Lipolytic methods
Compositions, formulations, methods, and systems for treating regional fat deposits comprise contacting a targeted fat deposit with a composition comprising long acting beta-2 adrenergic receptor agonist and a compound that reduces desensitization of the target tissue to the long acting beta-2 adrenergic receptor agonist, for example, glucocorticosteroids and/or ketotifen. Embodiments of the composition are administered, for example, by injection, and/or transdermally.
1. A method of treating adipose tissue, subcutaneous fat stores, regional fat accumulation or deposits, uneven fat accumulation in the abdomen in a patient, or cellulite in a patient, comprising administering to said patient a pharmaceutical formulation formulated for subcutaneous injection by contacting the formulation with the adipose tissue, subcutaneous fat stores, regional fat accumulation or deposits, uneven fat accumulation in the abdomen, or cellulite, the formulation comprising:
a therapeutically effective amount of a lipophilic long-acting selective beta-2 adrenergic receptor agonist selected from the group consisting of salmeterol, formoterol, and bambuterol, or a physiologically acceptable salt or solvate thereof or combination thereof, wherein the formulation is administered to said patient less frequently than once per day.
2. The method of claim 1 wherein the lipophilic long-acting selective beta-2 adrenergic receptor agonist is salmeterol or a physiologically acceptable salt or solvate thereof.
3. The method of claim 2 wherein the salmeterol is salmeterol xinafoate.
4. The method of claim 3 wherein a single dose comprises up to 250 micrograms of salmeterol xinafoate.
5. The method of claim 1 wherein the injectable formulation is delivered by injection using at least one needle.
6. The method of claim 1 wherein the injectable formulation is delivered by injection using multiple needles or a multi-needle array.
7. The method of claim 1 wherein the injectable formulation is injected over an area of about 10 cm 2 to about 20 cm 2 .
8. The method of claim 1 wherein the injectable formulation is delivered by needleless injection.
9. A method of reducing excess adipose tissue in a non-obese human patient, or reducing excess subcutaneous fat stores in a non-obese human patient, or reducing excess regional fat accumulation or deposits in a non-obese human patient, or reducing uneven fat accumulation in the abdomen in a human patient, or reducing cellulite in a non-obese human patient, by administering to said patient a pharmaceutical formulation formulated for subcutaneous injection, comprising:
a therapeutically effective amount of a lipophilic long-acting selective beta-2 adrenergic receptor agonist selected from the group consisting of salmeterol, formoterol, and bambuterol, or a physiologically acceptable salt or solvate thereof or combination thereof;
wherein the formulation is administered to said patient less frequently than once per day.
10. The method of claim 9 wherein the lipophilic long-acting selective beta-2 adrenergic receptor agonist is salmeterol or a physiologically acceptable salt or solvate thereof.
11. The method of claim 10 wherein the salmeterol is salmeterol xinafoate.
12. The method of claim 11 wherein a single dose comprises up to 250 micrograms of salmeterol xinafoate.
13. The method of claim 12 wherein the method provides an effect that is at least partially cosmetic in improving the appearance of excess adipose tissue, excess subcutaneous fat stores, excess regional fat accumulation or deposits, uneven fat accumulation, or cellulite in a non-obese human patient.
14. A method of reducing excess adipose tissue in a human patient by stimulating lipolysis or inhibiting adipogenesis, or a combination thereof, comprising administering to said patient a pharmaceutical formulation formulated for subcutaneous injection comprising:
an adipose tissue-reducing therapeutically effective amount of a lipophilic long-acting selective beta-2 adrenergic receptor agonist selected from the group consisting of salmeterol, formoterol, and bambuterol, or a salt or solvate, or combination thereof; and
wherein the formulation is administered less than once per day; and
wherein the reduction in excess adipose tissue is achieved by a reduction in lipid content of adipocytes or a reduction in adipocyte size, or a combination thereof.
15. The method of claim 14 wherein the lipophilic long-acting selective beta-2 adrenergic receptor agonist is salmeterol or a physiologically acceptable salt or solvate thereof.
16. The method of claim 15 wherein the salmeterol is salmeterol xinafoate.
17. The method of claim 14 wherein the injectable formulation is formulated for non-sustained release of the lipophilic long-acting selective beta-2 adrenergic receptor agonist.
18. The method of claim 17 wherein the non-sustained release of the lipophilic long-acting selective beta-2 adrenergic receptor agonist provides sustained activity for at least 4 hours.
19. The method of claim 17 wherein the non-sustained release of the lipophilic long-acting selective beta-2 adrenergic receptor agonist provides sustained activity for at least 12 hours.
20. The method of claim 17 wherein the non-sustained release of the lipophilic long-acting selective beta-2 adrenergic receptor agonist provides sustained activity for at least 24 hours.