• Title/Summary/Keyword: Sustained release microcapsules

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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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    • v.7 no.1
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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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Pharmaceutical Studies on Microencapsulated Etilefrine Hydrochloride (염산에틸에프린의 마이크로캅셀에 관한 약제학적 연구)

  • Kim, Johng-Kap;Choi, Soo-Il
    • Journal of Pharmaceutical Investigation
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    • v.16 no.1
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    • pp.12-17
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    • 1986
  • Etilefrine hydrochloride was microencapsulated with ethylcellulose by phase separation method to develop a sustained release dosage form. The results of dissolution test carried out with various microcapsules showed that the drug release was decreased with increasing the particle size of microcapsules at a constant core to wall ratio, and with decreasing the core to wall ratio. Also ethylcellulose 50 cps and fast stirring rate (900 rpm) was better in decreasing the drug release than ethylcellulose 22 cps and slow stirring rate (300 rpm), respectively.

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Preparation and Characteristics of Poly(ε-caprolactone) Microcapsules Containing Pseudomonas by W/O/W Emulsion (다중에멀젼법을 통한 슈도모나스를 함유하는 PCL 마이크로캡슐의 제조 및 특성 연구)

  • Kim, Ki-Seok;Lee, Seung-Yeop;Lee, Gun-Woong;Kim, Hyung-Gon;Park, Soo-Jin
    • Polymer(Korea)
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    • v.36 no.2
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    • pp.202-207
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    • 2012
  • Biodegradable poly(${\varepsilon}$-caprolactone)(PCL) microcapsules containing pseudomonas were prepared by W/O/W emulsion system. The characteristics and release behaviors of the microcapsules were investigated as a function of manufacturing conditions. The morphology and particle distribution of the microcapsules were observed by a scanning electron microscope and a particle size analyzer. The release behaviors of the pseudomonas were determined using a cell culture method. It was found that smooth and spherical microcapsules were formed by W/O/W emulsion system and particle size was in the range of 10 to 60 ${\mu}m$. The release behaviors of the pseudomonas were influenced by the manufacturing conditions. It was indicated that the increase of the surfactant content and stirring rate led to an increased release rate, resulting from the high specific surface area of the smaller particle size, and the increase of the PCL content provided the sustained release behaviors by the delay effect of diffusion in the release medium.

Revelation of the Susceptivility of Microcapsule by the Control of Polymer Structure (I) -preparation of polyurethane microcapsules- (고분자구조제어에 의한 microcapsule의 감성기능발현(I) -polyurethane microcapsule의 제조와 그 특성-)

  • Hong, Ki Jeong;Park, Soo Min
    • Textile Coloration and Finishing
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    • v.9 no.5
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    • pp.52-62
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    • 1997
  • Abstract Polyurethanes have been designed and fabricated into membranes with unique separation properties. Moreover, polyurethane microcapsules also have been reported actively as controlled release materials for their excellent blood compatibility, tensile strength and permeability. In this study, polyurethane microcapsules were synthesized by interfacial polymerization in an aqueous poly(ethylene glycol) dispersion of toluene diisocyanate in perfume oil using poly(vinyl alcohol) as the stabilizing agent. The effect of a few important process conditions on the average particle size and distributions, morphologies, and thermal properties to design microcapsules for the sustained release system was investigated.

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Water-insoluble, Whey Protein-based Microcapsules for Controlled Core Release Application (유청단백질을 이용한 미세캡슐의 응용)

  • Lee, Sung-Je
    • 한국유가공학회:학술대회논문집
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    • 2005.06a
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    • pp.37-61
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    • 2005
  • Microcapsules consisting of natural, biodegradable polymers for controlled and/or sustained core release applications are needed. Physicochemical properties of whey proteins suggest that they may be suitable wall materials in developing such microcapsules. The objectives of the research were to develop water-insoluble, whey protein-based microcapsules containing a model water-soluble drug using a chemical cross-linking agent, glutaraldehyde, and to investigate core release from these capsules at simulated physiological conditions. A model water soluble drug, theophylline, was suspended in whey protein isolate (WPI) solution. The suspension was dispersed in a mixture of dichloromethane and hexane containing 1% biomedical polyurethane. Protein matrices were cross-linked with 7.5-30 ml of glutaraldehyde-saturated toluene (GAST) for 1-3 hr. Microcapsules were harvested, washed, dried and analyzed for core retention, microstructure, and core release in enzyme-free simulated gastric fluid (SGF) and simulated intestinal fluid (SIF) at 37$^{\circ}C$, A method consisting of double emulsification and heat gelation was also developed to prepare water-insoluble, whey protein-based microcapsules containing anhydrous milkfat (AMF) as a model apolar core. AMF was emulsified into WPI solution (15-30%, pH 4.5-7.2) at a proportion of 25-50% (w/w, on dry basis). The oil-in-water emulsion was then added and dispersed into corn oil (50 $^{\circ}C$)to form an O/W/O double emulsion and then heated at 85$^{\circ}C$ for 20 min for gelation of whey protein wall matrix. Effects of emulsion composition and pH on core retention, microstructure, and water-solubility of microcapsules were determined. Overall results suggest that whey proteins can be used in developing microcapsules for controlled and sustained core release applications.

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Preparation and Evaluation of Sustained-Release $Eudragit^{\circledR}$ Microcapsules Containing ${\beta}-Lactam$ Antibiotics ($Eudragit^{\circledR}$ 마이크로캅셀화에 의한 ${\beta}$-락탐계 항생물질의 방출제어제제 개발)

  • Han, Kun;Shin, Do-Su;Jee, Ung-Kil;Chung, Youn-Bok
    • Journal of Pharmaceutical Investigation
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    • v.22 no.4
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    • pp.267-279
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    • 1992
  • Microencapsulations of amoxicillin and cephalexin, using Eudragit RS, RL, E, S and L were investigated. The microcapsules were prepared by the solvent evaporation process in liquid paraffin phase, which is based on dispersion of acetone/isopropanol containing the drug in liquid paraffin. Aluminium tristearate was used as an additive for the preparation of microcapsules. The size distribution, dissolution test and observation by SEM were examined. Good reproducibility in microcapsule preparation was observed. The microcapsules obtained were spherical and free-flowing particles. The dissolution rates of amoxicillin and cephalexin from the microcapsules were considerably decreased as compared with those from amoxicillin and cephalexin powder, respectively. As the dispersing agents (aluminium tristearate) increased, the particle size of microcapsules decreased and the dissolution rate increased. In order to control the release rate of drugs, microcapsules were prepared by mixing Eudragit RS/RL or Eudragit S/L. As Eudragit RL ratio in microcapsule of Eudragit RS/RL increased, the dissolution rate increased. As Eudragit L ratio in microcapsule of Eudragit S/L increased, the dissolution rate increased. Furthermore, the release rates of drugs from Eudragit RS/L or RS/polyelthylene glycol 1540 (PEG 1540) were examined. The dissolution rate of drugs increased with increasing of Eudragit L or PEG 1540 ratio. In conclusion, the release rates of drugs from Eudragit RS/RL or RS/PEG 1540 microcapsule could be controlled, and these microcapsules will be convenient for reducing frequency of administration.

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Studies on the Development of Sustained Release Preparation (I) Preparation and Evaluation of CAP Microcapsules of Sodium Ascorbate (지속성 제제의 개발에 관한 연구 (I) 아스코르빈산 나트륨의 CAP 마이크로캅셀의 제조 및 평가)

  • Shin, Sang-Chul;Koh, Ik-Bae
    • Journal of Pharmaceutical Investigation
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    • v.21 no.4
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    • pp.253-262
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    • 1991
  • Microencapsulation of sodium ascorbate with cellulose acetate phthalate(CAP) by coacervation/ phase separation method were carried out. Various factors affecting microencapsulation, i.e., surfactant concentration. CAP concentration, stirring speed and treatment of spermaceti as a sealing agent were studied. Dissolution rate. particle size distribution, surface feature and stability test were investigated. CAP microcapsules prepared using 0.5% span 80 as a surfactant showed smooth and round surfaces. The release of sodium ascorbate was retarded by microencapsulation with CAP and by sealant treatment with spermaceti. When triturated with sodium bicarbonate, CAP microcapsules were more stable than unencapsulated sodium ascorbate under various RH conditions at $37^{\circ}C$.

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Development of Sustained Release Microcapsules Containing Ion Exchange Resin-Dextromethorphan Hydrobromide Complex (이온교환수지 - 브롬화수소산덱스트로메토르판 복합체의 서방성 마이크로캅셀 개발에 관한 연구)

  • Kim, Chong-Kook;Hwang, Su-Won;Hwang, Sung-Joo;Lah, Woon-Lyong
    • Journal of Pharmaceutical Investigation
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    • v.19 no.2
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    • pp.99-107
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    • 1989
  • In order to develop a pediatric liquid preparation with sustained release properties, dextromethorphan hydrobromide (DEXT) was complexed with strong cation exchange resin (CG 120) and the-complex was coated with Eudragit RS using a phase separation method by non-solvent addition. The effect of pH, ionic strength of the release medium and drug/resin ratio on the release rate of DEXT was studied. The release rate of free drug from the uncoated complex, and coated complexes with 9.5 and 18.5% Eudragit RS in artificial gastric juice were measured. The release rate from the uncoated complex was faster with higher pH, higher ionic strength of the release medium and higher drug/resin ratio. The release rate from the coated complex could be controlled by the amount of coating material, and the surface after release did not rupture into.

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Microencapsulation of Caramel Flavor and Properties of Ready-to-drink Milk Beverages Supplemented with Coffee Containing These Microcapsules

  • Kim, Gur-Yoo;Lee, Jaehak;Lim, Seungtae;Kang, Hyojin;Ahn, Sung-Il;Jhoo, Jin-Woo;Ra, Chang-Six
    • Food Science of Animal Resources
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    • v.39 no.5
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    • pp.780-791
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    • 2019
  • This study aimed to extend the retention of flavor in coffee-containing milk beverage by microencapsulation. The core material was caramel flavor, and the primary and secondary coating materials were medium-chain triglyceride and maltodextrin, respectively. Polyglycerol polyricinoleate was used as the primary emulsifier, and the secondary emulsifier was polyoxyethylene sorbitan monolaurate. Response surface methodology was employed to determine optimum microencapsulation conditions, and headspace solid-phase microextraction was used to detect the caramel flavor during storage. The microencapsulation yield of the caramel flavor increased as the ratio of primary to secondary coating material increased. The optimum ratio of core to primary coating material for the water-in-oil (W/O) phase was 1:9, and that of the W/O phase to the secondary coating material was also 1:9. Microencapsulation yield was observed to be approximately 93.43%. In case of in vitro release behavior, the release rate of the capsules in the simulated gastric environment was feeble; however, the release rate in the simulated intestinal environment rapidly increased within 30 min, and nearly 70% of the core material was released within 120 min. The caramel flavor-supplemented beverage sample exhibited an exponential degradation in its flavor components. However, microcapsules containing flavor samples showed sustained flavor release compared to caramel flavor-filled samples under higher storage temperatures. In conclusion, the addition of coffee flavor microcapsules to coffee-containing milk beverages effectively extended the retention of the coffee flavor during the storage period.

Preparation of γ-oryzanol-loaded pectin micro and nanocapsules and their characteristics according to particle size (감마오리자놀 함유 칼슘-펙틴 미세 및 나노캡슐의 제조와 입자 크기에 따른 캡슐특성)

  • Lee, Seul;Kim, Eun Suh;Lee, Ji-Soo;Lee, Hyeon Gyu
    • Korean Journal of Food Science and Technology
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    • v.49 no.1
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    • pp.110-116
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    • 2017
  • ${\gamma}-Oryzanol-loaded$ calcium-pectin micro- and nanocapsules were prepared by ionic gelation to improve oxidation stability and the effect of particle size on capsule properties was investigated. The physical properties were influenced by preparation conditions such as concentrations of pectin, $CaCl_2$, ${\gamma}-oryzanol$, and hardening time. Particle sizes of micro- and nanocapsules that showed the maximum encapsulation efficiency and sustained release were $2.27{\pm}0.02mm$ and $347.7{\pm}58.1nm$, respectively. Microcapsules showed higher encapsulation efficiency ($50.73{\pm}1.98%$) than nanocapsules ($17.70{\pm}2.04%$), while nanocapsules showed more sustained release and higher stability than microcapsules. Release of ${\gamma}-oryzanol$ from both microand nanocapsules, which was low in gastric environments and promoted in intestinal environments, showed suitable characteristics for oral administration. Furthermore, antioxidant activity of ${\gamma}-oryzanol$ against autoxidation of linoleic acid was prolonged by both micro- and nanoencapsulation in a ferric thiocyanate test. Therefore, micro- and nanoencapsulation using pectin can be effective for improving biodelivery, stability, and antioxidant activity of ${\gamma}-oryzanol$.