Formulation and Evaluation of Bilayered Floating Tablets of Aceclofenac
Abstract
The objective of this study was to create and assess homogeneous bilayered floating tablets of aceclofenac in order to increase the drug's bioavailability and prolong its stomach release. One of the nonsteroidal anti-inflammatory drugs (NSAID) common side effects is poor solubility and minimal stomach retention, which makes it difficult to treat effectively. As matrix-forming polymers, ten formulations (F1–F10) were made with different amounts of HPMC K15 and additional excipients. Physical properties, buoyancy, in vitro drug release, and kinetic modelling were evaluated for each formulation. With a floating lag time of less than one minute and buoyancy maintained for more than 12 hours, Formulation 5 (F5) showed the most promising findings. With 97.01% of aceclofenac released over 12 hours, it showed a regulated drug release pattern that followed the Korsmeyer-Peppas release model well (R2 = 0.9242). Pre-compression and post-compression values for the optimised formulation F5 were adequate, suggesting good flow characteristics and tablet integrity. FTIR spectroscopy was used to verify the drug-excipient compatibility, guaranteeing stability and the lack of interactions. According to these results, aceclofenac's homogenous bilayered floating tablets, specifically formulation F5, may be able to improve gastric retention time and offer a sustained release profile. This could mean that the medication can be used to treat chronic inflammatory conditions more effectively and with better patient compliance.
Keywords: gastric retention, bioavailability, drug excipient compatibility.
Downloads
References
Rathore R, Gupta AK, Parashar AK. Formulation and Evaluation of fast dissolving films of Granisetron Hydrochloride. Journal of Drug Delivery and Therapeutics. 2019; 9(2-A):36-38.
Gaikwad SS, Chafle SA, Morris PS, Avari JG. Development and evaluation of bilayer tablets of combination of antibiotics for the treatment of sexually transmitted disease. Brazilian Journal of Pharmaceutical Sciences. 2016;(3):555-66. https://doi.org/10.1590/s1984-82502016000300020
Davis JR. Handbook of materials for medical devices. ASM International; 2003
Malviya Y, Kondalkar A. Formulation development and evaluation of gastroretentive floating tablets of ambroxol hydrochloride. Journal of Drug Delivery and Therapeutics, 2019;9(4-s):1016-21. https://doi.org/10.22270/jddt.v9i4-s.3354
Sangeetha R, Pillai MK, Haribabu Y. Bi-layer tablets: A flexible technology for oral drug delivery-An updated review. Res J Pharm Technol [Internet]. 2021; 14(1):547-51. https://doi.org/10.5958/0974-360X.2021.00099.8
Singh A, Das S, Gupta S, Ghosh S. The challenges of producing bilayer tablet: A review. Journal of Drug Delivery and Therapeutics, 2021; 11(4-S):171-5. https://doi.org/10.22270/jddt.v11i4-S.4922
Patra CN, Kumar AB, Pandit HK, Singh SP, Devi MV. Design and evaluation of sustained release bilayer tablets of propranolol hydrochloride. Acta Pharm [Internet]. 2007; 57(4):479-89. https://doi.org/10.2478/v10007-007-0038-0 PMid:18165191
Joseph D, Thomas GM. A review on current applications of bilayer tablets. Res J Pharm Technol. 2019; 12(5):2539. https://doi.org/10.5958/0974-360X.2019.00427.X
Parashar AK, Patel P, Gupta AK, Jain NK, Kurmi BD. Synthesis, characterization andin vivoEvaluation of PEGylated PPI dendrimer for safe and prolonged delivery of insulin. Drug Deliv Lett. 2019; 9(3):248-63. https://doi.org/10.2174/2210303109666190401231920
Akhtar M, Jamshaid M, Zaman M, Mirza AZ. Bilayer tablets: A developing novel drug delivery system. J Drug Deliv Sci Technol [Internet]. 2020; 60(102079):102079. https://doi.org/10.1016/j.jddst.2020.102079
Agiba AM, Abul-Ella SS, El-Monem RAA. Pharmacotechnical development and optimization of multilayered tablets: An updated industrial review with emphasis on bilayer tablets. Int j appl pharm. 2021; 55-64. https://doi.org/10.22159/ijap.2021v13i4.41528
Kushwaha N, Jain A, Jain PK, Khare B, Jat YS, An Overview on Formulation and Evaluation Aspects of Tablets, Asian Journal of Dental and Health Sciences, 2022;2(4):35-39 https://doi.org/10.22270/ajdhs.v2i4.23
Reddy M. S, Muppa L, A review of challenges and possibilities of bilayer tablet technology. Int J Adv Res. 2021;9(08):676-81. https://doi.org/10.21474/IJAR01/13315
Annapurna U, Priyanka KS. Bilayer Tablets-A Review. Research Journal of Pharmacy and Technology. 2019; 12(1):385-90 https://doi.org/10.5958/0974-360X.2019.00070.2
Maddiboyina B, Jhawat V, Sivaraman G, Sunnapu O, Nakkala RK, Naik MH, Gulia M. Formulation development and characterization of controlled release core-in-cup matrix tablets of venlafaxine HCl. Current Drug Therapy. 2020 Oct 1;15(5):503-11. https://doi.org/10.2174/1574885515666200331104440
The Merk Index, 1996, 12th Edition.
Rudnic EM et al, Kottke et al MK Tablet dosage form. In Banker GS, Rhodes CT, editors. Modern Pharmaceutics. 3rd ed., vol 72. New York: Marcel Dekker Inc. p 369.
Breech AJ et al, Lucisano L J et al, Franz RM et al Investigation into substrate cracking of a film coated bilayered tablet. J. Pharm.Pharmacol. 1998; 40:282-283. https://doi.org/10.1111/j.2042-7158.1988.tb05244.x PMid:2900310
Kalam MA, Humayun M, Parvez N, Yadav S, Garg A, Amin S, Sultana Y, Ali A, Continental et al J. Pharmaceutical Sciences;2007,1: 30-35
Li S.P. et al, Karth M.G. et al, Feld K.M. et al, Pendharkar C.M. et al, Willams R.O. et al, Evaluation of Bilayer tablet machines. A Case study. Drug Dev. Ind. Pharm. 1995; 21(5):571 590. https://doi.org/10.3109/03639049509048124
Aulton M E. The science of dosage form design. Ed Ist New York: Churuchill Livingstone; 1996 pp 247-248
Cooper J and gunn G. Powder flow and compaction, In; Tutorial pharmacy (carter SJ; Eds.) New Dehli. India; CBS Publisers and distributers; 1986: 211-233. (AR)
Shah D, Shah Y and Rampadhan M. Development and evaluation of controlled release diltiazem hydrochloride microparticles using cross-linked polymer (vinayl alcohol). Drug Dev. Ind. Pharm. 1997; 23(6): 567-574. https://doi.org/10.3109/03639049709149821
Aulton ME, and well TI. Pharmaceutics: The Sciences of Dosage form Design, London, England; Churchill Livingstone; 1998. (CI)
Lachman L, Lieberman A, Joseph H. In Theory & practice of Industrial Pharmacy, Ed. IIIrd Bombay: Vallabh Prakashan; 1987.Page No.430
Dollery SC, "Therapeutic Drugs," Churchill Livingstone, Philadelphia, 1991, pp. 25-26.
Chaudhari PD, Chaudhari SP, Kolhe SR, Dave KV, More DM. Formulation and evaluation of fast dissolving tablets of famotidine. INDIAN DRUGS-BOMBAY-. 2005;42(10):641.
M. K. Kiran, M. H. Shah, A. Ketkar, et al. Effect of drug solubility and different excipients on floating behavior and release from glyceryl monooleate matrices. Int. J. Pharm. 2004, 272: 151-160 https://doi.org/10.1016/j.ijpharm.2003.12.025 PMid:15019078
Baumgartner S, Kristl J, Vrecer F, Vodopivec P, Zorko B. Optimisation of floating matrix tablets and evaluation of their gastric residence time. Int J Pharm. 2000 Feb 15;195(1-2):125-35. https://doi.org/10.1016/S0378-5173(99)00378-6 PMid:10675690
M. Chavanpatil, P. Jain, S. Chaudhari, et al. Novel sustained release, swellable and bioadhesive gastroretentive drug delivery system for ofloxacin. Int. J.Pharm., 2006, 316: 86-92. https://doi.org/10.1016/j.ijpharm.2006.02.038 PMid:16567072
Nakhat P. D., Naidu R. A., Babla I. B., Khan S., Yeole P. G., Ind. J.Pharm. Sci., 2007;69:287-289. https://doi.org/10.4103/0250-474X.33160
Baveja S. K., Ranga Rao K. V., Devi P., Int. J. Pharm., 1987;39:435. https://doi.org/10.1016/0378-5173(87)90196-7
Wagner J. G., J. Pharm. Sci., 1969;58:1253. https://doi.org/10.1002/jps.2600581021 PMid:5349114
Higuchi W. I., J. Pharm. Sci., 1963;52:1145. https://doi.org/10.1002/jps.2600521210 PMid:14088963
Korsmeyer R. W., Gurny R., Doelker E., Buri P., Peppas N. A., Int. J.Pharm., 1983;15:25. https://doi.org/10.1016/0378-5173(83)90064-9
Costa, P., & Lobo, J. M. S., Modeling and comparison of dissolution profiles. Eur. J. Pharm. Sci., 2001;13:123-133 https://doi.org/10.1016/S0928-0987(01)00095-1 PMid:11297896
Copyright (c) 2024 Chenna M Shalini, S. Anila, Tadikonda Rama Rao
This work is licensed under a Creative Commons Attribution-NonCommercial 4.0 International License.
Authors who publish with this journal agree to the following terms:
- Authors retain copyright and grant the journal right of first publication with the work simultaneously licensed under a Creative Commons Attribution-NonCommercial 4.0 International (CC BY-NC 4.0). that allows others to share the work with an acknowledgment of the work's authorship and initial publication in this journal.
- Authors are able to enter into separate, additional contractual arrangements for the non-exclusive distribution of the journal's published version of the work (e.g., post it to an institutional repository or publish it in a book), with an acknowledgment of its initial publication in this journal.
- Authors are permitted and encouraged to post their work online (e.g., in institutional repositories or on their website) prior to and during the submission process, as it can lead to productive exchanges, as well as earlier and greater citation of published work (See The Effect of Open Access).
. 