pharmaceutical co-crystals
DESCRIPTION
TRANSCRIPT
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A Seminar On
Presented by:
Mr. Raviraj V. Jakapure
M. Pharm Ist Sem
Guided By:
Mr. S.P. Anantwar
Associate Professor (Pharmaceutics)
Department Of Pharmaceutics,
MVP Samaj’s College Of Pharmacy, Nashik
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CONTENTS
• Introduction• Design Of co-crystal• Physicochemical properties of co-crystal• Co-crystal formation methods• Co-crystal characterisation techniques• Marketed preparations• Conclusion• Reference
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INTRODUCTION
Solubility Enhancement Techniques
Salts, Solvates (Hydrates), Polymorphs And Co-crystal
Types of interactionAdvantages
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PHYSICOCHEMICAL PROPERTIES
o Melting pointo Stabilityo Solubilityo Intrinsic dissolutiono Bioavailability
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CO-CRYSTAL FORMATION METHODS
Solvent based Evaporation co-crystalisation Cooling crystalisation Slurry conversion Grinding method Neat grinding Liquid assisted grinding Antisolvent addition Supercritical fluid technology
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Slurry Conversion methodSolvent (100-200ml)
Crystal (20mg)
Stirring at R.T.
Decantation Drying PXRD
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CO-CRYSTAL CHARACTERISATION TECHNIQUES
Powder x-ray diffraction IR Raman spectroscopy DSC Scanning electron microscopy
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MARKETED PREPARATIONS
Carbamazepine (Tegretol®)Fluoxetine hydrochloride (Prozac®)Itraconazole (Sporanox®)AceclofenacIndomethacinTheophylline5-nitrouracil
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CONCLUSION
Number of pharmaceutical co-cryastals has been drammatically increased. Their NOVELTY, UTILITY, NONOBVIOUSNES co-crystal an intrasting approach from point of view of INTELLLECTUAL PROPERTY. Patent on co-crystal has commercial value.Pharmaceutical cocrystals are becoming increasingly important as an alternative way to improve the bioavailability of poorly watersoluble drugs, especially for these neutral compounds or those having weakly ionizable groups. Researchers have been putting much of their attention into exploring new cocrystals of an API. It is expected that many other pharmaceutical cocrystal systems will be explored in the near future. Meanwhile, there is an increasing need for a better understanding of the mechanism of the cocrystallisation process and theory for how pharmaceutical cocrystal improve the bioavailability of APIs.
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REFERENCES
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Ning Qiao, Mingzhong Li, Walkiria Schlindwein, Nazneen Malek, Angela Davies, Gary Trappitt . Int JPharm. 2011;419:1– 11
Guidence for Industry, Regulatory Classification of Pharmaceutical Co-Crystals, FDA, Center For Drug Evaluation And Research, December 2011
Orn Almarsson, Matthew L Peterson & Michael Zaworotko.The A to Z of Pharmaceutical Co-Crystals: A decade of fast moving new science and Patents. Pharm. Pat. Analyst.2012;1(3): 313-327
Abdul Amir H. Kadhum, Ahmed A. Al-Amiery, Hamdan A. Aday1, Yasamin K. Al-Majedy Ali A. Al-Temimi1, Redah I. Al-Bayati and Abu Bakar Mohamad.Co-crystal structure of mixed molecules. Int J Phy Sci March, 2012;7(10): 1564 - 1570, 2