Generation of Carbamazepine:Nicotinamide cocrystals

by spraydrying

Presented By:

Mr. NITIN KANWALE M. Pharm (Semester 3rd, Quality

Assurance techniques)

MVP-SAMAJ’S COLLEGE OF PHARMACY, NASHIK.

INTRODUCTION

• Most of the NCES being generated, having a problem of poor 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.

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 Wohler in 1844.

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.

Does spray drying technique is efficient for production of cocrystal on large scale?

Cocrystal generation by liquid assisted grinding & their characterization

Powder X-ray diffraction Differential Scanning Calorimetry (DSC)Thermo gravimetric analysis (TGA)

Solubility Study And Transition Concentration Determination

Phase Solubility Diagram

Ternary Phase Diagram

Generation of cocrystals by spray drying and their characterization

a) Powder X-ray diffraction b) Differential Scanning Calorimetry

c) Scanning electron microscopy (SEM) d) Specific surface area

e) In vitro dissolution study

Conclusion

Though several cocrystallization techniques have been reported in literature, they pose challenges in scale up. In the present investigation, spray drying technique was successfully utilized for the generation of Carbamazepine:Nicotinamide (1:1) cocrystals. This study has also demonstrated the utility of phase solubility diagram (PSD) and ternary phase diagram (TPD) in depicting cocrystallization regions.

1) Shashank P. Patil, Sameer R. Modi, Arvind K. Bansal, Generation Of 1:1 Carbamazepine:nicotinamide Cocrystals By Spray Drying, European Journal Of Pharmaceutical Sciences 2014 Page No. 1-7.

2) Agrawal, S., Pancholi, S., Jain, N., Agrawal, G., 2004. Hydrotropic Solubilization Of Nimesulide For Parenteral Administration. Int. J. Pharm. 149–155.

3) Sanghvi, R., Evans, D., Yalkowsky, S.H., 2007. Stacking Complexation By Nicotinamide: A Useful Way Of Enhancing Drug Solubility. Int. J. Pharm. 35–41

References

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