Etienne M C, Milano G, René N, Benedetti M S, Efthymiopoulos C, Vo Van M L, Hurteloup P, Montcuquet P, Frenay M, Namer M
Centre Antoine Lacassagne, Nice, France.
J Pharm Sci. 1991 Dec;80(12):1130-2. doi: 10.1002/jps.2600801208.
Medroxyprogesterone acetate (MPA) is widely used in the hormonal therapy of breast cancer. So far, oral formulations of MPA commercially available present a very low bioavailability, with a less than 10% extent of oral absorption. A new oral preparation of MPA has been recently developed. Based on a pilot study, an open, randomized, crossover trial has been performed on 22 breast and endometrial cancer patients to evaluate the relative bioavailability of this new oral formulation (200-mg sachet, twice daily) as compared with a standard formulation (Farlutal, 500-mg tablet, twice daily). The bioavailability evaluation was mainly based on the area under the curve measured between two administrations at steady state, after 15 days of continuous therapy. Wide interpatient variability of MPA plasma levels after oral MPA administration was confirmed. The MPA plasma levels were higher in patients treated with the new formulation than in patients treated with Farlutal. The relative bioavailability of the new preparation was 3.5 times higher than that of the standard. This new formulation represents a great improvement in the extent of oral absorption of MPA and could lead to better management of hormone-responsive tumors by hormonal therapy.
醋酸甲羟孕酮（MPA）广泛用于乳腺癌的激素治疗。到目前为止，市售的MPA口服制剂生物利用度非常低，口服吸收程度不到10%。最近开发了一种新的MPA口服制剂。基于一项初步研究，对22名乳腺癌和子宫内膜癌患者进行了一项开放、随机、交叉试验，以评估这种新口服制剂（200毫克小袋，每日两次）与标准制剂（法禄达，500毫克片剂，每日两次）相比的相对生物利用度。生物利用度评估主要基于连续治疗15天后在稳态下两次给药之间测量的曲线下面积。口服MPA后，MPA血浆水平在患者间存在很大差异得到了证实。新制剂治疗的患者MPA血浆水平高于法禄达治疗的患者。新制剂的相对生物利用度比标准制剂高3.5倍。这种新制剂在MPA口服吸收程度方面有很大改进，可能会通过激素治疗更好地管理激素反应性肿瘤。
