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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
Uppsala University, Disciplinary Domain of Science and Technology, Technology, Department of Engineering Sciences, Nanotechnology and Functional Materials. (Nanotechnology and Functional Materials)
Uppsala University, Disciplinary Domain of Science and Technology, Technology, Department of Engineering Sciences, Nanotechnology and Functional Materials.
Uppsala University, Disciplinary Domain of Science and Technology, Technology, Department of Engineering Sciences, Nanotechnology and Functional Materials. (Nanoteknologi och funktionella material)ORCID iD: 0000-0002-5496-9664
2014 (English)In: International Journal of Pharmaceutics, ISSN 0378-5173, E-ISSN 1873-3476, Vol. 472, no 1-2, 185-191 p.Article in journal (Refereed) Published
Abstract [en]

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.

Place, publisher, year, edition, pages
2014. Vol. 472, no 1-2, 185-191 p.
National Category
Nano Technology
Research subject
Engineering Science with specialization in Nanotechnology and Functional Materials
Identifiers
URN: urn:nbn:se:uu:diva-228395DOI: 10.1016/j.ijpharm.2014.06.025ISI: 000340328400022PubMedID: 24950364OAI: oai:DiVA.org:uu-228395DiVA: diva2:733848
Available from: 2014-07-11 Created: 2014-07-11 Last updated: 2017-12-05Bibliographically approved
In thesis
1. Mesoporous magnesium carbonate as a drug delivery vehicle for stabilising amorphous drugs and regulating their release rate
Open this publication in new window or tab >>Mesoporous magnesium carbonate as a drug delivery vehicle for stabilising amorphous drugs and regulating their release rate
2016 (English)Doctoral thesis, comprehensive summary (Other academic)
Abstract [en]

In today’s drug discovery, the number of candidate drugs based on new molecular entities with poor aqueous solubility is increasing. Since poor aqueous solubility of an active pharmaceutical ingredients (APIs) is associated with low bioavailability and thus limite their therapeutic effect, this is often a great challenge in the development of new drugs when oral administration is the preferred route of administration. A number of different strategies have been developed to circumvent this problem where salt formulations of an API is the most widely employed method. However, new strategies are needed since there is no one solution that solves this issue for all substances. In recent time, the concept of stabilizing poorly soluble APIs in their amorphous form has gained a lot of attention since amorphous compounds exhibit a higher apparent solubility compared to their crystalline counterparts. Amorphous substances are prone to crystallize if left in a non-constricted environment and thus need to be stabilized if the amorphous state is to be conserved until administration. Inorganic mesoporous materials have been proposed as an interesting type of excipients that can conserve the amorphous state of APIs.

In this work, the focus was to investigate the possibilities of using a mesoporous type of magnesium carbonate to stabilize the amorphous state of different APIs. Due to the nanometer sized pores in the material, complete conservation of amorphous APIs was obtained. This resulted in both an increase in in vitro release rate and a higher solubility of the substances which may translate to both a faster onset of action and an improved therapeutic effect of the APIs in a clinical situation. The long term stability of formulations was also investigated showing promising results.

The results presented in this work show that mesoporous magnesium carbonate represents an interesting type of excipient for oral formulations of APIs with poor aqueous solubility.

Place, publisher, year, edition, pages
Uppsala: Acta Universitatis Upsaliensis, 2016. 68 p.
Series
Digital Comprehensive Summaries of Uppsala Dissertations from the Faculty of Science and Technology, ISSN 1651-6214 ; 1452
Keyword
mesoporous, magnesium carbonate, drug delivery, solubility enhancement, bioavailability, pharmacokinetics, diffusion release, controlled release
National Category
Engineering and Technology
Research subject
Engineering Science with specialization in Nanotechnology and Functional Materials
Identifiers
urn:nbn:se:uu:diva-303832 (URN)978-91-554-9752-1 (ISBN)
Public defence
2016-11-11, Ång/2001, Ångströmlaboratoriet, Lägerhyddsvägen 1, Uppsala, 09:30 (English)
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Note

Felaktigt ISBN 978-91-554-9702-6 i tryck version.

Available from: 2016-10-20 Created: 2016-09-25 Last updated: 2016-11-18

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Zhang, PengForsgren, JohanStrömme, Maria

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