The Academy of Pharmaceutical Sciences
Promoting excellence in the Pharmaceutical Sciences sector.

Basic Biopharmaceutics Workshop 2023

8th June 2023 – Friends House, London

The Biopharmaceutics Focus Group hosted a workshop in June 2023 in London. The aim of the event was to provide the attendees with the core theoretical principles and the application of biopharmaceutics for the development of oral drug products, which were delivered by a mix of industrial and academic experts in oral biopharmaceutics. There were around 50 attendees at the event with many opportunities for the participants to network during the day. The talks involved different biopharmaceutics topics, where the speakers discussed the basic concepts, state of the art, current gaps and future challenges.

A recap of the workshop is presented below:

Biopharmaceutical properties (e.g., permeability)

Chris Roe from Quotient Sciences (Nottingham, UK) spoke about biopharmaceutical properties with a particular focus on permeability. Absorption mechanisms, how the permeability could direct the development towards improvement of formulations, and a detailed description of the in vitro Caco-2 assay (for estimation apparent human permeability) were shown. The main challenge for in vitro permeability estimation is the many important in vivo characteristics that are left aside as they could not be replicated easily in vitro.

Physicochemical properties for biopharmaceutics

Ibrahim Khadra from the University of Strathclyde (Glasgow, UK) discussed the importance of solubility, ionisation, lipophilicity, solid form as properties for biopharmaceutics. Characteristics of dissolution media are as important as those of the compounds, thus, an investigation of how a medium that simulates the human intestinal fluid was in development, by identifying which components are important using design of experiments. The relevance of these components was related to the characteristics of the compound.

Dissolution

Nikoletta Fotaki from the University of Bath (Bath, UK) presented a brief explanation of what is a dissolution test, dissolution apparatus and the current importance of the tests (quality control, in vitro in vivo correlation, in vivo predictions). As dissolution tests are on track to become more relevant for predictions, adaptations of apparatus and dissolution media to simulate the gastrointestinal conditions were given. Also, how to handle the dissolution data for further use in in silico predictions was reviewed.

Gastrointestinal physiology

Mark McAllister from Pfizer (Kent, UK) summarised the structure and function of the parts that comprise the gastrointestinal tract, from the oesophagus to the colon. Gastrointestinal physiology is a major topic for biopharmaceutics, as all the physicochemical properties interplay there and the in vitro tests meant to simulate the local conditions. The wide intra and inter subject variability of the

relevant physiological characteristics it is still a challenge when it comes to set a baseline or average conditions, for further use in dissolution media development or in silico simulations.

Basic Pharmacokinetics Principles

Hamid Merchant from the University of Huddersfield (Huddersfield, UK) gave a lecture on basic pharmacokinetics concepts. The presentation went through basic concepts such as Cmax, Area Under the Curve, half-life of elimination, steady state and why each of these parameters are important for clinical therapy.

Biopharmaceutics Classification Systems in drug development

James Butler from GlaxoSmithKline (Hertfordshire, UK) discussed the biopharmaceutics classification systems which are based on solubility, permeability, and disposition of drugs. Assigning a classification to drugs based on their characteristics, would give an idea if they are suitable for reduced regulatory investigation (biowaivers) or put the basis of formulation development (dissolution or solubility limited compounds). The systems are based on drugs alone, but excipients could interfere/improve solubility and permeability, thus, excipients should be investigated as well, or use in silico tools for a better understanding the drug exposure through their formulations.

Biomodels and Simulation

Jonathan Brown from Bristol Myers Squib (Liverpool, UK) focused on in silico modelling and simulation. In silico testing is a powerful tool that integrates the physicochemical properties of the compounds, permeability, dissolution, physiological characteristics of the organism, to create a model that allows explanation of in vivo pharmacokinetic data, with the objective to make further predictions. These could lead to better decision making and cost reductions. There is still discussion as to how the in vitro data is interpreted for use as input into the models, and even though there are several software alternatives, the models still need to be improved.

Regulatory Biopharmaceutics

Shanoo Budhdeo from SEDA (Cheadle, UK) spoke about aspects involved Quality by Design, Quality Target Product Profile, Biopharmaceutic Risk Assessment Roadmap (BioRam) which considers the target population. A hot topic is the control of drug products for clinically relevant dissolution methods and specification that could aid in the establishment of in vitro in vivo correlations. One particular challenge is that the drug products are constantly evolving and the regulatory has been outpaced. There is also a lack of guidance for special populations.

At the end of the event there was a discussion session about Future Challenges led by Mariana Guimaraes (GlaxoSmithKline, Stevenage, UK) and Ricardo Diaz de Leon (Quotient Sciences, Nottingham, UK). This was an interactive session where the participants were able to vote in real time about the current gaps and future challenges as a manner to start the discussion. The interest was focused on how to improve in vitro testing for a better simulation of the gastrointestinal tract in order to increase the predictive capabilities of in silico pharmacokinetic modelling. Participants were more interested in the simulation of disease states both in vitro and in silico.

In summary, the basic principles of biopharmaceutics were presented to the attendees with a future perspective in how to integrate this information into their current research and into in silico models.

The APS Biopharmaceutics Focus Group would like to thank all attendees and speakers for making this such a successful event. We have received great feedback from both attendees and speakers including one who said “I’m glad that I got the opportunity to attend the session. The workshop itself has been well-organised and I enjoyed the day very much. All the talks were detailed and had a good balance to suit people with limited knowledge as well as those with advanced knowledge in the area. Additionally, the audience had plenty of opportunity to ask questions and engage with others. The venue was easily accessible and nicely arranged.”

Thank you for supporting the APS and we hope to see you all again soon.