Abstract

Solubility, the phenomenon of dissolution of solute in solvent to give a homogenous system, is one of the important parameters to achieve desired concentration of drug in systemic circulation for desired (anticipated) pharmacological response. Low aqueous solubility is the major problem encountered with formulation development of new chemical entities as well as for the generic development. More than 40% NCEs (new chemical entities) developed in pharmaceutical industry are practically insoluble in water. Solubility is a major challenge for formulation scientist. Any drug to be absorbed must be present in the form of solution at the site of absorption. Various techniques are used for the enhancement of the solubility of poorly soluble drugs which include physical and chemical modifications of drug and other methods like particle size reduction, crystal engineering, salt formation, solid dispersion, use of surfactant, complexation, and so forth. Selection of solubility improving method depends on drug property, site of absorption, and required dosage form characteristics.

Highlights

  • Solubility is the property of a solid, liquid, or gaseous chemical substance called solute to dissolve in a solid, liquid, or gaseous solvent to form a homogeneous solution of the solute in the solvent

  • Many investigators studied solid dispersion of meloxicam, naproxen, and nimesulide using solvent evaporation technique. These findings suggest that the above-mentioned technique can be employed successfully for improvement and stability of solid dispersions of poorly water soluble drugs [15, 17]

  • Dissolution of drug is the rate determining step for oral absorption of the poorly water soluble drugs and solubility is the basic requirement for the absorption of the drug from GIT

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Summary

Introduction

Solubility is the property of a solid, liquid, or gaseous chemical substance called solute to dissolve in a solid, liquid, or gaseous solvent to form a homogeneous solution of the solute in the solvent. The extent of solubility of a substance in a specific solvent is measured as the saturation concentration where adding more solute does not increase its concentration in the solution [1]. Saturated solutions of ionic compounds of relatively low solubility are sometimes described by solubility constants. It is a case of equilibrium process. Similar to other equilibrium constants, temperature would affect the numerical value of solubility constant The value of this constant is generally independent of the presence of other species in the solvent. The Biopharmaceutics Classification System (BCS) is a guide for predicting the intestinal drug absorption provided by the U.S Food and Drug Administration This system restricts the prediction using the parameters solubility and intestinal permeability. All drugs have been divided into four classes: class I— high soluble and high permeable, class II—low soluble and high permeable, class III—low soluble and high permeable and class IV—low soluble and low permeable

Importance of Solubility
Techniques for Solubility Enhancement
Particle Size Reduction
Solid Dispersion
Nanosuspension
Cryogenic Techniques
Inclusion Complex Formation-Based Techniques
10. Micellar Solubilization
11. Hydrotrophy
12. Crystal Engineering
Findings
13. Conclusion
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