quantities to be effective. Therefore, in recent years, numerous studies have been conducted in the area of penetration enhancement. The most commonly used transdermal system is the skin patch using various types of technologies. Compared with other method of dosage, it is possible to use for a long term. It is also possible to stop the drug dosage are stopped if the drug dosage lead to side effect. Polysaccharide, such as xanthan gum and algin were selected as base materials of TDS. Also, these polymers were characterized in terms of enhancers and drug contents. Among these polysaccharide, the permeation rate of Paroxetine such as lipophilic drug was the fastest in xanthan gum matrix in vitro. We used glycerin, PEG400 and PEG800 as enhancers. Since dermis has more water content(hydration) than the stratum corneum, skin permeation rate at steady state was highly influenced when PEG400 was more effective for lipophilic drug. Proper selection of the polymeric materials which resemble and enhance properties of the delivering drug was found to be important in controlling the skin permeation rate.

• Journal of Pharmaceutical Investigation
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• v.30 no.4
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• pp.247-252
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• 2000

The advantages of transdermal administration are avoiding hepatic first pass effect, minimizing inter- and intra-patient variation, maintaining steady-state plasma level to provide long-term therapy from a single dose, and allowing a rapid termination of drug input. Clenbuterol, a selective ${\beta}_2-adrenergic$ receptor stimulant, has been introduced as a potent bronchodilator for patients with bronchial asthma, chronic obstructive bronchial disease. For the development of transdermal systems containing clenbuterol, two limiting factors - long lag time and low flux - must be overcome. In this study, we attempted to select optimal formulation for preparation of clenbuterol patch using hairless mouse skin and flow-through diffusion cell. The flux of clenbuterol increased as the percent of clenbuterol dose dependently in the concentration range of 5-15%. Based on this result, we fixed the concentration of clenbuterol as 15%. The effect of various penetration enhancers on percutaneous absorption of clenbuterol through hairless mouse skin was investigated. Labrafil was the most effective enhancer, which increased the permeability of clenbuterol approximately 4-fold compared with the control without penetration enhancer. Optimal enhancer concentration was 3%. The effect of various adhesives on penetration of clenbuterol was also investigated. Among the adhesives studied, MA-31 was the most effective adhesive. Furthermore, the clenbuterol patch composed of 15% clenbuterol, 3% Labrafil and 82% MA-31, which gave most excellent penetration of drug in in vitro penetration study, maintained therapeutic plasma levels in in vivo study using S.D. rats. These studies demonstrated a good feasibility of clenbuterol administration through the intact skin using a transdermal patch, and show a possibility of the development of clenbuterol patches.

• Journal of KIISE:Software and Applications
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• v.30 no.7_8
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• pp.727-743
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• 2003

This paper proposes an automatic highlight building algorithm for soccer video by using the structural characteristics of broadcasted sports video that an interesting (or important) event (such as goal or foul) in sports video has a continuous replay shot surrounded by gradual shot change effect like wipe. This shot editing rule is used in this paper to analyze the structure of broadcated soccer video and extracts shot involving the important events to build a highlight. It first uses the spatial-temporal image of video to detect wipe transition effects and zoom out/in shot changes. They are used to detect the replay shot. However, using spatial-temporal image alone to detect the wipe transition effect requires too much computational resources and need to change algorithm if the wipe pattern is changed. For solving these problems, a two-pass detection algorithm and a pixel sub-sampling technique are proposed in this paper. Furthermore, to detect the zoom out/in shot change and replay shots more precisely, the green-area-ratio and the motion energy are also computed in the proposed scheme. Finally, highlight shots composed of event and player shot are extracted by using these pre-detected replay shot and zoom out/in shot change point. Proposed algorithm will be useful for web services or broadcasting services requiring abstracted soccer video.

• Journal of Pharmaceutical Investigation
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• v.21 no.4
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• pp.215-222
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• 1991

The absorption characteristics of itraconazole, which is an antifungal agent, from intestinal segments in the anesthetized rat i1l situ were investigated in order to design an effective oral drug delivery system. The pH-solubility profile of itraconazole, the rate and extent of absorption of itraconazole, the optimal absorption site(s) of itraconazole and the absorption enhancing effect of sodium cholate on itraconazole were examined in the present study. In situ single-pass perfusion method and recirculating perfusion technique using duodenum(D), jejunum(J) and ileum(I) were employed for the calculation of apparent permeability(Pe) and apparent first-order rate constant(Kobs). respectively. The results of this study were as follows; (1) Itraconazole showed appreciable aqueous solubility only at pH values of below 2.0. (2) pe(cm/sec) decreased in the following order: $D(10.24{\pm}1.78{\times}10^{-4})>J(8.86{\pm}0.79{\times}10^{-4})>I(3.78{\pm}0.13 X 10^{-4})$. (3) $Kobs(min^{-1})$ decreased in the following order: $J(17.12{\pm}3.19{\times}10^{-3})>D(13.37{\pm}0.6{\times}10^{-3})>I(11.05{\pm}0.91{\times}10^{-3})$. (4) The solubility of itraconazole markedly increased with the increase of the concentration of sodium cholate. (5) The addition of 10 mM sodium cholate significantly increased the apparent first-order rate constant of itraconazole in the ileum by a factor of 6.8.

• Korean Institute of Interior Design Journal
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• v.19 no.4
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• pp.82-89
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• 2010

The studies published up to now, related to the correlation between spatial structure and visitors' behavior in a museum are rather relatively lacking when it comes to the in-depth consideration for the effect of the actual exhibition environment. So the main purpose of this study is to define the correlation between the light environment and the visitors' behavior. Towards this end, this study uses 'space syntax' to quantify the spatial structure with 'integration', 'connectivity' and 'control value'. Meanwhile, 'tracking score' and 'tracking frequency' were selected as the scope among the indices of behavior's analysis. The results of this study are as follows; First, integration and correlation of tracking score and tracking frequency are lowest when it comes to the extra large historical museums where the difference of intensity of illumination by each convex space. Meanwhile, the most considerable effect is exerted by control value. Compared to tracking score, tracking frequency is closely related to 'syntactic variables'. Second, visitors do not take the short cut the dark exhibition space even when very dark exhibition spaces continue after passing through relatively bright space. Analysis of visitors' behavior by control value in the exhibition space composed of this type of intensity of illumination environment is not valid. Third, visitors move to relatively brighter transitional space compared to the exhibition space with low intensity of illumination when passing through dark exhibition continually. Meanwhile, when visitors pass through the exhibition space there is some difference intensity of illumination they move to relatively dark exhibition center among the subsequent exhibition spaces. Accordingly, when the composition of exhibition space that continues onto the environment of low intensity of illumination is inevitable, differentiating intensity of illumination appropriately would be effective in inducing visit to the subsequent exhibition space.