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Services >> Biologics Development & Manufacturing >> Pre-Formulation / Formulation Screening

Pre-Formulation / Formulation Screening

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Pre-formulation

Before pharmaceutical drug product formulation activities are started-up, pre-formulation studies are initiated. During the pre-formulation phase, the physical and chemical properties of the active pharmaceutical ingredient (API) are determined. For chemical API’s, the gained knowledge will help you to select the right salt or polymorphic form and will support the design and development of your dosage form, both for pre-clinical and clinical use. For biological API’s, pre-formulation studies ensure the best candidate is selected in terms of CMC properties which will prove beneficial in further drug product development processes. Furthermore, during pre-formulation studies, relevant analytical methods can be optimized to be used later on in the drug product development phase.

Pre-formulation includes:

  • API characterization
  • Dissociation constant (pKa)
  • Partition coefficient (Log P)
  • Particle size and morphology (laser diffraction, microscopic imaging)
  • Crystallinity (X-ray diffraction)
  • Thermal analysis (melting point and glass transition)
  • Solubility studies in organic and pharmaceutical solvents
  • Excipient compatibility studies
  • Forced degradation studies (heat, acid, alkali, light, peroxides, metal ions, chemical modifications)
  • Protein charge (pI) and zeta potential
  • Protein expression levels

 

Formulation screening

In the formulation screening phase, different drug delivery concepts are selected and compared to one another in terms of stability, efficacy and feasibility. Eurofins CDMO has experience with a wide range of different drug delivery routes, drug delivery systems and drug production technologies.

Drug delivery concepts can be worked out for the following delivery routes:

  • Oral liquid/solid formulation
  • Parenteral formulation
  • Buccal delivery
  • Nasal/intranasal delivery
  • Pulmonary delivery
  • Ophthalmic
  • Topical

 

Depending on the selected drug delivery route, the API can be stabilized, bio-availability can be enhanced or the release-profile can be modified by multiple delivery concepts:

  • Solutions
  • Microsuspensions
  • Nanosuspensions
  • Amorphous Solid Dispersions
  • S(M)EDDS
  • Spray drying
  • Freeze-drying (lyophilization)
  • Fluid bed granulation
  • Dry granulation
  • Wet nanomilling
  • Bead layering
  • Tablet manufacturing
  • Dry compaction
  • Compression of tablets and minitablets
  • Capsule filling of coated particles, minitablets, powders
  • Capsules (encapsulation/over-encapsulation)
  • Enteric coated tablets/capsules
  • Emulsions (semi-solids)
  • Controlled release systems
  • Fluid bed and pan-coating

 

Depending on the selected concept, different analytical techniques are used to characterize the formulation and perform stability studies:

  • assay and content uniformity determination via UV-spectrophotometry or HPLC
  • pH
  • density
  • zeta potential measurement
  • in vitro drug release via dissolution testing
  • particle size distribution via laser diffraction analysis
  • physical tablet properties
  • solid state characterization via pXRD and mDSC
  • moisture determination

 

Choose Eurofins CDMO for your pre-formulation studies and formulation screening:

✔ We have experience with a wide array of different drug delivery routes
✔ We have a multitude of drug delivery concepts to accommodate your desired drug delivery route
✔ Analytical method development is performed in-line with pre-formulation studies and will guarantee time-saving later on in the drug product development phase.