Pharmaceutics (21) = Solubility Enhancement Techniques | Solubility Enhancement | Pharmaceutics 01

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Solution Pharmacy will cover this syllabus of medicinal chemistry 01 for B.Pharmacy 4th semester

SOLUBILITY ENHANCEMENT TECHNIQUES
Solubility is the phenomenon of the dissolution of a solid in a liquid phase to give a homogenous system. Solubility is one of the important parameters to achieve the desired concentration of drug in systemic circulation for pharmacological response to be shown. Poorly water-soluble drugs often require high doses in order to reach therapeutic plasma concentrations after oral administration. Low aqueous solubility is the major problem encountered with the formulation development of new chemical entities. Any drug to be absorbed must be present in the form of an aqueous solution at the site of absorption. Water is the solvent of choice for liquid pharmaceutical formulations. Most drugs are weakly acidic and weakly basic with poor aqueous solubility.
IMPORTANCE OF SOLUBILITY
1. Therapeutic effectiveness of a drug depends up on the bioavailability and ultimately upon the solubility of drug molecule.
2. It is important parameter to achieve desired concentration of drug in systemic circulation for pharmacological response to be shown .
3. Any drug to be absorbed must be soluble or present in the form of an aqueous solution at the site of absorption.
METHODS OF SOLUBILITY ENHANCEMENT:
1. Particle size reduction.
2. Surfactants
3. Salt formation
4. Co- solvency
5. pH adjustment
6. Solid dispersion
1. PARTICLE SIZE REDUCTION
The solubility of drug is related to drug particle size as a particle becomes smaller, the surface area increases , increase in solubility.
TECHNIQUES OF PARTICLE SIZE REDUCTION
• Micronization
• Nanosuspension
• Micronization
2. SALT FORMATION
Many a times an API cannot be formulated in its pure form due to various issues of instability. Thus they are converted to solid forms such as salts, co-crystals, solvates, hydrates, and polymorphs.
3. HYDROTROPY
Hydrotropy is a solubilization phenomenon whereby addition of large amount of a second solute results in an increase in the aqueous solubility of existing solute.
4. COSOLVENCY
The solubility of poorly soluble drugs in water can be increased by mixing it with some water-miscible solvent in which the drug is readily soluble. This process is known as co-solvency
and the solvent used in combination are known as cosolvent.
5. SOLID DISPERSION
Solid dispersion is defined as dispersion of one or more active ingredients (hydrophobic) in an inert carrier ( hydrophilic ) at solid state it is prepared by
1) Solvent evaporation method
2) hot melt method
3) fusion method

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