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Pharmaceutical Co-crystal technique


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Pharmaceutical Co-crystal technique

  2. 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. 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. 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. 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. 6. TYPE OF SOLID FORM Powerpoint Templates Page 6
  7. 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. 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. 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. 10. • Grinding method • Slurry Conversion method Solvent Crystal Stirring at R.T. Decantation Drying PXRD Powerpoint Templates Page 10
  11. 11. SUPERCRITICAL FLUID TECHNOLOGY Powerpoint Templates Page 11
  12. 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
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  14. 14. EVALUATION METHODS • PXRD (Powder X-rays diffraction study) • IR- Spectroscopic • Scanning Electron Microscope • Percentage Yield Powerpoint Templates Page 14
  15. 15. • Determination Of Melting Point • Solubility Analysis • Compatibility Studies (IR Spectroscopy) • In vitro drug release studies- Powerpoint Templates Page 15
  16. 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
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