Long acting GI and esophageal protectant

• US 5,670,163 A
• Filed: 05/02/1995
• Issued: 09/23/1997
• Est. Priority Date: 06/20/1994
• Status: Expired due to Term

• Current Assignee: Lumara Health IP Ltd. (Apollo Global Management, Inc.)
• Original Assignee: KV Pharmaceuticals (Apollo Global Management, Inc.)
• Inventors: Kirschner, Mitchell I., Cuca, Robert C., Levinson, R. Saul, Riley, Thomas Charles Jr., Lienhop, Keith S.
• Primary Examiner(s): Killos, Paul J.
• Application Number:
  US08/432,805
• Time in Patent Office: 875 Days
• Field of Search: 424/439
• US Class Current: 424/439
• 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 9/0058 Chewing gums non-medicinal aspects, preparing chewing gum A23G4/00; chewing gum for care of the teeth or oral cavity, e.g. with breath freshener A61Q11/00
• CPC Class Codes: A61K 9/006 Oral mucosa, e.g. mucoadhesive forms, sublingual droplets; Buccal patches or films; Buccal sprays
• 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

Abstract

A bioadherent, orally ingestible system, which comprises: a water-in-oil emulsion system having at least two phases, one phase comprises from about 75% to about 99% by volume of an internal hydrophylic phase and the other phase comprises from about 25% to about 1% by volume of an external hydrophobic phase, wherein the external hydrophobic phase comprises two components, one component being about 3% to about 97% by volume of the hydrophobic phase of a hydrophobic oil and the other being about 97% to about 3% of an emulsifier having a HLB value less than about 10.

Claims

1. A bioadherent, orally ingestible system, which comprises:

a water-in-oil system having at least two phases, one phase comprises from about 75 to about 99% by volume of an internal hydrophylic phase and the other phase comprises from about 25% to about 1% by volume of an external hydrophobic phase, wherein the external hydrophobic phase is comprised of two components, one component being about 3 to about 97% of a hydrophobic oil the other being about 97% to about 3% of an emulsifier having a HLB value less than 10 wherein the ingestible system adheres to oral mucosa and esophageal mucosa for 30 minutes to 24 hours.

2. The ingestible system of claim 1, wherein the hydrophylic phase contains an active pharmaceutical material.

3. The ingestible system of claim 2, wherein the active pharmaceutical material is water-soluble.

4. The ingestible system of claim 1, wherein the hydrophylic phase is selected from the group consisting of water, glycerine, sorbitol solutions, sugar syrups, polymer solutions and mixtures thereof.

5. The ingestible system of claim 1, wherein the phase is in the form of an emulsion or suspension.

6. The ingestible system of claim 1, wherein the internal phase is present in amounts of about 80 to about 90% by volume.

7. The ingestible system of claim 1, wherein the external phase contains an active pharmaceutical material.

8. The ingestible system of claim 7, wherein the active pharmaceutical material is water-insoluble.

9. The ingestible system of claim 1, wherein the hydrophobic oil is selected from the group consisting of mineral oil, natural or synthetic vegetable oil, long chain fatty acids and alcohols of straight chain alkyls having from 12 to 32 carbon atoms, waxes and mixtures thereof.

10. The ingestible system of claim 1, wherein the emulsifier present in the hydrophobic phase is selected from the group consisting of sorbitan esters, polyglycerol esters of fatty acids, glycerol esters of fatty acids, 1 to 5 mole ethoxylates of fatty acids or esters, saccharides derivatives and mixtures thereof.

11. The ingestible system of claim 10, wherein the emulsifier is selected from the group consisting of polyglycerol oleate, sorbitan monooleate, glycerol monooleate and mixtures thereof.

12. The ingestible system of claim 1, wherein the external phase is present in amounts of about 20% to about 10% by volume of the entire system.

13. The ingestible system of claim 9, wherein the wax is selected from the group consisting of animal waxes, vegetable waxes, synthetic waxes and mixtures thereof.

23. The ingestible system of claim 1, wherein the ingestible system is formulated to adhere to oral mucosa and esophageal mucosa for 2 to 8 hours.

14. A method for treating an oral, esophageal or GI tract disorder, which comprises:

administering orally a therapeutically effective amount of a bioadherent, orally ingestible system, which comprises;

a water-in-oil system having at least two phases, one phase comprises from about 75% to about 99% by volume of an internal hydrophylic phase and the other phase comprises from about 25% to about 1% by volume of an external hydrophobic phase, and wherein the external hydrophobic phase comprises two components, one component being about 3% to about 97% by volume of the hydrophobic phase of a hydrophobic oil and the other being about 97% to about 3% of an emulsifier having a HLB value less than 10 wherein the ingestible system adheres to oral mucosa and esophageal mucosa for 30 minutes to 24 hours.

15. The method of claim 14, wherein the hydrophylic phase contains an active pharmaceutical material which is water-soluble.

16. The method of claim 14, wherein the hydrophobic phase contains an active pharmaceutical material which is water-insoluble.

17. The method of claim 14, wherein the hydrophylic phase is selected from the group consisting of water, glycerine, sorbitol solutions, sugar syrups, polymer solutions and mixtures thereof.

18. The method of claim 14, wherein the internal phase is present in amounts of about 80 to about 90% by volume.

19. The method of claim 14, wherein the hydrophobic oil is selected from the group consisting of mineral oil, natural or synthetic vegetable oil, long chain fatty acids and alcohols of straight chain alkyls having from 12 to 32 carbon atoms, waxes and mixtures thereof.

20. The method of claim 14, wherein the emulsifier present in the hydrophobic phase is selected from the group consisting of sorbitan esters, polyglycerol esters of fatty acids, glycerol esters of fatty acids, 1 to 5 mole ethoxylates of fatty acids or esters, saccharides derivatives and mixtures thereof.

21. The method of claim 19, wherein the emulsifier is selected from the group consisting of polyglycerol oleate, sorbitan monooleate, glycerol monooleate and mixtures thereof.

22. The method of claim 14, wherein the ingestible system adheres to the oral mucosa and esophageal mucosa for 2 to 8 hours.