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.
Overcoming the Challenge of Poorly Soluble Drugs
How to Optimize Enabled Drug Products with Rapid Formulation Development and Clinical Testing (RapidFACT®).
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.
Development and optimization of MR formulations in the absence of predictive laboratory or preclinical models
The integration of formulation design space, real-time GMP manufacturing, and an iterative sequential pharmacokinetic (PK) study in healthy volunteers was successfully applied to develop an HPMC matrix tablet that achieved the desired PK characteristics for SLx-2101.The key formulation variables influencing performance were the range of dose and release rate, hence a two-dimensional (2D) design space was mapped by manufacturing and characterizing four “regulatory batches” bracketing the corners of the compositional ranges.
Integrated Early-Stage Drug Development and Manufacturing: Accelerating Molecules to Proof-of-Concept
This webinar highlights how by breaking down the barriers between traditional outsourcing channels and workflows, drug development activities and key functional groups including formulation development, manufacturing and clinical research can be much more closely integrated to accelerate early-stage drug development, reduce overall expenditure and shorten time to proof of concept.