Tablet dosage formulations of oleyl phosphocholine
AssigneeOblita Therapeutics BVBA
InventorJohannes Jan Platteeuw
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Abstract
The present invention relates to tablet dosage formulations of oleyl phosphocholine for oral administration and the processes for their preparation. Specifically, the present invention provides a process for preparing an oleyl phosphocholine containing granulate, said process comprising a blending step, a hot melt agglomeration step and a milling step. The present invention further provides a process for preparing a tablet comprising the oleyl phosphocholine containing granulate, said process comprising the step of preparing an OlPC containing granulate according to the invention, a blending step, a compression step, and optionally a coating step. The invention further provides any intermediate and/or en product resulting from these steps and processes.
Claims14
A process for making an olelyl phosphocholine (OlPC) containing granulate, said process comprising a blending step, a hot melt extrusion step and a milling step,
- wherein the blending step comprises preparing a granulation mixture of olelyl phosphocholine and granulation excipients, wherein said granulation excipients comprise at least a spacer, an antioxidant and a disintegrant, and optionally a binder and/or a lubricant;
- wherein the hot melt extrusion step comprises preparing an extrudate by heating said granulation mixture at a temperature of at least 50° C. and below 90° C. and extrudating said heated granulation mixture;
- wherein the milling step comprises cooling said extrudate and milling said cooled extrudate to obtain a milled extrudate;
- wherein no solvent is added during the process for granulation,
- wherein the concentration of oleyl phosphocholine in the milled extrudate is between 10 and 50 weight percent,
- wherein, if a binder is added as a granulation excipient, the concentration of the binder in the milled extrudate is between 10 and 50 weight percent,
- wherein, if a lubricant is added as a granulation excipient, the concentration of the lubricant in the milled extrudate is between 1 and 20 weight percent,
- wherein the concentration of the antioxidant in the milled extrudate is between 0.05 and 5 weight percent,
- wherein the concentration of the disintegrant in the milled extrudate is between 1 and 20 weight percent,
- wherein the concentration of the spacer in the milled extrudate is between 10 and 50 weight percent, and
- wherein the concentrations are relative to the milled extrudate.
Dependencies are inferred from the claim text.