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标题：Pharmaceutical and Clinical Assessment of Hydroquinone Ointment Prepared by Extemporaneous Nonsterile Compounding
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作者：Teruhisa Matsubayashi ; Toshiyuki Sakaeda ; Tomoko Kita 等
期刊名称：Biological and Pharmaceutical Bulletin
印刷版ISSN：0918-6158
电子版ISSN：1347-5215
出版年度：2002
卷号：25
期号：1
页码：92-96
DOI：10.1248/bpb.25.92
出版社：The Pharmaceutical Society of Japan
摘要：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.
关键词：hydroquinone;ointment;pharmaceutical assessment;clinical assessment