Author(s):
Selvamuthukumar R., Murali R., Srinivasan N., Mohankumar A., Nitin Panicker
Email(s):
selvapharm96@gmail.com
DOI:
10.5958/0974-360X.2020.00818.5 
Address:
Selvamuthukumar R.*, Murali R., Srinivasan N., Mohankumar A., Nitin Panicker
Department of Pharmacy, FEAT, Annamalai University, Annamalai Nagar, Chidambaram-608002, Tamilnadu, India.
*Corresponding Author
Published In:
Volume - 13,
Issue - 10,
Year - 2020
ABSTRACT:
The immediate release tablet of antifungal drug Terbinafine hydrochloride were prepared developed and evaluated to increase solubility and bioavailability of low soluble drug by using wet granulation method. The tablets were prepared by varying concentrations and compositions of microcrystalline cellulose, sodium starch glycolate, hydroxyl propyl methyl cellulose, magnesium stearate, and colloidal silicon dioxide for seven trial batches. The drug excipient compatability study was studied by photostability study. No significant changes were observed in photostability study. The tablets were evaluated for disintegration test, content uniformity, and friability. Invitro drug release profile Terbinafine hydrochloride was examined in four different media PH0.1N HCL, PH4.5 acidic buffers, PH6.8 phosphate buffer and PH3.0 citrate buffer for 45 minutes. The drug release for trial batch no.7 shows 100.4% of drug release and innovator shows 102% of drug release. The formulation trial no 6 and 7 showed no significant changes during the study period of accelerated stability study for 3 months. The result of all formulation 7 showed that good developed formulation of immediate release tablet containing Terbinafine hydrochloride drug was similar to the marketed product with all respect and stable to effect of temperature and humidity.
Cite this article:
Selvamuthukumar R., Murali R., Srinivasan N., Mohankumar A., Nitin Panicker. Formulation Development and Evaluation of Immediate release tablet of Terbinafine Hydrochloride. Research J. Pharm. and Tech. 2020; 13(10):4648-4654. doi: 10.5958/0974-360X.2020.00818.5
Cite(Electronic):
Selvamuthukumar R., Murali R., Srinivasan N., Mohankumar A., Nitin Panicker. Formulation Development and Evaluation of Immediate release tablet of Terbinafine Hydrochloride. Research J. Pharm. and Tech. 2020; 13(10):4648-4654. doi: 10.5958/0974-360X.2020.00818.5 Available on: https://rjptonline.org/AbstractView.aspx?PID=2020-13-10-21
REFERENCES:
1. Pratap, S., Formulation and Evaluation of Duloxetine Hydrochloride Delayed Release Capsules. 2013, CL Baid Metha College of Pharmacy, Chennai.
2. Nyol, S. and M. Gupta, Immediate drug release dosage form: a review. Journal of Drug Delivery and Therapeutics, 2013. 3(2).
3. Villars, V. and T. Jones, Clinical efficacy and tolerability of terbinafine (Lamisil)—a new topical and systemic fungicidal drug for treatment of dermatomycoses. Clinical and Experimental Dermatology, 1989. 14(2): p. 124-127.
4. Elewski, B.E., et al., Terbinafine hydrochloride oral granules versus oral griseofulvin suspension in children with tinea capitis: Results of two randomized, investigator-blinded, multicenter, international, controlled trials∗. Journal of the American Academy of Dermatology, 2008. 59(1): p. 41-54.
5. Petranyi, G., J.G. Meingassner, and H. Mieth, Activity of terbinafine in experimental fungal infections of laboratory animals. Antimicrobial Agents and Chemotherapy, 1987. 31(10): p. 1558-1561.
6. Kyle, A.A. and M.V. Dahl, Topical therapy for fungal infections. American journal of clinical dermatology, 2004. 5(6): p. 443-451.
7. Daneshmend, T. and D. Warnock, Clinical pharmacokinetics of systemic antifungal drugs. Clinical Pharmacokinetics, 1983. 8(1): p. 17-42.
8. Dun, E., Antifungal resistance in yeast vaginitis. The Yale Journal of Biology and Medicine, 1999. 72(4): p. 281.
9. Adams, B.B., Dermatologic disorders of the athlete. Sports Medicine, 2002. 32(5): p. 309-321.
10. Elewski, B.E., Mechanisms of action of systemic antifungal agents. Journal of the American Academy of Dermatology, 1993. 28(5): p. S28-S34.
11. Vergidis, P., et al., False‐positive Aspergillus galactomannan assay in solid organ transplant recipients with histoplasmosis. Transplant Infectious Disease, 2012. 14(2): p. 213-217.
12. Walter, J.E. and R.D. Jones, Serologic tests in diagnosis of aspergillosis. Diseases of the Chest, 1968. 53(6): p. 729-735.
13. Monod, M., Secreted proteases from dermatophytes. Mycopathologia, 2008. 166(5-6): p. 285.
14. Satish, S., et al., Antifungal activity of some plant extracts against important seed borne pathogens of Aspergillus sp. Journal of Agricultural Technology, 2007. 3(1): p. 109-119.
15. Darkes, M.J., L.J. Scott, and K.L. Goa, Terbinafine. American journal of clinical dermatology, 2003. 4(1): p. 39-65.
16. Khan, N.B. and A.N. Chohan, Accuracy of bottled drinking water label content. Environmental Monitoring and Assessment, 2010. 166(1-4): p. 169-176.
17. Pabla, D., F. Akhlaghi, and H. Zia, A comparative pH-dissolution profile study of selected commercial levothyroxine products using inductively coupled plasma mass spectrometry. European journal of Pharmaceutics and Biopharmaceutics, 2009. 72(1): p. 105-110.
18. Chien, W.Y., Potential development and new approaches in oral controlled-release drug delivery systems. Drug Development and Industrial Pharmacy, 1983. 9(7): p. 1291-1330.
19. Van Dooren, A., Design for drug-excipient interaction studies. Drug Development and Industrial Pharmacy, 1983. 9(1-2): p. 43-55.
20. Battista, O. and P. Smith, Microcrystalline cellulose. Industrial and Engineering Chemistry, 1962. 54(9): p. 20-29.
21. Siepmann, J. and N. Peppas, Modeling of drug release from delivery systems based on hydroxypropyl methylcellulose (HPMC). Advanced Drug Delivery Reviews, 2012. 64: p. 163-174.
22. Edge, S., et al., Chemical characterisation of sodium starch glycolate particles. International Journal of Pharmaceutics, 2002. 240(1-2): p. 67-78.
23. De Boer, A., G. Bolhuis, and C. Lerk, Bonding characteristics by scanning electron microscopy of powders mixed with magnesium stearate. Powder Technology, 1978. 20(1): p. 75-82.
24. Chang, R.-K., et al., Effect of colloidal silicon dioxide on flowing and tableting properties of an experimental, crosslinked polyalkylammonium polymer. Pharmaceutical Development and Technology, 1999. 4(2): p. 285-289.
25. Hentzschel, C.M., A. Sakmann, and C.S. Leopold, Suitability of various excipients as carrier and coating materials for liquisolid compacts. Drug Development and Industrial Pharmacy, 2011. 37(10): p. 1200-1207.
26. Fahmy, R., et al., Quality by design I: application of failure mode effect analysis (FMEA) and Plackett–Burman design of experiments in the identification of “main factors” in the formulation and process design space for roller-compacted ciprofloxacin hydrochloride immediate-release tablets. AAPS PharmSciTech, 2012. 13(4): p. 1243-1254.
27. Klein, H.J. and G.L. Szekeres, Container seal with tamper indicator. 1985, Google Patents.
28. Jivraj, M., L.G. Martini, and C.M. Thomson, An overview of the different excipients useful for the direct compression of tablets. Pharmaceutical Science and Technology Today, 2000. 3(2): p. 58-63.
29. Iveson, S.M., et al., Nucleation, growth and breakage phenomena in agitated wet granulation processes: a review. Powder Technology, 2001. 117(1-2): p. 3-39.
30. Chowhan, Z. and L. Palagyi, Hardness increase induced by partial moisture loss in compressed tablets and its effect on in vitro dissolution. Journal of Pharmaceutical Sciences, 1978. 67(10): p. 1385-1389.
31. Guideline, I.H.T. Validation of analytical procedures: text and methodology Q2 (R1). in International conference on harmonization, Geneva, Switzerland. 2005.
32. Patel, J., P. Tiwari, and J. Patel, Solid dispersion based tablets of poorly soluble drug flurbiprofen. Am J Pharmtech Res, 2011. 1(1): p. 18-24.
33. Whelan, M.R., J.L. Ford, and M.W. Powell, Simultaneous determination of ibuprofen and hydroxypropylmethylcellulose (HPMC) using HPLC and evaporative light scattering detection. Journal of Pharmaceutical and Biomedical Analysis, 2002. 30(4): p. 1355-1359.
34. Mettu, S.R. and P.R. Veerareddy, Formulation, evaluation and pharmacokinetics of flurbiprofen fast dissolving tablets. Brit J Pharm Res, 2013. 3(4): p. 617-631.
35. Nash, R.A., A response to recent GMP-validation interpretations. Clinical Research and Regulatory Affairs, 1993. 10(4): p. 253-264.
36. Kraszewski, A. and S. Kulinski, An improved microwave method of moisture content measurement and control. IEEE Transactions on Industrial Electronics and Control Instrumentation, 1976(4): p. 364-370.
37. Madsen, E. and G. Fladmark, Some finite difference methods for solution of heat conduction problems, in Numerical Solution of Partial Differential Equations. 1973, Springer. p. 223-240.
38. Garvey III, R.E. and A.A. Carey, Automatic determination of moisture content and lubricant type. 1997, Google Patents.
39. Arya, L.M. and J.F. Paris, A physicoempirical model to predict the soil moisture characteristic from particle-size distribution and bulk density data 1. Soil Science Society of America Journal, 1981. 45(6): p. 1023-1030.
40. Webb, P.A., Volume and density determinations for particle technologists. Micromeritics Instrument Corp, 2001. 2(16): p. 01.
41. Abdullah, E.C. and D. Geldart, The use of bulk density measurements as flowability indicators. Powder Technology, 1999. 102(2): p. 151-165.
42. Amidon, G.E., P.J. Secreast, and D. Mudie, Particle, powder, and compact characterization, in Developing solid oral dosage forms. 2009, Elsevier. p. 163-186.
43. Peterson, R.W., Apparatus and method for solid particle bulk density measurements. 1981, Google Patents.
44. Gregory, E., J. Pamela, and M. Deanna, Particle, Powder and Compact Characterization. ln: Developing Solid Oral Dosage Forms: Pharmaceutical Theory and Practice, Qiu, Y., Y. Chen, GGZ Zhang, L. Liu and W. Porter. 2009, Elsevier lnc., USA., ISBN-13.
45. Fassihi, A. and I. Kanfer, Effect of compressibility and powder flow properties on tablet weight variation. Drug Development and Industrial Pharmacy, 1986. 12(11-13): p. 1947-1966.
46. Saw, H.Y., et al., Correlation between powder flow properties measured by shear testing and Hausner ratio. Procedia Engineering, 2015. 102: p. 218-225.
47. Moked, I., et al., Apparatus for Blending Granular Materials. 1978, Google Patents.
48. Moes, J.J., et al., Application of process analytical technology in tablet process development using NIR spectroscopy: Blend uniformity, content uniformity and coating thickness measurements. International Journal of Pharmaceutics, 2008. 357(1-2): p. 108-118.
49. Danjo, K., C. Ertell, and J. Carstensen, Effect of compaction speed and die diameter on Athy-Heckel and hardness parameters of compressed tablets. Drug Development and Industrial Pharmacy, 1989. 15(1): p. 1-10.
50. Holm, P. and L. Slot, Disintegrating Loadable Tablets. 2009, Google Patents.
51. Sunada, H. and Y. Bi, Preparation, evaluation and optimization of rapidly disintegrating tablets. Powder Technology, 2002. 122(2-3): p. 188-198.
52. Riippi, M., et al., The effect of compression force on surface structure, crushing strength, friability and disintegration time of erythromycin acistrate tablets. European Journal of Pharmaceutics and Biopharmaceutics, 1998. 46(3): p. 339-345.
53. Seitz, J.A. and G.M. Flessland, Evaluation of the physical properties of compressed tablets I: Tablet hardness and friability. Journal of Pharmaceutical Sciences, 1965. 54(9): p. 1353-1357.
54. Fairchild, H. and F. Michel, Pfizer tablet hardness tester. Journal of Pharmaceutical Sciences, 1961. 50(11): p. 966-969.
55. Chatterjee, A. and P. Siarry, Nonlinear inertia weight variation for dynamic adaptation in particle swarm optimization. Computers and Operations Research, 2006. 33(3): p. 859-871.
56. Tayel, S.A., et al., Promising ion-sensitive in situ ocular nanoemulsion gels of terbinafine hydrochloride: design, in vitro characterization and in vivo estimation of the ocular irritation and drug pharmacokinetics in the aqueous humor of rabbits. International Journal of Pharmaceutics, 2013. 443(1-2): p. 293-305.
57. Iizhar, S.A., et al., In vitro assessment of pharmaceutical potential of ethosomes entrapped with terbinafine hydrochloride. Journal of Advanced Research, 2016. 7(3): p. 453-461.
58. Nazzal, S. and M.A. Khan, Controlled release of a self-emulsifying formulation from a tablet dosage form: Stability assessment and optimization of some processing parameters. International Journal of Pharmaceutics, 2006. 315(1-2): p. 110-121.
59. Belal, F., et al., Spectrofluorimetric determination of terbinafine hydrochloride and linezolid in their dosage forms and human plasma. Journal of fluorescence, 2013. 23(5): p. 1077-1087.
60. Kanakapura, B. and V.K. Penmatsa, Analytical methods for determination of terbinafine hydrochloride in pharmaceuticals and biological materials. Journal of Pharmaceutical Analysis, 2016. 6(3): p. 137-149.