New nanotech excipient makes for better delayed-release drugs say researchers
The claim is based on the results of a study in the Journal of Pharmaceutical Sciences this week that examined whether the porous magnesium carbonate excipient could be used to control the release of the active pharmaceutical ingredient (API) ibuprofen.
The Uppsala University team loaded Upsalite with two sizes of API particles and found that the active ingredient was released at two distinct periods.
“The initial release rate was controlled by the particle size; the dissolution rate of the loaded ibuprofen during this period was more than four times faster than that of the crystalline drug.
“An extended-release period of about 24 h followed the initial rapid-release period. The features of this extended-release period were dependent on the total drug concentration in the release medium.”
The researchers say the results indicate that, in addition to solubility enhancement, Upsalite can be used to formulate drug substances that need to be released over time in a controlled manner.
“Upsalite can be used not only to enhance the dissolution rate of poorly soluble drugs but also as a carrier in sustained-release applications by using larger particle sizes or even pellets of the material.”
Beyond solubility
When Upsalite was launched last year the focus was on its ability to make otherwise insoluble drugs soluble.
At the time Maria Stommer, head of Uppsala University’s nanotechnology department, told us Upsalite is dotted with 5nm pores that prevent insoluble API from forming crystals and coming out of solution.
The new application is in keeping with the aim of Disruptive Materials – a spin out company launched to promote the excipient to the drug industry – was is focusing on seeking new uses of the substance in drug formulation and development.
Company CEO Mattias Karls told us "Upsalite can be used for very fast release that is sought for in pain killers or similar drugs. It can also be used for slow release and reduce the need for taking pills several times per day.
"This very basic solution to control the release profile can be very useful also when developing generic drugs where the bioavailability should be the same for the new drug compared to the original drug."
He added that: "Upsalite is much less costly than competing excipients. The raw materials are magnesium oxide and carbon dioxide, and the production process is easy to scale. We can already today produce Upsalite on metric tonne scale per year now less than two years after the launch of the company."
Source: Journal of Pharmaceutical Sciences
Diffusion-Controlled Drug Release from the Mesoporous Magnesium Carbonate Upsalite
Peng Zhang et al
DOI: 10.1002/jps.24553
