• Title/Summary/Keyword: Immediate release

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Identification of Priority Pollutants in Shihwa-Banwol Techno Valley Area for Management of Environmental Health (시화.반월산업단지 인근지역의 환경보건 관리를 위한 우선관리대상 오염물질 선정에 관한 연구)

  • Kim, Jung-Kon;Park, Yoon-Suk;Paek, Do-Myung;Choi, Kyung-Ho
    • Journal of Environmental Policy
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    • v.6 no.3
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    • pp.33-56
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    • 2007
  • Use of chemicals has greatly increased along with development of human civilization. Concerns about potential effects of chemicals on human health and environment have also grown accordingly. Due to the enormous number of chemicals being used, however, it is neither practical nor feasible to regulate all the chemicals. Therefore, it is necessary to identify chemicals that deserve more immediate attention, based on the effects on receptors to be protected. This study was initiated by the need for developing management policies for Shihwa-Banwol Techno Valley and its vicinities of korea, where complaints and concerns on environmental contamination have been raised for long time. This study to identifies major chemicals that deserve most immediate attention in environmental health management in this area. For this purpose, the study employed CHEMS-1(Chemical Hazard Evaluation for Management Strategies), and used chemical data from Toxics Release Inventory(TRI) and environmental contamination data from the environmental pollution monitoring network. Top priority pollutants identified in Shihwa-Banwol Techno Valley area were metals and volatile organic compounds, such as dichloromethane, trichloroethylene, diazinon, tetrachloroethylene, chromium compounds, tin compounds, chloroacetic acid, ethyl acetate, and zinc compounds, in an order of decreasing importance. An evaluation of physicochemical properties of the priority chemicals and the environmental pollution monitoring network database in Shihwa-Banwol Techno Valley suggested that the media that are of potential concern would be the atmosphere and aquatic environment.

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Effects of Ethanol Extract of Liriope platyphylla on Allergic Inflammation (맥문동(麥門冬) 에탄올 추출물이 알레르기 염증 반응에 미치는 영향)

  • Kim, Ho Seok;Park, Ji Hye;Kim, Hyun Kab;Kim, Jae Hyun;Lee, Bina;Min, Ju Hee;Kim, Eun Young;Jung, Hyuk Sang;Lee, Hyang Sook;Sohn, Young Joo
    • Journal of Physiology & Pathology in Korean Medicine
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    • v.28 no.5
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    • pp.512-519
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    • 2014
  • This study investegated the effect of Liriope platyphylla (LP) on allergic reactions and its mechanism of action. We investigated the effect of LP on Evans Blue (EB) extravasation induced by anti-dinitrophenyl (DNP)-IgE in rats. We tested whether the ethanol extract of LP reduced ear skin thickness and historical changes induced by topical application of 2,4-dinitrofluorobenzene (DNFB) to ears of mice. We evaluated compound 48/80-induced release of histamine in rats peritoneal mast cell (RPMCs). We also investigated the regulatory effect of LP on the level of inflammatory mediators in PMACI-induced human mast cell (HMC-1); cytokine IL-6, IL-8, TNF-${\alpha}$ in HMC-1, MAPKs (ERK, JNK and p38) in HMC-1. The ethanol extract of LP (81.3 mg/100 g body weight) significantly inhibited the PCA reaction compared with the control (P < 0.05). However, LP did not prevent topical applications of DNFB-induced ear skin thickening and histological changes. In RPMCs, histamine release induced by compound 48/80 was significantly attenuated by LP at $100{\mu}g/ml$ (P < 0.05). LP extract ($100{\mu}g/ml$) significantly reduced the PMACI-induced IL-6, IL-8, and TNF-${\alpha}$ secretion via inhibition of ERK phosphorylation in HMC-1. In conclusion, the ethanol extract of LP inhibited mast cell-derived, immediate-type allergic reactions, and the result suggest the potential of LP for preventing allergic inflammatory disorders.

Beyond Clot Dissolution; Role of Tissue Plasminogen Activator in Central Nervous System

  • Kim, Ji-Woon;Lee, Soon-Young;Joo, So-Hyun;Song, Mi-Ryoung;Shin, Chan-Young
    • Biomolecules & Therapeutics
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    • v.15 no.1
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    • pp.16-26
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    • 2007
  • Tissue plasminogen activator (tPA) is a serine protease catalyzing the proteolytic conversion of plasminogen into plasmin, which is involved in thrombolysis. During last two decades, the role of tPA in brain physiology and pathology has been extensively investigated. tPA is expressed in brain regions such as cortex, hippocampus, amygdala and cerebellum, and major neural cell types such as neuron, astrocyte, microglia and endothelial cells express tPA in basal status. After strong neural stimulation such as seizure, tPA behaves as an immediate early gene increasing the expression level within an hour. Neural activity and/or postsynaptic stimulation increased the release of tPA from axonal terminal and presumably from dendritic compartment. Neuronal tPA regulates plastic changes in neuronal function and structure mediating key neurologic processes such as visual cortex plasticity, seizure spreading, cerebellar motor learning, long term potentiation and addictive or withdrawal behavior after morphine discontinuance. In addition to these physiological roles, tPA mediates excitotoxicity leading to the neurodegeneration in several pathological conditions including ischemic stroke. Increasing amount of evidence also suggest the role of tPA in neurodegenerative diseases such as Alzheimer's disease and multiple sclerosis even though beneficial effects was also reported in case of Alzheimer's disease based on the observation of tPA-induced degradation of $A{\beta}$ aggregates. Target proteins of tPA action include extracellular matrix protein laminin, proteoglycans and NMDA receptor. In addition, several receptors (or binding partners) for tPA has been reported such as low-density lipoprotein receptor-related protein (LRP) and annexin II, even though intracellular signaling mechanism underlying tPA action is not clear yet. Interestingly, the action of tPA comprises both proteolytic and non-proteolytic mechanism. In case of microglial activation, tPA showed non-proteolytic cytokine-like function. The search for exact target proteins and receptor molecules for tPA along with the identification of the mechanism regulating tPA expression and release in the nervous system will enable us to better understand several key neurological processes like teaming and memory as well as to obtain therapeutic tools against neurodegenerative diseases.

NEW DRUG THERAPY IN CHILD AND ADOLESCENT PSYCHIATRY-NEW LONG-ACTING PSYCHOSTIMULANTS (소아청소년 정신과 영역에서의 새로운 약물치료:새로운 장기작용형 중추신경자극제)

  • Choi, Sung-Ku
    • Journal of the Korean Academy of Child and Adolescent Psychiatry
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    • v.14 no.1
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    • pp.3-11
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    • 2003
  • Attention-deficit/Hyperactivity disorder(ADHD) is the most common psychiatric disorder of childhood and among the most prevalent chronic health conditions affecting school-aged children. Children with ADHD experience significant functional problems, such as school difficulties, academic underachievement, troublesome interpersonal relationships with family members and peers, and low self-esteem. The most widely used pharmacological treatments for ADHD are psychostimulants, such as methylphenidate and amphetamine salts. These medications provide clinical efficacy by increasing the availability of catecholamines, primarily dopamine, in the frontal lobe of the brain. immediate-release(IR) formulations of sychostimulants were among the most effective psychotrophic medications in the psychopharmacological treatment. However, there are some limitations of IR formulations:the short half-life and duration of efficacy, which result in the need for multiple daily dosing and the poor compliance. These limitations have led to the development of once-daily, extended-release(ER) formulations of methylphenidate and amphetamine salts. However, these ER formulations may not be as immediately helpful to ADHD children due to delayed onset of action and the acute tolerance which is the failure to sustain the efficacy with the same concentration of drug as the initial stage of medication. OROS-methylphenidate(Concerta$^{\circledR}$) given once a day produces an ascending-pattern plasma drug level generated by the osmotically released, timed drug-delivery system. These new formulations of the psychostimulants have been shown to be a useful alternative to old stimulant medications through the evidence by the clinical trials.

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Tapentadol: Can It Kill Two Birds with One Stone without Breaking Windows?

  • Chang, Eun Jung;Choi, Eun Ji;Kim, Kyung Hoon
    • The Korean Journal of Pain
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    • v.29 no.3
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    • pp.153-157
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    • 2016
  • Tapentadol is a novel oral analgesic with a dual mode of action as an agonist of the ${\mu}$-opioid receptor (MOR), and as a norepinephrine reuptake inhibitor (NRI) all in a single molecule. Immediate release (IR) tapentadol shows its analgesic effect quickly, at around 30 minutes. Its MOR agonistic action produces acute nociceptive pain relief; its role as an NRI brings about chronic neuropathic pain relief. Absorption is rapid, with a mean maximal serum concentration at 1.25-1.5 h after oral intake. It is present primarily in the form of conjugated metabolites after glucuronidation, and excretes rapidly and completely via the kidneys. The most common adverse reactions are nausea, dizziness, vomiting, and somnolence. Constipation is more common in use of the ER formulation. Precautions against concomitant use of central nervous system depressants, including sedatives, hypnotics, tranquilizers, general anesthetics, phenothiazines, other opioids, and alcohol, or use of tapentadol within 14 days of the cessation of monoamine oxidase inhibitors, are advised. The safety and efficacy have not been established for use during pregnancy, labor, and delivery, or for nursing mothers, pediatric patients less than 18 years of age, and cases of severe renal impairment and severe hepatic impairment. The major concerns for tapentadol are abuse, addiction, seeking behavior, withdrawal, and physical dependence. The presumed problem for use of tapentadol is to control the ratio of MOR agonist and NRI. In conclusion, tapentadol produces both nociceptive and neuropathic pain relief, but with worries about abuse and dependence.

Surfactant Effects upon Dissolution Patterns of Carbamazepine Immediate Release Tablet

  • Lee Hyeontae;Park Sang-Ae;Sah Hongkee
    • Archives of Pharmacal Research
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    • v.28 no.1
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    • pp.120-126
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    • 2005
  • The objective of this study was to investigate the effects of sodium lauryl sulfate upon the saturation solubility of carbamazepine, its dissolution kinetics, and $T_{50\%}$ defined as the time required for dissolving $50\%$ of carbamazepine. Water, 0.1N-HCI, and phosphate buffers at pH 4.0 and 6.8 containing 0.1, 0.5, 1, and $2\%$ sodium lauryl sulfate were used as dissolution media. The dissolution study was conducted by using the USP dissolution apparatus II with an agitation rate of 75 rpm. Samples of the dissolution media were taken in 7, 15, 30, 45, 60, 75, and 90 min, and the amounts of carbamazepine were determined spectrophotometrically at 285 nm. All dissolution data were fitted well into a four-parameter exponential equation: $Q\;=\;a(1\;-\;e^{-bxt})\;+\;c(1\;-\;e^{-dxt})$. In this equation Q represented $\%$ carbamazepine dissolved at a time t, and a, b, c, and d were constants. This equation led to the calculation of dissolution rates at various time points and $T_{50\%}$. It was found that the dissolution rate of carbamazepine was directly proportional to the aqueous concentration of sodium lauryl sulfate. In addition, under our experimental conditions $T_{50%}$ values ranged from 37.8 to 4.9 min. It was interesting to note that $T_{50\%}$ declined rapidly as the surfactant concentration increased from 0.1 to $0.5\%$, whereas it declined more slowly at concentrations greater than $1\%$. These results clearly demonstrated that the dissolution rate of carbamazepine and duration of its dissolution test could be tailored by optimizing the amount of sodium lauryl sulfate in a dissolution medium.

Effect of Terminalia chebula fruit on anaphylaxis by anal therapy

  • Shin, Hye-Young;Lee, Kyung-Bo;Jung, Yun-Hee;Kim, Eun-Ah;Lee, Mi-Young;Lee, Mi-Ri;Kim, Sang-Yong;Kim, Sang-Hyun;Shin, Tae-Yong
    • Advances in Traditional Medicine
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    • v.3 no.2
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    • pp.56-62
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    • 2003
  • The effect of aqueous extract of Terminalia chebula fruit (Combretaceae) (TCAE) by anal administration on mast cell-dependent immediate-type anaphylactic reactions was investigated. TCAE (0.005 to 1 g/kg) inhibited systemic anaphylaxis induced by compound 48/80 in mice. When TCAE was pretreated at the same concentrations with systemic anaphylaxis, the plasma histamine levels were reduced in a dose-dependent manner. TCAE (0.1 and 1 g/kg) also significantly inhibited local anaphylaxis activated by anti-DNP IgE. TCAE (0.001 to 1 mg/ml) dose-dependently inhibited the histamine release from rat peritoneal mast cells (RPMC) activated by compound 48/80 or anti-DNP IgE. Moreover, TCAE (0.01 and 0.1 mg/ml) had a significant inhibitory effect on anti-DNP IgE-mediated tumor necrosis $factor-{\alpha}$ $(TNF-{\alpha})$ production from RPMC. These results provide evidence that anal therapy of TCAE may be beneficial in the treatment of systemic and local mast cell-dependent anaphylaxis.

Real-time Imaging of Inositol 1,4,5-trisphosphate Movement in Mouse Salivary Gland Cells

  • Hong, Jeong-Hee;Lee, Syng-Ill;Shin, Dong-Min
    • International Journal of Oral Biology
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    • v.33 no.4
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    • pp.125-129
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    • 2008
  • Inositol 1,4,5-trisphosphate ($IP_3$) plays an important role in the release of $Ca^{2+}$ from intracellular stores into the cytoplasm in a variety of cell types. $IP_3$ translocation dynamics have been studied in response to many types of cell signals. However, the dynamics of cytosolic $IP_3$ in salivary acinar cells are unclear. A green fluorescent protein (GFP)-tagged pleckstrin homology domain (PHD) was constructed and introduced into a phospholipase C ${\delta}1$ (PLC ${\delta}1$) transgenic mouse, and then the salivary acinar cells were isolated. GFP-PHD was heterogeneously localized at the plasma membrane and intracellular organelles in submandibular gland and parotid gland cells. Application of trypsin, a G protein-coupled receptor activator, to the two types of cells caused an increase in GFP fluorescence in the cell cytoplasm. The observed time course of trypsin-evoked $IP_3$ movement in acinar cells was independent of cell polarity, and the fluorescent label showed an immediate increase throughout the cells. These results suggest that GFP-PHD in many tissues of transgenic mice, including non-cultured primary cells, can be used as a model for examination of $IP_3$ intracellular dynamics.

Treatment of Intraoperative Thrombosis and Spasm in Free Tissue Transfers Using the Fogarty Catheter (포가티 카테터를 이용한 유리조직 전이술 시 수술 중 혈전 및 연축의 치료)

  • Lee, Seung Ryul;Yun, Young Mook;Oh, Sang-Ha
    • Archives of Plastic Surgery
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    • v.35 no.2
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    • pp.159-164
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    • 2008
  • Purpose: Microvascular free tissue transfer has become a reliable technique for the reconstruction of complex wounds. Occasionally, unexpected intraoperative thrombosis and/or spasm of recipient artery might be annoying problems even for the technically competent microvascular surgeons. If such problems are not treated properly, they will inevitably cause to flap failure. Methods: From January 2006 to February 2007, soft tissue reconstructions by free tissue transfers were performed on 21 patients having complex defects in the lower extremity. Although segmental revision and various pharmacologic agents were repeatedly applied, arterial occlusions were not managed in 6 cases. For removal of thrombi and release of spasm, Fogarty No. 2 or No. 3 catheters were inserted into the lumen to the proximal recipient artery. Its balloon was then inflated after passing through a resistant area. Next, the catheter was gently withdrawn backward. Results: After the Fogarty catheter was inserted two or three times, the pulsatile arterial flow was restored. When the catheter was inserted into the lumen, a feeling of resistance existed in a 5-10cm more proximal portion that could not be easily accessed from the vascular end. After the reestablishment of blood flow, successful anastomoses were achieved and immediate rethrombosis or spasm did not occur. No long-term sequelae associated with balloon trauma to the arterial wall were observed. Conclusion: The use of the Fogarty catheter can be an effective method in treating pedicle thrombosis and spasm. This is a very simple and rapid technique that offers microvascular surgeons another option to increase the success rate of microvascular anastomosis in free tissue transfers.

Relationship Between Dissolution Patterns of Carbamazepine Tablet and Dissolution Medium Composition (카르바마제핀 정제 용출패턴과 용출액 조성과의 상관성)

  • Lee, Hyeon-Tae;Kim, Jeong-Ho;Kim, Hyun-Joo;Sah, Hong-Kee
    • Journal of Pharmaceutical Investigation
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    • v.34 no.3
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    • pp.185-192
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    • 2004
  • The objective of this study was to evaluate the effects of surfactant type and concentration upon dissolution rates of carbamazepine from an immediate-release tablet. The dissolution media used in this study were aqueous solutions containing 0.1-2% sodium lauryl sulfate, cetyltrimethylammonium bromide, or polysorbate 80. The solubility of carbamazepine in the dissolution media was determined at first. A dissolution study was then conducted by using the USP dissolution apparatus II (paddle method) with an agitation rate of 75 rpm. Aliquots of the dissolution media were taken at predetermined time intervals, and the amount of carbamazepine dissolved was measured spectrophotometrically at 285 nm. The dissolution data obtained were fitted into a biphasic exponential equation with four parameters. Excellent correlations were observed between the experimental data and the theoretical ones predicted by the equation. This equation permitted the calculation of $T_{50%}$ (the time required for dissolving 50% of carbamazepine) under various experimental conditions. Differentiation of the equation also led to the attainment of dissolution rates at dissolution time points. The addition of a surfactant to an aqueous solution led to increasing the solubility of carbamazepine by 3- to 12-folds, depending upon its type and concentration. This event also resulted in enhancing the magnitude of a sink condition during the dissolution study. As a result, the dissolution rate of carbamazepine was affected by the aqueous surfactant concentration in a proportional manner. Subsequently, $T_{50%}$ values declined rapidly, as the surfactant concentration increased. Such effects were observed in decreasing order of sodium lauryl sulfate, cetyltirmethylammonium bromide, and polysorbate 80. These results clearly demonstrated that it was possible to tailor a dissolution rate and $T_{50%}$ of carbamazepine by manipulating the type and concentration of a surfactant. Relevant information would be beneficial to setting up dissolution specifications for poorly water-soluble drug products.