Kim Eun-Young, Lee Sun Young, Jeon Ji-Young, Im Yong-Jin, Kim Yunjeong, Kim Hyun Il, Shin Kwang Seong, Park Su Jun, Seo Young-Hwan, Lee Jae-Yong, Park Jong Kwan, Chae Soo-Wan, Kim Min-Gul
Int J Clin Pharmacol Ther. 2014 Jun;52(6):437-45. doi: 10.5414/CP201995.
To compare the pharmacokinetic profiles and to assess bioequivalence of a newly developed orally soluble film formulation of sildenafil, taken without water, with those of a conventional formulation of sildenafil.
This study was conducted in a population of healthy subjects as an open-label, randomized sequence, two-period, two-formulation, single-dose, crossover design. The subjects were randomly assigned to 1 of 2 sequences of the two formulations: an orally soluble film (OSF) of 50 mg sildenafil as the test drug and a film-coated tablet (FCT) of 50 mg sildenafil as the reference drug. Blood samples were collected at intervals from 0 to 24 hours after administration. Plasma concentrations of sildenafil and its active metabolite N-desmethyl sildenafil were analyzed using a liquid chromatography/tandem mass spectrometry method.
48 healthy male subjects completed the study. The geometric mean (CV%) for Cmax in the OSF and FCT formulations were 267.21 (4.68%) ng/mL and 285.97 (5.32%) ng/mL, respectively. The geometric mean for AUClast in the OSF and FCT formulations were 664.48 (4.40%) ng x h/mL and 647.96 (4.63%) ng x h/mL, respectively. The geometric mean for AUCinf in the OSF and FCT formulations were 685.65 (4.37%) ng x h/mL and 666.28 (4.60%) ng x h/ mL, respectively. The 90% confidence intervals of the ratios of the geometric means of the Cmax, AUClast, and AUCinf were 0.844 - 1.030, 0.961 - 1.091, and 0.965 - 1.093, respectively.
The OSF sildenafil formulation exhibited no significant differences in its pharmacokinetics compared with those of the FCT formulation. Therefore this convenient OSF sildenafil formulation, which can be taken without the need for water or chewing, offers physicians a novel and attractive treatment option for men with erectile dysfunction. *These authors contributed equally to this work.
比较新开发的无水服用的西地那非口服可溶膜制剂与传统西地那非制剂的药代动力学特征，并评估其生物等效性。
本研究以健康受试者为研究对象，采用开放标签、随机序列、两周期、双制剂、单剂量、交叉设计。受试者被随机分配到两种制剂的2个序列之一：50mg西地那非口服可溶膜（OSF）作为受试药物，50mg西地那非薄膜包衣片（FCT）作为参比药物。给药后0至24小时期间间隔采集血样。采用液相色谱/串联质谱法分析西地那非及其活性代谢产物N-去甲基西地那非的血浆浓度。
48名健康男性受试者完成了本研究。OSF和FCT制剂中Cmax的几何均值（CV%）分别为267.21（4.68%）ng/mL和285.97（5.32%）ng/mL。OSF和FCT制剂中AUClast的几何均值分别为664.48（4.40%）ng·h/mL和647.96（4.63%）ng·h/mL。OSF和FCT制剂中AUCinf的几何均值分别为685.65（4.37%）ng·h/mL和666.28（4.60%）ng·h/mL。Cmax、AUClast和AUCinf几何均值比值的90%置信区间分别为0.844 - 1.030、0.961 - 1.091和0.965 - 1.093。
西地那非OSF制剂与FCT制剂相比，药代动力学无显著差异。因此，这种无需用水或咀嚼即可服用的便捷西地那非OSF制剂，为治疗勃起功能障碍的男性患者提供了一种新颖且有吸引力的治疗选择。*这些作者对本工作贡献相同。
