DEVELOPMENT AND OPTIMIZATION OF ORODISPERSIBLE TABLETS OF CARVEDILOL BY COMBINATION OF SUPER-DISINTEGRANTS ADDITION AND SUBLIMATION TECHNIQUES
Objective: Objective of the present research work was to prepare orodispersible tablets of carvedilol (CDL) for dysphagic patients.
Methods: Carvedilol, an anti-hypertensive drug, was chosen as a model drug in this study. Orodispersible tablets of carvedilol were prepared using different super-disintegrating agents such as crospovidone, croscarmellose sodium and sodium starch glycolate at different concentrations. The best formulation was selected based on disintegration and dissolution profile that was further taken for sublimation studies using camphor, menthol and thymol. Drug-excipients interaction studies were carried out by fourier transform infra-red (FTIR) spectrophotometer with pure drug sample and optimized formulation.
Results: The orodispersible tablet formulation having 4% croscarmellose sodium disintegrated in 92 sec. Hence this formulation was considered best formulation and taken further for sublimation studies. A formulation containing 10% w/w of menthol showed disintegration time of 16 sec with more than 96.64% drug release within 15 min. Menthol leaves the porous structure as it sublimates from the tablet. This might have contributed to the decrease in disintegration time. Hence, this formulation was considered optimized.
Conclusion: From this study, it can be concluded that orodispersible tablets of carvedilol may prove to be more efficacious in the treatment of hypertension particularly in dysphagic patients.
2. Punit BP, Rakshit CP, Dharmik MM, Pragna KS, Bhavesh SB. Quick dissolving films of nebivolol hydrochloride: formulation and optimization by a simplex lattice design. J Pharm Investign 2013;43:343â€“51.
3. Dixit AS, Parthasarathi KK, Hosakote GS. Gels and jellies as a dosage form for dysphagia patients: a review. Curr Drug Ther 2011;6:79-86.
4. COREG Â® [package insert]. NC: GlaxoSmithKline; 2015.
5. https://www.medicines.org.uk/emc/PIL.28229.latest.pdf. [Last accessed on 04 Nov 2016].
6. Kadria AE, Hassan MA, Afifi SA. Formulation and optimization of orodispersible tablets of flutamide. Saudi Pharm J 2014;22:53-61.
7. Sasidhar RC, Vidyadhara S, Deepti B, Nagaraju R, Satish KR. Formulation and optimization of orodispersible tablets containing an antidepressant. Pharm Lett 2014;6:156-64.
8. Aulton ME, Wells TI. Pharmaceutics: The science of dosage form design. Churchill Livingstone, London, England; 1998. p. 247-9.
9. Lachman L, Lieberman HA, Kanig JL. The theory and practice of industrial pharmacy. 3rd Ed. Varghese Publishing House, Mumbai; 1987. p. 293â€“9.
10. USP, NF. Asian edition, United States Pharmacopoeia Convention Inc; 2000. p. 1913â€“4.
11. Shirsand SB, Suresh S, Kusumdevi V, Swamy PV. Formulation design and optimization of fast dissolving clonazepam tablets by a sublimation method. Indian J Pharm Sci 2011;73:491-6.
12. Shinkar DM, Dhake AS, Setty CM. Development of UV spectrophotometric method for estimation of carvedilol in bulk and pharmaceutical formulations. Asian J Res Chem 2013;6:956-9.
13. Punna Rao R, Aditya N, Himanshu K, Srinivas M, Rahul V. Lipid nanoparticles for oral delivery of raloxifene: optimization, stability, in vivo evaluation and uptake mechanism. Eur J Pharm Biopharm 2014;87:114-24.
14. Bala R, Khanna S, Pawar P. Polymers in the fast disintegrating tablet a review. Asian J Pharm Clin Res 2011;5:8-14.
15. Guidance for Industry Orally Disintegrating Tablets. U. S. department of health and human services food and drug administration center for drug evaluation and research (CDER); 2008. Available from: http://www.fda.gov/downloads/Drugs/ GuidanceComplianceRegulatoryInformation/Guidances/ucm070578.pdf [Last accessed on 2016 Aug 12].
16. Ashok T, Veeravalli SK, Pavan KM, Roshitha B. Effect of effervescence in combination with super disintegrants in the formulation of propranolol HCL oral disintegrating tablets. Asian J Pharm Clin Res 2017;10:227-34.
17. Shivangi S, Navneet Verma. Taste masked orodispersible tablets: a highly patient complaint dosage form. Asian J Pharm Clin Res 2016;9:385-91.
18. Seema K, Megha S, Abhisek P. Ethylcellulose floating microspheres of antidiabetic agent: in vitro and in vivo evaluation. Int J Appl Pharm 2017;9:44-9.