Pharmaceutical Compositions having a Selected Release Duration
AssigneeForesee Pharmaceuticals Co., Ltd.
InventorsYuhua LI, Andrew J. GUARINO
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Abstract
The present invention provides for a stabilized biodegradable polymeric composition useful as a controlled release delivery system for peptide agents. The compositions of the present invention comprise a) a strong acid salt and a weak acid of a LHRH agonist or antagonist; b) a biodegradable polymer of poly(lactide-co-glycolide), wherein the ratio of lactide:glycolide of the copolymer is from 50:50 to about 100:0; and c) N-methyl-2-pyrrolidone (NMP), wherein the composition does not contain excess strong acid in addition to the strong acid used to form the salt of the LHRH agonist or antagonist. The composition, when injected, can provide a controlled release of leuprolide for a period of up to 6 months.
Claims12
A pharmaceutical composition having a selected release duration comprising:
- a. a mixture of a strong acid salt and a weak acid salt of leuprolide or triptorelin, wherein the molar ratio of (strong acid salt anion+weak acid salt anion) to leuprolide or triptorelin is ≤2:1 and the molar ratio of strong acid salt anion to leuprolide or triptorelin is from 1:1 to less than 2:1;
- b. a biodegradable polymer selected from the group consisting of a homopolymer polylactic acid (PLA) and a copolymer poly (lactic acid-co-glycolic acid) (PLGA), wherein the ratio of lactic acid:glycolic acid of the copolymer is from 50:50% to less than 100% and wherein the biodegradable polymer has an average molecular weight of 5,000 to 50,000 daltons and has a polydispersity less than or equal to 2.5;
- and
- c. a pharmaceutically acceptable organic solvent is selected from the group of N-methyl-2-pyrrolidone, dimethyl sulfoxide, and any combinations thereof,
- wherein the strong acid is methanesulfonic acid, and the weak acid is acetic acid or formic acid.
Dependencies are inferred from the claim text.