Pharmaceutical Co-crystal technique
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This document discusses the co-crystal technique for enhancing the solubility of poorly water soluble drugs. It introduces co-crystals as crystalline materials comprised of an active pharmaceutical ingredient and one or more co-crystal formers. Co-crystals can improve solubility and bioavailability through interactions like hydrogen bonding and pi-stacking. The document outlines various methods for preparing co-crystals, including solution methods, grinding, and supercritical fluid technology. It also discusses selecting appropriate co-formers, solvents, and evaluation methods like powder X-ray diffraction and solubility analysis. Several marketed drug products incorporating co-crystal technology are presented as examples.
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Pharmaceutical Co-crystal technique
- 1. CO-CRYSTAL TECHNIQUE PRESENTED BY MANOJ KUMAR AMITY UNIVERSITY Powerpoint Templates Page 1
- 2. INTRODUCTION • Out of the 40% or more NCEs being generated, nearly 60% of them are poorly water soluble. • These poorly water soluble drugs having slow drug absorption leads to inadequate and variable bioavailability and gastrointestinal mucosal toxicity. • Therefore, enhancing the aqueous solubility of poorly water soluble drugs is a major challenge for the pharmaceutical researchers. Powerpoint Templates Page 2
- 3. PHARMACEUTICAL CO-CRYSTAL • Pharmaceutical co-crystals can be defined as crystalline materials comprised of an API and one or more unique co-crystal formers, which are solids at room temperature. • Co-crystals can be constructed through several types of interaction, including hydrogen bonding, π-stacking, and Van der Waals forces. • The first known co-crystal Quinhydrone, was studied by Friedrich Wöhler in 1844. Powerpoint Templates Page 3
- 4. • Co-crystals can be divided into: 1- Co-crystal anhydrates 2-Co-crystal hydrates (solvates) 3-Anhydrates of co-crystals of salts 4-Hydrates (solvates) of co-crystals of salts. Powerpoint Templates Page 4
- 5. ADVANTAGES OF CO-CRYSTAL 1- It is a stable crystalline form as compared to amorphous solid. 2- It can enhance the solubility of poorly water soluble drugs. 3- It can also enhance the bioavailability due to increased solubility. 4- Co-crystal formation technique may be used for purification steps. Powerpoint Templates Page 5
- 6. TYPE OF SOLID FORM Powerpoint Templates Page 6
- 7. CO-FORMERS• Co-formers are the most important components of the co-crystal. • The co-crystal formation is based on the structure of the co-formers. • The solubility of co-crystal is also depends on the solubility of the co-formers. • Some examples like ascorbic acid, gallic acid, nicotinamide, citric acid , aglutamic acid, histidine, urea, saccharine, glycine,tyrosine,valine. Powerpoint Templates Page 7
- 8. SOLVENTS• Solvents are also important ingredients of co-crystal formation. • The co-crystal formation is also depend on the selection of solvents. • Selection of solvents depend on the solubility of drug and co-formers. • Some example of solvents used in co-crystal formation like-ethanol, methanol, acetonitrile and others organic solvents. Powerpoint Templates Page 8
- 9. METHODS OF CO-CRYSTAL PREPARATION1-SOLUTION METHODS• Evaporative co-crystallization • Cooling crystallization • Reaction crystallization 2-GRINDING METHOD • Neat/Dry grinding method • Liquid assisted grinding method 3-ANTISOLVENT METHOD 4-SLURRY CONVERSION METHOD 5-SUPERCRITICAL FLUID TECHNOLOGY Powerpoint Templates Page 9
- 10. • Grinding method • Slurry Conversion method Solvent Crystal Stirring at R.T. Decantation Drying PXRD Powerpoint Templates Page 10
- 11. SUPERCRITICAL FLUID TECHNOLOGY Powerpoint Templates Page 11
- 12. STEPS INVOLVED IN FORMATION OF CO-CRYSTAL• Selection of API • Selection of co-former • Empirical and theoretical guidance • Co-crystal screening • Co-crystal characterization • Co-crystal performation Powerpoint Templates Page 12
- 14. EVALUATION METHODS • PXRD (Powder X-rays diffraction study) • IR- Spectroscopic • Scanning Electron Microscope • Percentage Yield Powerpoint Templates Page 14
- 15. • Determination Of Melting Point • Solubility Analysis • Compatibility Studies (IR Spectroscopy) • In vitro drug release studies- Powerpoint Templates Page 15
- 16. MARKETED PREPARATION• Pharmaceutical co-crystals of carbamazepine (Tegretol® ) • Pharmaceutical co-crystals of fluoxetine hydrochloride (Prozac® ) • Pharmaceutical co-crystals of itraconazole (Sporanox® ) • Pharmaceutical co-crystals of sildenafil (Viagra® ) • Co-crystal of melamine and cyanuric acid • Co-crystals of theophylline • Co-crystals of aceclofenac • Co-crystal of 5-nitrouracil Powerpoint Templates • Co-crystals of indomethacin Page 16