Details for Patent: 8,188,037

Title:	Microparticles comprising somatostatin analogues
Abstract:	Disclosed are microparticles comprising a somatostatin analogue embedded in a biocompatible pharmacologically acceptable polymer matrix for a long acting release and pharmaceutical compositions comprising such microparticles.
Inventor(s):	Ahlheim; Markus (Staufen, DE), Ausborn; Michael (Lorrach, DE), Lambert; Olivier (Spechbach-le-Haut, FR), Riemenschnitter; Marc (Freiburg, DE)
Assignee:	Novartis AG (Basel, CH)
Filing Date:	Jun 08, 2010
Application Number:	12/796,132
Claims:	1. A method of treating cushing's disease in a subject in need thereof, which comprises administering microparticles wherein said microparticles comprising cyclo[{4-(NH.sub.2--C.sub.2H.sub.4--NH--CO--O--)Pro}-Phg-DTrp-Lys-Tyr(4-B- zl)-Phe] in free form, salt form or protected form embedded in a polymer matrix wherein the polymer matrix comprises a linear and a star polylactide-co-glycolide. 2. A method according to claim 1 wherein the cyclo[{4-(NH.sub.2--C.sub.2H.sub.4--NH--CO--O--)Pro}-Phg-DTrp-Lys-Tyr(4-B- zl)-Phe] is in pamoate salt form. 3. A method according to claim 1 wherein the polymer matrix comprises a linear polylactide-co-glycolide polymer and a star polylactide-co-glycolide polymer having a weight average molecular weight of about 50,000 Da. 4. A method according to claim 1 wherein the ratio of linear to star polylactide-co-glycolide is 50:50. 5. A method according to claim 1 wherein the cyclo[{4-(NH.sub.2--C.sub.2H.sub.4--NH--CO--O--)Pro}-Phg-DTrp-Lys-Tyr(4-B- zl)-Phe] is an amorphous powder having a particle size less than about 5 microns. 6. A method according to claim 1 where said microparticles further comprising a surfactant, a porosity influencing agent and/or a basic salt. 7. A method of treating cushing's disease in a subject in need thereof, which comprises administering a composition comprising microparticles wherein said microparticles comprising cyclo[{4-(NH.sub.2--C.sub.2H.sub.4--NH--CO--O--)Pro}-Phg-DTrp-Lys-Tyr(4-B- zl)-Phe] in free form, salt form or protected form embedded in a polymer matrix wherein the polymer matrix comprises a linear and a star polylactide-co-glycolide and a water-based vehicle comprising a wetting agent. 8. A method according to claim 7 wherein the wetting agent comprises a poloxamer and/or a polyoxyethylene-sorbitan-fatty acid ester. 9. A method according to claim 7 wherein the vehicle comprises a tonicity agent. 10. A method according to claim 7 wherein the vehicle comprises a viscosity increasing agent.