These capsules are designed to optimize the bioavailability of active ingredients, in order to obtain therapeutical advantages as compared to other traditional dosage forms.
|Low solubility (classes II and IV)||Increase of solubility / absorption||Enzalutamide, Olaparib, Nintedanib|
|Slow absorption||Increase of absorption speed||Etoricoxib, Tadalafil, Ibuprofen|
|Instability||Increase of stability||Cholecalciferol, Tretinoin|
|High potency / Low dosage||Dosage homogeneity||Lubiprostone, Calcitriol|
|Liquid or with low melting point||Simple solid formulation||Simethicone, Liquid and semi-solid vegetable extracts|
The microgranules form a multi-particulate system that allows to adjust in a very precise manner the dissolution profile of the formulations containing one or several active ingredients.
This technology consists in applying one or more layers of coating to spherical cores
containing the active ingredient. Depending on the desired dissolution profile, the coating
is done using soluble, insoluble or pH-dependent solubility polymers. Therefore, it is
possible to obtain extended, delayed, or colonic release profiles. It is also possible to
obtain pulsatile release and to combine two or more microgranule populations with different
dissolution profiles into one dosage form.
Microgranules can be filled into capsules, formulated as suspension, or compressed into tablets, without losing their properties. For better mouthfeel, it is possible to reduce the diameter of microgranules to less than 500 microns (micropellets).
One of the key advantages of microgranules is that they allow to combine in one pharmaceutical form different active components, each with its required dissolution profile.
pH-independent Extended Release
Tonibral XR (memantine HCI)
pH-dependent Extended Release
Dilantrend AP (carvedilol phosphate)
This technology enables the development of increased solubility formulations in which the
active ingredient is in amorphous (non-crystalline) state and forming a solid dispersion.
The solid dispersion is obtained by dissolving the active component together with an hydrophilic polymer in a suitable solvent and then spraying this solution onto inert cores. The technology allows the addition of crystallization inhibitors, surfactants and disintegrating agents to enhance the formulation performance.
Solid dispersion without surfactants
Panastat 200 (itraconazol)
Solid dispersion with surfactants
Reduprost Duo (dutasteride)
This technology makes it possible to enhance the stability of the active ingredients through the application of a soluble polymeric coating in cases such as:
This technology consists in applying a membrane directly over the crystals of active ingredients, thus obtaining taste masked particles of very small diameter (200-600 microns), which is ideal for suspensions as well as for dispersible or chewable tablets. The coating is designed to be insoluble in the mouth but to be rapidly soluble in the stomach, so as not to interfere with the bioavailability of the active ingredient.
Microcapsules for suspension
Macromax 2G (azithromycin)
Chewable Febratic Tablets (Ibuprofen)