What is Polymorphic Screening
Polymorphism refers to a single chemical entity's capability to form two or more crystalline phases. Understanding the polymorphic nature of your product is crucial for obtaining US FDA approval of your NDA. Selecting the optimal solid form for manufacturing is critical, as the polymorphic form can significantly affect physical characteristics, leading to reduced bioavailability.
Raleigh Molecular offers advanced screening of polymorphic forms for any API of interest using state-of-the-art analyses such as DSC, XRPD, FTIR, and dissolution/solubility testing. This allows us to determine the most suitable polymorphic form for your product. Additionally, we can identify additional polymorphs for intellectual property (IP) protection purposes, thereby supporting your filing process.
i) Polymorphs exhibit varying physicochemical properties such as solubility, dissolution rate, and melting point, which can impact their biological activity, pharmacodynamic properties, and stability. As a result, drug regulators consider polymorphic forms of an API to be distinct chemical entities.
ii) Your product’s current polymorphic form may not be thermodynamically stable, and during drug product formulation or storage, it may transform into another polymorph. Such transformations could potentially lead to rejection of the API or the dosage form product.
iii) Polymorphic forms are eligible for intellectual property (IP) protection. Innovator companies identify polymorphs in the active pharmaceutical ingredient (API) to safeguard the associated IP rights of a new API, thereby preventing premature competition from generic companies.
iv) Generic companies aim to identify viable polymorphic forms of drugs that are not covered by innovator patents. This allows them to develop and launch a non-infringing generic version of the product.
In numerous cases, crystalline polymorphs may not exhibit adequate aqueous solubility, necessitating the use of the amorphous form. Raleigh Molecular possesses extensive expertise in various techniques employed to induce the amorphous forms of active pharmaceutical ingredients.
Raleigh Molecular offers comprehensive polymorphic screening services, leveraging our deep knowledge and experience in this field. Our screening process typically involves analyzing different forms induced by various methods such as different solvent types, slow and fast evaporation, slow and fast crystallization, thermal treatments, and physical techniques like grinding. We utilize XRPD as an initial study method for polymorphic forms, followed by additional analyses including DSC, FTIR, Melting Point determination, and normal and accelerated stability studies. Furthermore, we conduct dissolution and solubility studies to provide you with all the necessary data, enabling you to make informed decisions regarding the desired polymorph for your API drug substance.
©2014-2024 Raleigh Molecular Laboratories – All Rights Reserved.