• Title/Summary/Keyword: biphasic system

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Evaluation of In Vitro Release Profiles of Fentanyl-Loaded PLGA Oligomer Microspheres

  • Gilson Khang;Seo, Sun-Ah;Park, Hak-Soo;John M. Rhee;Lee, Hai-Bang
    • Macromolecular Research
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    • v.10 no.5
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    • pp.246-252
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    • 2002
  • In order to the development of the delivery device of long-acting local anesthetics for postoperative analgesia and control of chronic pain of cancer patient, fentnyl-loaded poly (L-lactide-co-glycolido) (PLGA, molecular weight, 5,000 g/mole; 50 : 50 mole ratio by lactide to glycolide) microspheres (FMS) were studied. FMS were prepared by an emulsion solvent-evaporation method. The influence of several preparation parameters such as initial drug loading, PLGA concentration, emulsifier concentration, oil phase volume, and fabrication temperature has been investigated on the fentanyl release profiles. Generally, the drug showed the biphasic release patterns, with an initial diffusion followed by a lag period before the onset of the degradation phase, but there was no lag time in our system. Fentanyl was slowly released from FMS over 10 days in vitro with a quasi-zero order property. The release rate increased with increasing drug loading as well as decreasing polymer concentration with relatively small initial burst effect. From the results, FMS may be a good formulation to deliver the anesthetic for the treatment of chronic pain.

[$Zn^{2+}$ Modulates the Responses of Rat Dorsal Horn Neuron to C-Fiber Stimulation and Excitatory Amino Acids

  • Ahn, Chang-Hoon;Shin, Hong-Kee;Kim, Jin-Hyuk
    • The Korean Journal of Physiology and Pharmacology
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    • v.4 no.6
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    • pp.455-461
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    • 2000
  • Zinc contained in the neurons of central nervous system is activity-dependently released and then attenuates NMDA (N-methyl-D-aspartate)-induced neurotoxicity while augmenting non-NMDA-induced neurodegeneration. Zinc also has been reported to produce antinociceptive action on the inflammation- and nerve injury-induced hyperalgesia in the behavioral test. In this study, we investigated the effects of zinc on the responses of dorsal horn cells to NMDA, kainate and graded electrical stimulation of C-fibers. In the majority of WDR cells (70.6%), zinc current-dependently inhibited WDR cell responses to NMDA and in the remaining cells, produced biphasic responses; excitation followed by inhibition. Zinc augmented the responses of WDR cells to iontophoretical application of kainate. The dominant effect of $Zn^{2+}$ on the responses of WDR cells to C-fiber stimulation was excitatory, but inhibition, excitation-inhibition and no change of the responses to C-fiber stimulation were induced. $Ca^{2+}-EDTA$ antagonized the excitatory or inhibitory effects of $Zn^{2+}$ on the WDR cell responses. These experimental findings suggest that $Zn^{2+}$ modulates the transmission of sensory information in the rat spinal cord.

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Effects of Hesperidin Are Not Associated with Changes in Basal Synaptic Transmission, Theta-burst LTP, and Membrane Excitability in CA1 Neuron

  • Baek, Jin-Hee;Kim, Jae-Ick;Kaang, Bong-Kiun
    • Animal cells and systems
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    • v.13 no.4
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    • pp.357-362
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    • 2009
  • Hesperidin, the most abundant polyphenolic compound found in citrus fruits, has been known to possess neuroprotective, sedative, and anticonvulsive effects on the nervous system. In a recent electrophysiological study, it was reported that hesperidin induced biphasic change in population spike amplitude in hippocampal CA1 neurons in response to both single spike stimuli and theta-burst stimulation depending on its concentration. However, the precise mechanism by which hesperidin acts on neuronal functions has not been fully elucidated. Here, using whole-cell patch-clamp recording, we revealed that hesperidin did not affect excitatory synaptic activities such as basal synaptic transmission and theta-burst LTP. Moreover, in a current injection experiment, spike number, resting membrane potential and action potential threshold also remained unchanged. Taken together, these results indicate that the effects of hesperidin on the neuronal functions such as spiking activity might not be attributable to either modification of excitatory synaptic transmissions or changes in membrane excitability in hippocampal CA1 neuron.

Micro-Chemical Structure of Polyaniline Synthesized by Self-Stabilized Dispersion Polymerization

  • NamGoong, Hyun;Woo, Dong-Jin;Lee, Suck-Hyun
    • Macromolecular Research
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    • v.15 no.7
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    • pp.633-639
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    • 2007
  • A variety of NMR techniques were applied to the micro-chemical structural characterization of polyanilines prepared via an efficient synthetic method in a self-stabilized dispersion medium in which the polymerization was conducted in a heterogeneous organic/aqueous biphasic system without any stabilizers. Here, the monomer and growing polymer chain were shown to function simultaneously as a stabilizer, imparting compatibility for the dispersion of the organic phase, and as a form of flexible template in an aqueous reaction medium. Polymerizations predicated on this concept generated polyanilines with a low defect content: solution state $^{13}C-NMR$ and solid $^{13}CDD/CP/MAS$ spectroscopy indicated that the synthesized HCPANi and its soluble derivative, HCPANi-t-BOC, evidenced distinctly different NMR spectra with fewer side peaks, as compared to conventionally prepared PANis, and the complete structural assignments of the observed NMR peaks could be determined via the combination of both 1D and 2D techniques. Ortho-linked defects in HCPANi were estimated to be as low as 7%, as shown by a comparison of the integration of the carbonyl carbon resonance peaks.

Evaluation of the Device Failure Using Stimulus Artifact in the Cochlear Implantee (인공와우 이식자에서 자극 잡파를 이용한 고장 평가)

  • Heo, Seung-Deok;Kim, Sang-Ryeol;Ahn, Joong-Ki;Jung, Dong-Keun;Kang, Myung-Koo
    • Speech Sciences
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    • v.14 no.2
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    • pp.35-42
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    • 2007
  • The aim of this study is to analyze the correlation between current intensity and amplitude of stimulus artifact on the cochlear implantee, and to find out basic information to check the device failure. Subjects were a prelingual child and 3 postlingual adults with more than severe hearing losses. The charge-balanced biphasic pulses were presented at stimulus rates of 11 pulses per second, each pulse width of $25{\mu}s$ with monopolar mode(MP1+2). Current intensities were delivered at 27.5, 33.7, 41.3, 50.5, 61.9, $75.8{\mu}A$. Stimulus artifacts were recorded by evoked potential system. This procedure was performed just before the initial stimulation, and then, the amplitude of stimulus artifacts were compared with each current intensity. The amplitude of stimulus artifacts was increased significantly according to the current intensity (p<0.01). The results suggest that the change of the amplitude of stimulus artifact can be used as a good cue to check the device failure in the cochlear implantee.

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A Simple and Modified Photometric Method for Measuring Lipase Activity (리파제 활성측정을 위한 간편한 비색정량법)

  • Kim, Chul-Jin;Cheigh, Hong-Sik;Byun, Si-Myung
    • Korean Journal of Food Science and Technology
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    • v.16 no.2
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    • pp.251-253
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    • 1984
  • A simple and modified method is developed to determine a lipase activity. A linear relationship exists between the color intensity and the free fatty acid liberated by enzyme action. The range of determination is from 0.05 to $1.5\;{\mu}moles$ of long chain fatty acid (oleic acid) and 0.2 to $2.0\;{\mu}moles$ of short chain fatty acid (caproic acid). The cumbersome procedure of the removal of the upper aqueous phase which was required in the previous copper soap extraction method was eliminated by the movement of solvent phase to upper phase in the respective biphasic system with a mixture solvent (chloroform: n-hexane:ethanol = 49:49:2) and copper reagent saturated with sodium chloride.

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Bioimpedance Changes in Rats with CCl4-Induced Liver Fibrosis

  • Heo, Jeong;Jung, Dong-Keun
    • Journal of Sensor Science and Technology
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    • v.20 no.2
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    • pp.71-76
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    • 2011
  • To characterize the relationship between the stage of hepatic fibrosis and bioimpedance, several electric parameters were estimated in rats with $CCl_4$-induced liver fibrosis. Thirty three Sprague-Dawley rats were intraperitoneally injected with a $CCl_4$-mineral oil mixture (1:1, 0.2 mL/100 g) twice a week for 8 weeks. The resistance(R), reactance(X), impedance(Z), and dissipation factor(D) between 1 kHz and 100 kHz were then evaluated in the livers of the rats under pentobarbital anesthesia using an HP4294A Impedance Analyzer. The rats were killed 2, 4, 6, and 8 weeks later, and their livers were classified in accordance with Ishak's scoring system. R, X, and Z changed in accordance with the progression of hepatic fibrosis and the changes were greater at lower frequencies than at higher frequencies. In comparison, the D spectrum was biphasic; D increased initially then decreased with increasing frequency. All of the parameters(R, X, Z, and D) changed in accordance with the stage of fibrosis in the livers, but D changed specifically with the progression of fibrosis. These results indicate that hepatic fibrosis may be evaluated by determining the changes in D.

`oxicological study of carbaryl in rats

  • Lee, Wan-Koo;Hong, Sa-Uk
    • Archives of Pharmacal Research
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    • v.8 no.3
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    • pp.119-132
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    • 1985
  • The apparent effectiveness of 1-naphthyl-N-methyl carbamate (carbaryl) against a wide variety of insects motivated the study of its mammalian toxicity. In this toxicological study of carbaryl, mature male rats inhaled carbaryl at a mean concentration of 112mg, 168mg and 224 mg/$m^{3}$ for one hour. After inhalation, pentobarbital sleeping time, Nadph-cytochrome c reductase activity, cytochrome p-450 and protein content in liver microsomes, various tissue residues, cholinesterase inhibition in plasma and histopathological findings at autopsy were observed. The pentobarbital sleeping time was prolonged in rats inhaled with carbaryl for one day while the sleeping time was shortened in the 3 days inhaled group. The changes of cytochrome p-450 content and NADPH-cytochrome c reductase activity exhibited biphasic response showing the decrease in the one day inhaled group and the increase in the 3 days inhaled group. The marked depression of plasma ChE activity was observed in rats inhaled with carbaryl at 112 mg/$m^{3}$, however no more progressive effect was observed at the higher concentration of the compound. The main observations in histopathological finding were ciliary detachment, epithelial swelling and subepithelial inflammatory cellular infiltration in trachea due to the irritation.

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Development of Wireless Neuro-Modulation System for Stroke Recovery Using ZigBee Technology (ZigBee를 이용한 뇌졸중 치료용 무선 전기 자극기 개발)

  • Kim, G.H.;Ryu, M.H.;Shin, Y.I.;Kim, H.I.;Kim, N.G.;Yang, Y.S.
    • Journal of Biomedical Engineering Research
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    • v.28 no.1
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    • pp.153-161
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    • 2007
  • Stroke is the second most significant disease leading to death in Korea. The conventional therapeutic approach is mainly based on physical training, however, it usually provides the limited degree of recovery of the normal brain function. The electric stimulation therapy is a novel and candidate approach with high potential for stroke recovery. The feasibility was validated by preliminary rat experiments in which the motor function was recovered up to 80% of the normal performance level. It is thought to improve the neural plasticity of the nerve tissues around the diseased area in the stroked brain. However, there are not so much research achievements in the electric stimulation for stroke recovery as for the Parkinson's disease or Epilepsy. This study aims at the developments of a wireless variable pulse generator using ZigBee communication for future implantation into human brain. ZigBee is widely used in wireless personal area network (WPAN) and home network applications due to its low power consumption and simplicity. The developed wireless pulse generator controlled by ZigBee can generate various electric stimulations without any distortion. The electric stimulation includes monophasic and biphasic pulse with the variation of shape parameters, which can affect the level of recovery. The developed system can be used for the telerehabilitation of stroke patient by remote control of brain stimulation via ZigBee and internet. Furthermore, the ZigBee connection used in this study provides the potential neural signal transmission method for the Brain-Machine Interface (BMI).

Ketamine-Induced Blood Pressure Lowering in the Rat (흰쥐에서 Ketamine에 의한 혈압하강)

  • Yu Xian-Feng;Kim Shang-Jin;Lee Mun-Young;Kang Hyung-Sub;Kim Jin-Shang
    • Journal of Veterinary Clinics
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    • v.22 no.3
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    • pp.220-227
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    • 2005
  • Although ketamine has been used in the field of anesthetic medicine for its safety and favourable respiratory effects, the cardiovascular effects of ketamine is still controversial. To clarify the action and mechanism of ketamine upon cardiovascular system, arterial blood pressure, tension of aortic ring, left ventricular developed pressure and heart rate were measured in rats, Ketamine produced two types of effects on arterial blood pressure in anesthetized rats; monophasic effect (blood pressure lowering) and biphasic effect (initial transient blood pressure increasing following sustained lowering), The ketamine-induced lowering of aterial blood pressure showed a concentration-dependent manner, inhibited by the pretreament of $MgCl_2$ and potentiated by the pretreatment of $CaCl_2$. The ketamine-induced lowering of aterial blood pressure was suppressed by the pretreatment of nifedipine, verapamil or lidocaine. In phenylephrine-precontracted endothelium intact (+E) aortic rings, ketamine sometimes caused a small enhancement of contraction ($112.5{\pm}3.6{\%}$). However, in many experiments, ketamine produced a concentration-dependent relaxation in +E aortic rings precontracted with either phenylephrine or KCl. Ketamine-induced relaxation was significantly greater in KCl-precontracted strips than phenylephrine-precontracted strips. In phenylephrine-precontracted +E aortic rings, the ketamine-induced vasorelaxation was not suppressed by endothelium removal or by the pretreatment of a nitric oxide synthase inhibitors, L-$N^G$-nitro-arginine and a guanylate cyclase inhibitors, methylene blue, suggesting that the ketamine-induced vasorelaxation is not dependent on the endothelial function. In addition, ketamine elicited an increase in left ventricular developed pressure in perfused hearts accompanied by decrease in heart rate. These results suggest that ketamine could evoke a hypotension due to vasorelaxation and decrease in heart rate in rats. The inhibitory effect of cardiovascular system might be associated with modulation of $Ca^{2+}$ homeostasis.