New preparation method of intestinal pressure-controlled colon delivery capsules by coating machine and evaluation in beagle dogs.

DOI 15 References
  • Hu Zhaopeng
    Department of Pharmacokinetics, Kyoto Pharmaceutical University
  • Kimura Go
    Department of Pharmacokinetics, Kyoto Pharmaceutical University
  • Mawatari Shun-suke
    Department of Pharmacokinetics, Kyoto Pharmaceutical University
  • Shimokawa Tatsuhiro
    Department of Pharmacokinetics, Kyoto Pharmaceutical University
  • Takada Kanji
    Department of Pharmacokinetics, Kyoto Pharmaceutical University

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  • 大腸内圧崩壊型大腸デリバリーカプセルｉｎｔｅｓｔｉｎａｌ　ｌｕｍｉｎａｌ　ｐｒｅｓｓｕｒｅ‐ｃｏｎｔｒｏｌｌｅｄ　ｃｏｌｏｎ　ｄｅｌｉｖｅｒｙ　ｃａｐｓｕｌｅ（ＰＣＤＣ）のコーティング機による量産法の確立とその大腸送達性評価

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Description

A new method for preparing large amounts of intestinal luminal pressure-controlled colon delivery capsule (PCDC) which employs a pharmaceutical coating machine, Hicoater-mini®, has been developed. As a model drug, fluorescein (FL) powder was suspended with suppository base, polyethylene glycol (PEG) 1000, at 50°C, and was hardened in the capsular shape. The capsular shaped suppositories were coated with 5w/v % ethanolic EC (7G grade) solution by a coating machine. By increasing the coating time from 55min to 75min, the mean coating thickness of PCDCs increased. Several kinds of #0 PCDCs having the mean EC coating membrane thickness of 141±7 μm (type 1), 166±4 μm (type 2), 188±4 μm (type 3), 211±4 μm (type 4) as well as #2 PCDCs having thickness of 102±3 μm (type 5) and 110±5 μm (type 6) were administrated to beagle dogs. The mean first appearance times (Tis) of FL into the systemic circulation from #0 PCDCs were 2.3±0.5 for type 1, 3.3±0.5 for type 2, 4.8±1.0 for type 3 and 7.8±1.7hr for type 4 preparations while the mean Tis of #2 PCDCs were 3.2±0.4 for type 5 and 3.8±0.4 hr for type 6, respectively. Therefore, it was suggested that types 2, 3 and 5 PCDCs were delivered to the colon.

Journal

  • Drug Delivery System

    Drug Delivery System 14 (2), 123-127, 1999

    THE JAPAN SOCIETY OF DRUG DELIVERY SYSTEM

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