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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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DESIGN OF CO-CRYSTALS

Crystal Engineering Supramolecular synthon

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PHYSICOCHEMICAL PROPERTIES

o Melting pointo Stabilityo Solubilityo Intrinsic dissolutiono Bioavailability

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STEPS FOR CO-CRYSTAL DESIGN AND PREPARATION

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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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Grinding method•Neat grinding•Liquid assisted grinding

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Slurry Conversion methodSolvent (100-200ml)

Crystal (20mg)

Stirring at R.T.

Decantation Drying PXRD

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Antisolvent addition methodAceclofenac

homogenizer

Chitosan + GAA

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SUPERCRITICAL FLUID TECHNOLOGY

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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

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THANK YOU