Preparation and Evaluation of Tablets Rapidly Disintegrating in Salive Containing Bitter-Taste-Masked Granules by the Compression Method

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概要

• 論文の詳細を見る

• The aim of this study was to prepare, using taste-masked granules, tablets which can rapidly disintegrate in saliva (rapidly disintegrating tablet), of drugs with bitter taste (pirenzepine HCl or oxybutynin HCl). The taste-masked granules were prepared using aminoalkyl methacrylate copolymers (Eudragit E-100^[○!R]) by the extrusion method. None of the drugs dissolved from the granules (% of dissolved, <5%) even at 480 min at pH 6.8 in the dissolution test. However, the drugs dissolved rapidly in the medium at pH 1.2 in the dissolution test. Rapidly disintegrating tablets were prepared using the prepared taste-masked granules, and a mixture of excipients consisting of crystalline cellulose (Avicel PH-102^[○!R]) and low-substituted hydroxypropylcellulose (L-HPC, LH-11^[○!R]). The granules and excipients were mixed well (mixing ratio by weight, crystalline cellulose : L-HPC=8 : 2) with 1% magnesium stearate, and subsequently compressed at 500-1500 kgf in a single-punch tableting machine. The prepared tablets (compressed at 500 kgf) containing the taste-masked granules have sufficient strength (the crusing strength : oxybutynin tablet, 3.5 kg; pirenzepine tablet, 2.2 kg), and a rapid disintegration time (within 20 s) was observed in the saliva of healthy volunteers. None of the volunteers felt any bitter taste after the disintegration of the tablet which contained the taste-masked granules. We confirmed that the rapidly disintegrating tablets can be prepared using these taste-masked granules and excipients which are commonly used in tablet preparation.

• 公益社団法人日本薬学会の論文
• 1999-10-15

著者

• ISHIKAWA Tatsuya

  Department of Surgical Neurology, Research Institute for Brain and Blood Vessels-Akita

• Matsumoto M

  Osaka Medical Center For Cancer And Cardiovascular Diseases Osaka

• Matsumoto Misako

  Department Of Immunology Osaka Medical Center For Cancer And Cardiovascular Diseases

• Watanabe Yoshiteru

  Department of Pharmaceutics and Biopharmaceutics, Showa Pharmaceutical University

• Matsumoto Mitsuo

  Department of Pharmaceutics, Showa Pharmaceutical University

• Matsumoto Mitsuharu

  Takeda Chemical Industries Ltd. Pharmaceutical Research Division

• UTOGUCHI Naoki

  Department of Pharmaceutics and Biopharmaceutics, Showa Pharmaceutical University

• Ishikawa Tsutomu

  Dep. Of Medicinal Organic Chemistry Graduate School Of Pharmaceutical Sciences Chiba Univ.

• Watanabe Yoshiteru

  Department Of Pharmaceutics And Biopharmaceutics Showa Pharmaceutical University

• Watanabe Y

  Showa Pharmaceutical Univ.

• Ishikawa T

  Graduate School Of Pharmaceutical Sciences Chiba University

• Ishikawa Tsutomu

  Graduate School Of Pharmaceutical Sciences Chiba Univ.

• Watanabe Yoshiteru

  Showa Pharmaceutical Univ.

• Ishikawa Tatsuya

  Department Of Neonatology And Pediatrics Nagoya City University Graduate School Of Medical Sciences

• Utoguchi Naoki

  Department Of Biopharmaceutics School Of Pharmaceutical Sciences Teikyo University

• Matsumoto Mitsuhiro

  First Department Of Internal Medicine Kumamoto University School Of Medicine

• Matsumoto Mitsuo

  Department Of Pharmaceutics And Biopharmaceutics Showa Pharmaceutical University

• Ishikawa Tatsuya

  Department Of Civil Engineering Nagoya University

• Ishikawa Tatsuya

  Department Of Applied Chemistry Faculty Of Science Science University Of Tokyo

• Matsumoto Mitsuo

  Department Of Ophthalmology Hirosaki University School Of Medicine

• Ishikawa Toshihisa

  Department of Biomolecular Engineering, Graduate School of Bioscience and Biotechnology, Tokyo Institute of Technology

• Ishikawa Toshihisa

  Graduate School of Pharmaceutical Sciences, Chiba University

• Matsumoto Mitsuo

  Department of Hydrocarbon Chemistry, Faculty of Engineering, Kyoto University

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