Crystallization Technology Platform
Since more than 90% of drugs exist in the form of crystals, crystallization technology is widely used in the field of pharmaceutical production. BOC Sciences has rich experience in drug crystal form research. Our crystallization technology platform uses the most advanced instruments and equipment, and is in charge of a professional team of chemists, providing professional technical services such as crystal type screening and crystallization process development and optimization.
API Crystallization Process
For drug development, even the same drug component, under different crystal structures, will have different physical properties (such as solubility, water absorption, melting point). This directly leads to obvious differences in drug properties such as bioavailability and product stability. Therefore, in order to avoid various problems in the later analysis and testing and hinder the speed of product launch, detailed crystal type screening and investigation must be carried out in the early stage of drug development.
Our Crystallization Services
Solid-state Screening and Characterization
The solid-state form of the drug directly affects the solubility, dissolution rate, melting point, stability, tabletability and other properties of the active pharmaceutical ingredients, and these properties will further affect the efficacy of the drug. Therefore, it is necessary to use various experimental methods to obtain the various solid forms of drugs that may exist, use a variety of solid-state analysis techniques to characterize the physical and chemical properties of various forms, and use multi-disciplinary comprehensive methods to evaluate the performance of superior types of biopharmaceuticals to screen a superior drug crystal form suitable for production, high bioavailability, and favorable for preparations is produced. BOC Sciences can provide polymorph, salt, eutectic screening and amorphous dispersion screening. Our characterization and analysis instruments and equipment include X-ray powder diffractometer, differential scanning calorimeter, Raman microspectrometer, scanning electron microscope, etc., which can fully characterize the crystal form of the products.
Crystallization Process Development
The crystallization process plays a vital role in isolating active pharmaceutical ingredients (APIs) from mixtures. This is because crystallization purifies and separates the API from other components in the mixture, such as impurities and by-products. Determining the crystallization method, solvent system, controlling morphology, and crystal habit are very challenging. The size, shape, and purity of API crystals can be controlled through a customized crystallization process, which is important to ensure the quality and effectiveness of the final product. We provide process development for specific crystal types according to customer needs. Our crystallization technology includes conventional cooling crystallization, fusion crystallization and reaction crystallization, as well as spherical crystallization, ultrasonic crystallization, supercritical fluid crystallization, high-throughput crystallization, quasi-emulsification crystallization, micro-recrystallization, crystal mordant, etc. technology. We will first select the most stable crystal form for customers while ensuring product quality; then we will find the best crystallization process within the safe operating range.
Crystallization Process Optimization
The size and shape of the crystal particles can affect the performance of small molecule APIs in formulations. By optimizing crystallization, particle size and shape (size, density, morphology, hygroscopicity, static behavior, flowability, distribution and other particle properties) can be controlled to meet specific requirements for solubility, dissolution rate, and bioavailability. In addition, small molecule APIs can exist in different crystalline forms, which often have different physical and chemical properties. To address these issues, we can use different process parameters to determine the key factors that affect nucleation, including cooling temperature, stirring rate, seeding, degraders, and water activity. In the case that the crystallization process goal has been determined, different research methods are selected for different process goals. Our crystallization process optimization is generally carried out from the following six aspects:
Chiral separation is an important technology for enantioseparation in pharmaceutical industry. In drug development, the efficacy and safety of drugs may depend on the presence of specific enantiomers, and the presence of incorrect enantiomers may lead to adverse side effects or reduced efficacy. Therefore, in the crystallization of API, chiral resolution is used to separate the enantiomers of the API and produce a pure single enantiomer form. BOC Sciences can provide comprehensive chiral separation support to help customers understand the solid-state chemistry of racemates and enantiomers. We can perform crystal screening to find the best chiral resolution agent and crystal solvent, and develop HPLC analysis methods to determine enantiomeric excess. Then the absolute configuration of the enantiomeric pure compound was determined by single crystal X-ray diffraction. Our chiral separation ability is very comprehensive and can be customized according to the specific needs of customers in various industries such as pharmaceuticals, agricultural chemicals and fine chemicals.
What Can We Offer?
- Maximize process throughput
- Improve purity
- Control shape, form and particle size distribution
- Create processes suitable for transfer and scale-up
- Troubleshooting and optimization of process issues
- Strengthen intellectual property rights
- Method validation and transfer
In addition to the above services, we also provide customers with customized development of APIs and intermediates and non-GMP and GMP API manufacturing services. In addition, preclinical formulation development, compound solid state and physicochemical property analysis and overall solutions can also be obtained. If you are interested in our crystallization technology platform, please contact us immediately.