首页> 美国卫生研究院文献>Journal of Pain Research >Comparative evaluation of the pain-relieving properties of a lecithinized formulation of curcumin (Meriva®) nimesulide and acetaminophen
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Comparative evaluation of the pain-relieving properties of a lecithinized formulation of curcumin (Meriva®) nimesulide and acetaminophen

机译:姜黄素尼美舒利和对乙酰氨基酚的卵磷脂化制剂的止痛特性的比较评估

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摘要

In addition to its anti-inflammatory activity, Meriva®, a proprietary lecithin formulation of curcumin, has been anecdotally reported to decrease acute pain in patients with various chronic diseases. Given that curcumin can desensitize transient receptor potential A1, a nociceptor seemingly also mediating the analgesic effect of acetaminophen, as well as inhibiting and downregulating the expression of cyclo-oxygenase 2, the selective target of nimesulide, a nonsteroidal anti-inflammatory agent, we carried out a pilot comparative study of the acute pain-relieving properties of these three agents. At a dose of 2 g (corresponding to 400 mg of curcumin), Meriva showed clear analgesic activity, comparable with that of a standard dose (1 g) of acetaminophen, but lower than that of a therapeutic (100 mg) dose of nimesulide. The analgesic activity of lower (1.5 g) doses of Meriva was less satisfactory, and the onset of activity was longer than that of nimesulide for both doses. On the other hand, gastric tolerability was significantly better than that of nimesulide and comparable with that of acetaminophen. Taken together, our results show that the preclinical analgesic properties of curcumin have clinical relevance, at least at a dose of 2 g as the Meriva formulation. While this dose is significantly higher than that used to relieve chronic inflammatory conditions (1–1.2 g/day), its pain-relieving activity could benefit from the general downregulation of the inflammatory response induced by curcumin, considering that the transient receptor potential channel-mediated mechanisms of analgesia are magnified by attenuation of inflammation. In patients on treatment with Meriva, this would also translate into better control of acute pain, providing a rationale for the analgesic properties associated with this curcumin formulation.
机译:除抗炎作用外,据报道,姜黄素的专有卵磷脂制剂Meriva ®还可以减轻各种慢性疾病患者的急性疼痛。鉴于姜黄素可以使瞬时受体电位A1脱敏,因此伤害感受器似乎还介导对乙酰氨基酚的镇痛作用,以及抑制和下调非甾体类抗炎药尼美舒利的选择性靶标环氧化酶2的表达。进行了这三种药物的急性缓解疼痛性质的初步比较研究。在2 g(相当于400 mg姜黄素)的剂量下,Meriva表现出明显的止痛活性,与对乙酰氨基酚的标准剂量(1 g)相当,但低于治疗剂量(100 mg)的尼美舒利。较低剂量(1.5 g)的Meriva的镇痛活性较差,两种剂量的活性均比尼美舒利的镇痛作用长。另一方面,胃耐受性明显优于尼美舒利,与对乙酰氨基酚相当。两者合计,我们的结果表明姜黄素的临床前镇痛特性具有临床意义,至少以Meriva制剂的2 g剂量存在。虽然此剂量明显高于缓解慢性炎症的剂量(1-1.2 g /天),但考虑到瞬时受体电位通道可以缓解姜黄素引起的炎症反应,因此其缓解疼痛的作用可能受益于其普遍下调。炎症减轻可放大介导的镇痛作用。在接受Meriva治疗的患者中,这也将转化为更好地控制急性疼痛,从而为与该姜黄素制剂相关的镇痛特性提供了理论依据。

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