Dosage form for insertion into the mouth
Oral dosage forms and methods for delivering effective amounts of erectile dysfunction medicaments to patients to provide rapid uptake of said agents through the mucosa of the oral cavity are disclosed.
1. A fast onset pharmaceutical composition comprising:
a water soluble matrix comprising an effective amount of a pharmaceutically active agent selected from the group consisting of sildenafil, tadalafil, vardenafil and their pharmacologically acceptable salts and an absorption enhancer having an HLB of about 8 to about 16,
wherein the matrix is a film and the absorption enhancer is one or more sucrose fatty acid esters.
2. The pharmaceutical composition of claim 1 , further comprising a nonionic surfactant wherein the combined nonionic surfactant and sucrose fatty acid ester have a combined HLB of about 8 to about 17.
3. The pharmaceutical composition of claim 2 , wherein the nonionic surfactant is at least one or more of polysorbate and sorbitan fatty acid ester.
4. The pharmaceutical composition of claim 2 , further comprising a secondary absorption enhancer selected from the group consisting of glycerol, ginger oil, cineole and terpenes.
5. The pharmaceutical composition of claim 3 , wherein the polysorbate is selected from the group consisting of polyoxyethylene (20) sorbitan monolaurate, polyoxyethylene (20) sorbitan monopalmitate, polyoxyethylene (20) sorbitan and Polyoxyethylene (20) sorbitan monooleate.
6. The pharmaceutical composition of claim 3 , wherein the sorbitan fatty acid ester is selected from the group consisting of sorbitan monolaurate, sorbitan monopalmitate, sorbitan monostearate, sorbitan tristearate and sorbitan monooleate.
7. The pharmaceutical composition of claim 1 , further comprising a film forming agent selected from pullulan or a polymeric mixture of polyvinyl pyrrolidone and a polymeric alginate.
8. The pharmaceutical composition of claim 1 , wherein the pharmaceutical composition dissolves in the oral cavity in about 0.25 minutes to about 15 minutes.
9. The pharmaceutical composition of claim 7 , wherein the film forming agent is pullulan.
10. The pharmaceutical composition of claim 7 , wherein the ratio of polyvinyl pyrrolidone to polymeric alginate in the polymeric mixture is from about 5:1 to about 1:3.
11. The pharmaceutical composition of claim 1 , wherein the sucrose fatty acid esters are sucrose fatty acid esters having a monomer content of from about 20 percent to about 80 percent.
12. The pharmaceutical composition of claim 1 , wherein the sucrose fatty acid esters are selected from the group consisting of sucrose stearate, sucrose palmitate, sucrose laurate, sucrose behenate, sucrose oleate and sucrose erucate.
13. The pharmaceutical composition of claim 7 , wherein the polymeric mixture contains, from about 5% to about 95% by weight of polyvinyl pyrrolidone and from about 5% to about 95% by weight of an polymeric alginate, both of said weights being based on the weight of said polymeric mixture.
14. The pharmaceutical composition of claim 1 , further comprising a polymeric mixture of polyvinyl pyrrolidone and a polymeric alginate.
15. The pharmaceutical composition of claim 1 , wherein the film when placed in the oral cavity will dissolve in about 0.25 minutes to about 15 minutes.
16. The pharmaceutical composition of claim 1 , wherein said film contains one or more absorption enhancers in an amount of from about 0.1% by weight to about 20% by weight of the film.
17. The pharmaceutical composition of claim 1 , wherein said film contains one or more absorption enhancers in an amount of from about 0.1% by weight to about 15% by weight of the film.
18. The pharmaceutical composition of claim 7 , wherein the polymeric mixture contains from about 5% to about 95% by weight of polyvinyl pyrrolidone and from about 5% to about 95% by weight of an polymeric alginate, both of said weights being based on the weight of said polymeric mixture.
19. The pharmaceutical composition of claim 1 , wherein said matrix contains an absorption enhancer in a total amount of from about 0.1% by weight to about 20% by weight by weight of the matrix.
20. The pharmaceutical composition of claim 1 , wherein said sucrose fatty acid ester is a C 12 to C 20 saturated fatty acid ester of sucrose.
21. The pharmaceutical composition of claim 1 , wherein said sucrose fatty acid ester is a sucrose stearate.
22. The pharmaceutical composition of claim 1 , wherein the erectile dysfunction medicament is sildenafil or its pharmaceutically acceptable salts.
23. The pharmaceutical composition of claim 1 , wherein the erectile dysfunction medicament is tadalafil or its pharmaceutically acceptable salts.
24. The pharmaceutical composition of claim 1 , wherein the erectile dysfunction medicament is varenafil or its pharmaceutically acceptable salts.
25. A method for mitigating erectile dysfunction in a patient comprising administering the oral unit dosage form as a water soluble matrix to the oral mucosal membranes of the mouth of a patient, which matrix contains, dispersed therein, a pharmaceutical agent selected from the group consisting of sildenafil, tadalafil, varenafil or pharmaceutically acceptable salts thereof, said pharmaceutical agent being present in said matrix in an amount effective for combating said erectile dysfunction, said matrix composed of a one or more sucrose fatty acid esters having an HLB of about 8 to 16.
26. The method of claim 25 , further comprising a polymeric mixture of polyvinyl pyrrolidone and a polymeric alginate.
27. The method of claim 26 , wherein the ratio of polyvinyl pyrrolidone to polymeric alginate in the polymeric mixture is from about 5:1 to about 1:3.
28. The method of claim 26 , wherein the polymeric mixture contains, from about 5% to about 95% by weight of polyvinyl pyrrolidone and from about 5% to about 95% by weight of an polymeric alginate, both of said weights being based on the weight of said polymeric mixture.
29. The method of claim 25 , wherein said matrix is placed under the tongue of said patient.
30. The method of claim 25 , wherein said matrix is inserted on the buccal tissue of the mouth of the patient.
31. The method of claim 25 , wherein the sucrose fatty acid ester has a monomer content of from about 20 percent to about 80 percent.
32. The method of claim 25 , wherein the sucrose fatty acid esters are selected from the group consisting of sucrose stearate, sucrose palmitate, sucrose laurate, sucrose behenate, sucrose oleate and sucrose erucate.
33. The method of claim 25 , wherein said fatty acid esters are present in an amount of from about 1% to about 20% based upon the weight of the film.
34. The method of claim 25 , further comprising a nonionic surfactant wherein the combined nonionic surfactant and sucrose fatty acid ester have a combined HLB of about 8 to about 17.
35. The method of claim 25 , further comprising a secondary absorption enhancer selected from the group consisting of glycerol, tween, span, ginger oil, cineole and terpenes.
36. The method of claim 25 , wherein the matrix is a film.
37. The method of claim 25 , further comprising pullulan as a film forming agent.
38. The method of claim 25 , wherein the active agent is released over a period of time from about 0.25 minutes to about 15 minutes.