# US 11,992,482 B2 · Malleable controlled release local anesthetic with hemostatic composition > Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt - Number: US 11,992,482 B2 - Document ID: US11992482B2 - Status: Granted - Kind: B2 - Application number: 15/405,453 - Filed: 2017-01-13 - Published: 2018-06-21 - Granted: 2024-05-28 - Earliest claimed: 2016-12-21 - Assignees: Rilento Pharma, LLC - Applicants: Rilento Pharma, LLC - Inventors: Khashayar Kevin Neshat - Web page: https://patentgrep.com/patent/US11992482B2 ## CPC - A61K 31/445: Non condensed piperidines, e.g. piperocaine - A61K 9/06: Ointments; Bases therefor; {Other semi-solid forms, e.g. creams, sticks, gels (composition of ointments, creams or gels A61K47/00)} - A61K 9/1647: {Polyesters, e.g. poly(lactide-co-glycolide)} - A61K 9/19: lyophilised {, i.e. freeze-dried, solutions or dispersions (lyophilised products with subsequent particle size reduction A61K9/14; granules or pellets made by lyphilisation A61K9/1682; solid oral dosage forms made by lyophilisation A61K9/2095; lyophilisation additives A61K47/00)} - A61K 38/4833: {Thrombin (3.4.21.5)} - A61K 45/06: Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca - A61L 24/0015: {Medicaments; Biocides} - A61L 24/0036: {Porous materials, e.g. foams or sponges} - A61L 24/0094: {containing macromolecular fillers} - A61P 23/02: Local anaesthetics - C12Y 304/21005: Thrombin (3.4.21.5) - A61L 2300/402: Anaestetics, analgesics, e.g. lidocaine - A61L 2300/404: Biocides, antimicrobial agents, antiseptic agents - A61L 2300/418: Agents promoting blood coagulation, blood-clotting agents, embolising agents - 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) - A61L: METHODS OR APPARATUS FOR STERILISING MATERIALS OR OBJECTS IN GENERAL; DISINFECTION, STERILISATION OR DEODORISATION OF AIR; CHEMICAL ASPECTS OF BANDAGES, DRESSINGS, ABSORBENT PADS OR SURGICAL ARTICLES; MATERIALS FOR BANDAGES, DRESSINGS, ABSORBENT PADS OR SURGICAL ARTICLES (preservation of bodies or disinfecting characterised by the agents employed A01N; preserving, e.g. sterilising, food or foodstuffs A23; preparations for medical, dental or toiletry purposes A61K) - A61P: SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS - C12Y: ENZYMES ## Abstract A malleable sustained release formulation is created utilizing a local anesthetic wherein the composition is made sustained release by incorporating it into a bovine or porcine hemostatic agent. The composition is malleable enough to fit into a cavity such as a dental cavity and form the shape of the cavity. In addition to providing sustained release of the anesthetic, the composition also provides quicker reduction in bleeding. ## Claims ### Claim 1 A malleable sustained release formulation designed for packing and sticking in a dental extraction cavity, a surgical cavity or a wound cavity of a patient, the formulation comprising: a homogenous dry blend including a. a local anesthetic formulated into sustained release microparticles of a size between 0.1 and 100 microns, the microparticles encapsulating the local anesthetic for forming a primary sustained release vehicle for the local anesthetic by diffusion from the microparticles, and b. a gelatin powder, wherein the gelatin is selected from the group consisting of a bovine skin hemostatic agent and porcine skin hemostatic agent and having a Bloom value of about 200 to about 400; and an aqueous solution in an amount of about 1.5 to about 10 parts by weight to about 1 part by weight of the gelatin powder within the dry blend, wherein the gelatin powder and the aqueous solution form a gelled matrix with the local anesthetic sustained release microparticles incorporated into and suspended within the gelled matrix such that the gelled matrix comprises a secondary sustained release vehicle for the local anesthetic microparticles by diffusion through the matrix, and wherein the gelled matrix is present in an amount of about 1 to about 7 parts by weight to 1 part by weight of the local anesthetic microparticles such that the gelled matrix with the local anesthetic microparticles suspended therein is a malleable putty prior to its insertion into the cavity of a patient such that a bolus of the malleable formulation can be mixed by hand under low shear ambient conditions for molding a bolus manually sized and shaped to fit the cavity and be retained therein. ### Claim 2 (depends on 1) The formulation according to claim 1 wherein the local anesthetic is selected from the group consisting of bupivacaine, ropivacaine, dibucaine, etidocaine, tetracaine, lidocaine and xylocaine. ### Claim 3 (depends on 1) The formulation according to claim 1 which further comprises an augmenting agent. ### Claim 4 (depends on 1) The formulation according to claim 1 which further comprises an anti-infective. ### Claim 5 (depends on 1) The formulation according to claim 1 wherein poly(lactic-co-glycolic acid) is utilized to form sustained release microparticles of the anesthetic. ### Claim 6 (depends on 1) The formulation according to claim 1 wherein the anesthetic is bupivacaine. ### Claim 7 (depends on 1) The formulation according to claim 1 which further comprises thrombin. ### Claim 8 (depends on 1) The formulation according to claim 1 wherein the anesthetic begins its effect by between at least about an hour and about 5 hours when the anesthetic is utilized after any other local or topical anesthetics first. ### Claim 9 (depends on 1) The formulation according to claim 1 wherein when the formulation is not to be utilized after any other local or topical anesthetics and the onset of action of the formulation is immediate upon placement in the cavity. ### Claim 10 (depends on 1) The formulation according to claim 1 wherein the formulation further comprises an additional local anesthetic not in microparticles. ### Claim 11 (depends on 1) The formulation according to claim 1 wherein the local anesthetic begins its effect in about 1 to 5 hours. ### Claim 12 (depends on 1) The formulation according to claim 1 wherein the local anesthetic duration is up to about 5 days. ### Claim 13 A malleable sustained release formulation designed for packing and sticking in a dental extraction cavity, a surgical cavity or a wound cavity of a patient, the formulation comprising: a homogenous dry blend including a. bupivacaine formulated into sustained release microparticles formed from poly(lactic-co-glycolic acid) of a size between 0.1 and 100 microns, the microparticles encapsulating the bupivacaine for forming a primary sustained release vehicle for the bupivacaine by diffusion from the microparticles, and b. a gelatin powder comprising a porcine skin hemostatic agent having a Bloom value of about 200 to about 400; and an aqueous solution in an amount of about 1.5 to about 10 parts by weight to about 1 part by weight of the gelatin powder within the dry blend, wherein the gelatin powder and the aqueous solution form a gelled matrix with the bupivacaine sustained release microparticles incorporated into and suspended within the gelled matrix such that the gelled matrix comprises a secondary sustained release vehicle for the bupivacaine microparticles by diffusion through the matrix, and wherein the gelled matrix is present in an amount of about 1 to about 7 parts by weight to 1 part by weight of the bupivacaine microparticles such that the gelled matrix with the bupivacaine microparticles suspended therein is a malleable putty prior to its insertion into the cavity of a patient such that a bolus of the malleable formulation can be mixed by hand under low shear ambient conditions for molding a bolus manually sized and shaped to fit the cavity and be retained therein.