PREDICTION OF SULFAMETHOXAZOLE AND TRIMETHOPRIM PLASMA LEVELS FROM TABLETS AND DISSOLUTION MEDIA OF PHYSIOLOGICAL RELEVANCE

JOSE MANUEL RIOS-RODRIGUEZ; FELIPE DINO REYES-RAMIREZ; JUAN CARLOS RUIZ-SEGURA; JOSE RAUL MEDINA-LOPEZ

doi:10.22159/ijap.2024v16i3.50409

Authors

JOSE MANUEL RIOS-RODRIGUEZ Departamento Sistemas Biologicos, Universidad Autonoma Metropolitana Xochimilco, Mexico City, Mexico https://orcid.org/0009-0000-3993-2954
FELIPE DINO REYES-RAMIREZ Departamento Sistemas Biologicos, Universidad Autonoma Metropolitana Xochimilco, Mexico City, Mexico https://orcid.org/0009-0009-6876-9223
JUAN CARLOS RUIZ-SEGURA Departamento Sistemas Biologicos, Universidad Autonoma Metropolitana Xochimilco, Mexico City, Mexico
JOSE RAUL MEDINA-LOPEZ Departamento Sistemas Biologicos, Universidad Autonoma Metropolitana Xochimilco, Mexico City, Mexico https://orcid.org/0000-0002-4159-8403

DOI:

https://doi.org/10.22159/ijap.2024v16i3.50409

Keywords:

Convolution, Fixed-dose formulations, Sulfamethoxazole, Trimethoprim, Prediction error

Abstract

Objective: To estimate plasma concentrations-time profiles of Sulfamethoxazole (SMZ) and Trimethoprim (TMP) from fixed-dose combination formulations through in vitro data of dissolution media of physiological relevance and a convolution model.

Methods: Dissolution profiles of SMZ/TMP tablets (400/80 mg) were obtained with USP paddle apparatus at 100 rpm and 900 ml of 0.1 N HCl, pH 4.5 acetate buffer, and pH 6.8 phosphate buffer. The reference drug product and two generic formulations were tested. Drugs were quantified by a derivative method. Dissolution profiles were compared with model-dependent and independent methods. SMZ/TMP plasma levels were simulated with dissolution data and published in vivo information. Percent of prediction error (PE) for peak plasma concentration (C_max) and area under the curve from zero time to infinity (AUC_0-inf) at each condition were calculated.

Results: In all used conditions, similar dissolution profiles were found excepting for TMP at pH 1.2 (f₂<50). The in vitro release performance for reference and generic formulations was explained by the Weibull function only for SMZ at pH 6.8 and TMP at pH 4.5. Values of PE>19% for both generic formulations were found with TMP at pH 1.2.

Conclusion: Significant differences in TMP dissolution profiles of generic formulations at pH 1.2 reflect the subsequent differences found in predicted C_max and AUC_0-inf.

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