Controlled Long Acting Release Pharmaceutical Preparation For Use In The Oral Cavity

• US 20080085248A1
• Filed: 12/28/2005
• Published: 04/10/2008
• Est. Priority Date: 01/03/2005
• Status: Abandoned Application

• Current Assignee: Calcident Active Ltd.
• Original Assignee: Calcident Active Ltd.
• Inventors: Sela, Yoram
• Application Number:
  US11/794,168
• Publication Number:
  US 20080085248A1
• Time in Patent Office: Days
• US Class Current: 424/49
• CPC Class Codes: A61K 31/00 Medicinal preparations containing organic active ingredients
• CPC Class Codes: A61K 31/7048 having oxygen as a ring hetero atom, e.g. leucoglucosan, hesperidin, erythromycin, nystatin , digitoxin or digoxin
• CPC Class Codes: A61K 33/06 Aluminium, calcium or magnesium; Compounds thereof , e.g. clay
• CPC Class Codes: A61K 33/30 Zinc; Compounds thereof
• CPC Class Codes: A61K 8/19 containing inorganic ingredients
• CPC Class Codes: A61K 9/0004 Osmotic delivery systems; Sustained release driven by osmosis, thermal energy or gas
• CPC Class Codes: A61K 9/0056 Mouth soluble or dispersible forms; Suckable, eatable, chewable coherent forms; Forms rapidly disintegrating in the mouth; Lozenges; Lollipops; Bite capsules; Baked products; Baits or other oral forms for animals
• CPC Class Codes: A61K 9/0065 Forms with gastric retention, e.g. floating on gastric juice, adhering to gastric mucosa, expanding to prevent passage through the pylorus
• CPC Class Codes: A61K 9/2027 obtained by reactions only involving carbon-to-carbon unsaturated bonds, e.g. polyvinyl pyrrolidone, poly(meth)acrylates
• CPC Class Codes: A61K 9/2054 Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
• CPC Class Codes: A61K 9/2866 Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
• CPC Class Codes: A61Q 11/00 Preparations for care of the teeth, of the oral cavity or of dentures; Dentifrices, e.g. toothpastes; Mouth rinses

Abstract

The present invention relates to a controlled long acting release pharmaceutical preparation for use in the oral cavity either for the treatment of diseases of the oral cavity or; for releasing said pharmaceutical preparation into said oral cavity. Said pharmaceutical preparation comprises at least a therapeutic agent, a binder and a lubricant (hereinafter “the preparation” or “the pharmaceutical preparation”).

Claims

1. A controlled long acting release pharmaceutical preparation for the oral cavity either for the treatment of diseases of the oral cavity or for releasing said pharmaceutical preparation into said oral cavity, comprising at least a therapeutic agent, a binder and a lubricant.

2. The pharmaceutical preparation of claim 1, in the form of a drug comprising suitable pharmacological active materials.

3. The pharmaceutical preparation of claim 1, wherein the diseases are at least one of (1) a human disease or human diseases and (2) veterinary disease or veterinary diseases.

4. The pharmaceutical preparation of claim 1, wherein said pharmaceutical preparation is compatible with dental devices.

5. The pharmaceutical preparation of claim 1, comprising a therapeutic agent in the amount of from 0.1 mg to 1000 mg, a binder in the amount of from 1% w/w to 10% w/w of the preparation and a lubricant in the amount of from 1% w/w to 10% w/w of the preparation.

6. The pharmaceutical preparation of claim 1, further comprising a rate controlling polymer as a carrier, a filler, a glidant, and a rate controlling polymer as a coating material.

7. The pharmaceutical preparation of claim 6, which comprises a therapeutic agent in the amount of from 0.1 mg to 1000 mg, from 1% w/w to 10% w/w of the preparation of a binder, from 5% w/w to 50% w/w of the preparation of a rate controlling polymer, from 1% w/w to 10% w/w of the preparation of a glidant, from 1% w/w to 10% w/w of the preparation used as a lubricant and a pore forming agent used in amount of from 5% w/w to 50% w/w of the dry polymer.

8. A method of treating dental caries, comprising treating dental caries utilizing the pharmaceutical preparation of claim 1.

9. The method of claim 8, wherein the therapeutic agent is a Calcium salt or a Calcium salt in combination with therapeutic adjuvants.

10. The method of claim 9, wherein the therapeutic agent is at least one agent selected from the group consisting of Calcium Carbonate, Calcium Phosphate and Calcium Glycerophosphate.

11. The method of claim 9, wherein the Calcium salts are at least one salt selected from the group consisting of Calcium Fluoride, Calcium Hydroxide, Calcium Oxide, Calcium Saccharate, Calcium Sulphate, Calcium Acetate, Calcium Chloride, Calcium Citrate, Calcium Glubionate, Calcium Gluceptate, Calcium Gluconate, Calcium Lactate, Calcium Lactate Gluconate, Calcium Lactobionate, Calcium Laevulinate, Calcium Hydrogen Phosphate, Calcium Pidolate and Calcium Sodium Lactate.

12. The method of claim 9, wherein the therapeutic agent is at least one adjuvant selected from the group consisting of Casein Phosphopeptide and Zinc.

13. The pharmaceutical preparation of claim 1, further comprising 5% to 25% Klucel EF, 75% to 95% calcium glycerophosphate and 0.2% to 1% lubricant, wherein the release mechanism is based on diffusion.

14. The pharmaceutical preparation of claim 1, further comprising 5% to 25% Ethyl cellulose, 75% to 95% calcium glycerophosphate, and 0.2% to 1% lubricant wherein the release mechanism is based on erosion.

15. The pharmaceutical preparation of claim 1, wherein the therapeutic agent is utilized for anticandidiasis and antifungal treatments and is at least one member selected from the group consisting of Nystatin, Imidazols, Ciclopirox and Clotimazole.

16. The pharmaceutical preparation of claim 1, wherein said therapeutic agent is used for antiseptic treatment.

17. The pharmaceutical preparation of claim 1, wherein said therapeutic agent is used for breath refreshers used for the treatment of Xerostomy.

18. The pharmaceutical preparation of claim 1, wherein the therapeutic agent is used for the treatment of mouth ulcerations such as Aphthous Stomatitis/Cancer Sores selected among Triamcinolone Acetonide, and Tetracycline.

19. The pharmaceutical preparation of claim 1, wherein the therapeutic agent is selected from the group consisting of an anesthetic and Lidocaine.

20. The pharmaceutical preparation of claim 1, having a preferred absorption at the upper parts of the GI tract.

21. The pharmaceutical preparation of claim 20, wherein said pharmaceutical preparation is at least one member selected from the group consisting of:

any pharmacologically active material which is released at the upper parts of the G.I. tract, Immunosuppressants, Sirolimus, Tacrolimus, Antivirals, Acyclovir, Anti HIV agents, Azidothimidine (AZT), Antiparkinsonian agents, Levodopa, Carbidopa, Antibiotics, and Ciprofloxacin.

22. The pharmaceutical preparation of claim 1, said preparation being a capsule, a film, a pellet, a tablet, a pill, a gel or any other acceptable solid pharmaceutical dosage form or a combination thereof used in oral delivery of pharmaceutical preparations.

23. The pharmaceutical preparation of claim 1, wherein the preparation is well-suited for long term intra-oral deposition and mineral or drug release in the singular environment of the oral cavity.

24. The pharmaceutical preparation of claim 1, wherein the binder is at least one member selected from the group consisting of PVP, Methocel, Ethocel and Klucel.

25. The pharmaceutical preparation of claim 1, wherein the lubricant is at least one member selected from the group consisting of Syloid, PEG, Mg Stearate and Pruv.

26. The pharmaceutical preparation of claim 1, comprising a coating layer being a rate controlling polymer comprising at least one member selected from the group consisting of Ethocel (Ethylcellulose), Cellulose Acetate, Acrylic Polymers, HPMC (Hydroxypropyl Methylcellulose), Hydroxy Propyl Cellulose, and Polyox (high MW polyethylene oxide).

27. The pharmaceutical preparation of claim 1, wherein the coating layer is a semi permeable membrane and the dosage form comprises osmotic components.

28. The pharmaceutical preparation of claim 1, comprising a carrier base material that includes at least one member selected from the group consisting of hydrophilic polymers, hydroxypropylmethyl cellulose (HPMC), hydroxypropyl cellulose (HPC), GUMS, polyethylene oxide (Polyox), polyvinyl pyrolidone (PVP), hydrophobic polymers, ethyl cellulose (Ethocel), acrylate based polymers, Eudragit, PVA, and Kollidone SR.

29. The pharmaceutical preparation of claim 1, further comprising a filler selected from at least one of microcrystalline cellulose and lactose;

and a flavor comprising at least one member selected from the group consisting of Menthol, Saccharin, and Vanillin.

30. A method for the preparation of a pharmaceutical preparation comprising preparing the controlled long acting release pharmaceutical preparation of claim 1.

31. A method for utilizing a pharmaceutical preparation comprising utilizing the controlled long acting release pharmaceutical preparation of claim 1.

32. A method comprising applying the pharmaceutical preparation of claim 1 for an extended term in an oral cavity.

33. A method for promoting tooth re-mineralization, for avoiding tooth de-mineralization, and for applying a long term anti-demineralization therapy, comprising utilizing the using a pharmaceutical preparation of claim 1.

34. A method of manufacturing a medicament for treatment of diseases in an oral cavity, comprising utilizing the pharmaceutical composition of claim 1.

35. A method of manufacturing a medicament for absorption of upper parts of a GI tract, comprising utilizing the pharmaceutical composition of claim 1.

36. A pharmaceutical preparation according to claim 1, being stored in a device located in an oral cavity for at least one of (a) the treatment of diseases of the oral cavity;

or (b) releasing the pharmaceutical preparation into said oral cavity.

37. A device for maintaining a preparation according to claim 1, wherein said device has been in position in an oral cavity for a period of time in the range of from several hours to several months.

39. The pharmaceutical preparation of claim 6, further comprising pore forming agents.

38. (canceled)