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Claims for Patent: 5,639,480

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Claims for Patent: 5,639,480

Title: Sustained release formulations of water soluble peptides
Abstract:The invention discloses microparticles comprising a polypeptide, preferably somatostatin or an analog or derivative thereof, more preferably octreotide, in a polymeric matrix, preferably poly(lactide-co-glycolide)glucose. The invention also discloses sustained release formulations containing said microparticles and the use of said formulations in treating acromegaly and breast cancer.
Inventor(s): Bodmer; David (Klingnau, CH), Fong; Jones W. (Parsippany, NJ), Kissel; Thomas (Staufen, DE), Maulding; Hawkins V. (Mendham, NJ), Nagele; Oskar (Sissach, CH), Pearson; Jane E. (Ogendensburg, NJ)
Assignee: Sandoz Ltd. (Basel, CH)
Application Number:08/470,072
Patent Claims: 1. A microparticle having a diameter of between 1 and 250 microns comprising octreotide, in a free base, acid addition salt or complex form in a biodegradable, biocompatible polymeric matrix of a 40/60 to 60/40 polylactide-co-glycolide ester of a polyol, said polyol being selected from the group consisting of 1) a (C.sub.3-6) carbon chain containing alcohol having 3 to 6 hydroxyl groups, 2) a mono-saccharide and 3) a di-saccharide, and said esterified polyol having at least 3 polylactide-co-glycolide chains, wherein said octreotide is present in a therapeutically effective amount from at least 0.2 percent by weight relative to said polymeric matrix and said octreotide is distributed throughout said polymeric matrix.

2. A microparticle according to claim 1 wherein the octreotide is in a polymeric matrix of poly(D,L-lactide co-glycolide)glucose.

3. A sustained release formulation comprising a microparticle of claim 2.

4. A sustained release formulation according to claim 3 which when administered subcutaneously to a rat at a dosage of 10 mg of octreotide per kg of body weight exhibits an octreotide concentration in the blood plasma of at least 0.3 ng/ml and less than 20 ng/ml during a 30 day term.

5. A sustained release formulation according to claim 3 which when administered to a rabbit intramuscularly at a dosage of 5 mg of octreotide per kg of body weight exhibits an octreotide concentration of at least 0.3 ng/ml and at most 20 ng/ml during a 50 day term.

6. A sustained release formulation according to claim 3 which when administered to a rabbit intramuscularly at a dosage of 5 mg of octreotide per kg of body weight exhibits a retardation of at least 70% over a period of from 0 to 42 or 43 days.

7. A sustained release formulation according to claim 3 which when administered to a rat subcutaneously at a dosage of 10 mg of octreotide per kg of body weight exhibits an average plasma level of from 2.5 to 6.5 ng/ml over a period of from 0 to 42 days.

8. A sustained release formulation according to claim 3 which when administered to a rabbit intramuscularly at a dosage of 5 mg of octreotide per kg of body weight exhibits an average plasma level of from 3.5 to 6.5 ng/ml.

9. A microparticle according to claim 2 wherein the octreotide is in pamoate salt form.

10. A sustained release formulation comprising a microparticle of claim 9.

11. A microparticle according to claim 2 wherein the surface is substantially free of octreotide.

12. A sustained release formulation comprising a microparticle of claim 1.

13. A microparticle of claim 1 wherein said octreotide is an acetate salt.
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