伍思怡, 李佳奇, 董健, 叶军, 宁美英. 结合雌激素的剂型发展及临床应用现状J. 药学学报, 2025, 60(4): 949-958. DOI: 10.16438/j.0513-4870.2025-0015
引用本文: 伍思怡, 李佳奇, 董健, 叶军, 宁美英. 结合雌激素的剂型发展及临床应用现状J. 药学学报, 2025, 60(4): 949-958. DOI: 10.16438/j.0513-4870.2025-0015
WU Si-yi, LI Jia-qi, DONG Jian, YE Jun, NING Mei-ying. Current status of dosage forms and clinical use of conjugated estrogensJ. Acta Pharmaceutica Sinica, 2025, 60(4): 949-958. DOI: 10.16438/j.0513-4870.2025-0015
Citation: WU Si-yi, LI Jia-qi, DONG Jian, YE Jun, NING Mei-ying. Current status of dosage forms and clinical use of conjugated estrogensJ. Acta Pharmaceutica Sinica, 2025, 60(4): 949-958. DOI: 10.16438/j.0513-4870.2025-0015

结合雌激素的剂型发展及临床应用现状

Current status of dosage forms and clinical use of conjugated estrogens

  • 摘要: 结合雌激素(conjugated estrogens, CE) 广泛应用于绝经激素治疗, 能有效缓解绝经及其相关症状(如血管舒缩症状、神经精神症状、泌尿生殖道萎缩症状等), 且是预防绝经后骨质疏松症的有效方法。本文综述了CE的不同剂型(片剂、乳膏和注射剂) 的特点、药理作用及其在临床中的应用。CE片剂通过全身治疗作用有效调节体温中枢, 减轻潮热和盗汗, 促进骨形成, 增加骨密度; CE乳膏用于局部治疗, 改善更年期泌尿生殖系统综合征; CE注射剂用于治疗无器官病理的因激素失衡而引起的异常子宫出血, 但仅适合短期使用, 可以快速而暂时地增加雌激素水平。此外, CE在代谢方面具有重要作用, 能够提高胰岛素的清除率和敏感性, 并对神经系统和心血管系统有潜在的保护作用, 显示出广泛的治疗潜力。本文通过探讨CE的制剂和应用, 为药物剂型的设计和开发提供新思路。

     

    Abstract: Conjugated estrogens (CE) are widely used in menopausal hormone therapy (MHT) for the relief of menopause-related symptoms (e.g., vasodilatory symptoms, neuropsychiatric symptoms, genitourinary atrophy symptoms, etc.) and the prevention of postmenopausal osteoporosis. This article reviews the characteristics, pharmacological effects, and practical applications of different dosage forms of CE (tablets, creams, and injections) in clinical practice. It has been shown that tablet CE effectively regulates the body's temperature center through systemic treatment, reduces hot flashes and night sweats, promotes bone formation, and increases bone density. Cream CE is used for local treatment to improve the genitourinary syndrome of menopause (GSM). Injectable CE is used for the treatment of abnormal uterine bleeding caused by hormonal imbalance without organ pathology. CE administered intravenously is indicated only for short-term use to rapidly and temporarily increase estrogen levels. Additionally, CE plays an important role in metabolism by improving insulin clearance and sensitivity and potentially protecting the nervous and cardiovascular systems, demonstrating a wide range of therapeutic potential. This paper provides new ideas for the design and development of drug dosage forms by exploring the formulation and application of CE.

     

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