A novel approach for predicting the dissolution profiles of pharmaceutical tablets.

A novel approach for predicting the dissolution profiles of pharmaceutical tablets.

European journal of pharmaceutics and biopharmaceutics : official journal of Arbeitsgemeinschaft fur Pharmazeutische Verfahrenstechnik e.V (2015-07-15)

Raphael Paus, Elena Hart, Yuanhui Ji

PMID26170163

ABSTRACT

In this paper, the intrinsic dissolution profiles of naproxen (NAP) at pH values of 1.5 and 3.0 and of trimethoprim (TMP) at pH values of 1.5, 3.0, 5.0, 6.5 and 7.2 were measured. Meanwhile, the dissolution profiles of NAP and TMP from cylindrical tablets were measured at different temperatures (298.15K, 305.15K, 301.15K and 310.15K) and stirring speeds (50rpm, 100rpm and 150rpm) as well as at different pH values (1.5, 3.0, 5.0, 6.5 and 7.2). Additionally the pH-dependent solubilities of both APIs were measured and modeled. The chemical-potential-gradient model combined with the perturbed-chain statistical associating fluid theory (PC-SAFT) was applied to predict the dissolution profiles of the cylindrical tablets of NAP and TMP under different conditions based on the analysis of their intrinsic dissolution profiles as well as on the determination of the surface-area reduction of the API tablets during dissolution. It was shown that the predicted dissolution profiles of the tablets under different conditions were in a good accordance with the experimental findings.

MATERIALS

Product Number

Brand

Product Description

07104

Sigma-Aldrich

Hydrochloric acid, puriss., 24.5-26.0%

304174

Sigma-Aldrich

Hydrogen chloride solution, 1.0 M in acetic acid

294837

Sigma-Aldrich

Hydrogen chloride solution, 1.0 M in diethyl ether

455180

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345547

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P9791

Sigma-Aldrich

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P5379

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P5655

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705551

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Hydrogen chloride solution, 3 M in cyclopentyl methyl ether (CPME)

N8280

Sigma-Aldrich

Naproxen, meets USP testing specifications

60218

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284785

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229806

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Sigma-Aldrich

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04243

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295426

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84429

Sigma-Aldrich

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2104

Supelco

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07102

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30435

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258148

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30721

Sigma-Aldrich

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339253

Sigma-Aldrich

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