EFFECT OF EFFERVESCENCE IN COMBINATION WITH SUPERDISINTEGRANTS IN THE FORMULATION OF PROPRANOLOL HCL ORAL DISINTEGRATING TABLETS
Objective: The current research work is intended to formulate propranolol HCl (PLH) as orally disintegrating tablet (ODT). It is also intending to check
the superiority in a combination of superdisintegrants and effervescent mixture than the use of superdisintegrants alone by a direct compression
technique. To fasten the onset of action and thereby enhancing the bioavailability of PLH in comparison to its conventional tablets.
Methods: Standard calibration curve of PLH was obtained in pH 6.8 phosphate buffer by spectrophotometric method, drug-excipient compatibility
studies were carried by Fourier transform infrared (FT-IR) studies. All the formulations were evaluated for pre and postcompression studies.
Accelerated stability studies were carried out up to 6 months for the optimized formulation, EF3.
Results and Discussion: Superdisintegrants used in the study are compatible with PLH. Pre- and post-compression parameters were within the
acceptable limits for all formulations. In vitro dissolution kinetic studies indicate the release of PLH from ODT increases as the concentration of
superdisintegrants as well as the ratio of citric acid: NaHCO3 of effervescent mixture increases. Formulations with an effervescent mixture are having
rapid disintegration and dissolution rate when compared to the formulations with superdisintegrants alone. The order of superdisintegrants in
enhancing the dissolution rate of PLH is crospovidone (CPV) > croscarmellose sodium (CCS) > sodium starch glycolate (SSG). Formulation, EF3 (10%
CPV and 1:3, citric acid: NaHCO3 ratio, respectively) had the highest dissolution efficiency at 10 minutes (DE10=82.74%); the first order dissolution
rate constant (K1=0.141/minutes) with a regression coefficient (r2=0.974) and lesser time for 90% of drug release (t90=4 minutes), was considered as
the optimal ODT in this study. Formulation EF3, passed the test for stability.
Conclusion: Hence, an effective PLH ODT was formulated by the direct compression technique with disintegration by combination of superdisintegrants
and effervescent mixture, will fasten the onset of action and enhances the bioavailability of PLH in comparison to its conventional tablets.
Keywords: Propranolol HCl, Orally disintegrating tablet, Sodium starch glycolate, Croscarmellose sodium, Crospovidone, Direct compression, In vitro
1. Sharma S, Gupta GD. Formulation and characterization of fast dissolving tablet of promethazine theoclate. Asian J Pharm 2008;2(1):70-2.
2. Siddiqui MN, Garima G, Sharma PK. Fast dissolving tablets: Preparation, characterization and evaluation. Int J Pharm Sci Rev Res 2010;4(2):87-96.
3. Velmurugan S, Vinushitha S. Oral disintegrating tablets: An overview. Int J Chem Pharm Sci 2010;1(2):1-12.
4. Guyot-Hermann AM. The disintegration and disintegrating agent. STP Pharm Sci 1992;2(6):445-62.
5. Colombo P, Caramella C, Conte U, Manna AL, Guyot-Hermann AM, Ringard J. Disintegrating force and tablet properties. Drug Dev Ind Pharm 1981;7:135-53.
6. Hirani JJ, Rathod DA, Vadalia KR. Orally disintegrating tablet: A review. Trop J Pharm Res 2009;8(2):161-72.
7. Ghosh T, Ghosh A, Prasad D. A review on new generation orodispersible tablets and its future prospective. Int J Pharm Pharm Sci 2011;3(1):1-7.
8. Available from: http://www.accessdata.fda.gov/drugsatfda_docs/label/2011/016418s080,016762s017,017683s008lbl.pdf.
Fig. 5: Dissolution profiles of accelerated stability samples of formulation EF3
Fig 4: Fourier transform infrared spectra of (a) propranolol HCl and (b) 45Â°C/75% relative humidity - 6 month sample of formulation EF3
Asian J Pharm Clin Res, Vol 10, Issue 3, 2017, 227-234
Ashok Thulluru et al.
9. Singh VK, Singh U, Raj T, Maurya JK, Choudhary N, Chauhan HS. Formulation and evaluation of MDT of propranolol HCl using different superdisintegrant. Am J PharmTech Res 2013;3(6):582-90.
10. Srikanth MV, Rao NS, Sunil SA, Ram BJ, Kolapalli VR. Statistical design and evaluation of a propranolol HCl gastric floating tablet. Acta Pharm Sin B 2012;2(1):60-9.
11. Derle D, Joshi O, Pawar A, Patel J, Jagadale A. Formulation and evaluation of buccoadhesive bi-layer tablet of propranolol hydrochloride. Int J Pharm Pharm Sci 2009;1(1):206-12.
12. Banker GS, Anderson NR, Lachman L, Liberman HA. The Theory and Practice of Industrial Pharmacy. 3rd ed. Mumbai: Varghese Publishing House; 1987. p. 293-4.
13. EDQM. European Pharmacopeia. 6th ed. Strasburg, France; EDQM Publications; 2007. p. 2435.
14. Comoglu T, Dogan A, Comoglu S, Basci N. Formulation and evaluation of diclofenac potassium fast-disintegrating tablets and their clinical application in migraine patients. Drug Dev Ind Pharm 2011;37(3):260-7.
15. Thulluru A, Ramesh KV, Dinakaran SK, Jana SK, Immanni R, Doddi P, et al. Formulation and evaluation of orally disintegrating tablet of Nimesulide. J Pharm Res 2012;5(6):3204-7.
16. Brahmankar D, Jaiswal SB. Biopharmaceutics and Pharmacokinetics: A Treatise. 2nd ed. New Delhi: Vallabh Prakashan; 2009. p. 254-5.
17. Available from: http://www.ich.org/fileadmin/public_web_site/about_ich/organisation/sadc/guideline_for_stability_studies.pdf.
18. Nagar P, Singh K, Chauhan I, Verma M, Yasir M, Khan A, et al. Orally disintegrating tablets: Formulation, preparation techniques and evaluation. J Appl Pharm Sci 2011;1(4):35-45.
19. Elkhodairy KA, Hassan MA, Afifi SA. Formulation and optimization of orodispersible tablets of flutamide. Saudi Pharm J 2014;22(1):53-61.
20. Patel HK, Chauhan P, Patel KN, Patel BA, Patel PA. Formulation and evaluation of effervescent tablet of paracetamol and ibuprofen. Int J Pharm Res Sch 2012;1(2):509-20.
The publication is licensed under CC By and is open access. Copyright is with author and allowed to retain publishing rights without restrictions.