FORMULATION AND IN VITRO EVALUATION OF RAMELTEON TABLETS FOR COLON DRUG DELIVERY SYSTEM BY COMPRESSION COATING

  • TRINADHA RAO M. Department of Pharmaceutics, Vignan Institute of Pharmaceutical Technology, Duvvada, Visakhapatnam 530049, India
  • PARIMALA Y. Department of Pharmaceutics, Vignan Institute of Pharmaceutical Technology, Duvvada, Visakhapatnam 530049, India
  • YAMINI M. Department of Pharmaceutics, Vignan Institute of Pharmaceutical Technology, Duvvada, Visakhapatnam 530049, India
  • PHANINDRA CVS Department of Pharmaceutics, Vignan Institute of Pharmaceutical Technology, Duvvada, Visakhapatnam 530049, India
  • SRINIVASA RAO Y. Department of Pharmaceutics, Vignan Institute of Pharmaceutical Technology, Duvvada, Visakhapatnam 530049, India

Abstract

Objective: Ramelteon, is a sleep agent that selectively binds to the MT1 and MT2 receptors in the suprachiasmatic nucleus (SCN), instead of binding to GABAA receptors. In the present research work, the formulation of ramelteon targeted to colon by using various polymers developed.


Methods: Colon-targeted tablets were prepared in two steps. Initially, core tablets were prepared and then the tablets were coated by using different pH dependent polymers. Ethylcellulose, Eudragit RLPO and L100 were used as enteric coating polymers. The precompression blend of all formulations was subjected to various flow property tests and all the formulations were passed the tests. The tablets were coated by using polymers and the coated tablets were subjected to physical characterization, drug content, in vitro drug release and kinetics of drug release.


Results: Among all the formulations, F4 formulation was found to be optimized as it was retarded the drug release up to 18 h and showed maximum of 99.25% drug release. It followed the first-order kinetics mechanism. All the formulations having Korsmeyer-Peppas ‘n’ values are in the range of 0.540 to 0.818. Hence, it was concluded that the prepared formulations followed non-Fickian diffusion.


Conclusion: An effective and stable remelteon colon targeted formulation developed for treating insomnia.

Keywords: Ramelteon, Colon targeted drug delivery system, Ethylcellulose, Eudragit, RLPO, Eudragit L 100

References

1. Gadhave MV, Shevante Trupti B, Takale Avinash A, Jadhav SL, Gaikwad D. Formulation and evaluation of colon targeted drug delivery of mesalamine. Int J Pharm Clin Res 2017;9:26-34.
2. Siamidi A, Vlachou M, Efentakis M. New dosage forms for the delayed release of mesalazine to the colon. Int J Appl Pharm 2020;12:192-6.
3. Washington N, Washington C, Wilson CG. Physiological pharmaceutics: barriers to drug absorption. Taylor Francis 2001;10:144-9.
4. Bharat W Tekade, Umesh T Jadhao, Vicky R Vig, Vijay R Patil. Formulation and evaluation of colon-specific drug delivery system using Boswellia serrata gum. Pharma Innovation 2017;6:277-83.
5. Rajesh K, Deveswaran R, Bharath S, Basavaraj BV. Development of mesalazine microspheres for colon targeting. Int J Appl Pharm 2017;9:1-9.
6. Jagan Baheka, Shailesh Wadher. Formulation development of colon targeted mesalamine pellets: in vitro-in vivo release study. Int J Appl Pharm 2019;11:132-5.
7. Sajaymitra GN, K Ganesh. Dissolution and solubility enhancement strategies: current and novel prospectives. JCR 2018;5:1-10.
8. Sirisha VN, Eswariah MC, Rao AS. A novel approach of locust bean gum microspheres for colonic delivery of mesalamine. Int J Appl Pharm 2018;10:86-93.
9. Goyal N, A Kumar. Formulation and in vitro evaluation of salbutamol sulphate and theophylline extended-release tablets using modified polymers. Int J Pharm Sci 2018;10:67-71.
10. Rawoof MD, Rajnarayana K, Ajitha M. Formulation and evaluation of ph-dependent colon-targeted tablets of rifaximin by design of an experiment. Asian J Pharm Clin Res 2019;12:249-54.
11. Purushothaman M. Kalvimoorthi formulation and evaluation of colon targeted drug delivery system of flurbiprofen using HPMC and K4M sodium alginate as polymeric carrier. Int J ChemTech Res 2017;10:156-68.
12. Biresh Kumar Sarkar, Jain DA, Vikram Sharma. Formulation and evaluation of flurbiprofen matrix tablets for colon targeting. Int J Pharma Chem Sci 2012;1:95-9.
13. Wu, Z Chen, X Wei, N Sun, Y Lu, W Wu. Biphasic release of indomethacin from HPMC/pectin/calcium matrix tablet: I. Characterization and mechanistic study. Eur J Pharm Biopharm 2007;67:707–14.
14. Ravi, S Siddaramaiah, TM Pramod Kumar. Influence of natural polymer coating on novel colon targeting drug delivery system. J Mater Sci Mater Med 2008;19:2131–6.
15. Talukder, R Fassihi. Development and in vitro evaluation of a colon-specific controlled release drug delivery system. J Pharm Pharmacol 2008;60:1297–303.
16. Udayasree Konikuru, Rajavel P, Vijitha S. Bioequivalence studies of marketed clozapine tablets by using optimized validated liquid chromatographic method. Int J Curr Pharm Res 2018;10:47-51.
17. Rao MT, Vijaya Ratna J, Srinivasa Rao Y, Hemant Kumar T. Development and validation of RP-HPLC method for the determination of itraconazole in bulk and capsule dosage form. Int J Pharm Sci Rev Res 2015;31:221-5.
18. Vemula P, R Veerareddy. Formulation, evaluation and pharmacokinetics of ketorolac tromethamine time-dependent colon targeted drug delivery system. Expert Opin Drug Delivery 2013;10:33–45.
19. Pena R, Verain. Analysis of different parameters of an optimized prolonged-release formulation obtained by five processes. Pharma Technol Con Drug Release Ellis Horwood London 2005;2:57-70.
20. Costa P, Manuel J, Lobo S. Modeling and comparison of dissolution profiles. Eur J Pharm Sci 2001;13:123-33.
21. Korsmeyer RW, Peppas NA, Gurney R, Deckar B, Buri PP. Mechnism of solute release from porous hydrophilic polymers. Int J Pharm 1983;15:35-9.
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M., T. R., Y., P., M., Y., CVS, P., & Y., S. R. (2021). FORMULATION AND IN VITRO EVALUATION OF RAMELTEON TABLETS FOR COLON DRUG DELIVERY SYSTEM BY COMPRESSION COATING. International Journal of Applied Pharmaceutics, 13(2), 249-253. https://doi.org/10.22159/ijap.2021v13i2.40396
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