• 제목/요약/키워드: Modified- release

검색결과 309건 처리시간 0.029초

파모티딘-양이온 교환수지 복합체의 약물방출 특성 및 흰쥐에서의 체내동태 (Drug Release Characteristics of Famotidine-Cationic Exchange Resin Complexes and Their Pharmacokinetics in Rats)

  • 신동선;송우헌;최영욱
    • Journal of Pharmaceutical Investigation
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    • 제27권4호
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    • pp.313-321
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    • 1997
  • Ion exchange resin complexes of famotidine have been prepared by the reaction of famotidine solution with activated ion exchange resins. Complex formation efficiency between famotidine and ion exchange resin was about $80{\sim}90%$ in average, calculated by HPLC determination. Drug release characteristics from the resin complexes were evaluated by the modified percolation method. Famotidine release was dependent on the type of ion exchange resins. In the case of weakly acidic resin complexes, the cumulative released amount of famotidine was more than 90% for 1hr in pH 1.2 buffer solution. However, in the case of strongly acidic resin complexes, it was less than 5% for 3hr in the same medium. Strongly acidic resins revealed some advantages over weakly, acidic resins for overcoming instability of famotidine in gastric juice. In addition, strongly acidic resin complexes showed controlled release of famotidine in pH 6.8 buffer solution, showing the result of about 60 to 70% of drug release for 5hr. After oral administrations of famotidine-resin complexes to rats as dose of 40 mg equivalent/kg, the pharmacokinetic parameters of famotidine were obtained by model independent analysis and compared with those of famotidine solution or suspension. $C_{max}$ of famotidine-resin complex was lower than that of famotidine solution or suspension. MRT, MAT, and MDT of the complexes were greater than those of famotidine solution or suspension. From these results, it was expected that famotidine was released slowly from the complexes and absorbed continuously into systemic circulation. It was recognized that drug release from the complexes was the rate-limiting step in drug absorption, since there were close correlations between in vitro drug release and in vivo pharmacokinetic parameters.

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Preparation and evaluation of ethylcellulose microcapsules of indomethacin

  • Lee, Haeng-Ja;Shim, Chang-Koo;Shim, Chang-Koo
    • Archives of Pharmacal Research
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    • 제7권1호
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    • pp.33-40
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    • 1984
  • In domethacin was microencapsulated with ethylcellulose using a modified spherical agglomeration process, aiming at a sustained release proparation without side effects on the stomach. The surface morphology of the microcapsules was examined using scanning electron microscopy. The microcapsules were porous and spherical, and their porosity increased with increasing the viscosity of ethylcellulose. In vitro dissolution process followed Higuchi's diffusion model for first 3 hr. Release rate of the drug from microcapsules decreased as the viscosity of ethylcellulose was decreased. The release rate also decreased with increasing the microcapsule size. The microcapsules induced less gastric ulcer in rats than raw drug.

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Nanocellulose Applications for Drug Delivery: A Review

  • Lee, Seung-Hwan;Kim, Hyun-Ji;Kim, Jin-Chul
    • Journal of Forest and Environmental Science
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    • 제35권3호
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    • pp.141-149
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    • 2019
  • Nanocellulose, which can exist as either cellulose nanocrystals or cellulose nanofibrils, has been used as a biomaterial for drug delivery owing to its non-immunogenicity, biocompatibility, high specific area, good mechanical properties, and variability for chemical modification. Various water-soluble drugs can be bound to and released from nanocelluloses through electrostatic interactions. The high specific surface area of nanocellulose allows for high specific drug loading. Additionally, a broad spectrum of drugs can bind to nanocellulose after facile chemical modifications of its surface. Controlled release can be achieved for various pharmaceuticals when the nanocellulose surface is chemically modified or physically formulated in an adequate manner. This review summarizes the potential applications of nanocelluloses in drug delivery according to published studies on drug delivery systems.

Biphasic Release Characteristics of Dual Drug-loaded Alginate Beads

  • Lee, Beom-Jin;Cui, Jing-Hao;Kim, Tae-Wan;Heo, Min-Young;Kim, Chong-Kook
    • Archives of Pharmacal Research
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    • 제21권6호
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    • pp.645-650
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    • 1998
  • The dual drug-loaded alginate beads simultaneously containing drug in inner and outer layers were prepared by dropping plain (single-layered) alginate beads into $CaCl_2$ solution. The release characteristics were evaluated in simulated gastric fluid for 2 h followed by intestinal fluids thereafter for 12 h. The surface morphology and cross section of dual drug-loaded alginate beads was also investigated using scanning electron microscope (SEM). The poorlv water-soluble ibuprofen was chosen as a model drug. The surface of single-layered and dual drug-loaded alginate beads showed very crude and roughness, showing aggregated particles, surface cracks and rough crystals. The thickness of dual drug-loaded alginate beads surrounded by outer layer was ranged from about 57 to 329mcm. The distinct chasm between inner and outer layers was also observed. In case of single-layered alginate bead, the drug was not released in gastric fluid but was largely released in intestinal fluid. However, the release rate decreased as the reinforcing $Eudragit^{\circledR}$ polymer contents increased. When the plasticizers were added into polymer, the release rate largely decreased. The release rate of dual drug-loaded alginate beads was stable in gastric fluid for 2 h but largely increased when switched in intestinal fluid. The drug linearly released for 4 h followed by another linear release thereafter, showing a distinct biphasic release characteristics. There was a difference in the release profiles between single-layered and dual drug-loaded alginate beads due to their structural shape. However, this biphasic release profiles were modified by varying formulation compositions of inner and outer layer of alginate beads. The release rate of dual drug-loaded alginate beads slightly decreased when the outer layer was reinforced with $Eudragit^{\circledR}$ RS1OO polymers. In case of dual drug-loaded alginate beads with polymer-reinforced outer layer only, the initial amount of druc released was low but the initial release rate (slope) was higher due to more swellable inner cores when compared to polymer-reinforced inner cores. The current dual drug-loaded alginate beads may be used to deliver the drugs in a time dependent manner.

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고온시에서의 폴리머 시멘트 모르타르의 연소특성에 관한 연구 (Burn-up Characteristics of Polymer-Modified Cement Mortar Used for Building Repair)

  • 김형준;노구치 타카후미
    • 한국건축시공학회:학술대회논문집
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    • 한국건축시공학회 2012년도 춘계 학술논문 발표대회
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    • pp.295-298
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    • 2012
  • Repair and strengthening is necessary to extend the service life of existing buildings. Polymer-modified cement mortar (PCM) has been extensively used as a high performance material particularly for finishing and repairing works in concrete building because of itsexcellent adhesion, waterproofing, resistance to chemical attack, and workability. As PCM contains organic polymer, it is necessary to clarify its properties at high temperature under fire, on which sufficient data are not available. This paper evaluated the burn-up characteristics of polymer-modified cement mortar with cone calorimeter test, non-combustibility test and flammability test with experimental parameters such as the types of polymer, unit-polymer content, polymer-cement ratio and thickness of the specimen.

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선택적 외측 슬개 지지대 이완술의 장점 (Advantage of Selective Release of Lateral Patellar Retinaculum)

  • 손정환;사공은성;권영호;장재호;김재도
    • 대한관절경학회지
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    • 제10권1호
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    • pp.61-69
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    • 2006
  • 목적: 슬개-대퇴간 부정 정렬 환자에서 외측 지지대를 이완시키는 수술에는 지금까지 관혈적 이완술(Open release), 고식적 관절경적 이완술(arthroscopic complete release)등의 방법을 이용하여 왔으나 저자는 관절경적 선택적인 이완술(arthroscopic selective release)로 이환된 지지대만을 최소 절제하여 수술함으로써 수술 후 환자의 합병증 및 만족도 등의 결과를 비교 분석하여 환자에게 가장 유용한 방식을 알아보고자 한다. 대상 및 방법: 1993년 1월부터 1998년 6월까지 외측 지지대 이완술을 시행하고 추시 가능하였던 94명, 129예 중 관절경적 이완술의 경우 68명, 90예, 관혈적 이완술의 경우 26명, 39예였으며 관절경적 이완술의 경우 고식적인 방식에 의한 경우가 42명, 57예였으며 이환된 외측지지대만을 선택적으로 이완시킨 경우가 26명, 33예였다. 위 예를 대상으로 수술 전 계측과 수술 후 1년, 수술 후 5년 이상의 최종 추시를 시행하여 슬개골 경사, 전위, 수렴 각, O-angle을 방사선학적 및 임상적으로 측정하여 분석하였으며, 임상적 평가는 슬관절 평가 지수 및 변형 슬개골 지수를 이용하였다. 결과: 방사선학적 평가에서 슬개골 경사와 전이는 고식적인 방법에 의한 관절경적 이완시$13.4^{\circ}$, 12.1 mm에서 $3.6^{\circ}$, 3.8 mm로, 관절경하 선택적 이완시 $12.3^{\circ}$, 11.2 mm에서 $4.8^{\circ}$, 5.2 mm로, 관혈적 이완시 $13.6^{\circ}$, 12.3mm에서 $3.3^{\circ}$, 3.4 mm로 향상된 결과를 보였으나, 통계적으로는 유의한 상관관계를 보이지 않았다. 슬관절 평가 지수는 각각 84.2%(48/57), 81.8%(27/33), 82.1%(32/39)에서, 변형 슬개골 지수는 82.5%(47/57), 81.8%(27/33), 82.1%(32/39)에서 만족스러운 결과를 보였고 서로 간에 유의한 차이는 보이지 않았다. 결론: 슬개-대퇴 부정 정렬을 가진 환자의 수술방법 중 하나인 관절경적 선택적 이완술은 적은 수술범위에서 이환된 지지대를 이완시킴으로써 유착등의 합병증 없이 환자의 재활 및 만족도를 높이는 하나의 치료 방법으로서 관혈적 방법과 고식적 관절경적 수술보다 좋은 치료라고 판단된다.

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Allergenicity Test of Genetically Modified Soybean in Sprague Dawley Rats

  • Chang, Hyun-Sung;Bae, Youn-Kyoung;Lim, Si-Kyu;Jeong, Tae-Cheon;Kim, Hyung-Soo;Chung, Seung-Tae;Kim, Dong-Sup;Nam, Doo-Hyun
    • Archives of Pharmacal Research
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    • 제24권3호
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    • pp.256-261
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    • 2001
  • Allergenicity of genetically-modified (GM) soybean was evaluated in male Sprague Dawley rats. To confirm the GM soybean used in this study, the polymerase chain reaction (PCR) was performed using the chromosomal DNA of soybeans. The PCR result provided the clear discrimination of genetically-modified (GM) soybeans. To evaluate the allergenicity of GM soybean and non-GM control one, the soybean homogenate was sensitized subcutaneously 3 times a week for 3 weeks. The doses of soybean were 0, 2 and 20 mg/kg in the protein basis. A week after the last sensitization, antisera were recovered from individual animals. When the sera were injected intradermally on the clipped back of unsensitized rats with various dilutions, followed by a challenge with 20 mg/kg of soybean homogenate containing 1% Evans blue, no sign of passive cutaneous anaphylaxis reaction was detected. In addition, when the sera were treated in the cultures of peritoneal mast cells, the increase of histamine release by anti-(GM soybean) sera was not observed when compared to that by anti-(non-GM soybean) sera. The present results indicate that the GM soybean might not act as a strong allergen in male Sprague Dawley rats.

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수용성 염산슈도에페드린과 난용성 테르페나딘의 구형정석조립법과 액중미립구법을 이용한 서방성펠렛 복합제제의 개발 (Development of Multiparticulate-system Composed of Sustained Release-microspheres of Pseudoephedrin${\cdot}$HCI and Immediate Release-pellets of Terfenadine Using Solvent Evaporation Method and Spherically Agglomerated Crystallization Process)

  • 이계주;도기찬;김은희;박종범;황성주
    • 약학회지
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    • 제41권3호
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    • pp.305-311
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    • 1997
  • Sustained release-microspheres and immediate release-pellets were prepared to develop a controlled release multiparticulate system containing both water soluble and insoluble dr ug. Pseudoephedrin.HCl (EPD) and terfenadine (TRF) were used as model drugs, respectively. Sustained release-EPD microspheres were prepared by solvent evaporation method using Eudragit RL or RS as a matrix combined with pH-insensitive film coating. Smaller EPD microspheres were obtained when smaller amount of Eudragit as a matrix material or larger amount of magnesium stearate as a dispersing agent was used. However the obtained microspheres did not show syfficient sustained release characteristics. About 97% of EPD was released after 1 hr irrespective of matrix material used. Subsequent coating of the microspheres with pH-insensitive polymer such as Eudragit RS or ethylcelulose (EC) resulted good sustained in 37.5, 73.3 and 92.0% release of encapsulated EPD in distilled water after 1, 3 abd 7 hr, respectively. It corresponds to mean dissolution time (MDT) of 2.3 hr, which is much larger than that of un-coated EPD microspheres (0.0048 hr). Immediate release TRF pellets were prepared by spherically agglomerated crystallization using Eudragit E as an inert matrix and methylene chloride as a liquid binder. Using Eudragit E alone as a matrix resulted in satisfactory physical properties of the pellets such as sphericity, surface texture and flowability, but led to slower release of TRF from pellets than un-modified TRF powder (MDT of 1.70 vs 1.43 hr in pH 1.2 dissolution medium). Introducing propylene glycol or sodium lauryl sulfate as an emulsifier brought about faster release of TRF from pellets (MDT of 1.14 and 0.95 hr, respectively). In conclusion, microencapsulation by solvent evaporation combined with film coating and spherically agglomerated crystallization were successfully utilized to prepare controlled release multiparticulate system composed of sustained release EPD-microspheres and immediate release TRF pellets.

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플루란 아세테이트 미립구를 이용한 단백질 전달 시스템 개발 (Development of Protein Delivery System using Pullulan Acetate Microspheres (PAM))

  • 나건;최후균
    • Journal of Pharmaceutical Investigation
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    • 제36권2호
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    • pp.115-121
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    • 2006
  • The aim of this study was to develop new protein/peptide depot system instead of poly(DL-lactic acid-coglycolic acid) (PLGA) microspheres. Pullulan was chemically modified by the addition of acetic anhydride (pullulan acetate; PA) and then investigated as new depot system for protein/peptide delivery. PA microspheres (PAM) with lysozyme as a model protein were prepared by w/o/w double emulsion method. The microspheres had a mean size of 10-50 mm with a spherical shape. The size distributions reduced with increasing the degree of acetylation. The loading efficiency of lysozyme was also increased. Lysozyme aggregation behavior in the microsphere was monitored to estimate the change of protein stability during preparation step. The ratios of protein aggregation in PAMs are lower than that of PLGA microsphere, in particular, PA 5 showed lowest as about 16%. The result indicated that the increase of acetylation suppressed the aggregation of protein. The release profiles of lysozyme from PAMs were significantly different. High acetylation effectively improved lysozyme release kinetics by reducing initial burst release and extending continuous release over a period of time. To check the effect of preservation for structural stability of lysozyme, the activity of lysozyme released from PA 5 was also observed. The activity of lysozyme was maintained almost 100% for 25 day. Therefore, PAM may become to a useful carrier for delivery of protein/peptide drugs, if it will be supported by biocompatibility and biodegradability results.

Capsaicin이 연수후각의 흥분성 아미노산 전달물질에 미치는 영향 (Effect of Capsaicin on the Excitatory Amino Acids Neurotranmitters in Medullary Dorsal Horn)

  • 권수경;윤수한;이종흔
    • Restorative Dentistry and Endodontics
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    • 제19권2호
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    • pp.621-632
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    • 1994
  • This experiment was performed to study the effect of capsaicin on the excitatory amino acids (EAAs) neurotransmitter in medullary dorsal horn and to clarify the relationship between substance P and excitatory amino acids. Horizontal slice of rat medullary dorsal horn was prepared and perfused with modified Krebs-Ringer solution in brain slice chamber. Release of EAAs was induced by veratrine and capsaicin were added to perfusion solution to observe the changes in EAA release. Capsaicin and ruthenium red, capsaicin antagonist, were also systemically injected with 50mg/kg in first day and 100mg/kg in second day for 2 days. Medulla oblongata containing the medullary dorsal horn was isolated, homogenized and centrifused. Spernatant was freeze-dried and EAA was determined by HPLC. Release of glutamate and aspartate was significantly increased by veratrine or capsaicin, but veratrine evoked release of EAAs was blocked by capsaicin in vitro, and injected ruthenium red did not have effect on the contents of EMs in vivo. Systemically injected capsaicin evoked the slight decrease in content of glutamate and aspartate in medullary dorsal horn and this effect of capsaicin was unaffected by ruthenium red.

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