Co-crystals: A Novel Approach to Improve the Solubility of Apixaban

Amit V Asati; Kishor S Salunkhe; Rudra Pratap Singh Rajput; Sonali R Chintamani; Akshay U Khairnar; Nilesh S Patil; Ravindra N Chintamani

doi:10.5530/ijpi.13.2.033

Amit V Asati Department of Pharmaceutics, Amrutvahini College of Pharmacy, Sangamner, Ahmednagar, Maharashtra, INDIA.
Kishor S Salunkhe Department of Pharmaceutics, Sanjivani College of Pharmaceutical Education and Research, Kopargaon, Maharashtra, INDIA
Rudra Pratap Singh Rajput Department of Pharmaceutics, Columbia Institute of Pharmacy, Raipur, Chhattisgarh, INDIA
Sonali R Chintamani Department of Pharmaceutics, MCE Society’s Allana College of Pharmacy, Pune, Maharashtra, INDIA.
Akshay U Khairnar Department of Pharmaceutics, Rajmata Jijau Shikshan Prasarak Mandal’s, Institute of Pharmacy, Pune, Maharashtra, INDIA.
Nilesh S Patil Department of Pharmaceutics, Rajmata Jijau Shikshan Prasarak Mandal’s, Institute of Pharmacy, Pune, Maharashtra, INDIA
Ravindra N Chintamani Department of Pharmaceutics, Rajmata Jijau Shikshan Prasarak Mandal’s, Institute of Pharmacy, Pune, Maharashtra, INDIA.

DOI: https://doi.org/10.5530/ijpi.13.2.033

Keywords: Apixaban, Co-crystal, Solubility, Oxalic acid

Abstract

Objectives: The current study work was aimed to improve the solubility of Apixaban by forming co-crystals. Materials and Methods: Two solvents mainly Dimethyl Sulphoxide (DMSO) and 2,2,2-trifluoroethanol were tried during the formulation of co-crystals. The other chemicals oxalic acid, adipic acid and L-Tartaric acid were used. Results: From the different trials it was concluded that oxalic acid and DMSO combination with the drug gave the better results for improvement in the solubility. Hence the batch F3 was analysed further. The melting point of F3 was found lower than pure drug. Drug content was found optimum as 95.06 ±0.65%. FTIR-spectra demonstrated the combined peaks of drug and oxalic acid. DSC thermogram showed the sharp endothermic peak similar to pure drug. SEM and XRD spectra confirmed the formation of co-crystals. Conclusion: It was found that formation of co-crystals of apixaban and oxalic acid was satisfactory and it was beneficial to improve the solubility of the apixaban.

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