EVALUATION OF ORALLY DISINTEGRATING TABLET OF IBUPROFEN-β-CYCLODEXTRIN INCLUSION COMPLEX
Objective: This study aims to determine the effect of the inclusion complex formation of ibuprofen (IB) with β-cyclodextrin (β-CD) in improving water solubility and taste masking as well as to study the effect of the combined use of super disintegrants in IB-β-CD ODT (Orally disintegrating tablet).
Methods: IB-β-CD inclusion complex was prepared by spray drying technique with a 1:1 molar ratio. ODTs were prepared by the direct compression method using various ratios of Ac-Di-Sol® and Kollidon® CL as super disintegrant. The inclusion complex was characterized using spectroscopy FT-IR (Fourier-transform infrared) and DSC (Differential Scanning Calorimetry). The physical properties and dissolution rate of ODTs were evaluated. Dissolved drug concentration at 60 min (Q60) and Dissolution Efficiency (DE60) was calculated using the dissolution test result.
Results: The unpleasant taste of IB had been successfully masked by IB-β-CD. Formula 1 was observed having 14.5 sec of disintegration, fastest compared to the other formulas. Moreover DE60 value of formula I was higher than the other formulas (113.45).
Conclusion: IB-β-CD Inclusion complex prepared by spray drying method (1: 1) increased the water solubility and masked the unpleasant taste compared to IB moreover combination of Ac-Di-Sol® and Kollidon® CL increased ODT dissolution rate.
2. Tsume Y, Mudie DM, Langguth P, Amidon GE, Amidon GL. The biopharmaceutics classification system: subclasses for in vivo predictive dissolution (IPD) methodology and IVIVC. Eur J Pharm Sci 2014;57:152-63.
3. Newa M, Bhandari KH, Kim JO, Im JS, Kim JA, Yoo BK, et al. Enhancement of solubility, dissolution and bioavailability of ibuprofen in solid dispersion systems. Chem Pharm Bull 2008;4:569-74.
4. Hussain A, Smith G, Khan KA, Bukhari NI, Pedge NI, Ermolina I. Solubility and dissolution rate enhancement of ibuprofen by co-milling with polymeric excipients. Eur J Pharm Sci 2018;123:395-403.
5. Dugar RP, Gajera BY, Dave RH. Fusion method for solubility and dissolution rate enhancement of ibuprofen using block copolymer poloxamer 407. AAPS PharmSciTech 2016; 6:1428-40.
6. Stoyanova K, Vinarov Z, Tcholakova S. Improving ibuprofen solubility by surfactant-facilitated self-assembly into mixed micelles. J Drug Delivery Sci Technol 2016;36:208-15.
7. Sharma N, Baldi A. Exploring versatile applications of cyclodextrins: an overview. Drug Delivery 2016;3:729-47.
8. Gidwani B, Vyas A. A comprehensive review on cyclodextrin-based carriers for delivery of chemotherapeutic cytotoxic anticancer drugs. Biomed Res Int 2015:1-15. Doi:10.1155/ 2015/198268.
9. Tiwari G, Tiwari R, Rai AK. Cyclodextrins in delivery systems: applications. J Pharm Bioallied Sci 2010;2:72-9.
10. de Martino M, Chiarugi A, Boner A, Montini G, De’ Angelis GL. Working towards appropriate use of ibuprofen in children: an evidence-based appraisal. Drugs 2017;12:1295-311.
11. Wongrakpanich S, Wongrakpanich A, Melhado K, Rangaswami J. A comprehensive review of non-steroidal anti-inflammatory drug use in the elderly. Aging Dis 2018;1:143-50.
12. Ivanovska V, Rademaker CMA, van Dijk L, Mantel Teeuwisse AK. Pediatric drug formulations: a review of challenges and progress. Pediatrics 2014;2:361-72.
13. Desai S, Poddar A, Sawant K. Formulation of cyclodextrin inclusion complex-based orally disintegrating tablet of eslicarbazepine acetate for improved oral bioavailability. Mater Sci Eng C 2016;58:826-34.
14. Nazmi M, Islam SMA, Bhuiyan MA, Reza MS. Effect of super disintegrants and their mode of incorporation on disintegration time and release profile of carbamazepine from an immediate-release tablet. J Appl Pharm Sci 2013;5:80-4.
15. Khan GM, Wazir F, Zhu J. Ibuprofen-cyclodextrin inclusion complexes: evaluation of different complexation methods. J Med Sci 2001;4:193-9.
16. Heydari S, kakhki RM. Thermodynamic study of complex formation of ?-cyclodextrin with ibuprofen by conductometric method and determination of ibuprofen in pharmaceutical drugs. Arab J Chem 2017;10:1223-6.
17. El-menshawe SF, Eissa E, Ali AA, Abderhman AA. Enhancement of lornoxicam solubility by inclusion complexation with cyclodextrin: preparation and characterization. Int J Pharm Pharm Sci 2016;1:132-8.
18. Ghorab MK, Adeyeye MC. Elucidation of solution-state complexation in wet-granulated oven-dried ibuprofen and ?-cyclodextrin: FT-IR and 1H-NMR studies. Pharm Dev Technol 2001;3:315-24.
19. Ai F. Effect of drug particle size on complexation, physicochemical properties and dissolution of cyclodextrin inclusion complexes. Indian J Pharm Sci 2017;1:131-8.
20. Ti?a B, Fulia? A, Szabadai Z, Rusu G, Bandur G, Ti?a D. Compatibility study between ibuprofen and excipients in their physical mixtures. J Therm Anal Calorim 2011;2:517-27.
21. Obaidat A, Obaidat R. Development and evaluation of fast-dissolving tablets of meloxicam-?-cyclodextrin complex prepared by direct compression. Acta Pharm 2011;1:83-91.
22. Parfati N, Rani KC, Charles N, Geovany V. Preparation and evaluation of atenolol-?-cyclodextrin orally disintegrating tablets using co-process crospovidone-sodium starch glycolate. Int J Appl Pharm 2018;5:190-4.
23. Kraemer J, Gajendran J, Guillot A, Schichtel J, Tuereli A. Dissolution testing of orally disintegrating tablets. J Pharm Pharmacol 2012;7:911-8.
24. Patel AR, Vavia PR. Preparation and evaluation of taste-masked famotidine formulation using drug/beta-cyclodextrin/polymer ternary complexation approach. AAPS PharmSciTech 2008;2:544-50.
25. Malaquias LFB, Sá-Barreto LCL, Freire DO, Silva ICR, Karan K, Durig T, et al. Taste masking and rheology improvement of drug complexed with beta-cyclodextrin and hydroxypropyl-?-cyclodextrin by hot-melt extrusion. Carbohydr Polym 2018;185:19-26.
26. Simoes SMN, Rey Rico A, Concheiro A, Alvarez Lorenzo C. Supramolecular cyclodextrin-based drug nanocarriers. Chem Commun 2015;29:6275-89.
27. Shu T, Suzuki H, Hironaka K, Ito K. Studies of rapidly disintegrating tablets in the oral cavity using co-ground mixtures of mannitol with crospovidone. Chem Pharm Bull 2002;2:193-8.
28. Kovvasu SP, Chowdary K. Formulation development and in vivo evaluation of pioglitazone inclusion complexes: a factorial study. Int J Appl Pharm 2018;3:49-55.
29. Ghogari IS, Jain PS. Development of orally disintegrating tablets of memantine hydrochloride-a remedy for Alzheimer's disease. Int J Appl Pharm 2019;3:147–52.
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