Phase 1 Clinical Trial Center, Deyang People's Hospital, Deyang, Sichuan, People's Republic of China.
Research Center for Clinical Pharmacy, State Key Laboratory for Diagnosis and Treatment of Infectious Diseases, The First Affiliated Hospital, Zhejiang University School of Medicine, Hangzhou, Zhejiang, People's Republic of China.
Drug Des Devel Ther. 2024 Jul 10;18:2891-2904. doi: 10.2147/DDDT.S460681. eCollection 2024.
Estradiol valerate (Progynova) is used as hormone therapy to supplement estrogen deficiency. This study aimed to assess the bioequivalence of an estradiol valerate tablet and its generic form, under fasting and fed conditions.
A randomized, open-label, single-dose, 2-period crossover study was conducted on healthy postmenopausal Chinese female volunteers under fasting and fed conditions. For each period, the subjects received either a 1 mg tablet of estradiol valerate or its generic. Blood samples were collected before dosing and up to 72 hours after administration. Plasma levels of total estrone, estradiol, and unconjugated estrone were quantified using a validated liquid chromatography-tandem mass spectrometry method.
A total of 54 volunteers were enrolled in this study. The primary pharmacokinetic parameters, including C, AUC, and AUC, were similar for the two drugs under both fasting and fed conditions, with 90% confidence intervals for the geometric mean ratios of these parameters, all meeting the bioequivalence criterion of 80-125%. A total of 48 adverse events (AEs) were reported in the fed study compared with 24 AEs in the fasting study.
Estradiol valerate and its generic form were bioequivalent and well tolerated under both fasting and fed conditions.
戊酸雌二醇（普罗雌烯）用作激素替代疗法，以补充雌激素缺乏。本研究旨在评估戊酸雌二醇片及其仿制药在空腹和进食条件下的生物等效性。
在空腹和进食条件下，对健康的绝经后中国女性志愿者进行了一项随机、开放标签、单剂量、2 期交叉研究。每个时期，受试者分别接受 1 毫克戊酸雌二醇片或其仿制药。在给药前和给药后 72 小时内采集血样。使用经过验证的液相色谱-串联质谱法定量测定总雌酮、雌二醇和未结合雌酮的血浆水平。
共有 54 名志愿者参加了这项研究。两种药物在空腹和进食条件下的主要药代动力学参数（包括 C、AUC 和 AUC）相似，这些参数的几何均数比值的 90%置信区间均符合 80-125%的生物等效性标准。与空腹研究相比，进食研究中总共报告了 48 例不良事件（AE），而空腹研究中报告了 24 例 AE。
戊酸雌二醇及其仿制药在空腹和进食条件下均具有生物等效性和良好的耐受性。
