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Claims for Patent: 6,248,358

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Claims for Patent: 6,248,358

Title: Bioadhesive progressive hydration tablets and methods of making and using the same
Abstract:A bioadhesive tablet 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 and more importantly may be protected from moisture and the immediate septic environment until after the patient has applied the tablet, 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 tablet is available for absorption (bioavailable).
Inventor(s): Bologna; William J. (Paris, FR), Levine; Howard L. (Oceanside, NY), Cartier; Philippe (Paris, FR), de Ziegler; Dominique (Paris, FR)
Assignee: Columbia Laboratories, Inc. (Rockville Centre, NY)
Application Number:09/379,310
Patent Claims: 1. A sustained release, progressive hydration bioadhesive tablet comprising:

an effective amount of active ingredient selected from the group consisting of glycoproteins, proteins, sex hormones, anti-hormones, nitrates, beta-agonists, beta-antagonists, opioids, opioid-antagonists, antidepressants, HMG CoA reductase inhibitors, antihistamines, ACE inhibitors, prostagladins, and any other active ingredient which is metabolized or degraded by moisture, enzymes or pH,

about 5% to about 50% by weight cellulose,

about 0.5% to about 25% by weight starch,

about 1% to about 50% by weight lactose,

about 0.5% to about 10% by weight water insoluble cross-inked polycarboxylic polymer, and

about 1% to about 75% by weight water soluble polymer.

2. The tablet of claim 1, wherein said tablet comprises between a minuscule amount and about 50% by weight active ingredient.

3. The tablet of claim 2, further comprising:

about 1% by weight silica.

4. The tablet of claim 3, further comprising:

about 0.5% to about 2% by weight talc.

5. The tablet of claim 4, further comprising:

about 0.5% to about 1% by weight magnesium stearate.

6. The tablet of claim 5, wherein said starch is present in about 2% to about 10% by weight, said lactose is present in about 8% to 16% by weight, and said water soluble polymer is present in about 25% to about 35% by weight, and wherein said tablet is adapted for delivering said active ingredient to the bloodstream of a patient via the patient's vaginal cavity.

7. The tablet of claim 5, wherein said starch is present in about 14% to 24% by weight, said lactose is present in about 17% to 27% by weight, and said water soluble polymer is present in about 5% to about 20% by weight, and wherein said tablet is adapted for delivering said active ingredient to the bloodstream of a patient via the patient's buccal cavity.

8. A sustained release, progressive hydration bioadhesive tablet comprising:

an effective amount of an active ingredient selected from the group consisting of glycoproteins, proteins, sex hormones, anti-hormones, nitrates, beta-agonists, beta-antagonists, opioids, opioid-antagonists, antidepressants, HMG CoA reductase inhibitors, antihistamines, ACE inhibitors, prostagladins, and any other active ingredient which is metabolized or degraded by moisture, enzymes or pH,

about 2% to about 30% by weight binder,

about 5% to about 40% by weight lactose,

about 1% to about 3% by weight water insoluble cross-linked polycarboxylic polymer, and

about 5% to about 50% by weight water soluble polymer.

9. The tablet of claim 8, further comprising:

about 0.2 to 2% by weight silica.

10. The tablet of claim 9, further comprising:

about 0.5% to about 2% by weight talc.

11. The tablet of claim 10, further comprising:

about 0.5% to about 2% by weight magnesium stearate.

12. The tablet of claim 10, wherein said active ingredient is testosterone and said testosterone is present in an amount of about 1% to about 30% by weight.

13. The tablet of claim 12, wherein said binder is starch and is present in about 2% to about 10% by weight, said lactose is present in about 8% to 16% by weight, said water soluble polymer is present in about 25% to about 35% by weight, and said tablet is adapted for delivering said active ingredient to the bloodstream of a patient via the patient's vaginal cavity.

14. The tablet of claim 12, wherein said starch is present in about 14% to 24% by weight, said lactose is present in about 17% to 27% by weight, said water soluble polymer is present in about 5% to about 20% by weight, and said tablet is adapted for delivering said active ingredient to the bloodstream of a patient via the patient's buccal cavity.

15. A method of delivering an active ingredient to a person comprising administering the active ingredient via a progressive hydration bioadhesive tablet, wherein said tablet comprises an effective amount of the active ingredient selected from the group consisting of glycoproteins, proteins, sex hormones, anti-hormones, nitrates, beta-agonists, beta-antagonists, opioids, opioid-antagonists, antidepressants, HMG CoA reductase inhibitors, antihistamines, ACE inhibitors, prostagladins, and any other active ingredient which is metabolized or degraded by moisture, enzymes or pH, about 1% to about 50% by weight lactose, about 0.5% to about 10% by weight water insoluble cross-linked polycarboxylic polymer, and about 1% to about 75% by weight water soluble polymer.

16. The method of claim 15 wherein the active ingredient is testosterone.

17. A method of treating or preventing ischemia or Alzheimer's disease comprising administering to a patient a sustained release, progressive hydration bioadhesive tablet comprising a therapeutically effective amount of testosterone, about 1% to about 50% by weight lactose, about 0.5% to about 10% by weight water insoluble cross-linked polycarboxylic polymer, and about 1% to about 75% by weight water soluble polymer.

18. The method of claim 17 wherein the bioadhesive tablet is formulated for buccal administration.

19. The method of claim 17, wherein the bioadhesive tablet is formulated for vaginal administration.

20. A sustained release, progressive hydration bioadhesive tablet, comprising a therapeutically effective amount of an active ingredient selected from the group consisting of glycoproteins, proteins, sex hormones, anti-hormones, nitrates, beta-agonists, beta-antagonists, opioids, opioid-antagonists, antidepressants, HMG CoA reductase inhibitors, antihistamines, ACE inhibitors, prostagladins, and any other active ingredient which is metabolized or degraded by moisture, enzymes or pH, about 1% to about 50% by weight lactose, about 0.5% to about 10% by weight water insoluble cross-linked polycarboxylic polymer, and about 1% to about 75% by weight water soluble polymer.

21. A method for preparing a sustained release, progressive hydration bioadhesive tablet, comprising combining an effective amount of an active ingredient selected from the group consisting of glycoproteins, proteins, sex hormones, anti-hormones, nitrates, beta-agonists, beta-antagonists, opioids, opioid-antagonists, antidepressants, HMG CoA reductase inhibitors, antihistamines, ACE inhibitors, prostagladins, and any other active ingredient which is metabolized or degraded by moisture, enzymes or pH together with about 1% to about 50% by weight lactose, about 0.5% to about 10% by weight water insoluble cross-linked polycarboxylic polymer and 1% to about 75% by weight water soluble polymer.

22. The tablet of claim 5, wherein the active ingredient is terbutaline.

23. A The tablet of claim 22, wherein the cellulose is hydroxpropylmethyl cellulose, the starch is corn starch, the insoluble cross-linked polycarboxylic polymer is polycarbophil, the water soluble polymer is carbomer or Carbomer 974P, and the silica is silicon dioxide.

24. The tablet of claim 12, further comprising cellulose.

25. The tablet of claim 24, wherein the cellulose is hydroxpropylmethyl cellulose, the starch is corn starch, the insoluble cross-linked polycarboxylic polymer is polycarbophil, the water soluble polymer is carbomer or Carbomer 974P, and the silica is silicon dioxide.
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