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: Aceclofenac 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 hydrotropes such as urea and sodium citrate and blends (urea + sodium citrate) on the solubility of aceclofenac was investigated. The enhancement in the solubility of aceclofenac was more than 5 and 25 folds in 30% sodium citrate solution and 30% urea solution, respectively, as compared to its solubility in distilled water. The enhancement in the solubility of aceclofenac in a mixed hydrotropic solution containing ≥ 20% urea and 10% sodium citrate solution was more than 250 folds (compared to its solubility in distilled water). This proved a synergistic enhancement in solubility of a poorly water- soluble drug due to mixed hydrotropy. Synergistic combination of hydrotropic agents can minimize the amount of hydrotropic agents employed, minimizing the chances of their toxicities. Aqueous injection of aceclofenac, using the mixed hydrotropic solubilization technique, was developed and by using the lyophilization method, the problem of inadequate stability of aceclofenac in aqueous solution was overcome. The developed formulation was studied for physical and chemical stability.
    Full-text · Article · Mar 2010 · Iranian journal of pharmaceutical research (IJPR)
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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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