용매증발법에 의한 부피바카인 microsphere의 제조 및 평가

곽손혁(Son Hyok Kwak),황성주(Sung Joo Hwang),이병철(Byung Chul Lee) 대한약학회 2000 약학회지 Vol.44 No.6

Various bupivacaine-loaded microspheres were prepared from poly (d,l-lactide) (PLA) or poly (d,l-lactic-co-glycolide) (PLGA) by a solvent evaporation method for the sustained release of drug. PLA and PLGA microspheres were prepared by w/o/w and w/o/o multiple emulsion solvent evaporation, respectively. The effects of process conditions such as emulsification speed, emulsifier type, emulsifier concentration and internal/external phase ratio on the characteristics of microspheres were investigated. The prepared microspheres were characterized for their drug loading, size distribution, surface morphology and release kinetics. Drug loading efficiency was higher in the microspheres prepared by w/o/o multiple emulsion than that by w/o/w multiple emulsion mehtod, because the solubility of bupivacaine HCl was decreased in oil phase compared with water phase. The prepared microspheres had an average diameter between 1 and 2mcm in all conditions of two methods. In morphology studies the PLA microspheres showed an irregular shape and smooth surface, but PLGA microspheres had a spherical shape and smooth surface. The release pattern of the drug from microspheres was evaluated on the basis of the burst effect and the extent of the release after 24h. The in vitro release of bupivacaine HCl from microspheres showed a large initial burst release and 60-80% release within one day in all conditions of two methods. The extents of the burst release against PLA and PLGA microspheres were 30-50% and 50-80% within 20min, respectively. This burst release seems to be due to the smaller size of microspheres and the solubility of drug in water.

Release behavior of biodegradable microcapsules containing geranium oil by solvent evaporation method

이민우,김영진,박관우 한국공업화학회 2015 한국공업화학회 연구논문 초록집 Vol.2015 No.1

In this work, the biodegradable poly(ε-caprolactone)(PCL) microcapsules containing geranium oil were prepared by solvent evaporation method. Physicochemical properties and release behaviors of microcapsules were tested with various manufacturing conditions. Fragrant oil, from Geranium, was used as a core substance. Two polymers were used polycaprolactone(PCL) as a capsule wall material and poly(vinyl alcohol) (PVA) as a stabilizer. The microcapsules were investigated to verify the effects of the stirring rate, concentration of stabilizer and molecular weight of PCL. The size and shape of the microcapsules were observed by scanning electron microscope(SEM). Also, the release behaviors of fragrant oil from microcapsule were characterized by UV/vis. spectrophotometer.

분무건조 방법의 차이가 글리메피라이드 함유 고체분산체의 특성에 미치는 영향

양현석(Hyun Seok Yang),오유림(Yu Rim Oh),김동욱(Dong Wuk Kim) 대한약학회 2021 약학회지 Vol.65 No.6

Glimepiride (GLI) is a third-generation sulfonylurea class antidiabetic drug that has low aqueous solubility. The objective of this study was to evaluate the effect of solvents in the development of GLI-loaded solid dispersions (GLISD) using spray drying technique. Two GLI-SD were prepared by adding GLI, polyvinylpyrrolidone (PVP K30), and sodium lauryl sulfate (SLS) in an ethanol/water mixture (solvent evaporation, SE) and water only (surface attached, SA). Intrinsic saturated solubilities and in-vitro dissolution were evaluated and compared to the GLI powder and physical mixture (PM). In addition, physicochemical studies such as scanning electron microscopy, differential scanning calorimetry, and X-ray diffraction were also evaluated. We found that the solubility of GLI was significantly improved by both the preparation methods. The SE method showed 4,960-fold improvement while the SA method displayed 2,900-fold enhancement, which is equivalent to the PM. The in-vitro dissolution studies showed that both methods had a higher release rate, about 1.3-fold for SE and 2-fold for SA, as compared to pure GLI powder. However, GLI release slightly decreased with time for the SA method. Furthermore, solid-state characterizations also revealed that most of the crystalline drug was transformed to the amorphous form in both GLI-SD. Thus, these results indicate that choice of the solvent system plays an important role in the spray drying technique which affects the solubility, dissolution, and crystallinity of poorly soluble drugs such as GLI.

Enhancement of stability and controlled drug release of lipid nanoparticles by modified solvent-evaporation method

Lee, S.E.,Lee, J.K.,Jang, W.S.,Kim, T.H.,Tunsirikongkon, A.,Choi, J.S.,Park, J.S. Elsevier 2016 Colloids and surfaces. A, Physicochemical and engi Vol.508 No.-

<P>The purpose of this study was to improve the physicochemical properties of solid lipid nanoparticles (SLNs) by modified solvent-evaporation methods. Stearylamine, Tween 80, egg phosphatidylcholine, and docetaxel were used to prepare SLNs. In the conventional method, the lipid is heated to 5-10 degrees C above its melting point; however, the samples prepared using the modified method were heated to twice the lipid melting point. The particle size, polydispersity index (PdI), and zeta potentials were measured to compare the physicochemical characteristics of SLNs prepared using the conventional and modified methods. The morphologies of the SLNs were observed using scanning electron microscopy (SEM) and the crystal forms confirmed using DSC thermograms. The aqueous stability of the SLNs was evaluated by examining changes in mean particle size and polydispersity during storage at 4 degrees C. An in vitro drug release test was conducted to study the release patterns of each SLN formulation. mSLN particles were smaller and more uniform than those of cSLNs in dynamic light-scattering (DLS) and SEM measurements. The particle size and Pdl were 321 +/- 15.5 nm, 0.208 +/- 0.0208 for mSLNs and 403.2 +/- 24.7 nm, 0.486 +/- 0.0138 for cSLNs, respectively. The zeta potentials of mSLNs and cSLNs were +26.2 +/- 2.01 and +24.1 +/- 0.83, respectively. Docetaxel was incorporated in both SLNs with about 80% encapsulation efficiency. Mean particle diameters and PdI of mSLNs were maintained throughout the observation period. However, in cSLNs, extensive particle growth and gelation were observed when the cSLNs were stored at 4 degrees C. The in vitro drug release test showed that mSLNs had a more sustained release pattern. In conclusion, the stability and controlled drug release of SLNs can be enhanced by fabrication using modified solvent-evaporation methods. (C) 2016 Elsevier B.V. All rights reserved.</P>

방출제어를 위한 잘토프로펜이 함유된 폴리옥살레이트 미립구의 제조와 특성

김경희(Kyoung Hee Kim),이천중(Cheon Jung Lee),조선아(Sun A Jo),이정환(Jung Hwan Lee),장지은(Ji Eun Jang),이동원(Dong Won Lee),권순용(Soon Yong Kwon),정진화(Jin Wha Chung),강길선(Gil Son Khang) 한국고분자학회 2013 폴리머 Vol.37 No.6

서방성방출을 위해 잘토프로펜을 함유한 미립구를 oil-in-water(O/W) 에멀젼용매 증발법을 이용하여 제조하였다. 제조온도, 교반속도, 초음파분쇄기의 강도, 약물농도, POX의 분자량과 농도, 유화제 농도 등의 제조조건에 따른잘토프로펜의 방출거동을 평가하였다. 잘토프로펜을 함유한 POX 미립구의 물리화학적 성질 및 형태를 X선 회절분석법(XRD)과 시차주사열량계(DSC), 적외선 분광분석기(FTIR), 주사현미경(SEM)을 통해 연구하였다. 이러한 연구결과로부터 제조조건들에 따른 미립구의 특성을 확인할 수 있었다. 또한 POX 미립구의 분해성을 10일 동안 in vitro 실험을 통해 조사하였다. 본 연구를 통해 잘토프로펜을 함유한 POX 미립구를 최적화된 용매증발방법으로 제조하였고, 이 미립구로부터 약물의 방출제어를 확인할 수 있었다. Zaltoprofen loaded polyoxalate (POX) microspheres were prepared by an emulsion solvent-evaporation/extraction method like oil-in-water (O/W) for sustained release of zaltoprofen. The influence of several preparation parameters such as fabrication temperature, stirring speed, intensity of the sonication, initial drug ratio, molecular weight (Mw) of POX, concentration of POX and concentration of emulsifier has been investigated on the zaltoprofen release profiles. Physicochemical properties and morphology of zaltoprofen loaded POX microspheres were investigated by scanning electron microscopy (SEM), X-ray diffraction (XRD), differential scanning calorimeter (DSC) and Fourier transform infrared (FTIR). Through the analyzed results, it was demonstrated that the characteristics of the microspheres greatly affected by the prepared condition. The releases behavior of zaltoprofen was investigated for 10 days in vitro. It was confirmed that the release behavior of zaltoprofen can be controlled by the manufacturing factor of solvent-evaporation/extraction method.

레몬그라스 오일을 함유하는 PCL마이크로캡슐의 특성과 방출거동

박종권 ( Jong Kwon Park ),김지은 ( Ji Eun Kim ),정노희 ( Noh Hee Jeong ) 한국공업화학회 2015 공업화학 Vol.26 No.3

In this study, poly ε-caprolactone(PCL) microcapsules containing lemongrass oil was prepared by the solvent evaporation method. Effects of concentrations of PCL and poly vinyl alcohol (PVA) as well as stirring speeds when preparing microcapsuleswere investigated. Specific peaks of lemongrass oil in PCL microcapsules at 1600 and 2900 cm-1 were observed by FT-IR. The particle size and shape of microcapsules were also measured by polarizing microscope and optical microscopy. The average particle size of microcapsules decreased with increasing the stirring rate. At the stirring speed of 1500 rpm, and 1 wt% of each PCL and PVA concentrations, the smallest particles were formed. Collection efficiencies of lemongrass oil of 77.5% and 69.5% were obtained when 1.5 wt% of PCL and 2 wt% of PVA were used, respectively. In addition, the release behavior and antioxidant activity of lemongrass oil from PCL microcapsules were examined using UV-Vis spectrophotometry. When 0.5 wt% PCL and 2.0 wt% PVA were used with the slow stirring rate, microcapsules showed a fast release rate. The characteristics of antioxidant activity exhibited similar to that of the release behavior.

용매 증발법을 이용한 열가소성 폴리우레탄의 마이크로 캡슐화

박찬수(Chan-Su Park),이지원(Ji-Won Lee),조남주(Nam-Ju Jo) 한국고분자학회 2019 폴리머 Vol.43 No.1

고무 제조의 초기 공정인 혼련 공정에서 발생하는 열로 인한 고무의 바람직하지 않은 사전 가교를 방지하고 분산성을 높이기 위해 가황제와 가황 촉진제를 마이크로 캡슐화한다. 이후 마이크로 캡슐은 고무 제조의 후 공정인 성형 공정에서 용해되어 가황제와 가황 촉진제를 방출하게 한다. 이에 마이크로 캡슐화는 궁극적으로 고무 제품의 제조 공정의 용이성과 경제성을 개선할 수 있다. 마이크로 캡슐의 재료로는 하드 세그먼트와 소프트 세그먼트의 함량을 조절하여 원하는 융점과 기계적 강도를 얻을 수 있는 열가소성 폴리우레탄을 선택하고 용매 증발법으로 마이크로 캡슐을 제조하였다. 또 제조한 마이크로 캡슐의 열적 성질과 기계적 성질을 조사하여 혼련 공정에서 발생하는 120 ℃의 열과 13 MPa의 인장 응력을 견디고 가황온도인 150 ℃에서 녹는 시료를 선정하였으며, 실제 공정에의 적용가능성을 검토하였다. It is essential to encapsulate vulcanizing agent and vulcanizing acceleration agent to enhance their dispersion and block the undesirable crosslinking by the heat generated during the kneading process in rubber manufacture. And the microcapsules are melted at the vulcanization temperature and controlled to release the vulcanizing agent and the vulcanization accelerator. Then the microencapsulation would ultimately promote the formability and ease of the manufacturing process of rubber product. As a wall material, thermoplastic polyurethane (TPU), where the content of the hard segment and the soft segment can be controlled to obtain the desired melting point and mechanical strength, was used, and microcapsule was made by solvent evaporation method. Also TPUs which were durable to the temperature of 120 ℃ and the tensile stress of 13MPa and melt at the vulcanization temperature of 150 ℃ were achieved, and then the application to the rubber manufacture process was discussed.

삼원계를 통한 페북소스타트 고체분산체 개발 및 평가

정하늘(Ha Neul Jung),최진석(Jin-Seok Choi) 대한약학회 2024 약학회지 Vol.68 No.2

Febuxostat is classified as a biopharmaceutical with low solubility in aqueous solution and high intestinal permeability (Biopharmaceutics Classification System [BCS] Class II drug). The solubility of a drug has the characteristic of increasing as pH increases. This study aims to improve the dissolution of febuxostat with Neusilin® US2 and Gelucire®50/13 by a solvent evaporation method. The optimal formulation (solid dispersion, SD1) is developed as a solid dispersion of febuxostat : Gelucire®50/13 : US2®= 1:2:4 (w/w), with a final weight of 280 mg. The dissolution of SD1 in distilled water is 72.0±2.8%, which is 1.67-fold higher than that of the commercial product, Feburic Tab® (43.2±1.8%). The SD1 formulation is believed to have improved dissolution due to changes in physicochemical properties (thermal, interaction, and crystallinity). In conclusion, through the solid dispersion manufacturing method, febuxostat is changed from a crystalline form to an amorphous form in SD1 formulation, and the improved dissolution of febuxostat formulation is developed.

Release behavior and characterization of PCL microcapsule containing lemongrass oil

김지은,정노희 한국공업화학회 2014 한국공업화학회 연구논문 초록집 Vol.2014 No.1

In this study, it was prepared PCL microcapsules consisted of lemongrass oil as core material by solvent evaporation method. The effects of concentration of core material, shell material, emulsifier and stirring rates on the preparing of the microcapsules were investigated. It was confirmed that lemongras oil has been encapsulated into PCL microcapsules by FT-IR. The size and form of the microcapsules was observed by SEM. The average particle size of microcapsules was confirmed by PSA. Entrapment efficiency and release behavior of the microcapsules was observed by UV-Vis absorbance.

용매증발법을 이용한 Poly-L-Lactic Acid (PLLA) 마이크로스피어 제조

김태형,송기창,Kim, Tae Hyoung,Song, Ki Chang 한국화학공학회 2018 Korean Chemical Engineering Research(HWAHAK KONGHA Vol.56 No.4

Poly-L-lactic acid (PLLA)를 출발물질로 하여 용매증발법에 의해 마이크로스피어를 제조하고, 제조 변수가 형성된 마이크로스피어의 형상 및 평균 입경에 미치는 영향을 살펴보았다. PVA 수용액의 농도가 1~5 wt%로 증가함에 따라 평균입경이 $370{\sim}160{\mu}m$으로 감소하다가 7 wt%에서다시 $240{\mu}m$으로 증가하였다. 그리고 PVA의첨가부피가 10~50 mL로 증가함에 따라 평균 입경은 $370{\sim}220{\mu}m$으로 감소하였다. 또한 교반속도가 500~1,500 rpm으로 증가함에 따라 평균 입경은 $370{\sim}110{\mu}m$으로 감소하였다. 유기용매로써 dichloromethane과 chloroform을 각각 사용한 경우 평균 입경은 큰 차이를 보이지 않았으며, dichloromethane을 사용한 경우 표면에서 공극이 확인되었으나 chloroform을 사용한 경우 매끈한 형상의 구형입자가 얻어졌다. Microspheres were prepared by solvent-evaporation method with Poly-L-lactic acid (PLLA) as a starting material, and the effects of preparation variables on microsphere shape and average particle size were investigated. As the concentration of PVA solution increased from 1 to 5 wt%, the average particle size decreased from $370{\mu}m$ to $160{\mu}m$ and then increased to $240{\mu}m$ at 7 wt%. On the other hand, As the addition volume of PVA solution increased from 10 mL to 50 mL, the average particle size decreased from $370{\mu}m$ to $220{\mu}m$. Also, as the stirring speed increased from 500 rpm to 1,500 rpm, the average particle size decreased from $370{\mu}m$ to $110{\mu}m$. When dichloromethane and chloroform were used as organic solvents, respectively, the average particle size did not show any significant difference. However, when dichloromethane was used, voids were observed on the particle surface, but when chloroform was used, smooth spherical particles were obtained.