Sustained and controlled release of water insoluble polypeptides
AssigneeDebiopharm S.A.
InventorsPiero Orsolini, Rolland-Yves Mauvernay, Romano Deghenghi
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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.
Claims14
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.
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.
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.
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.
Dependencies are inferred from the claim text.