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绝经后女性的经皮激素治疗:代谢效应与药物递送技术综述

Transdermal hormone therapy in postmenopausal women: a review of metabolic effects and drug delivery technologies.

作者信息

Kopper Nathan W, Gudeman Jennifer, Thompson Daniel J

机构信息

KV Pharmaceutical, 2503 South Hanley Road, St. Louis, MO 63144, USA.

出版信息

Drug Des Devel Ther. 2009 Feb 6;2:193-202. doi: 10.2147/dddt.s4146.

Abstract

Vasomotor symptoms (VMS) associated with menopause can cause significant discomfort and decrease the quality of life for women in the peri-menopausal and post-menopausal stages of life. Hormone therapy (HT) is the mainstay of treatment for menopausal symptoms and is currently the only therapy proven effective for VMS. Numerous HT options are available to treat VMS, including estrogen-only and estrogen-progestogen combination products to meet the needs of both hysterectomized and nonhysterectomized women. In addition to selecting an appropriate estrogen or estrogen-progestogen combination, consideration should be given to the route of administration to best suit the needs of the patient. Delivery systems for hormone therapy include oral tablets, transdermal patches, transdermal topical (nonpatch) products, and intravaginal preparations. Oral is currently the most commonly utilized route of administration in the United States. However, evidence suggests that oral delivery may lead to some undesirable physiologic effects caused by significant gut and hepatic metabolism. Transdermal drug delivery may mitigate some of these effects by avoiding gut and hepatic first-pass metabolism. Advantages of transdermal delivery include the ability to administer unmetabolized estradiol directly to the blood stream, administration of lower doses compared to oral products, and minimal stimulation of hepatic protein production. Several estradiol transdermal delivery technologies are available, including various types of patches, topical gels, and a transdermal spray.

摘要

与更年期相关的血管舒缩症状(VMS)会给处于围绝经期和绝经后阶段的女性带来极大不适,并降低其生活质量。激素疗法(HT)是治疗更年期症状的主要方法,也是目前唯一被证明对VMS有效的疗法。有多种HT方案可用于治疗VMS,包括仅含雌激素以及雌激素 - 孕激素联合制剂,以满足子宫切除和未切除子宫女性的需求。除了选择合适的雌激素或雌激素 - 孕激素组合外,还应考虑给药途径以最适合患者的需求。激素疗法的给药系统包括口服片剂、透皮贴剂、透皮局部(非贴剂)产品和阴道内制剂。在美国,口服是目前最常用的给药途径。然而,有证据表明口服给药可能会因显著的肠道和肝脏代谢而导致一些不良生理效应。透皮给药可以通过避免肠道和肝脏的首过代谢来减轻其中一些效应。透皮给药的优点包括能够将未代谢的雌二醇直接输送到血流中,与口服产品相比给药剂量更低,以及对肝脏蛋白质生成的刺激最小。有几种雌二醇透皮给药技术可供选择,包括各种类型的贴剂、局部凝胶和透皮喷雾剂。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/2bd7/2761184/1e58555344b0/dddt-2-193f1.jpg

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