Development and Optimization of Liquisolid Compact Tablet of Ebastine
DOI:
https://doi.org/10.22270/ajprd.v14i3.1759Abstract
Ebastine is a second-generation non-sedating antihistaminic drug indicated for the prevention and treatment of allergic rhinitis and chronic idiopathic urticaria. It is classified under Biopharmaceutical Classification System Class II and exhibits poor aqueous solubility, resulting in dissolution-limited oral absorption. The present work was undertaken to develop and optimize liquisolid compact tablets of Ebastine in order to improve dissolution behavior and pharmaceutical performance.
Solubility of Ebastine was evaluated in various non-volatile solvents. Based on maximum drug solubility, Cremophor RH 40 was selected as non-volatile liquid vehicle. Neusilin US2 and Aerosil 200 were selected as carrier and coating materials respectively. Drug-excipient compatibility studies were performed using Fourier Transform Infrared Spectroscopy and Differential Scanning Calorimetry. The formulation was optimized using Design Expert® version 10 software by response surface methodology employing 3² full factorial design. Drug concentration in liquid medication (Cd) and carrier-coating ratio (R) were selected as independent variables, while angle of repose and cumulative percentage drug release at 20 minutes were selected as dependent responses.
The optimized formulation was obtained with Cd value of 15.0 and carrier-coating ratio of 26.7. Validation batches confirmed close agreement between predicted and observed values. Crospovidone was selected as suitable superdisintegrant and optimized at 7%. The optimized formulation showed acceptable flow properties and post-compression characteristics. Comparative dissolution study demonstrated faster release than marketed conventional tablet. FTIR studies confirmed compatibility between drug and excipients. DSC and PXRD analysis indicated reduced crystallinity and improved dispersion of drug in final formulation. Accelerated stability study at 40 ±2°C and 75 ±5% RH for one month showed no remarkable change in tablet characteristics.
The study confirmed that liquisolid compact technology is a promising and effective approach for enhancing dissolution of poorly water-soluble Ebastine.
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References
Vekariya D, Zalavadiya D. Enhancement of bioavailability of poorly water-soluble drugs by liquisolid technique: A review. Int J Pharm Chem Sci. 2012;1(2):850-858.
Jung E, Kim JY, Ko D, Seo J, Lee SY, Lee D, Kim S, Park M, Kim S, Park S, Lee K. Ebastine targets HER2/HER3 signaling and cancer stem cell traits to overcome trastuzumab resistance in HER2 positive breast cancer. International Journal of Molecular Medicine. 2026 Apr 1;57(4):1-3.
Sahoo CK, Das S, Mishra S, et al. Formulation and characterization of liquisolid tablets for improving dissolution of telmisartan. FABAD J Pharm Sci. 2025;50(1):5-18.
Paun JS, Buddhadev S, Hirawala J, Christian P, Rathod N, Prajapati B. Optimization and Characterization of Lafutidine Liquisolid Pellets: A Novel Strategy for Improved Solubility and Drug Release. BioNanoScience. 2026 Feb 16;16(3):189.
Vieira RJ, Gil-Mata S, Ferreira A, Riera-Serra P, Bognanni A, Duarte VH, Viegas H, Pereira AM, Ferreira-da-Silva R, Ferreira-Cardoso H, Marques-Cruz M. Efficacy and safety of oral antihistamines for allergic rhinitis: Network meta-analysis. The Journal of Allergy and Clinical Immunology: In Practice. 2026 Feb 16.
Mehta S, Mansi P, Dudhat K, Borkhataria C, Soniwala M, Pethani T, Mehul R, Shah V, Manek R, Dhaval M. Liquisolid compact technology for enhancing the dissolution and bioavailability of Ticagrelor: DoE-based optimization and solid-state characterization. Journal of Drug Delivery Science and Technology. 2026 Mar 17:108241.
Mohamed MS, Ogawa K, Mahmoud RA, Ramadan AE, Elkarim RA, El-Shenawy AA, Ozeki T. Formulation and Evaluation of Liquisolid Orally Disintegrating Tablets of Agomelatine with Natural Excipients for Enhanced Oral Bioavailability. Journal of Pharmaceutical Innovation. 2026 Aug;21(4):412.
Paun JS, Buddhadev S, Hirawala J, Christian P, Rathod N, Prajapati B. Optimization and Characterization of Lafutidine Liquisolid Pellets: A Novel Strategy for Improved Solubility and Drug Release. BioNanoScience. 2026 Feb 16;16(3):189.
Barot T, Patel J, et al. Liquisolid compact of meclizine hydrochloride: development and optimization using factorial design. Int J Pharm Sci Res. 2025;16(2):1-12.
Rane B, Chaure P, Gawade S, Jain A, Shirode A, Kolhe Y. Design, Development, and Optimization of Ebastine-Loaded Nanofibers-Dispersed Transdermal Gel for the Chronic Urticaria (Hives). Journal of Pharmaceutical Innovation. 2026 Feb;21(1):48.
Rane B, Chaure P, Gawade S, Jain A, Shirode A, Kolhe Y. Design, Development, and Optimization of Ebastine-Loaded Nanofibers-Dispersed Transdermal Gel for the Chronic Urticaria (Hives). Journal of Pharmaceutical Innovation. 2026 Feb;21(1):48.
Mevada J, Patel K, Raval AM. Materiovigilance: From device failure to safety reform, the growing importance of materiovigilance systems. Int J Pharm Sci. 2026;4(1):962-74.
Research Journal of Pharmacy and Technology. Refined liquisolid system for enhancement of dissolution profile of poorly water-soluble drugs. Res J Pharm Technol. 2025;18(7).
Falwariya, R., Jethva, T., Raval, A.M. and Lokhande, D., 2026. Comprehensive review: Microneedle patches-A painless revolution in transdermal drug delivery. World J Pharm Med Res, 12(1), pp.199-207.
Mevada J, Patel K, Raval AM. Role of pharmacovigilance in drug safety monitoring. World J Pharm Med Res. 2025;11(11):235-40.
International Journal of Pharmaceutical Sciences Review and Research. Liquisolid technique: a newer approach for research in dissolution enhancement of poorly soluble drugs. Int J Pharm Sci Rev Res. 2025;85(8):1-9.
World Journal of Biology Pharmacy and Health Sciences. Formulation and evaluation of liquisolid compact of nitrofurantoin for dissolution enhancement. World J Biol Pharm Health Sci. 2025;22(2):1-10.
Hussain Y, Khan H, et al. The most recent advances in liquisolid technology. Pharmaceutical Science Advances. 2024; published online ahead of 2025 indexing.
Biotech Asia. Liquisolid compact-based strategy for augmented solubility and dissolution profile of dolutegravir sodium. Biotechnol Asia. 2026;22(4)
Kulkarni AS, Aloorkar NH. Liquisolid system: A review. Int J Pharm Sci Nanotechnol. 2010;3(1):795-802.
Rathi S. Physicochemical Characterization and In-Vitro Dissolution Enhancement of Ranolazine Using Solid Dispersion Method. Available at SSRN 3507970. 2019 Dec 21.
Hassan G, Jafar D, Jafar M. Improving dissolution of meloxicam using solid dispersion. Indian J Pharm Res. 2004;23:231-238.
Yadav V, Yadav A. Enhancement of solubility and dissolution rate of BCS class II pharmaceuticals by nonaqueous granulation technique. Int J Pharma Res Dev. 2010;1(12):1-12.
Raval AM, Bhavsar PR, Pandya FU, Patel D. Co-processed excipients in pharmaceutical formulation: advances, characterization, and applications. Asian Journal of Pharmaceutical Research and Development. 2026 Feb 16;14(01):105-13.
Zaheer A, Maurya N. Solubility enhancement of poorly water-soluble drugs: A review. Int J Pharm Tech. 2011;3(1):807-823.
Patel N, Raval AM. Gastro-retentive drug delivery system: A review. Int J Pharm Sci. 2026;4(1):734-42.
Kadam SV. Review on solubility enhancement techniques. Int J Pharm Bio Sci. 2013;3(3):462-475.
Kumar S. Various techniques for solubility enhancement: An overview. Pharma Innov J. 2016;5(1):23-28.
Thakor AD, Dharajiya RM, Shaikh MZ, Raval AM. A review on neuropharmacology: mechanisms, drug classes, and clinical applications. Asian Journal of Pharmaceutical Research and Development. 2026 Feb 15;14(01):114-21.
Datkhile S, Jadhav S. Liquisolid compacts: A review. Int J Inst Pharm Life Sci. 2014;4(2):1-10.
Zankhwala MF, Raval MA, Kushkiwala MA, Sarvaiya MS, Raval MK, Thakar MN, Barjod MS. Formulation And Evaluation Of Optimized Polymer Blends For Diclofenac Diethylamine Transdermal System. The Review of Diabetic Studies. 2025 Sep 14:701-8.
Kumar C, Venugopalaiah P. Liquisolid systems: An emerging strategy for solubilization and dissolution rate enhancement of BCS class II drugs. Int J Pharm Rev Res. 2013;3(2):56-66.
Kumar PA, Mohmmed N, Chandragirivar PC, Raval AM. Design space exploration of trazodone nanocrystals via DOE: formulation and in vitro-in vivo assessment. Int J Drug Deliv Technol. 2026;16(42s):1358-1368. doi:10.25258/ijddt.16.42s.146.
Chandragirivar PC, Banu A, Raval AM, Kusuma R, Srinidhi G, Yashwanth HB, Suheel A. Improved dissolution performance of fenoprofen calcium using PEG 6000 solid dispersions: preparation by fusion method and physicochemical characterization. Int J Drug Deliv Technol. 2026;16(36s):771-781. doi:10.25258/ijddt.16.36s.87.
Joshi SY, Detholia KK, Raval AM, Dharu NR, Rathod SR, Kushkiwala AM. Development and validation of a stability-indicating RP-HPLC method for quantitative estimation of sunitinib malate in pharmaceutical dosage form. Int J Drug Deliv Technol. 2026;16(12s):418-426. doi:10.25258/ijddt.16.12s.48.
Bhatt R, Raval AM, Patel J, Patel D. Oral thin film drug delivery systems for thrombosis therapy: a comprehensive review. Int J Pharm Sci. 2026;4(1):3563-3576. doi:10.5281/zenodo.18423515.
Prajapati A, Yadav P, Raval AM, Patel J. Review on solid dispersion-based fast dissolving tablets: formulation approaches and evaluation. World J Pharm Med Res. 2025;11(11):109-112. doi:10.5281/zenodo.17483241.
Rowe RC, Sheskey PJ, Quinn ME. Handbook of Pharmaceutical Excipients. 5th ed. London: RPS Publishing; p. 545.
Patel PS, Raval AM, Kumar PA, Kumar PP, Ghanshyam PT. A comprehensive review of antibiotic resistance: mechanisms, causes, and novel therapeutic approaches. Asian Journal of Pharmaceutical Research and Development. 2026 Apr 15;14(2):117-28.
Raval MA, Suthar MA, Durani MB, Thakar MN, Zankhwala MF, Kushkiwala MA, Rathod MS. Smart Co-Processed Excipient Platforms: A Novel Strategy for Multifunctional Optimization of Ibuprofen Tablet Formulations. practice.;1:2.
Kushkiwala AM, Zankhwala FM, Patel MD, Raval AM. Flurbiprofen loaded ethosomal gel: Design, optimization, and anti-inflammatory activity. Int J Res Anal Rev. 2024;11(4):709-42.
Shastri DH, Shaikh MT. A review on liquisolid system. J Drug Deliv Ther. 2014;4(3):25-31.
Amar M. Raval AMR, Krina N Chaudhari KNC, Dr. Bhoomi Arora DBA, Dr. Aastha Ukani DAU, Riddhi Modh RM, Dr. Kuldeep Choubisa DKC, Dr. Ashok Kumar DAK. Emerging Role of GLP-1 and Dual Incretin Agonists in the Management of Type 2 Diabetes Mellitus: Mechanisms, Clinical Evidence, Dosing Strategies, and Future Perspectives. International Journal of Medical and Pharmaceutical Research. 2026 May;7(3):357-370.
Chandel P, Kumari R, Kapoor A. Liquisolid technique: An approach for enhancement of solubility. J Drug Deliv Ther. 2013;3(4):131-137.
Upadhyay J, Yadav P, Patel D, Raval A, Patel J. Review on in-situ depot-based controlled drug delivery for treatment of rheumatoid arthritis treatment. World Journal of Pharmaceutical and Medical Research. 2025 Nov;11(11):113-117. doi:10.5281/zenodo.17483326
Sayed IA, Pavani E. The liquisolid technique-based drug delivery system. Int J Pharm Sci Drug Res. 2012;4(2):88-96.
Raval AM, Rana T, Joshi SY, Buch S, Arora B, Patel VS. Artificial intelligence in pharmacy and healthcare: applications in drug discovery, precision medicine, clinical practice, and future perspectives. Asian Journal of Pharmaceutical Research and Development. 2026 Apr 15;14(2):62-9.
Peddi MG. Novel drug delivery system: Liquisolid compact. J Mol Pharm Org Process Res. 2013;1(3):1-5.
kumar Patel PB, Raval AM, Patel HB, Patel KH, Poorv P, Vaidya PA, Kahar KH. A comprehensive review of polycystic ovary syndrome (PCOS): pathophysiology, diagnosis and management. Asian Journal of Pharmaceutical Research and Development. 2026 Apr 15;14(2):32-41.
Senjaliya T, Patel M, Raval AM. Strategies for combating the global health threat of antibiotic resistance: novel therapeutics and combination approaches. Asian Journal of Pharmaceutical Research and Development. 2026 Feb 15;14(01):122-30.
Chaplin DD. Overview of the human immune response. J Allergy Clin Immunol. 2006;117:S430-S435.
Raval AM, Maneklal RJ, Dilipbhai MU. Development and Evaluation of PolyherbalTopical Cream for Wound Healing Applications Using Alum, Turmeric, and Aloe Vera. Asian Journal of Pharmaceutical Research and Development. 2026 Apr 15;14(2):234-40.
Brodie DH. The pathophysiology of allergic rhinoconjunctivitis. Allergy Asthma Proc. 2007;28:398-403.
Choi SH. Bronchial hyperresponsiveness in young children with allergic rhinitis and associated risk factors. Allergy. 2007;62:1051-1056.
Raval AM, Utpalkumar PF, Utpalkumar PV, Ratnakar BP. Development and Evaluation of Multifunctional Co-Processed Excipients for Fast Dissolving Tablet Formulation. Asian Journal of Pharmaceutical Research and Development. 2026 Apr 15;14(2):226-33.
Bousquet J, Warner JO. Requirements for medications commonly used in treatment of allergic rhinitis. Allergy. 2003;58:192-197.
Simons FE. Advances in H1-antihistamines. N Engl J Med. 2004;351:2203-2217.
Raval AM, Verma AR, Prajapati DS. Efficacy and Safety of Major Antihypertensive Drug Classes in Adults with Hypertension: A Systematic Review. Asian Journal of Pharmaceutical Research and Development. 2026 Apr 15;14(2):216-25.
Wahn U. Levocetirizine in children: Efficacy and safety in a randomized seasonal allergic rhinitis trial. Pediatr Allergy Immunol. 2005;16:267-275.
McNeely W, Wiseman LR. Intranasal azelastine: A review of efficacy in allergic rhinitis. Drugs. 1998;56:91-114.
Panthaki J, Bhai YL, Kumar VS, Raval AM. Formulation and Evaluation of Body Scrub Using Walnut Shell Powder. Asian Journal of Pharmaceutical Research and Development. 2026 Apr 15;14(2):241-7.
Yanez A, Rodrigo GJ. Intranasal corticosteroids versus topical H1 receptor antagonists in allergic rhinitis: Systematic review and meta-analysis. Ann Allergy Asthma Immunol. 2002;89:479-484.
Berger WE, White MV. Efficacy of azelastine nasal spray in patients with unsatisfactory response to loratadine. Ann Allergy Asthma Immunol. 2003;91:205-211.
Lee BJ, Kim YJ. Comparative study of intranasal budesonide and oral terfenadine in perennial allergic rhinitis. J Asthma Allergy Clin Immunol. 2001;21:216-222.
Dhamne MR. TABLET DOSAGE FORM. Journal of Pharmaceutical Research. 2015 Jul;14(3):66-70.
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