Compositions of GnRH related compounds and processes of preparation

A process for preparing a GnRH antagonist selected from the group consisting of acyline, abarelix, cetrorelix, degarelix, ganirelix, and a pharmaceutically acceptable salt thereof, wherein the process comprises preparing the GnRH antagonist in the presence of a co-solvent system in a manner such that the gelation of the GnRH antagonist is reduced;

• and wherein the co-solvent system comprises water and at least one water-miscible solvent selected from the group consisting of methanol, ethanol, iso-propanol, tert-butanol, acetonitrile and methylene chloride.

A method for preparation of a solid oral dosage form of one or more GnRH antagonists selected from the group consisting of acyline, abarelix, cetrorelix, degarelix, ganirelix, and a pharmaceutically acceptable salt thereof, wherein the process comprises mixing the GnRH antagonists with one or more anti-gelling agents, wherein at least one anti-gelling agent is a medium chain fatty acid salt and has a carbon chain length of from about 8 to about 14 carbon atoms;

• wherein the final step of the preparation of the GnRH antagonist is conducted in the presence of a co-solvent system in a manner such that the gelation of the GnRH antagonist is reduced, wherein the co-solvent system comprises water and at least one water-miscible solvent selected from the group consisting of methanol, ethanol, iso-propanol, tert-butanol, acetonitrile and methylene chloride.

A method of treating a medical condition treatable by a GnRH antagonist comprising administering to a patient suffering from said condition a solid oral dosage form comprising a therapeutically effective amount of one or more GnRH antagonists selected from the group consisting of acyline, abarelix, cetrorelix, degarelix, ganirelix, and a pharmaceutically acceptable salt thereof, and a sufficient amount of at least one anti-gelling agent to reduce the gelation of the GnRH antagonist, wherein at least one anti-gelling agent is a medium chain fatty acid salt and has a carbon chain length of from about 8 to about 14 carbon atoms;

• wherein the solid oral dosage form is prepared by mixing the one or more GnRH antagonists with the at least one anti-gelling agent;
• wherein the final step of the preparation of the GnRH antagonist is conducted in the presence of a co-solvent system in a manner such that the gelation of the GnRH antagonist is reduced, wherein the co-solvent system comprises water and at least one water-miscible solvent selected from the group consisting of methanol, ethanol, iso-propanol, tert-butanol, acetonitrile and methylene chloride.