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本品(多泼尼酯)是A、B、C、D环均为六元环的新型结构的皮质激素,是右旋高皮质甾类中第一个开发为外用的皮肤用药。合成 17β,17 aα-二羟基-D-高孕甾-1,4-二烯-3,20-二酮(Ⅰ)与2,2-二氯乙酰氯进行部分酰化作用,得化合物Ⅱ再与丁酐反应得到17 aα-丁酰氧基-11β-二氯乙酰氧基D-高孕甾-1,4-二烯-3,20-二酮(Ⅲ),Ⅲ与氢氧化铵溶液、甲醇进行部分水介,即可制得多泼尼酯[US 4202841]。药理经局部使用巴豆油、(口恶)唑酮和斑蝥素的三个经典动物皮肤炎症试验证明,多泼尼酯是一个很有效的抗炎皮质激素。在巴豆油引起小鼠炎症的夹钳试验中,本品局部抗炎作用比去羟米松强10倍,比泼尼龙强
This product (prednisone) is a new type of corticosteroid with A, B, C and D rings all six-membered rings. It is the first dermal drug developed for topical use in dextro-corticosteroids. Synthesis of 17β, 17α-dihydroxy-D-homoprosta-1,4-diene-3,20-dione (Ⅰ) with 2,2-dichloroacetyl chloride for partial acylation to give compound II With butyric anhydride to give 17 aα-butyryloxy-11β-dichloroacetoxy D-norpregna-1,4-diene-3,20-dione (III), Ⅲ and ammonium hydroxide solution, Methanol partially water-mediated, you can get more prednisone [US 4202841]. Pharmacology By the local use of croton oil, (oral evil) and ketanserin three classical animal skin inflammation test proved that prednisolone is a very effective anti-inflammatory cortical hormone. Croton oil-induced mouse inflammation in the clamp test, the local anti-inflammatory effect of this product 10 times stronger than dexamethasone, prednisolone stronger than