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Technology: Biorise®

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  • 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.

Biorise

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

Biorise Mills

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.

Biorise

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.

Proprietary Activation Systems Biorise Proprietary Activation Systems Biorise Mills 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

Biorise®

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.

Click to Enlarge
Proprietary Client Program

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)

Click to Enlarge
Mesulid fast

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