Petersen M C, Ashley J J, McBride W G, Nation R L
Br J Clin Pharmacol. 1984 Sep;18(3):383-92. doi: 10.1111/j.1365-2125.1984.tb02480.x.
When betamethasone phosphate equivalent to 8 mg betamethasone was administered intramuscularly in solution (Celestone Injection) to pregnant women, a large proportion of this ester was absorbed unchanged. Bioavailability of betamethasone from the phosphate ester was as high as after intravenous injection. When pregnant patients received the equivalent of either 6 or 12 mg betamethasone in a formulation containing 3.1 mg/ml betamethasone acetate suspended in a solution of 4 mg/ml betamethasone phosphate (Celestone Chronodose), much of the phosphate ester was absorbed intact but betamethasone acetate was not detected in plasma. Availability of betamethasone from Celestone Chronodose was much lower than from Celestone Injection. After administration of either formulation, maternal plasma cortisol concentrations fell towards a basal level but were rising again within 2 to 3 days of the last dose. We conclude that Celestone Chronodose does not provide prolonged release of betamethasone and offers no advantage over Celestone Injection.
当向孕妇肌内注射相当于8毫克倍他米松的磷酸倍他米松溶液(Celestone注射剂)时,很大一部分这种酯未发生变化就被吸收了。磷酸酯中倍他米松的生物利用度与静脉注射后一样高。当孕妇接受了含有3.1毫克/毫升醋酸倍他米松悬浮于4毫克/毫升磷酸倍他米松溶液中的制剂(Celestone Chronodose),相当于6毫克或12毫克倍他米松时,大部分磷酸酯完整地被吸收,但血浆中未检测到醋酸倍他米松。Celestone Chronodose中倍他米松的可用性远低于Celestone注射剂。两种制剂给药后,母体血浆皮质醇浓度降至基础水平,但在最后一剂后的2至3天内又开始上升。我们得出结论,Celestone Chronodose不能提供倍他米松的缓释,与Celestone注射剂相比没有优势。