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Development and Evaluation of Drug-cyclodextrin-polymer Ternary System Of Cefuroxime Axetil to Enhance the Solubility and Dissolution Efficiency


Affiliations
1 Government College of Pharmacy, Karad, 415124, Maharashtra,, India
2 School of Pharmacy, SRTM University, Nanded, 431606, Maharashtra,, India
3 Dr. D. Y. Patil Institute of Pharmaceutical Sciences and Research, Pimpri, Pune, 411018, Maharashtra,, India
     

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Cefuroxime axetil (CA) is BCS class II drug and has 55% absolute oral bioavailability due to poor aqueous solubility hence the present work is an attempt to enhance the solubility and hence dissolution of CA by inclusion complexation with natural Cyclodextrins (CDs). The complexation efficiency of Cyclodextrin is low and hence large amount of CDs are required to solubilize small amount of poorly water-soluble drug. To overcome this limitation the hydrophilic polymers were used to improve the complexation efficiency of cyclodextrin through the formation of ternary complexes. In association with water soluble polymers like Polyvinyl Pyrrolidone (PVP) and Hydroxy Propyl Methyl Cellulose (HPMC) the complexation potential CDs (β- CD and HP-β-CD) was found to be improved which was analyzed by comparative evaluation of binary (drug: cyclodextrin) and ternary system (drug:cyclodextrin:polymer). Binary and ternary complexes were prepared by lyophilization method. On the basis of physicochemical characterization techniques like TLC, FTIR, DSC, and XRPD, the complex formation between CA, CD and water-soluble polymers was confirmed. The dissolution rate studies were also carried out in order to assess the in-vitro performance of complexes. Drug-HP-β-CD-HPMC lyophilized system showed higher solubility and dissolution rate as compared to other systems.

Keywords

Cefuroxime axetil (CA), Cyclodextrins (CDs), Ternary complex, Hydroxy Propyl Methyl Cellulose (HPMC), Polyvinyl Pyrrolidone (PVP).
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  • Development and Evaluation of Drug-cyclodextrin-polymer Ternary System Of Cefuroxime Axetil to Enhance the Solubility and Dissolution Efficiency

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Authors

Ashok T. Jadhav
Government College of Pharmacy, Karad, 415124, Maharashtra,, India
Kishorkumar B. Burade
Government College of Pharmacy, Karad, 415124, Maharashtra,, India
Deepak A. Kulkarni
School of Pharmacy, SRTM University, Nanded, 431606, Maharashtra,, India
Sanjay S. Pekamwar
School of Pharmacy, SRTM University, Nanded, 431606, Maharashtra,, India
Shweta S. Kulkarni
Dr. D. Y. Patil Institute of Pharmaceutical Sciences and Research, Pimpri, Pune, 411018, Maharashtra,, India

Abstract


Cefuroxime axetil (CA) is BCS class II drug and has 55% absolute oral bioavailability due to poor aqueous solubility hence the present work is an attempt to enhance the solubility and hence dissolution of CA by inclusion complexation with natural Cyclodextrins (CDs). The complexation efficiency of Cyclodextrin is low and hence large amount of CDs are required to solubilize small amount of poorly water-soluble drug. To overcome this limitation the hydrophilic polymers were used to improve the complexation efficiency of cyclodextrin through the formation of ternary complexes. In association with water soluble polymers like Polyvinyl Pyrrolidone (PVP) and Hydroxy Propyl Methyl Cellulose (HPMC) the complexation potential CDs (β- CD and HP-β-CD) was found to be improved which was analyzed by comparative evaluation of binary (drug: cyclodextrin) and ternary system (drug:cyclodextrin:polymer). Binary and ternary complexes were prepared by lyophilization method. On the basis of physicochemical characterization techniques like TLC, FTIR, DSC, and XRPD, the complex formation between CA, CD and water-soluble polymers was confirmed. The dissolution rate studies were also carried out in order to assess the in-vitro performance of complexes. Drug-HP-β-CD-HPMC lyophilized system showed higher solubility and dissolution rate as compared to other systems.

Keywords


Cefuroxime axetil (CA), Cyclodextrins (CDs), Ternary complex, Hydroxy Propyl Methyl Cellulose (HPMC), Polyvinyl Pyrrolidone (PVP).

References