Claims for Patent: 6,706,276

Summary for Patent: 6,706,276

Title:	Compositions and methods for trapping and inactivating pathogenic microbes and spermatozoa
Abstract:	Antimicrobial and contraceptive compositions and methods which prevent and/or reduce the risk of transmission of sexually transmitted diseases through sexual activity as well as prevent and/or reduce the risk of pregnancy are provided. The compositions contain (1) a matrix-forming agent, (2) a bio-adhesive agent, (3) a buffering agent, (4) optionally a humectant, (5) optionally a preservative, and (6) water; wherein the composition is suitable for application within the vagina; wherein the compositions forms a semisolid matrix on contact with ejaculate (thereby trapping ejaculated microbes and spermatozoa); wherein the composition causes hardening of cervical mucus (thereby decreasing the probability of sperm entry); wherein the composition forms a bio-adhesive layer over vaginal surfaces (thereby preventing or reducing the risk of contact of STD-causing microbes with the vaginal surfaces); wherein the composition maintains an acidic vaginal pH of less than about 5 in the presence of semen ejaculated from the male; and wherein the composition does not significantly impair the natural microbiological balance within the vagina. The antimicrobial and contraceptive compositions may also contain additional antimicrobial and/or contraceptive agents (e.g., nonoxynol-9, octoxynol-9, benzalkonium chloride, phosphorylated hesperidins, sulfonated hesperidins, polystyrene sulfonates, substituted benzenesulfonic acid formaldehyde co-polymers, H.sub.2 SO.sub.4 -modified mandelic acids, povidone iodine, itraconazole, ketoconazole, metronidazole, clotrimazole, fluconazole, teraconazole, miconazole, tinidazole, iconazole, chloramphenicol, nystatin, cyclopiroxolamine, and the like).
Inventor(s):	Garg; Sanjay (Punjab, IN), Zaneveld; Lourens Jan Dirk (Chicago, IL), Anderson, Jr.; Robert Anthony (Chicago, IL), Waller; Donald Paul (Oak Brook, IL)
Assignee:	Rush-Presbyterian-St. Luke's Medical Center (Chicago, IL)
Application Number:	09/800,036
Patent Claims:	1. An antimicrobial and contraceptive composition that reduces the risk of transmission of, or infection by, a sexually transmitted disease through sexual activity involving a vagina of a female and a penis of a male, said composition comprising (1) about 1 to about 10 percent of a matrix-forming agent selected from the group consisting of alginic acid, chitosan, gellan gum, and poloxamer, (2) about 1 to about 10 percent of a bio-adhesive agent selected from the group consisting of xanthan gum, hydroxypropyl cellulose, hydroxypropyl methyl cellulose, sodium carboxymethyl cellulose, chitosan, polycarbophil, and a crosslinked polyacrylic acid, (3) about 1 to about 10 percent of a buffering agent selected from the group consisting of lactic acid, citric acid, potassium acid tartrate, benzoic acid, alginic acid, sorbic acid, fumaric acid, ascorbic acid, stearic acid, oleic acid, tartaric acid, edetic acid, and malic acid, and (4) water; wherein the composition is suitable for application within the vagina; wherein the composition forms a semisolid matrix on contact with semen; wherein the composition causes hardening of cervical mucus; wherein the composition forms a bio-adhesive layer over vaginal surfaces; wherein the composition maintains an acidic vaginal pH of less than about 5 in the presence of semen ejaculated from the male; wherein the composition is hypertonic: and wherein the composition is antimicrobial and contraceptive without addition of antimicrobial or contraceptive agents. 2. The composition as defined in claim 1, wherein the composition further comprises a humectant and a preservative. 3. The composition as defined in claim 1, wherein the composition further comprises an antimicrobial or contraceptive agent. 4. The composition as defined in claim 2, wherein the composition further comprises an antimicrobial or contraceptive agent. 5. The composition as defined in claim 1, wherein the composition maintains the acidic vaginal pH in the range of about 3.5 to about 4.5; and wherein the composition does not significantly impair the natural microbiological balance within the vagina. 6. The composition as defined in claim 2, wherein the composition contains about 3 to about 5 percent of the matrix-forming agent, about 2.5 to about 6 percent of the bio-adhesive agent, about 1 to about 7 percent of the buffering agent, about 6 to about 10 percent of the humectant, and about 0.1 to about 1 percent of the preservative; wherein the composition maintains the acidic vaginal pH in the range of about 3.5 to about 4.5; and wherein the composition does not significantly impair the natural microbiological balance within the vagina. 7. The composition as defined in claim 4, wherein the composition contains about 3 to about 5 percent of the matrix-forming agent, about 2.5 to about 6 percent of the bio-adhesive agent, about 1 to about 7 percent of the buffering agent, about 6 to about 10 percent of the humectant, about 0.1 to about 1 percent of the preservative, and about 0.2 to about 5 percent of the antimicrobial or contraceptive agent; wherein the composition maintains the acidic vaginal pH in the range of about 3.5 to about 4.5; and wherein the composition does not significantly impair the natural microbiological balance within the vagina. 8. The composition as defined in claim 2, wherein the humectant is selected from the group consisting of glycerol, polyethylene glycols, propylene glycols, sorbitol, and triacetin; and wherein the preservative is selected from the group consisting of benzoic acid, sodium benzoate, methylparaben, ethylparaben, butylparaben, propylparaben, benyalkonium chloride, phenylmercuric nitrate, and chlorhexidine. 9. The composition as defined in claim 4, wherein the humectant is selected from the group consisting of glycerol, polyethylene glycols, propylene glycols, sorbitol, and triacetin; wherein the preservative is selected from the group consisting of benzoic acid, sodium benzoate, methylparaben, ethylparaben, butylparaben, propylparaben, benyalkonium chloride, phenylmercuric nitrate, and chlorhexidine; and wherein the antimicrobial or contraceptive agent is selected from the group consisting of nonoxynol-9, octoxynol-9, benzalkonium chloride, phosphorylated hesperidins, sulfonated hesperidins, polystyrene sulfonates, substituted benzenesulfonic acid formaldehyde co-polymers, H.sub.2 SO.sub.4 -modified mandelic acids, povidone iodine, itraconazole, ketoconazole, metronidazole, clotrimazole, fluconazole, teraconazole, miconazole, tinidazole, iconazole, chloramphenicol, nystatin, and cyclopiroxolamine. 10. The composition as defined in claim 4, wherein the matrix-forming agent is alginic acid; wherein the bio-adhesive agent is xanthan gum or hydroxypropyl cellulose; wherein the buffering agent is selected from the group consisting of lactic acid, citric acid, and potassium acid tartrate; wherein the humectant is selected from the group consisting of glycerol, polyethylene glycols, propylene glycols, sorbitol, and triacetin; wherein the preservative is selected from the group consisting of benzoic acid and sodium benzoate; and wherein the antimicrobial or contraceptive agent is selected from the group consisting of nonoxynol-9, octoxynol-9, benzalkonium chloride, phosphorylated hesperidins, sulfonated hesperidins, polystyrene sulfonates, substituted benzenesulfonic acid formaldehyde co-polymers, and H.sub.2 SO.sub.4 -modified mandelic acids. 11. A method of reducing the risk of transmission and infection by a sexually transmitted disease through sexual activity involving a vagina of a female and a penis of a male, said method comprising administering an effective amount of an antimicrobial and contraceptive composition within the vagina prior to, or shortly after, sexual activity; wherein the composition comprises (1) about 1 to about 10 percent of a matrix-forming agent selected from the group consisting of alginic acid, chitosan, gellan gum, and poloxamer, (2) about 1 to about 10 percent of a bio-adhesive agent selected from the group consisting of xanthan gum, hydroxypropyl cellulose, hydroxypropyl methyl cellulose, sodium carboxymethyl cellulose, chitosan, polycarbophil, and a crosslinked polyacrylic acid, (3) about 1 to about 10 percent of a buffering agent selected from the group consisting of lactic acid, citric acid, potassium acid tartrate, benzoic acid, alginic acid, sorbic acid, fumaric acid, ascorbic acid, stearic acid, oleic acid, tartaric acid, edetic acid, and malic acid, and (4) water; wherein the composition is suitable for application within the vagina; wherein the composition forms a semisolid matrix on contact with semen; wherein the composition causes the hardening of cervical mucus; wherein the composition forms a bio-adhesive layer over vaginal surfaces; wherein the composition maintains an acidic vaginal pH of less than about 5 in the presence of semen ejaculated from the male; wherein the composition is hypertonic; and wherein the composition is antimicrobial and contraceptive without addition of antimicrobial or contraceptive agents. 12. The method as defined in claim 11, wherein the composition further comprises a humectant and a preservative. 13. The method as defined in claim 11, wherein the composition further comprises an antimicrobial or contraceptive agent. 14. The method as defined in claim 12, wherein the composition further comprises an antimicrobial or contraceptive agent. 15. The method as defined in claim 11, wherein the composition maintains the acidic vaginal pH in the range of about 3.5 to about 4.5; and wherein the composition does not significantly impair the natural microbiological balance within the vagina. 16. The method as defined in claim 12, wherein the composition contains about 3 to about 5 percent of the matrix-forming agent, about 2.5 to about 6 percent of the bio-adhesive agent, about 1 to about 7 percent of the buffering agent, about 6 to about 10 percent of the humectant, and about 0.1 to about 1 percent of the preservative; wherein the composition maintains the acidic vaginal pH in the range of about 3.5 to about 4.5; and wherein the composition does not significantly impair the natural microbiological balance within the vagina. 17. The method as defined in claim 14, wherein the composition contains about 3 to about 5 percent of the matrix-forming agent, about 2.5 to about 6 percent of the bio-adhesive agent, about 1 to about 7 percent of the buffering agent, about 6 to about 10 percent of the humectant, about 0.1 to about 1 percent of the preservative, and about 0.2 to about 5 percent of the antimicrobial or contraceptive agent; wherein the composition maintains the acidic vaginal pH in the range of about 3.5 to about 4.5; and wherein the composition does not significantly impair the natural microbiological balance within the vagina. 18. The method as defined in claim 12, wherein the humectant is selected from the group consisting of glycerol, polyethylene glycols, propylene glycols, sorbitol, and triacetin; and wherein the preservative is selected from the group consisting of benzoic acid, sodium benzoate, methylparaben, ethylparaben, butylparaben, propylparaben, benyalkonium chloride, phenylmercuric nitrate, and chlorhexidine. 19. The method as defined in claim 14, wherein the humectant is selected from the group consisting of glycerol, polyethylene glycols, propylene glycols, sorbitol, and triacetin; wherein the preservative is selected from the group consisting of benzoic acid, sodium benzoate, methylparaben, ethylparaben, butylparaben, propylparaben, benyalkonium chloride, phenylmercuric nitrate, and chlorhexidine; and wherein the antimicrobial or contraceptive agent is selected from the group consisting of nonoxynol-9, octoxynol-9, benzalkonium chloride, phosphorylated hesperidins, sulfonated hesperidins, polystyrene sulfonates, substituted benzenesulfonic acid formaldehyde co-polymers, H.sub.2 SO.sub.4 -modified mandelic acids, itraconazole, ketoconazole, and metronidazole. 20. The method as defined in claim 12, wherein the matrix-forming agent is alginic acid; wherein the bio-adhesive agent is xanthan gum or hydroxypropyl cellulose; wherein the buffering agent is selected from the group consisting of lactic acid, citric acid, and potassium acid tartrate; wherein the humectant is selected from the group consisting of glycerol, polyethylene glycols, propylene glycols, sorbitol, and triacetin; wherein the preservative is selected from the group consisting of benzoic acid and sodium benzoate; and wherein the antimicrobial or contraceptive agent is selected from the group consisting of nonoxynol-9, octoxynol-9, benzalkonium chloride, phosphorylated hesperidins, sulfonated hesperidins, polystyrene sulfonates, substituted benzenesulfonic acid formaldehyde co-polymers, and H.sub.2 SO.sub.4 -modified mandelic acids. 21. An antimicrobial and contraceptive composition for reducing the risk of transmission and infection by a sexually transmitted disease through sexual activity, said composition comprising (1) about 1 to about 10 percent of a matrix-forming agent selected from the group consisting of alginic acid, chitosan, gellan gum, and poloxamer, (2) about 1 to about 10 percent of a bio-adhesive agent selected from the group consisting of xanthan gum, hydroxypropyl cellulose, hydroxypropyl methyl cellulose, sodium carboxymethyl cellulose, chitosan, polycarbophil, and a crosslinked polyacrylic acid, (3) about 1 to about 10 percent of a buffering agent selected from the group consisting of lactic acid, citric acid, potassium acid tartrate, benzoic acid, alginic acid, sorbic acid, fumaric acid, ascorbic acid, stearic acid, oleic acid, tartaric acid, edetic acid, and malic acid, (4) 0 to about 2 percent of a humectant, (5) 0 to about 2 percent of a preservative, (6) 0 to about 10 percent of an antimicrobial or contraceptive agent, and (7) water; wherein the composition is suitable for application within a vagina; wherein the composition forms a semisolid matrix on contact with semen ejaculated from a male into the vagina; wherein the composition causes hardening of cervical mucus of the vagina; wherein the composition forms a bio-adhesive layer over vaginal surfaces; wherein the composition maintains an acidic vaginal pH of less than about 5 in the presence of semen ejaculated from the male; wherein the composition is hypertonic; and wherein the composition is antimicrobial and contraceptive without addition of antimicrobial or contraceptive agents. 22. The composition as defined in claim 21, wherein the composition contains about 3 to about 5 percent of the matrix-forming agent, about 2.5 to about 6 percent of the bio-adhesive agent, about 1 to about 7 percent of the buffering agent, about 6 to about 10 percent of the humectant, and about 0.1 to about 1 percent of the preservative; wherein the composition maintains the acidic vaginal pH in the range of about 3.5 to about 4.5; and wherein the composition does not significantly impair the natural microbiological balance within the vagina. 23. The composition as defined in claim 21, wherein the matrix-forming agent is alginic acid; wherein the bio-adhesive agent is xanthan gum or hydroxypropyl cellulose; wherein the buffering agent is selected from the group consisting of lactic acid, citric acid, and potassium acid tartrate; wherein the humectant, if present, is selected from the group consisting of glycerol, polyethylene glycols, propylene glycols, sorbitol, and triacetin; wherein the preservative, if present, is selected from the group consisting of benzoic acid and sodium benzoate; and wherein the antimicrobial or contraceptive agent, if present, is selected from the group consisting of nonoxynol-9, octoxynol-9, benzalkonium chloride, phosphorylated hesperidins, sulfonated hesperidins, polystyrene sulfonates, substituted benzenesulfonic acid formaldehyde co-polymers, and H.sub.2 SO.sub.4 -modified mandelic acids. 24. The composition as defined in claim 22, wherein the matrix-forming agent is alginic acid; wherein the bio-adhesive agent is xanthan gum or hydroxypropyl cellulose; wherein the buffering agent is selected from the group consisting of lactic acid, citric acid, and potassium acid tartrate; wherein the humectant is selected from the group consisting of glycerol, polyethylene glycols, propylene glycols, sorbitol, and triacetin; wherein the preservative is selected from the group consisting of benzoic acid and sodium benzoate; and wherein the antimicrobial or contraceptive agent is selected from the group consisting of nonoxynol-9, octoxynol-9, benzalkonium chloride, phosphorylated hesperidins, sulfonated hesperidins, polystyrene sulfonates, substituted benzenesulfonic acid formaldehyde co-polymers, and H.sub.2 SO.sub.4 -modified mandelic acids. 25. A solid composition that reduces the risk of transmission of, or infection by, a sexually transmitted disease through sexual activity involving a vagina of a female and a penis of a male, said solid composition comprising (1) a matrix-forming agent selected from the group consisting of alginic acid, chitosan, gellan gum, and poloxamer, (2) a bio-adhesive agent selected from the group consisting of xanthan gum, hydroxypropyl cellulose, hydroxypropyl methyl cellulose, sodium carboxymethyl cellulose, chitosan, polycarbophil, and a crosslinked polyacrylic acid, and (3) a buffering agent selected from the group consisting of lactic acid, citric acid, potassium acid tartrate, benzoic acid, alginic acid, sorbic acid, fumaric acid, ascorbic acid, stearic acid, oleic acid, tartaric acid, edetic acid, and malic acid; wherein the solid composition is suitable for application within the vagina; wherein the solid composition is readily dispersable in aqueous based medium either outside or inside the vagina to form a dispersed composition; wherein the solid composition contains sufficient matrix-forming agent, bio-adhesive agent, and buffering agent to provide the dispersed composition containing about 1 to about 10 percent of the matrix-forming agent, about 1 to about 10 percent of the bio-adhesive agent, and about 1 to about 10 percent of the buffering agent within the vagina; wherein the dispersed composition forms a semisolid matrix on contact with semen; wherein the dispersed composition causes hardening of cervical mucus; wherein the dispersed composition forms a bio-adhesive layer over vaginal surfaces; wherein the dispersed composition maintains an acidic vaginal pH of less than about 5 in the presence of semen ejaculated from the male; wherein the dispersed composition is hypertonic; and wherein the dispersed composition is antimicrobial and contraceptive without addition of antimicrobial or contraceptive agents. 26. The solid composition as defined in claim 25, wherein the solid composition further comprises a humectant and a preservative. 27. The solid composition as defined in claim 25, wherein the solid composition further comprises an antimicrobial or contraceptive agent. 28. The solid composition as defined in claim 26, wherein the solid composition further comprises an antimicrobial or contraceptive agent. 29. The solid composition as defined in claim 25, wherein the dispersed composition maintains the acidic vaginal pH in the range of about 3.5 to about 4.5; and wherein the dispersed composition does not significantly impair the natural microbiological balance within the vagina. 30. The solid composition as defined in claim 26, wherein the solid composition contains sufficient matrix-forming agent, bio-adhesive agent, and buffering agent to provide the dispersed composition containing about 3 to about 5 percent of the matrix-forming agent, about 2.5 to about 6 percent of the bio-adhesive agent, about 1 to about 7 percent of the buffering agent, about 6 to about 10 percent of the humectant, and about 0.1 to about 1 percent of the preservative within the vagina; wherein the dispersed composition maintains the acidic vaginal pH in the range of about 3.5 to about 4.5; and wherein the dispersed composition does not significantly impair the natural microbiological balance within the vagina. 31. The solid composition as defined in claim 28, wherein the solid composition contains sufficient matrix-forming agent, bio-adhesive agent, and buffering agent to provide the dispersed composition containing about 3 to about 5 percent of the matrix-forming agent, about 2.5 to about 6 percent of the bio-adhesive agent, about 1 to about 7 percent of the buffering agent, about 6 to about 10 percent of the humectant, about 0.1 to about 1 percent of the preservative, and about 0.2 to about 5 percent of the antimicrobial or contraceptive agent within the vagina; wherein the dispersed composition maintains the acidic vaginal pH in the range of about 3.5 to about 4.5; and wherein the dispersed composition does not significantly impair the natural microbiological balance within the vagina. 32. The composition as defined in claim 26, wherein the humectant is selected from the group consisting of glycerol, polyethylene glycols, propylene glycols, sorbitol, and triacetin; and wherein the preservative is selected from the group consisting of benzoic acid, sodium benzoate, methylparaben, ethylparaben, butylparaben, propylparaben, benyalkonium chloride, phenylmercuric nitrate, and chlorhexidine. 33. The solid composition as defined in claim 28, wherein the humectant is selected from the group consisting of glycerol, polyethylene glycols, propylene glycols, sorbitol, and triacetin; wherein the preservative is selected from the group consisting of benzoic acid, sodium benzoate, methylparaben, ethylparaben, butylparaben, propylparaben, benyalkonium chloride, phenylmercuric nitrate, and chlorhexidine; and wherein the antimicrobial or contraceptive agent is selected from the group consisting of nonoxynol-9, octoxynol-9, benzalkonium chloride, phosphorylated hesperidins, sulfonated hesperidins, polystyrene sulfonates, substituted benzenesulfonic acid formaldehyde co-polymers, H.sub.2 SO.sub.4 -modified mandelic acids, povidone iodine, itraconazole, ketoconazole, metronidazole, clotrimazole, fluconazole, teraconazole, miconazole, tinidazole, iconazole, chloramphenicol, nystatin, and cyclopiroxolamine. 34. The solid composition as defined in claim 28, wherein the matrix-forming agent is alginic acid; wherein the bio-adhesive agent is xanthan gum or hydroxypropyl cellulose; wherein the buffering agent is selected from the group consisting of lactic acid, citric acid, and potassium acid tartrate; wherein the humectant is selected from the group consisting of glycerol, polyethylene glycols, propylene glycols, sorbitol, and triacetin; wherein the preservative is selected from the group consisting of benzoic acid and sodium benzoate; and wherein the antimicrobial or contraceptive agent is selected from the group consisting of nonoxynol-9, octoxynol-9, benzalkonium chloride, phosphorylated hesperidins, sulfonated hesperidins, polystyrene sulfonates, substituted benzenesulfonic acid formaldehyde co-polymers, and H.sub.2 SO.sub.4 -modified mandelic acids. 35. The solid composition as defined in claim 25, wherein the solid composition is in the form of a tablet which can be inserted into the vagina. 36. The solid composition as defined in claim 31, wherein the solid composition is in the form of a tablet which can be inserted into the vagina.