FORMULATION AND EVALUATION OF FAST DISSOLVING TABLET OF APREPITANT BY USING NATURAL AND SYNTHETIC SUPERDISINTEGRANTS
DOI:
https://doi.org/10.22159/ijap.2020v12i1.35222Keywords:
Aprepitant, Superdisintegrants, Fast dissolving tablet, Direct compression, Evaluation, In vivo studiesAbstract
Objective: The present study was aimed to formulate fast dissolving tablets (FDTs) of Aprepitant (APT) using natural and synthetic superdisintegrants with the desired onset of action, increased bioavailability by reducing the frequency of dosage and also reduce the first-pass metabolism of the drug.
Methods: In this research, the gum isolated from cordia dichotoma was investigated as super disintegrants in fast dissolving tablets (FDTs). The aprepitant tablets were prepared separately using cordia dichotoma (natural), sodium starch glycolate and croscarmellose sodium (synthetic) as superdisintegrants by direct compression method. The tablets were evaluated for various precompression and post-compression parameters.
Results: The optimized formulation (APT F3) of cordia dichotoma (8%) showed satisfactory physicochemical properties, minimum disintegration time (34 seconds) and highest dissolution rate (86.52%) in 10 min than the other synthetic superdisintegrants. Also, the pharmacokinetic study of the optimized formulation showed effective results as compared with marketed product of aprepitant.
Conclusion: The developed formulation can improve the onset of action as well as improve patient compliance.
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Spiegel DR, Pattison A, Lyons A, Ansari U, Mccroskey AL, Luehrs E, et al. The role and treatment implications of peripheral and central processing of pain, pruritus, and nausea in heightened somatic awareness: a review. Innov Clin Neurosci 2017;14:11–20.
Merck and Co. Inc. EMEND® (aprepitant) capsules. US FDA Label, Whitehouse Station, NJ; 2003.
Warr DG MD. Chemotherapy-and cancer-related nausea and vomiting. Curr Oncol 2008;15:S4–9.
Stephenson J, Davies A. An assessment of etiology-based guidelines for the management of nausea and vomiting in patients with advanced cancer. Support Care Cancer 2006;14:348–53.
Hickok JT, Roscoe JA, Morrow GR, Bole CW, Zhao H, Hoelzer KL, et al. 5-Hydroxytryptamine-receptor antagonists versus prochlorperazine for control of delayed nausea caused by doxorubicin: a URCC CCOP randomised controlled trial. Lancet Oncol 2005;6:765–72.
Hickok JT, Morrow GW, Roscoe JA. Prevalence and severity of acute and delayed NV association with 3 highly emetogenic chemotherapies. Supportive Care Cancer 2001;9:289.
Hofman M, Morrow GR, Roscoe JA. Cancer patient's expectations of experiencing treatment-related side effects. Cancer 2004;101:851–7.
James G, Steven DA, Niesha G, Lee S. Recent advances in antiemetics: new formulations of 5HT3-receptor antagonists. Cancer Manag Res 2018;10:1827–57.
LeBourgeois JP, McKenna CJ, Coster B, Feyer P, Franzen L, Goedhals L, et al. Efficacy of ondansetron orally disintegrating tablet: a novel oral formulation of this 5-HT receptor antagonist in the treatment of fractionated radiotherapy-induced nausea and emesis. Emesis study group for the ondansetron orally disintegrating tablet in radiotherapy treatment. Clin Oncol (R Coll Radiol) 1999;11:340-7.
Hannan PA, Khan JA, Khan A, S Safiullah. Oral dispersible system: a new approach in the drug delivery system. Indian J Pharm Sci 2016;78:2–7.
Parul S, Anoop K, Pankaj S, Sharad V. Fast disintegrating oral films: a recent trend of drug delivery. Int J Drug Dev Res 2012;4:80–94.
Sastry SV, Nyshadham JR, Fix JA. Recent technological advances in oral drug delivery–a review. Pharm Sci Technol Today 2000;3:138–45.
Parkash V, Maan S, Yadav SV, Jogpal V. Fast disintegrating tablets: opportunity in drug delivery system. J Adv Pharm Technol Res 2011;2:223–35.
Dave V, Yadav RB, Ahuja R, Yadav S. Formulation design and optimization of novel fast dissolving tablet of chlorpheniramine maleate by using lyophilization techniques. Bull Fac Pharm (Cairo Univ) 2017;55:31–9.
Pawara HA, Jadhavba P. Isolation, characterization and investigation of Cordia dichotoma fruit polysaccharide as a herbal excipient. Int J Biol Macromol 2015;75:1228–36.
Khandelwal KR. Practical pharmacognosy techniques and experiments. Nirali Prakashan; 2008.
Pawar H, Varkhade C, Jadhav P, Mehra K. Development and evaluation of orodispersible tablets using a natural polysaccharide isolated from Cassia tora seeds. Int Med Res 2014;3:91–8.
Indian Pharmacopoeia. Controller of publications. 4th ed. Ministry of Health and Family Welfare, Govt. of India. New Delhi, India; 1996. p. 78.
World Health Organization, Quality Control Methods for Medicinal Plant Material, WHO, Geneva; 1998.
Jarald EE, Sumati S, Edwin S. Characterization of Moringa oleifera Lam. Gum to establish it as a pharmaceutical excipient. Indian J Pharm Educ Res 2012;46:211–6.
Cooper J, Gunn C. Powder flow and compaction. In: SJ Carter. Ed. Tutorial Pharmacy, CBS Publishers and Distributors, New Delhi, India; 1986.
Leon L, Herbert AL, Joseph LK. The theory and practices of industrial pharmacy. 3rd ed. Bombay: Varghese Publishing House; 2008.
Zhao N, Augsburger LL. Functionality comparison of three classes of super-disintegrants in promoting aspirin tablet's disintegration and dissolution. AAPS PharmSciTech 2005;6:634–40.
Mashru RC, Sutariya VB, Sankalia MG, Parikh PP. Development and evaluation of fast-dissolving film of salbutamol sulphate. Drug Dev Ind Pharm 2005;31:25–34.
Panchal NS, Patel H, Bagada A, Vadalia K. Formulation and evaluation of mouth dissolving film of ropinirole hydrochloride by using pullulan polymer. Int J Pharm Res Allied Sci 2012;1:60–72.
Chaudhari PD, Chaudhari SP, Kohle SR, Kumar SRS, Thirupathi AT. Formulation and evaluation of fast dissolving tablets of famotidine. Ind Drug 2005;42:641–9.
Costa P, Lobo JMS. Modeling and comparison of dissolution profiles. Eur J Pharm Sci 2001;13:123–33.
Kumar SK, Nagabhushanam MV, Rao KRS, Bhikshapathi DVRN. Preparation and in vivo evaluation of oral dissolving films containing sumatriptan succinate. Scholars Res Libraray 2013;5:27-38.
Sri J, Bhikshapathi DVRN. Formulation, development, and in vivo evaluation of mouth dissolving films containing palonosetron HCL. Int J Drug Delivery 2016;8:23-36.
Zeng F, Wang L, Zhang W, Shi KZ, Ong L. Formulation and in vivo evaluation of oral disintegrating tablets of clozapine hydroxy propyl-Beta-cyclodextin inclusion complexes. AAPS PharmTech 2013;14:854-60.
Chavez Eng CM, Constanzer ML, Matuszewski BK. Simultaneous determination of Aprepitant and two metabolites in human plasma by high-performance liquid chromatography with tandem mass spectrometric detection. J Pharm Biomed Anal 2004;35:1213-29.
Sreekanth N, Bahlul ZA, Babu RC, Mukkanti K. A validated stability-indicating RP-HPLC method for the determination of aprepitant in bulk and pharmaceutical dosage forms. Recent Res Sci Technol 2011;3:16-24.
Ashok S, Raghunadhababu CV, Satish VM, Balaswamy G. Separation and quantification of process-related impurities and diastereomers in aprepitant bulk drug substance. J Liq Chromatogr Relat Technol 2012;35:677-87.
Sharma R, Kamboj S, Singh G, Rana V. Development of aprepitant loaded orally disintegrating films for enhanced pharmacokinetic performance. Eur J Pharm Sci 2016;84:55-69.
Rajeswari S, Kumari MY. Formulation and evaluation of famotidine fast dissolving tablets using synthetic superdisintegrants. Int J Pharm Pharm Sci 2019;1:17-25.
Kalia A, Khurana S, Bedi N. Formulation and evaluation of mouth dissolving tablets of oxcarbazepine cellulose. Int J Pharm Pharm Sci 2009;1:164-79.
Mohammed S, R Sharma SK, Kaucha K, Hiremath D. Formulation and evaluation of flurbiprofen fast disintegrating tablets using natural super disintegrants. Asian J Pharm Clin Res 2016;9:247-54.
Dhahir RK, Al-Kotaji M. Formulation of orally disintegrating tablets of cinnarizine by using direct compression method. Int J Appl Pharm 2019;11:117-23.
Kamboj S, Sharma R, Singh K, Rana V. Aprepitant loaded solid preconcentrated microemulsion for enhanced bioavailability: a comparison with micronized aprepitant. Eur J Pharm Sci 2015;78:90–102.
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