• Title/Summary/Keyword: Slow-release

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The Formulation and Bioavailability of Oral Sustained Release Sulindac Delivery System (설린닥의 경구용 지속성 제제설계 및 생체이용율)

  • Rhee, Gye-Ju;Park, Sun-Hee;Whang, Sung-Joo
    • YAKHAK HOEJI
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    • v.41 no.1
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    • pp.60-73
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    • 1997
  • In order to design a 24 hr sustained release preparation of sulindac for oral administration, fast release pellet (FR), slow release pellet (SR) and two combined formulation (1 : 1 and 1 : 2) were prepared. The pharmacokinetic effect of such preparations has been evaluated using rabbits as a suitable in vivo model, and tested in man. Dose determination was carried out using curve fitting according to RSTPJP II program. In bioavailability test using rabbit, AUCs of sulindac in a few designed formulations were similar to each other. $C_{max}$- of RF and SR were 1.8 times and 1.2 times higher, respectively, compared to that of combined formulation (FR:SR=1:1). While plasma concentration of FR and SR decreased rapidly, that of combined formulation (FR:SR 1:1) lasted at the level close to $C_{max}$ for 24 hrs. Plasma concentration of sulfide form from the combined pellet(FR:SR=1:1) lasted for 24 hrs, and its AUC value was 1.4-fold, 2.7-fold. and 1.2-fold greater than FR pellet, SR pellet and combined pellet (FR:SR 1 : 2). Thus, the combined pellet of 1:1 ratio was found to be the most effective for oral sustained release formulation. Bioavailability test in human showed that AUC of sulfide from TSRP (1 : 1) was approximately 1.5 times greater than total AUC of Immbaron$^{\circledR}$ administered twice in a day. While $T_{max}$ of sulfide from lmmbaron$^{\circledR}$ was 4.33 +/- 1.37 hr (lst administration) and 3.33 ${pm}$ 0.82 hr (2nd administration), respectively, that of sulfide from TSRP increased to 7.17 ${pm}$ 2.86 hr. Plasma concentration of sulfide from TSRP was sustained at more, than 1.0 ${\mu}g{\cdot}$hr/ml until 24 hrs after one dose administration. In addition, TSRP may decrease local adverse reaction in the stomach, since plasma concentration of sulfide from the combined pellet was low within 2hrs in the stomach. In conclusion, it is suggested that TSRP formulation may be effective for oral 24 hr sustained release formulation of sulindac dosing 300 ~ 350mg once a day.

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The Release of Albumin from PLGA and PCL Wafers Containing Natural and Synthetic Additives for Protein Delivery (단백질 전달체로서 천연 및 합성재료의 첨가에 따른 PLGA와 PCL웨이퍼로부터 알부민의 방출거동)

  • Hyun Hoon;Lee Jae Ho;Seo Kwang Su;Kim Moon Suk;Rhee Jhon M.;Lee Hai Bang;Khang Gilson
    • Polymer(Korea)
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    • v.29 no.5
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    • pp.468-474
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    • 2005
  • PLGA and PCL copolymers initiated by carbitol as drug carriers were synthesized by ring-opening polymerization of L-lactide (LA), glycolide (GA), and $\varepsilon-caprolactone(\varepsilon-CL)$. Implantable wafers were simply fabricated by direct compression method after physical mixing of copolymers and bovine serum albumin-fluorescein isothiocyanate (BSA-FITC) as a model protein drug. The release amounts of BSA-FITC from wafers were determined by fluorescence intensity using the fluorescence spectrophotometer. Also, the release behavior of BSA-FITC on wafers was controlled by adding the additives such as collagen, small intestinal submucosa (SIS), poly(vinyl pyrrolidone) (PVP), and poly(thylene glycol) (PEG). The wafer prepared by PLGA and PCL exhibited slow release within $10\%$ for 30 days. But, those prepared by a variety of additives exhibited the controlled BSA release patterns with a dependence on the additive contents. furthermore, the wafers containing natural materials such as collagen and SIS showed more zero-order release profile than that with synthetic materials such as PVP and PEG. It was confirmed that the release of BSA from implantable wafers could be easily controlled by adding natural additives.

Response of the Application of Slow-release Potassium Fertilizer Using Natural Zeolite to Flue-cured Tobacco (Nicotiana tabacum L.) (천연(天然) Zeolite를 이용한 완효성(緩效性) K 비료(肥料)의 황색종(黃色種) 연초(煙草)에 대(對)한 시용효과(施用效果))

  • Lee, Dong-Hoon;Park, Soo-June;Choi, Jyung
    • Korean Journal of Soil Science and Fertilizer
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    • v.22 no.3
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    • pp.215-220
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    • 1989
  • For development of slow releaseing K-fertilizer using natural zeolite, two kinds of K adsorbed zeolite were made by ion exchange reaction in $K^+$ saturated aqueous solution. K-Zeolite was prepared by removing the excess salt after K adsorption on zeolite, however, NW. K-Zeolite was prepared only by K adsorption reaction without removing the excess salt. The adsorbed K on zeolite was not easily released, but continuously and slowly released from the surface of zeolite. By the results of application for tobacco cultivation, the K contents in soil treated with K-Zeolite and NW. K-Zeolite were lower than that of control (20kg/10a) at the early growth stage, but were higher at the late growth stage. Therefore, the results suggest that K adsorbed zeolite could be applied as a slow-releasing K fertilizer.

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Changes in th Chemical Components and Antioxidant Activity of Strawberry by Slow-released ClO2 Gas Gel-Pack during Storage (서방형 이산화염소 가스 젤팩을 이용한 딸기저장 중 주요 성분 및 항산화 활성의 변화)

  • Lee, Kyung-Haeng;Yoon, Ye-Ji;Lee, Bom;Bong, So-Jung;Kim, Hyun-Kyoung;Kwak, Il-Hwan;Kim, Hong-Gil
    • The Korean Journal of Food And Nutrition
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    • v.30 no.4
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    • pp.823-829
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    • 2017
  • To increase the shelf-life of strawberry, samples were treated with two gel packs containing slow-released chlorine dioxide ($ClO_2$) gas at 3~5 ppm for 6 days at room temperature and the changes in the major chemical components (ascorbic acid, polyphenols, flavonoids and anthocyanin) contents and antioxidative activities (DPPH, ABTS radical scavenging and metal chelating activity) were investigated. The content of ascorbic acid of control was 40.38 mg% and contained 35.67~44.75 mg% during 6 days. There was no tendency to increase or decrease during storage period. The contents of ascorbic acid of control and 3~5 ppm $ClO_2$ gas treated samples were not significantly different during storage period. The content of polyphenol compounds of initial stage was 111.23 mg% and contained 117.78~132.40 mg% during 6 days. The contents of polyphenol compounds of 3~5 ppm $ClO_2$ gas treated samples were 103.51~130.25 mg%. There were no significant different between them during storage. The flavonoids and anthocyanin contents were not different from the control during storage period regardless of 3~5 ppm $ClO_2$ gas treatment. Furthermore, antioxidative activities were not different among the control and $ClO_2$ gas treatments during storage.

Changes in Lipid Oxidation and Taste Compounds of Chicken Breast Meat by Slow-released ClO2 Gas Gel-pack during Storage (서방출형 이산화염소 가스 젤팩 첨가가 닭가슴육 저장 중 지질산패 및 정미성분의 변화)

  • Lee, Kyung-Haeng;Kwon, Hye-Won;Yoon, Ye-Ji;Kim, Hong-Gil
    • The Korean Journal of Food And Nutrition
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    • v.32 no.4
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    • pp.294-303
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    • 2019
  • To extend the shelf-life of chicken breast meat, samples were treated with gel-packs containing slow-released $ClO_2$ gas at 7-15 ppm for 8 days at $4^{\circ}C$. And the changes in lipid oxidation and taste compounds of the samples were investigated. TBARS value of the chicken breast was slightly increased during storage. TBARS value of gas treatments was similar to the control during storage. There were 14 fatty acids in the chicken breast. And there was no change in the fatty acid composition during storage, and there was no significant difference between the control and gas treatments. The content of free amino acids was gradually increased during storage. The content of free amino acids were not significantly different between the control and gas treatments during storage. The content of GMP in the control and gas treatments were decreased during storage. However, gas treatments showed slightly higher content than that of control. AMP was not significantly different between the control and gas treatments. IMP gradually decreased during storage and the content of inosine and hypoxanthine was increased. IMP, inosine and hypoxanthine contents of gas treatment were similar to control, but the control tended to change more rapidly than those of gas treatments.

The Influence of Several Drugs Affecting $Ca^{2+}$ Influx on Frequency-tension Curve of Rat Left Atrium (쥐의 좌심방에서 세포막을 통한 $Ca^{2+}\;Flux$에 영향을 주는 약물이 자극빈도-장력 곡선에 미치는 영향)

  • Kim, Chan-Yun;Ahn, Sok-Kyun;Suh, Chang-Kook;Kang, Doo-Hee
    • The Korean Journal of Physiology
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    • v.23 no.2
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    • pp.329-337
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    • 1989
  • Cardiac muscles show stimulation frequency-dependent tension changes i.e. Bowditch phenomenon and Woodworth phenomenon, the former is an increase of tension with the increase of stimulation frequency, whereas the latter is an increase of tension with a decrease of stimulation frequency. Bowditch phenomenon is seen in the range of frequency 1.0 cps and above, and Woodworth phenomenon below the frequency 1.0 cps in the most of mammalian cardiac atrium. To throw some light on the possible mechanism of both phenomena in rat atrium, influences of drugs affecting $Ca^{2+}$ influx through the plasma membrane $(verapamil,\;La^{3+},\;norepinephrine)$ and $Ca^{2+}$ release from sarcoplasmic reticulum (SR) on frequency-tension curve were studied. The results obtained are summarized as follows: 1) At low temperature $(27.5^{\circ}C)$, both Bowditch and Woodworth phenomenon were demonstrated. But Bowditch phenomenon disappeared at the temperature above $(32.5^{\circ}C)$. 2) At $(27.5^{\circ}C)$, in the presence of verapamil, a $Ca^{2+}$ channel blocker, a time course of change in the frequency-tension was studied. It was found that Bowditch phenomenon was affected before the Woodworth phenomenon, then the former was completely disappeared. At $(32.5^{\circ}C)$, where no Bow-ditch is seen in normal atrial muscle, Bowditch phenomenon was reappeared by an administration of norepinephrine suggesting again that slow inward current of such as $Ca^{2+}$ channel is closely related to Bowditch phenomenon. 3) At $27.5^{\circ}C$, in the presence of $La^{3+}$, although tensions were decreased at all stimulation frequencies, Bowditch and Woodworth phenomenon were still demonstrated. However in the presence of both $La^{3+}$ and verapamil, Bowditch phenomena was disappeared suggesting that $La^{3+}$ is less effective in blocking $Ca^{2+}$ channel than verapamil. 4) At $27.5^{\circ}C$, in the presence of ryanodine, an inhibitor of calcium release from SR, Woodworth phenomenon was disappeared, which was consistent with previous reports of others, suggesting that $Ca^{2+}$ release from SR is closely related to Woodworth phenomenon. From the above findings, it may be concluded that Bowditch phenomenon is dependent on the magnitude of $Ca^{2+}$ influx through slow channel and Woodworth phenomenon is dependent on the amount of $Ca^{2+}$ stored in SR.

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Evaluating Various Nitrogen Sources for Divot Recovery on Creeping bentgrass (Creeping bentgrass의 생육과 디봇피해 회복을 위한 질소의 유형별 효과)

  • Lee, Sang-Kook
    • Asian Journal of Turfgrass Science
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    • v.26 no.2
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    • pp.135-139
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    • 2012
  • Creeping bentgrass (Agrostis stolonifera) is one of the most popular turfgrasses for high-quality playing surface such as putting green on golf courses and athletic fields. Continues damage such as divot injury on creeping bentgrass is major issue to maintain golf course properly. Although plentiful researches to maximize divot resistance have been reported, minimal research has focused on relation between nitrogen (N) sources and divot resistance. The study was conducted to determine the effect of N source for turfgrass divot recovery and overall tee performance. Eleven fertilizer treatments as N sources were applied to creeping bentgrass 'Penncross'. Before the first application, divot injuries were simulated by removing a core of soil and turfgrass from established plots and backfilling with native soil. Data collection included turfgrass color and quality. N release speed did not influenced divot recovery. Frequency of urea application had no effects on divot recovery. Urea with split application had no difference with no treatment for divot recovery. Polyon product especially polyon mini (41-0-0) had the best performance for divot recovery and for maintaining better turfgrass quality. Overall, small particle size of slow-release N form would influence creeping bentgrasss to recover divot damage.

Effect of Sustained-Release of Adenosine by Elvax 40P Implant on Mouse Mammary Development (생쥐의 유선발달에 있어서 Elvax 40P Implant를 이용한 서방형 Adenosine의 역할)

  • 여인서;박춘근;홍병주
    • Korean Journal of Animal Reproduction
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    • v.16 no.4
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    • pp.387-397
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    • 1993
  • To examine local response of adenosie(purine nucleoside) on the developing mammary gland, Elvax 40P implants containing adenosine were surgically implanted into mammary fat pad of the five week old female ICR mice. Inguinal(the 4th) mammary glands of anesthetized mice were exposed andplaced the implants for 12 days. One gland was treated with an adenosine implant, while the contralateral gland received a blank implant as control. For whole-mount preparations, glands were stained with alum carmine, and for histological observation, micro-selected mammary glands were stained with hematoxylin and eosin Y. Implantation with Elvax 40P did not affect on the damage of neighboring mammary tissue. Adenosie 25 or 250$\mu\textrm{g}$ per slow-release implant stimulated local mammary end bud formation of ovariectomized mice such as end bud size and numbers of end bud per gland in a dose dependent manner(P<0.05), and lower concentration of adenosie(2.5 or 25$\mu\textrm{g}$/implant) increased numbers of end bud(P<0.05) and end bud size(P<0.1) of intact mice. Adenosine treatment and intact ovarian function had moderate interation effects on the stimulation of end bud formation at 2.5$\mu\textrm{g}$ adenosine/implant(P<0.1). In histological observation, adenosine implants increased numbers of mammary epithelial type of cells at mammary duct in the presence or absece ofovary. These results indicate that adenosine should be one of regulators in mouse mammary ductal growth.

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Synthesis and Drug-Releasing Behavior of Various Polymeric Prodrugs of PGE1 with PEG and Its Derivative as Polymer Carriers

  • Lee, Chan-Woo
    • Journal of Biomedical Engineering Research
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    • v.28 no.4
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    • pp.484-493
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    • 2007
  • Two polymeric prodrugs of PGE1 (prodrugs IVg and PNg) were newly synthesized. The drug conjugation proceeded in quantitative yield without decomposition of PGE1 to PGA1. With two types conjugates, PEG-PGE1 and PN-PGE1 with different spacer groups, we first discovered a possibility of slow release of PGE1 in blood circulatory system. PGE1 is conjugated with PEG and PN through the long alkylene spacers, and their availability as polymeric prodrugs is evaluated. Their drug-releasing behavior was examined both in phosphate buffer (pH=7.4) and rat plasma. Each prodrug was known to be highly stabile in the buffer solution. The drug-releasing rate became much faster in rat plasma than in the buffer solution due to the acceleration by the plasma enzymes. The drug-release was found to reach a plateau in rat plasma because the released PGE1 or its derivatives may be captured or decomposed by the plasma proteins. The slower drug-releasing rate of pro drug PNg in rat plasma is reasonably attributed to the molecular aggregation due to the hydrophobic bonding between the PGE1 moieties and spacers.

Calibration and Sensitivity Analysis of the RICEWQ Model (RICEWQ 모형의 보정 및 민감도 분석)

  • Chung, Sang-Ok;Park, Ki-Jung;Son, Seung-Ho
    • Journal of The Korean Society of Agricultural Engineers
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    • v.50 no.2
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    • pp.3-10
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    • 2008
  • The main objectives of this study are to calibrate the RICEWQ model with Korean field data and then analyse the sensitivity of the parameters to identify sensitive parameters. The RICEWQ is widely used to predict pesticide fate in a paddy plot. An experimental paddy plot of 0.2 ha($100{\times}20\;m$) at Seobyeon-dong, Daegu, Korea was selected, and field observations for water and pesticide balance were performed from 4 June to 2 September 2006. The molinate, which is a herbicide widely used for weed control in rice culture, was selected. The RICEWQ model was successfully calibrated both for the water and pesticide mass balance. The calibrated model showed a RMSE of 0.537 cm for ponded water depths and a RMSE of 0.036 mg/L for the molinate concentrations in the ponded water. The most sensitive parameters for molinate concentrations in ponded water were the metabolism degradation rate in water, volatilization coefficient, and release rate for slow release formulation. In contrast, the RICEWQ model was not sensitive to parameters such as hydrolysis degradation rate in water and degradation rate in unsaturated soil.