Dissolution of propranolol tablets for biowaiver

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J. Pharm. Pharmacogn. Res., vol. 12, no. 5, pp. 814-821, Sep-Oct 2024. DOI: https://doi.org/10.56499/jppres23.1853_12.5.814 Original Article Dissolution kinetics of propranolol hydrochloride 40 mg tablets under biowaiver conditions [Cinética de disolución de tabletas de propanolol clorhidrato 40 mg en condiciones de bioexención] Lennin R. Rodriguez-Saavedra1,2*, Pedro M. Alva-Plasencia3, Yuri F. Curo-Vallejos1, Segundo F. Saavedra-Suárez1,     Luis A. … Continue reading Dissolution of propranolol tablets for biowaiver

J. Pharm. Pharmacogn. Res., vol. 12, no. 5, pp. 814-821, Sep-Oct 2024.

DOI: https://doi.org/10.56499/jppres23.1853_12.5.814

Original Article

Dissolution kinetics of propranolol hydrochloride 40 mg tablets under biowaiver conditions

[Cinética de disolución de tabletas de propanolol clorhidrato 40 mg en condiciones de bioexención]

Lennin R. Rodriguez-Saavedra1,2*, Pedro M. Alva-Plasencia3, Yuri F. Curo-Vallejos1, Segundo F. Saavedra-Suárez1,     Luis A. Chávez-Abanto1, Olga E. Caballero-Aquiño4, Miriam E. Gutiérrez-Ramos1, Junior F. Sánchez-Bautista5

1Departamento de Bioquímica, Facultad de Farmacia y Bioquímica, Universidad Nacional de Trujillo, 13006, Trujillo, Perú.

2Facultad de Ciencias Químicas y Farmacéuticas, Universidad de Chile, 1007, Santiago, Chile.

3Departamento de Farmacotecnia, Facultad de Farmacia y Bioquímica, Universidad Nacional de Trujillo, 13006, Trujillo, Perú.

4Departamento de Farmacología, Facultad de Farmacia y Bioquímica, Universidad Nacional de Trujillo, 13006, Trujillo, Perú.

5Facultad de Farmacia y Bioquímica, Universidad Nacional de Trujillo, 13006, Trujillo, Perú.

*E-mail: lrodriguezsa@unitru.edu.pe

Abstract

Context: Ensuring the quality of a generic drug is essential for its commercialization. Propranolol hydrochloride is a drug in great demand on the market as it is widely used as an antihypertensive, antianginal, antiarrhythmic, and for the treatment of migraine, requiring a complete evaluation to determine equivalence.

Aims: To evaluate the dissolution biopharmaceutical characteristic in multisource products marketed in the Peruvian market, taking Inderal® as a reference product.

Methods: In vitro conditions are simulated using the USP apparatus II at 50 rpm and 900 mL of the dissolution media pH 1.2, 4.5, and 6.8 at 37°C. The dependent mathematical models were characterized by the Akaike information criterion, and the similarity was evaluated using the independent parameters (MDT, DE, and the similarity factor f2).

Results: The average dissolution percentages demonstrate a difference between the multisource and the innovator in the three-dissolution media. The model that best characterizes the dissolution kinetics in all products is that of Hixson–Crowell. A significant difference was obtained in the MDT and DE between the innovative and multisource products and in the three-dissolution media. The similarity factor was not within the acceptable range for multisource products in the three-dissolution media.

Conclusions: The 40 mg propranolol hydrochloride tablets included in the study are not equivalent in vitro to the innovative product and, therefore, are not interchangeable.

Keywords: beta-blockers; bioequivalence; interchangeability; similarity factor.

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Resumen

Contexto: Garantizar la calidad de un medicamento genérico es esencial para su comercialización. El clorhidrato de propranolol es un fármaco de gran demanda en el mercado por ser ampliamente utilizado como antihipertensivo, antianginoso, antiarrítmico y para el tratamiento de la migraña, requiriendo una evaluación completa para determinar su equivalencia.

Objetivos: Evaluar la característica biofarmacéutica de disolución en productos multifuentes comercializados en el mercado peruano, tomando como producto de referencia el Inderal®.

Métodos: Se simulan condiciones in vitro utilizando el aparato USP II a 50 rpm y 900 mL del medio de disolución pH 1,2, 4,5 y 6,8 a 37°C. Los modelos matemáticos dependientes se caracterizaron con el criterio de información de Akaike, y la similitud se evaluó con los parámetros independientes (MDT, DE y el factor de similitud f2).

Resultados: Los porcentajes medios de disolución demuestran una diferencia entre la multifuente y el innovador en los tres medios de disolución. El modelo que mejor caracteriza la cinética de disolución en todos los productos es el de Hixson-Crowell. Se obtuvo una diferencia significativa en la MDT, DE entre el producto innovador y los productos multifuente y en los tres medios de disolución. El factor de similitud no estuvo dentro del rango aceptable para los productos multifuente en los medios de tres disoluciones.

Conclusiones: Los comprimidos de clorhidrato de propranolol 40 mg incluidos en el estudio no son equivalentes in vitro al producto innovador y, por tanto, no son intercambiables.

Palabras Clave: betabloqueantes; bioequivalencia; intercambiabilidad; factor de similitud.

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Citation Format: Rodriguez-Saavedra LR, Alva-Plasencia PM, Curo-Vallejos YF, Saavedra-Suárez SF, Chávez-Abanto LA, Caballero-Aquiño OE, Gutiérrez-Ramos ME, Sánchez-Bautista JF (2024) Dissolution kinetics of propranolol hydrochloride 40 mg tablets under biowaiver conditions. J Pharm Pharmacogn Res 12(5): 814–821. https://doi.org/10.56499/jppres23.1853_12.5.814
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