Most of the drugs according to BCS classification are poorly water soluble. Apart from routine methods anybody suggest some new methods to increase the solubility.
Use co-solvents at the Tox acceptable level. Do an optimization.
- Cosolvents increase the solubility but strong electrolytes (salts) reduce the solubility of nonpolar solutes
- Nonpolar solutes are solubilized more efficiently than polar solutes by nonpolar cosolvents → they reduce solvent-solvent (H2O) interactions
- Generally, there is a linear relationship between the log Smix (nonpolar) in a mixed solvent and vol.% (or vol. fraction , fi) of cosolvent
- For less nonpolar solutes there is a downward concavity of the curve at high cosolvent composition
- The effect of multiple cosolvents on solubility is additive and the undesirable effects (toxicity, viscosity) are not
log Smix = log Sw + Σi〖σi fi 〗
σ = S x log Kow + T
where,
Smix and Sw are the solubility in mixed solvents, and water
σ is the solubilizing power of the cosolvent
Fi is the volume fraction of cosolvent i
Kw is the partition coefficient in octanol/water
S and T are polarity dependent constants – correlate w/ H-bond
Dear all, dobilock copolymers and surfactants are used for such a purpose. My Regards
Hi;
There are several approaches reported in literature to enhance the solubility of poorly water-soluble drugs. The techniques are chosen on the basis of certain aspects such as properties of drug under consideration, nature of excipients to be selected, and nature of intended dosage form. Generally, to improve the solubility of poorly soluble drugs, methods such as reduction in particle size, crystal engineering, salt formation and complexation are used. Other techniques that enhance the solubility of poorly water soluble drugs include change in dielectric constant of solvent, chemical modification of the drug and application of ultrasonic waves.
With my best regards
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