The growing life expectancy of today’s society can partially be credited to the rapid development of disease treatments, such as drugs. These not only cure and prevent disease but also alleviate the symptoms of conditions, giving those affected a longer and higher quality of life. To ensure this can continue new discoveries and developments are needed to treat diseases, which are currently under researched. To do this the pharmaceutical industry, which is responsible for the research, development, production, and distribution of medication, has established well-ordered processes to ensure efficient drug production.
Drug Discovery
The first process which takes place is drug discovery, which encompasses the steps of finding a molecule with known pharmacological effects, which may be helpful when dealing with a certain disease or aliment. There is a multitude of factors considered within the drug discovery steps, which are detailed below.
- The most common starting point is finding a focus disease area, where a therapeutic would be beneficial and taking the time to find a chemical structure that could prove useful. At this stage a variety of designs are tested and fine-tuned to ensure only high potential candidates more onto the next stages.
- The next stage is to use High Throughput Screening to find valid ‘HITS’, which can be studied for their pharmacokinetic profiles and toxicity. This leads to a handful of compounds being successful and ready to move into the lead optimisation programme.
- The Lead optimisation programme is where the currently successful compounds are now assessed for their biological activity and physiochemical properties to determine if its appropriate for this compound to continue to preclinical and clinical studies.
- Within preclinical and clinical trials there are a number of optimising steps, which include technical development to ensure quality and safety, relating to its synthesis and formulation; Investigating studies also ensure safety of the product and efficacy through evaluating its toxicity and its pharmacokinetic suitability; and finally administrative functions such as quality control, logistics, communication and decision making are needed to reduce delayed production but also that data related to the tested drug is of high quality.
Drug Development
Drug discovery is then followed by the next process drug development, which is responsible for converting this potential therapeutic molecule into an approved and registered drug. This mainly involves taking the pure drug substance and modifying it to an appropriate dosage and formulation for safe human use. To do this there are two main steps which are described below.
Pre-formulation Studies: These may use some information obtained from the lead optimisation programme during drug discovery combined with investigations into the physical and chemical properties of the drug to evaluate the best approach to formulation. These physical and chemical properties include:
- Solubility and Dissolution rates
- Acidity and alkalinity (pKa)
- Stability
- Lipophilicity
- Particle morphology
- Melting point
- Facture behaviour
After that, the formulation studies take place, which is the engineering of this drug substance into a useable form. This may entail the conversion of a powder or liquid into a stable, deliverable product, while considering the factors assesses in the pre-formulation studies. It is key here to reach a balance between safety, efficiency, and ability to reach therapeutic objectives.
Merrow Scientific
During the above processes a variety of techniques are needed to ensure correct and efficient development of drug substances, which is where the analytical techniques offered at Merrow Scientific could be useful to you!
MIPAR: This advanced image analysis software can be utilised during the drug discovery process to analyse potential cellular and molecular structures, to help narrow down candidates to be moved forwarded in development. MIPAR can do this with the use of its Deep Learning tools, which allows for the extraction of complex patterns and information.
Rheosense: Rheosense can provide viscosity measurements which are very vital during the formulation studies in drug development. It is important to know how a formulated drug will change at different temperatures, like when it is being stored or traveling through the body, to ensure the drug can reach its desired location. As well as that the drug needs to efficiently enter the body, if a formulation is too thick this may not be possible. This is where Rheosense can provide useful measurements on viscosity at temperature and different shear rates to provide information such as formulation stability, composition and injectability.
Timegate: The Timegate instrument is a Raman Spectrometer so can be used to look at how a drug formulation may change over time, as many drugs are stored for weeks to months at a time. It is important to understand how components may change and what effects this may have on the drug itself before it is approved for commercial use. Raman spectroscopy can be used to do this as it is a very useful tool for identifying components within a sample, so will show if there have been any changes over time. Timegate is particularly suited to this application as some molecules tend to fluoresce when excited, meaning the important peaks are hidden by noise, but Timegate solves this problem!
Symcel: The most important factor of a drug, is its ability to do its intended purpose. For some drugs this is being able to kill off bacteria, viruses, and fungi. So, before such a drug can be approved it is important to quantify its effectiveness. Symcel can be used here, as it is an instrument which tracks the metabolic activity of organisms over time, so this combined with the potential drug, we can see how the bacteria for example are affected by it.
Nicoya: Finally, Nicoya can be used in a similar way as Symcel but to look at drugs which for used for interaction in the body such as protein-protein interactions. Nicoya use LSPR technology, which you can find our more about here to provide kinetics data on a drug e.g. containing protein and its ability to interact with its intended target.
If you have any questions about the instruments/techniques described above and want to find out more please contact us here.