Formulation and evaluation of orally disintegrating tablet containing a high concentration of micronized Lurasidone
DOI:
https://doi.org/10.12923/cipms-2026-0017Słowa kluczowe:
specific surface area, orally disintegrating tablets, lurasidone hydrochloride, fluid bed granulationAbstrakt
This study presents the formulation and evaluation of orally disintegrating tablets (ODTs) containing high concentrations of micronized lurasidone hydrochloride, an atypical antipsychotic agent. The research focuses on optimizing two key material attributes: particle size distribution (PSD) and specific surface area (SSA). These optimizations enhance granulation performance and tablet quality. Fluidized-bed granulation was employed alongside dry coating techniques and various glidants to improve powder flowability and reduce cohesion. Comprehensive characterization included pre- and post-compression parameters such as visual evaluation, sieve analysis, weight variation, hardness, tensile strength, friability, disintegration, and dissolution testing. The results demonstrated that API batches with D50 > 3.5 µm achieved 85% drug release within 15 minutes. No significant differences were observed between formulations containing different glidants, indicating flexibility in excipient selection. These results underscore the importance of controlling PSD and SSA and employing effective dry coating and fluidization strategies to produce robust and reproducible ODTs. The developed tablets improve patient compliance and therapeutic efficacy for psychotic disorders and provide valuable insights for the future development of patient-friendly dosage forms.
Bibliografia
1. Greenberg WM, Citrome L. Pharmacokinetics and pharmaco-dynamics of lurasidone hydrochloride, a second-generation antipsychotic: a systematic review of the published literature. Clin Pharmacokinet. 2017;56(5):493-503. doi:10.1007/s40262-016-0475-4.
2. Wasik A, Kołaczkowski M, Wesołowska A. Lurasidon – nowy atypowy neuroleptyk o właściwościach przeciwdepresyjnych. Psychiatria. 2014;11(1):1-18. Available at: www.psychiatria.viamedica.pl
3. Wang J, Huang B, Dai J, Chen G, Ren L. Inclusion complex of lurasidone hydrochloride with sulfobutylether-β-cyclodextrin has enhanced oral bioavailability and no food effect. Am J Transl Res. 2022;14(3):1495-1506.
4. Drugs.com. Lurasidone dosage. Published 2024. https://www.drugs.com/dosage/lurasidone.html. Accessed January 2025.
5. Khailkhura S, Singh B, Joshi D, Semwal N. Orally disintegrating tablet: a review. World J Biol Pharm Health Sci. 2022;11(3):18-25.
6. Prabhu RS, U D, S B, et al. Formulation and management of diseases using oral disintegrating tablet – a review. Int J Pharm Sci Med. 2025;
10(7):1-13.
7. Patil AM, Patil JK, Pawar SP. A review orally disintegrating tablets: recent advancement in formulation & new market opportunities. Int Res J Pharm. 2012;3(4):3212-3231.
8. Przywara M, Leszczak P. Quality by design strategies in fluidized bed granulation: a focus on granules for tablet manufacturing. Adv Sci Technol Res J. 2024;19(2):429-444.
9. Ahlbom J. Comparison of Properties on Orally Disintegrating Tablets (ODTs) Produced by Direct Compression or Fluid Bed Granulation [master's thesis]. Lund, Sweden: Lund University; 2023.
10. Šantl M, Ilić I, Vrečer F, Baumgartner S. A compressibility and compactibility study of real tableting mixtures: the effect of granule particle size. Acta Pharm. 2012;62(3):325-340.
11. Hawkins W, Carlson C. Identifying and resolving common fluid bed dryer issues. FEECO International. Published December 19, 2024. Accessed January 2025. https://feeco.com/identifying-and-resolving-common-fluid-bed-dryer-issues
12. Zhou Y, Zhu J. A review on fluidization of Geldart Group C powders through nanoparticle modulation. Powder Technol. 2021;381:698-720.
13. Ruschmann J. The impact of granule particle size distribution for tablet compression. Hanningfield. Published October 23, 2020. Accessed January 2025. https://www.hanningfield.com/perfecting-particle-size-distribution/
14. Sunkara D, Capece M. Influence of material properties on the effectiveness of glidants used to improve the flowability of cohesive pharmaceutical powders. AAPS PharmSciTech. 2018;19(4):1920-1930.
15. Yang J, Sliva A, Banerjee A, Dave RN, Pfeffer R. Dry particle coating for improving the flowability of cohesive powders. Powder Technol. 2005;158(1-3):21-33.
16. Ho R. Dry coating approaches to enhance powder properties. Presented at: FDA and M-CERSI Workshop ‘Co-Processed API’; 2022.
17. Ramlakhan M, Wu CY, Watano S, Dave RN, Pfeffer R. Dry particle coating using magnetically assisted impaction coating: modification of surface properties and optimization of system and operating parameters. Powder Technol. 2000;112(1-2):137-148.
18. Kim SS, Castillo C, Cheikhali M, Darweesh H, Kossor C, Davé RN. Enhanced blend uniformity and flowability of low drug loaded fine API blends via dry coating: the effect of mixing time and excipient size. Int J Pharm. 2023;635:122722.
19. Leane M, Pitt K, Reynolds G, et al. A proposal for a drug product manufacturing classification system (MCS) for oral solid dosage forms. Pharm Dev Technol. 2015;20(1):12-21.
20. Shah DS, Moravkar KK, Jha DK, Lonkar V, Amin PD, Chalikwar SS. A concise summary of powder processing methodologies for flow enhancement. Heliyon. 2023;9(6):e16498.
21. Murase Y, Takayama K, Uchimoto T, Uchiyama H, Kadota K, Tozuka Y. Prediction of tablet weight variability from bulk flow properties by sparse modeling. Powder Technol. 2022;407:117681.
22. Ghourichay MP, Kiaie SH, Nokhodchi A, Javadzadeh Y. Formulation and quality control of orally disintegrating tablets (ODTs): recent advances and perspectives. Biomed Res Int. 2021;2021:6618934.
23. Kamińska Z, Basa A, Pyzel Ł, Wojasiński M, Szymańska E. Development studies on the orodispersible freeze-dried platforms for lurasidone hydrochloride − understanding the effect of amino acid additive and lyophilization stage. Int J Pharm. 2025;670:125122.
24. Diab ZF, Fares AR, El-Gazayerly ON, AbouGhaly MHH. Lurasidone hydrochloride nanomixed micelles in sublingual orodispersible tablets: in-vitro and in-vivo evaluation. J Drug Deliv Sci Technol. 2026;117:107999.
25. Sanganwar G.P., Gupta R.B. Dissolution-rate enhancement of fenofibrate by adsorption onto silica using supercritical carbon dioxide Int. J. Pharm., 360 (2008), pp. 213-218.
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Prawa autorskie (c) 2026 Bartłomiej Kubiak, Tomasz Bołtromiuk, Katarzyna Sulikowska, Maciej Gajda, Katarzyna Rudzińska, Łukasz Dobrzyński (Autor)
Utwór dostępny jest na licencji Creative Commons Uznanie autorstwa – Użycie niekomercyjne – Bez utworów zależnych 4.0 Międzynarodowe.
