Academic and Public Partnerships in Solid-State Chemistry - Pharmaceutical Technology

Latest Issue
PharmTech

Latest Issue
PharmTech Europe

Academic and Public Partnerships in Solid-State Chemistry
Solid-state chemistry is an important part of drug development, and public research is advancing the field.


Pharmaceutical Technology
Volume 37, Issue 5, pp. 56

Although the actual synthesis of an API is crucial, it is not the exclusive consideration in API development. In addition to producing an API with high purity, yield and stereoselectivity, an API must be able to remain stable during storage and distribution and have the desired drug mechanism once administered to a patient. Solid-state chemistry is an important part of drug development, and public research is advancing the field.

Researchers at the Institute of Chemical and Engineering Sciences (ICES) at Singapore's Agency for Science, Technology, and Research (A*STAR) recently reported on a novel method for producing cocrystals. The researchers discovered that adding water droplets can help form cocrystals of caffeine. Caffeine is unstable to humidity and cocrystal formation is possible with biocompatible compounds such as 4-hydroxybenzoic acid (4HBA). Previous research showed that computer models could predict cocrystals of caffeine and 4HBA in the ratio of 1:1, which would be the form with the most stable structure. To date, researchers had only been able to produce 2:1 and 1:2 co-crystals, according to information from A*STAR (1).

The ICES researchers successfully formed 1:1 cocrystals of caffeine and 4HBA in the form of a monohydrate. By grinding together a 1:1 mixture of the two components with two drops of water, a crystal structure was formed in which each pair of crystallization partners is partly held together by a water molecule. The key to the water's ability to produce the 1:1 cocrystal is its capacity to both donate and accept hydrogen bonds, the intermolecular force that holds cocrystals components together. In the case of the caffeine-4HBA cocrystal hydrate, unused hydrogen-bond acceptors and donors are satisfied by forming hydrogen bonds with the water molecule. Without water, the number of hydrogen-bond donors and acceptors is unbalanced, resulting in the preferential formation of the 2:1 and 1:2 crystals instead, according to the A-STAR information. The researchers have also applied the process to other APIs. They generated a 1:1 cocrystal hydrate of 4HBA with piracetam, a cognitive-enhancing drug. The results suggest that forming hydrates offers an alternative way to generate cocrystals with particular ratios of constituents, expanding the options for forming pharmaceutical materials.

The Synthesis & Solid State Pharmaceutical Center (SSPC) at the University of Limerick in Ireland was recently one of seven research centers that received part of an EUR 300 million ($391 million) investment through the Science Foundation Ireland's (SFI) Research Centers Program. SFI is the national research foundation in Ireland, and the funding represents funding from both SFI and private funding from industry. SSPC is a collaboration between 17 companies and academic institutions. These groups have expertise in process modelling and design, scale-up, computational fluid dynamics, in situ solution and solid-phase monitoring, crystallography and powder characterisation. The center's goal is to rationally design solid-state pharmaceutical materials in the required physical and chemical forms for advanced formulation and drug-delivery systems.

Reference

1. S. Aitipamula et al., Cryst. Eng. Comm. 14 (7), 2381–2385 (2012).

ADVERTISEMENT

blog comments powered by Disqus
LCGC E-mail Newsletters

Subscribe: Click to learn more about the newsletter
| Weekly
| Monthly
|Monthly
| Weekly

Survey
FDASIA was signed into law two years ago. Where has the most progress been made in implementation?
Reducing drug shortages
Breakthrough designations
Protecting the supply chain
Expedited reviews of drug submissions
More stakeholder involvement
Reducing drug shortages
70%
Breakthrough designations
4%
Protecting the supply chain
17%
Expedited reviews of drug submissions
2%
More stakeholder involvement
7%
View Results
Eric Langerr Outsourcing Outlook Eric LangerRelationship-building at Top of Mind for Clients
Cynthia Challener, PhD Ingredients Insider Cynthia ChallenerRisk Reduction Top Driver for Biopharmaceutical Raw Material Development
Jill Wechsler Regulatory Watch Jill Wechsler Changes and Challenges for Generic Drugs
Faiz Kermaini Industry Insider Faiz KermainiNo Signs of a Slowdown in Mergers
CMOs and the Track-and-Trace Race: Are You Engaged Yet?
Ebola Outbreak Raises Ethical Issues
Better Comms Means a Fitter Future for Pharma, Part 2: Realizing the Benefits of Unified Communications
Better Comms Means a Fitter Future for Pharma, Part 1: Challenges and Changes
Sandoz Wins Biosimilar Filing Race
Source: Pharmaceutical Technology,
Click here