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Salt/cocrystal Screening

The solid state of a given substance and its inherent properties have a profound impact in several crucial areas such as bioavailability, processability and physical/chemical stability. A series of fundamental features such as solubility, melting temperature or the presence of channels in the crystal structure can greatly affect drug development efforts. Therefore, it is very important to carry out reliable screening of salt-forming to select the optimal selection of final form for development. BOC Sciences is equipped with advanced facilities and skills to perform these studies. Our teams work with our customers to tailor a target profile for the desired solid state properties and screen for the best possible match. In addition, we provide reliable guidance on relevant development methods based on the final obtained characteristics, taking into account the product characteristics required for the actual project.

Advantages of salt/cocrystal screening

  • Efficient development of drug candidates
  • Improved bioavailability
  • Enhanced physicochemical properties

Salt/cocrystal ScreeningFigure 1. Various factors affecting the salt selection process. (Gupta, D.; et al. 2018)

Our Services

To make it easier and better for researchers, BOC Sciences provides salt/cocrystal screening service in a competitive fashion. We have provided a more efficient way to increase the number of new drugs, greatly shorten the R&D cycle, and reduce the development costs

  • BOC Sciences works to screen for optimal salt forms to improve the dissolution rate and oral bioavailability of APIs
  • Our team is able to identify and evaluate various salt forms of drug substances, selecting an optimal counterion early in the life cycle and reducing the chances of risk later in drug development
  • We help our clients improve the physical properties of APIs while retaining the benefits of the crystalline solid form

Salt/cocrystal screening process

1) Determine the required development properties and select appropriate counterions

2) Evaluate the physical stability of the salts

3) Study the physical and chemical properties of one or two major candidate salts and select one for the subsequent development

4) Salts are formed by the reaction of an acid with a base

5) Different types of evaporation and crystallization techniques are applied to prepare various salts of the compound of interest. In addition, various solvents with attributes conducive to the compound and the counterions can be manipulated to produce salts

Our strategies

  • BOC Sciences supports various analytical techniques to determine if the salt has actually formed including nuclear magnetic resonance, x-ray powder diffraction, thermal analysis, microscopy, and spectroscopy
  • Preparation and crystallization of all possible salt forms, assessment of crystallinity and water solubility, and selection of salts with acceptable crystallinity and solubility
  • Evaluation of thermal properties and hygroscopicity
  • Studies on the physical stability regarding polymorphs forms, pseudo-polymorphs forms or disproportionation
  • Assessment of bioavailability, chemical stability, compatibility and processability

Why choose BOC Sciences?

Our dedicated CMC team has provided tailored solutions to our clients from engagement to launch. With many years of industry experience, we provide clients with the following:

  • Comprehensive, integrated CMC services with a flexible service model that grows with your programs
  • Knowledgeable industry experts who deliver scalable, actionable insights
  • World-class facilities and equipment that remain at the forefront of the global pharmaceutical research, analytical and development standards
  • Our comprehensive services support products at every stage of the product lifecycle, from early-stage discovery to full commercial cGMP manufacture
  • A focus on risk management that is designed to ensure completion of your technical goals

BOC Sciences provides professional, rapid and high-quality services of salt/cocrystal screening at competitive prices for global customers. Personalized and customized services of salt/cocrystal screening can satisfy any innovative scientific study demands. Our clients have direct access to our staff and prompt feedback to their inquiries. If you are interested in our services, please contact us immediately!

Reference

  1. Gupta, D.; et al. Salts of Therapeutic Agents: Chemical. Physicochemical and Biological Considerations. 2018. 23.

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