Nimulid-MD™

Formulations Available Technology Mechanism Of Action
Indication Development Stage Clinical /Bioequivalence studies
Patent Status   References

 

  Name of the active Pharmaceutical Ingredient: Nimesulide 

  Formulations Available

  1. Nimulid-MD
    (Nimesulide flavoured dispersible tablet) Strength Available - 100 mg
  2. Nimulid-MD Kid Tablet
    (Nimesulide flavoured dispersible tablet) Strength Available - 50 mg

  Technology

Nimulid - MD is a flavoured dispersible tablet with fast mouth dissolving characteristics thereby providing immediate relief. Nimesulide is micronized (particle size less than 5 u) in Nimulid -MD, dispersed in a highly soluble matrix with a unique combination of rapidly soluble polyols. This matrix, as also the tablet ingredients like flavours, stimulate saliva secretion. Further, the composition contains drug in taste masked form, along with sweeteners which are modified with special polymers to have mucoadhesive properties. These sweeteners provide long lasting sweetness in mouth, thus preventing the bitter after - taste of Nimesulide.

  Mechanism Of Action

Nimesulide appears to exert its therapeutic effects through a variety of mechanisms viz :Selective cyclooxygenase 2 inhibition, Inhibition of generation of superoxide anions from stimulated polymorphonuclear leucocytes, Inhibition of platelet activating factor synthesis, Prevention of Bradykinin/Cytokine induced hyperalgesia of nerves (Inhibiting release of TNF-a ), Scavenging of hypochlorous acid, Blocking of histamine release. Prevention of cartilage damage by inhibition of metalloprotease synthesis. Phosphodiesterase type IV inhibition.

  Indication

Clinical studies have established the analgesic, anti-inflammatory and antipyretic effectiveness of orally (mostly 200 mg/day) administered Nimesulide in the treatment of a variety of painful inflammatory conditions, including those associated with osteoarthritis, rheumatoid arthritis, oncology, post operative trauma, sports injuries, ear, nose and throat disorders, dental surgery, bursitis/tendinitis, thrombophlebitis, upper airways inflammation and gynaecological disorders. Nimesulide therapy was characterised by a rapid onset of analgesia and symptomatic relief in pain in clinical trials where a significant difference in clinical efficacy between active treatments was observed. Also Nimesulide has shown to be well tolerated even by aspirin sensitive asthmatic patients.

  Development Stage: Phase IV

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  Clinical /Bioequivalence studies

  1. A pharmacodynamic evaluation of analgesic activity of single dose treatment of nimesulide 100 mg in six healthy volunteers was done at MGM Medical College, Mumbai 1. Nimulid - MD or Nimulid 100 mg was administered in a two way crossover design and ischemic pain test were repeated at regular intervals till 8 hours after the administration of the drug. Maximum analgesic score (E-max), time for maximum effect (T-emax) and area under the clock time versus time to tolerance (AUC) was calculated for both the groups (Table 1).

Table 1: Mean Pharmacodynamic Parameters

Parameters Nimulid-MD 100 mg Nimulid -100 mg
Emax (sees) 44.33 ± 12.84 35.66 ± 11.63
T-emax (hours) 02.41 ± 00.49 02.58 ± 00.66
AUC 0-8 hr (sec x hours) 150.37 ± 51.83 136.45 ± 35.48
  1. A comparative bioavailability study was conducted at PGIMER, Chandigarh2 on twelve healthy male volunteers who were administered either 100 mg of Nimulid - MD (N1;Panacea Biotec Ltd.) or Nise(N2;Dr. Reddy's Labs) in a two-way, crossover design. The various pharmacokinetic parameters for both the drugs were calculated and the results reflected significantly greater rate and extent of N^s as compared to that of N^ since Cmax and AUCo-a were significantly increased with N1 as compared to N2, (Fig. 1).


  1. An open labeled non-comparative trial was conducted to evaluate the efficacy and safety of mouth dissolving formulation of nimesulide in acute low back pain at MAMC, New Delhi3. Fifty-six patients with acute low back pain (LBP) were enrolled and were given nimesulide mouth dissolving tablets (Nimulid MD-100mg) in morning and evening for 14 days. Pain intensity was measured on visual analogue scale at various points of time on day 1, then on day 4, day 8 and day 15. Forty-nine patients completed the trial and various parameters of pain were reduced significantly as measured on VAS scoring (Fig. 2). Adverse effects were seen in 8.16% of patients in the form of epigastric pain, nausea and heartburn.

A single blind comparative evaluation of efficacy and safety of Nimulid - MD (Nimesulide Mouth Dissolving Tablets - 100mg) with Piroxicam and Diclofenac was done in patients of acute low back pain at SMS Medical college and attached hospitals, Jaipur4. Nimulid - MD showed a rapid relief from pain as seen with reduction in VAS score in all the parameters which were measured. The pain reduction was significant as compared to piroxicam and diclofenac. Nimulid-MD was well tolerated with no side effects and good acceptability by the patients.

WHO-GMP Certification -Available 

  Patent Status - Patent in pipeline

  References

  1. Kulkarni RD et al. A pharmacodynamic evaluation of analgesic activity of single dose treatment of nimesulide 100 mg in six healthy volunteers. Data on file.
  2. Bhargava VK and Garg SK. A randomized, two-treatment, two-sequence, single dose, crossover bio-availability study on Nimesulide mouth dissolving tablets 100 mg (Nimulid MD 100mg) comparing with conventional Nimesulide formulation (Nise 100 mg) in 12 healthy, adult, male human subjects under fasting conditions. The Indian Practitioner, 2001:54(10)703-706
  3. Dhaon BK et al. Evaluation of efficacy and safety of Nimulid - MD (Nimesulide Mouth Dissolving Tablets-100 mg) in patients of acute low back pain. The Indian Practitioner 2001:54(6):417-422.
  4. Gupta SP et al. Single blind comparative evaluation of efficacy and safety of Nimulid -MD (Nimesulide Mouth Dissolving Tablets-100 mg) Vs piroxicam Vs diclofenac tablets in patients of acute low back pain. Data on file. 

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