Abstract
Objective: Nateglinide is a commonly used oral hypoglycemic, biopharmaceutical classification system Class II drug, which shows relatively poor water solubility and variable bioavailability. The objective of the present investigation was to develop the binary and ternary solid dispersions of nateglinide for improved solubility and dissolution.
 Methods: Nateglinide solid dispersions were prepared by a common solvent evaporation method. Polymers like soluplus, kolliphor P188, sylloid 244FP, gelucire 48/16, affinisol (HPMCAS), HPβCD, βCD were used in different combinations. The physicochemical characterization of the optimized ternary dispersion was studied by using FT-IR, DSC, and PXRD. Solubility and dissolution behavior of all dispersions were studied.
 Result: From all prepared ternary solid dispersions, nateglinide dissolution was significantly faster than pure nateglinide. With ternary solid dispersion of NTG, soluplus and kolliphor P188 there was a big improvement in solubility and dissolution. This combination enhanced the solubility of NTG by 23 folds. Another ternary dispersion of NTG with soluplus and gelucire 48/16 enhanced solubility by 25 fold.
 Conclusion: Ternary solid dispersion found superior over binary dispersions. For the ternary dispersions, showing the best solubility, tablets were prepared. Dissolution and drug release from the formulated tablet was as good as a marketed product.
Highlights
Enhancement of the solubility of the poorly water-soluble drug is one of the most challenging issues in the pharmaceutical industry
Amorphous solid dispersion has been proved as an effective method to enhance the solubility and dissolution behavior of many BCS II class drugs [2]
All the batches of the above Binary mixtures, ternary mixtures, and pure drugs were subjected to saturation solubility studies at room temperature in 0.5% SLS in 0.01N HCl, which is reported dissolution media for nateglinide
Summary
Enhancement of the solubility of the poorly water-soluble drug is one of the most challenging issues in the pharmaceutical industry. Limited drug Dissolution and bioavailability depend on its solubility and permeability [1]. Amorphous solid dispersion has been proved as an effective method to enhance the solubility and dissolution behavior of many BCS II class drugs [2]. Nateglinide is an oral hypoglycemic agent used in the treatment of type II diabetes mellitus (non-insulin-dependent diabetes mellitus, NIDDM). Nateglinide is a non-sulfonylurea drug, belonging to BCS class II, low solubility and high permeability [3]. Nateglinide is the most effective antidiabetic drug; lipophilic, belongs to family meglitinide, recommended in 60 mg or 120 mg dose. It has very poor water solubility 0.061 mg/ml. Studies say that NTG exhibits pHdependent solubility and variable bioavailability [5]
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