Hydrotropic solubilization of nimesulide for parenteral administration.
Nimesulide is a non-steroidal anti-inflammatory drug (NSAID) that exhibits analgesic, antipyretic and anti-inflammatory activities. It is practically insoluble in water. The effect of various hydrotropes such as nicotinamide, sodium ascorbate, sodium benzoate, sodium salicylate and piperazine on the solubility of nimesulide was investigated. The solubility enhancement of nimesulide by the hydrotropes was observed in decreasing order as piperazine > sodium ascorbate > sodium salicylate > sodium benzoate > nicotinamide. In order to elucidate the probable mechanism of solubilization, various solution properties of hydrotropes such as viscosity, specific gravity, surface tension, refractive index, specific conductance of hydrotropic solutions were studied at 25 +/- 2 degrees C on the basis of earlier studies. The hydrotropic solubilization of nimesulide at lower hydrotrope concentration may be attributed to weak ionic interactions while that at higher hydrotrope concentration may be due to molecular aggregation. Parenteral formulations using piperazine as a hydrotrope were developed and studied for physical and chemical stability.
Agrawal
Shikha
S
Department of Pharmaceutical Sciences, Pharmaceutics Research laboratory, Dr. H.S. Gour University, Sagar 470 003, MP, India. shikhuagrawal@rediffmail.com
Pancholi
S S
SS
Jain
N K
NK
Agrawal
G P
GP
D007263:Infusions, Parenteral; D012995:Solubility / Q000187:drug effects; D013449:Sulfonamides / Q000008:administration & dosage* / Q000737:chemistry*; D013500:Surface Tension / Q000187:drug effects; D014783:Viscosity / Q000187:drug effects
D013449:Sulfonamides; C012655:nimesulide