PHARMACEUTICALS
for further progression and ensuring a robust selection procedure .
Computational methods are increasingly used , for example , in the smart selection of solvents in a polymorph screen or co-formers in a co-crystal screen . A number of informatic tools are now routinely employed within crystallisation development to link small-scale solid form recommendations to the larger scale in a robust way , so that there are no unwanted surprises downstream .
Once the most appropriate solid form has been identified , PE can be used in its most fundamental application to control the desired solid form at scale such that consistency by design is built in . PE techniques can be used to modify drug particles with specific sizes , shapes and surface properties . A range of PE technologies can further enhance the solubility and bioavailability of the drug . For example , micronisation can be used to produce fine drug particles that can dissolve more quickly and easily in the body , leading to faster and more effective drug absorption .
Spray drying and hot melt extrusion can be used to stabilise amorphous APIs , which are inherently unstable , both chemically and from a solid form standpoint . Through a thorough understanding of the drug molecule ’ s properties particularly its stability , an amorphous API within an appropriate ( usually polymer ) matrix can be utilised to preserve the desired high aqueous solubility typical of amorphous material .
In parallel with PE approaches , we use a range of analytical techniques such as particle size analysis , surface area analysis and powder X-ray diffraction to monitor and control particle properties during the drug development process .
It ’ s all connected
The successful development of new drugs depends on understanding the underlying chemistry and applying the most appropriate techniques . With the right approach , drug developers can overcome solubility and bioavailability issues , creating more effective and reliable drugs . However , because of the increasing number of poorly soluble APIs and growing attrition rates within the pipeline , it is also important to take a step back and think about how we can improve drug discovery and development .
Veranova works with partners and clients to implement a holistic approach to drug discovery and development through our leading solid form and particle engineering services . By following a candidate molecule fully through the development process , gathering data at every stage , we optimise solubility , stability and other fundamental properties before they can become a hurdle and thus can accelerate time-to-market .
Candidate selection is one of the most important stages of drug development . Here , researchers must evaluate multitudes of new chemical entities to select the most promising candidate .
Therapeutic efficacy and safety are the key drivers at this stage , with
candidates ranked based on specificity and selectivity for key biological targets in the desired therapeutic area . By keeping the end product in mind , Veranova works to understand its partners and their target product profile and ultimate end goal , allowing us to evaluate efficacy , safety , developability and market potential .
For example , when looking at oral solid dosage forms , solubility and permeability can greatly impact development speed . We use characterisation technologies to measure molecular properties with in silico absorption , distribution , metabolism , excretion , and toxicity ( ADMET ) models , to significantly increase the robustness of candidate selection , which subsequently reduces failure rate during clinical trials .
In this way , we can help partners to achieve their objectives from the start , including the route of administration , drug target , dosage form and much more . Moreover , by designing a molecule-specific pharmaceutical development plan , we can help avoid formulation pitfalls , accelerating speed to market . ●
* - Pharmorphix is a registered trade mark of Veranova
References : 1 : D . V . Bhalani , B . Nutan , A . Kumar & A . K . Singh Chandel , Biomedicines 2022 , 10 ( 9 ), 2055 : https :// doi . org / 10.3390 / biomedicines10092055 2 : F . Thomas , Pharm . Technol . 2022 , 46 ( 8 )
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Craig Grant
GLOBAL DIRECTOR , SOLID FORM & PARTICLE ENGINEERING
VERANOVA craig . grant @ veranova . com www . veranova . com
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