CapsMorph™
Capsulution amorphous technology for oral delivery of poorly solubles
Physical Background
- The saturation solubility of amorphous drugs is higher than of crystalline material.
- Nanosized particles possess a higher saturation solubility than µm-sized drug crystals.
Ideal oral Formulations
Preparations with the drug being in a solid solution or being amorphous with a size dimension in the nm range (amorphous drug nanoparticles).
The Problem
Because of thermodynamics, for both there is a tendency to re-crystallize. The time point of crystallization is difficult to predict, because the initiation is primarily a random event and difficult to control. Resulting crystals or crystalline nanoparticles (nanocrystals) have a lower bioavailability.
The Solution - CapsMorph™
It is known, that with decreasing size of a liquid, crystallization is retarded and in very small size dimension does not occur anymore (e.g. melted o/w emulsions with droplets < 50 nm form a supercooled amorphous melt upon cooling, e.g. coenzyme Q10). The CapsMorph technology limits the space for the drug to very tiny dimensions, e.g. 50-60 Angstrom, by evaporating drug solutions in small pores, e.g. in Neusilin US2, thus not allowing formation of crystals.
In vitro Dissolution & Oral Bioavailability Enhancement
With CapsMorph™...
- Fast dissolution
- Neusilin carriers are easy to compress to tablets
- About 4 times higher BA
- In contrast to fast dissolving nanocrystals avoidance of plasma peak and prolonged release
Contact
Michaela Grabo, Senior Research Scientist New Technologies
Capsulution Pharma AG, Volmerstr. 7b, 12489 Berlin, Germany
Mail: m.grabo@capsulution.com
Tel.: +49 (0)30-670 69 19 0
Fax: +49 (0)30-670 69 19 101
www.capsulution.com
