Crystalin Research
Our Services
Crystalin Research
API Characterization
Form Screen
PC/PK/PD Improvement
Phase Behavior
Patent Advice
Home Services Milestones Technical Labs Media Careers Contact Us


The Problem Facing the Pharmaceutical Industry?
About 80% of drugs are marketed as tablets and over 90% new drugs discovered in the last decade have polymorphs or hydrates. Over 50% of lead drug candidates fall off in R&D pipeline due to PC-PK-PD problems of low solubility and bioavailability, lack of stability in the pH/ temperature/ humidity range, difficulty of filtration, tablet compression, etc. Many drugs are marketed as a mixture of polymorphs and/or in variable hydration states and this creates inconsistent drug activity and composition for regulatory authorities.

The Answer is Pharmaceutical Cocrystals
A pharmaceutical cocrystal (PCC) is a hydrogen-bonded molecular complex of fixed stoichiometry between an API (drug molecule) and a coformer (CCF) selected from the GRAS/ EAFUS list of chemicals.

How the Problem Started?
With ever increasing number of patents being filed on closely related drug molecules, pharmaceutical companies are manipulating more complex molecular scaffolds, multi-functional molecules, and sensitive and/ or chiral centers, etc. to navigate the available patents space. These molecular features at times make it difficult to make salts, the most common method employed to increase solubility, stability and filterability of drugs. So what is the solution?

Advantages of Pharmaceutical Cocrystals as ICEs
The emphasis in the pharmaceutical industry has shifted from NCEs to ICEs (Improved chemical entities) to face the challenges in the current decade of patent cliffs. Pharmaceutical cocrystals will offer new improved medicines of drugs which were left aside in the past because of difficulties in salt formation due to (1) fragile sensitive chiral center in molecule, (2) degradation of drug in salt forming conditions, (3) lack of ionizable acidic/ basic functional groups at physiological pH, etc.

For More Info Download:
Tech Poster1
Tech Poster2
© 2012 All Rights Reserved. Powered by ONS, Optimization by ShopaMagic