Process Department Solid Form Screening Platform

The solid screening platform of Medicilon process department strictly complies with the registration regulations and regulatory requirements of China NMPA, FDA and other regulatory authorities, studies and controls the solid morphology of drug molecules in API and preparations, and can formulate the optimal screening strategy according to the material characteristics, including but not limited to crystallization method, solvent selection and ion selection.

The Importance of Solid Form Screening
The solid form screening of APIs is an important tool in the early process development of new drugs. The purpose is to find as many crystal forms as possible and determine the most suitable solid form for development, so that you can:
Improve the Quality of DrugsThere are significant physical and chemical differences between different polymorphs of the same drug (hygroscopicity, physical/chemical/mechanical stability, purity and impurities). This could lead to differences in solubility, dissolution rate and bioavailability, which directly affect the quality of the final product.Optimize Intellectual PropertyAs a material structure patent, crystal form is an effective tool for prolonging the life cycle of new drugs. For generic drugs, it can break through the patent barriers of the original research and obtain the right to enter the market.Compliance with Registration RegulationsThe drug regulatory laws and regulations of China, US and other developed countries have set clear requirements for the content of crystal form research in new drug clinical trial applications, new drug marketing applications, and generic drug applications, and have formulated relevant guiding principles for crystal form research.
The solid form screening platform of Medicilon Process Department strictly complies with the registration regulations and regulatory requirements of China’s NMPA, the US FDA and other regulatory agencies. It conducts research and control on the solid form of drug molecules in APIs and preparations, and can formulate the best effect based on the characteristics of the substance screening strategies, including but not limited to crystallization methods, solvent selection, and ion selection.
Service Scope of Solid Form Screening Platform
DiscoveryVarious Salt Forms/Crystal Forms/Eutectic of APIEvaluationThe Druggability of Different Crystal Forms of API DevelopmentThe API crystallization production process to obtain the target crystal form, morphology and particle size

Salt Screening

Purpose
Improve Drug PropertiesDiscover the Most Suitable Salt Type for DevelopmentEnsure Effective Patent ProtectionAvoid Prior Technology Patents
Technology
Free State Property CharacterizationSolubility in Different SolventsChoose the Right Counter IonVarious Salt-Forming TechnologiesCharacterization of Physical and Chemical PropertiesSolid and Solution Stability ResearchSalt Type Selection and RecommendationPatent Disclosure Materials
Salt Type Screening Process
Thermal Analysis (TGA/DSC): Solvent (water) and Non-Solvate Analysis
No Crystal Type
Solvent (water) Compound
Dynamic Moisture Sorption (DVS) Applications – Inspection of Sample Moisture Absorption

Eutectic Screening

Purpose
Improve the Defects of the Free State PropertyDiscover the Most Suitable Eutectic Form for DevelopmentEnsure Effective Patent ProtectionAvoid Prior Technology Patents

Polymorph Screening

Purpose
Discover the Most Suitable Crystal Form for DevelopmentEnsure Effective Patent ProtectionAvoid Prior Technology Patents
Technology
Analysis of Existing TechnologiesMultiple Crystallization TechniquesCharacterization of Physical and Chemical PropertiesSolid and Solution StabilityAnalysis of the Relative Stability of PolymorphsCrystal Type Selection and RecommendationPatent Disclosure Materials
Polymorph Screening Process
Characterization→Scheme Design→Screening→Enlarge→Evaluation→Report Patent

Development and Verification of Qualitative, Quantitative and Limit Analysis Methods

Raw Material Crystallinity or Impurity Crystal Type AnalysisQualitative and Quantitative Analysis of Crystal Forms of Raw Materials in PreparationsDevelopment and Verification of Particle Size Distribution Analysis Method
X-Ray Powder Diffraction Method (XRPD)
Crystallinity Check
Qualitative Analysis of Crystal Forms of Raw Materials in Preparations

FAQs

Why does the API for Crystal Structures Screening Require Sample Purity?

Impurities can affect their dynamic stability in solution and suspension by affecting nucleation and growth rates. Therefore, the screening of polymorph with earlier batches of APIs still containing many impurities may yield different results than screening with later, purer batches. In unfortunate cases, significant forms may not be found in the initial screening. Therefore, it is recommended to repeat the polymorph screening at least several times for a batch of APIs with impurity characteristics of the product to be marketed produced by the final GMP procedure.
What are Polymorphs?

In July 2007, the United States FDA issued the technical guidelines for generic drug crystal research, pointing out that polycrystalline polymorph includes crystal or amorphous, as well as solvates and hydrates, which are described as follows:
(1) In the crystal state, the molecules have different arrangements or conformations in the lattice;
(2) In the amorphous state, the arrangement of molecules is not regular, and there is no identifiable lattice;
(3) Solvent is the crystal lattice containing equivalent or non-equivalent solvent. If the solvent is water, the solvent is usually called hydrate