Microparticles comprising GNRH made by PGSS
AssigneeFerring B.V.
InventorsGregoire Charles Joseph Schwach, Lars Schiefelbein, Andrew Naylor, Mark Andrew Whitaker, Nicholas John Arrowsmith
Life of this patent
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Abstract
A pharmaceutical formulation comprising a solid matrix of one or more biodegradable polymers, the solid matrix including a pharmaceutically active substance or a pharmaceutically acceptable salt thereof distributed homogeneously or substantially homogeneously within the matrix; wherein the pharmaceutically active substance is, for example, a gonadotropin releasing hormone (GnRH), a GnRH agonist or a GnRH antagonist.
Claims27
A pharmaceutical formulation comprising a solid matrix of one or more biodegradable polymers and a pharmaceutically active substance or a pharmaceutically acceptable salt thereof,
- wherein the active substance is distributed uniformly within the matrix on a micrometer scale and the active substance is chosen from gonadotropin releasing hormone (GnRH), a GnRH agonist, and a GnRH antagonist,
- wherein the formulation is made by a process comprising the steps of:
- (a) providing in a vessel the biodegradable polymer in solid form, the pharmaceutically active substance or salt thereof in solid form, and optionally an excipient;
- (b) adding a solvent to the vessel which includes the polymer in solid form and the pharmaceutically active substance in solid form;
- (c) adding a fluid which is capable of existing in a supercritical state to the vessel;
- (d) increasing the temperature and pressure in the vessel to convert the fluid to the supercritical state, optionally mixing the polymer, pharmaceutically active substance, and excipient (if present) prior to, during, and/or after conversion of the fluid to the supercritical state;
- (e) decreasing one or both of the temperature and pressure in the vessel to convert the fluid to a sub-critical state;
- and then increasing one or both of the temperature and pressure in the vessel to return the fluid to the supercritical state;
- and
- (f) recovering the solid matrix.
A method of treating prostate cancer or benign prostate hyperplasia comprising:
- administering to a patient in need thereof a pharmaceutical formulation comprising a solid matrix of one or more biodegradable polymers and a pharmaceutically active substance or a pharmaceutically acceptable salt thereof,
- wherein the active substance is distributed uniformly within the matrix on a micrometer scale and the active substance is chosen from gonadotropin releasing hormone (GnRH), a GnRH agonist, and a GnRH antagonist
- wherein the pharmaceutical formulation is made by a process comprising the steps of:
- (a) providing in a vessel the biodegradable polymer in solid form, the degarelix or salt thereof in solid form, and optionally an excipient;
- (b) adding a solvent to the vessel which includes the polymer in solid form and the degarelix in solid form;
- (c) adding a fluid which is capable of existing in the supercritical state to the vessel;
- (d) increasing the temperature and pressure in the vessel to convert the fluid to the supercritical state, optionally mixing the polymer, degarelix and excipient (if present) prior to, during, and/or after conversion of the fluid to the supercritical state;
- (e) decreasing one or both of the temperature and pressure in the vessel to convert the fluid to a sub-critical state;
- and then increasing one or both of the temperature and pressure in the vessel to return the fluid to the supercritical state;
- and
- (f) recovering the solid matrix.
A method of making a pharmaceutical formulation comprising an active substance or pharmaceutically acceptable salt thereof is distributed uniformly within a matrix on a micrometer scale, the method comprising:
- (a) providing in a vessel a biodegradable polymer in solid form, the active substance or salt thereof in solid form, and optionally an excipient;
- (b) adding a solvent to the vessel which includes the polymer in solid form and the active substance or salt thereof in solid form;
- (c) adding a fluid which is capable of existing in the supercritical state to the vessel;
- (d) increasing the temperature and pressure in the vessel to convert the fluid to the supercritical state, optionally mixing the polymer, the active substance or salt thereof and excipient (if present) prior to, during, and/or after conversion of the fluid to the supercritical state;
- (e) decreasing one or both of the temperature and pressure in the vessel to convert the fluid to a sub-critical state;
- and then increasing one or both of the temperature and pressure in the vessel to return the fluid to the supercritical state;
- and
- (f) recovering the solid matrix.
Dependencies are inferred from the claim text.