Pharmaceutical Co-crystal technique
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Pharmaceutical Co-crystal technique






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    Pharmaceutical Co-crystal technique Pharmaceutical Co-crystal technique Presentation Transcript

    • 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
    • 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
    • • 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
    • 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
    • TYPE OF SOLID FORM Powerpoint Templates Page 6
    • 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
    • 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
    • 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
    • • Grinding method • Slurry Conversion method Solvent Crystal Stirring at R.T. Decantation Drying PXRD Powerpoint Templates Page 10
    • SUPERCRITICAL FLUID TECHNOLOGY Powerpoint Templates Page 11
    • 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
    • Powerpoint Templates Page 13
    • EVALUATION METHODS • PXRD (Powder X-rays diffraction study) • IR- Spectroscopic • Scanning Electron Microscope • Percentage Yield Powerpoint Templates Page 14
    • • Determination Of Melting Point • Solubility Analysis • Compatibility Studies (IR Spectroscopy) • In vitro drug release studies- Powerpoint Templates Page 15
    • 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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