Pharmaceutical and Clinical Assessment of Hydroquinone Ointment Prepared by Extemporaneous Nonsterile Compounding.

• Matsubayashi Teruhisa

  Department of Hospital Pharmacy, School of Medicine, Kobe University

• Sakaeda Toshiyuki

  Department of Hospital Pharmacy, School of Medicine, Kobe University

• Kita Tomoko

  Department of Hospital Pharmacy, School of Medicine, Kobe University

• Nara Michiyo

  Department of Hospital Pharmacy, School of Medicine, Kobe University

• Funasaka Yoko

  Department of Dermatology, School of Medicine, Kobe University

• Ichihashi Masamitsu

  Department of Dermatology, School of Medicine, Kobe University

• Fujita Takuya

  Department of Biopharmaceutics, Kyoto Pharmaceutical University

• Kamiyama Fumio

  Department of Biopharmaceutics, Kyoto Pharmaceutical University

• Yamamoto Akira

  Department of Biopharmaceutics, Kyoto Pharmaceutical University

• Nordlund James J.

  Department of Dermatology, University of Cincinnati College of Medicine

• Kaneko Masafumi

  Department of Synthetic Organic Chemistry, Graduate School of Pharmaceutical Sciences, Kyoto University

• Iida Akira

  Department of Synthetic Organic Chemistry, Graduate School of Pharmaceutical Sciences, Kyoto University

• Hirai Midori

  Department of Clinical Pharmacy, Kobe Pharmaceutical University

• Okumura Katsuhiko

  Department of Hospital Pharmacy, School of Medicine, Kobe University

抄録

Ointments of the skin depigmentation agent hydroquinone (HQ) have been prepared by extemporaneous nonsterile compounding in Japan by imitating skin lightening creams commercially available in the U.S.A. and European Union. In our hospital, HQ ointments consisting of 5 or 10% HQ, 1.6% l(+)-ascorbic acid (AsA), 0.5% (w/w) Na₂SO₃, 10% (v/w) glycerin and hydrophilic ointment have been prepared. However, various problems have been observed including chromatic aberration of HQ ointments, relatively large variability of efficacy, and undesirable side effects although they were mild. Herein, the pharmaceutical and clinical properties of the HQ ointments were evaluated. HQ ointments were highly effective for treatment of various types of skin pigmentation. Chromatic aberration occurred during 3 months of storage, but this could be suppressed by storage at 4 °C. Chromatic aberration was independent of prescribed HQ content, and was not explained by alterations of HQ or p-benzoquinone (p-BQ) contents. Unexpectedly, removal of both antioxidants resulted in suppression of chromatic aberration, but an increase in p-BQ content. Acidification by removal of Na₂SO₃ only was further effective for the suppression of chromatic aberration, but with a decrease of p-BQ content except in the initial period. Chromatic aberration was due to water soluble material and insoluble material both formed by co-existence of HQ and p-BQ at a molecular ratio of 5 : 3 to 1 : 1. ¹H-NMR analysis elucidated that the water soluble material was not HQ or p-BQ, and the insoluble material was a complex of HQ and p-BQ with non-covalent binding.

収録刊行物

• Ｂｉｏｌｏｇｉｃａｌ　＆　Ｐｈａｒｍａｃｅｕｔｉｃａｌ　Ｂｕｌｌｅｔｉｎ

  Ｂｉｏｌｏｇｉｃａｌ　＆　Ｐｈａｒｍａｃｅｕｔｉｃａｌ　Ｂｕｌｌｅｔｉｎ 25 (1), 92-96, 2002

  公益社団法人 日本薬学会

キーワード

• hydroquinone
• ointment
• pharmaceutical assessment
• clinical assessment

詳細情報

• CRID: 1390282679603995904
• NII論文ID: 110003638673
• NII書誌ID: AA10885497
• DOI: 10.1248/bpb.25.92
• COI: 1:CAS:528:DC%2BD38XhvVegsA%3D%3D
• ISSN: 13475215
• ISSN: 09186158
• NDL書誌ID: 6031412
• PubMed: 11824565
• Web Site: https://ndlsearch.ndl.go.jp/books/R000000004-I6031412
• Web Site: http://www.jstage.jst.go.jp/article/bpb/25/1/25_1_92/_pdf
• Web Site: https://search.jamas.or.jp/link/ui/2002142429
• 本文言語コード: en
• データソース種別:
  • JaLC
  • NDL
  • Crossref
  • PubMed
  • CiNii Articles
• 抄録ライセンスフラグ: 使用不可