Method for alleviating keratoconjunctivitis sicca
Improved methods and compositions are disclosed for treating dry eye by administering intranasally a therapeutically effective amount of a capsaicinoid compound embedded in multiple layers of solid lamellar crystals of monoglycerides to patients with deficient tear production. The lipophilic capsaicinoid drug is embedded in multiple layers of solid lamellar crystals of monoglycerides, and these crystals are incorporated into pharmaceutically acceptable vehicles comprised of solutions, suspensions, foams, creams, ointments, and gels. The resulting formulations of the capsaicinoid are more stable, less irritating to skin and mucous membranes, and provide increased and more controlled release of the capsaicinoid compound.
1. A method of treating keratoconjunctivitis sicca comprising:
intranasally administering to the nasal mucosa an effective amount of a composition comprising a capsaicinoid compound embedded in lamellar crystals of a monoglyceride and in a vehicle suitable for intranasal administration;
wherein the capsaicinoid compound is present in the composition in a range of about 0.001% by weight to about 1% by weight,
wherein the composition does not cause nasal irritation.
2. The method of claim 1 , wherein said capsaicinoid compound is selected from the group consisting of capsaicin, civamide, acetylated derivatives of capsaicin and civamide, and pharmaceutically acceptable salts of the above.
3. The method of claim 1 , wherein the capsaicinoid compound is present in the composition in a range of about 0.01% by weight to about 0.50% by weight.
4. The method of claim 2 , wherein the capsaicinoid compound is present in the composition in a range of about 0.01% by weight to about 0.50% by weight.
5. The method of claim 1 , wherein the vehicle is selected from the group consisting of solutions, suspensions, creams, ointments, gels and foams.
6. The method of claim 1 , wherein the monoglyceride comprises a fatty acid with a 4 to 28 carbon atom chain.
7. The method of claim 1 , wherein the monoglyceride has a melting point of about 25° C. to about 65° C.
8. The method of claim 1 , wherein the composition comprises two or more monoglycerides.
9. The method of claim 1 , wherein the monoglyceride is selected from the group consisting of: 1-glyceryl monolaurate, 1-glyceryl monomyristate, and combinations thereof.
10. The method of claim 6 , wherein the fatty acid is a saturated fatty acid.