# US 9,517,242 B2 · Dosage forms for oral administration of zoledronic acid or related compounds for treating disease > Agents: this data is available as JSON from the patentgrep API and MCP server — see https://patentgrep.com/llms.txt - Number: US 9,517,242 B2 - Document ID: US9517242B2 - Status: Granted - Kind: B2 - Application number: 15/043,281 - Filed: 2016-02-12 - Published: 2016-06-09 - Granted: 2016-12-13 - Earliest claimed: 2012-05-14 - Assignees: Antecip Bioventures II LLC - Applicants: Antecip Bioventures II LLC - Inventors: Herriot Tabuteau - Web page: https://patentgrep.com/patent/US9517242B2 ## CPC - A61K 31/675: having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate - A61K 9/0053: {Mouth and digestive tract, i.e. intraoral and peroral administration} - A61K 9/20: Pills, tablets, {discs, rods (A61K9/0004, A61K9/0007, A61K9/0056, A61K9/0065 take precedence; for reconstitution of a drink A61K9/0095)} - A61K 9/2004: {Excipients; Inactive ingredients} - A61K 9/2009: {Inorganic compounds} - A61K 9/2013: {Organic compounds, e.g. phospholipids, fats} - A61K 9/2027: {obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates} - A61K 9/2054: {Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose} - A61K 9/28: Dragees; Coated pills or tablets {, e.g. with film or compression coating (A61K9/2072 takes precedence, e.g. partially coated tablets A61K9/2072, coated multilayer tablets A61K9/2086, tablets with drug-coated core A61K9/209)} - A61K 31/663: Compounds having two or more phosphorus acid groups or esters thereof, e.g. clodronic acid, pamidronic acid - A61K 45/06: Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca - A61K 47/12: Carboxylic acids; Salts or anhydrides thereof - 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 Oral dosage forms of bisphosphonate compounds, such as zoledronic acid, can be used to treat or alleviate pain or related conditions. The bioavailability of zoledronic acid can be enhanced by administering the zoledronic acid in the disodium salt form. ## Claims ### Claim 1 A method of delivering zoledronic acid to the blood of a human being comprising orally administering zoledronic acid in the disodium salt form to a human being in need of treatment with zoledronic acid, wherein the human being is instructed not to eat or drink for at least 1 hour before and at least 30 minutes after the zoledronic acid in the disodium salt form is administered, wherein the zoledronic acid in the disodium salt form is administered in a manner that results in a bioavailability of zoledronic acid in the human being of 1% to about 4%. ### Claim 2 (depends on 1) The method of claim 1, wherein the zoledronic acid in the disodium salt form is administered in a manner that results in a bioavailability of zoledronic acid in the human being of 1.5% to 3%. ### Claim 3 (depends on 1) The method of claim 1, wherein the zoledronic acid in the disodium salt form is administered in a dosage form that contains at least 10% w/w of zoledronic acid in the disodium salt form. ### Claim 4 (depends on 1) The method of claim 1, wherein about 10 mg to about 200 mg of zoledronic acid in the disodium salt form is administered within a month. ### Claim 5 (depends on 1) The method of claim 1, wherein about 25 mg to about 150 mg of zoledronic acid in the disodium salt form is administered within a month. ### Claim 6 (depends on 1) The method of claim 1, wherein about 400 mg to about 500 mg of zoledronic acid in the disodium salt form is administered within a month. ### Claim 7 (depends on 1) The method of claim 1, wherein the zoledronic acid in the disodium salt form is administered only once. ### Claim 8 (depends on 1) The method of claim 1, wherein the zoledronic acid in the disodium salt form is administered once daily to once weekly. ### Claim 9 (depends on 1) The method of claim 1, wherein there is a period of about one week to about one month between instances of administration of the zoledronic acid in the disodium salt form. ### Claim 10 (depends on 1) The method of claim 1, wherein there is a period of at least one month between instances of administration of the zoledronic acid in the disodium salt form. ### Claim 11 (depends on 1) The method of claim 1, wherein the zoledronic acid in the disodium salt form is administered once a month for only 3 months. ### Claim 12 (depends on 1) The method of claim 1, wherein the zoledronic acid in the disodium salt form is administered in a manner that results in a bioavailability of zoledronic acid in the human being of 1.2% to 3%. ### Claim 13 (depends on 1) The method of claim 1, wherein the zoledronic acid in the disodium salt form is administered in a manner that results in a bioavailability of zoledronic acid in the human being of 1.5% to 2%. ### Claim 14 (depends on 1) The method of claim 1, wherein the zoledronic acid in the disodium salt form is administered in a manner that results in a bioavailability of zoledronic acid in the human being of 2% to 3%. ### Claim 15 (depends on 1) The method of claim 1, wherein the zoledronic acid in the disodium salt form is administered in a solid dosage form. ### Claim 16 (depends on 1) The method of claim 1, wherein the zoledronic acid in the disodium salt form is administered in a solid dosage form that has a hardness of at least about 5 kPa. ### Claim 17 (depends on 1) The method of claim 1, wherein the zoledronic acid in the disodium salt form is administered in a solid dosage form that contains about 50% w/w to about 90% w/w of zoledronic acid in the disodium salt form. ### Claim 18 (depends on 1) The method of claim 1, wherein the zoledronic acid in the disodium salt form is administered in a manner that results in the zoledronic acid having a 24 hour sustained plasma factor of at least about 3. ### Claim 19 (depends on 1) The method of claim 1, wherein the human being remains upright for at least one hour after administration of the zoledronic acid in the disodium salt form. ### Claim 20 (depends on 12) The method of claim 12, wherein about 30 mg to about 500 mg of zoledronic acid in the disodium salt form is administered per month. ### Claim 21 A method of delivering zoledronic acid to the blood of a human being comprising orally administering zoledronic acid in the disodium salt form to a human being in need of treatment with zoledronic acid, wherein the human being is instructed not to eat or drink for at least 1 hour before and at least 30 minutes after the zoledronic acid in the disodium salt form is administered, wherein the zoledronic acid in the disodium salt form is administered in an amount and frequency that results in an AUC of zoledronic acid that is about 100 ng·h/mL to about 2000 ng·h/mL each time the zoledronic acid in the disodium salt form is administered. ### Claim 22 (depends on 21) The method of claim 21, wherein about 10 mg to about 100 mg of zoledronic acid in the disodium salt form is administered within one month. ### Claim 23 (depends on 21) The method of claim 21, wherein about 100 mg to about 300 mg of zoledronic acid in the disodium salt form is administered within one month. ### Claim 24 (depends on 21) The method of claim 21, wherein about 200 mg to about 300 mg of zoledronic acid in the disodium salt form is administered within one week. ### Claim 25 (depends on 21) The method of claim 21, wherein there is a period of about one week to about one month between instances of administration of zoledronic acid in the disodium salt form. ### Claim 26 (depends on 21) The method of claim 21, wherein the zoledronic acid in the disodium salt form is administered at least three times. ### Claim 27 A method of delivering zoledronic acid to the blood of a human being comprising orally administering zoledronic acid in the disodium salt form to a human being in need of treatment with zoledronic acid; wherein the zoledronic acid in the disodium salt form is administered at least once weekly and no more often than once daily and in a manner that results in a bioavailability of zoledronic acid in the human being of 1% to about 4% after each administration. ### Claim 28 (depends on 27) The method of claim 27, wherein about 30 mg to about 200 mg of zoledronic acid in the disodium salt form is administered within two months. ### Claim 29 (depends on 27) The method of claim 27, wherein about 300 mg to about 500 mg of zoledronic acid in the disodium salt form is administered within two months. ### Claim 30 (depends on 27) The method of claim 27, wherein about 100 mg to about 500 mg of zoledronic acid in the disodium salt form is administered within two months.