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Development of Oral Dosage form for Poorly Absorbable Drugs

Research Project

Project/Area Number 05557102
Research Category

Grant-in-Aid for Developmental Scientific Research (B)

Allocation TypeSingle-year Grants
Research Field Physical pharmacy
Research InstitutionTokyo University of Pharmacy and Life Science

Principal Investigator

AWAZU Shojii  School of Pharmacy Professor, 薬学部, 教授 (60012621)

Co-Investigator(Kenkyū-buntansha) HOSOI Kaoru  Meiji Seika K.K.Shinier Researcher, 薬品総合研・製剤研究所, 室長
HAYASHI Masahiro  Science University of Tokyo Professor, 薬学部, 教授 (20012669)
Project Period (FY) 1993 – 1994
Project Status Completed (Fiscal Year 1994)
Budget Amount *help
¥11,100,000 (Direct Cost: ¥11,100,000)
Fiscal Year 1994: ¥4,000,000 (Direct Cost: ¥4,000,000)
Fiscal Year 1993: ¥7,100,000 (Direct Cost: ¥7,100,000)
KeywordsCaco-2 / Absorption enhancement / Bioadhensive / Microsphere / Peptide / Intestinal / Concanvaline A / Peyer's Patch / Coco-2細胞 / ヒト結腸 / 吸収促進剤 / 粘膜付着性マイクロカプセル / ポリカーボフィル / 保水効果 / 小腸パイエル板 / エンドサイトーシス
Research Abstract

Assessment System of Drug Absorption by Cultured Cells, and Control of Whole Study. Caco-2 cell monolayr system for absorption was established. The absorptions were well correlated with the results in human colon. The absorption from the bioadhesive microsphere (MS) developed by Meiji Seika group was determined in this system. Polycarbophil (PCP) that is used for adhesive coating exhibited absorption enhancement. MS coated with decanoyl carnitine(absorption enhancer)and PCP showed more 10 times absorbability than control, showing the promise of adhesive MS.Cationic polyamino acids showed the possibility to be used as adhesive coating material with absorption enhancement. Absorbability of Polypeptides and Prodrug in Peyer's Patch. Concanavalin (Con A) , a rectin, that is expected to target to Peyer's patch (PP) was conjugated with BSA in the ratio 1/1 (maleimide method) . This conjugate showed higher permeability in PP than BSA itself. This showed the possibility to use rectin protein conjugate as a prodrug for absorption enhancement. Polylacetic acid Polyglycolic acid copolymer MS was prepared as DDS for PP.The absorption of BSA,HRP and SOD from the MS was examined, but the determination of transported amounts of these compounds in this system remained as future problem. Development of Membrane Adhesive Micorosphere (MC) and MS targeted to PP.The adhesive MC was not prepared because of surface activity of the enhancers encapsulated in MC.since MS can be substituted, the adhesive MS preparation was examined. PVP as base was found unsuitable, because the prepared MS shapes were not uniform. Gelatine MS coated with PCP exhibited enough adhesiveness with good release.

Report

(3 results)
  • 1994 Annual Research Report   Final Research Report Summary
  • 1993 Annual Research Report
  • Research Products

    (8 results)

All Other

All Publications (8 results)

  • [Publications] S.Haseto,H.Ohuchi,T.Isoda,T.Mizuma,M.Hayashi and S.Awazu: "Transport of low and high molecular peptides across rabbit Peyer's patches" Pharm.Res.11. 361-364 (1994)

    • Description
      「研究成果報告書概要(和文)」より
    • Related Report
      1994 Final Research Report Summary
  • [Publications] M.Tomita,M.Hayashi and S.Awazu: "Comparison of absorption-enhancing effect between sodium caprate and disodium ethylenediaminetetraacetate in Caco-2 cells" Bio.Pharm.Bull.17. 753-755 (1994)

    • Description
      「研究成果報告書概要(和文)」より
    • Related Report
      1994 Final Research Report Summary
  • [Publications] Shingo Haseto, Hiroyuki Ohuchi, Tomonori Isoda, Takashi Mizuma, Masahiro Hayashi and Shoji Awazu: "Transport of low and high molecular peptides across rabbit Peyer's patches" Pharm.Res. 11. 361-364 (1994)

    • Description
      「研究成果報告書概要(欧文)」より
    • Related Report
      1994 Final Research Report Summary
  • [Publications] Mikio Tomita, Mahasiro Hayashi and Shoji Awazu: "Comparison of absorption-enhancing effect between sodium caprate and disodium ethylenediaminetetraacetate in Caco-2cells" Bio.Pharm.Bull. 17(5). 753-755 (1994)

    • Description
      「研究成果報告書概要(欧文)」より
    • Related Report
      1994 Final Research Report Summary
  • [Publications] S.Haseto,H.Ohuchi,T.Isoda,T.Mizuma,M.Hayashi and S.Awazu: "Transport of low and high molecular peptides across rabbit Peyer′s patches" Pharm.Res.11. 361-364 (1994)

    • Related Report
      1994 Annual Research Report
  • [Publications] M.Tomita,M.Hayashi and S.Awazu: "Comparison of absorption-enhancing effect between sodium caprate and disodium ethyleneviaminetetraacetate in Caco-2 cells" Bio.Pharm.Bull.17. 753-755 (1994)

    • Related Report
      1994 Annual Research Report
  • [Publications] Shingo Haseto: "Transport of low and high molecular peptides across rabbit peyer s patch" Pharmaceutical Research. 11(3). 361-364 (1994)

    • Related Report
      1993 Annual Research Report
  • [Publications] Mikio Tomita: "Comparison of absorption-enhancing effect between sodium caprate and disodium ethylenediaminetetraacetate in Caco-2 cells" Biological and Pharmaceutical Bulletin in press.

    • Related Report
      1993 Annual Research Report

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Published: 1993-04-01   Modified: 2025-11-19  

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