• 제목/요약/키워드: rate of release

검색결과 2,219건 처리시간 0.027초

Effect of Manufacturing Method and Acidifier on the Dissolution Rate of Carvedilol from Solid Dispersion Formulations

  • Lim, Dong-Kyun;Bae, Jeong-Woo;Song, Byung-Joo;Jo, Han-Su;Kim, Hyoung-Eun;Lee, Dong-Won;Khang, Gil-Son
    • Journal of Pharmaceutical Investigation
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    • 제41권6호
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    • pp.363-369
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    • 2011
  • In this study, we demonstrated the release behavior of carvedilol with the content of polyvinylpyrrolidone K-30 (PVP K-30) and the effect of citric acid and fumaric acid as acidifiers on the release behavior of drug. In addition, it tries to inquire into the release behavior difference of the carvedilol according to the manufacturing method. The release behavior of the tablets was compared with Dilatrand$^{(R)}$ in the simulated gastric fluid (pH1.2). Differential scanning calorimeter (DSC), X-ray diffraction (XRD) and Fourier-transform infrared spectroscopy (FT-IR) were characterized for the physicochemical properties of the tablets. In case of mixing the carvedilol and PVP K-30, in case the ratio of the carvedilol and PVP K-30 was 1:5, the release behavior was the highest among. As well as the dissolution rate of tablets manufactured by lyophilization and rotary evaporator was higher than physical mixture. The dissolution rate of containing acidifiers was more improved. But, rather the excessive amount of the acidifier addition reduced the dissolution rate.

Propranolol이 심근 sarcoplasmic reticulum 및 mitochondria 의 $Ca^{++}$ 조절작용에 미치는 효과에 관한 연구 (Effect of Propranolol on the $Ca^{++}$-regulation of Cardiac Sarcoplasmic Reticulum and Mitochondria)

  • 최수승
    • Journal of Chest Surgery
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    • 제19권2호
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    • pp.197-208
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    • 1986
  • Propranolol is one of clinically useful antiarrhythmic agents and electrophysiologically classified as group II. And the negative inotropic effect which is not related to adrenolytic effect has been demonstrated with high concentration of propranolol. On the other hand, it has been well known that the calcium plays a central role in excitation-contraction coupling process of myocardium and also in electrophysiological changes of cell membrane. Author studies the effect of propranolol on calcium uptake and release in sarcoplasmic reticulum and mitochondria prepared from porcine myocardium to investigate the mechanism of action of propranolol on myocardium. The results are summarized as follow: 1] The maximum Ca++-uptake of sarcoplasmic reticulum is inhibited by propranolol in a dose dependent manner. 2] The release of calcium from sarcoplasmic reticulum is not affected by propranolol but with higher than 1x10-3 M of propranolol, rate of calcium release from sarcoplasmic reticulum is decreased. 3] Propranolol inhibits the maximum uptake and uptake rate of calcium in mitochondria non-competitively. [Ki = 6.21 x 10-4 M] 4] The rate of Na+ induced calcium release from mitochondrion shows a function of [Na+]2 and is inhibited by propranolol with the concentration significantly lower than that affect the calcium uptake in sarcoplasmic reticulum and in mitochondria [Ki = 2.91 x 10-5 M]. These results suggest that propranolol affects the intracellular calcium homeostasis which may considered to be one of the mechanism of action of propranolol on myocardium.

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멜록시캄 함유 poly (D,L-lactic acid) 미소립자의 제조 및 평가 (Preparation and Evaluation of Meloxicam-loaded Poly(D,L-lactic acid) Microspheres)

  • 임종섭;오동훈;이동훈;성정훈;유봉규;김정애;우종수;이용복;김세미;최한곤;용철순
    • Journal of Pharmaceutical Investigation
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    • 제38권1호
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    • pp.63-72
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    • 2008
  • Meloxicam-loaded microspheres were prepared with poly(D,L-lactic acid)(PLA) by a solvent-emulsion evaporation method. The morphology, particle size, drug loading capacity, drug entrapment efficiency (EE) and release patterns of drug were investigated in vitro. Various batches of micro spheres with different size and drug content were obtained by changing the ratio of meloxicam to $PLA^{\circ}{\AE}s$ with different molecular weight, PLA concentration in the dispersed phase and stirring rate. Meloxicam crystals on microsphere surface, which were released rapidly and could act as a loading dose, were observed with increasing drug content. The release rate was increased with increase in drug contents and decrease in the molecular weight of PLA. Microspheres prepared with smaller molecular weight produced faster drug release rate. The release rate of meloxicam for long-acting injectable delivery system in vitro, which would aid in predicting in vivo release profile, could be controlled by properly optimizing various factors affecting characteristics of microspheres. Blood concentration-time profile of meloxicam after intramuscular injection of meloxicam-loaded microspheres in rabbits showed possibility of long term application of this system in clinical settings.

Controlled Transdermal Delivery of Loxoprofen from an Ethylene-Vinyl Acetate Matrix

  • Ryu, Sang-Rok;Shin, Sang-Chul
    • Journal of Pharmaceutical Investigation
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    • 제41권6호
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    • pp.347-354
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    • 2011
  • Repeated oral administration of loxoprofen can induce many side effects such as gastric disturbances and acidosis. Therefore, we considered alternative routes of administration for loxoprofen to avoid such adverse effects. The aim of this study was to develop an ethylene-vinyl acetate (EVA) matrix system containing a permeation enhancer for enhanced transdermal delivery of loxoprofen. The EVA matrix containing loxoprofen was fabricated and the effects of drug concentration, temperature, enhancer and plasticizer on drug release were studied from the loxoprofen-EVA matrix. The solubility of loxoprofen was highest at 40% (v/v) PEG 400. The release rate of drug from drug-EVA matrix increased with increased loading dose and temperature. The release rate was proportional to the square root of loading dose. The activation energy (Ea), which was measured from the slope of log P versus 1000/T, was 5.67 kcal/mol for a 2.0% loaded drug dose from the EVA matrix. Among the plasticizer used, diethyl phthalate showed the highest release rate of loxoprofen. Among the enhancers used, polyoxyethylene 2-oleyl ether showed the greatest enhancing effect. In conclusion, for the enhanced controlled transdermal delivery of loxoprofen, the application of the EVA matrix containing plasticizer and penetration enhancer could be useful in the development of a controlled drug delivery system.

로라제팜을 함유한 poly(D,L-lactic acid) 마이크로스피어 개발 (Development of Poly(D,L-lactic acid) Microspheres Containing Lorazepam)

  • 최한곤;유봉규;이종달;김정애;권태협;우종수;용철순
    • Journal of Pharmaceutical Investigation
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    • 제36권3호
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    • pp.175-184
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    • 2006
  • Poly(D,L-lacic acid)(PLA) microshperes containing loazepam were prepared by a solvent-emulsion evaporation method and their release patterns were investigated in vitro. Various batches of microspheres with different size and drug content were obtained by changing the ratio of lorazepam to PLA, PLA concentration in the dispersed phase and stirring rate. Rod-like lorazepam crystals on microsphere surface, which were released rapidly and could act as a loading dose, were observed with increasing drug content. The release rate was increased with increase in drug contents and decrease in the molecular weight of PLA. The release rate of lorazepam for long-acting injectable delivery system in vitro, which would aid in Predicting in vivo release Profile, could be controlled by properly optimizing various factors affecting characteristics of microspheres.

EFFECT OF ADDITIVE ON THE HEAT RELEASE RATE AND EMISSIONS OF HCCI COMBUSTION ENGINES FUELED WITH RON90 FUELS

  • Lu, X.C.;Ji, L.B.;Chen, W.;Huang, Z.
    • International Journal of Automotive Technology
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    • 제8권1호
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    • pp.1-7
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    • 2007
  • The effect of the di-tertiary butyl peroxide (DTBP) additive on the heat release rate and emissions of a homogeneous charge compression ignition (HCCI) engine fueled with high Research Octane Number (RON) fuels were investigated. The experiments were performed using 0%, 1%, 2%, 3%, and 4% (by volume) DTBP-RON90 blends. The RON90 Fuel was obtained by blending 90% iso-octane with 10% n-heptane. The experimental results show that the operation range was remarkably expanded to lower temperature and lower engine load with the DTBP additive in RON90 fuel. The first ignition phase of HCCI combustion was observed at 850 K and ended at 950 K while the hot ignition occurred at 1125 K for all fuels at different engine working conditions. The chemical reaction scale time decreases with the DTBP addition. As a result, the ignition timing advances, the combustion duration shortens, and heat release rates were increased at overall engine loads. Meanwhile, the unburned hydrocarbon (UHC) and CO emissions decrease sharply with the DTBP addition while the NOx emissions maintain at a lower level.

골 재흡수 치료를 위한 파미드로네이트를 함유한 이식형 생분해성 PLGA 웨이퍼의 제조와 특성결정 (Preparation and Characterization of Pamidronate-loaded PLGA Wafer for the Treatment of Bone Resorption)

  • 유제영;김상욱;강길선;성하수;정제교
    • 폴리머
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    • 제26권5호
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    • pp.680-690
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    • 2002
  • 골 재흡수 치료를 목적으로 파미드로네이트를 지속적으로 방출하는 제형으로 제조하기 위하여 락타이드-글리콜라이드 공중합체 (PLGA, 락타이드 : 글리콜라이드 몰비 = 75 : 25, 분자량 20000 g/mole 및 90000 g/mole)를 이용하여 직접압축 성형방법으로 생분해성 웨이퍼를 제조하였다. 약물과 고분자의 함량비 웨이퍼의 두께, PLGA 분자량 등을 조절하여 PLGA 웨이퍼를 제조하였고 이들의 형태학적 특성과 방출거동 및 분해거동을 살펴보았다. 웨이퍼의 제조는 혼합된 분말을 웨이퍼 제작용 몰드에 넣은 후 프레스를 이용하여 일정 압력으로 일정시간 동안 상온에서 가압하여 제조하였다. 제조된 웨이퍼는 약물의 초기함량이 증가할수록 방출속도가 빠르게 나타났으며, 제형의 두께가 두꺼워질수록 시간이 경과함에 따라 약물의 방출속도가 증가하였다. 또한 고분자의 분자량이 큰 것이 작은 것에 비해 상대적으로 초기 약물 방출량이 적고 방출되는 속도 또한 느려져. 저분자보다 오랫동안 약물이 방출되었다. 이러한 약물전달 시스템은 압축성형방법에 의해 제조하므로 제조가 간단하고 약물방출속도를 정확하게 제어할 수 있으므로 이식을 위한 제형으로 제조시 유용하게 쓰일 것으로 예상되었다.

연속회분식반응조에서 유기물 부하와 질산염농도에 따른 생물학적 질소 및 인 제거 특성 (Biological Nitrogen and Phosphorus Removal Characteristics on Organic Material and Nitrate Loadings in SBR Process)

  • 김이태;이희자;김광수;배우근
    • 한국물환경학회지
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    • 제20권6호
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    • pp.571-576
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    • 2004
  • Since anaerobic/anoxic/oxic process, which is a typical mainstream biological nitrogen and phosphorus removal process, utilizes influent organic matter as an external carbon source for phosphorus release in anaerobic or anoxic stage, influent COD/T-P ratio gives a strong influence on performance of phosphorus removal process. In this study, a bench scale experiment was carried out for SBR process to investigate nitrogen and phosphorus removal at various influent COD/T-P ratio and nitrate loadings of 23~73 and 1.6~14.3g $NO_3{^-}-N/kg$ MLSS, respectively. The phosphorus release and excess uptake in anoxic condition were very active at influent COD/T-P ratios of 44 and 73. However, its release and uptake was not obviously observed at COD/T-P ratio of 23. Consequently, phosphorus removal efficiency was decreased. In addition, the phosphorus release and uptake rate in anoxic condition increased as the nitrate loading decreased. Specific denitrification rate had significantly high correlation with organic materials and nitrate loadings of the anoxic phase too. The rate of phosphorus release and uptake in the anoxic condition were $0.08{\sim}0.94kg\;S-P/kg\;MLSS{\cdot}d$ and $0.012{\sim}0.1kg\;S-P/kg\;MLSS{\cdot}d$, respectively.

대심도터널 화재 안전 설계를 위한 승용차의 열방출률 및 화재전파 특성에 관한 연구 (A study of the HRR and fire propagation phenomena for the fire safety design of deep road tunnel)

  • 유용호;권오상
    • 한국터널지하공간학회 논문집
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    • 제12권4호
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    • pp.321-328
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    • 2010
  • 본 연구에서는 최근 국내 도심지 대심도 지하교통터널 계획과 함께 중요성이 대두되고 있는 터널내 화재 안전 설계에 가장 기본적인 설계 요소인 자동차의 열방출률을 제시하고자 실물화재실험을 실시하였다. 산소소모율법을 적용한 라지스케일칼로리미터를 이용하여 승합차의 열방출률을 측정하였으며, 또한 두 대의 승용차를 인접시켜 터널 정체시 화재 전파 특성을 파악 하였다. 그 결과 승합차의 최대 열방출률은 5.9 MW를 나타내었으며, 일산화탄소는 최대 482 ppm이 방출되었다. 두 대의 승용차의 화재 전파 특성 실험의 경우 화재 발생 후 약 3분 30초 경과부터 인접 승용차에 화재 전파가 시작되어, 15분 경과 후에는 완전한 화재로 발달하였다. 최대 발열량은 9 MW를 나타내었다. 이러한 실물화재실험에서 얻어낸 결과는 향후 수치해석시 중요한 입력 자료로 이용됨과 동시에 터널의 방재설비 설계에 유용하게 적용 될 수 있을 것이다.

디젤기관에서의 어유의 연소특성과 기관성능에 관한 연구 (A Study on the Engine Performance and Combustion Characteristics of Fish Oil in a Diesel Engine)

  • 서정주;왕우경;안수길
    • 한국자동차공학회논문집
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    • 제2권3호
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    • pp.85-93
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    • 1994
  • The engine performance and combustion characteristics of diesel oil and fish oil blended with diesel oils were investigated at various blending rate of fish oil in a diesel engine. The maximum pressure showed no significant difference among test fuels at low load, but it was higher as the blending rate of fish oil increases at high load. Increasing the blending rate of fish oil, the rate of heat release and burned fraction were higher than those of diesel oil. The ignition delay became longer than that of diesel oil as the blending rate of fish oil increases, and its differences were larger at different loads. The combustion duration and density of smoke were shorter and lower as the blending rate of fish oil increases. The rate of fuel consumption showed no significant difference between diesel oil and fish blended with diesel oils.

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