双氯芬酸性质、用途与生产工艺
双氯芬酸商品名有扶他林、待克菲那、服他灵等，是一种衍生于苯乙酸类的非甾体抗炎药（NSAID），主要用于治疗骨关节炎、类风湿关节炎、多发性肌炎、皮肌炎、脊柱关节病、强直性脊柱炎、痛风，以及偏头痛、牙痛、胆结石和肾结石等需要急性止痛的情况。药用双氯芬酸常使用钠盐或钾盐，在中国主要以钠盐为主，即双氯芬酸钠，各个国家的情况各有不同。
双氯芬酸的作用机理为抑制环氧化酶活性，从而阻断花生四烯酸向前列腺素的转化生成，因前列腺素为引起疼痛、发烧及发炎等之现象的主要因子。
双氯芬酸为白色结晶性粉末，无臭，易溶于丙酮，溶于甲，乙醇，微溶于水。
双氯芬酸具有显著的抗风湿，消炎，止痛和解热作用，其抗炎作用比阿司匹林强26—50倍，能很好的解除关节疼能，消肿，改善其活动，同时具有良好的耐受性。
Diclofenac acid是一种非类固醇的消炎药，具有止痛、消炎和退热活性，在治疗多种急性和慢性疼痛、炎症反应中有效。它能抑制cyclooxygenase-1 (COX-1)和cyclooxygenase-2 (COX-2)，具有相近的效力。
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Human COX-2
1.3 nM (IC
50
, in CHO cells)
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Human COX-1
4 nM (IC
50
, in CHO cells)
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Ovine COX-2
0.84 μM (IC
50
)
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Ovine COX-1
5.1 μM (IC
50
)
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Diclofenac effectively blocks COX-1 mediated prostanoid production from U937 cell microsomes, with an IC
50
of 7±3 nM.
Diclofenac (1-60 μM; 1 day) induces neural stem cells (NSCs)death in a concentration-dependent manner.
Diclofenac (10-60 μM; 6 hours) increases the expression of cleaved (activated) caspase-3.
Cell Viability Assay
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Cell Line:
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Neural stem cells (NSCs)
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Concentration:
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1, 3, 10, 30, 60 μM
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Incubation Time:
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1 day
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Result:
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Induction of cell death was concentration-dependent and the effect was not saturated at a concentration of up to 60 μM.
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Western Blot Analysis
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Cell Line:
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Neural stem cells (NSCs)
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Concentration:
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10, 30 or 60 μM
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Incubation Time:
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6 hours
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Result:
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The activation of caspase-3 was increased in a concentration-dependent manner.
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Diclofenac (3 mg/kg, b.i.d., for 5 days) significantly increases faecal
51
Cr excretion in rats, and such effect is also observed in squirrel monkeys after administrated of 1 mg/kg twice daily for 4 days.
Diclofenac (10 mg/kg; administered via oral route just prior to induction of inflammation) shows in vivo anti-inflammatory activity in Wistar rats.
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Animal Model:
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Male Sprague-Dawley rats (150±200 g)
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Dosage:
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3 mg/kg
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Administration:
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Oral administration, b.i.d., for 5 days
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Result:
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Resulted in a significant increase in faecal
51
Cr excretion.
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Animal Model:
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Wistar rats (150-175 g) bearing Formalin-induced rat foot paw edema model
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Dosage:
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10 mg/kg
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Administration:
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Administered via oral route just prior to induction of inflammation
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Result:
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Showed in vivo anti-inflammatory activity (% edema inhibition=29.2, 1 h; 22.2, 3 h; 20, 6 h).
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用途
用作消炎镇痛药
双氯芬酸
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