• Journal of Pharmaceutical Investigation
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• 제27권4호
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• pp.271-277
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• 1997

Because omeprazole(OMP) is very unstable in aqueous condition, $OMP-{\beta}-CD$, the inclusion complex of OMP and ${\beta}-cyclodextrin({\beta}-CD)$ was made and physicochemical properties of it were compared with those of OMP. Skin permeability of OMP and $OMP-{\beta}-CD$ in propylene glycol vehicle and the reciprocal action of ${\beta}-CD$ with various enhancers were examined through hairless mouse. Adhesive patches were prepared with polyisobutylene and the skin permeability and stability of OMP were investigated. The inclusion complex showed higher solubility and lower partition coefficient than OMP itself. DMSO, 1-methyl 2-pyrrolidone and sodium cholate had an enhancing effect. However ethanol and polysorbate 80 hardly showed the enhancing effect of OMP. When sodium lauryl sulfate and sodium cholate as enhancer were added in patch, the former case showed higher permeability of OMP.

• Journal of Pharmaceutical Investigation
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• 제37권3호
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• pp.159-166
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• 2007

In order to develop an optimum formulation for iontophoretic delivery of vitamine C-2-phosphate (VCP) from Carbopol hydrogel, we have investigated various factors which can affect the iontophoretic flux through skin. Such factors as drug concentration, current density, current profile, current duration, ionic strength, pH and percutaneous enhancers (ethanol, glycerine, propylene glycerol, sorbitol, urea) were studied. Compared to the flux by passive or anodal delivery, the flux by cathodal delivery increased markedly, and thus, only cathodal delivery was used in the rest of the flux experiments. Flux increased linearly as the drug concentration and current density increased. As the duration of current application increased from 30 min to 120 min, flux increased linearly, however the AUC was not directly proportional to the applied amount of current. Flux also increased as the pH increased, possibly due to the increase in ionization of phosphate group. As the ionic strength increased, flux decreased. No significant increase in flux was observed after enhancer application, indicating that the effect of current on flux is dominating over the effect of percutaneous enhancers (P>0.05). These results provide important informations that are needed for optimal formulation of iontophortic delivery for VCP.

• Journal of Pharmaceutical Investigation
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• 제39권1호
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• pp.19-21
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• 2009

This study was performed to examine the possibility of increasing the level of furosemide permeation from the ethylene-vinyl acetate (EVA) matrix through the skin by incorporating various enhancers in the EVA matrix. The effects of the enhancers on the level of furosemide permeation through the skin were evaluated using Franz diffusion cells with intact excised rat skins. The enhancers examined were the fatty acids (saturated, unsaturated), the pyrrolidones, the propylene glycol derivatives, the glycerides and the non-ionic surfactants. Among the enhancers used, polyoxyethylene-2-oleyl ether (a non-ionic surfactant) showed the best enhancement. The polyoxyethylene 2-oleyl ether as a permeation enhancer could be used for development of furosemide-EVA transdermal matrix system.

• Journal of Pharmaceutical Investigation
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• 제29권2호
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• pp.137-143
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• 1999

Ketoprofen together with various permeation enhancers was incorporated into a novel soft hydrogel which is semi-solid in a container and to form a thin film within a few minutes after applying on the skin. The effect of various enhancers on the skin permeation of ketoprofen from a soft hydrogel was investigated using in vitro and in vivo method. In vitro rat skin permeation of ketoprofen from soft hydrogel was conducted using modified Keshary-Chien diffusion cells. In vivo ketoprofen absorption was also investigated in rats, and the results were compared with that of commercial products. Anti-inflammatory activities were determined using carrageenan-induced paw edema method and adjuvant-induced arthritis method in rats. The anti-inflammatory activity of ketoprofen soft hydrogel formulation with that of commercial products were compared. In vitro as well as in vivo studies showed that $HPE-101^{\circledR}$ was the most effective skin permeation enhancer among those used in this study. Addition of an adhesive (polyisobutylene) in the soft hydrogel decreased skin permeation of ketoprofen. Paw edema and anti-arthritis tests showed that soft hydrogel containing $HPE-101^{\circledR}$ was more effective than the commercial products, which was consistent with the in vivo absorption experiment results.

• Journal of Pharmaceutical Investigation
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• 제40권1호
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• pp.33-38
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• 2010

Sibutramine is a serotonin-norepinephrine reuptake inhibitor indicated for the management of obesity in conjunction with a reduced calorie diet. The oral administration of sibutramine is followed by its dose-related side effects. In this study, sibutramine was formulated into drug in adhesive (DIA) patches in an attempt to overcome these problems. The effects of different formulation variables including pressure-sensitive adhesive (PSA), loading amount of drug, thickness of matrix and enhancer on the skin permeation of the drug were evaluated using excised hairless mouse skin. In the acrylic adhesive with carboxyl functional group, low release of sibutramine was observed due to the strong interaction between carboxyl group of adhesive and amine group of sibutramine. The acrylic adhesive without functional group provided good adhesion force and allowed high drug loading. Changing drug load as well as thickness of the matrix was found to alter permeation rate. $Crovol^{(R)}$ PK40 and $Crovol^{(R)}$ A40, were found to be effective enhancers for sibutramine. The optimized patch contained 20% sibutramine, and 5% $Crovol^{(R)}$ A40 as permeation enhancer, in $80\;{\mu}m$ thick Duro-$Tak^{(R)}$ 87-9301 matrix.

• Asian Pacific Journal of Cancer Prevention
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• 제16권15호
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• pp.6545-6548
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• 2015

Background: Synovial sarcoma is a mesenchymal neoplasm that accounts for around 10% of all soft tissue sarcomas. The diagnosis of synovial sarcoma can be a challenging task, particularly with small biopsy specimens. Aim: We investigated transducer-like enhancer of split 1 (TLE1), monoclonal antibody, expression by immunohistochemical analysis in a group of 74 synovial sarcoma cases, 20 cases of MPNST, 12 cases of neurofibroma, 15 cases of schwannoma, 5 cases of MFH, 10 cases of lieomyosarcoma and 10 cases of solitary fibrous tumor. Materials and Methods: Whole tissue sections were examined: (39 biphasic and 35 monophasic). Nuclear immunoreactivity was scored as negative (<5% of cells positive), 1+(mild /5-25%), 2+ (moderate/25-50%), and 3+ (strong >50%). Results: Overall, 71 (96%) of 74 synovial sarcomas were positive for TLE1, including 37 biphasic (95%) and 34 monophasic (97%) tumors. Other spindle cell tumors showed very low or absent staining of TLE1. Conclusions: We conclude that TLE1 is a sensitive marker and can be a useful diagnostic marker for synovial sarcoma, particularly the monophasic forms.

• 한국공작기계학회:학술대회논문집
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• 한국공작기계학회 2004년도 추계학술대회 논문집
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• pp.86-91
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• 2004

It is very important to detect the bearing defects in rotating machinery since the critical failure of bearing cause a machinery shutdown. However it is difficult to detect the vibration signal resulting from the initial defects of bearing because of the high level of broadband noise. A signal processing technique, called the adaptive line enhancer(ALE) as one of adaptive filter, is studied in this work. This technique is to eliminate broadband noise without a prior knowledge of the noise and signal characteristics. Also we propose the optimal methods for selecting the three main ALE parameters such as correlation length, filter order and adaptation constant used in the adaptative process. Vibration signals for three abnormal bearings, including inner and outer raceways and ball defects, were acquired from Anderon(angular derivative of radius on)meter. The experimental results showed that the proposed technique can reliably detect the bearing defective signals masked by broadband noise.

• 대한기계학회논문집A
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• 제21권2호
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• pp.281-287
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• 1997

In the conventional inverse modeling method for on-line modeling of the secondary path transfer function, the signal to noise ratio between the arbitrary random signal and the plant noise have to keep at -10 - -20 dB. For these reasons, the modeling can't be exactly implemented by the conventional method alone and the convergence time for modeling becomes too long. In this study, by combining the conventional inverse modeling method with an adaptive line enhancer, or with an adaptive noise canceller, a rigorous transfer functions of secondary path modeling and the control of a primary noise have been implemented simultaneously.

• Molecules and Cells
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• 제26권3호
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• pp.291-298
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• 2008

Human karyopherin ${\beta}3$, highly homologous to a yeast protein secretion enhancer (PSE1), has often been reported to be associated with a mediator of a nucleocytoplasmic transport pathway. Previously, we showed that karyopherin ${\beta}3$ complemented the PSE1 and KAP123 double mutant. Our research suggested that karyopherin beta has an evolutionary function similar to that of yeast PSE1 and/or KAP 123. In this study, we performed yeast two-hybrid screening to find a protein which would interact with karyopherin ${\beta}3$ and identified apolipoprotein A-I (apo A-I), a secretion protein with a primary function in cholesterol transport. By using in vitro binding assay, co-immunoprecipitation, and colocalization studies, we defined an interaction between karyopherin ${\beta}3$ and apo A-I. In addition, overexpression of karyopherin ${\beta}3$ significantly increased apo A-I secretion. These results suggest that karyopherin ${\beta}3$ plays a crucial role in apo A-I secretion. These findings may be relevant to the study of a novel function of karyopherin ${\beta}3$ and coronary artery diseases associated with apo A-I.

• 약학회지
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• 제43권4호
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• pp.447-457
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• 1999

The purpose of this study is to prepare the adhesive type patch containing flurbiprofen, and to demonstrate the feasibility of flurbiprofen administration through the intact skin using adhesive type patch preparation. For this purpose, two pressure sensitive adhesives, Polyisobutylene(PIB) and $Gelva^{\circledR}737$, were selected from the chemical grade of polymers, and the adhesive type patches of flurbiprofen were prepared. The release rate of flurbiprofen from the PIB-based adhesive patch was higher than that from $Gelva^{\circledR}737$ based adhesive patch. The release rate of flurbiprofen from the PIB-based A-type patch with 1.0mm, 1.5mm or 2.0mm thicknesses followed the first order kinetics. In the skin permeation study, using male hairless mouse skin, a monophasic skin permeation profile was observed with 1% flurbiprofen loading dose. The inclusion of palmitic acid or SLS(0.25~0.5%) as an enhancer produced a remarkable enhancement in the skin permeation rate of flurbiprofen, and the percentile ratio of drug and enhancer appeared to be important for the effective enhancement. In the in vivo percutaneous absorption study, the plasma concentration of the optimal formulation was significantly (p<0.01) higher than that of the conventional cataplasma ($Bifen^{\circledR}$). These studies demonstrate a good feasibility of flurbiprofen administration through the intact skin using a transdermal patch, and show a possibility of the development of flurbiprofen patches.