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  • Stabilisation of amorphous ibuprofen in Upsalite, a mesoporous magnesium carbonate, as an approach to increasing the aqueous solubility of poorly soluble drugs.

Stabilisation of amorphous ibuprofen in Upsalite, a mesoporous magnesium carbonate, as an approach to increasing the aqueous solubility of poorly soluble drugs.

International journal of pharmaceutics (2014-06-21)
Peng Zhang, Johan Forsgren, Maria Strømme
ABSTRACT

One attractive approach to increase the aqueous solubility and thus the bioavailability of poorly soluble drugs is to formulate them in their amorphous state since amorphous compounds generally exhibit higher apparent solubilities than their crystalline counterparts. In the current work, mesoporous magnesium carbonate was used to stabilise the amorphous state of the model substance ibuprofen. Crystallisation of the drug was completely supressed in the formulation, resulting in both a higher apparent solubility and a three times faster dissolution rate of the drug where the drug release was shown to be diffusion controlled. It was also shown that the formulation is stable for at least three months when stored at 75% relative humidity. The simple synthesis together with a high loading capacity and narrow pore size distribution of the mesoporous magnesium carbonate is foreseen to offer great advantages in formulations of poorly soluble drugs.

MATERIALS
Product Number
Brand
Product Description

Sigma-Aldrich
Magnesium oxide, tested according to Ph. Eur., heavy
Supelco
Ethanol solution, certified reference material, 2000 μg/mL in methanol
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Ethanol standards 10% (v/v), 10 % (v/v) in H2O, analytical standard
Ibuprofen for peak identification, European Pharmacopoeia (EP) Reference Standard
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Methanol, suitable for HPLC, gradient grade, ≥99.9%
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Methanol, ACS reagent, ≥99.8%
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Ethyl alcohol, Pure 190 proof, for molecular biology
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Ibuprofen, Pharmaceutical Secondary Standard; Certified Reference Material
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Ibuprofen, United States Pharmacopeia (USP) Reference Standard
Ibuprofen, European Pharmacopoeia (EP) Reference Standard
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Dehydrated Alcohol, United States Pharmacopeia (USP) Reference Standard
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Magnesium oxide, puriss., meets analytical specification of Ph. Eur., BP, USP, FCC, E 530, light, 98.0-100.5% (calc. for dried substance)
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Magnesium oxide, -10-+50 mesh, 98%
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Methanol, ACS reagent, ≥99.8%
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