DESIGN AND EVALUATION OF INTRAGASTRIC BUOYANT TABLETS OF VENLAFAXINE HYDROCHLORIDE

  • RADHIKA PR J.K.K.NATTARAJA COLLEGE OF PHARMACY, KOMARAPALAYAM, NAMAKKAL DISTRICT
  • Nishala N J.K.K.NATTARAJA COLLEGE OF PHARMACY, KOMARAPALAYAM, NAMAKKAL DISTRICT
  • Kiruthika M J.K.K.NATTARAJA COLLEGE OF PHARMACY, KOMARAPALAYAM, NAMAKKAL DISTRICT
  • Sree Iswarya S J.K.K.NATTARAJA COLLEGE OF PHARMACY, KOMARAPALAYAM, NAMAKKAL DISTRICT

Abstract

Objective: The present study was undertaken to prolong the release of orally administered drug. The aim is to formulate, develop, and evaluate the
intragastric buoyant tablets of venlafaxine hydrochloride, which releases the drug in a sustained manner over a period of 12 hrs. Different formulations
were formulated using the polymers Carbopol 934 P, xanthan gum, hydroxypropyl methylcellulose (HPMC K100M) with varying concentration of
drug: Polymer ratio of 1:1, 1:1.5, 1:2, in which sodium bicarbonate acts as gas generating agent, and microcrystalline cellulose as a diluent.

Methods: The tablets were prepared by direct compression and evaluated for tablet thickness, weight variation, tablet hardness, friability, in vitro
buoyancy test, in vitro drug release and Fourier transform infrared spectroscopy. Formulations were evaluated by floating time, floating lag time and in vitro drug release. Dissolution profiles were subjected for various kinetic treatments to analyze the release pattern of drug.
Results: It was found that drug release depends on swelling, erosion, and diffusion, thus following the non-Fickian/anomalous type of diffusion.
Formulation F8 was considered as an optimized formulation for gastro retentive floating tablet of venlafaxine hydrochloride. The optimized
formulation showed sustained drug release and remained buoyant on the surface of the medium for more than 12 hrs. As the concentration of HPMC
K100M increases in the formulation the drug release rate was found to be decreased. The optimized formulation was subjected for the stability studies
and was found to be stable as no significant change was observed in various evaluated parameters of the formulation.
Conclusion: It can be concluded that floating drug delivery system of venlafaxine hydrochloride can be successfully formulated as an approach to
increase gastric residence time, thereby improving its bioavailability.
  

Keywords: Venlafaxine hydrochloride, Intragastric buoyant, Floating drug delivery systems, Hydroxypropyl methyl cellulose K100M, Carbopol 934 P, Xanthan gum.

Author Biography

RADHIKA PR, J.K.K.NATTARAJA COLLEGE OF PHARMACY, KOMARAPALAYAM, NAMAKKAL DISTRICT

DEPARTMENT OF PHARMACEUTICS,

References

1. Sood A, Panchagnula R. Design of controlled release delivery system using a modified pharmacokinetic approach, a case study for drugs having a short elimination half-life and a narrow therapeutic index. Int J Pharm 2003;261:27-41.
2. Vyas SP, Khar RK. Gastro Retentive Systems in Controlled Drug Delivery, Concepts and Advances. 1st ed. New Delhi: CBS Publications; 2002. p. 196-217.
3. Chickering DE, Jacob JS, Mathowitze E. Bioadhesive microspheres characterization and evaluation of bioadhesion involving hard, erodible polymers and soft tissues. React Polym 1995;25:189-206.
4. Garg S, Sharma S. Review-gastro retentive drug delivery system. Pharm Technol 2003;13:160-6.
5. Garg S, Sharma S. Gastro retentive drug delivery systems. Bus Brief Pharm Technol 2003;3:160-6.
6. Narang N. An updated review on floating drug delivery system (FDDS). Int J Appl Pharm 2011;3(1):1-7.
7. Koner P, Saudagar RB, Dharwal J. Gastro-Retentive Drugs a Novel Approach Towards Floating Therapy. Available from: http//www. pharma info.net/ exclusive/ reviews/ gastro retentive drugs a novel approach towards floating therapy/2007.
8. Tayade P. Gastro retentive drugs. A review. Express Pharm Pulse 2003;14:1-4.
9. Hilton AK, Deasy PB. In vitro and in vivo evaluation of oral sustained release floating dosage forms of amoxillintrihydrate. Int J Pharm 1992;86:79-88.
10. Sheth PR, Tossounian J. The hydrodynamically balanced system (HBSTN). A novel drug delivery system for oral use. Drug Dev Ind Pharm 1984;10:313-39.
11. Rubinstein A, Friend DR. Specific delivery to the gastrointestinal tract. In: Domb AJ, editor. Polymeric Site-Specific Pharmacotherapy. Chichester: Wiley; 1994. p. 282-3.
12. Ritschel WA. Targeting in the gastrointestinal tract: New approaches. Methods Find Exp Clin Pharmacol 1991;13(5):313-36.
13. Michaels AS, Bashwa JD, Zaffaroni A Integrated Device for Administering Beneficial Drug at Programmed Rate. US Patent 3, 901, 232 August 26; 1975.
14. Michaels AS. Drug Delivery Device with Self-actuated Mechanism for Retaining Device in Selected Area. US Patent 3, 786, 813, January 22; 1974.
15. Keith S. Advances in psychotropic formulations. Prog Neuropsychopharmacol Biol Psychiatry 2006;30:996-1008.
16. Dickson RB, Hardik T, Bhai R, Sureshkumar P, Jamsheer AK, Senthil A. Formulation and evaluation of gastro retentive floating tablet of glipizide. Int J Res Ayurveda Pharm 2011;2(3):911-7.
17. Liu L, Porter WR. Developing Solid Oral Dosage Forms: Pharmaceutical Theory and Practice. Ch. IV. USA, London: Academic Press; 2008. p. 125-35.
18. Pare A, Yadav SK, Patil UK. Formulation and evaluation of effervescent floating tablet of amlodipine besylate. Res J Pharm Technol 2008;1(4):526-30.
19. Peck GE, Baley GJ, McCurdy VE, Banker GS. Tablet Formulation and Design. New York: Marcel Dekker, Inc.; 1989. p. 88-120.
20. Liberman HA, Lachman L, Schwartz JB. Pharmaceutical Dosage Forms: Tablets. Vol. 1. New York: Marcel Dekker, Inc.; 1989. p. 1-5.
21. Shah D, Shah Y, Rampradhan M. Development and evaluation of controlled release diltiazem hydrochloride, micro particles using cross linked poly vinyl alcohol. Drug Dev Ind Pharm 1997;23:557-64.
22. Cooper J, Gunn C. Powder flow and compaction. Tutorial Pharmacy. New Delhi: CBS Publishers and Distributors; 1986. pp. 211-3.
23. Aulton ME, Wells TI. Pharmaceutics: The Science of Dosage form Design. London: Churchill Livingstone; 1998. p. 247-8.
24. Lachman L, Liberman HA, Konig JL. The Theory and Practice of Industrial. Philadelphia, PA: Pharmacy Leo & Febiger; 1987. p. 317-8.
25. Singh S, Prajapati K, Pathak AK, Mishra A. Formulation and evaluation of floating tablet of captopril. Int J Pharm Techol Res 2011;3(1):333-41.
26. Aulton ME. Pharmaceutics: The Science of Dosage Forms Design. 2nd ed. London: Churchill Livingstone; 1988.
27. Liu L, Porter WR. Developing Solid Oral Dosage Forms: Pharmaceutical Theory and Practice. Ch. IV. USA, London: Academic Press; 2008. p. 125-35.
28. Patel VM, Prajapati BG, Patel AK. Controlled release gastroretentive dosage form of verpamil hydrochloride. Int J Pharm Technol Res 2009;1(2):215-21.
29. Rosa M, Zia H, Rhodes T. Dosing and testing in vitro of a bio adhesive and floating drug delivery system for oral application. Int J Pharm 1994;105:65-70.
30. Patel DM, Patel NM, Pandya NN, Jogani PD. Gastro retentive drug delivery system of carbamazepine: Formulation and optimization using simplex lattice design; A technical note. AAPS Pharm Sci Technol 2001;8(1):11, E1-5.
31. Pandit V, Suresh S, Joshi H. Gastro retentive drug delivery system of amoxicillin: Formulation and in vitro evaluation. IJPBS 2010;1(2):1-10.
32. Wagner JG. Interpretation of percentage dissolved time plots derived from in vitro testing of conventional tablets and capsules. J Pharm Sci 1969;58:1253-7.
33. Higuchi T. Mechanism ODF sustained action medication, theoretical analysis of rate of release of solid drugs dispersed in solid matrices. J Pharm Sci 1963;52:1145-9.
34. Koresmeyer R, Gurny R, Peppas N. Mechanisms of solute release from porous hydrophilic polymers. Int J Pharm 1983;15:25-35.
35. ICH Stability Testing Guidelines: Stability Testing of New Drug Substances and Products.
36. Mohideen S, Kumar PS, Krishnan SN, Ayana TS, Shaji G, Surendranath Y, et al. Formulation and evaluation of gastroretentive floating tablets of venlafaxine hydrochloride. Int J Pharm Pharm Sci 2012;4(2):329-3.
37. Ananthakumar R, Raja N, Mohan P, Ruckmani K. Design and evaluation of intragastric buoyant tablets of metformin hydrochloride. Int J Pharm Pharm Sci 2013;5(3):479-84.
38. Pawar HA, Dhavale R. Development and evaluation of gastro retentive floating tablets of an antidepressant drug by thermoplastic granulation technique. Beni Suef Univ J Basic and Appl Sci 2014;3(2):122-32.
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RADHIKA PR, N. N, K. M, and S. I. S. “DESIGN AND EVALUATION OF INTRAGASTRIC BUOYANT TABLETS OF VENLAFAXINE HYDROCHLORIDE”. Asian Journal of Pharmaceutical and Clinical Research, Vol. 10, no. 5, May 2017, pp. 166-70, doi:10.22159/ajpcr.2017.v10i5.16948.
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