• Title/Summary/Keyword: Site release

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Enhanced Transdermal Delivery of Pranoprofen from the Bioadhesive Gels

  • Shin, Sang-Chul;Cho, Cheong-Weon
    • Archives of Pharmacal Research
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    • v.29 no.10
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    • pp.928-933
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    • 2006
  • Percutaneous delivery of NSAIDs has advantages of avoiding hepatic first pass effect and delivering the drug for extended period of time at a sustained, concentrated level at the inflammation site that mainly acts at the joint and the related regions. To develop the new topical formulations of pranoprofen that have suitable bioadhesion, the gel was formulated using hydroxypropyl methylcellulose (HPMC) and poloxamer 407. The effects of temperature on drug release was performed at $32^{\circ}C$, $37^{\circ}C$ and $42^{\circ}C$ according to drug concentration of 0.04%, 0.08%, 0.12%, 0.16%, and 0.2% (w/w) using synthetic cellulose membrane at $37{\pm}0.5^{\circ}C$. The increase of temperature showed the increased drug release. The activation energy (Ea), which were calculated from the slope of lop P versus 1000/T plots was 11.22 kcal/ mol for 0.04%, 10.79 kcal/mol for 0.08%, 10.41 kcal/mol for 0.12% and 8.88 kcal/mol for 0.16% loading dose from the pranoprofen gel. To increase the drug permeation, some kinds of penetration enhancers such as the ethylene glycols, the propylene glycols, the glycerides, the non-ionic surfactants and the fatty acids were incorporated in the gel formulation. Among the various enhancers used, propylene glycol mono laurate showed the highest enhancing effects with the enhancement factor of 2.74. The results of this study suggest that development of topical gel formulation of pranoprofen containing an enhancer is feasible.

The cytokine-inducing activities of surface components of the periodontopathogenic bacterium Porphyromonas gingivalis (Porphyromonas gingivalis의 각종 표면성분이 싸이토카인 형성에 미치는 영향)

  • Kim, Sung-Jo
    • Journal of Periodontal and Implant Science
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    • v.35 no.3
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    • pp.799-811
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    • 2005
  • This study was carried out to examine the potency of the three surface compo- nents from Porphyromonas gingivalis to stimulate the murine macrophage cell line RAW264.7 to synthesize the pro-inflammatory cytokine tumor necrosis factor alpha($TNF-{\alpha}$) and nitric oxide (NO). Lipopolysaccharide(LPS). lipid A-associated proteins(LAP) and saline-extractable surface -associated material(SAM) were isolated from P. gingivalis 381. $TNF-{\alpha}$ release into culture supernatants was determined by two-site ELISA. NO production was assayed by measuring the accumulation of nitrite in culture supernatants. Western blot analysis of iNOS and analysis of reverse transcription(RT)-PCR products were carried out. The surface components extracted from this bacterium were almost equally potent in stimulating release of $TNF-{\alpha}$ and NO by RAW264.7 cells. $TNF-{\alpha}$ that was being measured immunologically was due to activation of $TNF-{\alpha}$ gene transcription. The present study clearly shows that P. gingivalis surface components fully induced iNOS expression in RAW264.7 cells in the absence of other stimuli. The ability of P. gingivalis surface components to promote the production of $TNF-{\alpha}$ and NO may be important in the pathogenesis of inflammatory periodontal disease.

A Study on the Improvement of Classification of Explosion Hazardous Area using Hypothetic Volume through Release Characteristic (누출특성을 통한 폭발위험장소 선정방법의 개선에 대한 연구)

  • Kim, Dae-Yeon;Chon, Young-Woo;Lee, Ik-Mo;Hwang, Yong-Woo
    • Journal of the Korea Safety Management & Science
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    • v.19 no.2
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    • pp.31-39
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    • 2017
  • Classify of explosion hazardous areas must be made at the site where flammable materials are used. This reason is that it is necessary to manage ignition sources in of explosion hazardous areas in order to reduce the risk of explosion. If such an explosion hazard area is widened, it becomes difficult to increase the number of ignition sources to be managed. The method using the virtual volume currently used is much wider than the result using CFD(Computational Fluid Dynamics). Therefore, we tried to improve the current method to compare with the new method using leakage characteristics. The result is a realistic explosion hazard if the light gas is calibrated to the mass and the heavy gas is calibrated to the lower explosion limit. However, it is considered that the safety factors should be taken into account in the calculated correction formula because such a problem should be considered as a buffer for safety.

Clinical Analysis of Cases of Segmental Resection and Primary Anastomosis in Tracheal Stenosis (기관 절제 및 단단 문합술에 의한 기관 협착증의 치료)

  • 신호승;김영민
    • Korean Journal of Bronchoesophagology
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    • v.4 no.1
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    • pp.27-34
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    • 1998
  • Despite improvement in respiratory care, including use of low pressure and high volume cuffed tubes, tracheal stenosis remains a serious complication after a long-term tracheal intubation and tracheostomy. In such patients, tracheal resection and primary anastomosis is still considered ideal therapeutic modality. Between 1989 and 1997, we performed tracheal resections with end-to-end anastomosis on 14 patients with no operative mortality and some morbidity. Tracheal stenosis was caused by tracheostomy in nine patients, by endotracheal intubation in three patients and by thyroid carcinoma in two patients. The length of stenosis was various from 2cm to 4.5cm. All patient underwent segmental tracheal resection and primary anastomosis(14 patients) and additional procedures were cricoid cartilage reconstruction(2 patients), suprahyoid laryngeal release(3patients), carinal release technique(2 patients) and arytenoidectomy(2 patients). We have nine complications: granulona at anastomosis site in four patients, vocal cord palsy in two patients and restenosis, pneumonia, skin necrosis in each of those patients. The granuloma was removed by bronchoscopic forceps(4 patients). Vocal cord palsy was treated by arytenoidectorny(2 patients), restenosis by T-tube insertion, pneumonia by antibiotics and skin necrosis was treated by skin graft. We reviews our expenence of clinical features of tracheal stenosis and surgical treatment by tracheal one-to-end anastomosis with additional procedures to avoid postoperative complications for sucessful results.

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Effect of Encapsulating Nitrate in Sesame Gum on In vitro Rumen Fermentation Parameters

  • Mamvura, Chiedza Isabel;Cho, Sangbuem;Mbiriri, David Tinotenda;Lee, Hong-Gu;Choi, Nag-Jin
    • Asian-Australasian Journal of Animal Sciences
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    • v.27 no.11
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    • pp.1577-1583
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    • 2014
  • Encapsulation is a method used to protect material from certain undesirable environments, for controlled release at a more favorable time and place. Animal productivity would be enhanced if feed additives are delivered to be utilized at their site of action, bypassing the rumen where they are likely to be degraded by microbial action. A novel method of encapsulation with sesame gum was used to coat nitrate, a known enteric methane mitigating agent, and tested for the effect on methane reduction and other in vitro fermentation parameters using rumen fluid from cannulated Hanwoo steers. Orchard grass was used as basal diet for fermentation. The treatments were matrix (1.1 g sesame gum+0.4 g sesame oil cake) only, encapsulated nitrate (matrix+nitrate [21 mM]), free nitrate (21 mM), and a control that contained no additive. Analyses of fermentation parameters were done at 0, 3, 6, 9, 12, 24, and 48 h time periods. In comparison to control, both free and encapsulated nitrate produced significantly reduced (p<0.01) methane (76% less) and also the total volatile fatty acids were reduced. A significantly higher (p<0.01) concentration of ammonia nitrogen was obtained with the encapsulated nitrate treatment (44%) compared to the free form (28%) and matrix only (20%) (p = 0.014). This might suggest slow release of encapsulated nitrate so that it is fully reduced to ammonia. Thus, this pioneering study found a significant reduction in methane production following the use of sesame gum encapsulated nitrate that shows the potential of a controlled release system in enhancing sustainability of ruminant production while reducing/eliminating the risk of nitrite toxicity.

Analysis of Gas Flow Behavior with Experiments for LPG releasing and 3D Mapping of Gas Sensor (LPG 누출 및 가스센서 3D Mapping을 통한 가스유동현상 분석)

  • Kim, Jeong Hwan;Lee, Min-Kyung;Kil, Seong-Hee;Lee, Jin-han;Jo, Young-do;Moon, Jong-Sam
    • Journal of the Korean Institute of Gas
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    • v.21 no.5
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    • pp.45-55
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    • 2017
  • Release and fire/explosion tests of flammable gas are extremely dangerous. Furthermore, it is difficult to select the site where the experiment can be performed. In these reasons, gas flow analysis(CFD) has been used as much as possible. However, with the opening of the Energy Safety Empirical Research Center in Yeongwol-gun, Gangwon-do in October 2016, it was possible to conduct releases and detection tests of small scale combustible gas as well as large scale / high pressure / ultra low temperature experiments. In this study, LPG leaked after the calibration and placement of the sensor, the sensor detected LPG and the data were visualized as a contour map. And the differences between the actual release(28s, max 3.7[m]) and the analysis were analyzed compared to the FLACS analyzed under the same conditions.

Induced Death of Escherichia coli Encapsulated in a Hollow Fiber Membrane as Observed In Vitro or After Subcutaneous Implantation

  • Granicka, L. H.;Zolnierowicz, J.;Wasilewska, D.;Werynski, A.;Kawiak, J.
    • Journal of Microbiology and Biotechnology
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    • v.20 no.1
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    • pp.224-228
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    • 2010
  • The encapsulation of bacteria may be used to harness them for longer periods of time in order to make them viable, whereas antibiotic treatment would result in controlled release of therapeutic molecules. Encapsulated Escherichia coli GFP (green fluorescent protein) (E. coli GFP) was used here as a model for therapeutic substance - GFP fragments release (model of bioactive substances). Our aim was to evaluate the performance of bacteria encapsulated in hollow fibers (HFs) treated with antibiotic for induction of cell death. The polypropylene-surface-modified HFs were applied for E. coli encapsulation. The encapsulated bacteria were treated with tetracycline in vitro or in vivo during subcutaneous implantation into mice. The HF content was evaluated in a flow cytometer, to assess the bacteria cell membrane permeability changes induced by tetracycline treatment. It was observed that the applied membranes prevented release of bacteria through the HF wall. The E. coli GFP culture encapsulated in HF in vitro proved the tetracycline impact on bacteria viability and allows the recognition of the sequence of events within the process of bacteria death. Treatment of the SCID mice with tetracycline for 8 h proved the tetracycline impact on bacteria viability in vivo, raising the necrotic bacteria-releasing GFP fragments. It was concluded that the bacteria may be safely enclosed within the HF at the site of implantation, and when the animal is treated with antibiotic, bacteria may act as a local source of fragments of proteins expressed in the bacteria, a hypothetical bioactive factor for the host eukaryotic organism.

Preparation of Dexamethasone-21-palmitate Incorporated Lipid Nanosphere: Physical Properties by Varying Components and Ratio of Lipid (팔미틴산덱사메타손이 봉입된 지질나노입자의 제조: 지질종류와 함량에 따른 물리적 특성)

  • Jung, Suk-Hyun;Lee, Jung-Eun;Seong, Ha-Soo;Shin, Byung-Cheol
    • Journal of Pharmaceutical Investigation
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    • v.36 no.6
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    • pp.355-361
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    • 2006
  • Intraarticular corticosteroid injections for therapy of rheumatic arthritis are administered with the aim of optimal local anti-inflammatory effect at the injection site. Since the side effects of corticosteroidal drug, dexamethasone(DEX), administered at hish dose limited the therapeutic efficacy, there was a need to design a new drug delivery system for controlled release of dexamethasone. As a prodrug for continuous therapeutic efficacy, dexamethasone-21-palmitate(DEX-PAL) was prepared via esterification of palmitoyl chloride and dexamethasone. DEX-PAL was identified by NMR and MASS analysis. DEX-PAL or DEX was entrapped in lipid nanosphere which could be prepared by using a self emulsification-solvent evaporation method. Physicochemical characteristics such as mean particle diameter, zeta potential and drug loading efficiency of the lipid nanospheres were investigated with variation of either the kind of lipid or the lipid composition. The lipid nanospheres had a mean diameter $83{\sim}95$ nm and DEX-PAL loading efficiency of up to 95%. The drug loading efficiency increased with the increase of aliphatic chain length attached to the phospholipid. The incorporation of cationic lipid was very efficient for both reducing particle size of lipid nanospheres and enhancing drug loading efficiency. The lipid nanospheres containing DEX-PAL may be a promising novel drug carrier for the controlled release of the poorly water-soluble drugs.

Roles of ERK and NF-${\kappa}$ B in Interleukin-8 Expression in Response to Heat Shock Protein 22 in Vascular Smooth Muscle Cells

  • Kang, Seung-Hun;Lee, Ji-Hyuk;Choi, Kyung-Ha;Rhim, Byung-Yong;Kim, Koan-Hoi
    • The Korean Journal of Physiology and Pharmacology
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    • v.12 no.4
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    • pp.171-176
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    • 2008
  • Heat shock proteins (HSPs) serve as molecular chaperones and play a role in cell protection from damage in response to stress stimuli. The aim of this article is to investigate whether HSP22 affects IL-8 expression in vascular smooth muscle cells (VSMCs), and which cellular factors are involved in the HSP-mediated IL-8 induction in that cell type in terms of mitogen activated protein kinase (MAPK) and transcription element. Exposure of aortic smooth muscle cells (AoSMCs) to HSP22 not only enhanced IL-8 release but also induced IL-8 transcript via promoter activation. HSP22 activated ERK and p38 MAPK in AoSMCs. HSP22-induced IL-8 release was inhibited by U0126, but not by SB202190. A mutation in the IL-8 promoter region at the binding site of NF-${\kappa}$ B, but not AP-1 or C/EBP, impaired promoter activation in response to HSP22. Delivery of I ${\kappa}$ B, but not dominant negative c-Jun, lowered HSP22-induced IL-8 release from AoSMCs. These results suggest that HS P22 induces IL-8 in VSMCs via ERK1/2, and that transcription factor NF-kB may be required for the HSP22-induced IL-8 up-regulation.

Noninvasive Treatment and Rehabilitation of a Northern Goshawk (Accipiter gentilis) with Coracoid and Scapular Fracture (오훼골과 견갑골이 골절된 참매의 비침습적 재활 치료 성공 사례)

  • Kim, Mun-Jeong;Kim, Hee-Jong;Kim, Young-Jun;Park, Young-Seok;Kim, Bong-Kyun;An, Byeong-Deok;Park, Se-Young;Lee, Hang
    • Journal of Veterinary Clinics
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    • v.34 no.5
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    • pp.396-399
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    • 2017
  • This is a case report of a northern goshawk (Accipiter gentilis), admitted to the wildlife rescue center with right coracoid and scapular fracture which received conservative treatment and was soft-released successfully. At the admission, the goshawk had callus formed on the fractured bones, scars on eyebrows and severely damaged tail feathers with inability to fly. Cage rest was indicated to prevent further occurrence of fracture and to promote reunion of the fracture surface. The bird went through a rehabilitation process with appropriate physical training in flying cage to recover its fitness and flying ability. Complete molting of flight feathers with damaged rectrices was achieved during the rehabilitation period and its flight ability was recovered favorably. It was released into a proper habitat for northern goshawks, but the bird was found near the aviary where its last phase of rehabilitation was performed. A soft-release program was applied and finally the bird returned to near the first rescue location 235 km away from the release site.