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Technology: Biorise®
- Technology Overview
- Technology Description
- Case Studies
Our Biorise technology enhances bioavailability by creating new physical entities (NPEs) with improved solubility profiles.
New Physical Entities (NPEs) are produced by breaking down the crystalline drug into nanocrystals and/or amorphous (noncrystalline) drug that is stabilized in a carrier system to maintain the drug in its activated form for the duration of its shelf life.
This approach creates a greater surface area to volume ratio that increases the intrinsic solubility and dissolution rate of poorly water-soluble drugs, thereby enhancing their rate and extent of absorption.
Advantages of Biorise
- Increases solubility of Class II compounds
- Provides a faster onset of action, equivalent therapy at lower doses, and/or oral dosing of poorly soluble drug candidates
- Short manufacturing cycle time and single processing step
Proprietary HEMA system equipment for Biorise
Learn more about the
Biorise technology.
New Physical Entities (NPEs) are produced by breaking down the crystalline drug into nanocrystals and/or amorphous (noncrystalline) drug that is stabilized in a carrier system to maintain the drug in its activated form for the duration of its shelf life.
This approach creates a greater surface area to volume ratio that increases the intrinsic solubility and dissolution rate of poorly water-soluble drugs, thereby enhancing their rate and extent of absorption.
The Biorise technology can be applied to Class II compounds with solubilities in the range of <10 to 500 μg/mL.
Aptalis Pharmaceutical Technologies has developed 2 distinct proprietary activation systems to create NPEs by converting drugs into their stabilized, thermodynamically activated state. These systems provide flexibility and allow the technology to be applied to a range of compounds with differing physicochemical characteristics.
The Biorise technology manufacturing process provides both time savings and cost efficiencies with its short cycle time, single processing step, batch consistency, and formulation stability.
Biorise Proprietary Activation Systems 
Benchtop mills for small batch testing
The Biorise technology portfolio includes a number of granted patents that provide international coverage. There are also over 20 pending patent applications relating to this technology as we continue to innovate and build around this platform. In addition to our background IP, we are able to apply for patent coverage for the new formulations specific to our partners’ compounds, thus providing the potential to extend patent life beyond that of the compound.
Learn more about our Biorise case studies.
Megestrol Acetate | Nimesulide
Megestrol Acetate
Drug |
Marketed analgesic |
Goals |
Improve bioavailablity of a marketed pain drug |
Challenge(s) |
Improve onset-of-action and increase overall bioavailability, in comparison to the marketed reference |
Solution |
|
Data |
Clinical studies show a clear increase in the rate at which therapeutic blood levels were achieved with the Biorise formulation and a marked increase in bioavailability. Comparison of plasma levels of drug for Biorise formulation (in red) versus the reference product (in green) in healthy human subjects (N=36). |
Result |
The Biorise formulation is clearly a superior pain-relief medication as it acts more rapidly. In addition, the formulation potentially allows a lower amount of drug to be used for an equivalent therapeutic effect, a valuable and differentiating feature. |
Product Achieved |
Proprietary |
Learn more about the Biorise case study Nimesulide.
Nimesulide
Drug |
Nimesulide is a nonsteroidal anti-inflammatory agent (NSAID) with a usual dose of 100 mg twice per day |
Goals |
Faster pain relief |
Challenge(s) |
Increase the rate of drug absorption in a marketed analgesic drug to achieve a rapid onset of action without increasing overall drug exposure |
Solution |
Utilize Biorise® technology to convert nimesulide into a stabilized, thermodynamically activated state. Several factors contributed to the choice of the HEMA (high-energy mechano-chemical activation) manufacturing process to create a powder that can be formulated into tablets. The drug to polymer ratio is 1:3 (w/w). |
Data |
A single-dose pharmacokinetic study compared one 100 mg tablet formulated using Biorise technology (activated nimesulide) to one 100 mg of reference product (nonactivated nimesulide) |
Result |
Biorise technology delivered a faster peak concentration (tmax = 2 hours intead of 3 hours) with a similar total drug exposure. |
Product Achieved |
Mesulid Fast® - marketed in Italy |
