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Explore how Lonza’s Solid Form Services help developers select, characterize, and advance promising drug forms
Optimizing solid forms in small molecule drug development
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Photo credit: Lonza Small Molecules
Ensuring the selected drug form is stable and manufacturable, and meets performance requirements
Designing and developing processes to isolate that solid form
Evaluating and characterizing potential solid forms to identify a candidate form with optimal properties
SFS offerings include
Solid form services (SFS) aims to bridge the gap between a small molecule drug substance and the final drug product.
What are Solid Form Services?
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Polymorphs of the same compound can have different solubilities. This impacts drug bioavailability and performance.
Polymorph B
Polymorph A
Solubility
Types of Solid Forms
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Stability
Different polymorphic forms of a drug can have different chemical properties, including
Every compound has a number of potential solid forms.
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Different solid forms of the same API may have drastically different characteristics both in and out of the body. Thorough characterization of potential forms is vital to ensure drugs are safe and effective.
Packing
Purity
Ease of manufacturing and processing
Bioavailability
Finding and evaluating all possible polymorphs early in the development process enables research teams to select the right form first, saving time and money.
Polymorphs have different molecular arrangements
Salts are ionic crystals with 2 or more components
Amorphous forms have no long range order
Cocrystals are non-ionic crystals with 2 or more components
Solvates and hydrates have solvent trapped in the crystal structuree crystal structure
The Workflow
What is the propensity of the active pharmaceutical ingredients to form polymorphs?
Each step in the workflow aims to answer specific critical questions about solid form identification and characterization, such as
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Tools for Solid Form Screening
Which salt form is stable?
How can we isolate this salt form?
How can we maximize or control bioavailability?
What is the most efficient crystallization process?
EARLY DEVELOPMENT
LATER Dev
Characterization of Available Form and Absorption Risk Assessment
Polymorph Screen*
Other BA Enhancement Screens (e.g. amorphous form screening)
Salt Screen (if applicable)
&/or Cocrystal Screen
Additional screens to reduce risk and/or strengthen IP
Crystallization process development for troubleshooting
Why solid forms?
Physical stability
Chemical purity
Physical properties
IP
Can we make them?
Do they have desired attributes?
Solubility & performance testing
Lead selection
Performance
Manufacturability
Lonza’s solid form services experts leverage state-of-the-art analytical tools to understand a solid form’s physical and chemical properties.
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Regulation for Solid Forms
Solid State Characterization
Study of the relationships between the structure, synthetic method, and properties of a solid form. Scientists characterize attributes of different polymorphs using techniques that include
Microscopy
Spectroscopy
X-ray powder diffraction
Vapor sorption
Dynamic mechanical analysis
Thermal analysis
Chemical Composition
Solubility and Dissolution
Powder Properties
Solvent content analysis
Chromatography
In-depth assessment of the impurity profile and properties of a solid form using techniques that include
Elemental analysis
Water content analysis
pKa and logP
Disintegration
Biorelevant dissolution
Intrinsic dissolution
Amorphous solubility
Solubility in biorelevant media and process solvents
Investigates the solubility and dissolution rate of a solid form under different conditions (such as temperature and pH) to predict its behavior in the body, using assessments like
Permeation testing
Photo credit: Korsch
Flow rate
Density
Tabletability (capacity of material to be compacted into a tablet)
Particle size, shape, and morphology
Characterization of the properties and behavior of a powder form to optimize production, formulation, and final drug product design. Assesses powder attributes such as
Solid form services help research teams to achieve goals at every phase of the drug development process. Interact with the boxes below to see how solid form data is used.
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Learn more about Lonza Small Molecules
Discovery
Preclinical/Early Development
Clinical Phase to Launch
Post approval
Characterize incoming solid forms
Select a lead candidate
Understand absorption risks
Inform design of toxicity testing and in vivo studies
Finalize formulation of drug product
Streamline crystallization process
Decide on optimal form to support late-phase studies and product launch
Strengthen intellectual property by ensuring all possible polymorphs are captured in portfolio
Further explore and optimize formulations to support new product indications
Explore alternative formulations to improve bioavailability of poorly soluble compounds
Select stable form for development
Identify all possible polymorphs
Download the Leveraging Advanced Analytical Tools to De-risk Pharmaceutical Development eBook to learn more about the science of SFS, as well as Lonza’s other derisking techniques.
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