Formulation Development and Evaluation of Mucoadhesive Buccal Tablets of Acebutolol Hydrochloride

  • Priyanka Dilip Chaudhari Department of Quality Assurance, Sandip Institute of Pharmaceutical Sciences, Mahiravani, Nashik, Maharashtra, India
  • Amol Bhalchandra Deore Department of Pharmacology, MVP Samaj’s Institute of Pharmaceutical Sciences, Adgaon, Nashik, Maharashtra, India
  • Manoj Jagannath Jagtap Department of Pharmaceutics, MGV’s Institute of Industrial and Pharmaceutical Technology, Nashik, Maharashtra, India
  • Devanshi Sunil Gupta Department of Pharmaceutics, MGV’s Institute of Industrial and Pharmaceutical Technology, Nashik, Maharashtra, India

Abstract

A mucoadhesive drug delivery system is an oral dosage form, where the tablet, gel, or patch is attached to the buccal region for direct absorption of the drug into blood circulation. This dosage form has been employed to improve the bioavailability of drugs that undergoes significant hepatic first-pass metabolism. Acebutolol is a beta sympatholytic agent used to treat high blood pressure and irregular heartbeat (arrhythmia). Lowering high blood pressure helps prevent strokes, heart attacks, and kidney problems. In present investigation, mucoadhesive buccal tablets of acebutolol HCl were prepared using carbopol 940 in varying concentrations with secondary polymer xanthan gum by direct compression method. Nine batches were prepared as per 32 factorial designs, to investigate the combined effects of independent variables namely carbopol 940 and xanthan gum on dependant variables namely swelling index, mucoadhesion strength and in-vitro drug release using design expert software version 8.0.7.1. Preformulation studies confirmed the identity and purity of the drug by means of UV spectroscopy, IR spectroscopy, DSC analysis, and melting point determination. The tablets were evaluated for hardness, thickness, weight variation, friability, and drug content concluded that all these parameters were in an acceptable range of pharmacopoeial specification. The buccal tablets were studied for surface pH, swelling index, in vitro drug release study, adhesion force, in vitro mucoadhesive strength, stability, and compatibility study to optimise the formula. Amongst all factorial batches (F1 to F9), batch F5 (30 mg carbopol 940 and 30 mg xanthan gum) showed maximum drug release of 99.96 % after 12 hr of study and also showed better contact with biological membrane. The drug release kinetics of batch F5 was found to be best fitted to zero order kinetic model and exhibited anomalous diffusion release mechanism. The formulation F5 exhibited good correlation (R2=0.992) for in-vitro drug release. All the evaluation parameters give positive results and comply with the standards. Stability studies were carried out on the developed formulations indicating that the formulations were stable during the period of 6 months. In conclusion, the formulation F5 is stable and effective for quick action and seems to be alternative to the conventional tablet.


 

Keywords: Acebutolol, Mucoadhesive, Buccal, Polymer, Swelling Index

Downloads

Download data is not yet available.

Author Biographies

Priyanka Dilip Chaudhari, Department of Quality Assurance, Sandip Institute of Pharmaceutical Sciences, Mahiravani, Nashik, Maharashtra, India

Department of Quality Assurance, Sandip Institute of Pharmaceutical Sciences, Mahiravani, Nashik, Maharashtra, India

Amol Bhalchandra Deore, Department of Pharmacology, MVP Samaj’s Institute of Pharmaceutical Sciences, Adgaon, Nashik, Maharashtra, India

Department of Pharmacology, MVP Samaj’s Institute of Pharmaceutical Sciences, Adgaon, Nashik, Maharashtra, India

Manoj Jagannath Jagtap, Department of Pharmaceutics, MGV’s Institute of Industrial and Pharmaceutical Technology, Nashik, Maharashtra, India

Department of Pharmaceutics, MGV’s Institute of Industrial and Pharmaceutical Technology, Nashik, Maharashtra, India

 

Devanshi Sunil Gupta, Department of Pharmaceutics, MGV’s Institute of Industrial and Pharmaceutical Technology, Nashik, Maharashtra, India

Department of Pharmaceutics, MGV’s Institute of Industrial and Pharmaceutical Technology, Nashik, Maharashtra, India

 

References

1. Shaikh R, Thakur RRS, Garland MJ, Woolfson AD, Donnelly RF, Mucoadhesive drug delivery systems, J Pharm Bioallied Sci. 2011; 3(1):89-100.
2. Madhav N.V., Shakya A.K., Shakya P., Singh K. Orotransmucosal drug delivery systems: a review. J. Contr. Release. 2009;140(1): 2-11.
3. Smart J.D. Buccal drug deliveryExpet. Opin. Drug. Deliv.2005; 2(3):507-517.
4. Shanker G., Kumar C.K., Gonugunta C.S.R., Kumar B.V., Veerareddy P.R. Formulation and evaluation of bioadhesive buccal drug delivery of tizanidine hydrochloride tablets AAPS Pharm Sci Tech. 2009;10(2):530-539.
5. B. Çelik. Risperidone mucoadhesive buccal tablets: formulation design, optimization and evaluation. Drug Des. Dev. Ther. 2017;11: 3355-3365.
6. Boddupali B.M., Mohammed Z.N.K., Nath R.A., Bhanji D. Mucoadhesive drug delivery system: an overview. J. Adv. Pharm. Technol. Res. 2010;1(4):381-387
7. Brunten L., Parker K., Blumenthal D., Buxton I. Goodman & Gilman’s Manual of Pharmacology and Therapeutics, 11th edition, Mcgraw-Hill, 2008, pp.179.
8. Bertram G. Katzung- Basic & Clinical Pharmacology. 9thEdition, McGraw-Hill Education / Medical, 2004, pp.211.
9. Gary C. Rosenfeld, David S. Loose. BRS Pharmacology, 6th edition, Lippincott Williams & Wilkins, a Wolters Kluwer business, 2014, pp.88.
10. Carl A.Gruetter. Acebutolol. xPharm: The Comprehensive Pharmacology Reference. 2007,1-5. https://doi.org/10.1016/B978-008055232-3.61153-5
11. Zore S., Bangar B., Shingate A. Formulation and evaluation of buccoadhesive drug delivery system of acebutolol hydrochloride. Int J Pharm and Bio Sci -IJPBSTM (2019) 9 (3): 124-132.
12. Saraf AJ, Pange S, Deshmukh S, Hajgude R. Res J Pharm Technol. 2013; 6(4): 406-414.
13. Balaji A, Vaddepalli R and Goud V: Formulation and evaluation of mucoadhesive buccal tablets by using natural polymer. IJPSR 2014; 5(11): 4699-4708.
14. Rao N, Devi KS, Kumar UN, Reddy S and Reddy KK: Formulation and evaluation of bilayed propranolol hydrochloride tablets. Int J Pharm Bio Sci, 2013; 3(2): 390-409.
15. Gore Mm, Gurav Y, Yadav A. Formulation and Evaluation af Mucoadhesive buccal Tablets of Propranolol Prepared Using Natural Polymer. Intern J Pharm Sci Res, 2018; 9(7): 2905-2913.
16. Jaffar I and Maraie N: Formulation and in-vitro evaluation of buccal mucoadhesive tablets of promethazine HCl. Int. J. Pharm. Sci. Rev. Res 2014; 24(1): 61-69.
17. Jadhav S, Mali A, Pawar S, Kharat R, Tamboli A. Difference spectroscopic method for the estimation of acebutolol hydrochloride in bulk and in its formulation. Inventi Rapid: Pharm Analysis & Quality Assurance. 2015;2(1):1-4.
18. Pawar S, Jadhav S, Tamboli A, Shaikh A, Mali S. Simultaneous UV Spectrophotometric Estimation of Acebutalol Hydrochloride and Hydrochlorothiazide in Bulk and Combined Tablet Dosage Form. Glob J Pharmaceu Sci. 2017; 3(1):555604.
19. Han-Gon Choi, Chong-Kook Kim. Development of omeprazole buccal adhesive tablets with stability enhancement in human saliva. J controlled release. 2000; 68:397-404.
20. Pandey S, Gupta A, Yadav J, Shah Y. Formulation and in-vitro evaluation of bilayered buccal tablets of carvedilol. Indian J.Pharm. Educ. Res.2010; 44(3):1-8.
21. Shirsand SB, Sarsija S, Keshvshetti GG, Swamy PV, Reddy PVP. Design and evaluation of mucoadhesive bilayer buccal tablets of nebivolol. RGUHS J Pharm Sci; 2013, 3(1): 40-47.
22. Balamurugan M, Saravanan VS, Ganesh P, Senthil SP, Hemalatha PV, Sudhir P. Development and in-vitro evaluation of mucoadhesive buccal tablets of domperidone. Research J. Pharm. and Tech. 2008; 1(4): 377-380
23. Li1 KL, Castillo AL. Formulation and evaluation of a mucoadhesive buccal tablet of mefenamic acid. Braz. J. Pharm. Sci. 2020;56: e18575: 1-19.
24. Fatima S, Panda N, Reddy AV, Fatima S. Buccal mucoadhesive tablets of sumatriptan succinate for treatment of sustainable migraine: design, formulation and in vitro evaluation. Int J Pharm Res. 2015;4(30):114-126.
25. Indian Pharmacopoeia, Government of India, Ministry of Health and Family Welfare, Published by The Indian Pharmacopoeia commission, Ghaziabad; 3rd ed., Vol. I, 2018: 272-350.
26. Buckingham R. Martindale-complete drug reference. 40th ed. Published by pharmaceutical press. 2020; 1153.
27. Velmurugan S and Srinivas P: Formulation and in-vitro evaluation of losartan potassium mucoadhesive buccal tablets. Asian J Pharm Clin Res 2013; 6(3): 125-130.
28. Shabaraya A, Aiswaraya K and Azharauddin M: Formulation and evaluation of mucoadhesive bi- layer buccal tablets of labetalol hydrochloride using natural polymers IJAPBC 2012; 1(3): 305-314.
29. Shirsand SB, Sarasijia S, Keshavshetti G, Swamy PV and Reddy PV: Formulation and optimization of mucoadhesive bilayer buccal tablets of atenolol using simplex design method. Int J Pharm Inv 2012; 2(1): 34-41.
30. Srinivas B, Mohanty C, Pattanoik P, Naik R and Brahma C: Design and in-vitro evaluation of muco-adhesive buccal tablets of salbutamol sulphate. IJPBS 2011; 1(3): 240-245.
31. Shisand S, Wadageri G, Raju S and Kolli G: Design and evaluation of mucoadheisve bilayer buccal tablets of nebivolol. RJPS 2013; 3(1): 40-47.
32. Gupta A, Garg S, Khar RK. Measurement of bioadhesive strength of mucoadhesive buccal tablets: Design of an in vitro assembly. Indian Drugs. 1993;30:152–5.
33. Madgulkar A., Kadam S., Pokharkar V. Development of Buccal Adhesive Tablet with Prolonged Antifungal activity: Optimization and ex vivo Deposition Studies, Indian J Pharm Sci. 2009; 71(3): 290–294
34. Biswajit B, Kharan N and Bhavsar B: Formulation and evaluation of repaglinide buccal tablets: Ex-vivo bioadhesion study and ex-vivo permeability study. Journal of Applied Pharm Sci 2014; 4(5): 96-103.
35. Krishna M, Uppala P, Kumar K and Patro S: Formulation and evaluation of mucoadhesive tablets of linagliptin. IJPPR 2015; 4(2): 141-158.
36. Dias R, Sakhare S and Mail K: Design and development of Mucoadhesive acyclovir tablet. IJPR 2009; 8(4): 231-239.
37. Çelik B. R Risperidone mucoadhesive buccal tablets: formulation design, optimization and evaluation. Drug Design, Development and Therapy 2017:11 3355–3365.
38. Varelas CG, Dixon DG, Steiner CA. Zero-order release from biphasic polymer hydrogels. J Control Release. 1995;34(3):185–192.
39. Wagner JG. Interpretation of percent dissolved-time plots derived from in vitro testing of conventional tablets and capsules. J Pharm Sci. 1969;58(10):1253–1257.
40. Higuchi T. Rate of release of medicaments from ointment bases containing drugs in suspension. J Pharm Sci. 1961;50(10):874–875.
41. Korsmeyer RW, Gurny R, Doelker E, Buri PA, Peppas NA. Mechanisms of solute release from porous hydrophilic polymers. Int J Pharm. 1983;15(1):25–35.
42. Guidance for Industry Q1A (R2) Stability testing of new drug substances and products, November 2003ICH Revision 2.
43. Sogias IA, Williams AC, Khutoryanskiy VV. Chitosan-based mucoad¬hesive tablets for oral delivery of ibuprofen. Int J Pharm. 2012;436(1–2):602–610.
44. Ramakrishna P, Mallikarjuna B, Chandra Babu A, Sudhakar P, ChowdojiRao K, Subha MCS. Interpenetrating polymer network of crosslinked blend microspheres for controlled release of Acebutolol HCl. Journal of Applied Pharmaceutical Science 01 (06); 2011: 212-219.
45. Mylangam CK, Beeravelli S, Medikonda J, Pidaparthi JS, Kolapalli VRM. Badam gum: a natural polymer in mucoadhesive drug delivery. Design, optimization, and biopharmaceutical evaluation of badam gum-based metoprolol succinate buccoadhesive tablets.Drug Deliv. 2016;23(1):195–206.
Statistics
48 Views | 33 Downloads
How to Cite
Chaudhari, P., Deore, A., Jagtap, M., & Gupta, D. (2022). Formulation Development and Evaluation of Mucoadhesive Buccal Tablets of Acebutolol Hydrochloride. Asian Journal of Pharmaceutical Research and Development, 10(4), 34-46. https://doi.org/https://doi.org/10.22270/ajprd.v10i4.1156