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Quotient Sciences Formulation Strategies for Poorly Soluble Molecules
As the number of poorly soluble compounds continues to increase in the industry development pipeline, conventional formulation strategies may not be sufficient to achieve acceptable levels of solubility.
Access our latest data sheet to learn about Quotient's formulation strategies and technologies that can help your challenging molecule achieve clinical success by clicking here.
One proven method of improving the solubility, and hence bioavailability, of your drug candidates is spray drying. The technique involves dissolving the drug in an organic solvent in the presence of a polymer. The resulting solution is then spray dried to form a dispersion (a spray-dried dispersion or SDD).
Quotient has a proven track record of developing and manufacturing SDDs to overcome your poor drug solubility and delivery challenges. We tailor the development of your SDD toward the specific physical and biopharmaceutics properties of each molecule. Over the past two years we have advanced more than 25 SDD formulations into clinical studies. Using state-of-the-art equipment, including ProCepT spray dryers for up to 1 kg batches and a Niro Mobile Minor spray dryer for batches of 1 to 10 kg, we develop your SDDs using both aqueous and solvent-based processing intended for both oral and inhaled drug delivery. Developed SDDs can be administered either as powder in a bottle reconstitution prior to dosing or can be further formulated as a powder in capsule or tablet presentation.
Particle size reduction
Highly experienced Quotient experts utilize a suite of particle size reduction processing equipment including mills, nanomills and micronizers depending on your intended final drug product. Your developed products can be presented as a drug in a bottle or can be further formulated as a drug in capsule or tablet formulation.
Lipidic vehicles and complexes
Recent years have seen lipid-based drug delivery systems and complexes become increasingly important tools in the quest to improve the oral bioavailability of poorly soluble drugs. Lipid-based solubility enhancement has developed from the observation that many poorly water-soluble drugs see an improvement in bioavailability when administered with a fat-rich meal; essentially the stimulation of biliary secretion can promote drug solubilization within the GI tract. Lipidic vehicles are designed to mimic this effect by pre-dissolving the drug within an appropriate lipid structure, thus bypassing the need for the poorly soluble, crystalline material to dissolve in situ.
Similarly, cyclodextrin drug-inclusion complexes act to improve aqueous solubility by essentially shielding the hydrophobic drug within an interior cavity of the hydrophilic cyclodextrin, thus enabling the entire complex to drive improved oral bioavailability.
Quotient has considerable expertise in the development of your lipid-based and complex drug delivery vehicles. In collaboration with you, we screen a range of lipidic and complexation vehicles including self-emulsifying drug delivery systems, self-microemulsifying drug delivery systems, single oil phases and cyclodextrins. Your formulations are then characterized in vitro, prior to progression into the clinic.
Formulation Strategies for Poorly Soluble Molecules
With nearly 30 years of experience, Quotient has established a broad suite of technologies and formulation approaches to address these complex solubility challenges. Our approach allows us to dramatically speed up the optimization of your drug products to improve oral bioavailability.
Formulation Development - Spray Drying
We use a broad range of formulation approaches to address complex solubility and bioavailability challenges, ensuring technology selection is driven by molecule need.
AAPS 2020 Poster - Flexible formulation assessments in FIH studies for poorly soluble drugs accelerates dosage form development, manufacturing and supply for patient POC trials
Here we describe how the integration of formulation development, compounding and GMP manufacturing activities within the FIH to POC program can streamline development and maximize potential for clinical success.
AAPS 2020 Poster - Development of High Drug Load Multiparticulate Beads Using an Extrusion-Spheronization Process
During high shear wet massing, changes in impellor torque occur as a result of changes in cohesive forces in the wet powder bed, and can be used to assess end points. However, for these formulations the change in torque was not sensitive enough for end point identification. Optimal end point for extrusion-spheronization reached just before the traditional wet granulation end point.