# US 3,976,071 A · Methods of improving control of release rates and products useful in same > Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt - Number: US 3,976,071 A - Document ID: US3976071A - Status: Granted - Kind: A - Application number: 05/431,493 - Filed: 1974-01-07 - Granted: 1976-08-24 - Earliest claimed: 1974-01-07 - Assignees: Dynatech Corporation - Inventors: Safik E. Sadek - Web page: https://patentgrep.com/patent/US3976071A ## CPC - A61K 9/204: {Polyesters, e.g. poly(lactide-co-glycolide)} - A61K: PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES (devices or methods specially adapted for bringing pharmaceutical products into particular physical or administering forms A61J3/00; chemical aspects of, or use of materials for deodorisation of air, for disinfection or sterilisation, or for bandages, dressings, absorbent pads or surgical articles A61L; soap compositions C11D) ## Abstract Improved processes for obtaining the sustained release of pharmaceuticals from polymer matrices comprising the utilization of such steps as will allow the formation of solid solutions between pharmaceutical and its matrix or, conversely and in a proper case, substantially avoiding formation of any solid solution between the matrix and pharmaceutical. The advantage of such processes is the greater predictability of qualitative and quantitative nature of release rates of products formed therewith. ## Claims ### Claim 1 Solid-shaped articles for use as an implant in living tissue which implant is a means for administering at a more favorable dosage rate, said articles formed of (1) an active pharmaceutical chemical agent and (2) an organic polymer matrix, said agent and polymer normally forming a composition wherein there is substantial insolubility of one in the other, wherein said articles are formed of a composition of said agent and said polymer which is a solid solution and comprises substantially all of said agent in solution. ### Claim 2 (depends on 1) Articles as defined in claim 1 wherein said active agent is an organic pharmaceutical chemical. ### Claim 3 (depends on 2) Articles as defined in claim 2 wherein said organic chemical is a steroid. ### Claim 4 (depends on 2) Articles as defined in claim 2 wherein said organic polymer matrix is a poly(glycolic acid) or a polylactic acid. ### Claim 5 (depends on 1) Articles as defined in claim 1 wherein said solid solution is a supercooled solution containing a quantity of a solute that have substantial insolubility with said matrix when said matrix is in the liquid state. ### Claim 6 (depends on 1) Articles as defined in claim 1 wherein said active agent is an organic pharmaceutical chemical. ### Claim 7 (depends on 6) Articles as defined in claim 6 wherein said organic chemical is a steroid. ### Claim 8 (depends on 6) Articles as defined in claim 6 wherein said organic polymer matrix is a poly(glycolic acid) a polylactic acid. ### Claim 9 Solid-shaped articles for use as an implant in living tissue which implant is a means for administering at a more favorable dosage rate, said articles formed of (1) an active pharmaceutical chemical agent and (2) an organic polymer matrix, said agent and polymer normally forming a composition wherein there is substantial solubility of one in the other, wherein said articles are formed of a composition of said agent and said polymer which there is no substantial solution of one in the other. ### Claim 10 (depends on 9) Articles as defined in claim 9 wherein said active agent is an organic pharmaceutical chemical. ### Claim 11 (depends on 10) Articles as defined in claim 10 wherein said organic chemical is a steroid. ### Claim 12 (depends on 10) Articles as defined in claim 10 wherein said organic polymer matrix is a poly(glycolic acid) a polylactic acid. ### Claim 13 In a process for administering medication at more favorable dosage rates over an extended period of time by implanting into a host body a solid medicine-bearing implant formed of a polymeric matrix and an active medicinal agent which normally has substantial insolubility in said matrix, the improvement comprising the step of modifying the administering rate by implanting said matrix and agent in a composition which is a substantially complete solid solution of said matrix and said agent. ### Claim 14 (depends on 13) In a process as defined in claim 13 wherein said active agent is an organic pharmaceutical chemical. ### Claim 15 (depends on 14) In a process as defined in claim 14 wherein said organic chemical is a steroid. ### Claim 16 (depends on 14) In a process as defined in claim 14 wherein said organic polymer matrix is a poly(glycolic acid) or a polylactic acid. ### Claim 17 A process for making a medicinal implant article for use as an implant in living tissue which implant is a means for administering at a more favorable dosage rate, said article being made from (1) a polymer matrix which is decomposable in a physiological environment into physiologically-tolerable decomposition products and (2) an organic pharmaceutical chemical which normally has substantial insolubility in said matrix polymer when said polymer is a solid state, said process comprising the mixing of said matrix and said polymer to form a solid solution which is stable under physiological conditions and free from said chemical in non-solute form. ### Claim 18 (depends on 17) A process as defined in claim 17 wherein said article is formed by making a supercooled solution of said solute in said matrix. ### Claim 19 (depends on 17) A process as defined in claim 17 wherein said pharmaceutical is a steroid. ### Claim 20 (depends on 19) A process as defined in claim 19 wherein said polymer is a poly(lactic acid) or a poly(glycolic acid). ### Claim 21 A process for making a medicinal implant article for use as an implant in living tissue which implant is a means for administering at a more favorable dosage rate, said article being made from (1) a polymer matrix which is decomposable in a physiological environment into physiologically-tolerable decomposition products and (2) an organic pharmaceutical chemical which is normally soluble in said matrix polymer when said polymer is in a liquid state, said process comprising the mixing of said matrix and said polymer without liquifying and matrix and thereby maintaining said pharmaceutical entirely in a non-solute state. ### Claim 22 In a process for administering medication at more favorable dosage rates over an extended period of time by implanting into a host body a solid medicine-bearing implant formed of a polymeric matrix and an active medicinal agent which normally has substantial solubility in said matrix, the improvement comprising the step of modifying the administering rate by implanting said matrix and agent as a composition substantially free from any solution of said agent in said matrix.