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Key expertise

Bioavailability

Bi
Bio availability

40% of drugs fail in preclinical trials due to bioavailability issues

As the average molecular weight of small molecules is increasing, there is a trend towards a higher share of low solubility molecules.

Improving bioavailability allows to reduce API dosage and minimize potential side effects.

Physical form (choice of the right salt, co-crystal, polymorph, amorphous) and morphology / size (particle engineering) need to be controlled in order to optimize solubility, dissolution rate, stability and powder flowability 

Selection of functional excipients for galenic formulations will allow to further improve solubility and permeability.

 

Early evaluation of potential bioavailability issues

Solubility and permeability evaluation according to the Developability Classification System (DCS) for an early detection of potential bioavailability issues for oral drug candidates and solutions to be implemented.

  • 40% to 60% of approved APIs are poorly soluble  (classes II and IV)
  • Most NCEs are in class II
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Solutions to improve bioavailability

Screening and optimization of crystal structure activities

  • Improve physico-chemical properties
  • Polymorph screen (metastable form, hydrates and solvates)
  • Salt formation (counter ion)
  • Co-crystal formation (co-formers)
  • Predictive tool XTAlpi (AI)

Particle size reduction

  • Increase surface area
  • Improve dissolution kinetics

Formulation

  • Increase solubility and stability
  • Enable controlled release :
  • Pre formulation (physico-chemical characterization)
  • Excipients: catalogue and custom polymers
  • Amorphous solid dispersion: amorphization techniques such as spray drying or hot melt extrusion
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SEQENS bioavailability services to support each stage of drug development

1/ Early Development (Preclinical, Phase I and IIa)

  • Selection of the most appropriate physical form 
  • Polymorph screening: mandatory for IND application 
  • Salt / co-crystals screening: improve physical properties in order to increase chance of success at preclinical phase
  • Amorphous solid dispersion : improve solubility and stability
  • API Characterization
  • Crystallization Process development
  • Particle size and solid dispersion engineering

Generation of Intellectual Property : New polymorphs or co-crystals allow to generate new patents and extend IP protection for the generics phase

2/ Late Development (Phase IIb, III)

  • Comprehensive screening for an IP perspective
  • In-depth API Characterisation
  • Process optimisation

Why Choose Seqens ?

  • Fully integrated (from preclinical to commercial supply) avoiding the risk of discontinuity in drug development
  • Comprehensive integrated and standalone solid state offering
  • Scientific and regulatory consulting expertise 
  • Agile service delivery model 

Global R&D presence (US, EU, INDIA)

Discover other R&D services

Ap

Analytical Platform

Analytical Platform

Seqens provides GMP testing on Active Pharmaceutical Ingredients (API) and excipients. We have an extensive team focused on the development and clinical phase appropriate validation of sensitive and specific analytical methods

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Bi

Biocatalysis

Biocatalysis

Biocatalysis is the usage of enzymes as catalysts of chemical reactions. Learn more about Seqens extensive expertise.

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Ch

Characterization

Characterization of APIs

Physical Characterization Testing Capabilities includes a full set of advanced technologies

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Dc

Drug Conjugates

Drug Conjugates

The field of drug conjugates is emerging, with the possibility to achieve 2 functions with one (bifunctional) compound, usually allowing targeted therapies or improved bioavailability properties.

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Li

Lipids

Lipids

In the pharmaceutical industry, lipids are core excipients in the development of drug delivery systems. Lipids can be used in most dosage forms as support vehicles, solubilizers, permeation enhancers, stabilizers, transfection agents and release rate modifiers.

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Mu

Multipurpose Flow

Multipurpose Flow Chemistry

In flow chemistry, a chemical reaction is run in a continuously flowing stream rather than in batch production, leading to many key advantages.

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P

Polymers

Polymers

Seqens strongly believes in the potential of new cutting-edge technologies to improve the use and efficiency of existing APIs. To support its customers, Seqens offers a range of drug delivery polymers.

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So

Solid State

Solid State characterization

The need to investigate the solid state properties of APIs has become important in the pharmaceutical development industry. Physical properties can vary widely between batches, leading to batch-to-batch variability.

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Sy

Synthetic Biology

Synthetic Biology for bioinspired and sustainable innovations

Part of Seqens group, Alganelle is an innovative biotechnology company at the cutting edge of synthetic biology and metabolic engineering.

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