Sudoxicam 是一种可逆的口服活性的COX拮抗剂，是烯醇-羧酰胺类的非甾体抗炎药 (NSAID)。Sudoxicam 具有有效的抗炎，抗浮肿和退热作用。
| 生物活性 | Sudoxicam is a reversible and orally activeCOXantagonist and a non-steroidal anti-inflammatory drug (NSAID) from the enol-carboxamide class. Sudoxicam has potent anti-inflammatory, anti-edema and antipyretic activity[1][2][3]. |
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体外研究
(In Vitro) | Sudoxicam demonstrates NADPH-dependent covalent binding to human liver microsomes. With addition of glutathione (GSH) in microsomal incubations, about half of the covalent incorporation of Sudoxicam is blocked by addition of GSH[1].
Metabolite identification studies on [14C]-Sudoxicam in NADPH-supplemented human liver microsomes indicated that the primary route of metabolism involved a P450-mediated thiazole ring scission to the corresponding acylthiourea metabolite (S3), a well-established pro-toxin[1].
In vitro, Sudoxicam underwent the oxidative thiazole-open biotransformation, resulting in the formation of an acylthiourea and the subsequent hydroxylated metabolite[3].
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体内研究
(In Vivo) | Sudoxicam (1-10 mg/kg; oral administration; daily; for 7 days; rats) treatment effective reduces plasma inflammation units, reduces the swelling of inflamed hind-paws and restores toward normal the daily gain in body weight[2].
In the intact rat, Sudoxicam significantly inhibited edema formation at doses as low as 0.1 mg/kg, p.o[2].
Sudoxicam inhibits the erythema caused by ultraviolet irradiation in the guinea pig.
Sudoxicam (3.3 mg/kg, i.p.) is capable of counteracting the pyrexia induced by the intraperitoneal injection of typhoid/paratyphoid vaccine in rats, maintaining body temperature about that of uninjected control rats[2].
The plasma half-life of Sudoxicam ranged between 8 hours (monkey), 13 hours (rat), and 60 hours (dog)[2].
| Animal Model: | Rats injected with ,i>M. butyrieum[2] | | Dosage: | 1 mg/kg, 3.3 mg/kg, 10 mg/kg | | Administration: | Oral administration; daily; for 7 days | | Result: | Were both effective in reducing plasma inflammation units, in reducing the swelling of inflamed hind-paws. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : 83.33 mg/mL(247.00 mM;ultrasonic and warming and heat to 80℃) 配制储备液 | 1 mM | 2.9641 mL | 14.8205 mL | 29.6410 mL | | 5 mM | 0.5928 mL | 2.9641 mL | 5.9282 mL | | 10 mM | 0.2964 mL | 1.4821 mL | 2.9641 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 |
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