Formulation and evaluation of stiripentol oral suspension
DOI:
https://doi.org/10.30827/ars.v66i3.31529Keywords:
Stiripentol, suspension, viscosity, sedimentation volume, zeta potentialAbstract
Introducción: El trabajo de investigación se llevó a cabo para desarrollar una suspensión estable y eficaz de estiripentol para el tratamiento de la epilepsia.
Método: Se utilizó el estudio FT-IR para evaluar la compatibilidad entre el fármaco y el excipiente y también se examinó la apariencia física de la mezcla del fármaco y el excipiente después de un mes de estudio de estabilidad. La suspensión se preparó mediante un agitador mecánico y se evaluó la viscosidad, el pH, el volumen de sedimentación, el potencial zeta y los estudios de liberación de fármaco in vitro. La formulación optimizada se evaluó adicionalmente para determinar el potencial zeta y el índice de polidispersidad.
Resultados: Los resultados de FT-IR confirmaron la compatibilidad del fármaco y los excipientes. La apariencia física de la mezcla no se alteró durante las condiciones de almacenamiento aceleradas. La viscosidad, el pH y el volumen de sedimentación de la formulación oscilaron entre 22,92 ±1,2 cPs y 54,8 ± 2,1 cPs; 5,32 ± 0,04 y 6,01 ± 0,1 y 83,19 ± 0,9 % y 98,87 ± 1,2 % respectivamente. El potencial zeta y el índice de polidispersidad de la formulación optimizada fueron -52,1 mV y 0,198 respectivamente. Estos resultados fueron indicativos de una suspensión monodispersa estable. La formulación optimizada fue estable a temperaturas y humedad más altas y en presencia de luz, lo que indica una buena vida útil.
Conclusiones: El estudio demostró que la suspensión oral de estiripentol puede formularse como una forma farmacéutica estable y eficaz para el tratamiento de la epilepsia.
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Hameed Z, Saleem S, Mirza J, Mustafa MS,Qamar Ul I. Characterisation of ictal and interictal states of epilepsy: A system dynamic approach of principal dynamic modes analysis. PLoS One. 2018; 13(1):e0191392. doi:10.1371/journal.pone.0191392. DOI: https://doi.org/10.1371/journal.pone.0191392
Rho JM,Sankar R. The pharmacologic basis of antiepileptic drug action. Epilepsia. 1999; 40(11):1471-83. DOI: https://doi.org/10.1111/j.1528-1157.1999.tb02029.x
Fisher JL. The effects of stiripentol on GABA(A) receptors. Epilepsia. 2011; 52 Suppl 2(2):76-8. doi:10.1111/j.1528-1167.2011.03008.x. DOI: https://doi.org/10.1111/j.1528-1167.2011.03008.x
Uchida Y, Terada K, Madokoro Y, et al. Stiripentol for the treatment of super-refractory status epilepticus with cross-sensitivity. Acta Neurol Scand. 2018; 137(4):432-37. doi:10.1111/ane.12888. DOI: https://doi.org/10.1111/ane.12888
Chiron C, Chemaly N, Chancharme L,Nabbout R. Initiating stiripentol before 2 years of age in patients with Dravet syndrome is safe and beneficial against status epilepticus. Dev Med Child Neurol. 2023; 65(12):1607-16. doi:10.1111/dmcn.15638. DOI: https://doi.org/10.1111/dmcn.15638
Wheless J,Weatherspoon S. Use of Stiripentol in Dravet syndrome: A guide for clinicians. Pediatr Neurol. 2024; doi:10.1016/j.pediatrneurol.2024.10.015. DOI: https://doi.org/10.1016/j.pediatrneurol.2024.10.015
Wang Y, Xu S, Xiao Z, et al. Stiripentol enteric solid dispersion-loaded effervescent tablets: Enhanced dissolution, stability, and absorption. AAPS PharmSciTech. 2022; 23(5):141. doi:10.1208/s12249-022-02261-5. DOI: https://doi.org/10.1208/s12249-022-02261-5
Vázquez-Blanco S, González-Freire L, Dávila-Pousa MC,Crespo-Diz C. pH determination as a quality standard for the elaboration of oral liquid compounding formula. Farm Hosp. 2018; 42(6):221-27. doi:10.7399/fh.10932.
Oppong EE, Osei-Asare C,Klu MW. Evaluation of the suspending properties of shea tree gum. Int J Pharm Pharm Sci. 2016; 8(7):409-13.
Shah PP,Mashru RC. Formulation and evaluation of taste masked oral reconstitutable suspension of primaquine phosphate. AAPS PharmSciTech. 2008; 9(3):1025-30. doi:10.1208/s12249-008-9137-6. DOI: https://doi.org/10.1208/s12249-008-9137-6
Giupponi G,Pagonabarraga I. Determination of the zeta potential for highly charged colloidal suspensions. Philos Trans A Math Phys Eng Sci 2011; 369(19):2546-54. doi:10.1098/rsta.2011.0024. DOI: https://doi.org/10.1098/rsta.2011.0024
Patel MS, Patel AD,Damor S. Design and development of dual release reconstitutable oral suspension of cefpodoxime proxetil for pediatric patient using risk-based quality by design approach. J Pharm Innov. 2022; 17(3):955-78. doi:10.1007/s12247-021-09577-y. DOI: https://doi.org/10.1007/s12247-021-09577-y
Rahman MS, Hasan MS, Nitai AS, et al. Recent developments of carboxymethyl cellulose. Polymers. 2021; 13(8):1345. doi: 10.3390/polym13081345 DOI: https://doi.org/10.3390/polym13081345
Almutairi M, D R L, Ghabbour H, Joe IH,Attia M. Spectroscopic identification, structural features, Hirshfeld surface analysis and molecular docking studies on stiripentol: An orphan antiepileptic drug. Journal of Molecular Structure. 2018; 1180(1):doi:10.1016/j.molstruc.2018.11.088. DOI: https://doi.org/10.1016/j.molstruc.2018.11.088
Pongjanyakul T,Puttipipatkhachorn S. Polymer-magnesium aluminum silicate composite dispersions for improved physical stability of acetaminophen suspensions. AAPS PharmSciTech. 2009; 10(2):346-54. doi:10.1208/s12249-009-9215-4. DOI: https://doi.org/10.1208/s12249-009-9215-4
Attebäck M, Hedin B,Mattsson S. Formulation optimization of extemporaneous oral liquids containing naloxone and propranolol for pediatric use. Sci Pharm. 2022; 90(1):15. doi:10.3390/scipharm90010015. DOI: https://doi.org/10.3390/scipharm90010015
Owusu FW, Asare CO, Enstie P, et al. Formulation and in vitro evaluation of oral capsules and suspension from the ethanolic extract of cola nitida seeds for the treatment of diarrhea. Biomed Res Int. 2021; 2021(1):1-7. doi:10.1155/2021/6630449. DOI: https://doi.org/10.1155/2021/6630449
Cheng Z, Kandekar U, Ma X, et al. Optimizing fluconazole-embedded transfersomal gel for enhanced antifungal activity and compatibility studies. Front Pharmacol. 2024; 15(1):1353791. DOI: https://doi.org/10.3389/fphar.2024.1353791
Júnior JAA,Baldo JB. The behavior of zeta potential of silica suspensions. New J GC. 2014; 4(02):1-9. doi:10.4236/njgc.2014.42004. DOI: https://doi.org/10.4236/njgc.2014.42004
Adeleke OA, Hayeshi RK,Davids H. Development and evaluation of a reconstitutable dry suspension containing isoniazid for flexible pediatric dosing. Pharmaceutics. 2020; 12(3):286. DOI: https://doi.org/10.3390/pharmaceutics12030286
Santoveña A, Suárez-González J, Martín-Rodríguez C,Fariña JB. Formulation design of oral pediatric Acetazolamide suspension: dose uniformity and physico-chemical stability study. Pharm Dev Technol. 2017; 22(2):191-97. doi:10.1080/10837450.2016.1175475. DOI: https://doi.org/10.1080/10837450.2016.1175475
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