Oryza sativa hydroxypropylated crosslinked starch as disintegrant in tablet

J. Pharm. Pharmacogn. Res., vol. 10, no. 4, pp. 701-716, July-August 2022.

Original Article

Application of hydroxypropylated crosslinked starch from the grains of Oryza sativa L. as potential disintegrant in compressed solid dosage form

[Aplicación de almidón reticulado hidroxipropilado de los granos de Oryza sativa L. como desintegrante potencial en forma de dosificación sólida comprimida]

Elizabeth A. Pagtalunan1,2,3*, Judson Lowie T. Ramos4, Gerard Q. De Guzman5

1Graduate School, Adamson University, Manila, Philippines.

2Belo Medical Group, San Juan, Manila, Philippines.

3School of Pharmacy, Saint Jude College, Manila, Philippines.

4School of Chemical, Biological and Materials Engineering, and Sciences, Mapua University, Manila, Philippines.

5Department of Pharmacology and Toxicology, College of Medicine, University of the Philippines, Manila, Philippines.

*E-mail: elizabeth.pagtalunan@adamson.edu.ph

Abstract

Context: The modification of starch from the grains of NSICRc222 rice variety may provide a new material with enhanced disintegrating functionality in compressed solid dosage forms.

Aims: To synthesize hydroxypropylated crosslinked rice starch that may possess characteristics of a good disintegrant.

Methods: Starch was isolated by the wet milling method. The crosslinking was performed using trisodium trimetaphosphate as crosslinking agent, and successively hydroxypropylated by using phosphorous oxychloride. The evidences of chemical modifications were determined by FTIR, TGA, and DSC. The application of modified rice starch as a disintegrant was evaluated by determining the dissolution profile, and was compared to the performance of commercially available disintegrants. The compatibility of modified rice starch was employed using FTIR, and the stability of the formulation was subjected to an accelerated stability study.

Results: The changes in infrared spectra and thermogram confirmed successful chemical modification of rice starch. Allopurinol and modified starch mixture staged from 0 to 3 months showed no significant changes in the infrared spectra, which suggest compatibility of HCR with allopurinol. The dissolution rate of allopurinol tablets at pH 1.2, pH 4.5, and pH 6.8 with various superdisintegrants were comparable to the dissolution rate that utilized hydroxypropylated crosslinked rice starch as disintegrant. The accelerated stability study showed no significant changes from 0th to 3rd month, and no degradation products were detected in the HPLC analysis.

Conclusions: The chemical modification of rice starch through crosslinking and hydroxypropylation yielded a novel material comparable to the commercially available superdisintegrants.

Keywords: crosslinking; disintegrant; hydroxypropylation; immediate release; NSIC Rc222-Tubigan 18; rice starch.

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Resumen

Contexto: La modificación del almidón de los granos de la variedad de arroz NSIC RC 222 puede proporcionar un nuevo material con una funcionalidad de desintegración mejorada en formas de dosificación sólidas comprimidas.

Objetivos: Sintetizar almidón de arroz reticulado hidroxipropilado que pueda poseer características de un buen desintegrante.

Métodos: El almidón se aisló por el método de molienda húmeda. El entrecruzamiento se realizó con trimetafosfato trisódico como agente de entrecruzamiento, y sucesivamente se hidroxipropiló utilizando oxicloruro de fósforo. Las evidencias de modificaciones químicas fueron determinadas por FTIR, TGA y DSC. La aplicación de almidón de arroz modificado como desintegrante se evaluó determinando el perfil de disolución y se comparó con el desempeño de los desintegrantes disponibles comercialmente. La compatibilidad del almidón de arroz modificado se empleó mediante FTIR y la estabilidad de la formulación se sometió a un estudio de estabilidad acelerado.

Resultados: La caracterización por FTIR reveló una modificación exitosa del almidón de arroz según los cambios de espectros. Los cambios en los termogramas confirmaron la modificación exitosa del almidón de arroz. La mezcla de alopurinol y almidón modificado en etapas de 0 a 3 meses no mostró cambios significativos en los espectros infrarrojos, lo que sugiere compatibilidad de HCR con alopurinol. La velocidad de disolución de las tabletas de alopurinol a pH 1,2, pH 4,5 y pH 6,8 con varios superdesintegrantes fue comparable a la velocidad de disolución de HCR. El estudio de estabilidad acelerada no mostró cambios significativos del mes O al 3, y no se detectaron productos de degradación en el análisis HPLC.

Conclusiones: La modificación química del almidón de arroz a través de la reticulación y el hidroxipropilado produjo un material novedoso comparable a los superdesintegrantes disponibles comercialmente.

Palabras Clave: almidón de arroz; desintegrante; hidroxipropilado; liberación inmediata; NSIC Rc222-Tubigan 18; reticulado.

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Citation Format: Elizabeth AP, Judson Lowie TR, Gerard QDG (2022) Application of hydroxypropylated crosslinked starch from the grains of Oryza sativa L. as potential disintegrant in compressed solid dosage form. J Pharm Pharmacogn Res 10(4): 701–716.
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