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

P5655

Sigma-Aldrich

Potassium phosphate monobasic, powder, suitable for cell culture, suitable for insect cell culture, suitable for plant cell culture, ≥99.0%

H1758

Sigma-Aldrich

Hydrochloric acid, 36.5-38.0%, BioReagent, for molecular biology

30721

Sigma-Aldrich

Hydrochloric acid, puriss. p.a., ACS reagent, reag. ISO, reag. Ph. Eur., fuming, ≥37%, APHA: ≤10

320331

Sigma-Aldrich

Hydrochloric acid, ACS reagent, 37%

339253

Sigma-Aldrich

Hydrochloric acid, 37 wt. % in H₂O, 99.999% trace metals basis

258148

Sigma-Aldrich

Hydrochloric acid, ACS reagent, 37%

30435

Sigma-Aldrich

Sodium phosphate dibasic dihydrate, puriss. p.a., reag. Ph. Eur., 98.5-101.0% (calc. to the dried substance)

04243

Sigma-Aldrich

Potassium phosphate monobasic, meets analytical specification of Ph. Eur., NF, E340, anhydrous, 98-100.5% (calc. to the dried substance)

04272

Sigma-Aldrich

Sodium phosphate dibasic dihydrate, meets analytical specification of Ph. Eur., BP, 98.5-101% (calc. to the dried substance)

P0662

Sigma-Aldrich

Potassium phosphate monobasic, ACS reagent, ≥99.0%

07102

Sigma-Aldrich

Hydrochloric acid, meets analytical specification of Ph. Eur., BP, NF, fuming, 36.5-38%

60220

Sigma-Aldrich

Potassium phosphate monobasic, buffer substance, anhydrous, puriss. p.a., ACS reagent, reag. ISO, reag. Ph. Eur., 99.5-100.5%

705551

Sigma-Aldrich

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

13-1790

Sigma-Aldrich

Hydrogen chloride – ethanol solution, 0.1 M in ethanol

13-1683

Sigma-Aldrich

Hydrochloric acid solution, 12 M

13-1760

Sigma-Aldrich

Hydrochloric acid solution, 0.01 M

13-1700

Sigma-Aldrich

Hydrochloric acid solution, 1 M

13-1710

Sigma-Aldrich

Hydrochloric acid solution, 0.5 M

13-1686

Sigma-Aldrich

Hydrochloric acid solution, 6 M

13-1740

Sigma-Aldrich

Hydrochloric acid solution, 0.05 M

13-1690

Sigma-Aldrich

Hydrochloric acid solution, 2 M

13-1650

Sigma-Aldrich

Hydrochloric acid, SAJ first grade, 35.0-37.0%

13-1750

Sigma-Aldrich

Hydrochloric acid solution, 0.02 M

W530574

Sigma-Aldrich

Hydrochloric acid solution, 32 wt. % in H₂O, FCC

455180

Sigma-Aldrich

Hydrogen chloride solution, 2.0 M in diethyl ether

345547

Sigma-Aldrich

Hydrogen chloride solution, 4.0 M in dioxane

294837

Sigma-Aldrich

Hydrogen chloride solution, 1.0 M in diethyl ether

304174

Sigma-Aldrich

Hydrogen chloride solution, 1.0 M in acetic acid