Cosolvent solubilization and formulation of an aqueous injection of ketoprofen

Department of Pharmaceutical Sciences, University of Saugar, India.
Pharmazie (Impact Factor: 1.05). 11/1996; 51(10):737-40.
Source: PubMed


Ketoprofen (1) an analgesic, antipyretic and anti-inflammatory agent, is practically insoluble in water. An increase in the aqueous solubility of 1 was attempted by various cosolvents. The solubility increased up to 8556 times (maximum) in case of ethanol while it was 33 times (minimum) in case of glycerol. Using selected cosolvents and hydrotropes, aqueous injections of 1 were formulated.

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    • "Utilization of this method in the formulation of dosage forms made of water insoluble drugs can also reduce the concentration of individual hydrotropic agents, in order to minimize the side effects (in place of using a large concentration of one hydrotrope, a blend of several hydrotropes can be employed in much smaller concentrations, reducing their individual toxicities). Hydrotropic solubilization technique for the formulation development of aqueous injection of various poorly water-soluble drugs has also been demonstrated (23-27). "
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    ABSTRACT: The increase in aqueous solubility of ketoprofen using hydrotropes and cosolvents in formulation, as well as stability studies of its aqueous injections have been reported earlier. These formulations were further evaluated in vitro (physical evaluation, haemolytic activity) and in vivo (pharmacokinetic studies). Some of the formulations have shown promising results.
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