Design and evaluation of the floating oral in situ gelling system of levofloxacin hemihydrate to dysphagia patients
Keywords:
floating oral, in situ gel, levofloxacin hemyhdrate, optimization, sustained release
Abstract
Pediatric, geriatric, and dysphagia patients often experience difficulty swallowing solid preparations and discomfort when administered by injection. Levofloxacin is marketed as available in tablet and injection forms, such as in Indonesia. This study aims to develop an aqueous dispersion formulation for a floating oral gelling system of levofloxacin hemihydrate with sustained release delivery. HPMC and sodium alginate were combined as polymers to form an in situ gel system in an acidic environment. The optimization was performed based on the simplex lattice mixture design method. The effect of variations in the concentration of both polymers influenced the viscosity of the formula. The optimum formula was 0.378% sodium alginate and 0.122% HPMC. The drug release mechanism of the optimum formula followed the Korsmeyer-Peppas model. The kinetic mechanism of drug release fits into 2-compartment. The developed formulation offers augmented gastric retention of levofloxacin hemihydrate, leading to improved efficacy.
References
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Ahmed, M. G., Kapoor, C., & A, S. (2017). FORMULATION AND EVALUATION OF ORAL SUSTAINED IN SITU GELLING SYSTEM OF ROXATIDINE. INDONESIAN JOURNAL OF PHARMACY, 28(3), 178. https://doi.org/10.14499/indonesianjpharm28iss3pp178
Arshad, M. S., Kiran, M., Mudassir, J., Farhan, M., Hussain, A., & Abbas, N. (2022). Formulation, Optimization, in vitro and in-vivo evaluation of levofloxacin hemihydrate Floating Tablets. Brazilian Journal of Pharmaceutical Sciences, 58, e18630. https://doi.org/10.1590/s2175-97902022e18630
Bashir, R., Majeed, A., Ali, T., Farooq, S., & Khan, N. A. (2019). Floating Oral In-Situ Gel: A Review. Journal of Drug Delivery and Therapeutics, 9(2), 442–448. https://doi.org/10.22270/jddt.v9i2.2372
Direktorat Registrasi Obat. (2024). Produk obat komparator. https://registrasiobat.pom.go.id/daftar-produk/produk-obat-komparator
El-Zahaby, S. A., Kassem, A. A., & El-Kamel, A. H. (2014a). Design and evaluation of gastroretentive levofloxacin floating mini-tablets-in-capsule system for eradication of Helicobacter pylori. Saudi Pharmaceutical Journal, 22(6), 570–579. https://doi.org/10.1016/j.jsps.2014.02.009
El-Zahaby, S. A., Kassem, A. A., & El-Kamel, A. H. (2014b). Formulation and in vitro evaluation of size expanding gastro-retentive systems of levofloxacin hemihydrate. International Journal of Pharmaceutics, 464(1–2), 10–18. https://doi.org/10.1016/j.ijpharm.2014.01.024
Hani, U., Osmani, R. A. M., Alqahtani, A., Ghazwani, M., Rahamathulla, M., Almordy, S. A., & Alsaleh, H. A. (2021). 23 Full Factorial Design for Formulation and Evaluation of Floating Oral In Situ Gelling System of Piroxicam. Journal of Pharmaceutical Innovation, 16(3), 528–536. https://doi.org/10.1007/s12247-020-09471-z
Patil, H., Tiwari, R. V., & Repka, M. A. (2016). Recent advancements in mucoadhesive floating drug delivery systems: A mini-review. Journal of Drug Delivery Science and Technology, 31, 65–71. https://doi.org/10.1016/j.jddst.2015.12.002
Pawestri, S. A., Nugroho, A. K., & Lukitaningsih, E. (2021). In vitro Transdermal Transport of Domperidone by Compartmental Modeling Approach. Indonesian Journal of Pharmacy, 10–16. https://doi.org/10.22146/ijp.608
Pawestri, S. A., Nugroho, A. K., Lukitaningsih, E., & Purwantiningsih. (2021a). Compartmental Modeling Approach: Application on Transdermal Delivery for In Vitro Drug Permeation Mechanism Analysis. Journal of Food and Pharmaceutical Sciences, 481–486. https://doi.org/10.22146/jfps.2198
Pawestri, S. A., Nugroho, A. K., Lukitaningsih, E., & Purwantiningsih. (2021b). Evaluation and Optimization on Developed Transdermal Patch of Domperidone Formulation. International Journal of Pharmaceutical Research, 13(2), 3345–3353.
Permanadewi, I., Kumoro, A. C., Wardhani, D. H., & Aryanti, N. (2019). Modelling of controlled drug release in gastrointestinal tract simulation. Journal of Physics: Conference Series, 1295(1), 012063. https://doi.org/10.1088/1742-6596/1295/1/012063
Rajendra Suryawanshi, V., Ramashray Yadav, H., & Chatur Surani, H. (2022). Formulation & charecterizaion of anti-microbial property of herbal oral in-situ gel. Materials Today: Proceedings, 51, 2339–2347. https://doi.org/10.1016/j.matpr.2021.11.569
Rowe, R., Sheskey, P., & Quinn, M. (2009). Handbook of Pharmaceutical Excipients (6. ed). APhA, (PhP) Pharmaceutical Press.
Sharma, A., Sharma, J., Kaur, R., & Saini, V. (2014). Development and Characterization of In Situ Oral Gel of Spiramycin. BioMed Research International, 2014, 1–7. https://doi.org/10.1155/2014/876182
Sharma, S., Sarkar, G., Srestha, B., Chattopadhyay, D., & Bhowmik, M. (2019). In-situ fast gelling formulation for oral sustained drug delivery of paracetamol to dysphagic patients. International Journal of Biological Macromolecules, 134, 864–868. https://doi.org/10.1016/j.ijbiomac.2019.05.092
Siripruekpong, W., Kerdsakundee, N., Parinyakub, T., & Wiwattanapatapee, R. (2017). Development and Evaluation of floating In situ gel for oral delivery of propranolol HCl. 5.
Solanki, R., Parikh, F. J., & Goyal, S. (2018). Formulation and Evaluation of Floatable In Situ Gel of Ofloxacin. Asian Journal of Pharmaceutics (AJP), 12(02), Article 02. https://doi.org/10.22377/ajp.v12i02.2420
Xu, H., Shi, M., liu, Y., Jiang, J., & Ma, T. (2014). A Novel In Situ Gel Formulation of Ranitidine for Oral Sustained Delivery. Biomolecules & Therapeutics, 22(2), 161–165. https://doi.org/10.4062/biomolther.2013.109
Zhang, Y., Huo, M., Zhou, J., Zou, A., Li, W., Yao, C., & Xie, S. (2010). DDSolver: An Add-In Program for Modeling and Comparison of Drug Dissolution Profiles. The AAPS Journal, 12(3), 263–271. https://doi.org/10.1208/s12248-010-9185-1
Published
2025-02-14
How to Cite
Pawestri, S. A., & Nugroho, A. K. (2025). Design and evaluation of the floating oral in situ gelling system of levofloxacin hemihydrate to dysphagia patients. Indonesian Journal of Pharmacy. https://doi.org/10.22146/ijp.12224
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Research Article
