Abstract
Objective: Mefenamic acid (MFA) is an NSAID that exhibits anti-inflammatory analgesic and antipyretic activity. Peak plasma levels are attained in 2-4 h and the elimination half-life approximates 2 h, repetitive administration of tablets for 3-5 times a day is desired. It is supplied only in the form of tablets for oral administration. In acute conditions drug administered parenterally could give rapid relief from severe symptoms like pain. Thus, formulation of injectable formulation of MFA could be better alternative compared to conventional tablet dosage form. The low aqueous solubility of MFA precludes its use in parenteral formulation development.
 Methods: In this work attempt were made to enhance the aqueous solubility of mefenamic acid using mixed solvency technique. For that different hydrotropic agents such as Urea, Sodium acetate, sodium benzoate, sodium citrate and their blends were evaluated. Optimal concentration of hydrotropic agent in blend was determined using D-optimal mixture experimental design. The optimized bled was used to develop the aqueous injection of mefenamic acid. The developed injection was subjected for various quality control tests and stability of developed formulation was also evaluated.
 Results: The aqueous solubility in optimized blend of hydrotropic agent batches (U: SA: SB: SC, 4:4:23:9 %w/v) showed 835.71-fold compared to MFA solubility in distilled water. The quality control tests for parenteral formulation and accelerated stability study were found to be within prescribed limits and stable.
 Conclusion: The inadequate solubility of MFA was overcome, and aqueous injection was successfully developed which can be serve as cost effective treatment in various indications.
Highlights
For poorly soluble drugs usually, dissolution becomes the decisive factor for its poor bioavailability which again can limit their therapeutic effectiveness [1]
The inadequate solubility of Mefenamic acid (MFA) was overcome, and aqueous injection was successfully developed which can be serve as cost effective treatment in various indications
From the results it was concluded that saturation solubility (SS) of mefenamic acid was increasing with increasing concentrations of hydrotropic agents, for example, solubility in 40 %
Summary
For poorly soluble drugs usually, dissolution becomes the decisive factor for its poor bioavailability which again can limit their therapeutic effectiveness [1]. The active site of absorption for mefenamic acid is stomach and upper part of small intestine. Once emptied from stomach the passage through the small intestine is rapid, limiting the extent of absorption. It is supplied only in the form of tablets and capsules for oral administration. Solubility enhancement of insoluble drug mefenamic acid has been extensively studied to overcome difficulties that frequently come across during formulation development [4,5,6]. Hydrotropic agents and cosolvents have been observed to enhance the aqueous solubility of poorly water-soluble drugs [7,8,9]. Maheshwari et al have demonstrated the synergistic solubilizing capability due to a mixed hydrotropy approach and this approach has been applied to enhance the solubility of various poorly soluble drug [10, 11]
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