Solubility enhancement

How do I overcome solubility challenges in my molecule? Quotient is your answer.

Recognizing that poor solubility is becoming increasingly prevalent in drug pipelines across the industry — about 70 percent of drugs that enter development possess insufficient aqueous solubility for adequate and consistent gastrointestinal absorption — Quotient Sciences has an extensive offering to tackle your solubility challenges.

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.

Spray drying

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.

Solubility enhancement

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