Sustained release of active agents from bioadhesive microcapsules

• US 5,077,051 A
• Filed: 04/10/1990
• Issued: 12/31/1991
• Est. Priority Date: 04/10/1990
• Status: Expired due to Fees

• Current Assignee: Warner-Lambert Company (Pfizer Inc.)
• Original Assignee: Warner-Lambert Company (Pfizer Inc.)
• Inventors: Gallopo, Andrew R., Dills, Steven S.
• Primary Examiner(s): Page, Thurman K.
• Assistant Examiner(s): BENSTON JR, WILLIAM E
• Application Number:
  US07/508,216
• Time in Patent Office: 630 Days
• Field of Search: 424/485, 424/489, 424/435, 424/76.3, 424/497
• US Class Current: 424/435
• CPC Class Codes: A61K 2800/412 Microsized, i.e. having sizes between 0.1 and 100 microns
• CPC Class Codes: A61K 2800/52 Stabilizers
• CPC Class Codes: A61K 8/11 Encapsulated compositions
• CPC Class Codes: A61K 9/006 Oral mucosa, e.g. mucoadhesive forms, sublingual droplets; Buccal patches or films; Buccal sprays
• CPC Class Codes: A61K 9/1652 Polysaccharides, e.g. alginate, cellulose derivatives; Cyclodextrin homeopathic globules A61K9/1623
• CPC Class Codes: A61K 9/1658 Proteins, e.g. albumin, gelatin
• CPC Class Codes: A61K 9/5015 Organic compounds, e.g. fats, sugars
• CPC Class Codes: A61P 1/02 Stomatological preparations, e.g. drugs for caries, aphtae, periodontitis
• 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

Bioadhesives microcapsules capable of sustained release comprise xanthan gum, locust bean gum, a bulking agent and an active agent. The microcapsules are particularly useful for delivering buffering agents to the oral cavity for anticaries purposes.

Claims

1. A composition of matter comprising bioadhesive microcapsules said microcapsules, being bioadhesive to the oral cavity and having anti-caries activity and consisting essentially of on a solid weight basis 1) about 1% or greater of a mixture of approximately equal amounts of xanthan gum and locust bean gum, 2) at least about 4% of a substantially water-soluble bulking agent selected from the group consisting of gelatin, hydrocolloids, glycerin, methylcellulose, polyvinylpyrrolidone, sodium carboxymethylcellulose, whey solids, and mixtures thereof, and 3) about 4.5% or greater of an active buffering agent selected from the group consisting of potassium phosphate dibasic, calcium carbonate, sodium potassium dibasic, sodium bicarbonate, ammonium bicarbonate, potassium carbonate, magnesium carbonate, calcium phosphate tribasic, sodium sesquicarbonate, ammonium carbonate, tetrasodium pyrophosphate, calcium hydroxide, sodium hydroxide, potassium hydroxide and mixtures thereof.

2. The composition of claim 1, wherein said bulking agent comprises gelatin.

3. The composition of claim 1, wherein said buffering agent comprises potassium phosphate dibasic.

4. The composition of claim 1, wherein said buffering agent comprises calcium carbonate.

5. The composition of claim 1, wherein said buffering agent comprises potassium phosphate dibasic and calcium carbonate.

6. The composition of claim 1, wherein said microcapsules are coated with a wax selected from the group consisting of animal waxes, vegetable waxes, mineral waxes, synthetic waxes and mixtures thereof.

7. The composition of claim 6, wherein said wax comprises carnauba wax.

8. The composition of claim 6, wherein said wax coating includes calcium carbonate.

9. The composition of claim 1, wherein said bioadhesive microcapsules are incorporated into a delivery system.

10. The composition of claim 9, wherein said delivery system comprises a gel.

11. The composition of claim 9, wherein said delivery system comprises a center-filled chewing gum.

12. The composition of claim 9, wherein said delivery system comprises a pressed mint.