Abstract
The aim of the present study was to enhance the dissolution rate of an NSAID drug Ketoprofen by formulating it into solid dispersions with water soluble carrier Poloxamer 188 and Eudragit S 100. The solid dispersions of Ketoprofen with Poloxamer 188 were prepared at 1:1, 1:1.5 and 1:2 (Ketoprofen: Poloxamer 188) ratio by Solvent evaporation methods. The same concentration ratio was used for the preparation of solid dispersion with Eudragit S 100 by melting/fusion technique. Further, solid dispersions were investigated by solubility, ATR-FTIR, XRD, DSC, surface morphology, in-vitro dissolution and accelerated stability study. Results demonstrated that both Poloxamer 188 and Eudragit S 100 improve solubility of drugs by 8–10 folds. The result of ATR-FTIR study showed the slight shifting/broadening of principle peaks. In vitro dissolution studies showed that in the solid dispersion system containing Ketoprofen: Poloxamer 188 batch P2 (1:1.5) gives faster dissolution rate of Ketoprofen than the physical mixtures. The solid dispersion with Eudragit S 100, batch E1 (1:1) gives faster dissolution rate of Ketoprofen than the physical mixtures. In phase solubility study with Poloxamer 188 showed concentration dependent solubilization of drug but Eudragit S 100 produced opposite result. The effect of pH on solubility of Eudragit S 100 was carried out which showed solubility at pH 7.4. The dissolution profile of solid dispersion with Eudragit S 100 at pH 7.4 gives excellent result. The Accelerated stability of solid dispersions & its physical mixtures were studied at 400±2 °C/75 ± 5% RH for a period of 1 month. In these studies, Solid Dispersion batches produced an unstable formulation. The Ketoprofen solid dispersions with Poloxamer 188 and Eudragit S 100 could be introduced as a suitable form with improved solubility.
Highlights
The aqueous solubility of a drug is a significant limitation to its oral absorption
Poloxamer 188 and Eudragit S 100 were from Fine Laboratories (Mumbai) and all other materials and reagents used were of analytical grade
The results suggest that there may be a mild interaction between Ketoprofen and Poloxamer 188, Eudragit S 100 in solid dispersion which changes orientation during crystal growth phase
Summary
The aqueous solubility of a drug is a significant limitation to its oral absorption. Water-soluble drugs are associated with slow drug absorption leading to inadequate and variable bioavailability (Amidon et al, 1995; Leuner, Dressman, 2000). The Biopharmaceutical Classification System (BCS) is the scientific framework for classifying drug substances based on their aqueous solubility and intestinal permeability. BCS class II and IV drugs which have low. Solid Dispersion (SD) technique has been extensively used to improve the dissolution rate, solubility and oral absorption of poorly water-soluble drugs. The dispersion method allows preparation of physically modified forms of drug that is much more rapidly soluble in water.
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