Development and evaluation of an amorphous solid dispersion-based probucol immediate-release tablet
DOI:
https://doi.org/10.69857/joapr.v13i2.997Keywords:
Solid dispersion, Bioavailability, Immediate release, Probucol, SolubilityAbstract
Background: In its crystalline form, probucol has an extremely low bioavailability and is a poor water-soluble drug. The main aim of this study was to enhance the solubility and dissolution rate of probucol by using a solvent evaporation method to develop a solid dispersion that contains polyvinyl pyrrolidone K30 (PVP-K30) and polyethylene glycol 6000 (PEG 6000). Methodology: The solvent evaporation method is considered superior to other techniques for preparing solid dispersions due to its ability to achieve uniform drug distribution at the molecular level. This method ensures homogeneity by dissolving the drug and carrier in a common solvent, reducing the risk of drug recrystallization and enhancing solubility and bioavailability. Result: The drug-to-carrier ratio is the determining factor for dissolution enhancement. The FTIR spectra do not suggest any chemical interaction between PVP-K30 or PEG 6000. The immediate release profiles of both formulations were favourable, with F3 releasing approximately 95.31% of the drug and F6 releasing around 86.77% within 2 hours. This indicates a rapid drug dissolution, which is beneficial for achieving a fast onset of action and enhancing bioavailability. Conclusion: The solid dispersion formulations F3 & F6 successfully transformed crystalline probucol to an amorphous state, enhancing solubility & dissolving rates appropriate for immediate-release tablets.
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References
Budiman A, Hafidz NPM, Azzahra RSS, Amaliah S, Sitinjak FY, Rusdin A, et al. Advancing the Physicochemical Properties and Therapeutic Potential of Plant Extracts Through Amorphous Solid Dispersion Systems. Polymers, 16(24), 3489 (2024) https://doi.org/10.3390/polym16243489.
Miki A, Hara K, Shibata T, Morioka T, Kobayashi A, Yoshimura N, et al. Development of a solid dispersion system for polyvinyl alcohol nanofibers embedded with silicon dioxide particles via emulsion electrospinning for improved solubility of poorly water-soluble drugs. Journal of Drug Delivery Science and Technology, 99, 105915 (2024) https://doi.org/10.1016/j.jddst.2024.105915.
Budiman A, Anastasya G, Handini AL, Lestari IN, Subra L, Diah &, et al. Characterization of Drug with Good Glass-Forming Ability Loaded Mesoporous Silica Nanoparticles and Its Impact Toward in vitro and in vivo Studies. International Journal of Nanomedicine, 6(19), 2199–2225 (2024) http://doi.org/10.2147/IJN.S453873.
Lennernäs H, Brisander M, Liljebris C, Jesson G, Andersson P. Enhanced Bioavailability and Reduced Variability of Dasatinib and Sorafenib with a Novel Amorphous Solid Dispersion Technology Platform. Clinical Pharmacology in Drug Development, 13(9), 985–99 (2024) http://doi.org/10.1002/cpdd.1416.
Zhang J, Guo M, Luo M, Cai T. Advances in the development of amorphous solid dispersions: The role of polymeric carriers. Asian Journal of Pharmaceutical Sciences, 18(4), 100834 (2023) https://doi.org/10.1016/j.ajps.2023.100834.
Butola M, Bhatt V, Nainwal N, Jakhmola V, Dobhal K, Ale Y. Preparation and Evaluation of Polymer Fused Metformin Hydrochloride Sustained Release Tablet. Indian Journal of Pharmaceutical Education and Research, 57(3),711–717 (2024) http://doi.org/10.5530/ijper.57.3.86.
Salazar-Barrantesid KA, Abdala-Saiz A, Roberto Vega-Baudritid J, Navarro-Hoyos M, Araya-Sibajaid AM. Formulation, and evaluation of atorvastatin calcium trihydrate Form I tablets. PLoS One, 20(2), 1-21 (2025) https://doi.org/10.1371/journal.pone.0317407
Butola M, Badola A, Nainwal N, Rana S, Jakhmola V, Ale Y, et al. Formulation of Sustained-Release Tablets of Tolperisone HCl Using Different Blends of Hydrophilic and Hydrophobic Polymers. Indian Journal of Pharmaceutical Education and Research, 58(3s), s872-s879 (2024) http://doi.org/10.5530/ijper.58.3s.88.
Rusli D, Umar S, Aldi Y, Usman H, Siregar MN, Zaini E. Enhancement of Aceclofenac Dissolution Rate via Solid Dispersion with Hydroxypropyl Methylcellulose. Tropical Journal of Natural Product Research, 9(1), (2025) https://doi.org/10.26538/tjnpr/v9i1.22.
Shah DD, Taylor LS. Chemistry and ionization of HPMCAS influences the dissolution and solution-mediated crystallization of posaconazole amorphous solid dispersions. Journal of Drug Delivery Science and Technology, 114(1), 223–233 (2025) https://doi.org/10.1016/j.xphs.2024.08.023.
Sapkal R, Devangan P, Madan J, Dikundwar AG. Neat amorphous form and amorphous solid dispersions of apalutamide: A comparative study. Journal of Drug Delivery Science and Technology, 106, 106678 (2025) https://doi.org/10.1016/j.jddst.2025.106678.
Chavan RB, Lodagekar A, Yadav B, Shastri NR. Amorphous solid dispersion of nisoldipine by solvent evaporation technique: preparation, characterization, in vitro, in vivo evaluation, and scale up feasibility study. Drug Delivery and Translational Research, 10(4), 903–918 (2020) https://doi.org/10.1007/s13346-020-00775-8.
Yilmaz A, Mutlu-Agardan NB, Takka S. Development of immediate release tablet formulations of lornoxicam with hot melt extrusion-based three-dimensional printing technology. Drug Delivery and Translational Research, 51(1), 64-76 (2024) http://doi.org/10.1080/03639045.2024.2447277.
Lee J, Goodwin DJ, Dhenge RM, Nassar J, Zeitler A. Terahertz-Based Analysis of Immediate-Release Tablet Hydration and Disintegration: Effects of Croscarmellose Sodium and Magnesium Stearate. International journal of pharmaceutics, (675), 125478 (2025) http://doi.org/10.1016/j.ijpharm.2025.125478.
Phanapithakkun S, Yusakul G, Sitthisak C, Plyduang T. Development of tablet formulations containing genistein solid dispersion optimized using Box-Behnken design for enhanced solubility. Journal of Applied Pharmaceutical Sciences, 15(4), (2025) http://doi.org/10.7324/JAPS.2025.222224.
Qu B, Wu H, Ding Z, Bu R, Zhang H, Han J, et al. Amorphous Solid Dispersion Formulation of Pimobendan for Bioavailability Enhancement: A Comprehensive Study on Miscibility, Interactions, and in Vitro Dissolution Behavior. Journal of Drug Delivery Science and Technology, 108, 106884 (2025) https://doi.org/10.1016/j.jddst.2025.106884.
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Copyright (c) 2025 Vaibhav Adhikari, Mansi Butola, Vikash Jakhmola, Abhijeet Ojha, Arvind Negi
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