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Effect of Intermittent Versus Continuous Infusion of Progesterone on LHRH Release In Viuo from the Rat Mediobasal Hypothalamus

  • 김경진
    • The Korean Journal of Zoology
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    • v.32 no.4
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    • pp.329-338
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    • 1989
  • Present study examined the effect of intermittent versus continuous infusion of progesterone(P) on LHRH release in uiuo from the mediobasal hvpothalamus of ovariectomiEed, estradiol-primed adult rats bearing push-pull cannulae. Three experimental groups were studied: 1) control (perfusion medium only),2) intermittent perfusion of P (10-min on,20-min off, and 3) continuous perfusion of p. p (10 ng/mll was directly infused into the MBH following a 3 hr basal collection. Perfusates were collected at 10 min intents린s on ice and LHRH release was measured by LHRH radioimmunoassav. Cycle detector analysis revealed that the spontaneous HRH output in the control group was pulsatile over a 7 hr push-pull perfusion period. The mean basal LHRH release, pulse amplitude and pl서se period were 0.68 $\pm$ 0.03 ps110 min, 1.15 $\pm$0.08 pg and 60 $\pm$ 9 min, respectivelv. Intermi구eat perfusion of P clearly stimulated the mean LHRH release (pre-P vs post-P: 1.14 $\pm$ 0.18 vs 1.99 $\pm$ 0.53 pg) without changes in LHRH pulse frequency. In contrast to intermittent infusion of p, continuous administration of P faithed to modify LHRH release, since the mean LHRH release and pulse amplitude between pre-P and post-P perfusion urere similar. The in vitro study clearly showed that intermittent, but not continuous administration of P is effective in stimulating LHRH release. Therefore, it appears that rhythmic secretion of P mal be the erective signal for activating the neural LHRH apparatus.

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Stereocomplex Poly(lactic acid) Discoidal Microparticles for Sustained Drug Release (약물지연방출을 위한 스테레오컴플렉스 PLA 원반형 마이크로입자)

  • Park, Chaewon;Park, Sanghyo;Kim, Woo Cheol;Key, Jaehong
    • Journal of Biomedical Engineering Research
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    • v.41 no.1
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    • pp.62-66
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    • 2020
  • Controlled drug release is important for effective treatment of cancer. Poly(DL-lactide-co-glycolide) acid (PLGA) is a Food and Drug Administration (FDA) approved polymer and have been extensively studied as drug delivery carriers with biodegradable and biocompatible properties. However, PLGA drug delivery carriers are limited due to the initial burst release of drug. Certain drugs require an early rapid release, but in many cases the initial rapid release can be inefficient, reducing therapeutic effects and also increasing side effects. Therefore, sustained release is important for effective treatment. Poly Lactic Acid stereo complex (PLA SC) is resistant to hydrolysis and has high stability in aqueous solutions. Therefore, in this work, PLGA based discoidal polymeric particles are modified by Poly Lactic Acid stereocomplex (PLAsc DPPs). PLAsc DPPs are 3 ㎛ in diameter, also showing a relatively sustained release profile. Fluorescein 5(6)-isothiocyanate (FITC) released from PLAsc DPPs was continuously observed until 38 days, which showed the initial release of FITC from PLAsc DPPs was about 3.9-fold reduced as compared to PLGA based DPPs at 1 hour.

Core Release Model Evaluation in the ISAAC Code for PHWR

  • Song Yong-Mann;Park Soo-Yong;Kim Dong-Ha;Kim Hee-Dong
    • Nuclear Engineering and Technology
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    • v.36 no.1
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    • pp.36-46
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    • 2004
  • The ISAAC fission product release calculation is based on detailed FPRAT models developed by Jaycor. For volatile fission product release calculations, either the Cubicciotti steam oxidation correlation or the NUREG-0772 correlation is used. In this study, evaluation is carried out for these volatile fission product release models. As a result, in the case of early release, the IDCOR model with an in-vessel Te release option shows the most conservative results and for the late release case, the NUREG-0772 model shows the most conservative results. Considering both early and late release, the IDCOR model with an in-vessel Te bound option is evaluated to show mitigated conservative results. In addition, a sensitivity study on detailed core nodalization is performed. In the study, 380 horizontal fuel channels in the Wolsong plant are nodalized into 12 (6 channels per loop, $3{\times}3$ Core Pass) representative channels and detailed by 16/20/24 channels. For reference accidents, LOAH and large LOCA are selected as representing high and low pressure sequences, respectively. According to the results, the original 12 channel approach with $3{\times}3$ core passes is evaluated to be sufficient as an optimal scheme.

Release and Bioavailability of Naloxone Sustained-Release Implants (Naloxone의 Polyphosphazene 이식제제에 관한 연구)

  • Suh, Sung-Yun;Park, Joo-Ae;Kim, Kil-Soo
    • Journal of Pharmaceutical Investigation
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    • v.27 no.3
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    • pp.225-231
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    • 1997
  • For the effective administration of naloxone, we attempted to investigate the naloxone sustained-release implants. Using the biodegradable polymer, poly[(diethyl glutamate)-co-(ethyl glycinate)phosphazenes](PGGP), the implantable devices containing naloxone hydrochloride(NLX HCl) and naloxone base(NLX) were prepared. The release rates of NLX and NLX HCl were compared. Influences of NLX contents on release rates were examined. For pharmacokinetic studies, NLX and NLX HCl loaded devices were implanted subcutaneously in rabbits and then the plasma concentrations of NLX were determined by HPLC(ECD). NLX-containing devices were implanted with various doses and pharmacokinetic parameters according to dose were calculated. The relative bioavailabilities were evaluated and compared. Incorporation of NLX in the polymer leaded to a slow release. There were no differences of release rates based on drug contents. In pharmacokinetic parameters determined in 216 hours, NLX loaded devices resulted in enhanced bioavailability with the higher AUC (p<0.01) than NLX HCl loaded devices and MRT was significantly (p<0.05) increased. This result demonstrates that NLX is more suitable for sustained release devices than NLX HCl. Therefore it is anticipated that the effective concentrations of naloxone could be maintained for longer periods and bioavailabilities could be improved by naloxone sustained-release implants, with varying drug base/hydrochloride.

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Dissolution of Chlorpheniramine Mallate (CMP) from Sustained-Release Tablets Containing CPM in the Coated Film Layer (핵정(核鐘)에 코팅된 필름층 중에 함유되어 있는 말레인산클로르페니라민의 방출특성)

  • Yu, Jei-Man;Shim, Chang-Koo;Lee, Min-Hwa;Kim, Shin-Keun
    • Journal of Pharmaceutical Investigation
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    • v.20 no.2
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    • pp.89-95
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    • 1990
  • Ethylcellulose-PEG 4000 film coated on core tablets was investigated as a potential drug delivery system for the controlled release of chlorpheniramine maleate (CPM). The kinetic analysis of the release data indicated that CPM release followed a diffusion-controlled model, where the quantity released per unit area is proportional to the square root of time. The effect of the film composition, CPM concentration, plasticizer concentration and CPM solubility on the release characteristics were examined. The release rate constant increased as CPM concentration increased. It also increased as the PEG 4000 content in the film increased above 10%(w/w), however, it decreased as the PEG 4000 content increased in the concentration range below 10%(w/w). The release rate constant was not affected by the coated weight on the core tablet. The film-coated tablets which contain CPM only in the coated film layer seemed to be a potential oral drug delivery system for the controlled release of CPM.

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EFFECTS OF A VARIOUS DRUGS ON THE RELEASE OF NEUROTRANSMITTERS FROM TRIGEMINAL SENSORY NUCLEUS (삼차신경 감각핵의 신경전달물질 유리에 대한 수 종 약물의 효과)

  • Yoon, Jung-Hae;Lee, Myung-Jong
    • Restorative Dentistry and Endodontics
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    • v.20 no.2
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    • pp.423-431
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    • 1995
  • Trigeminal spinal sensory nucleus is a main relay site in transmission of orofacial pain. Glutamate and aspartate playa role in transmission of primary afferents. This experiment was performed to study the role of capsaicin, KR-25018 and shogaol on the release of glutamate and aspartate from trigeminal spinal sensory nucleus. Release of excitatory amino acids(EAAs) was induced by electrical stimulation of oral mucosa with innocuous or noxious stimuli. Capsaicin($10{\mu}M$), KR-25018($10{\mu}M$), shogaol($10{\mu}M$), ruthenium red and capsazapine were added to perfusion solution to observe the changes in EAA release, and glutamate and aspartate were determined by HPLC. Release of glutamate and aspartate from trigeminal sensory nucleus was increased by noxious stimulation of oral mucosa, but innocuous stimulation did not affect on the release of EAA Capsaicin and KR-25018 increased the release of glutamate and aspartate, and effect of KR-25018 on release of EAA was more potent than capsaicin. But shogaol had a weak effect on release of EAA. Effect of capsaicin and KR-25018 was partially blocked by capsaicin antagonists, ruthenium red and capsazepine.

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A Study on Combustion of Living Leaves for Various Coniferous Trees and Broadleaf Trees in Youngdong Areas (영동지역 주요 침엽수종 및 활엽수종 생엽의 연소특성에 관한 연구)

  • Lee, Hae-Pyeong;Lee, Si-Young;Park, Young-Ju
    • Journal of the Korean Society of Safety
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    • v.24 no.4
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    • pp.96-103
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    • 2009
  • This study was fulfilled to investigate the forest fire risk of forest fuels based on the combustion characteristics of living leaves of coniferous trees and broadleaf trees naturally growing in Youngdong areas of Gangwon Province by using cone calorimeter and smoke density chamber. According to the result, Pinus densiflora and Pinus rigida among coniferous trees released a greater amount of heat release than other kinds. The total smoke release varied depending on the species, whereas Pinus koraiensis showed the largest amount of smoke release. With regard to maximum smoke density, it was much higher in coniferous trees than in broadleaf trees. With regard to smoke temperature, Pinus densiflora showed the lowest compared to other kinds up until 200s from the ignition, but all most trees uniformly maintained constant temperature of about $70^{\circ}C$ after 200s. The concentrations of CO and $CO_2$ release were drastically increased at about 150s and then gradually decreased thereafter. Pinus densiflora showed a bit higher CO release than broadleaf trees, but there was no distinct difference in $CO_2$ release among tress.

Batch Variation and Pharmacokinetics of Oral Sustained Release Melatonin-loaded Sugar Spheres in Human Subjects

  • Lee, Beom-Jin;Ryu, Seung-Goo;Choi, Han-Gon;Kim, Chong-Kook;Parrott, Keith-A.;Ayres, James-W.;Sack, Robert-L.
    • Archives of Pharmacal Research
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    • v.20 no.6
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    • pp.555-559
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    • 1997
  • The three different batches of an oral sustained release melatonin (MT) delivery system were prepared by aqueous-based fluid-bed coating of the sugar spheres for the evaluation of in vitro release characteristics and plasma concentration profiles in human subjects. The MT contents in 20% coated sugar spheres of three batches (B1, B2 and B3) were $3.3{\pm}0.08$, $2.4{\pm}0.1$ and $2.5{\pm}0.13$ mg per gram of coated sugar spheres, respectively. The release profiles of three different batches had a very similar fashion. However, the release profiles of three different batches had a very similar fashion. However, the release half-lives $(T_{50%})$ of MT from B1, B2 and B3 was $3.70{\pm}0.2$, $5.2{\pm}0.2$ and $4.9{\pm}0.07h$, respectively. Plasma concentration profiles of sustained release 0.2mg melatonin-loaded sugar spheres containing 10% immediate release melatonin in gelatin capsules (B1 and B2) were then evaluated in human subjects. The in vivo plasma concentration profies of the two batches (B1 and B2) were very similar each other and located between the physiological endogenous ranges. The time to reach the peak concentration $(T_max)$ was more advanced in case of B1 when compared to B2. However, there was no statistically significant difference in the maximum concentration $(C_max)$ and the area under the curve (AUC) between B1 and B2. The AUC of melatonin-loaded sugar spheres containing 10% and 20% immediate release MT in human subjects had a good linearity between dose and AUC, regardless of the fraction of immediate release MT, indicating the first order elimination process of MT within these doses. The current oral sustained release MT delivery system may be utilized to treat circadian rhythm disorders if it is proven to be more clinically useful when compared to immediate release MT.

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Study on the Negligible Extent(NE) and Release Characteristic of KS C IEC 60079-10-1(2015) Standard (KS C IEC 60079-10-1 규격의 무시할 수 있는 정도와 누출특성에 관한 연구)

  • Cho, Pil-rae;Lee, Hyang-jig;Baek, Jong Bae
    • Journal of the Korean Society of Safety
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    • v.35 no.2
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    • pp.111-117
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    • 2020
  • When KS C IEC 60069-10-1(2015) standard is applied to estimate a hazardous area, the chart showing the relationship between a hazardous area distance and release characteristic is used as a guide to determine the extent of hazardous zones for various forms of release. Three release characteristic lines based on the three types of release as an unimpeded jet release with high velocity, a diffusive jet release with low velocity, and a release of heavy gases or vapours that spread along horizontal surfaces are given. As these characteristic lines have the low limit threshold, it is difficult to estimate the hazardous area distance when the value of release characteristic is under the low limit threshold. And KS C IEC 60079-10-1(2015) standard shows the concept for a zone of Negligible extent(NE) which can be considered as non hazardous area, but it is also difficult to apply the concept of a Negligible extent. The purpose of this paper is to suggest the guideline for the release characteristic to decide a hazardous area distance and the Negligible extent(NE) being considered as non-hazardous area when deciding a hazardous area distances by the KS C IEC 60079-10-1 standard.

Controlled Release Dosage Form of Narcotic Antagonist(I): Synthesis of Biodegradable Polyphosphazenes and Preparation and Release Characteristics of Naloxone Implant (마약길항제의 방출 제어형 제제 (제1보) : 생체분해성 polyphosphazenes의 합성과 나록손 이식제제의 제조 및 용출특성)

  • Park, Joo-Ae;Lee, Seung-Jin;Kim, Hyung-Kuk;Kim, Kil-Soo
    • Journal of Pharmaceutical Investigation
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    • v.25 no.2
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    • pp.109-116
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    • 1995
  • For the administration of narcotic antagonist with short half-life and low patient compliance, the sustained release system using biodegradable matrix is effective. Polyphosphazenes are of considerable interest as biodegradable matrix systems for controlled release of drugs. In this study, biodegradable polyphosphazenes available for the sustained release implantable device were synthesized, and their application was examined. Poly[dichlorophosphazene] was synthesized by solution polymerization method and confirmed with IR spectrum. Poly[bis(ethyl glycinate) phosphazene] and poly[ (diethyl glutamate)-co-(ethyl glycinate)phosphazene] were then produced by substitution of amino acid alkyl esters for chloride side groups. Using these polymers, the implantable devices of 1 mm thickness and $10{\times}10\;mm$ size containing naloxone hydrochloride were prepared and their release and degradation profiles were measured. In the case of poly[bis(ethyl glycinate)phosphazene] with swelling characteristics, degradation rate was slower than the release rate, showing that the release rate is partly dependent on the swelling rate. In contrast, the degradation rate of polyl[(diethyl glutamate)-co-(ethyl glycinate)phosphazene] matrix was identical with release rate of naloxone hydrochloride. On the basis of these results, it is expected that these polymers can be applied to sustained release implantable systems delivering narcotic antagonist.

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