SERVICES

Puritanlabs provides Medicinal chemistry solutions through an experienced team of medicinal chemists augmented by synthetic chemists, biologists and support teams. With expertise in early target identification, hit-finding strategies, hit-to-lead, lead optimization, patent strategy, and preparation for IND filing, we work with you to understand your requirements and deliver development candidates that meet agreed target product profiles.

Our medicinal chemistry services focus on the delivery of key target compounds, with a high success rate. Our expertise in route design and parallel synthesis of small focused library sets (typically 5 to 50 compounds) ensures your leads are efficiently optimised. In-house custom synthesis capability and state-of-the-art equipment allow us to quickly and cost effectively synthesise, optimise and progress leads to the next stage of development.

Typical medicinal chemistry services include:

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Route evaluation and development of new synthetic routes for target molecules.

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Process development and optimization (early to late stage, small to large scale).

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Optimization of reaction conditions to reduce cost and maximize throughput by classical methods or statistical design of experiments.

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Development of reliable methods for in-process testing and analysis of intermediates and APIs.

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Ability to perform work under cryogenic conditions or high pressures (& 100 psi).

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Rapid screening of reaction conditions using parallel equipment.

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Analytical development and validation.

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Synthesis and purification of analytical reference standards.

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Scale-up capabilities for GMP and non GMP purposes.

We are here to deliver your custom small molecule API development projects on time, within budget and to the highest quality standards.

From initial Discovery leads, our research team will progress your project expeditiously through the lead and lead optimisation stages. Our team can provide preclinical quantities of Development candidates with robust routes and technology transfer packages to facilitate the manufacture of clinical quantities of compounds that may progress to become new medicines.

We have the expertise, flexibility and resources to provide a full range of pharmaceutical custom development services. Ranging from investigational new drug (IND) support from pre-clinical to Phase III clinical trials and technology transfer for commercial supply…we can support your products at every stage of the lifecycle.

Our custom development capabilities include:

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Route evaluation and development of new synthetic routes for target molecules.

N

Process development and optimization (early to late stage, small to large scale).

N

Optimization of reaction conditions to reduce cost and maximize throughput by classical methods or statistical design of experiments.

N

Development of reliable methods for in-process testing and analysis of intermediates and APIs.

N

Ability to perform work under cryogenic conditions or high pressures (& 100 psi).

N

Rapid screening of reaction conditions using parallel equipment.

N

Analytical development and validation.

N

Synthesis and purification of analytical reference standards.

N

Scale-up capabilities for GMP and non GMP purposes.

Puritanlabs understands the critical importance of analytical parameters and controls for effective and robust Product development. Our highly experienced Analytical Development team works closely with their Pharmaceutical Development counterparts to ensure your product is fully supported at every phase in the development process. Fully equipped, we provide the following range of analytical services to help bring your project to fruition:

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Active ingredient characterization (e.g. NMR, Mass, IR, UPLC and HPLC-MC)

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Development of analytical methods for RM, intermediate, API, Impurities

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Determination of physicochemical properties of drug substances

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Forced Degradation Studies for drug substances

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Validation of analytical methods

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Structural elucidation of unknown chemical substances

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Support, adaptation and optimization of your methods

Puritanlabs has extensive experience and a wide range of analytical and synthetic equipment to conduct successful impurity identification in pharmaceutical products.

We know that the control of pharmaceutical impurities is a critical challenge to the pharmaceutical industry. Structure elucidation of pharmaceutical impurities is a major component of the drug product development process. According to the ICH Q3A(R2) and Q3B(R2) guidelines, impurities in any dosage form, or API, must be identified during product development. Identification and quantification of impurities (Impurity Profile) has become a key focus of and subject to critical review by regulatory authorities. Additionally, any degradation product, observed in stability studies at recommended storage conditions, at a level greater than the identification threshold must be identified.

 

Our impurity identification services include:

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Development of a mass spectrometry suitable High performance liquid chromatography method for the separation of the examined impurity.

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High resolution mass spectrometry analysis for the determination of molecular weight and formula of the impurity

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Fragmentation mass spectrometry analysis of the impurity and related compounds for the structure elucidation of the impurity

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Isolation of the impurity, from the drug product, using preparative high-performance liquid chromatography (HPLC) with or with of DAC column

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Nuclear magnetic resonance (NMR) analysis for the structure elucidation of the impurity

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Proposition of the molecular structure of the examined impurity based on the Mass and NMR analysis results

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Chemical synthesis of the reference material with the proposed structure

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Confirmation of the proposed structure by comparative HPLC-MS/MS analysis employing the synthesised reference material

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Suggestion of the impurity origin and its formation pathway

Impurity Characterization Techniques

ISOLATION

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Liquid/liquid or solid phase extractions

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Preparatory TLC

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Preparatory HPLC

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Flash Chromatography

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Liquid/liquid or solid phase extractions

Purification

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Preparatory Chromatography

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Recrystallization

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Solid Phase Extraction (SPE)

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Semi-preparatory HPLC

Structural Elucidation:

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NMR (1H and 13C)

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FTIR

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MS and MS/MS

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Elemental Analysis (CHNSO)

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High Resolution LC/MS/MS

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High Resolution GC/MS

Purity Characterization:

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Assay (UV, HPLC, GC, CE, and IC)

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Chromatographic Purity (TLC, CE, GPC/SEC, HPLC, and GLC)

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Metallurgical Catalysts (ICP, ICP-MS, AA, AE)

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Inorganic Ash (ROI, ICP, ICP-MS, AA)

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Residual Solvents (Headspace GC)

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Moisture (KF, CKF)

The results from our impurity characterization studies can be presented as a formal report suitable for regulatory submissions.

Puritanlabs utilizes the widest range of purification technologies including Flash, DAC and HPLC systems. Development and optimization of chromatography processes are one of our core areas of expertise. We design, develop and optimize all kinds of chromatography steps from feasibility studies to process transfer and qualification.

Flash chromatography is relatively more productive and can be a great workhorse in our lab, and offer automated peak collection. The DAC (Dynamic Axial Compression) technology allows high separative performance to be maintained over time and guarantees high-quality products, even for long-standing operations. Prep HPLC is the perfect solution to reach high purity and recovery yield from complex mixtures and to separate your target API from product-related impurities.

We offer a full range of technologies to address your purification requirements. By combining all the above chromatography techniques to separate your molecule, you can secure the production of your APIs and make sure your next clinical trials start on time.

Our chemists are well-versed in asymmetric synthesis using chemical transformations at mg to multi gram scale. The enantiomeric purity of each deliverable is adjudged through specific rotation, as well as using chiral HPLC methods. In case of unknown substances, we perform synthesis in racemic series in parallel to avoid any ambiguity. Our expertise in this area consists of the following:

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Enantiospecific synthesis from chiral pool approach using commercially available amino acids, Terpenes and Carbohydrates

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Synthesis of compounds using chiral auxiliary approach

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Asymmetric catalysis for e.g. Sharpless’s Epoxidation, Dihydroxylation (AD)/Aminohydroxylation (AA) & Jacobsen’s hydrolytic kinetic resolution, and Reduction reactions (e.g. CBS catalyst and Noyori’s catalysis)

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Conventional resolution using acid/base approach

Puritanlabs offers specialist solid state services that are integrated with our other chemistry services, and focused on cutting lead times and ensuring processes are scalable. Our solid state services can be carried out in parallel with process development, or after, depending on your project needs.

Currently, a high percentage of drugs are formulated in solid dosage form. Thus, the need to understand, control and characterise the individual forms of a drug substance, particularly the polymorphic form, is vital. Each polymorph displays unique physicochemical properties that can affect bioavailability, manufacturability, stability and other performance characteristics of the drug.

Our solid state services are designed to gather information about your drug substance to give your project the best chance of success.

Our complete suite of capabilities includes:

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Crystallization Study – crystallize to obtain stable solids, for purification or isolation

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Material Characterization – polymorph identification

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Solubility Determination – in production solvents and buffer solutions

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Salt Selection – suitable form selection

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Polymorph Study – behavior in production solvents

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Crystallization Process Development – combine optimal synthesis conditions with optimal crystallization conditions

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Crystal Habit Optimization – control of particle size and shape