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1995 Fiscal Year Final Research Report Summary

Functional Adaptation of Subsieve-size Pharmaceutical Particles by an Air-suspension Technique

Research Project

Project/Area Number 05671798
Research Category

Grant-in-Aid for General Scientific Research (C)

Allocation TypeSingle-year Grants
Research Field Physical pharmacy
Research InstitutionFaculty of Pharmaceutical Sciences, Kobe Gakuin University

Principal Investigator

FUKUMORI Yoshinobu  Kobe Gakuin University, Faculty of Pharmaceutical Sciences, Professor, 薬学部, 教授 (60102927)

Project Period (FY) 1993 – 1995
KeywordsMicrocapsule / Coating / Fluidized bed / Chemoembolization therapy / Neutron-capture therapy / Controlled release / Latex / Powder
Research Abstract

Polymer molecular structure, phase structure of polymer, formulation of mixtures and particle structure were designed to prepare functional microcapsules (MCs).
1. Coating of fine particles with compisite latices : (1) Physico-chemical properties of latex polymer required to successfully perform coating of subsieve-size particles were made clear. A composite latex with 12 : 6 : 4 poly (ethyl acrylate (EA) /methyl methacrylate (MMA) /2-hydroxyethyl methacrylate (HEMA)) core and 6 : 12 : 8 poly (EA/MMA/HEMA) shell was synthesized. This latex exhibited an excellent coating performance even for tens mum particles. (2) A composite latex with N-isopropylacrylamide shell newly synthesized exhibited excellent coating performance, self-film-formability in water and thermosensitive drug release.
2. Multi-functional MCs with lecithin membrane : (1) MCs with membrane copmosed of soybean lecithin (SL), cholesterol (CH), stearic acid (SA) and polyvinylpyrrolidone (PVP) exhibited short-term delayd, pro … More longed release and bioerosion in vivo. Phase structure in MC membrane was determined by differential scanning calorimetry, X-ray diffractometry and polarizing microscopy and a phase diagram of SL-CH-SA-PVP system was drawn. (2) The behaviors of SL MCs could be widely controlled even in vivo by changing their membrane formulation, membrane thickness and type of lecithin.
3. MCs for neutron-capture therapy : (1) Hydrophobic gadolinium chelate, Gd diethylene-pentaacetic acid distearylamide (Gd-DTPA-SAm), -containing MCs with 9 : 9 : 4 poly (EA/MMA/HEMA) membrane had a mass median diameter of 52 mum and a Gd-DTPA-SAm content of 29.3%, and released Gd of only 0.23% for 60 days. This showed the prepared MCs to be used as depots for neutron-capture therapy. (2) By hepatic arterial injection of 29.3 % Gd-DTPA-SAm-containing SL-Mcs, 41.6 % of the dose was retained by rat livers. Hepatic tissue damage by the intraarterial injection of the MCs was determined biochemically and histologically. The results suggested that the prepared SL-MSs could be used for treatment of hepatoma without serious tissue necrosis when appropriate formulation and dose were chosen. Less

  • Research Products

    (24 results)

All Other

All Publications (24 results)

  • [Publications] Hideki Ichikawa: "Coating of Pharmaceutical Powders by Fluidized Bed Process. V. Agglomeration and Efficiency in the Coating with Aqueous Latices of Copoly (Ethyl Acrylate-Methyl Methacrylate-2-Hydroxyethyl Methacrylate)" Chemical and Pharmaceutical Bulletin. 41. 1132-1136 (1993)

    • Description
      「研究成果報告書概要(和文)」より
  • [Publications] Yoshinobu Fukumori: "Design and Preparation of Ethyl Cellulose Microcapsules of Gadopentetate Dimeglumine for Neutron-Capture Therapy Using the Wurster Process" Chemical and Pharmaceutical Bulletin. 41. 1144-1148 (1993)

    • Description
      「研究成果報告書概要(和文)」より
  • [Publications] 福森義信: "噴流層での湿式造粒とコーティングによる医薬品製剤の機能化" 粉体と工業. 25. 27-33 (1993)

    • Description
      「研究成果報告書概要(和文)」より
  • [Publications] 福森義信: "微粒子の湿式スプレーコーティング" PHARM TECH JAPAN. 9. 763-769 (1993)

    • Description
      「研究成果報告書概要(和文)」より
  • [Publications] Hideki Ichikawa: "Coating of Pharmaceutical Powders by Fluidized Bed Process. VI. Microencapsulation Using Blend and Composite Latices of Copoly(Ethyl Acryl-ate-Methyl Methacrylate-2-Hydroxyethyl Methacrylate)" Chemical and Pharmaceutical Bulletin. 42. 1308-1314 (1994)

    • Description
      「研究成果報告書概要(和文)」より
  • [Publications] Yoshinobu Fukumori: "Dissolution Properties of Soybean Lecithin Microcapsules for Short-Term Controlled Release Prepared Using the Wurster Process," Chemical and Pharmaceutical Bulletin. 42. 2604-2611 (1994)

    • Description
      「研究成果報告書概要(和文)」より
  • [Publications] 福森義信: "水系分散剤コーティングによる徐放性微粒子の調製と評価" 化学光学. 59. 174-177 (1995)

    • Description
      「研究成果報告書概要(和文)」より
  • [Publications] Hideki Ichikawa: "Coating Performance of Aqueous Composite Latices with N-Isopropylacrylamide Shell and Thermosensitive Permeation Properties of Their Microcapsule Membranes" Chemical and Pharmaceutical Bulletin. 44. 383-391 (1996)

    • Description
      「研究成果報告書概要(和文)」より
  • [Publications] Kaori Jono: "Phase Separation in Microcapsule Membranes Composed of Soybean lecithin,Cholesterol,Stearic Acid and Polyvinylpyrrolidone" Chemical and Pharmaceutical Bulletin. 44. 392-398 (1996)

    • Description
      「研究成果報告書概要(和文)」より
  • [Publications] 川島嘉明: "粒子設計と製剤技術" 薬業時報社, 232 (1993)

    • Description
      「研究成果報告書概要(和文)」より
  • [Publications] A. H. Soloway: "Advances in Neutron Capture Therapy" Plenum Press, 829 (1993)

    • Description
      「研究成果報告書概要(和文)」より
  • [Publications] I. Gherbre-Sellassie: "Multiparticulate Oral Drug Delivery" Marcel Dekker,Inc., 480 (1994)

    • Description
      「研究成果報告書概要(和文)」より
  • [Publications] Hideki Ichikawa: "Coating of Pharmaceutical Powders by Fluidized Bed Process. V.Agglomeration and Efficiency in the Coating with Aqueous Latices of Copoly (Ethyl Acrylate -Methyl Methacrylate- 2-Hydroxyethyl Methacrylate)" Chem.Pharm.Bull.41. 1132-1136 (1993)

    • Description
      「研究成果報告書概要(欧文)」より
  • [Publications] Yoshinobu Fukumori: "Design and Preparation of Ethyl Cellulose Microcapsules of Gadopentetate Dimeglumine for Neutron-Capture Therapy Using the Wurster Process" Chem.Pharm.Bull.41. 1144-1148 (1993)

    • Description
      「研究成果報告書概要(欧文)」より
  • [Publications] Yoshinobu Fukumori: "Fluidized Bed Agglomeration and Coating in Preparation of Novel Pharmaceutical Dosage Forms" Powder Sci.Eng.25. 27-33 (1993)

    • Description
      「研究成果報告書概要(欧文)」より
  • [Publications] Yoshinobu Fukumori: "Wet Spray Coating of Fine Particles" PHARM TECH JAPAN. 9. 763-769 (1993)

    • Description
      「研究成果報告書概要(欧文)」より
  • [Publications] Hideki Ichikawa: "Coating of Pharmaceutical Powders by Fluidized Bed Process.VI.Microencapsulation Using Blend and Composite Latices of Copoly (Ethyl Acrylate-Methyl Methacrylate-2-Hydroxyethyl Methacrylate)" Chem.Pharm.Bull.42. 1308-1314 (1994)

    • Description
      「研究成果報告書概要(欧文)」より
  • [Publications] Yoshinobu Fukumori: "Dissolution Properties of Soybean Lecithin Microcapsules for Short-Term Controlled Release Prepared Using the Wurster Process" Chem.Pharm.Bull.42. 2604-2611 (1994)

    • Description
      「研究成果報告書概要(欧文)」より
  • [Publications] Yoshinobu Fukumori: "Preparation of Controlled Releasing Fine Particles Using Aqueous Dispersion and Their Evaluation" KAGAKU KOGAKU. 59. 174-177 (1995)

    • Description
      「研究成果報告書概要(欧文)」より
  • [Publications] Hideki Ichikawa: "Coating Performance of Aqueous Composite Latices with N-Isopropylacrylamide Shell and Thermosensitive Permeation Properties of Their Microcapsule Membranes" Chem.Pharm.Bull.44. 383-391 (1996)

    • Description
      「研究成果報告書概要(欧文)」より
  • [Publications] Kaori Jono: "Phase Separation in Microcapsule Membranes Composed of Soybean Lecithin, Cholesterol, Stearic Acid and Polyvinylpyrrolidone" Chem.Pharm.Bull.44. 392-398 (1996)

    • Description
      「研究成果報告書概要(欧文)」より
  • [Publications] Yoshiaki Kawashima: Particulate Design and Pharmaceutical technique. Yakugyo Jihosha, 232 (1993)

    • Description
      「研究成果報告書概要(欧文)」より
  • [Publications] A.H.Soloway: Advances in Neutron Capture Therapy. Plenum Press, 829 (1993)

    • Description
      「研究成果報告書概要(欧文)」より
  • [Publications] Issac Ghebre-Sellassie: Multiparticulate Oral Drug Delivery. Marcel Dekker, Inc., 480 (1994)

    • Description
      「研究成果報告書概要(欧文)」より

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Published: 1997-03-04  

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