• Title/Summary/Keyword: Order release

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Preparation of Biodegradable PLGA Microspheres for Sustained Local Anesthesia and Their in vitro Release Behavior (지속적인 국소마취를 위한 생분해성 PLGA 미립구의 제조와 생체외 방출 거동)

  • 조진철;강길선;최학수;이종문;이해방
    • Polymer(Korea)
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    • v.24 no.5
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    • pp.728-735
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    • 2000
  • Fentanyl-loaded biodegradable poly(L-lactide-co-glycolide) (75 : 25 by mole ratio of lactide to glycolide, PLGA) microspheres (MSs) were prepared to study the possibility for long-acting local anesthesia. We developed the fentanyl base (FB, slightly water-soluble)-loaded PLGA MSs by means of conventional O/W solvent evaporation method. The size of MSs was in the range of 10~150 ${\mu}{\textrm}{m}$. The morphology of MSs was characterized by SEM, and the in vitro release amounts of FB were analyzed by HPLC. The lowest porous cross-sectional morphology and the highest encapsulation efficiency were obtained by using gelatin as an emulsifier. The influences of several preparation parameters, such as emulsifier types, molecular weights and concentrations of PLGA, and initial drug loading amount, etc., have been observed in the release patterns of FB. The release of FB in vitro was more prolonged over 25 days, with close to zero-order pattern by controlling the preparation parameters. We also investigated the physicochemical properties of FB-loaded PLGA MSs by X-ray diffraction and differential scanning calorimeter.

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Kinematical Analysis of Handball Step Shoot according to Attack Position (공격위치에 따른 핸드볼 스텝슛의 운동학적 분석)

  • Kang, Sang-Hack
    • Korean Journal of Applied Biomechanics
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    • v.15 no.4
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    • pp.55-66
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    • 2005
  • The present study used a video analysis system to quantify the kinematical data of step shoot motion by male university handball players. From the results of analyzing dynamic variables of step shoot motion according to shooting direction were drawn conclusions as follows. 1. The height of release was proportional to the height of players, and the height of release appeared low in left-side attacks. This is probably because the left-right-throwing angle is larger in left-side attacks than that in center attacks and right-side attacks and, as a result, the throwing arm is lowered down in throwing. 2. The leftward inclination angle of the body was larger in order of right-side attacks > center attacks > left side attacks. 3. Players' throwing form was close to three quarter style in left-side attacks. In center and right-side attacks, the arm was somewhat more upright but still it was more three quarter style than overhand style. 4. The front-rear throwing angle at the moment of release was much higher in right-side attacks than in left-side ones. This is probably because the point of time for releasing the ball is usually late in right-side attacks and, as a result, the front-rear throwing angle becomes quite large. 5. The contribution of body parts on the ball speed was higher in order of the forearm > upper arm, hand > shoulder joint. 6. In players whose distance between the two legs at the moment of release, their body usually did not incline to the side much. Thus it is considered necessary to correct the right leg in their shooting motion. 7. According to the result of analyzing throwing form, the speed of the ball at the moment of leaving the hand was faster in right-side attacks than in left-side and center attacks.

Study on Physicochemical Characteristics and Bioavailability of Fenbufen Suppositories (Fenbufen 좌제(坐劑)의 물리화학적(物理化學的) 성상(性狀) 및 생체이용률(生體利用率)에 관(關)한 연구(硏究))

  • Kim, Johng-Kap;Hong, Soun-Uk
    • Journal of Pharmaceutical Investigation
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    • v.14 no.2
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    • pp.55-61
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    • 1984
  • This investigation was designed to determine the release of fenbufen from suppositories and their bioavailability in rabbits. Suppositories containing fenbufen were made by the fusion method with Witepsol H-15, Wecobee and PEG 1540 base. Displacement value, weight variation, content uniformity, melting point and melting time were determined for preformulation of the fenbufen suppositories. The release rates were determined with the KP dissolution apparatus and with cellophane tube dialysis device and were increased in order of PEG 1540, Witespol H-15 and Wecobee. The bioavailabilities of fenbufen after rectal administration were also increased in order of PEG 1540, Witespol H-15 and Wecobee.

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Characteristics of $A_1\;and\;A_2$ Adenosine Receptors upon the Acetylcholine Release in the Rat Hippocampus

  • Kim, Do-Kyung;Lee, Young-Soo;Choi, Bong-Kyu
    • The Korean Journal of Physiology and Pharmacology
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    • v.2 no.1
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    • pp.31-39
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    • 1998
  • As it has been reported that the depolarization induced acetylcholine (ACh) release is modulated by activation of presynaptic $A_1$ adenosine heteroreceptor and various lines of evidence suggest the $A_2$ adenosine receptor is present in the hippocampus. The present study was undertaken to delineate the role of adenosine receptors on the hippocampal ACh release. Slices from the rat hippocampus were equilibrated with $[^3H]choline$ and then the release amount of the labelled product, $[^3H]ACh$, which was evoked by electrical stimulation (rectangular pulses, 3 Hz, 2 ms, 24 mA, $5\;V/cm^{-1}$, 2 min), was measured, and the influence of various adenosine receptor-related agents on the evoked tritium outflow was investigated. And also, the drug-receptor binding assay was performed in order to confirm the presence of $A_1$ and $A_2$ adenosine receptors in the rat hippocampus. N-ethylcarboxamidoadenosine (NECA), a potent adenosine receptor agonist with nearly equal affinity at $A_1$ and $A_2$ adenosine receptors, in concentrations ranging from $1{\sim}30\;{\mu}M$, decreased the electrically-evoked $[^3H]ACh$ release in a concentration-dependent manner without affecting the basal rate of release. And the effect of NECA was significantly inhibited by 8-cyclopentyl-1,3-dipropylxanthine (DPCPX, 2 ${\mu}M$), a selective $A_1$ adenosine receptor antagonist, but was not influenced by 3,7-dimethyl-1-propargylxanthine (DMPX, 5 ${\mu}M$), a specific $A_2$ adenosine receptor antagonist. $N^6-cyclopentyladenosine$ (CPA), a selective $A_1$ adenosine receptor agonist, in doses ranging from 0.1 to 10 ${\mu}M$, reduced evoked $[^3H]ACh$ release in a dose-dependent manner without the change of the basal release. And the effect of CPA was significantly inhibited by 2 ${\mu}M$ DPCPX treatment. 2-P-(2-carboxyethyl)-phenethylamino-5'-N-ethylcarboxamidoadenosine hydrochloride (CGS-21680C), a potent $A_2$ adenosine receptor agonist, in concentrations ranging from 0.1 to 10 ${\mu}M$, did not alter the evoked ACh release. In the drug-receptor binding assay, the binding of $[^3H]2-chloro-N^6-cyclopentyladenosine$ ($[^3H]$CCPA) to the $A_1$ adenosine receptor of rat hippocampal membranes was inhibited by CPA ($K_i$ = 1.22 nM), NECA ($K_i=10.17 nM$) and DPCPX ($K_i=161.86 nM$), but not by CGS-21680C ($K_i=2,380 nM$) and DMPX ($K_i=22,367 nM$). However, the specific binding of $[^3H]CGS-21680C$ to the $A_2$ adenosine receptor was not observed. These results suggest that the $A_1$ adenosine heteroreceptor play an important role in evoked ACh release, but the presence of $A_2$ adenosine receptor is not confirmed in this study.

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Concentration of elemental ions released from non-precious dental casting alloys (치과주조용 비귀금속 합금의 금속 용출 수준)

  • Sakong, Joon;Park, Soo-Chul
    • Journal of Technologic Dentistry
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    • v.35 no.1
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    • pp.1-17
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    • 2013
  • Purpose: This study was to assess the extents of the release of metals from the non-precious alloys used for dental casting by measuring the differences in the extents of the release of metals by types of alloys, pH level and elapsed time. Methods: Uniform-sized specimens(10 each) were prepared according to the Medical Device Standard of the Korea Food and Drug Administration(2010) and International Standard Organization(ISO22674, 2006), using four types of alloys(one type of Ni-Cr and one type of Co-Cr used for fixed prosthesis, and one type of Ni-Cr and one type of Co-Cr used for removable prosthesis). A total of 12 metal-release tests were performed at one-day, three-day, and two-week intervals, for up to 20 weeks. The metal ions were quantified using an Inductively Coupled Plasma-Atomic Emission Spectrometer. Results: The results showed that the extent of corrosion was higher in the ascending order of Jdium-$100^{(R)}$, Bellabond-$Plus^{(R)}$, Starloy-$C^{(R)}$, and Biosil-$F^{(R)}$. The lower the pH and the longer the elapsed time were, the greater the increase in metal corrosion. At pH 2.4, the release of Ni from Jdium-$100^{(R)}$, a Ni-Cr alloy, was up to 15 times greater than the release of Co from the Co-Cr alloy from two weeks over time, indicating that the Ni-Cr alloy is more susceptible to corrosion than the Co-Cr alloy. Conclusion: It is recommended that Co-Cr alloy, which is highly resistant to corrosion, be used for making dental prosthesis with a non-precious alloy for dental casting, and that non-precious alloy prosthesis be designed in such a way as to minimize the area of its oral exposure. For patients with non-precious alloy prostheses, a test of the presence or absence of periodontal tissue inflammation or allergic reaction around the prosthesis should be performed via regular examination, and education on the good management of the prosthesis is needed.

Generalization of Vertical Plume Despersion in the concective Boundary Layer at Long Distances on Mesoscale (중거리에서 대류경계층 연직방향 plume 확산의 일반화)

  • 서석진
    • Journal of Korean Society for Atmospheric Environment
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    • v.16 no.2
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    • pp.141-150
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    • 2000
  • In order to genralize the vertical dispersion of plume at long distances on mesoscale over complex terrain dispersion coefficients data have been obtained systematically according to lapsed time after release by using a composite turbulence water tank that simulates convective boundary layer. Dispersion experiments have been carried out for various combined conditions of thermal turbulence intensity mechanical turbulence intensity and plume release height at slightly to moderately unstable conditions. Results of tracer dispersion experiments conducted using water tank camera and image processing system have been converted into atmospheric dispersion data through the application of similarity law. The equation $\sigma$z/Zi=aX/(b+c X2)0.5 where $\sigma$2; vertical dispersion coefficient zi : mixing height X : dimen-sionaless downwind distance was confirmed to be an appropriate and general equation for expressing $\sigma$2 variation with turbulence intensity and plume release height, The value of "a" was found to be principally affected by mechanical turbulence intensity and that of "b" by mechanical turbulence intensity and release height. It was confirmed that the magnitude of "c" varies with release height. Results of water tank experiments on the relationship of $\sigma$2 vs downwind distance x have been compared with actual atmospheric dispersion data such as CONDORS data and Bowne's nomogram Operating conditions of a composite turbulence water tank for simulating the field turbulence situations of CONDORS experiments and Bowne's $\sigma$2(x) nomogram for suburban area have also been investigated in terms of water temperature difference between convection water tank and bottom plate heating tank grid plate stroke mixing water depth length scale and velocity scale. Moreover the effect of mechanical turbulence intensity on vertical dispersion has been discussed in the light of release height and downwind distance. height and downwind distance.

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Effect of Heavy Metals on the Secretion of Amylase in Rat Pancreatic Fragments (중금속류가 취절편의 Amylase 분비에 미치는 영향)

  • Kim, Hea-Young;Kim, Won-Joon
    • The Korean Journal of Pharmacology
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    • v.17 no.2
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    • pp.31-36
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    • 1981
  • Heavy metals which are present as trace elements in human body have been known to modify various enzymatic reaction. These metals can be essential or non-essential. Zinc, copper and calcium are essential in maintaining some biological processes, whereas non-essential metals such as cadmium, lead and mercury produce accumulatve toxic effect. Cadmium accumulated in pancreas can cause toxicity and damage of pancreatic cells, thereby influencing CHO metabolism. Lead compounds are known to produce toxic effects on the kidney, digestive system and brain fellowed by inhibition of activity of ${\rho}-aminolevulinic$ acid and biosynthesis of hemoproteins and cytochrome. Evidence has been accumulated that zinc not only acts as a cofactor in enzyme reaction but also prevents toxic effect induced by heavy metal such as copper and cadmium. To demonstrate the effect of heavy metals on pancreatic secretion, part of uncinate pancreas was taken and incubated in Krebs-Ringer bicarbonate buffer with heavy metals used. Additional treatment with CCK-OP was performed when needed. After incubation during different period of time, medium was analyzed for amylase activity using Bernfeld's method. The present study was attempted in order to elucidate the effect of several kinds of heavy metal on exocrine pancreatic secretion in vitro. The results obtained are as follows: 1) CCK-OP stimulated significantly amylase release from pancreatic fragments in vitro. 2) CCK-OP response of amylase release from pancreatic fragments was inhibited by treatmant with cadmium, especially high doses of cadmium. 3) CCK-OP response of amylase release from pancreatic fragments was inhibited when pretreated with $10^{-4}M$ copper chloride. 4) Lead chloride at the concentration of $10^{-3}M\;and\;10^{4}M$ stimulated the basal amylase release in vitro but CCK-OP response did not augment by lead chloride. 5) Zine chloride did not affect amylase release from pancreatic fragment in vitro. From the results mentioned above, it is suggested that CCK-OP response was inhibited it the amylase release from pancreatic fragments pretreated with cadmium and copper chloride.

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Characteristics of Nifedipine Loaded PLGA Wafer (니페디핀을 함유한 생분해성 PLGA 웨이퍼의 제조와 특성분석)

  • 서선아;최학수;이동헌;강길선;이해방
    • Polymer(Korea)
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    • v.25 no.6
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    • pp.884-892
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    • 2001
  • Biodegradable wafers were prepared with poly (L-lactide-co-glycolide) (50 : 50 mole ratio of lactide to glycolide, molecular weight:5000 g/mole) by direct compression method for the sustained release of nifedipine to investigate the possibility of the treatment of hypertension. PLGA wafers were prepared by altering initial drug/polymer loading ratio, wafer thickness, and hydroxypropyl methylcellulose (HPMC) content. These wafers showed new zero-order release patterns for 11 days, and various biphasic release patterns could be obtained by altering the composition of wafers such as addition of matrix binder as HPMC to the PLGA wafer to reduce release rate of initial phase. The onset of polymer mass loss only occured after 4 days and about 40% of mass loss was observed after 11 days nifedipine release. This system had advantages in terms of simplicity in design and obviousness of drug release rate and may be useful as an implantable dosage form.

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Release Properties of BSA from Pectin Heads for Colonic Drug Delivery (Colonic Delivery를 위한 펙틴 비드로부터 BSA의 방출 특성)

  • 최춘순;박상무;송원현;이창문;이기영;김동운;김진철
    • KSBB Journal
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    • v.18 no.2
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    • pp.161-164
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    • 2003
  • Oral drug delivery system using pectin gel was developed for colon-targeting of peptide drug. BSA(bovine serum albumin)-loaded pectin and pectin-alginate beads were prepared for drug release properties in vitro. Morphological studies by electron microscopy indicated that pectin and pectin-alginate beads were spherical in shape and approximately 1.0 mm. In order to find the suitable beads, effects of cross-linking agents (calcium chloride or zinc acetate) and drying temperature of beads were investigated. Drug release decreased with concentration of cross-linking agents and drying temperature. For colonic drug delivery from pectin and pectin-alginate beads, pectin degradable enzymes were added at 5 hrs from the beginning of drug release. After addition of enzymes, drug release was suddenly increased against free enzymes. Therefore, pectin and pectin-alginate beads can be promised as useful drug release carriers for colon-targeted delivery.

Preparation of BCNU-loaded PLGA Wafers and In Vitro Release Behavior (BCNU 함유 PLGA 웨이퍼의 제조와 생체외 방출거동)

  • 성하수;문대식;강길선;이정식;이해방
    • Polymer(Korea)
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    • v.26 no.1
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    • pp.128-138
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    • 2002
  • 1,3-Bis(2-chloroethyl)-1-nitrosourea (BCNU, Carmustine)-loaded poly(D, L-lactide-co-glycolide) (PLGA, lactide/glycolide mole ratio 75 : 25) microparticles were prepared and fabricated into wafers in an attempt to study the possibility for the treatment of malignant glioma by direct inserting the wafers to the tumor or the cavity remained after surgical resection of the tumor. SEM observation of the microparticles prepared by spray drying method revealed that the microparticles were spherical, i. e. microspheres. Significant reduction of the crystallinity of BCNU encapsulated in PLGA was confirmed by X-ray diffraction and differential scanning calorimetry analyses of the BCNU-loaded PLGA microparticles. Release pattern of BCNU was dependent on several preparation parameters, such as the molecular weight and concentration of PLGA, and initial BCNU loading amount, etc. In vitro release of BCNU was prolonged over 8 weeks with close to zero-order release pattern after initial burst effect. Observations of morphological change of wafers and pH change of release media during release test period confirmed that hydration and degradation of PLGA would be facilitated with an increase of BCNU-loading amount.