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  • 标题:Pharmaceutical Studies of Levothyroxine Sodium Hydrate Suppository Provided as a Hospital Preparation
  • 本地全文:下载
  • 作者:Yuhei Hamada ; Kazushi Masuda ; Masato Okubo
  • 期刊名称:Biological and Pharmaceutical Bulletin
  • 印刷版ISSN:0918-6158
  • 电子版ISSN:1347-5215
  • 出版年度:2015
  • 卷号:38
  • 期号:4
  • 页码:625-628
  • DOI:10.1248/bpb.b14-00721
  • 出版社:The Pharmaceutical Society of Japan
  • 摘要:

    The levothyroxine sodium hydrate suppository (L-T4-suppository) is provided as a hospital preparation for the treatment of hypothyroid patients with dysphagia in Japan because only oral preparations of levothyroxine sodium (L-T4) are approved for the treatment of hypothyroidism. However, it has been found that serum thyroxine and triiodothyronine levels do not increase as expected with the hospital preparation, requiring a higher dosage of L-T4 in the L-T4-suppository than in the oral preparations. In this study, to determine an effective thyroid gland hormone-replacement therapy for patients with dysphagia, the pharmaceutical properties of the L-T4-suppository were investigated. Suppositories containing 300 µg L-T4 in a base of Witepsol H-15 and Witepsol E-75 (ratio of 1 : 1) were prepared according to Chiba University Hospital’s protocol. Content uniformity, stability, and suppository release were tested. The L-T4-suppository had uniform weight and content. The content and release property were stable over 90 d when the L-T4-suppository was stored at 4°C and protected from light. The release rate of L-T4 increased as pH increased. However, no L-T4 was released below pH 7.2. The release rate of L-T4 decreased as temperature decreased. These findings suggest that the low level of release of L-T4 in the rectum under physiological conditions may be the cause of the low serum thyroxine and triiodothyronine levels following L-T4-suppository administration.

  • 关键词:levothyroxine sodium hydrate; suppository; hospital preparation; hypothyroidism; pharmaceutical study; thyroid gland hormone replacement therapy
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