DEVELOPMENT OF THE COMPOSITION OF NIMESULIDE GRANULES FOR ORAL SUSPENSION
DOI:
https://doi.org/10.11603/2312-0967.2022.3.13237Keywords:
granules, pharmaco-technological parameters, organoleptic characteristics, nimesulide, dissolution profilesAbstract
The aim of the work. Development of the composition of nimesulide granules for oral suspension, study the influence of the particle size of active ingredient as well as excipients on the critical quality attributes of the finished product.
Materials and Methods. The active substance nimesulide and the excipients from the groups of fillers, binders, pH stabilizers, flavor correctors, flavoring agents, and solubilizers were used. Preparation of granules was carried out by the wet granulation. Determination of pharmaco-technological parameters was performed by using of modern equipment. Organoleptic methods were used to analyze the characteristics of powder masses and the finished suspension. Quantitative content of the active substance was determined by the HPLC method.
Results and Discussion. According to the experimental results it was established that the micronized nimesulide substance (D90 < 30 μm) ensures compliance of Description test of prepared suspension, as well as compliance of the dissolution profile with the reference product. The best organoleptic characteristics of the suspension are obtained when using powdered sugar from 75.50 % to 90.00 % as a filler. pH value similar to the reference product is achieved by adding 0.95 % to 1.0 % of anhydrous citric acid. Cetomacrogol 1000 as a solubilizer in the amount 1 % ensures the dissolution profile and the quantitative content in accordance with the established requirements.
Conclusions. During development of composition of nimesulide granules for oral suspension the target profile was established, critical quality attributes were determined, a risks assessment of the formulation variability were performed. The optimal particle size of the active substance was selected, the influence of excipients on the pharmaco-technological and physico-chemical parameters was studied, and a scientifically based composition of the product, which corresponds to the target profile, was proposed.
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