• Archives of Pharmacal Research
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• v.13 no.2
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• pp.151-160
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• 1990

In order to develop a controlled-release oral drug delivery system (DDS) which sustains the plasma acetaminophen (AAP) concentration for a certain period of time, microporous membrane-coated tablets were prepared and evaluated in vitro. Firstly, highly water-soluble core tablet of AAP were prepared with various formulations by wet granulation and compression technique. Then the core tablets were coated with polyvinychloride (PVC) in which micronized sucrose particles were dispersed. Effect of formula compositions of core tablets and coating suspensions on the pharmaceutical characteristics such as drug release kinetics and membrane stability of the coated tablets was investigated in vitro. AAP was released from the coated tablets as a zero-order rate in a pH-independent manner. This independency of AAP release to pH change from 1.2 to 7.2 is favorable for the controlled oral drug delivery, since it will produce a constant drug release in the stomach and intestine regardless of the pH change in the GI tract. Drug release could be extended upto 10 h according to the coating condition. The release rate could be controlled by changing the formula compositions of the core tablets and coating suspensions, coat weight per each tablet, and especially PVC/sucrose ratio and particle size of the sucrose in the coating suspension. The coated tablets prepared in this study had a fairly good pharmaceutical characteristics in vitro, however, overall evaluation of the coated tablet should await in vivo absorption study in man.

• Journal of Korean Neurosurgical Society
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• v.46 no.3
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• pp.245-251
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• 2009

Objective : The authors analyzed the effectiveness and therapeutic response of Novalis shaped beam radiosurgery for metastatic brain tumors, and the prognostic factors which influenced the outcome. Methods : We performed a retrospective analysis of 106 patients who underwent 159 treatments for 640 metastatic brain lesions between January 2000 and April 2008. The pathologies of the primary tumor were mainly lung (45.3%), breast (18.2%) and GI tract (13.2%). We classified the patients using Radiation Therapy Oncology Group Recursive Partitioning Analysis (RPA) and then analyzed the survival and prognostic factors according to the Kaplan Meier method and univariate analysis. Results : The overall median actuarial survival rate was 7.3 months from the time of first radiosurgery treatment while 1 and 2 year actuarial survival estimates were 31% and 14.4%, respectively. Median actuarial survival rates for RPA classes I, II, and III were 31.3 months, 7.5 months and 1.7 months, respectively. Patients' life spans, higher Karnofsky performance scores and age correlated closely with RPA classes. However, sex and the number of lesions were not found to be significantly associated with length of survival. Conclusion : This result suggests that Novalis radiosurgery can be a good treatment option for treatment of the patients with brain metastases.

• Journal of The Korean Society of Clinical Toxicology
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• v.9 no.1
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• pp.34-38
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• 2011

Vinegar is a very popular ingredient used in many cuisines. It is also known for its beneficial health, beauty and possible weight-loss properties. The authors report on a patient who presented to the emergency department with unstable vital signs complaining of generalized abdominal pain after ingestion of 450 ml of apple cider vinegar. We documented a case of corrosive gastrointestinal injury with persistent metabolic acidosis occurring after ingesting apple cider vinegar with an acetic acid concentration of 12~14%. Toxic damage to the liver and kidney were also observed, peaking on post-ingestion day 3. The patient received supportive care and hemoperfusion for three days without much clinical improvement and died in the seventh day of intensive care due to disseminated intravascular coagulation and multi organ failure. Edible vinegar, when taken in large amounts, is capable of inducing corrosive injuries of the GI tract as well as severe systemic toxicities, such as metabolic acidosis. Safety precautions regarding vinegar deserve more public attention and clinicians also should be astute enough to recognize the potential damage accompanying vinegar ingestion.

• Journal of Korea Game Society
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• v.15 no.4
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• pp.19-28
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• 2015

According to the Infant Educational Law, learning of the children are encouraged through playing, but there are not many tools to learn. Educational Serious Game is a game developed for the purpose of learning. And so, in this paper, we produced serious games for education learning for young children. Contents of the game is the digestive system. And we utilized touch and drag which are kinds of intuitive interface of the mobile platform being able to play easy. At the end of each stage, and it contained a scene that can learn the characteristics of the digestive system. After producing this game, we supplemented something that is inadequate through testing. In addition, the learning effect of the game was confirmed by interviews with the teachers. We hope this will be a fun and informative game for the digestive tract to the children.

• Asian-Australasian Journal of Animal Sciences
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• v.18 no.8
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• pp.1141-1146
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• 2005

A trial was conducted to evaluate the level of wheat substituted for corn in a traditional corn-soy diet and the xylanase supplementation effect on the growth performance and nutrient digestion of broiler chickens. This experiment was a randomized design with a 4${\times}$2 factorial arrangement with four levels of wheat substitution and two levels of enzyme inclusion in the diet. Wheat replaced 0, 25, 50 or 100% corn with or without 1 g/kg xylanase supplementation in iso-nitrogenous and iso-calorific experimental diets. The results showed that in the growing period, broilers attained the highest (p<0.05) body weight gain, feed intake, and relative small intestine weight when wheat was substituted at 25% for corn. The relative caecum weight increased (p<0.05) linearly with increasing levels of wheat substitution for corn. However, during the finishing period and entire experimental period from 0 to 6 weeks, no significant difference was shown in the growth performance among all treatments. Xylanase inclusion significantly improved the body weight gain, fat availability (p<0.01) and diet metabolisable energy (p<0.1) but decreased (p<0.05) the relative GI tract weight during the growing period. The digesta viscosity of 6-week old broilers was also decreased (p<0.05). It appears that wheat substituted for corn did not affect the growth performance, nutrient digestion, and the digesta viscosity of chickens. It is acceptable to completely substitute wheat for corn. Xylanase supplementation improved performance.

• Journal of Acupuncture Research
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• v.17 no.2
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• pp.261-276
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• 2000

본 실험은 pseudorabies 바이러스 (PRV) 의 Bartha strain 을 안면신경의 측두지, 하지를 지배하는 신경 (좌골신경) 및 상지를 지배하는 신경 (요골, 척골, 정중신경) 에 주입한 후 4 일간의 생존시간이 경과한 후 척수와 뇌를 적출하여 동결절편을 제작한 후 면역조직화학적 염색기법과 X-gal 조직화학 염색법을 시행하여 염색된 신경세포체를 척수와 뇌에 투사된 공통영역을 관찰하고 두침의 영역중 하나인 운동구와 사지와의 관계에 대한 실험적 증거를 제시하고자 시행하였다. 위의 실험에서 얻어진 결과는 아래와 같다. 1. 안면신경의 측두지, 하지를 지배하는 신경 (좌골신경) 및 상지를 지배하는 신경 (요골, 측골, 정중신경) 에서 투사된 공통된 영역은 척수에서 경수의 층판 1-IV, 흉수의 intermediolateral nucleus(IML), dorsal nucleus(D) 및 층판 X, 요수의 층판 IV, V, 천수의 층판 IV, V, IX, X 등의 영역에서 관찰되었고, 뇌줄기에서는 caudoventrolateral reticular nucleus(CVL), nucleus solitary tract(Sol), rostroventrolateral nucleus(RVL), area postrema(AP), raphe nuclei(raphe pallidus, raphe obscurus, raphe magnus), inferior olivary nucleus 의 등쪽부분 (gigantocellular reticular nucleus, Gi), Kolliker-Fuse nucleus(KF), central gray(CG), dorsal raphe nucleus (DR) and A5 영역에 표지된다. 또한 paraventricular hypothalamic nucleus(PRV) 와 lateral hypothalamic reticular nucleus(LH)에서도 관찰되고 locus coeruleus(LC) 와 subcoeruleus nuc!eus(SubCA) 에서도 관찰된다.

• Molecules and Cells
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• v.41 no.6
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• pp.532-544
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• 2018

Gastrointestinal stromal tumours (GIST) are the most common mesenchymal tumors of the gastrointestinal (GI) tract. In order to investigate a new treatment fot GIST, we hypothesized the effect of miR-374b targeting PTEN gene-mediated PI3K/Akt signal transduction pathway on proliferation and apoptosis of human gastrointestinal stromal tumor (GIST) cells. We obtained GIST tissues and adjacent normal tissues from 143 patients with GIST to measure the levels of miR-374b, PTEN, PI3K, Akt, caspase9, Bax, MMP2, MMP9, ki67, PCNA, P53 and cyclinD1. Finally, cell viability, cell cycle and apoptosis were detected. According to the KFGG analysis of DEGs, PTEN was involved in a variety of signaling pathways and miRs were associated with cancer development. The results showed that MiR-374b was highly expressed, while PTEN was downregulated in the GIST tissues. The levels of miR-374b, PI3K, AKT and PTEN were related to tumor diameter and pathological stage. Additionally, miR-374b increased the mRNA and protein levels of PI3K, Akt, MMP2, MMP9, P53 and cyclinD1, suggesting that miR-374b activates PI3K/Akt signaling pathway in GIST-T1 cells. Moreover, MiR374b promoted cell viability, migration, invasion, and cell cycle entry, and inhibited apoptosis in GIST cells. Taken together, the results indicated that miR-374b promotes viability and inhibits apoptosis of human GIST cells by targeting PTEN gene through the PI3K/Akt signaling pathway. Thus, this study provides a new potential target for GIST treatment.

• Journal of Pharmaceutical Investigation
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• v.37 no.6
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• pp.339-347
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• 2007

SMEDDS is mixture of oils, surfactants, and cosurfactants, which are emulsified in aqueous media under conditions of gentle agitation and digestive motility that would be encountered in the gastro-intestinal(GI) tract. The main purpose of this work is to prepare self-microemulsifying drug delivery system(SMEDDS) for oral bioavailability enhancement of a poorly water soluble drug, atorvastatin calcium. Solubility of atorvastatin calcium was determined in various vehicles. Pseudo-ternary phase diagrams were constructed to identity the efficient self-emulsification region and particle size distributions of the resultant micro emulsions were determined using a laser diffraction sizer. Optimized formulations for in vitro dissolution and bioavailability assessment were $Capryol^{(R)}$ 90(50%), Tetraglycol(16%), and $Cremophor^{(R)}$ EL(32%). The release rate of atorvastatin from SMEDDS was significantly higher than the conventional tablet ($Lipitor^{(R)}$), 2-fold. Our studies illustrated the potential use of SMEDDS for the delivery of hydrophobic compounds, such as atorvastatin calcium by the oral route.

• Archives of Pharmacal Research
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• v.26 no.9
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• pp.768-772
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• 2003

Tween 80 (Polysorbate 80) is a hydrophilic nonionic surfactant commonly used as an ingredient in dosing vehicles for pre-clinical in vivo studies (e.g., pharmacokinetic studies, etc.). Tween 80 increased apical to basolateral permeability of digoxin in Caco-2 cells suggesting that Tween 80 is an in vitro inhibitor of P-gp. The overall objective of the present study was to investigate whether an inhibition of P-gp by Tween 80 can potentially influence in vivo absorption of P-gp substrates by evaluating the effect of Tween 80 on the disposition of digoxin (a model P-gp substrate with minimum metabolism) after oral administration in rats. Rats were dosed orally with digoxin (0.2 mg/kg) formulated in ethanol (40％, v/v) and saline mixture with and without Tween 80 (1 or 10％, v/v). Digoxin oral AUC increased 30 and 61％ when dosed in 1 ％ and 10％ Tween 80, respectively, compared to control (P＜0.05). To further examine whether the increase in digoxin AUC after oral administration of Tween 80 is due, in part, to a systemic inhibition of digoxin excretion in addition to an inhibition of P-gp in the GI tract, a separate group of rats received digoxin intravenously (0.2 mg/kg) and Tween 80 (10％ v/v) orally. No significant changes in digoxin IV AUC was noted when Tween 80 was administered orally. In conclusion, Tween 80 significantly increased digoxin AUC and Cmax after oral administration, and the increased AUC is likely to be due to an inhibition of P-gp in the gut (i.e., improved absorption). Therefore, Tween 80 is likely to improve systemic exposure of P-gp substrates after oral administration. Comparing AUC after oral administration with and without Tween 80 may be a viable strategy in evaluating whether oral absorption of P-gp substrates is potentially limited by P-gp in the gut.

• Journal of Radiation Industry
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• v.12 no.4
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• pp.355-363
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• 2018

A novel $N_3S_1$ chelate, Pro-Lys-Cys (PKC) to cyclic RGD to radiolabel with $^{99m}Tc$ was conjugated in an effort to decrease the high intestinal accumulation observed for $^{99m}Tc$-labeled PGC-RGD. The target specificity of the resulting PKC-RGD was similar to that of PGC-RGD as determined by a cell binding assay and a competition binding assay. The $^{99m}Tc$ radiolabeling of PKC-RGD resulted in radiochemical yields of 98% under mild conditions at high specific activities. Biodistribution data in normal mice clearly showed a significant decrease in intestinal uptake at 2 h postinjection for the $^{99m}Tc-PKC-c$ (RGDyK) compared to the $^{99m}Tc-GC-c$ (RGDyK) (from $19.65%ID{\cdot}g^{-1}$ to $7.31%ID{\cdot}g^{-1}$ for the GI tract). The $^{99m}Tc-PKC-c$ (RGDyK) biodistribution was also shown by a higher retention of radioactivity in the whole body, but with kidney accumulation over 8-fold higher than observed with $^{99m}Tc-PGC-c$ (RGDyK) at 2 h ($12.62%ID{\cdot}g^{-1}$ for PKC-RGD and $1.54%ID{\cdot}g^{-1}$ for PGC-RGD, respectively). These results show that the biodistribution may be altered especially concerning lipophilicity resulting in renal rather than hepatobiliary excretion. This comparative study made it possible to explore the effects of lipophilicity on the biodistribution of $^{99m}Tc$-labeled c (RGDyK) through the use of different tripeptide $N_3S_1$ chelators. Therefore, $^{99m}Tc-PKC-c$ (RGDyK) may be an attractive alternative for the in vivo imaging of integrin receptors.