Sustained release of topical anesthetics
View Patent ↗A composition and method to alleviate oral mucosal discomfort and irritation in an orthodontic patient. A wax matrix containing less that 15% analgesic/anesthetic agent such as benzocaine and excipients enhanced and extended release of the analgesic/anesthetic agent compared to known art formulations. The composition exhibited desirable aesthetic properties, was easy to apply, and the relatively lower concentration of active agent provided enhanced safety.
1. A method of alleviating orthodontic discomfort in a patient in need thereof, the method comprising applying a pharmaceutically acceptable composition of a wax, from 0.01% to less than 15% of an analgesic/anesthetic agent, and up to 30% xanthum gum to provide to the patient under conditions to alleviate orthodontic discomfort for at least eight hours and up to 24 hours after the application.
2. A method of alleviating orthodontic discomfort in a patient in need thereof, the method comprising applying a pharmaceutically acceptable composition of wax, glyceryl monostearate, heavy mineral oil, PEG 1500, Tween 80, from 0.01% to less than 15% of an analgesic/anesthetic agent, and up to 30% xanthum gum.
3. A method of alleviating orthodontic discomfort in a patient in need thereof, the method comprising applying a pharmaceutically acceptable composition of 83% microcrystalline wax, 2.7% glyceryl monostearate, 1.0% heavy mineral oil, 5% PEG 1500, 5% analgesic/anesthetic agent, 0.3% Tween 80, and 3% xanthum gum, the composition applied to an oral mucosal surface of the orthodontic patient under conditions to alleviate the orthodontic discomfort.
4. A method of alleviating orthodontic discomfort in a patient in need thereof, the method comprising applying a pharmaceutically acceptable composition of 50%-99% microcrystalline wax, 0%-10% glyceryl monostearate, 0%-30% heavy mineral oil, 0%-30% PEG 1500, 0.01%-14.99% analgesic/anesthetic agent, 0%-10% Tween 80, and 0.1%-30% xanthum gum, the composition applied to an orthodontic bracket or brace of the orthodontic patient under conditions to alleviate orthodontic discomfort.
5. The method of claim 1 , the composition comprising from 50%-99% microcrystalline wax.
6. The method of claim 1 , the composition comprising 83% microcrystalline wax.
7. The method of claim 1 , the composition further comprising up to 10% glyceryl monostearate.
8. The method of claim 1 , the composition further comprising up to 30% heavy mineral oil.
9. The method of claim 1 , the composition further comprising up to 30% PEG 1500.
10. The method of claim 1 , the composition further comprising up to 10% Tween 80.
11. The method of claim 1 , the composition comprising 5% analgesic/anesthetic agent.
12. The method of claim 1 , wherein the analgesic/anesthetic agent is benzocaine.
13. The method of claim 1 , wherein the applying step applies the composition to an orthodontic bracket or brace affixed to at least one tooth of a patient.
14. The method of claim 1 , wherein the applying step applies the composition to an oral mucosal surface in a patient.
15. A extended release pharmaceutically acceptable composition comprising microcrystalline wax, glyceryl monostearate, heavy mineral oil, PEG 1500, Tween 80, less than 15.0% of an analgesic/anesthetic agent, and up to 30% xanthum gum, the composition having an in-vitro release of the analgesic/anesthetic agent of about 28% to about 56% over eight hours.
16. The composition of claim 15 , the composition comprising from 50%-99% microcrystalline wax.
17. The composition of claim 15 , the composition further comprising up to 10% glyceryl monostearate.
18. The composition of claim 15 , the composition further comprising up to 30% heavy mineral oil.
19. The composition of claim 15 , the composition further comprising up to 30% PEG 1500.
20. The composition of claim 15 , the composition further comprising up to 10% Tween 80.
21. The composition of claim 15 , the composition comprising 5% analgesic/anesthetic agent.
22. The composition of claim 15 , wherein the analgesic/anesthetic agent is benzocaine.