Topical glycopyrrolate formulations
View Patent ↗Individually packaged topical formulations comprising about 0.25 to about 6% w/w of glycopyrrolate for the treatment of hyperhidrosis, wherein said wipe is contained within a pouch resistant to leakage. The formulations may further comprise ethanol, a buffering agent and water. In addition, the formulations may further comprise a polymer system comprising a hydrophobic polymer in combination with a hydrophilic polymer.
1. A glycopyrrolate base solution comprising:
about 0.5 to about 4.0% w/w of a glycopyrrolate compound having the following formula:
wherein X − is a pharmaceutically acceptable counter ion salt;
ethanol and water in a weight ratio of about 50:50 to about 60:40; and
a buffering agent, comprising citric acid and a base selected from the group consisting of sodium citrate and tromethamine, said acid and base at a total concentration of about 0.2 to about 0.5% w/w and at an acid:base ratio sufficient to maintain a pH of the glycopyrrolate base solution of about 3.5 to about 6 for at least nine months at 25° C.
2. The glycopyrrolate base solution of claim 1 , wherein the buffering agent maintains a pH of the base solution of 4.0+/−0.5.
3. The glycopyrrolate base solution of claim 1 , wherein the buffering agent maintains a pH of the base solution of about 4.0.
4. The glycopyrrolate base solution of claim 1 , wherein the glycopyrrolate compound degrades by less than 1% when stored at 0 to 25° C. for at least one month, two months, six months or one year.
5. The glycopyrrolate base solution of claim 4 , wherein the glycopyrrolate compound degrades by up to 0.2% when stored at 0 to 25° C. for at least three months.
6. The glycopyrrolate base solution of claim 1 , further comprising propylene glycol.
7. The glycopyrrolate base solution of claim 1 , wherein the base is sodium citrate.
8. The glycopyrrolate base solution of claim 7 , wherein the buffering agent maintains a pH of the base solution of 4.0+/−0.5.
9. The glycopyrrolate base solution of claim 7 , wherein the buffering agent maintains a pH of the base solution of about 4.0.
10. The glycopyrrolate base solution of claim 7 , wherein the buffering agent is about 0.15% citric acid and about 0.06% sodium citrate.
11. The glycopyrrolate base solution of claim 7 , wherein the ethanol to water weight ratio is about 60:40.
12. The glycopyrrolate base solution of claim 10 , wherein the ethanol and water are in a weight ratio of about 60:40.
13. The glycopyrrolate base solution of claim 10 , comprising about 59% ethanol and about 39% water.
14. The glycopyrrolate base solution of claim 1 , wherein the base is tromethamine.
15. The glycopyrrolate base solution of claim 1 , wherein the buffering agent maintains a pH of the base solution of about 4.5.
16. The glycopyrrolate base solution of claim 1 , wherein the ethanol is at about 53.7 to about 57.3% w/w, and the water is added to 100% w/w.
17. The glycopyrrolate base solution of claim 1 , further comprising a polymer system comprising a hydrophobic polymer in combination with a hydrophilic polymer.
18. The glycopyrrolate base solution of claim 17 , wherein the polymer system comprises a polyvinyl pyrrolidone and a butyl ester of polyvinylmethylether/maleic anhydride copolymer.
19. The glycopyrrolate base solution of claim 1 , wherein the ethanol and water are in a weight ratio of about 60:40.
20. An individually packaged wipe for the treatment of hyperhidrosis comprising a wipe loaded with the glycopyrrolate base solution of claim 1 contained within a pouch resistant to leakage.
21. The individually packaged wipe of claim 20 , wherein the wipe is selected from the group consisting of nonwoven material, paper material, woven material, knitted material, tufted material, stitched-bonded material, and material felted by wet-milling material.
22. A method for alleviating hyperhidrosis in a mammal comprising the topical administration of the wipe of claim 20 , following removal from the pouch, to an area of the body such that the hyperhidrosis is reduced.
23. An individually packaged wipe for the treatment of hyperhidrosis comprising a wipe loaded with the glycopyrrolate base solution of claim 13 contained within a pouch resistant to leakage.
24. The individually packaged wipe of claim 23 , wherein the wipe is selected from the group consisting of nonwoven material, paper material, woven material, knitted material, tufted material, stitched-bonded material, and material felted by wet-milling material.
25. A method for alleviating hyperhidrosis in a mammal comprising the topical administration of the wipe of claim 23 , following removal from the pouch, to an area of the body such that the hyperhidrosis is reduced.
26. An individually packaged wipe for the treatment of hyperhidrosis comprising a wipe loaded with the glycopyrrolate base solution of claim 16 contained within a pouch resistant to leakage.
27. The individually packaged wipe of claim 26 , wherein the wipe is selected from the group consisting of nonwoven material, paper material, woven material, knitted material, tufted material, stitched-bonded material, and material felted by wet-milling material.
28. A method for alleviating hyperhidrosis in a mammal comprising the topical administration of the wipe of claim 26 , following removal from the pouch, to an area of the body such that the hyperhidrosis is substantially reduced.
29. A glycopyrrolate base solution, consisting essentially of
about 0.5 to about 4.0% w/w of a glycopyrrolate compound having the following formula:
wherein X − is a pharmaceutically acceptable counter ion salt;
ethanol and water in a weight ratio of about 50:50 to about 60:40; and
a buffering agent, comprising citric acid and a base selected from the group consisting of sodium citrate and tromethamine, said acid and base at a total concentration of about 0.2 to about 0.5% w/w and at an acid:base ratio sufficient to maintain a pH of the glycopyrrolate base solution of about 3.5 to about 6 for at least nine months at 25° C.