USRE31787EExpiredUtility

Compositions for reducing elution of therapeutic agents from teeth

Priority: Apr 2, 1979Filed: May 7, 1982Granted: Jan 1, 1985
Est. expiryApr 2, 1999(expired)· nominal 20-yr term from priority
A61K 8/29A61K 8/44A61K 8/55A61K 8/58A61K 8/585A61K 8/70A61K 8/81A61K 8/8117A61K 8/8147A61Q 11/00
27
PatentIndex Score
15
Cited by
22
References
12
Claims

Abstract

A dentrifice composition containing a water-dispersible, membrane-forming material which, when applied to tooth surfaces in an oral environment, attaches thereto and forms a substantially continuous, hydrophobic barrier thereon which substantially reduces elution of a previously applied therapeutic agent.

Claims

exact text as granted — not AI-modified
What is claimed is: 
     
       1. A dentifrice composition for substantially effectively coating previously fluoride-treated teeth and thereby reducing elution of said fluoride from said teeth, said composition comprising a fluoride-containing caries prophylactic agent provided that said agent is substantially free from polyvalent metal atoms; and   at least about 0.05% by weight of an anionic water-dispersible membrane-forming material which, when applied to the surface of said previously fluoride-treated teeth in an oral environment, complexes with the calcium of said teeth and forms a substantially continuous hydrophobic barrier thereon which substantially reduces the elution of said previously applied fluoride from said teeth and which, when at equilibrium with the complex, has a formation constant in the range of about 0.5 to 8, said anionic membrane-forming material being a non-polymeric fluorinated material selected from the group   (R.sub.f SO.sub.2 N(R.sup.2)R.sup.3 O).sub.m PX(XB).sub.3-m       (C.sub.g F.sub.2g+1 CH.sub.2 O).sub.k PO(OM).sub.q       R.sub.f COOM       R.sub.f R.sup.3 COOM       R.sub.f SO.sub.2 OM       .Iadd.R.sub.f SO.sub.2 OY .Iaddend.     wherein R f  is a monovalent, stable, inert, fluorinated, saturated aliphatic non-polar radical containing from about 4 to 16 carbon atoms; R 2  is selected from hydrogen and alkyl groups containing from about 2 to 3 carbon atoms; R 3  is selected from alkylene, chloro- substituted alkylene and alkarylene groups that contain from about 1 to 10 carbon atoms; X is selected from oxygen and sulfur; B is selected from hydrogen, alkali metal, ammonium and amine groups, and alkyl, aryl, cycloalkyl, alkaryl, and aralkyl groups each containing up to 20 carbon atoms; M is selected from hydrogen, alkali metal, ammonium and amine groups; .Iadd.Y is an aryl group; .Iaddend.m is 1 or 2; g is an integer of from 1 to 10; k is 1 or 2; and q is 3-k.     
     
     
       2. A dentifrice composition according to claim 1 wherein said membrane-forming material has the formula (R f  SO 2  N(R 2 )R 3  O) m  PX(XB) 3-m . 
     
     
       3. A dentifrice composition according to claim 2 wherein R f  is a fully fluorinated alkyl radical containing eight carbon atoms, R 2  is selected from hydrogen, methyl and ethyl and butyl, and R 3  is ethylene. 
     
     
       4. A dentifrice composition according to claim 3 wherein said membrane-forming material is selected from   (C.sub.8 F.sub.17 SO.sub.2 N(C.sub.2 H.sub.5)C.sub.2 H.sub.4 O).sub.2 PSSH       (C.sub.8 F.sub.17 SO.sub.2 N(C.sub.2 H.sub.5)C.sub.2 H.sub.4 O).sub.2 POOH       .[.C.sub.8 F.sub.17 SO.sub.2 N(C.sub.2 H.sub.5)C.sub.2 H.sub.4 OPO(OH.sub.2).].       .Iadd.C.sub.8 F.sub.17 SO.sub.2 N(C.sub.2 H.sub.5)C.sub.2 H.sub.4 OPO(OH).sub.2 .Iaddend.       C.sub.8 F.sub.17 SO.sub.2 N(C.sub.2 H.sub.5)C.sub.10 H.sub.20 OPO(OH).sub.2       C.sub.8 F.sub.17 SO.sub.2 N(C.sub.2 H.sub.5)C.sub.2 H.sub.4 OP(OH)(O)OC.sub.18 H.sub.37       C.sub.8 F.sub.17 SO.sub.2 N(C.sub.4 H.sub.9)C.sub.2 H.sub.4 OPO(OH).sub.2.     
     
     
       5. A dentifrice composition according to claim 4 wherein said membrane-forming material is   C.sub.8 F.sub.17 SO.sub.2 N(C.sub.2 H.sub.5)C.sub.2 H.sub.4 OPO(OH).sub.2.     
     
     
       6. A dentifrice composition according to claim 1 wherein said membrane-forming material has the formula   R.sub.f COOM.     
     
     
       7. A dentifrice composition according to claim 6 wherein said membrane-forming material is selected from   C.sub.8 F.sub.17 COOH       C.sub.11 F.sub.23 COOH.     
     
     
       8. A dentifrice composition according to claim 1 wherein said membrane-forming material has the formula   R.sub.f R.sup.3 COOM.     
     
     
       9. A dentifrice composition according to claim 8 wherein said membrane-forming material is selected from   C.sub.8 F.sub.17 CH.sub.2 CHCl.sub.8 H.sub.16 COOH       C.sub.8 F.sub.17 C.sub.10 H.sub.20 COOH.     
     
     
       10. A dentifrice composition according to claim 9 wherein said membrane-forming material is   C.sub.8 F.sub.17 C.sub.10 H.sub.20 COOH.     
     
     
       11. A dentifrice composition according to claim 1 wherein said membrane-forming material has the formula R f  SO 2  OM. 
     
     
       12. A dentifrice composition to claim 11 wherein said membrane-forming material is C 8  F 17  SO 2  OK. .Iadd.13. A dentifrice composition according to claim 1 wherein said membrane-forming material has the formula R f  SO 2  OY. .Iaddend. .Iadd.14. A dentifrice composition according to claim 13 wherein said membrane-forming material is selected from ##STR17##.Iaddend.

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