TO FORMULATE AND STUDY THE RELEASE KINETICS OF RIVAROXABAN TABLETS USING CO-PROCESSED EXCIPIENTS

KOLWALKAR S; KENY S; SAWAIKAR L; JADHAV A

doi:10.22159/ajpcr.2025v18i11.56072

Authors

KOLWALKAR S Department of Pharmaceutics, PES’s Rajaram and Tarabai Bandekar College of Pharmacy, Ponda, Goa, India,
KENY S Department of Pharmaceutics, PES’s Rajaram and Tarabai Bandekar College of Pharmacy, Ponda, Goa, India https://orcid.org/0009-0001-7825-3409
SAWAIKAR L Department of Pharmaceutical Chemistry, PES’s Rajaram and Tarabai Bandekar College of Pharmacy, Ponda, Goa, India. https://orcid.org/0009-0001-0467-2352
JADHAV A Department of Pharmaceutical Chemistry, PES’s Rajaram and Tarabai Bandekar College of Pharmacy, Ponda, Goa, India. https://orcid.org/0000-0003-2771-6167

DOI:

https://doi.org/10.22159/ajpcr.2025v18i11.56072

Keywords:

Blood clot,, Co-processed excipient, Ludiflash®, Orodispersible tablets, Pearlitol® 200 SD Mannitol, PROSOLV® ODT G2, Rivaroxaban, Rivaroxaban: β-cyclodextrin complex

Abstract

Objectives: The current study aimed at designing, developing, and characterizing orodispersible tablets of Rivaroxaban for treating the blood clots, minimizing the chances of stroke and systemic embolism.

Methods: The tablets were prepared by the direct compression method using co-processed excipients (Prosolv® Oro dispersible tablets [ODT] G2, Ludiflash®, Pearlitol). A co-processed excipient is a particle engineering technique where multiple excipients merge at a sub-particle level with the objective to attain functionality improvement as well as masking of the undesirable properties.

Results: Various parameters such as thickness, weight variation, hardness, friability, dispersion time, wetting time, disintegration time, content uniformity, and in vitro drug release were evaluated. Fourier-transform infrared spectroscopy analysis revealed no drug-excipient interactions. The presence of sharp peaks in the X-ray diffraction patterns of Rivaroxaban confirms its crystalline nature. Differential Scanning Calorimetry Thermogram of the physical mixture corresponds to the melting point of Rivaroxaban and β-cyclodextrin, suggesting no physical and chemical interaction between the active and the complexing agent. Among all the formulations, FM2 showed the most promising results in terms of disintegration time of 72 Seconds and in vitro drug release of 97 Percent (%) within 20 minutes.

Conclusion: The study concludes that the orodispersible tablets of Rivaroxaban complexed with β-cyclodextrin can potentially enhance drug bioavailability and achieve rapid drug intervention.

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References

1. Kale MK, Wagh SA, Walunj AA, Dhage SS, Awari MS, Bhalekar SM, et al. Recent advances in oral solid dosage form formulation and development. Int J Pharm Sci. 2024;2(10):1075-91. doi: 10.5281/ zenodo.13955626

2. Debjit B, Chiranjib B, Krishnakanth P, Chandira MR. Fast dissolving tablet: An overview. J Chem Pharm Res. 2009;1(1):163-77.

3. Barde L, Suruse P, Agrawal S, Kalkotwar R, Sable V, Tare H. Design, development and fabrication[u1] of mouth-dissolving tablets containing extract of Tribulus terrestris for the treatment of hypertension. Int J Appl Pharm. 2023;15(3):234-41. doi: 10.22159/ijap.2023v15i3.47662

4. Jain HK, Nikam VK. Formulation development and stability indicating HPLC assay of tablets of apixabn. Int J Pharm Pharm Sci. 2017;9(10):24-32. doi: 10.22159/ijpps.2017v9i10.20343

5. Kaloge P, Kad T, Kale R, Kaloge R, More Y. Recent advancements in co-processed excipients. Int J Pharm Sci. 2025;3(1):1489-97. doi: 10.5281/zenodo.14688740

6. Alburyhi MM, Hamidaddin MA, Saif AA, Noman MA. Formulation and evaluation of Rivaroxaban orodispersible tablets. World J Pharm Pharm Sci. 2024;13(2):2066-92. doi: 10.20959/wjpps20242-26698

7. Mueck W, Schwers S, Stampfuss J. Rivaroxaban and other novel oral anticoagulants: Pharmacokinetics in healthy subjects, specific patient populations and relevance of coagulation monitoring. Thromb J. 2023;11(1):10. doi: 10.1186/1477-9560-11-10

8. Borse LB, Bendale AR, Borse LS, Naphade VD, Jadhav AG. Formulation and evaluation of mouth dissolving tablet Rivaroxaban and its validation. Biosci Biotechnol Res Asia. 2022;19(4):943-54. doi: 10.13005/bbra/3043

9. Patra RK, Acharya AK, Mahapati AK, Mallick S. Solubility enhancement of Rivaroxaban by solid dispersion with polyethylene glycol 4000. Int J Appl Pharm. 2023;15(2):78-85. doi: 10.22159/ ijap.2023v15i2.46687

10. Jaiswal S, Kanugo A. Design and development of fast-dissolving tablets of apixaban using single coprocessed excipient. Scopus Indexed. 2024;17(2):7217-26. doi: 10.37285/ijpsn.2024.17.2.2

11. Godbole AM, Somnache SN, Thakker SP, Iliger SR, Joshi AS, Patel BV. Formulation and in-vitro evaluation of sublingual tablets of ondansetron hydrochloride using coprocessed excipients. Indian J Pharm Educ Res. 2014;48 Suppl:7-17. doi: 10.5530/ijper.48.4s.2

12. Lakshmi Prasanna M, Prajna P, Chinnari P, Anusha P, Sri Harshini PN, Ratna PV. Formulation and evaluation of Rivaroxaban immediate release tablet. Int J Res Pharm Chem. 2022;12(1):129-38. doi: 10.33289/IJRPC.12.2.2022.12(20)

13. Solomon C, Anuța V, Sarbu I, Ozon EA, Musuc AM, Bratan V, et al. Enhancing the drug release and physicochemical properties of Rivaroxaban via cyclodextrin complexation: A comprehensive analytical approach. Pharmaceuticals (Basel). 2025;18(6):761. doi: 10.3390/ph18060761, PMID 40573162

14. Alburyhi MM, Hamidaddin MA, Noman MA, Saif AA, Yahya TA, Al-Ghorafi MA. Rivaroxaban-excipient compatibility studies for advanced drug delivery systems development. Eur J Pharm Med Res. 2024;11(9):370-404.

15. Bidkar SJ, Sadakal SU, Dama GY, Bidkar JS, Umalkar DG. Formulation development and evaluation of immediate release Rivaroxaban tablets. World J Pharm Pharm Sci. 2019;8(8):1669-83. doi: 10.20959/ wjpps20198-14586

16. Nadendla RR, Satynarayana J, Burri JK. Rivaroxaban: Compatibilty with pharmaceutical excipients using DSC and FTIR spectrophotometry. J Pharm Res Int. 2022;34(12):43-50. doi: 10.9734/jpri/2022/ v34i12A35554

17. Ahire PP, More YM, Kothawade VR. Formulation development and evaluation of famotidine orodispersible tablets. Res J Pharm Dosage Forms Technol. 2024;16(4):317-24. doi: 10.52711/0975- 4377.2024.00049

18. Patil IS, Patil OA, Bilaskar VV. Formulation and evaluation of orodispersible tablets of clopidogrel bisulfate using natural superdisintegrant. Indian J Novel Drug Deliv. 2018;10(1):17-23. doi: 10.20959/wjpr20246-31744

19. Gupta R, Jain N, Mishra S, Parveen S. Formulation and evaluation of apixaban tablet. Int J Novel Res Dev. 2024;9:80-6. doi: 10.54085/ ap.2024.13.1.96

20. Aglawe SB, Gayke AU, Sancheti VP, Metkar PS. Formulation and evaluation of mouth dissolving tablets of oxcarbazepine. World J Pharm Res. 2017;6(10):1130-7. doi: 10.20959/wjpr201710-9460

TO FORMULATE AND STUDY THE RELEASE KINETICS OF RIVAROXABAN TABLETS USING CO-PROCESSED EXCIPIENTS

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