Chronic arthritis Pain symptoms Oral Hypoglycemic Agents Rheumatic pain
1, Product title:Diclofenac sodium
2, Product parameter table:
|appearance||White crystalline powder|
|Use of the product||Anti-inflammatory analgesic||content||99%|
|Molecular formula||C14H10Cl2NNaO2||Shelf Life||2 Years|
|CAS||15307-79-6||Storage||Cool Dry Place|
3, Product Description:
The analgesic, anti-inflammatory and antipyretic effects of indomethacin are 2 ~ 2.5 times stronger than indomethacin and 26 ~ 50 times stronger than aspirin. The main mechanism of action is inhibition of prostaglandin synthase, which hinders the biosynthesis of prostaglandin. Characterized by strong efficacy, less adverse reactions, small dose, small individual differences, small individual differences.
4, Use of the product:
It is used to relieve the symptoms of acute or persistent swelling and pain of various chronic arthritis, rheumatic pain of various soft tissues, and primary dysmenorrhea, toothache, headache, etc.
5. Bioactivity of diclofenac sodium:
Diclofenac sodium is an effective COX inhibitor. The IC50 of COX-1 and COX-2 in CHO cells is 4 nM and 1.3 nM, respectively. Diclofenac effectively blocks COX-1-mediated prostaglandin production in UX37 cell microsomes with IC50 of 7±3 nM . Sodium diclofenac exhibited inhibition of COX-1 and COX-2 enzymes with IC50 of 5.1 and 0.84μM, respectively .
In vivo diclofenac (3mg/kg, bid, 5 days) significantly increased fecal excretion of 51Cr in rats and was also observed in squirrel monkeys after application of 1mg/kg twice daily for 4 days . Diclofenac (10mg/kg) showed anti-inflammatory activity in mice . Diclofenac (10 mg/kg) can reduce oxidized low density lipoprotein (ox-LDL), but has no effect on catalase and glutathione peroxidase kinetic parameters by intramuscular injection in rats .
Animal experimental rats  Male Sprague-Dawley rats (150±200g) were orally given diclofenac once (acute administration) or twice daily for 5 days (chronic administration). Plasma samples were obtained 1 hour after morning dose on day 4 to measure diclofenac concentration. Immediately after the final dose on day 5, 0.5mL 51Cr-labeled erythrocytes from donor rats were injected via the tail vein and incubated with sodium 51 chromate. Rats were placed alone in metabolic cages and given free food and water. 48 hours after fecal collection, 51Cr fecal excretion was calculated as a percentage of the total injection dose (20mCi per animal) . Squirrel monkey (Saimiri Sciureus; 0.8±1.4 kg) diclofenac was taken orally twice a day for 1±5 days. One hour after the last dose, sterile saline solution of 51CrCl3 (1mL/kg, 4±5mCi per animal) was injected through the saphenous vein, and plasma samples were obtained for measurement of diclofenac concentration. The monkeys were then placed in separate metabolic cages. After 24 hours of fecal collection, 51Cr fecal excretion was calculated as a percentage of the total injection dose .
. Riendeau D, et al. Biochemical and pharmacological profile of a tetrasubstituted furanone as a highly selective COX-2 inhibitor. Br J Pharmacol. 1997 May; 121 (1) : 105-17.
. Labib MB, et al. Design, synthesis of novel isoindoline hybrids as COX-2 inhibitors: Anti-inflammatory, analgesic activities and docking study. Bioorg Chem. 2018 Oct; 80:70-80.
. Curcelli EC, et al. Beneficial effects of diclofenac therapy on serum lipids, oxidized low-density lipoprotein and antioxidant defenses in rats. Life Sci. 2008 Apr 9; 82 (15 to 16) : 892-8.
6. Pictures of the product: