Formulation and in vitro evaluation of an effervescent floating tablet of cefpodoxime proxetil prepared as an amorphous solid dispersion
Article Sidebar
Main Article Content
Abstract
This study aimed to prepare an effervescent floating tablet to protect cefpodoxime proxetil (CP) from enzymatic hydrolysis and higher pH degradation in the lower parts of the gastrointestinal tract (GIT). CP was prepared as amorphous solid dispersion (ASD) with soluplus and Polyvinylpyrrolidone K30 (PVP K30) in a ratio of 1:1:1 by solvent evaporation technology.
Effervescent floating tablet formulations were prepared in different compositions and ratios by direct compression techniques using polyethylene oxide (PEO), hydroxypropyl methylcellulose K4M (HPMC K4M), sodium alginate (Na alginate) as a hydrophilic matrix, sodium bicarbonate (NaHCO3), and citric acid as a gas-generating agent. These formulations were evaluated for floating ability and in vitro drug release. Then, an optimized tablet was performed to determine the hardness, friability, content uniformity, weight variation, and swelling index. The optimum formulation showed good buoyancy properties and extended drug release characteristics for 24 hours (hrs). The post-compression evaluation's parameters are within the limits of U.S. Pharmacopoeia. According to these results, the development of effervescent floating tablets of CP prepared as ASD could be effectively applied.
Article Details
Section
This work is licensed under a Creative Commons Attribution 4.0 International License.
How to Cite
References
1- Bajracharya, R., J.G. Song, S.Y. Back and H.-K. Han, Recent advancements in non-invasive formulations for protein drug delivery. Computational and structural biotechnology journal, 2019. 17: p. 1290-1308. DOI: https://doi.org/10.1016/j.csbj.2019.09.004
2- Zainab Saad, K., M. Masar Basim Mohsin and N. Nawfal Am, Organogel investigations as a floating oral system with depot property. Al Mustansiriyah Journal of Pharmaceutical Sciences, 2022. 20(4): p. 132-146. DOI: https://doi.org/10.32947/ajps.v20i4.783
3- Devadasu, V.R., P.K. Deb, R. Maheshwari, P. Sharma and R.K. Tekade, Physicochemical, pharmaceutical, and biological considerations in GIT absorption of drugs, in Dosage Form Design Considerations. 2018, Elsevier. p. 149-178. DOI: https://doi.org/10.1016/B978-0-12-814423-7.00005-8
4- Wang, Y., C. Pi, X. Feng, Y. Hou, L. Zhao and Y. Wei, The influence of nanoparticle properties on oral bioavailability of drugs. International journal of nanomedicine, 2020: p. 6295-6310. DOI: https://doi.org/10.2147/IJN.S257269
5- Lang, X., T. Wang, M. Sun, X. Chen and Y. Liu, Advances and applications of chitosan-based nanomaterials as oral delivery carriers: A review. Int J Biol Macromol, 2020. 154: p. 433-445. DOI: https://doi.org/10.1016/j.ijbiomac.2020.03.148
6- Ahadian, S., J.A. Finbloom, M. Mofidfar, S.E. Diltemiz, F. Nasrollahi, E. Davoodi, et al., Micro and nanoscale technologies in oral drug delivery. Adv Drug Del Rev, 2020. 157: p. 37-62. DOI: https://doi.org/10.1016/j.addr.2020.07.012
7- Ding, H., P. Tan, S. Fu, X. Tian, H. Zhang, X. Ma, et al., Preparation and application of pH-responsive drug delivery systems. J Control Release, 2022. 348: p. 206-238. DOI: https://doi.org/10.1016/j.jconrel.2022.05.056
8- Raza, A., S.C. Ngieng, F.B. Sime, P.J. Cabot, J.A. Roberts, A. Popat, et al., Oral meropenem for superbugs: challenges and opportunities. Drug Discovery Today, 2021. 26(2): p. 551-560. DOI: https://doi.org/10.1016/j.drudis.2020.11.004
9- Prajapati, V.D., G.K. Jani, T.A. Khutliwala and B.S. Zala, Raft forming system—An upcoming approach of gastroretentive drug delivery system. J Control Release, 2013. 168(2): p. 151-165. DOI: https://doi.org/10.1016/j.jconrel.2013.02.028
10- Chen, Y.-C., H.-O. Ho, T.-Y. Lee and M.-T. Sheu, Physical characterizations and sustained release profiling of gastroretentive drug delivery systems with improved floating and swelling capabilities. Int J Pharm, 2013. 441(1-2): p. 162-169. DOI: https://doi.org/10.1016/j.ijpharm.2012.12.002
11- Sen, O., S. Manna, G. Nandi, S. Jana and S. Jana, Recent advances in alginate based gastroretentive technologies for drug delivery applications. Medicine in Novel Technology and Devices, 2023: p. 100236. DOI: https://doi.org/10.1016/j.medntd.2023.100236
12- Shakya, R., P. Thapa and R.N. Saha, In vitro and in vivo evaluation of gastroretentive floating drug delivery system of ofloxacin. asian journal of pharmaceutical sciences, 2013. 8(3): p. 191-198. DOI: https://doi.org/10.1016/j.ajps.2013.07.025
13- de Souza, M.P.C., R.M. Sábio, T. de Cassia Ribeiro, A.M. Dos Santos, A.B. Meneguin and M. Chorilli, Highlighting the impact of chitosan on the development of gastroretentive drug delivery systems. Int J Biol Macromol, 2020. 159: p. 804-822. DOI: https://doi.org/10.1016/j.ijbiomac.2020.05.104
14- Chen, R.-N., H.-O. Ho, C.-Y. Yu and M.-T. Sheu, Development of swelling/floating gastroretentive drug delivery system based on a combination of hydroxyethyl cellulose and sodium carboxymethyl cellulose for Losartan and its clinical relevance in healthy volunteers with CYP2C9 polymorphism. Eur J Pharm Sci, 2010. 39(1-3): p. 82-89. DOI: https://doi.org/10.1016/j.ejps.2009.10.015
15- Vo, A.Q., X. Feng, M. Pimparade, X. Ye, D.W. Kim, S.T. Martin, et al., Dual-mechanism gastroretentive drug delivery system loaded with an amorphous solid dispersion prepared by hot-melt extrusion. Eur J Pharm Sci, 2017. 102: p. 71-84. DOI: https://doi.org/10.1016/j.ejps.2017.02.040
16- Sarparanta, M.P., L.M. Bimbo, E.M. Mäkilä, J.J. Salonen, P.H. Laaksonen, A.K. Helariutta, et al., The mucoadhesive and gastroretentive properties of hydrophobin-coated porous silicon nanoparticle oral drug delivery systems. Biomaterials, 2012. 33(11): p. 3353-3362. DOI: https://doi.org/10.1016/j.biomaterials.2012.01.029
17- Eberle, V.A., J. Schoelkopf, P.A. Gane, R. Alles, J. Huwyler and M. Puchkov, Floating gastroretentive drug delivery systems: Comparison of experimental and simulated dissolution profiles and floatation behavior. Eur J Pharm Sci, 2014. 58: p. 34-43. DOI: https://doi.org/10.1016/j.ejps.2014.03.001
18- Sheikh, F.A., M.A. Hussain, M.U. Ashraf, M.T. Haseeb and M. Farid-ul-Haq, Linseed hydrogel based floating drug delivery system for fluoroquinolone antibiotics: Design, in vitro drug release and in vivo real-time floating detection. Saudi Pharmaceutical Journal, 2020. 28(5): p. 538-549. DOI: https://doi.org/10.1016/j.jsps.2020.03.005
19- Sharma, N., D. Agarwal and M. Gupta, A comprehensive review on floating drug delivery system.
20- Rahamathulla, M., S. Saisivam and H. Gangadharappa, Development of valsartan floating matrix tablets using low density polypropylene foam powder: In vitro and in vivo evaluation. AAPS PharmSciTech, 2019. 20: p. 1-10. DOI: https://doi.org/10.1208/s12249-018-1265-z
21- Safa Mohammed, N., A.-S. Athmar Dhahir Habeeb and A. Alaa, Effect of using high molecular weight crosslinker on the physical properties of super porous hydrogel composite. Al Mustansiriyah Journal of Pharmaceutical Sciences, 2023. 23(4): p. 355-366. DOI: https://doi.org/10.32947/ajps.v23i4.1091
22- Lopes, C.M., C. Bettencourt, A. Rossi, F. Buttini and P. Barata, Overview on gastroretentive drug delivery systems for improving drug bioavailability. Int J Pharm, 2016. 510(1): p. 144-158. DOI: https://doi.org/10.1016/j.ijpharm.2016.05.016
23- Liu, H., S. Wang, H. Shi, R. Zhang, K. Qu, Y. Hu, et al., Gastric floating tablet improves the bioavailability and reduces the hypokalemia effect of gossypol in vivo. Saudi Pharmaceutical Journal, 2021. 29(4): p. 305-314. DOI: https://doi.org/10.1016/j.jsps.2021.03.001
24- Hani, U., R.A.M. Osmani, A. Alqahtani, M. Ghazwani, M. Rahamathulla, S.A. Almordy, et al., 2 3 full factorial design for formulation and evaluation of floating oral in situ gelling system of piroxicam. J Pharm Innov, 2021. 16: p. 528-536. DOI: https://doi.org/10.1007/s12247-020-09471-z
25- Pawar, V.K., S. Kansal, G. Garg, R. Awasthi, D. Singodia and G.T. Kulkarni, Gastroretentive dosage forms: A review with special emphasis on floating drug delivery systems. Drug Deliv, 2011. 18(2): p. 97-110. DOI: https://doi.org/10.3109/10717544.2010.520354
26- Kim, S., K.-M. Hwang, Y.S. Park, T.-T. Nguyen and E.-S. Park, Preparation and evaluation of non-effervescent gastroretentive tablets containing pregabalin for once-daily administration and dose proportional pharmacokinetics. Int J Pharm, 2018. 550(1-2): p. 160-169. DOI: https://doi.org/10.1016/j.ijpharm.2018.08.038
27- Nabil, R., O.Y. Mady, A.A. Mubarak and A. Donia, Formulation & assessment of combined antibiotics in a floating oblong tablet for treatment of H. pylori:(A) Radiological imaging to prove the floating of a high-weight oblong tablet. J Drug Deliv Sci Technol, 2021. 64: p. 102573. DOI: https://doi.org/10.1016/j.jddst.2021.102573
28- Zhou, Y., N. Gu and F. Yang, In situ microbubble-assisted, ultrasound-controlled release of superparamagnetic iron oxide nanoparticles from gastro-retentive tablets. Int J Pharm, 2020. 586: p. 119615. DOI: https://doi.org/10.1016/j.ijpharm.2020.119615
29- Gambhire, M.N., K.W. Ambade, S.D. Kurmi, V.J. Kadam and K.R. Jadhav, Development and in vitro evaluation of an oral floating matrix tablet formulation of diltiazem hydrochloride. AAPS PharmSciTech, 2007. 8: p. E166-E174. DOI: https://doi.org/10.1208/pt0803073
30- Todd, W.M., Cefpodoxime proxetil: a comprehensive review. Int J Antimicrob Agents, 1994. 4(1): p. 37-62. DOI: https://doi.org/10.1016/0924-8579(94)90062-0
31- Veeraraghavan, B., Y.D. Bakthavatchalam and R.D. Sahni, Oral antibiotics in clinical development for community-acquired urinary tract infections. Infectious Diseases and Therapy, 2021. 10(4): p. 1815-1835. DOI: https://doi.org/10.1007/s40121-021-00509-4
32- O’Donnell, J., A. Tanudra, A. Chen, D. Hines, R. Tommasi and J. Mueller, Pharmacokinetic/pharmacodynamic determination and preclinical pharmacokinetics of the β-lactamase inhibitor ETX1317 and its orally available prodrug ETX0282. ACS Infectious Diseases, 2020. 6(6): p. 1378-1388. DOI: https://doi.org/10.1021/acsinfecdis.0c00019
33- Mujtaba, A., M. Ali and K. Kohli, Statistical optimization and characterization of pH-independent extended-release drug delivery of cefpodoxime proxetil using Box–Behnken design. Chem Eng Res Des, 2014. 92(1): p. 156-165. DOI: https://doi.org/10.1016/j.cherd.2013.05.032
34- Patil, P., S. Suryawanshi, S. Patil and A. Pawar, HME-assisted formulation of taste-masked dispersible tablets of cefpodoxime proxetil and roxithromycin. Journal of Taibah University Medical Sciences, 2023. DOI: https://doi.org/10.1016/j.jtumed.2023.12.004
35- Yurtdaş-Kırımlıoğlu, G., Development and characterization of lyophilized cefpodoxime proxetil-Pluronic® F127/polyvinylpyrrolidone K30 solid dispersions with improved dissolution and enhanced antibacterial activity. Pharm Dev Technol, 2021. 26(4): p. 476-489. DOI: https://doi.org/10.1080/10837450.2021.1889584
36- Jindal, A. and A. Kumar, Physical characterization of clove oil based self Nano-emulsifying formulations of cefpodoxime proxetil: Assessment of dissolution rate, antioxidant & antibacterial activity. OpenNano, 2022. 8: p. 100087. DOI: https://doi.org/10.1016/j.onano.2022.100087
37- Kakumanu, V.K., V. Arora and A.K. Bansal, Investigation of factors responsible for low oral bioavailability of cefpodoxime proxetil. Int J Pharm, 2006. 317(2): p. 155-160. DOI: https://doi.org/10.1016/j.ijpharm.2006.03.004
38- Crauste-Manciet, S., J. Huneau, M. Decroix, D. Tome, R. Farinotti and J. Chaumeil, Cefpodoxime proxetil esterase activity in rabbit small intestine: a role in the partial cefpodoxime absorption. Int J Pharm, 1997. 149(2): p. 241-249. DOI: https://doi.org/10.1016/S0378-5173(97)04881-3
39- Khan, F., R. Katara and S. Ramteke, Enhancement of bioavailability of cefpodoxime proxetil using different polymeric microparticles. AAPS PharmSciTech, 2010. 11: p. 1368-1375. DOI: https://doi.org/10.1208/s12249-010-9505-x
40- Hamaura, T., A. Kusai and K. Nishimura, Gel formation of cefpodoxime proxetil. STP Pharma Sci, 1995. 5(4): p. 324-331.
41- Pooresmaeil, M., S. Javanbakht, H. Namazi and A. Shaabani, Application or function of citric acid in drug delivery platforms. Med Res Rev, 2022. 42(2): p. 800-849. DOI: https://doi.org/10.1002/med.21864
42- Borin, M.T., A review of the pharmacokinetics of cefpodoxime proxetil. Drugs, 1991. 42: p. 13-21. DOI: https://doi.org/10.2165/00003495-199100423-00005
43- Merchant, H.A., H.M. Shoaib, J. Tazeen and R.I. Yousuf, Once-daily tablet formulation and in vitro release evaluation of cefpodoxime using hydroxypropyl methylcellulose: a technical note. AAPS PharmSciTech, 2006. 7: p. E178-E183. DOI: https://doi.org/10.1208/pt070378
44- Sharma, N., N. Jain, C. Sudhakar and S. Jain, Formulation and evaluation of gastro retentive floating tablets containing cefpodoximeproxetil solid dispersions. International Journal of Current Pharmaceutical Research, 2012. 4(4): p. 82-87.
45- Kukati, L., K. Chittimalli and N. Shaik, Formulation and Evaluation of Floating Tablets of Cefpodoxime Proxetil. Journal of scientific research, 2014. 6(3). DOI: https://doi.org/10.3329/jsr.v6i3.18339
46- Wan, S., C. Dai, Y. Bai, W. Xie, T. Guan, H. Sun, et al., Application of multivariate methods to evaluate differential material attributes of HPMC from different sources. ACS omega, 2021. 6(43): p. 28598-28610. DOI: https://doi.org/10.1021/acsomega.1c03009
47- Jadach, B., W. Świetlik and A. Froelich, Sodium alginate as a pharmaceutical excipient: novel applications of a well-known polymer. J Pharm Sci, 2022. 111(5): p. 1250-1261. DOI: https://doi.org/10.1016/j.xphs.2021.12.024
48- Mahdi, A.A., Q.A. Al-Maqtari, W. Al-Ansi, W. Hu, S.B. Hashim, H. Cui, et al., Replacement of polyethylene oxide by peach gum to produce an active film using Litsea cubeba essential oil and its application in beef. Int J Biol Macromol, 2023. 241: p. 124592. DOI: https://doi.org/10.1016/j.ijbiomac.2023.124592
49- Lateef, S., M. Basim and A. Mohammed, Effect Of Different Variables On The Formulation Of Sodium Alginate Beads. Al Mustansiriyah Journal of Pharmaceutical Sciences, 2024. 24(2): p. 117-126. DOI: https://doi.org/10.32947/ajps.v24i2.1007
50- Bharati, S., V. Gaikwad and B. Chellampillai, Biopharmaceutical advancement of efonidipine hydrochloride ethanolate through amorphous solid dispersion of a Parteck SLC mesoporous silica polymer. RSC Pharmaceutics, 2024. DOI: https://doi.org/10.1039/D4PM00113C
51- Szabó, E., P. Záhonyi, D.n. Brecska, D.n.L. Galata, L.A. Mészáros, L. Madarász, et al., Comparison of amorphous solid dispersions of spironolactone prepared by spray drying and electrospinning: The influence of the preparation method on the dissolution properties. Mol Pharm, 2020. 18(1): p. 317-327. DOI: https://doi.org/10.1021/acs.molpharmaceut.0c00965
52- Tkachenko, Y. and P. Niedzielski, FTIR as a method for qualitative assessment of solid samples in geochemical research: a review. Molecules, 2022. 27(24): p. 8846. DOI: https://doi.org/10.3390/molecules27248846
53- Huang, Z., C. Xu, L. Zhao, C. Wei, Y. Wu, J. Qiu, et al., Preparation, optimization and in vivo study of gastric floating tablets of constunolide and dehydrocostus lactone with ideal therapeutic effect on gastric diseases. J Drug Deliv Sci Technol, 2022. 78: p. 103942. DOI: https://doi.org/10.1016/j.jddst.2022.103942
54- Rahamathulla, M., S.M. Alshahrani, A. Al Saqr, A. Alshetaili and F. Shakeel, Effervescent floating matrix tablets of a novel anti-cancer drug neratinib for breast cancer treatment. J Drug Deliv Sci Technol, 2021. 66: p. 102788. DOI: https://doi.org/10.1016/j.jddst.2021.102788
55- Amrutkar, P., P. Chaudhari and S. Patil, Design and in vitro evaluation of multiparticulate floating drug delivery system of zolpidem tartarate. Colloids Surf B Biointerfaces, 2012. 89: p. 182-187. DOI: https://doi.org/10.1016/j.colsurfb.2011.09.011
56- Raza, A., N. Shen, J. Li, Y. Chen and J.-Y. Wang, Formulation of zein based compression coated floating tablets for enhanced gastric retention and tunable drug release. Eur J Pharm Sci, 2019. 132: p. 163-173. DOI: https://doi.org/10.1016/j.ejps.2019.01.025
57- 57. Li, P., S. Zhang, W. Sun, M. Cui, H. Wen, Q. Li, et al., Flexibility of 3D extruded printing for a novel controlled-release puerarin gastric floating tablet: design of internal structure. AAPS PharmSciTech, 2019. 20: p. 1-13. DOI: https://doi.org/10.1208/s12249-019-1455-3
58- Qi, X., H. Chen, Y. Rui, F. Yang, N. Ma and Z. Wu, Floating tablets for controlled release of ofloxacin via compression coating of hydroxypropyl cellulose combined with effervescent agent. Int J Pharm, 2015. 489(1-2): p. 210-217. DOI: https://doi.org/10.1016/j.ijpharm.2015.05.007
59- Arza, R.A.K., C.S.R. Gonugunta and P.R. Veerareddy, Formulation and evaluation of swellable and floating gastroretentive ciprofloxacin hydrochloride tablets. AAPS PharmSciTech, 2009. 10: p. 220-226. DOI: https://doi.org/10.1208/s12249-009-9200-y
60- Alhamdany, A.T. and A.K. Abbas, Formulation and in vitro evaluation of amlodipine gastroretentive floating tablets using a combination of hydrophilic and hydrophobic polymers. Int J App Pharm, 2018. 10(6): p. 126-134. DOI: https://doi.org/10.22159/ijap.2018v10i6.28687
61- Hamdi, D.S. and M.B.M. Mohamed, Formulation of metoclopramide HCl gastroretentive film and in vitro-in silico prediction using Gastroplus® PBPK software. Saudi Pharmaceutical Journal, 2022. 30(12): p. 1816-1824. DOI: https://doi.org/10.1016/j.jsps.2022.10.011
62- Streubel, A., J. Siepmann and R. Bodmeier, Floating matrix tablets based on low density foam powder: effects of formulation and processing parameters on drug release. Eur J Pharm Sci, 2003. 18(1): p. 37-45. DOI: https://doi.org/10.1016/S0928-0987(02)00223-3
63- Monton, C., T. Wunnakup, J. Suksaeree, L. Charoenchai and N. Chankana, Impact of Compressional Force, Croscarmellose Sodium, and Microcrystalline Cellulose on Black Pepper Extract Tablet Properties Based on Design of Experiments Approach. Sci Pharm, 2023. 91(3): p. 30. DOI: https://doi.org/10.3390/scipharm91030030
64- Tadros, M.I., Controlled-release effervescent floating matrix tablets of ciprofloxacin hydrochloride: Development, optimization and in vitro–in vivo evaluation in healthy human volunteers. Eur J Pharm Biopharm, 2010. 74(2): p. 332-339. DOI: https://doi.org/10.1016/j.ejpb.2009.11.010
65- Nguyen, T.-T., K.-M. Hwang, S.-H. Kim and E.-S. Park, Development of novel bilayer gastroretentive tablets based on hydrophobic polymers. Int J Pharm, 2020. 574: p. 118865. DOI: https://doi.org/10.1016/j.ijpharm.2019.118865