Solubility enhancement – Transform insoluble drugs into stable and efficient formulations
Recent industry trends show many pharmaceutical manufacturers are creating drugs with greater degrees of lipophilicity, higher molecular weight, greater physical form complexity and lower aqueous solubility. Unfortunately, these characteristics often produce poorly soluble drugs, which means the formulators need to use excipients or processes which improve solubility, dissolution and in turn bioavailability of the drug product.
Manufacturers seeking to improve drug solubility can turn to Nutrition & Biosciences. Leveraging our versatile cellulose-based excipient, AFFINISOL™ HPMC HME, we help manufacturers overcome their solubility challenges and provide consumers with a high-performing drug.
Enhanced solubility for multiple dosage forms
AFFINISOL™ HPMC HME can be used via hot-melt extrusion or spray-drying methods, to enhance drug solubility for a variety of dosage forms, including tablets, powders and capsules. By incorporating AFFINISOL™ HPMC HME into their formulations, manufacturers can expand thermal processing ranges, allowing the excipient to be extruded without the use of plasticizers.
Unique to this polymer, formulators using hot-melt extrusion can simultaneously enhance the drug’s solubility while also creating a modified release profile, if desired. The high molecular weight grade of AFFINISOL™ HPMC HME can stabilize the drug in a more readily soluble form while also acting as a matrix forming polymer to extend release of the solubility-enhanced drug over a prolonged time period. Formulators can use AFFINISOL™ HPMC HME to directly extrude tablets, or to grind into a powder which can be combined with other formulation ingredients and compressed into tablets or loaded into capsules.
The revolutionary properties of AFFINISOL™ HPMC HME which enable extrusion across a wide range of processing conditions are also responsible for enhancing the solubility of the polymer in a range of commonly used spray-drying solvents. In spray drying applications, the poorly soluble drug and stabilizing polymer are co-dissolved in a mutual solvent and then spray-dried to form a stabilized dispersion. Many formulators prefer to screen solubility enhancing polymers at small scale using spray drying techniques but would prefer to utilize a more cost-effective melt extrusion process at commercial scale. The possibilities are endless when formulating with AFFINISOL™ HPMC HME.
Whichever method you choose, our team of global experts will guide you through every step of the manufacturing process to find a method and ingredient that creates a high-quality, water-soluble formulation every time.
| Application | Product Recommendation | |
|---|---|---|
| Hot-Melt Extrusion | AFFINISOL™ HPMC HME Grade | Recommended Extrusion Temperature Range (no plasticizer) |
| 15 LV | 135 - 190°C | |
| 100 LV | 145 - 195°C | |
| 4M | 155 - 200°C | |
| Hot-Melt Extrusion with Extended Release | AFFINISOL™ HPMC HME 4M | |
| Spray-Drying | AFFINISOL™ HPMC HME 15 LV | |