Compositions for delivering bisphosphonates

• US 20040147484A1
• Filed: 08/19/2003
• Published: 07/29/2004
• Est. Priority Date: 03/01/2001
• Status: Active Grant

• Current Assignee: NOVO Nordisk North America Operations A/S
• Original Assignee: Emisphere Technologies, Inc. (Novo Nordisk A/S)
• Inventors: Dinh, Steve, Boyd, Maria Aurora P.
• Granted Patent: US 7,309,698 B2
• Time in Patent Office: Days
• US Class Current: 514/75
• CPC Class Codes: A61K 2300/00 Mixtures or combinations of active ingredients, wherein at least one active ingredient is fully defined in groups A61K31/00 - A61K41/00
• CPC Class Codes: A61K 31/135 having aromatic rings , e.g. ketamine, nortriptyline methadone A61K31/137
• CPC Class Codes: A61K 31/195 having an amino group
• CPC Class Codes: A61K 31/66 Phosphorus compounds
• CPC Class Codes: A61K 31/663 Compounds having two or more phosphorus acid groups or esters thereof, e.g. clodronic acid, pamidronic acid
• CPC Class Codes: A61K 47/12 Carboxylic acids; Salts or anhydrides thereof
• CPC Class Codes: A61K 47/18 Amines; Amides; Ureas; Quaternary ammonium compounds; Amino acids; Oligopeptides having up to five amino acids
• CPC Class Codes: A61K 47/183 Amino acids, e.g. glycine, EDTA or aspartame
• CPC Class Codes: A61K 9/0053 Mouth and digestive tract, i.e. intraoral and peroral administration rectal administration A61K9/0031
• CPC Class Codes: A61P 19/08 for bone diseases, e.g. rachitism, Paget's disease
• CPC Class Codes: A61P 19/10 for osteoporosis
• CPC Class Codes: C07C 235/60 having the nitrogen atoms of the carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
• CPC Class Codes: C07C 235/64 having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a six-membered aromatic ring
• CPC Class Codes: C07C 59/68 the oxygen atom of the ether group being bound to a non-condensed six-membered aromatic ring
• CPC Class Codes: C07C 59/90 containing singly bound oxygen-containing groups

Abstract

Compounds and compositions for the delivery of bisphosphonates are provided. Methods of preparation, administration and treatment are provided as well.

Claims

1. A composition comprising:

(A) at least one bisphosphonate; and

(B) at least one of compounds 1-10 or salts thereof.

2. The composition of claim 1, wherein the bisphosphonate is selected from alendronate, clodronate, etidronate, ibandronate, incadronate, minodronate, neridronate, olpadronate, pamidronate, risedronate, tiludronate, zoledronate, EB1053, YH529, analogs, mimetics, and polyethylene glycol-modified derivatives thereof.

3. The composition of claim 2, wherein the bisphosphonate is alendronate.

4. The composition of claim 1 wherein (B) is compound 1 or a salt thereof.

5. The composition of claim 1 wherein (B) is compound 2 or a salt thereof.

6. The composition of claim 1 wherein (B) is compound 3 or a salt thereof.

7. The composition of claim 1 wherein (B) is compound 4 or a salt thereof.

8. The composition of claim 1 wherein (B) is compound 5 or a salt thereof.

9. The composition of claim 1 wherein (B) is compound 6 or a salt thereof.

10. The composition of claim 1 wherein (B) is compound 7 or a salt thereof.

11. The composition of claim 1 wherein (B) is compound 8 or a salt thereof.

12. The composition of claim 1 wherein (B) is compound 9 or a salt thereof.

13. A dosage unit form comprising:

(A) the composition of claim 1;

and

(B) (a) an excipient

(b) a dilutent

(c) a disintegrant,

(d) a lubricant,

(e) a plasticizer,

(f) a colorant,

(g) a dosing vehicle, or

(h) any combination thereof.

14. The dosage unit form of claim 12, wherein the dosage unit form comprises a dosing vehicle comprising a tablet, a capsule, a powder, or a liquid.

15. The dosage unit form of claim 12, wherein the dosing vehicle is liquid selected from the group consisting or water, 1,2-propane diol, ethanol, and any combination

16. A method for administering bisphosphonate to an animal in need thereof, the method comprising

administering orally to the animal the composition of claim 1.

17. A method for treating or preventing bone-related disorders comprising administering orally the composition of claim 1.

18. A method for preventing osteoporosis comprising administering orally the composition of claim 1.

19. A method for preparing a composition comprising mixing:

(A) at least one bisphosphonate;

(B) a compound selected from compounds 1-9 and salts thereof; and

(C) optionally, a dosing vehicle.

20. A composition comprising:

(A) at least one bisphosphonate; and

(B) at least one of compound A or a salt thereof.

21. A composition comprising:

(A) at least one bisphosphonate; and

(B) at least one of compound B or a salt thereof.