• 제목/요약/키워드: Slow release

검색결과 234건 처리시간 0.025초

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

  • 이계주;박선희;황성주
    • 약학회지
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    • 제41권1호
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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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단백질 전달체로서 천연 및 합성재료의 첨가에 따른 PLGA와 PCL웨이퍼로부터 알부민의 방출거동 (The Release of Albumin from PLGA and PCL Wafers Containing Natural and Synthetic Additives for Protein Delivery)

  • 현훈;이재호;서광수;김문석;이종문;이해방;강길선
    • 폴리머
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    • 제29권5호
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    • pp.468-474
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    • 2005
  • 약물 전달체로서 캬비톨에 의해 개시된 PLGA와 PCL은 락타이드, 글라이콜라이드, 그리고 카프로락톤의 개환 중합에 의해서 합성되었다. 이들 합성고분자를 이용한 이식형 웨이퍼는 합성고분자와 모델 단백질 약물로서 소혈청알부민의 물리적 혼합 후에 성형 압축법에 의해서 간단히 제조되었다. 웨이퍼로부터 알부민의 방출량은 형광측정기를 사용하여 형광 강도에 의해서 측정되었다. 또한 웨이퍼에서 알부민의 방출거동은 콜라겐, 소장점막하조직, 폴리비닐피롤리돈, 그리고 폴리에틸렌글리콜과 같은 첨가제를 통해 조절되었다. PLGA와 PCL로만 준비된 웨이퍼에서의 알부민의 방출은 30일 동안 $10\%$ 미만의 느린 방출거동을 보였다. 그러나 첨가제를 함유한 웨이퍼는 첨가제 함량에 따라서 다양한 서방형의 방출거동을 보였다. 더욱이 콜라겐과 소장점막하조직과 같은 천연재료를 함유한 웨이퍼는 폴리비닐피롤리돈, 폴리에틸렌글리콜과 같은 합성재료를 함유한 웨이퍼보다 0차 방출의 거동을 보였다. 이러한 이식형 웨이퍼로부터 알부민의 방출은 천연재료의 첨가를 통해 쉽게 조절할 수 있음을 확인하였다.

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) (Response of the Application of Slow-release Potassium Fertilizer Using Natural Zeolite to Flue-cured Tobacco (Nicotiana tabacum L.))

  • 이동훈;박수준;최정
    • 한국토양비료학회지
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    • 제22권3호
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    • pp.215-220
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    • 1989
  • 천연(天然) zeolite를 이용한 완효성(緩效性) K비료(肥料)를 개발(開發)하기 위하여 K포화용액(飽和溶液)에 zeolite를 첨가(添加)하여 흡착반응(吸着反應)을 유도(誘導)하였다. 표면(表面)에 K가 포화(飽和)된 zeolite(K-Zeolite)와 과잉염(過剩鹽)이 남아있는 zeolite(NW. K-Zeolite)를 조제(調製)하였다. 흡착(吸着)된 K는 쉽게 용출(溶出)되지 않았으며 서서히 지속적(持續的)으로 용출(溶出)되었다. 또 이들 K-Zeolite와 NW. K-Zeolite를 연초재배(煙草栽培)에 시용(施用)한 결과(結果) 생육초기(生育初期)에는 KCl 처리(處理)에 비해 토양중(土壤中) K함량(含量)이 적었으나 생육후기(生育後期)에는 K함량(含量)이 오히려 높았다. 따라서 K-Zeolite는 완효성(緩效性) 가리비료(加里肥料)로 이용(利用)할 수 있음이 인정(認定)되었다.

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

  • 이경행;윤예지;이봄;봉소정;김현경;곽일환;김홍길
    • 한국식품영양학회지
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    • 제30권4호
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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.

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

  • 이경행;권혜원;윤예지;김홍길
    • 한국식품영양학회지
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    • 제32권4호
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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.

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

  • 김찬윤;안석균;서창국;강두희
    • The Korean Journal of Physiology
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    • 제23권2호
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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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Creeping bentgrass의 생육과 디봇피해 회복을 위한 질소의 유형별 효과 (Evaluating Various Nitrogen Sources for Divot Recovery on Creeping bentgrass)

  • 이상국
    • 아시안잔디학회지
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    • 제26권2호
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    • pp.135-139
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    • 2012
  • Creeping bentgrass 는 골프장의 티나 퍼팅그린 그리고 경기장과 같이 집중관리가 요구되는 곳에 가장 많이 사용되는 잔디의 종류중 하나이다. 골프장에서 계속해서 발생하는 디봇과 같은 피해는 골프장을 관리하는데 있어서 가장 큰 장애요인중 하나이다. 디봇피해를 회복하기 위한 많은 연구결가가 선행 되었음에도 불구하고, 질소의 유형에 따른 디봇피해의 회복에 대해서는 그 연구결과가 제한적이다. 본 연구는 creeping bentgrass 에 발생한 디봇 피해에 대한 질소의 유형별 효과에 대해 알아보기 위해서 수행되었다. 11가지 질소가 creeping bentgrass 'Penncross' 에 시비되었다. 첫번째 시비처리 이전에 일정한 단위규격당 디봇피해가 만들어 졌으며 피해가 생긴 빈자리에 원토양이 채워졌다. 실험기간동안 잔디의 색과 질이 평가되었다. 질소의 분해속도에 따른 효과는 디봇피해를 회복시키거나 creeping bentgrass 생육에 대해 영향을 미치지는 않았다. 총 4번에 걸쳐 시비한 urea 처리구는 질소가 시비되지 않은 대조구와 비교했을때 디봇의 회복이나 creeping bentgrass 생육에 대해 차이가 나타나지 않았다. 디봇피해에 대한 회복과 creeping bentgrass 생육에 대해 polyon 제품군, 특히 polyon mini (41-0-0)가 가장 좋은 효과를 보여 주었다. 본 실험결과 입자의 지름이 작은 완효성질소가 입자의 지름이 큰 완효성질소나 속효성질소 보다 creeping bentgrass 에 발생한 디봇피해의 회복에 좋은 효과를 나타냈다.

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

  • 여인서;박춘근;홍병주
    • 한국가축번식학회지
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    • 제16권4호
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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
    • 대한의용생체공학회:의공학회지
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    • 제28권4호
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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.

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

  • 정상옥;박기중;손성호
    • 한국농공학회논문집
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    • 제50권2호
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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.