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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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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?

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.

Types of Solid Forms

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

Solubility

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

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What are Solid Form Services?

The Workflow

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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

The Workflow

Tools for Solid Form Screening

Types of Solid Forms

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

Solubility

Chemical purity

Physical properties

Can we make them?

Do they have desired attributes?

Solubility & performance testing

Lead selection

Stability

Performance

Manufacturability

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Lonza’s solid form services experts leverage state-of-the-art analytical tools to understand a solid form’s physical and chemical properties.

Tools for Solid Form Screening

Regulation for Solid Forms

The Workflow

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

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Chemical Composition

Solubility and Dissolution

Powder Properties

Solid State Characterization

Powder Properties

Solubility and Dissolution

Chemical Composition

Solid State Characterization

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Solvent content analysis

Spectroscopy

Chromatography

In-depth assessment of the impurity profile and properties of a solid form using techniques that include

Elemental analysis

Water content analysis

Chemical Composition

Solubility and Dissolution

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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

Powder Properties

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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 State Characterization

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Vapor sorption

Dynamic mechanical analysis

Thermal analysis

X-ray powder diffraction

Spectroscopy

Microscopy

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

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Photo credit: Lonza Small Molecule

Vapor sorption

Dynamic mechanical analysis

Thermal analysis

X-ray powder diffraction

Spectroscopy

Microscopy

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

Solid state characterization

Chemical Composition

Solubility and Dissolution

Powder Properties

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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.

Regulation for Solid Forms

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Tools for Solid Form Screening

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

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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.

Learn more about Lonza Small Molecules

Regulation for Solid Forms

Download E-book

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