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Formulation development

Oral liquid formulation

AmatsiSEPS develops and evaluates oral liquid formulations for preclinical and early human studies. Novel drug candidates are mainly poorly water soluble drug candidates. Therefore, different strategies to develop an oral liquid formulation can be proposed.

  • Solutions:
    Solubility is determined in aqueous and/or lipid solvents, depending on the drug candidate chemical properties and demands of the formulation. Surfactants, complexation agents and co-solvents can be added to increase solubility, and hence enhance bioavailability.
  • Microsuspensions:
    Particle size is a critical parameter for the dissolution rate. Micronization of the drug substance or wet milling in a suspending vehiculum to microfine particles can therefore be important to obtain a good bioavailability of a poorly water soluble drug substance.
  • Nanosuspensions:
    Nanonization of a poorly water soluble drug substance increases the dissolution rate by an important increase of the surface area but also by some increase of the solubility. A nanosuspension of poorly water soluble drug substances shows a faster dissolution and a higher bioavailability when compared to a microfine suspension.
  • Emulsions:
    Based on solubility data in oily vehicles, (co-) surfactants and solvents, emulsions – a fine dispersion of droplets – can be formulated. Drug may be dissolved or suspended in either the oily liquid or aqueous liquid phase.

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- and zeta potential measurement, in vitro drug release via dissolution testing, and particle size distribution via laser diffraction analysis to evaluate the suspensions and droplet size of emulsions.

Oral solid formulation

AmatsiSEPS develops and evaluates oral solid formulations for preclinical and early human studies. We offer a wide range of advanced technologies for your drug delivery challenges: 

  • Immediate release
  • Bioavailability enhancement
    Solid nanoformulations and solid dispersions can be processed
    • as free-flowing powders by spray drying.
    • as spherical single- or multilayered particles containing one or more drug substance by fluidized-bed coating.
  • Controlled release
    Taste masking, enteric protection, colon targeting, sustained ph-independent release, pulsed release or combinations thereof.  A modified drug release profile can be accomplished using different technologies:
    • Matrix tablet technology
    • Coating of multiparticulates (spherical single- or multilayered particles or minitablets) by fluidized-bed coating
  • Combination therapies
  • Equipment/technologies
    • Drug-Excipient Compatibility Study
    • Fluid-bed granulation
    • Dry compaction
    • Compression of tablets and minitablets
    • Capsule filling of coated particles, minitablets, powders
    • Fluid bed coating
    • Spray drying

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, physical tablet properties, solid state characterisation via pXRD and mDSC, in vitro drug release via dissolution testing, moisture determination, particle size distribution via laser diffraction analysis and zeta potential measurement.

Parenteral formulation

AmatsiSEPS develops and evaluates parenteral formulations for preclinical and early human studies. The development of a parenteral pharmaceutical product has a number of considerations such as the administration route and device; the most commonly used routes are intravenous, intramuscular, subcutaneous and intradermal. The formulation must meet the specific requirement for sterility, isotonicity, must be pyrogen-free and free of particulate matter, in a narrow pH range.

During development, the parenteral formulation is optimized via pH adjustments, co-solvents, complexation, surfactants and combinations of these methods are commonly used to select a formulation vehiculum. Different concepts can be developed: solutions, suspensions, emulsions, and a powder for reconstitution via freeze-drying, also called lyophilization, in case of stability issues.

Stability, syringe ability and compatibility with the administration device must be investigated.