Trends in drug characteristics increasingly favor greater degrees of lipophilicity, higher molecular weight, greater physical form complexity, and significantly lower aqueous solubility. Consequently, many chemical entities in drug development pipelines have poor water solubility.
Low aqueous solubility severely limits a compound’s oral bioavailability and therefore also limits the commercial viability of a new product. As a consequence, many active pharmaceutical ingredients (APIs) that could potentially help cure diseases and improve consumers’ lives never enter the market.
Dow Pharma Solutions is committed to addressing the solubilization performance requirements of your APIs with a portfolio of solubility enhancing products.
To meet the industry needs, we utilize an array of technologies including:
- High-throughput polymer synthesis
- API polymer performance screening
- Laboratory-scale product development
- Structure/property optimization
- cGMP market-development plant capable of supporting clinical development of optimized solutions.
Solutions for Solubility Enhancement
AFFINISOL™ HPMCAS (SDD) Polymers
AFFINISOL™ Hypromellose Acetate Succinate (HPMCAS) and AFFINISOL™ High Productivity HPMCAS for Spray-Dried Dispersion (SDD) Formulations
AFFINISOL™ HPMCAS is a soluble polymer that can help optimize solubility enhancement by maintaining stable solid dispersions and inhibiting API crystallization.
AFFINISOL™ HPMC HME Polymers
AFFINISOL™ HPMC HME for Hot Melt Extrusion (HME) formulations is designed for use by pharmaceutical companies looking to enhance the solubilization and inhibit the recrystallization of APIs in hot melt extrusion formulations.
CARBOWAX™ SENTRY™ PEGs
CARBOWAX™ SENTRY™ PEGs are ingredients in liquid oral-dose medications such as cough medicines and elixirs, where they function as solubilizers and non-alcohol diluents. They also play a role in capsule formulations designed for solubility enhancement.
AMBERLITE™ and DUOLITE™ Ion Exchange Resins
AMBERLITE™ & DUOLITE™ resins can be used to enhance the solubility and disintegration of poorly soluble drugs. In the case of poorly soluble ionizable drugs, the release of drug from a resinate can be faster than the rate of dissolution of the solid form of the drug. Hence, with AMBERLITE™IRP69 ion exchange resin or DUOLITE™AP143, one can increase the rate at which poorly soluble drugs dissolve. We believe that this rapid dissolution occurs because of two factors:
- Each individual drug molecule is bound to a functional site. There is no crystal lattice energy to overcome.
- The ion exchange matrices are relatively hydrophilic and therefore allow water and aqueous solutions easy access into a 3-dimensional structure – eliminating problems with “wetting out” the drug.