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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.
Int J Pharm. 2014 Sep 10; 472(1-2):185-91.IJ

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.

Authors+Show Affiliations

Division for Nanotechnology and Functional Materials, Department for Engineering Sciences, P.O. Box 534, SE-751 21 Uppsala, Sweden. Electronic address: peng.zhang@angstrom.uu.se.Division for Nanotechnology and Functional Materials, Department for Engineering Sciences, P.O. Box 534, SE-751 21 Uppsala, Sweden. Electronic address: johan.forsgren@angstrom.uu.se.Division for Nanotechnology and Functional Materials, Department for Engineering Sciences, P.O. Box 534, SE-751 21 Uppsala, Sweden; Science for Life Laboratory, Uppsala University, P.O. Box 534, SE-751 21 Uppsala, Sweden. Electronic address: maria.stromme@angstrom.uu.se.

Pub Type(s)

Journal Article
Research Support, Non-U.S. Gov't

Language

eng

PubMed ID

24950364

Citation

Zhang, Peng, et al. "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, vol. 472, no. 1-2, 2014, pp. 185-91.
Zhang P, Forsgren J, Strømme M. Stabilisation of amorphous ibuprofen in Upsalite, a mesoporous magnesium carbonate, as an approach to increasing the aqueous solubility of poorly soluble drugs. Int J Pharm. 2014;472(1-2):185-91.
Zhang, P., Forsgren, J., & Strømme, M. (2014). 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, 472(1-2), 185-91. https://doi.org/10.1016/j.ijpharm.2014.06.025
Zhang P, Forsgren J, Strømme M. Stabilisation of Amorphous Ibuprofen in Upsalite, a Mesoporous Magnesium Carbonate, as an Approach to Increasing the Aqueous Solubility of Poorly Soluble Drugs. Int J Pharm. 2014 Sep 10;472(1-2):185-91. PubMed PMID: 24950364.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Stabilisation of amorphous ibuprofen in Upsalite, a mesoporous magnesium carbonate, as an approach to increasing the aqueous solubility of poorly soluble drugs. AU - Zhang,Peng, AU - Forsgren,Johan, AU - Strømme,Maria, Y1 - 2014/06/17/ PY - 2014/05/02/received PY - 2014/06/13/revised PY - 2014/06/14/accepted PY - 2014/6/21/entrez PY - 2014/6/21/pubmed PY - 2015/3/31/medline KW - Bioavailability KW - Ibuprofen KW - Magnesium carbonate KW - Mesoporous KW - Poorly soluble drug SP - 185 EP - 91 JF - International journal of pharmaceutics JO - Int J Pharm VL - 472 IS - 1-2 N2 - 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. SN - 1873-3476 UR - https://www.unboundmedicine.com/medline/citation/24950364/Stabilisation_of_amorphous_ibuprofen_in_Upsalite_a_mesoporous_magnesium_carbonate_as_an_approach_to_increasing_the_aqueous_solubility_of_poorly_soluble_drugs_ L2 - https://linkinghub.elsevier.com/retrieve/pii/S0378-5173(14)00445-1 DB - PRIME DP - Unbound Medicine ER -