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Enhancing Mechanism of Enhancers as a Basis for Delivery of Bioactive Peptides

Research Project

Project/Area Number 06453195
Research Category

Grant-in-Aid for Scientific Research (B)

Allocation TypeSingle-year Grants
Section一般
Research Field 応用薬理学・医療系薬学
Research InstitutionKumamoto University

Principal Investigator

NAKANO Masahiro  Kumamoto University Hospital Pharmacy Professor, 医学部・附属病院, 教授 (40002125)

Co-Investigator(Kenkyū-buntansha) ARIMORI Kazuhiko  Kumamoto University Hospital Pharmacy Associate Professor, 医学部・附属病院, 助教授 (70253739)
Project Period (FY) 1994 – 1996
Project Status Completed (Fiscal Year 1996)
Budget Amount *help
¥6,200,000 (Direct Cost: ¥6,200,000)
Fiscal Year 1996: ¥1,100,000 (Direct Cost: ¥1,100,000)
Fiscal Year 1995: ¥1,400,000 (Direct Cost: ¥1,400,000)
Fiscal Year 1994: ¥3,700,000 (Direct Cost: ¥3,700,000)
Keywordschitosan / insulin / riboflavin phosphate / absorption enhancer / nasal mucosa / lidocaine / diltiazem / salmon calcitonin / 塩基性高分子 / エグアレン / 粘膜透過 / ウサギ / リボフラビン / 口腔粘膜 / 皮膚透過 / グリチルリチン誘導体 / 1ーメントール / d-リモネン / 透過促進
Research Abstract

When lidocaine is dissolved in an aqueous gel, the drug is absorbed well, and decreased pain when a needle is inserted through the skin for injection of human growth hormone.
Al though diltiazem is absorbed through the gastrointestinal tract well, formulations which enable to absorb the drug fast through oral mucosa is required since absorption of diltiazem through the oral mucosa is not very efficient. High concentrations in the mouth caused by fast dissolution of the drug in the mouth are required to increase absorption from the mouth and to give enough concentrations in the blood.
Amphotericin B with molecular weight of 924 is a large molecule and is poorly absorbed from the gastrointestinal tracts. In order to absorb the drug in a predictable fashion, some modification in formulation is necessary. Concentrations of the drug in the blood were measured both in adults and children and low in both.
Effect of chitosan, a polysaccaride with amino groups, on nasal absorption of hydrophilic drugs was studied as a representative of basic polymers. Aqueous solubility is limited in high molecular weight chitosan, and moderately soluble chitosan samples weer examined. Riboflavin phosphate was used as a model of peptides because of its hydrophilic nature and its easy assay. Chitosan samples were obtained from several companies and four samples with high aqueous solubility were employed in the study. Effect of chitosan on absorption of riboflavin phosphate through nasal mucosa in rabbits was studied. Effect of concentrations of chitosan on enhancing absorption of riboflavin phosphate was studied in Chitosan C-9 because other samples were less soluble than this in water. Maximal enhancing effect was noted at 0.5% among 0.5,1, and 2%. Bioavailability of insulin was increased by chitosan.
Egualen, a delivative of azulene was effective in increasing bioavailability of insulin and salmon calcitonin.

Report

(4 results)
  • 1996 Annual Research Report   Final Research Report Summary
  • 1995 Annual Research Report
  • 1994 Annual Research Report
  • Research Products

    (19 results)

All Other

All Publications (19 results)

  • [Publications] N.Iwatani et al.: "Dermal anesthesia using a lidocaine gel patch for pain of human growth hormone (hGH) self-injection and relief of anxiety." Clin.Pediatr.Endocrinol.3(2). 113-116 (1994)

    • Description
      「研究成果報告書概要(和文)」より
    • Related Report
      1996 Final Research Report Summary
  • [Publications] 塩津和則他: "ジルチアゼムのヒト口腔からの吸収と塩酸ジルチアゼム速溶錠の調製ならびにその基礎的検討." 病院薬学. 21(5). 389-395 (1995)

    • Description
      「研究成果報告書概要(和文)」より
    • Related Report
      1996 Final Research Report Summary
  • [Publications] 藤井淳子他: "成人および小児における経口大量投与時のamphotericin Bの血清中濃度" 臨床薬理. 26(4). 779-784 (1995)

    • Description
      「研究成果報告書概要(和文)」より
    • Related Report
      1996 Final Research Report Summary
  • [Publications] 中野眞汎: "DDSタイプ製剤の現状" 日本病院薬剤師会雑誌. 31(7-8). 821-824 (1995)

    • Description
      「研究成果報告書概要(和文)」より
    • Related Report
      1996 Final Research Report Summary
  • [Publications] 中野眞汎他: "安全性をめざした医薬品適用" 医歯薬出版, 102 (1995)

    • Description
      「研究成果報告書概要(和文)」より
    • Related Report
      1996 Final Research Report Summary
  • [Publications] 中野眞汎: "臨床薬理学" 医学書院, 124-128 (1996)

    • Description
      「研究成果報告書概要(和文)」より
    • Related Report
      1996 Final Research Report Summary
  • [Publications] N.Iwatani et al.: "Dermal anesthesia using a lidocaine gel patch for pain of human growth hormone (hGH) self-injection and relief of anxiety" Clin.Pediatr.Endocrinol. 3-2. 113-116 (1994)

    • Description
      「研究成果報告書概要(欧文)」より
    • Related Report
      1996 Final Research Report Summary
  • [Publications] K.Shiotsu et al.: "Absorpton of diltiazem from the oral cavity, and development of fast-release tablets" Jap.J.Hosp.Pharm.21-5. 389-395 (1995)

    • Description
      「研究成果報告書概要(欧文)」より
    • Related Report
      1996 Final Research Report Summary
  • [Publications] J.Fujii et al.: "Serum levels of amphotericin B in adults and children following large-dose oral administration" Jap.J.Clin.Pharmacol.Ther.26-4. 779-784 (1995)

    • Description
      「研究成果報告書概要(欧文)」より
    • Related Report
      1996 Final Research Report Summary
  • [Publications] M.Nakano: "Present status of DDS type pharmaceutical preparations" J.Jap.Soc.Hosp.Pharmacists. 31-7,8. 821-824 (1995)

    • Description
      「研究成果報告書概要(欧文)」より
    • Related Report
      1996 Final Research Report Summary
  • [Publications] M.Nakano ed.: Administration of drugs to insure safety. Midical-Dental-Pharmaceutical Publisher, (1995)

    • Description
      「研究成果報告書概要(欧文)」より
    • Related Report
      1996 Final Research Report Summary
  • [Publications] M.Nakano: Drug delivery system. Clinical Pharmacology S.Nakano et al.eds., Medical Publisher, 124-128 (1996)

    • Description
      「研究成果報告書概要(欧文)」より
    • Related Report
      1996 Final Research Report Summary
  • [Publications] Matsuo,M.et al.: "Delayed-releease tablets using hydroxyethylcellullose as a gelforming matrix" International Journal of Pharmaceutics. 138(2). 225-235 (1996)

    • Related Report
      1996 Annual Research Report
  • [Publications] 中野眞汎: "臨床薬理学" 医学書院, 124-128 (1996)

    • Related Report
      1996 Annual Research Report
  • [Publications] M.Matsuo,C.Nakamura,K.Arimori,M.Nakano: "Evaluation of hybroxyethylcellulose as a hydrophilic swellable material for delay-ed release tablets." Chemical and Pharmaceutical Bulletin. 43(2). 311-314 (1995)

    • Related Report
      1995 Annual Research Report
  • [Publications] 中野眞汎: "DDSタイプ製剤の現状" 日本病院薬剤師会雑誌. 31(7/8). 821-824 (1995)

    • Related Report
      1995 Annual Research Report
  • [Publications] 塩津和則,有森和彦,中野眞汎: "ジルチアゼムのヒト口腔からの吸収と塩酸ジルチアゼム速溶錠の調製ならびにその基礎的検討" 病院薬学. 21(5). 389-395 (1995)

    • Related Report
      1995 Annual Research Report
  • [Publications] N.Iwatani,M.Kodama,T.Miike,T.Kano,M.Nakano,M.Mishima,O.Tsuzuki: "Dermal anesthesia using a lidocaine gel patch for pain of human growth hormone(hGH) self-injection and relief of anxiety" Clinical Pediatrics and Endocrinology. 3. 113-116 (1994)

    • Related Report
      1994 Annual Research Report
  • [Publications] M.matsuo,C.Nakamura,K.Arimori,M.Nakano: "Evaluation of hydroxyethylcelluse as a hydroxyethylcelluse as a hydrophilic swellable material for delayed-release tablets" Chemical and Pharmaceutical Bulletin. 43. 311-314 (1995)

    • Related Report
      1994 Annual Research Report

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Published: 1994-04-01   Modified: 2016-04-21  

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