Oral osmotic device

• US 5,200,194 A
• Filed: 12/18/1991
• Issued: 04/06/1993
• Est. Priority Date: 12/18/1991
• Status: Expired due to Term

• Current Assignee: ALZA Corporation (Johnson & Johnson)
• Original Assignee: ALZA Corporation (Johnson & Johnson)
• Inventors: Edgren, David E., Bhatti, Gurdish K.
• Primary Examiner(s): Page, Thurman K.
• Assistant Examiner(s): HORNE, LEON
• Application Number:
  US07/809,741
• Time in Patent Office: 475 Days
• Field of Search: 424/473, 424/472, 424/468
• US Class Current: 424/473
• CPC Class Codes: A61K 9/0004 Osmotic delivery systems; Sustained release driven by osmosis, thermal energy or gas

Abstract

An osmotic device (10) for delivering a beneficial drug, such as an anti-microbial drug, into the mouth of a human patient is disclosed. The device (10) has a size and shape adapting it to be comfortably retained in the mouth for extended periods of time. The device comprises a thin semipermeable membrane wall (12) surrounding a compartment (13) housing a beneficial agent (14) that has at least some degree of solubility in aqueous biological fluids, e.g., saliva, and a fibrous support material (15) composed of hydrophilic water-insoluble fibers. A passageway (17) in the wall (12) connects the agent 14) with the exterior of the device (10). The wall (12) is permeable to the passage of aqueous biological fluid but substantially impermeable to the passage of the fibrous support material (15). The fibrous support material (15), once hydrated, provides a rigid support for the thin semipermeable wall (12) and prevents the device (10) from prematurely releasing the beneficial agent (14) even when the device (10) is subjected to patient sucking.

Claims

1. An osmotic device for the controlled delivery of a beneficial agent to an oral cavity of an animal over an extended delivery period, the device having a size and shape suitable for comfortably retaining the device in the oral cavity for the extended delivery period, the device including a wall surrounding a solid dose of the beneficial agent, the beneficial agent exhibiting at least some degree of solubility in an aqueous fluid present in the oral cavity, and a fibrous support material comprised of hydrophilic water-insoluble fibers selected from the group consisting of cellulose fibers, microcrystalline cellulose fibers, cellulose ester fibers, cross-linked sodium carboxymethyl cellulose fiber, low-substituted hydroxypropyl cellulose fibers, seaweed fibers, chitin fibers, chitsan fibers, and blends thereof, the wall having a passageway communicating the solid dose with the exterior of the device, the wall being formed of a semipermeable material which is (i) permeable to the passage of the aqueous fluid and (ii) substantially impermeable to the passage of the fibrous support material.

2. The osmotic device of claim 1, wherein the solid dose contains an amount of the fibrous support material sufficient to impart a buckling pressure of at least about 100 mm Hg during use.

3. The osmotic device of claim 1, wherein the solid dose contains about 5 to 70 vol % of the fibrous support material.

5. The osmotic device of claim 1, wherein the device exhibits a buckling pressure of greater than about 200 mm Hg during use.

6. The osmotic device of claim 1, wherein the semipermeable wall has a fluid permeability of greater than about 2×

10^-4 cm.mil/atm.hr.

7. The osmotic device of claim 1, wherein the semipermeable wall has a thickness in the range of about 1 to 10 mils and a porosity of about 40 to 70 vol. %.

8. The osmotic device of claim 1, wherein the semipermeable wall has an overcoating containing beneficial agent.

9. The osmotic device of claim 1, wherein the device has a smooth oval shape with an aspect ratio in the range of about 1.2:

1 to about 3;

1, a height of about 0.5 to about 10 mm, and a volume of less than about 2 cm³.

10. The osmotic device of claim 1, wherein the beneficial agent has a low degree of solubility in the aqueous fluid and the compartment also contains an osmagent.

11. The osmotic device of claim 1, wherein the device is substantially free of any gelling agent.

12. The osmotic device of claim 1, wherein the beneficial agent is a member selected from the group consisting of anti-plaque agents, antifungal agents, antiviral agents, antimicrobial agents, antibiotics, non-steroidal anti-inflammatory agents, anti-dental caries agents, saliva-enhancing agents, smoking cessation agents, oral ulcer healing agents and breath fresheners.

13. The osmotic device of claim 12, wherein the beneficial agent comprises an anti-plaque agent selected from the group consisting of clorhexidine digluconate, chlorhexidine dichloride, chlorhexidine diacetate, cetylpyridinium chloride, ethanol, sanguinarine, sanguinarine chloride, sodium salicylate, sodium borate, sodium benzoate, dequalinium chloride, benzalkonium chloride, aminacridine hydrochloride, mepacrine hydrochloride, hydrogen peroxide, potassium peroxidiphosphate, proguanil hydrochloride, dibromopropamidine diisothionate, hexidine, alexidine, octenidine, zinc citrate, thymol, triclosan, mutanases, amylogycosidase, glucose-oxidase, xylitol, mannitol, stannous fluoride, sodium fluoride, decapinol, sodium polyvinylphosphonic acid, perfluoroalkyl surfactants and cetyldimethylbenzyl ammonium chloride.

4. A method for controlled delivery of a beneficial agent into an oral cavity of an animal over an extended delivery period, comprising:

a) placing in the oral cavity of the animal an osmotic device having a size and shape suitable for comfortably retaining the device in the oral cavity for the extended delivery period, the device including a shaped semipermeable wall surrounding a solid dose of a beneficial agent that exhibits at least some degree of solubility in an aqueous fluid present in the oral cavity, a fibrous support material comprising hydrophilic water-insoluble fibers, and a passageway in the semipermeable wall connecting the exterior of the device and the agent for delivering the agent from the device into the oral cavity at a controlled rate over the extended delivery period, the wall being permeable to the passage of the aqueous fluid and substantially impermeable to the passage of the fibrous support material;

b) allowing the aqueous fluid present in the oral cavity to permeate through the semipermeable wall to form a liquid solution of the beneficial agent; and

c) delivering the solution of the beneficial agent into the oral cavity over the extended delivery period.

14. The method of claim 4, wherein the extended delivery period is about 0.5 to 12 hours.

15. The method of claim 4, wherein the extended delivery period is about 1 to 6 hours.

16. The method of claim 4, wherein the extended delivery period is about 1 to 4 hours.

17. The method of claim 4, wherein the beneficial agent is an anti-plaque agent which is administered to suppress the formation of plaque on teeth.

18. The method of claim 17, wherein the anti-plaque agent is selected from the group consisting of clorhexidine digluconate, chlorhexidine dichloride, chlorhexidine diacetate, cetylpyridinium chloride, ethanol, sanguinarine, sanguinarine chloride, sodium salicylate, sodium borate, sodium benzoate, dequalinium chloride, benzalkonium chloride, aminacridine hydrochloride, mepacrine hydrochloride, hydrogen peroxide, potassium peroxidiphosphate, proguanil hydrochloride, dibromopropamidine diisothionate, hexidine, alexidine, octenidine, zinc citrate, thymol, triclosan, mutanases, amylogycosidase, glucose-oxidase, xylitol, mannitol, stannous fluoride, sodium fluoride, decapinol, sodium polyvinylphosphonic acid, perfluoroalkyl surfactants and cetyldimethylbenzyl ammonium chloride.

19. The method of claim 17, wherein the anti-plaque agent comprises cetylpyridinium chloride.