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Nimesulide showed efficacy in the treatment of pain and inflammation associated with rheumatoid arthritis and osteoarthritis. Nimesulide 200 mg/day was generally more effective than the usual therapeutic doses of naproxen, ibuprofen, ketoprofen mefenamic acid and suprofen in reducing clinical sysmtoms associated with variety of conditions including respiratory tract infections, ear, nose and throat disorders, dysmenorrhoea, dental surgery, urogentital tract disorders and musculoskeletal injuries. Nimesulide is conventionally administered in tablet form of 100 mg/day to 400 (mostly 200 mg/day) for 5 to 21 (mean 12 days). Conventional Nimesulide therapy starts with 100 mg adminstrered twice daily. The dosage is gradually increased to 100 mg administratered four times a day until optimum response is obtained. The oral and rectal dosages of nimesulide in adults are 100 and 200 mg twice daily respectively. In children, nimesulide dosage is commonly 5 mg/kg/day divided in 2 or 3 daily doses administered in the form of suspension, granules or suppositories. Conventional Nimesulide tablets are administered two or four times daily. Such a frequent drug adminstration may reduce patient compliance, there is possiblity of exhibiting toxic effects accompained by side effect. However, Nimesulide is also required to be given in higher doses of 400 mg and 600 mg / day in post operative pain providing moderate relief to the pain. Nimesulide also is topically applied at the affected area for releving post operative pain (US Appl. 5998480). Moreover, transdermal drug delivery system (US Appl. 6024,976), formulations in form of thixotropic gel (US Appl. 5858330) and composition containing nimesulide and piperine (US Appl. 6017932) to enhance therapeutic efficacy have been disclosed in the references stated hereinabove. Earlier studies reported that in a double-blind study in the patient for saphenectomy or inguinal hernioplasty were randomly assigned to the treatment with nimesulide (200mg 3 times daily) administered rectally. This therapy resulted in significantly less pain, oedema and hyperaemia and resolution of mild fever and no adverse reaction was attributated by Ramella, G. et. al. (Drugs 46 (Suppl. 1), 159-161, 1993). In Coscarelli, S. et.al. (Drugs 46, (suppl. 1) 174-176, 1993), it is disclosed that Nimesulide (200 mg twice daily) when admistered rectally gave relief in the pain associated with postoperative inflammatory complications of ear, nose and throat surgery. Moreover Pierleoni, P. et. al. (Drugs 46, (suppl. 1) 168-170, 1993) also disclosed that nimesulide gave relief when adminstered at the same doses of 200 mg twice daily in dental surgery. Toscani, F. et. al. (Drugs 46 (Suppl. 1) 156-158, 1993) reported analgesic efficacy of nimesulide with advanced cancer who needed to be treated with NSAID drug according to the first step of the pharmacological analgesic scale of the WHO. Patient receiving 200 mg twice dalily administered as granular formulation. This therapy resulted in similarly reduced pain with naproxen 500 mg twice daily. Nimesulide is frequently adminstered, such frequent drug administration may reduce patient compliance resulting thereby every possiblity of exhibiting toxic effect accompanied by side effect. To attain and maintain a blood level which exceeds the minimum effective level required for response, but does not exceed the minimum toxic level, the dose of 200 mg in controlled release formulation is convenient. In the cases where special indications need i.e in saphenectomy or inguinal hernioplasty the 400 mg tablet with controled release profile can be convenient for once a day administration. |
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