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Details for Patent: 8,765,177

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Details for Patent: 8,765,177

Title:Bioadhesive progressive hydration tablets
Abstract: A bioadhesive controlled, extended release progressive hydration composition wherein the active ingredient may be protected from water or the surrounding environment, thereby protecting it from metabolism or from other degradation caused by moisture, enzymes, or pH effects, and making it bioavailable only at a controlled rate. The active ingredient may be protected from moisture during the manufacturing process, as necessary or desired, and more importantly may be protected from moisture and the immediate septic environment until well after the patient has applied the composition, and then only at a slow and controlled rate. It is by this process of progressive hydration that the active ingredient remains protected for many hours after administration. It is also by the process of progressive hydration that controlled and sustained release is achieved because only that part of the active ingredient that is the hydrated (aqueous) fraction of the composition is available for absorption (bioavailable).
Inventor(s): Levine; Howard L. (Oceanside, NY), Bologna; William J. (Paris, FR), De Ziegler; Dominique (Geneva, CH)
Assignee: Columbia Laboratories, Inc. (Boston, MA)
Filing Date:May 11, 2006
Application Number:11/431,611
Claims:1. A bioadhesive controlled, sustained release progressive hydration pharmaceutical composition for delivering an active ingredient to a mucosal surface of a mammal, comprising: an effective amount of a dry reservoir of an active ingredient, and a sustained release active ingredient delivery system comprising a bioadhesive water insoluble, water-swellable cross-linked polycarboxylic polymer present in the delivery system in a non-salt form, and a bioadhesive water soluble polymer, wherein the polymers are present in amounts which enable the composition to become progressively hydrated to provide extended release of the active ingredient over time; wherein the delivery system includes amounts of the polymers which are effective to allow the composition to adhere when contacting a mucosal surface of a mammal for a time sufficient to provide extended release of the active ingredient to the mucosal surface.

2. The composition of claim 1, wherein the composition is formulated as a tablet for delivery of the active ingredient via the mucosal surface of a buccal, vaginal, nasal, or rectal cavity.

3. The composition of claim 2, wherein the water insoluble, water-swellable cross-linked polycarboxylic polymer is polycarbophil.

4. The composition of claim 3, wherein the composition is in the form of a tablet that is formulated to gelify or swell to avoid asphyxiation.

5. The composition of claim 3, wherein the water soluble polymer is carbomer 974P.

6. The composition of claim 1, wherein the active ingredient comprises one or more of non-steroidal anti-inflammatory drugs (NSAIDS), anti-infectives, anesthetics, immune system modifiers, muscarinic agonists, muscarinic antagonists, anti-neoplastic agents, vitamin K, ondansetron, levocarnitine, anti-fungals, carbamide peroxide, dopamine antagonists, biphosphonates, nicotine, anti-virals, anti-diabetagenics, peptides, insulin, anti-parkinson agents, low molecular weight heparins, or antimicrobials.

7. The composition of claim 1, wherein the active ingredient comprises one or more of follicle-stimulating hormone (FSH), luteinizing hormone (LH), human chorionic gonadotropin (HCG), thyroid-stimulating hormone (TSH), tamoxifen, mifepristone, raloxifene, nitroglycerin, isosorbide, erythrityl tetranitrate, pentaerythritol tetranitrate, terbutaline, albuterol, pirbuterol, bitolterol, ritodrine, propranolol, metoprolol, nadolol, atenolol, timolol, esmolol, pindolol, acebutolol, labetalol, morphine, hydromorphone, oxymorphone, codeine, hydrocodone, oxycodone, levorphanol, levallorphan, buprenorphine, fentanyl, nalbuphine, butorphanol, pentazocine, naloxone, nalmefene, diclofenac, etodolac, fenoprofen, lurbiprofen, ibuprofen, indomethacin, ketoprofen, ketorolac, meclofenamate, mefenamic acid, meloxicam, nabumetone, naproxin, oxaprozin, piroxicam, sulindac, tolmetin, lidocaine, cocaine, chloroprocaine, tetracaine, prilocalne, mepivacaine, buipivacaine, levobupivacaine, articaine, ropivacaine, phenol, benzocaine, pramoxine, dyclonine, etidocaine, procaine, proparacaine, dibucaine, pramoxine, misoprostol, imiquimod, bethanecol, oxybutynin, melphalan, fluorouracil, vinca alkaloids, bleomycin, cisplatin, bromocriptine, acyclovir, metformin, octreotide, desmopressin, GNRH, levodopa, or metronidazole.

8. The composition of claim 1, wherein the active ingredient comprises one or more of estradiol, testosterone, progesterone, terbutaline, prostaglandin E2, desmopressin, metronidazole, or ibuprofen.

9. The composition of claim 8, wherein the active ingredient comprises testosterone and is present in an amount of about 0.04 mg to 45 mg per unit dosage of the composition.

10. The composition of claim 1, wherein the delivery system releases the active ingredient for a period of time longer than the immediate release dosage form of the active ingredient.

11. A method for sustained release delivery of an active ingredient to the bloodstream of a mammal through a mucosal surface which comprises administering to a mucosal surface of a mammal in need of receiving the active ingredient a composition that includes an effective amount of a dry reservoir of the active ingredient and a sustained release active ingredient delivery system comprising a bioadhesive water insoluble, water-swellable cross-linked polycarboxylic polymer in a non-salt form, and a bioadhesive water soluble polymer, wherein the delivery system includes amounts of the polymers which are effective to allow the composition to adhere and progressively hydrate when contacting the mucosal surface of a mammal for a time sufficient to provide extended release of the active ingredient to the mucosal surface.

12. The method of claim 11, wherein the administration is via the mucosal surface of a buccal, vaginal, nasal, or rectal cavity of the mammal.

13. The method of claim 12, wherein the water insoluble, water-swellable cross-linked polycarboxylic polymer is polycarbophil.

14. The method of claim 13, wherein the composition is in the form of a tablet is formulated to gelify or swell to avoid asphyxiation.

15. The method of claim 13, wherein the water soluble polymer is carbomer 974P.

16. The method of claim 11, wherein the active ingredient comprises one or more of non-steroidal anti-inflammatory drugs (NSAIDS), anti-infectives, anesthetics, immune system modifiers, muscarinic agonists, muscarinic antagonists, anti-neoplastic agents, vitamin K, ondansetron, levocarnitine, anti-fungals, carbamide peroxide, dopamine antagonists, biphosphonates, nicotine, anti-virals, anti-diabetagenics, peptides, insulin, anti-parkinson agents, low molecular weight heparins, or antimicrobials.

17. The method of claim 11, wherein the active ingredient comprises one or more of follicle-stimulating hormone (FSH), luteinizing hormone (LH), human chorionic gonadotropin (HCG), thyroid-stimulating hormone (TSH), tamoxifen, mifepristone, raloxifene, nitroglycerin, isosorbide, erythrityl tetranitrate, pentaerythritol tetranitrate, terbutaline, albuterol, pirbuterol, bitolterol, ritodrine, propranolol, metoprolol, nadolol, atenolol, timolol, esmolol, pindolol, acebutolol, labetalol, morphine, hydromorphone, oxymorphone, codeine, hydrocodone, oxycodone, levorphanol, levallorphan, buprenorphine, fentanyl, nalbuphine, butorphanol, pentazocine, naloxone, nalmefene, diclofenac, etodolac, fenoprofen, lurbiprofen, ibuprofen, indomethacin, ketoprofen, ketorolac, meclofenamate, mefenamic acid, meloxicam, nabumetone, naproxin, oxaprozin, piroxicam, sulindac, tolmetin, lidocaine, cocaine, chloroprocaine, tetracaine, prilocalne, mepivacaine, buipivacaine, levobupivacaine, articaine, ropivacaine, phenol, benzocaine, pramoxine, dyclonine, etidocaine, procaine, proparacaine, dibucaine, pramoxine, misoprostol, imiquimod, bethanecol, oxybutynin, melphalan, fluorouracil, vinca alkaloids, bleomycin, cisplatin, bromocriptine, acyclovir, metformin, octreotide, desmopressin, GNRH, levodopa, or metronidazole.

18. The method of claim 11, wherein the active ingredient comprises one or more of estradiol, testosterone, progesterone, terbutaline, prostaglandin E2, desmopressin, metronidazole, or ibuprofen.

19. The method of claim 18, wherein the active ingredient comprises testosterone and is present in an amount of about 0.04 mg to 45 mg per unit dosage of the composition.

20. The method of claim 11, wherein the delivery system releases the active ingredient for a period of time longer than the immediate release dosage form of the active ingredient.

21. A method of treating a health condition in a human which comprises administering a tablet to a mucosal surface of the human, wherein the tablet progressively hydrates to release an active ingredient over an extended period of time, the tablet comprising an effective amount of a dry reservoir of the active ingredient, and a sustained release active ingredient delivery system comprising a bioadhesive water insoluble, water-swellable cross-linked polycarboxylic polymer present in a non-salt form, and a bioadhesive water soluble polymer, wherein the delivery system includes amounts of the polymers which are effective to allow the composition to adhere and to progressively hydrate when contacting a mucosal surface of a mammal to provide extended release of the active ingredient to the human.

22. The method of claim 21, wherein the administration is via the mucosal surfaces in a buccal, vaginal, nasal, or rectal cavity of the human.

23. The method of claim 22, wherein the water insoluble, water-swellable cross-linked polycarboxylic polymer is polycarbophil.

24. The method of claim 23, wherein the composition is in the form of a tablet is formulated to gelify or swell to avoid asphyxiation.

25. The method of claim 23, wherein the water soluble polymer is carbomer 974P.

26. The method of claim 21, wherein the active ingredient comprises one or more of non-steroidal anti-inflammatory drugs (NSAIDS), anti-infectives, anesthetics, immune system modifiers, muscarinic agonists, muscarinic antagonists, anti-neoplastic agents, vitamin K, ondansetron, levocarnitine, anti-fungals, carbamide peroxide, dopamine antagonists, biphosphonates, nicotine, anti-virals, anti-diabetagenics, peptides, insulin, anti-parkinson agents, low molecular weight heparins, or antimicrobials.

27. The method of claim 21, wherein the active ingredient comprises one or more of follicle-stimulating hormone (FSH), luteinizing hormone (LH), human chorionic gonadotropin (HCG), thyroid-stimulating hormone (TSH), tamoxifen, mifepristone, raloxifene, nitroglycerin, isosorbide, erythrityl tetranitrate, pentaerythritol tetranitrate, terbutaline, albuterol, pirbuterol, bitolterol, ritodrine, propranolol, metoprolol, nadolol, atenolol, timolol, esmolol, pindolol, acebutolol, labetalol, morphine, hydromorphone, oxymorphone, codeine, hydrocodone, oxycodone, levorphanol, levallorphan, buprenorphine, fentanyl, nalbuphine, butorphanol, pentazocine, naloxone, nalmefene, diclofenac, etodolac, fenoprofen, lurbiprofen, ibuprofen, indomethacin, ketoprofen, ketorolac, meclofenamate, mefenamic acid, meloxicam, nabumetone, naproxin, oxaprozin, piroxicam, sulindac, tolmetin, lidocaine, cocaine, chloroprocaine, tetracaine, prilocalne, mepivacaine, buipivacaine, levobupivacaine, articaine, ropivacaine, phenol, benzocaine, pramoxine, dyclonine, etidocaine, procaine, proparacaine, dibucaine, pramoxine, misoprostol, imiquimod, bethanecol, oxybutynin, melphalan, fluorouracil, vinca alkaloids, bleomycin, cisplatin, bromocriptine, acyclovir, metformin, octreotide, desmopressin, GNRH, levodopa, or metronidazole.

28. The method of claim 21, wherein the active ingredient comprises one or more of estradiol, testosterone, progesterone, terbutaline, prostaglandin E2, desmopressin, metronidazole, or ibuprofen.

29. The method of claim 21, wherein the delivery system releases the active ingredient for a period of time longer than the immediate release dosage form of the active ingredient.
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