Microparticles comprising somatostatin analogues
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.
1. Microparticles comprising cyclo[{4-(NH 2 —C 2 H 4 —NH—CO—O—)Pro}-Phg-DTrp-Lys-Tyr(4-Bzl)-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. Microparticles according to claim 1 wherein the cyclo[{4-(NH 2 —C 2 H 4 —NH—CO—O—)Pro}-Phg-DTrp-Lys-Tyr(4-Bzl)-Phe] is in pamoate salt form.
3. Microparticles 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. Microparticles according to claim 1 wherein the ratio of linear to star polylactide-co-glycolide is 50:50.
5. Microparticles according to claim 1 wherein the cyclo[{4-(NH 2 —C 2 H 4 —NH—CO—O—)Pro}-Phg-DTrp-Lys-Tyr(4-Bzl)-Phe] is an amourphous powder having a particle size less than about 5 microns.
6. Microparticles according to claim 1 further comprising a surfactant, a porosity influencing agent and/or a basic salt.
7. A pharmaceutical composition comprising microparticles according to claim 1 and a water-based vehicle comprising a wetting agent.
8. A composition according to claim 7 wherein the wetting agent comprises a poloxamer and/or a polyoxyethylene-sorbitan-fatty acid ester.
9. A composition according to any one of claim 7 wherein the vehicle comprises a tonicity agent.
10. A composition according to any one of claim 7 wherein the vehicle comprises a viscosity increasing agent.
11. A kit comprising microparticles according to claim 1 and a water-based vehicle.