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Claims for Patent: 5,192,741

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Claims for Patent: 5,192,741

Title: Sustained and controlled release of water insoluble polypeptides
Abstract:There is disclosed a pharaceutical composition for sustained and controlled release of drug over an extended period of time comprising a polylactide, a copolymer of lactic and glycolic acid, a mixture of such polymers and a water-insoluble peptide which, when placed in an aqueous physiologically-type environment releases the peptide in continuous manner for a period of at least one week, and with an initial release for the first twenty-four hours of not more than 30% of the total amount released. There is thus provided the control of the release pattern and in general a decrease of the initial burst effect.
Inventor(s): Orsolini; Piero (Martigny, CH), Mauvernay; Rolland-Yves (Lausanne, CH), Deghenghi; Romano (Lausanne, CH)
Assignee: Debiopharm S.A. (Lausanne, CH)
Application Number:07/247,060
Patent Claims: 1. A process for preparing a pharmaceutical composition designed for sustained and controlled release of a peptide, said process comprising selecting a water-insoluble peptide salt; dispersing the water-insoluble peptide salt into a solution of a polylactide polymer, a polyglycolide polymer, a copolymer of lactic and glycolic acids, or a mixture of said polymers and a solvent; removing the solvent of the solution to form a residue; and shaping the residue into solid particles of said pharmaceutical composition suitable for administration by parenteral injection or as a subcutaneous implant.

2. A process for preparing a pharmaceutical composition designed for sustained and controlled release of a peptide, said process comprising selecting a water insoluble peptide salt; dispersing a water-insoluble peptide salt into a solution of a polylactide polymer, a polyglycolide polymer, a copolymer of lactic and glycolic acids or a mixture of said polymers; adding a coacervation agent to the solution to form microcapsules of the peptide salt and polymer(s); pouring the resulting microcapsules into a pharmaceutically acceptable hardening liquid; and collecting the microcapsules for use as a pharmaceutical composition suitable for administration by parenteral injection or as a subcutaneous implant.

3. A process as claimed in claim 1 or 2 which further comprises selecting said water-insoluble peptide from pharmaceutically acceptable salts of LHRH and synthetically prepared analogues thereof.

4. A process as claimed in claim 3 wherein the pharmaceutically acceptable salt is selected from the group consisting of pamoate, tannate and stearate salts.

5. A process as claimed in claim 1 or 2 which further comprises selecting said water-insoluble peptide from pharmaceutically acceptable salts of oxytocin, vasopressin, ACTH, calcitonin, epidermal growth factor, prolactin, inhibin, interferon, somatstatin insulin, glucagon, atrial natriuretic factor, endorphin, a peptide renin inhibitor, growth hormone releasing factor, peptide T and synthetic analogues thereof.

6. A process as claimed in claim 1 or 2 wherein said water-insoluble peptide salt is dispersed within said solution by high shear mixing.

7. A process as claimed in claim 1 or 2 which further comprises sterlizing said composition by exposure to gamma radiation at between 2.5 and 2.8 Mrad.

8. The process of claim 1 wherein said peptide, polymer or copolymer is selected so as to provide a continuous release of said peptide when placed in a physiological environment.

9. The process of claim 1 further comprising selecting a water-insoluble peptide and polylactide polyglycolide polymer or copolymer molar ratio, and dosing said polymer or copolymer with said peptide salt so that said subcutaneous implant provides a continuous release of peptide when placed in a physiological environment.

10. The process of claim 2 further comprising selecting a water-insoluble peptide and polylactide polyglycolide polymer or copolymer molar ratio, and dosing said polymer or copolymer with said peptide salt so that said microspheres provide a continuous release of peptide when placed in a physiological environment.

11. A process for preparing a pharmaceutical composition for sustained and controlled release of a peptide, said process comprising:

forming a water-insoluble salt of LHRH or a synthetic analog thereof;

dispersing the water-insoluble peptide salt with mixing into a solution of a polylactide polymer, a polyglycolide polymer, a copolymer of lactic and glycolic acids or a mixture of said polymers and a solvent;

forming microparticles of the peptide salt and polymer(s) by evaporating the solvent;

drying the microparticles;

extruding the microparticles into rods;

grinding the rods into granular material;

sieving the granular materials; and

collecting a fraction and sterlizing the fraction for use as the pharmaceutical composition.

12. A process for preparing a pharmaceutical composition designed for sustained and controlled release of a peptide, said process comprising forming a water insoluble peptide salt from a water-soluble peptide; dispersing said water-insoluble peptide salt into a solution of a polylactide polymer, a polyglycolide polymer, a copolymer of lactic and glycolic acids or a mixture of said polymers; adding a coacervation agent to the solution to form microcapsules of the peptide salt and polymer(s); pouring the resulting microcapsules into a pharmaceutically acceptable hardening liquid; and collecting the microcapsules for use as a pharmaceutical composition suitable for administration by parenteral injection or as a subcutaneous implant.

13. The process of claim 12, further comprising selecting said peptide from the group consisting of pamoate, tannate and stearate salts of D-Trp.sup.6 -LHRH and selecting a mixture of D,L-lactide and glycolide as said polymer.

14. The process of claim 11 wherein the rods are ground cryogenically into the granular material.
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