单次口服或舌下给药后两种米索前列醇制剂的相对生物利用度研究。,Frontiers in Pharmacology

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单次口服或舌下给药后两种米索前列醇制剂的相对生物利用度研究。
Frontiers in Pharmacology ( IF 4.4 ) Pub Date : 2020-02-12 , DOI: 10.3389/fphar.2020.00050
Mahdi Amini ₁ , Margareta Reis ₂ , Dag Wide-Swensson ₁

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介绍米索前列醇（Cytotec）主要用于治疗胃溃疡。然而，今天它主要用于流产、治疗产后出血和引产。该片剂含有200微克米索前列醇，但用于引产的剂量要小得多（25-50微克），导致日常使用剂量不确定。目的评估和比较两种米索前列醇产品（Angusta 25 µg 和 Cytotec 200 µg 片剂）在每日临床环境中口服或舌下给予足月引产妇女的相对生物利用度。方法包括在头位怀有活的单胎胎儿且胎龄在 259 至 296 天之间的妇女。在 0、5、10、20、30、40、50、75、100、120、180 和 240 分钟收集血样。进行血清分析测定并计算药代动力学参数。患者被分配到三组之一。结果共纳入72例患者。没有发现人口统计学特征的显着差异。所有三组的 AUC、AUC (0-t) 和 Cmax 的比率相似，但 CI 值超出了要求的 80-125%。与口服途径相比，舌下给药产生了高出 20-30% 的生物利用度和高出 50% 的 Cmax。结. 造成这种情况的原因可能是进行研究的现实生活中的非标准化环境。舌下给药似乎比口服给药具有更高的生物利用度。需要更多的研究来确定平衡母婴安全性和有效性的最佳剂量方案。临床试验注册 www.ClinicalTrials.gov，标识符 NCT02516631。

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A Relative Bioavailability Study of Two Misoprostol Formulations Following a Single Oral or Sublingual Administration.

INTRODUCTION Misoprostol (Cytotec) was primarily made for treating gastric ulcers. However today it is mostly used for abortion, treating postpartum hemorrhage, and for induction of labor. The tablet contains 200 µg of misoprostol, yet the dosages used for induction of labor are much smaller (25-50 µg), leading to uncertainty of dosage in daily use. AIM To evaluate and compare the relative bioavailability of two misoprostol products (Angusta 25 µg and Cytotec 200 µg tablets) administered orally or sublingually given in a daily clinical setting to women admitted for induction of labor at term. METHODS Women carrying a live, singleton fetus in a cephalic position and with a gestational age between 259 and 296 days were included. Blood samples were collected at 0, 5, 10, 20, 30, 40, 50, 75, 100, 120, 180, and 240 minutes. A serum analytical assay was performed and pharmacokinetic parameters were calculated. Patients were assigned to one of three groups. RESULTS A total of 72 patients were included. No significant differences demographic characteristics were found. The ratios for AUC, AUC (0-t), and Cmax were similar in all three groups, but CI-values were outside the required 80-125%. Sublingual administration yielded a 20-30% higher bioavailability and a 50% higher Cmax than compared to the oral route. CONCLUSION The relative bioavailability between Angusta and Cytotec could not be confirmed as being equal at the 25 µg or 50 µg level because the 90% CI-values when comparing the ratios for AUC, AUC(0-t), and Cmax were wider than accepted. The reason for this could be the real-life, non-standardized circumstances in which the study was conducted. Sublingual administration seems to have higher bioavailability than oral administration. More studies are needed to ascertain an optimal dosage regime balancing both safety and efficacy for mother and child. CLINICAL TRIAL REGISTRATION www.ClinicalTrials.gov, identifier NCT02516631.

更新日期：2020-02-12

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