• Title/Summary/Keyword: ibuprofen

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Particle Size Distribution, Drug Loading Capacity and Release Profiles of Solid Lipid Nanoparticles of Phenylpropionic Acids (페닐프로피온산계 해열진통제 고형지질나노입자의 입도분포와 약물봉입 및 용출특성)

  • Kim, Yoon-Sun;Kim, Kil-Soo
    • Journal of Pharmaceutical Investigation
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    • v.28 no.4
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    • pp.249-255
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    • 1998
  • Solid Lipid Nanoparticle(SLN), one of the colloidal carrier systems, has many advantages such as good biocompatibility, low toxicity and stability. In this paper, the effects of drug lipophilicity and surfactant on the drug loading capacity, particle size and drug release profile were examined. SLNs were prepared by homogenization of melted lipid dispersed in an aqueous surfactant solution. Ketoprofen, ibuprofen and pranoprofen were used as model drugs and tweens and poloxamers were tested for the effect of surfactant. Mean particle size of prepared SLNs was ranged from 100 to 150nm. The drug loading capacity was improved with the most lipophilic drug and low concentration of surfactant. Particle size and polydispersity of SLNs were changed according to the used lipid and surfactant. The rates of drug release were controlled by the loading drug and surfactant concentration. SLN system with effective drug loading efficiency and proper particle size for the intravenous or oral formulation can be prepared by selecting optimum drug and surfactant.

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Action of Phospholipase $A_2$in Histamine Release from Mast Cells (비만세포에서 Histamine유리에 관여하는 Phospholipase $A_2$의 작용)

  • 이윤혜;이승준;서무현;장용운;윤정이
    • YAKHAK HOEJI
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    • v.45 no.3
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    • pp.287-292
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    • 2001
  • To investigate whether phospholipase $A_2$pathway is involved in histamine release of rat peritoneal mast cells, we measured histamine release in the presence of various enzyme inhibitors involved in eicosanoid pathway, such as phospholipase $A_2$, cyclooxygenase and lipoxygenase. Phospholipase $A_2$inhibitors, manoalide and OPC, significantly inhibited histamine release induced by 100 $\mu$M ATP and 1$\mu$g/ml compound 48/80. Cyclooxygenase inhibitors, ibuprofen and indomethacin, significantly inhibited ATP-induced histamine release and lipoxygenase inhibitors, baicalein and caffeic acid, also significantly inhibited. To investigate the involvement of protein kinase in ATP- and compound 48/80-induced histamine release, we observed effects of protein kinase inhibitors on histamine release. Bisindolmaleimide (protein kinase C antagonist) dose-dependently inhibited both ATP and compound 48/80-induced histamine release. Tyrosine kinase inhibitors (methyl 2,5-dihydroxy cinnamate and genistein) dose-dependently inhibited ATP and compound 48/80-induced histamine release. Protein kinase C and tyrosine kinase seem to be involved in histamine release induced by ATP and compound 48/80. These results suggest that phospholipase $A_2$pathway as well as protein kinase C and tyrosine kinase are involved in histamine release of rat peritoneal mast cells by ATP and compound 48/80.

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Predicting Environmental Concentrations of Selected Pharmaceuticals Using the PhATETM Model in Keum-River, Korea (PhATETM 모형을 적용한 금강수계 중 의약물질 농도 추정)

  • Lim, Deuck-Soon;Park, Jeong-Im
    • Journal of Environmental Health Sciences
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    • v.35 no.1
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    • pp.45-52
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    • 2009
  • In recent years, pharmaceuticals in the aquatic environment have become a matter of increasing public concern. Environmental risk assessment (ERA), including an exposure assessment, is considered the best scientifically based approach for evaluating the potential effects of pharmaceuticals on ecosystems. Computerized exposure models constitute an important tool in predicting environmental exposures of pharmaceuticals. This paper presents the applicability of an exposure model by comparing measured data of selected pharmaceuticals with predicted environmental concentrations from an exposure model. $PhATE^{TM}$ (Pharmaceutical Assessment and Transport Evaluation) model developed by the Pharmaceutical Research and Manufacturers of America (PhRMA) was adapted to run simulations for the Keum River. A set of 7 pharmaceuticals of high production in Korea was modeled. The PECs generated by the $PhATE^{TM}$ model that were then compared to the measured concentrations. The $PhATE^{TM}$ model predicted concentrations for 7 pharmaceuticals including acetaminophen, acetylsalicylic acid, erythromycin, ibuprofen, lincomycin, mefenamic acid, and naproxen were in good agreement with actual measured concentrations, which demonstrated the utility of $PhATE^{TM}$ as a predictive tool. In conclusion, $PhATE^{TM}$, although it does not intend to accurately represent reality, could be utilized for rapid predictions of the environmental concentrations of pharmaceuticals.

Fever and Fever Management in Children: A Literature Review (아동의 발열과 발열관리: 문헌고찰)

  • Jeong, Yong-Sun;Kim, Jin-Sun
    • Child Health Nursing Research
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    • v.16 no.1
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    • pp.30-40
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    • 2010
  • Purpose: The purposes of this review were to identify whether available evidence supports the nursing interventions that are commonly used to reduce fever in children and to introduce research findings into practice. Methods: Journal databases and clinical guidelines from 1990 to 2009 were searched. The search terms were fever, febrile convulsion, fever management, fever phobia, child, antipyretics, temperature, external cooling, tepid sponge bath, and physical treatment. Results: Evidence suggests that uncomplicated fever is relatively harmless, but it is an important immunological defense. Antipyretics should not routinely be used with the sole aim of reducing body temperature in children with fever who are otherwise well. Currently a lack of evidence supports the practice of alternating acetaminophen and ibuprofen, and the routine use of tepid sponge bath. Conclusion: Currently, fever management in children does not reflect research evidence. Pediatric nurses can play an important role by encouraging clinical research in this area and also by enhancing research utilization in their practice. Moreover, pediatric nurses can educate parents about evidence-based fever management. Evidence-based educational interventions for pediatric nurses need to be developed and evaluated to improve the quality of nursing care in the management of childhood fever.

Graphene nanosheets encapsulated poorly soluble drugs with an enhanced dissolution rate

  • Shen, Shou-Cang;Ng, Wai Kiong;Letchmanan, Kumaran;Lim, Ron Tau Yee;Tan, Reginald Beng Hee
    • Carbon letters
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    • v.27
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    • pp.18-25
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    • 2018
  • In this study, graphene oxide(GO) was used as drug carriers to amorphize poorly watersoluble drugs via a co-spray drying process. Two poorly water-soluble drugs, fenofibrate and ibuprofen, were investigated. It was found that the drug molecules could be in the graphene nanosheets in amorphous or nano crystalline forms and thus have a significantly enhanced dissolution rate compared with the counterpart crystalline form. In addition, the dissolution of the amorphous drug enwrapped with the graphene oxide was higher than that of the amorphous drug in activated carbon (AC) even though the AC possessed a larger specific surface area than that of the graphene oxide. The amorphous formulations also remained stable under accelerated storage conditions ($40^{\circ}C$ and 75% relative humidity) for a study period of 14 months. Therefore, graphene oxide could be a potential drug carrier and amorphization agent for poorly water-soluble drugs to enhance their bioavailability.

Study on Binding of Ketoprofen and Ketoprofen Lysinate to Human Serum Albumin (Ketoprofen 및 Ketoprofen Lysinate와 Human Serum Albumin의 결합(結合)에 관한 연구(硏究))

  • Lee, Wan-Ha;Park, Eun-Seok;Jee, Ung-Kil;Rhyu, Byung-Tae
    • Journal of Pharmaceutical Investigation
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    • v.13 no.2
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    • pp.66-72
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    • 1983
  • Ketoprofen, 2-(3-benzoyl phenyl) propionic acid, has many advantages over the other antiinflammatory drugs, such as salicylates, phenytbutazone, and indomethacin. According to the reports, ketoprofen is well tolerated by patients and has very low incidence of side effects and toxic reactions. Although ketoprofen is widely used as an antiinflammatory agent, it shows poor solubility in water. In order to enhance water solubility, ketoprofen was made as lysine salt, such as acetylsalicylate lysine salt, ibuprofen lysine salt and amino acid salt of phenylbuatzone. The purpose of this study was to compare with ketoprofen lysinate in aspect of binding to human serum albumin (HSA) were made, and the association constant and the number of binding site were obtained using difference spectrophotometry. The number of binding site of HSA for ketoprofen and ketoprofen lysinate appears to be 3.3,3.2 respectively and association constants were found as follow; HSA-ketoprofen $2.23{\times}10^4\;M^{-1}$, HSA-ketoprofen lysinate $1.02{\times}10^4\;M^{-1}$.

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Acupuncture for Facet Joint Syndrome: A Review of Clinical Study (후관절 증후군의 침 치료에 대한 문헌 연구 보고)

  • Ji-Hyang Gu
    • Journal of Korean Medicine Rehabilitation
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    • v.33 no.1
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    • pp.13-29
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    • 2023
  • Objectives To evaluate the evidence supporting the effectiveness of acupuncture for facet joint syndrome. Methods We conducted search across 9 electronic databases (PubMed, EMBASE, Cochrane CENTRAL (CENTRAL), KoreaMed, Kmbase, Koreanstudies Information Service System (KISS), ScienceOn, China National Knowledge Infrastructure (CNKI), and Wanfang) to find clinical trials that used acupuncture as treatment for facet joint syndrome. The methodological quality of randomized controlled clinical trials (RCTs) were assessed using the Cochrane Risk of Bias (RoB) tool, while non-randomized controlled clinical trials (nRCTs) were assessed using the Cochrane Risk of Bias Assessment tool for Non-randomized Study (RoBANS) tool. Results Nine RCTs and one nRCT met our inclusion criteria. Fire needle was more effective than medial branch block in terms of visual analogue scale (VAS) after 1 month (p=0.02). Also, Fire needle was more effective than Ibuprofen in terms of VAS and oswestry disability index (ODI) (p<0.05). However, in the rest of the study results, the intervention group did not show a statistically significant difference than the control group. Conclusions Although our review found encouraging but limited evidence of acupuncture for facet joint syndrome, most of the studies included in the analysis were evaluated as methodologically high risk of bias. From now on further well-designed RCTs should be encouraged.

Clinical manifestations of headache in children younger than 7 years

  • Kang, Bu Seon;Lee, Jinsun;Choi, Jin Hyuk;Kwon, Hyeok Hee;Kang, Joon Won
    • Clinical and Experimental Pediatrics
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    • v.61 no.11
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    • pp.355-361
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    • 2018
  • Purpose: Headache is a common symptom during childhood. It is usually persistent and requires special care. This study aimed to identify the characteristics of headache in children <7 years of age. Methods: We reviewed 3 years of clinical files on children <7 years of age with a chief complaint of headache. Results: This study included 146 children (66 males, 80 females; mean age, $5.5{\pm}1.0years$). Mean symptom duration was $5.8{\pm}7.9months$. Attack durations were longer than 2 hours in 31 patients, shorter than 2 hours in 70 patients, and unchecked in 45 patients. Attack frequency was $15.1{\pm}10.6$ times per month. Pain locations and characteristics were also variable. Mean pain severity score was $5.1{\pm}2.2$ on the visual analog scale. Of 38 patients who underwent electroencephalography, 9 showed positive findings. Of 41 who underwent brain magnetic resonance imaging, 20 showed positive findings. The diagnoses were migraine (including probable migraine) in 34, tension-type headache in 5, and congenital malformations in 3. Medications were used in 29 patients: acetaminophen in 17, ibuprofen in 8, naproxen sodium in 1, and topiramate or amitriptyline in 3. Conclusion: In children aged <7 years, headache has a relatively benign course, but detailed history taking is needed for more accurate diagnosis.

Study on the Action by PAF on IL-1 Modulation in Alveolar Macrophages: Involvement of Endogenous Arachidonate Metabolites and Intracellular $Ca^{++}$ Mobilization

  • Lee, Ji-Hee;Kim, Won-Ki;Hah, Jong-Sik
    • The Korean Journal of Physiology and Pharmacology
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    • v.2 no.2
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    • pp.241-249
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    • 1998
  • Platelet-activating factor(PAF) enhanced interleukin-1(IL-1) activity by the interaction with a specific receptor in rat alveolar macrophages. In this study, we investigated the role of endogenous arachidonate metabolites and intracellular calcium mobilization in the PAF-induced IL-1 activity. Alveolar macrophages were preincubated with 5-lipoxygenase and cyclooxygenase inhibitors 30 min before the addition of PAF and lipopolysaccharide(LPS). After 24h culture, IL-1 activity was measured in the supernate of sample using the thymocyte proliferation assay. Inhibition of 5-lipoxygenase by nordihydroguaiaretic acid and AA-861 completely blocked the PAF-induced enhancement of IL-1 activity with $IC_{50}\;of\;2\;{\mu}M\;and\;5\;{\mu}M$, respectively. In contrast, the inhibition of cyclooxygenase pathway by indomethacin and ibuprofen resulted in the potentiation in PAF-induced IL-1 activity with maximal effect at $1\;{\mu}M\;and\;5\;{\mu}M$, respectively. In addition, leukotriene $B_4$ and prostaglandin $E_2$ production were observed in PAF-stimulated alveolar macrophage culture. As could be expected, 5-lipoxygenase and cyclooxygenase inhibitors abolished PAF- stimulated leukotriene $B_4$ and prostaglandin $E_2$ production, respectively. The effects of PAF on intracellular calcium mobilization in alveolar macrophages were evaluated using the calcium-sensitive dye fura-2 at the single cell level. PAF at any dose between $10^{-16}\;and\;10^{-8}$ M did not increase intracellular calcium. Furthermore, there was no effective change of intracellular calcium level when PAF was added to alveolar macrophages in the presence of LPS or LPS+LTB4, and 4, 24 and 48h after treatment of these stimulants. Together, the results indicate that IL-1 activity induced by PAF is differently regulated through subsequent induction of endogenous 5-lipoxygenase and cyclooxygenase pathways, but not dependent on calcium signalling pathway.

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Interventions for anesthetic success in symptomatic irreversible pulpitis: A network meta-analysis of randomized controlled trials

  • Sivaramakrishnan, Gowri;Alsobaiei, Muneera;Sridharan, Kannan
    • Journal of Dental Anesthesia and Pain Medicine
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    • v.19 no.6
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    • pp.323-341
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    • 2019
  • Background: Local anesthetics alone or in combination with adjuncts, such as oral medications, have routinely been used for pain control during endodontic treatment. The best clinical choice amongst the vast numbers of agents and techniques available for pain control for irreversible pulpitis is unclear. This network meta-analysis combined the available evidence on agents and techniques for pulpal anesthesia in the maxilla and mandible, in order to identify the best amongst these approaches statistically, as a basis for future clinical trials. Methods: Randomized trials in MEDLINE, DARE, and COCHRANE databases were screened based on inclusion criteria and data were extracted. Heterogeneity was assessed and odds ratios were used to estimate effects. Inconsistencies between direct and indirect pooled estimates were evaluated by H-statistics. The Grading of Recommendation, Assessment, Development, and Evaluation working group approach was used to assess evidence quality. Results: Sixty-two studies (nine studies in the maxilla and 53 studies in the mandible) were included in the meta-analysis. Increased mandibular pulpal anesthesia success was observed on premedication with aceclofenac + paracetamol or supplemental 4% articaine buccal infiltration or ibuprofen+paracetamol premedication, all the above mentioned with 2% lignocaine inferior alveolar nerve block (IANB). No significant difference was noted for any of the agents investigated in terms of the success rate of maxillary pulpal anesthesia. Conclusion: Direct and indirect comparisons indicated that some combinations of IANB with premedication and/or supplemental infiltration had a greater chance of producing successful mandibular pulpal anesthesia. No ideal technique for maxillary anesthesia emerged. Randomized clinical trials with increased sample size may be needed to provide more conclusive data. Our findings suggest that further high-quality studies are required in order to provide definitive direction to clinicians regarding the best agents and techniques to use for mandibular and maxillary anesthesia for irreversible pulpitis.