Drug Solid-State Research Service

Medicilon's pharmaceutical solid-state research service platform is dedicated to crystal form research services in the development of new drugs and generic drugs. It can provide salt form and polymorph screening, single crystal culture and structure analysis, crystallization process development, chiral separation and other services to assist global pharmaceutical research and development.

Solid-state research on drugs is an essential part of the drug research and development process. For innovative pharmaceutical companies, solid-state research is a magic weapon to promptly identify advantageous forms, expand the scope of patent protection, and extend the product life cycle. For generic pharmaceutical companies, solid-state research is expected to break through the patent barriers of original research, improve the technical content of products, and obtain market entry benefits. Therefore, developing the "right" solid form is a critical aspect of drug development.
Medicilon's pharmaceutical solid-state research service platform is dedicated to crystal form research services in the development of new drugs and generic drugs. It can provide salt form and polymorph screening, single crystal culture and structure analysis, crystallization process development, chiral separation and other services to assist global pharmaceutical research and development.

Services Capabilities

1. Salt and Polymorph Screening
Improve the key physicochemical properties of drugsImproving drugabilityIdentifying and deciding whether the uncharged molecule or a salt or a co-crystal should be developedForm selection and recommendationThe Layout and breakthrough of crystal patents
2. Single Crystal Culture and Structural Analysis
3D structureAbsolute configrurationCrystal structure confirmationSimulated XRPD pattern
3. Crystallization Process Development
Control of crystal form, crystal habit, and particle sizeYieldPhysical and chemical puritySolvent residue
4. Chiral Resolution
Selection of chiral resolution agentsSolvent selection
5. Qualitative and Quantitative Analysis of Crystal Forms
Qualitative and quantitative analysis of crystal forms of APIsQualitative analysis of crystal forms of start materials in preparations

Typical Steps for Solid-State Screening and Evaluation

Medicilon Solid-State Research Advantages

1. Senior Team with Extensive Experience
Medicilon solid-state researchers have extensive experience in salt form/eutectic screening, crystal form screening, and crystallization process development. The project leaders have all worked in the solid-state pharmaceutical industry for 5-10 years and are familiar with the regulatory requirements for drug crystal forms in the US and China’s registration regulations. In addition, they have experience in more than 50 projects and are able to formulate optimal screening strategies based on material properties.
2. Technical Expertise, Focus on Cutting-Edge
Medicilon is particularly good at the research and control of the solid form of drug molecules in raw materials and preparations. In addition, Medicilon actively seeks breakthroughs and innovations in the latest technologies and continuously explores cutting-edge solid-state research technologies.
3. Whole-Process Management and Control Optimization Strategy
From drug discovery to IND filing, one-stop pharmaceutical preclinical R&D services, Medicilon empowers the solid-state screening team with a more systematic crystal form (salt form) evaluation. The solid-state research team and the medicinal chemistry, formulation, PK, PD and other teams work together to follow the molecule and consider whether the crystal form needs to be changed based on comprehensive factors and iteratively optimize strategies to accelerate the research process of new drugs.

Partial case presentation, total of 100+

Case Studies

01 Case Study - Salt Screening
New Drug Project: MED220*
A foreign company has a compound in the preclinical stage. Since this compound has low solubility and cannot meet the in vivo exposure requirements, it is hoped to carry out salt screening work in order to select salt forms with better physical and chemical properties for subsequent development.
Screening Result
1. Select candidate salt forms based on the results of salt form screening and characterization, and factors such as ion safety level, polymorphic form, and thermal properties.
2. To further evaluate the hygroscopicity of candidate salt forms, the solid-state stability and solubility are comprehensively evaluated together with the free state, and the dominant salt type with suitable properties in all aspects is selected.
02 Case Study - Polymorph Screening
Project Code: MED2*33
A new drug development company wants to conduct a comprehensive polymorph screening for compounds in the preclinical stage, hoping to select crystals with better physicochemical properties for subsequent development.
Screening Result
1. A comprehensive polymorph screening test designed based on compound characteristics resulted in a total of 11 new crystalline forms and amorphous forms.
2. The new crystal forms discovered through physical and chemical property characterization and crystal form identification include 3 amorphous forms, 3 hydrates, 2 solvates, 3 metastable crystal forms and amorphous forms.
3. The results of the study on the crystalline transformation relationship show that the non-crystalline Form A is stable under specific water activity conditions at room temperature, has good physical and chemical stability, has almost no hygroscopicity, and has a solubility that meets development needs. It is recommended as the dominant crystal form for subsequent development and research.
03 Case Study - Particle Size Control
Project Code: XYM23*1M
The sample has small particle size, poor mobility and obvious electrostatic phenomenon, which leads to inconsistent dissolution behavior with the reference preparation in vitro and has a great impact on the preparation development. Therefore, develop new crystallization processes to increase particle size and meet formulation requirements.
Batch number Feeding weight Feeding weight(Solvent-1) Feeding weight (Solvent-2) Seed weight d90/μm Yield
009740-22-*** 25.0 g 108.1 g 39.2g 0.5% 136.29 92.8%
04 Case Study - Crystallization Process Development (Preparation of Crystalline State)
Project Code: MED23*3
The sample is a salt, amorphous foam solid, easy to absorption moisture into oil. Various crystallization methods have been tried, but crystals can not be obtained, which is not conducive to the subsequent process development and quality control. Therefore, it is urgent to develop a new crystallization process to prepare crystals.
05 Case Study - Single Crystalgrowing, Changing Crystal Habits
Project Code: MLP2*01
Conventional methods (slow volatilization, gas-liquid permeation, slow cooling, liquid surface diffusion, reaction crystallization, pH crystallization, hydrothermal crystallization, inorganic salt-mediated crystallization, polymer-mediated crystallization, etc), could not afford the single crystal for structure analysis.
Medicilon developed several special crystallization method based on compound structure analysis. Good single crystals were successfully obtained!