ZoomLab™-Webinar: Digitally Predicting And Optimizing Enteric-Release Coatings Formulations

A few weeks ago we did an interview with Dr. Ferdinand Brandl about ZoomLab™ in general.
Now, we had the pleasure to do a webinar about the newly introduced enteric-release coating module. Three ZoomLab™ team members (Valerie van Hulle, Dr. Ferdinand Brandl & Thorsten Cech) from BASF joined our webinar and presented the new module. Furthermore, they answered all the questions from the audience.

CLICK HERE TO DIRECTLY WATCH THE FULL WEBINAR

In the following, you can watch the introduction from Pharma Excipients and Valerie Van Hullen about the enteric coating module as well as some Q&A from the presentation.

Introduction into the new enteric-release coating module:

Valerie: In today’s session we will talk about ZoomLab and its new enteric-release coatings module. Before I begin, I would like to start by explaining why BASF developed ZoomLab as a virtual formulation assistant. Here at BASF, we received feedback from customers about the drug development process. Formulation development can be time-intensive, costly, and has a high risk of failure. Drug formulation is currently based on empirical methods, with outcomes often depending on the expertise and intuition of individual formulators.

Digitalization can help formulators of oral solid dosage forms address the challenges they typically face in their formulation journey. To support our customers, BASF has developed ZoomLab, a virtual formulation assistant for formulators. The virtual assistant is a science-based formulation prediction and optimization tool, allowing formulators to instantly optimize and predict their next starting formulation for a pharmaceutical product.

The system predicts the process ability of hypothetical drug excipients blends, identifying the most promising combinations in calculating a starting formulation depending on the selected dosage and defined target profile. The virtual assistant’s algorithms are based on scientific publications and the manufacturing classification system, ensuring an optimized an accurate starting formulation. The algorithm can predict what the optimal formulation should be, and even show step-by-step instructions on how to process it.

The formulator’s experience is at the forefront of BASF creation of ZoomLab. With this in mind, it is important to note that to maintain confidentiality, the assistant does not require the formulator to disclose the identity of the active ingredient. Users enter a few nonconfidential physical properties of the medicine and the target dosage, and ZoomLab provides instant recommendations. The virtual assistant offers pre-populated active ingredients, and there is no obligation to enter the name of the active ingredient at any time.

Ultimately, ZoomLab provides the user with an instant starting formulation, helping formulators save time and money by reducing costly pre-formulation and trial and error. ZoomLab is a free digital tool available online 24/7. We invite you to try out ZoomLab for yourself. You can go to info-mypharma.basf.com to sign up for ZoomLab, as well as any of BASF’s virtual pharma assistants. I would now like to turn it over to Thorsten to share more information about the science behind ZoomLab’s enteric-release coatings formulation module.

Question 1:

Pharma Excipients: You normally showed, of course, some excipients for BASF, but obviously ZoomLab will also work with all the other excipients, right?

Valerie: This is correct. So, the idea is, ZoomLab provides you a full starting formulation, and then to do that, it expands beyond BASF’s portfolio. So we do have partners and we have other products available in ZoomLab in order to provide this recommendation.

Question 2:

Pharma Excipients: Are the enteric coating levels recommended in ZoomLab a minimum to provide acid resistance, and thus the fastest release in the duodenum? Are the recommendations for enteric coat level based on observed/literature in-vivo performance?

Thorsten: Okay, those are question I can take as well. Let’s start from the drug release point of view. So, to really delay drug release, you need to apply a lot of coating material. So, drug release is typically not the major issue, so even if you applied a really high quantity of coating material, the drug release will still be comparatively quick and meet all the requirements of the pharmacopeia. The coating level required to really have no water permeation into the core and to prevent any drug liberation, this pretty much goes hand-in-hand with the specific need for a dedicated API.

The recommendations in ZoomLab are aiming for the fact that you don’t have any drug release at all during the first two hours of testing the dosage form in artificial gastric juice, and also to reduce the amount of water permeating to a minimum. This is the aim for…and there is a kind of safety bufferin’, so even though we see that the actual functionality can be provided at slightly lower coating level, the ZoomLab recommendation is slightly above this limit. So, this is part of formulation development to really evaluate the precise value.

The prediction of ZoomLab will definitely meet the specification so it’s rather unlikely that with the ZoomLab-based recommendation, you fail in the dissolution testing, so we can be pretty sure that this is given. Whether this is a really optimized formulation later on for production, well, there is still some room to play around, but it gives you an excellent starting point, and your first trial will definitely meet the specification.

Question 3:

Pharma Excipients: Can you tell us something about the future and the features in development, one of you? Because obviously we’re interested, where ZoomLab is heading. What is on the plan next?

Ferdinand: Yes, I think I can answer this question. So last year in November we launched our version 1.0 and this version was really focused on direct compression of uncoated tablet. Uncoated tablet, then a couple of days ago we released an update, this is the first version of ZoomLab which lets you calculate enteric-release coating formulation. And we are planning for another update in October, this will be presented at AAPS, and this version will allow you to calculate instant-release coating formulation, that means protective coatings and taste-masking coating, and this upcoming version will also contain a new feature, a new tool, which lets you simulate the dissolution profile of your active ingredient.

So a lot of exciting features coming up in October, and mid to long term, we are also looking into different areas such as solubilization, sustained-release, and also in delivery.