Selective, lipophilic, and long-acting beta agonist monotherapeutic formulations and methods for the cosmetic treatment of adiposity and contour bulging

Abstract

Provided herein are pharmaceutical and cosmetic formulations and methods for regional adiposity reduction and treatment of body contour defects such as abdominal bulging; comprising an injectable formulation, said formulation comprising: an active ingredient that consists essentially of an adipose tissue-reducing amount of one or more lipophilic long-acting selective beta-2 adrenergic receptor agonists, or salts, solvates, or polymorphs thereof; and one or more subcutaneously acceptable inactive ingredients.

What is claimed is: 
     
         1 . An injectable monotherapeutic formulation for treating a body contour defect in a human subject, wherein the single active agent is a lipophilic long-acting selective beta-2 adrenergic receptor agonist, or a salt, solvate, or polymorph thereof that is present in an effective amount that is less than about 1 microgram and wherein the formulation is formulated for subcutaneous administration and further consists of one or more subcutaneously acceptable inactive ingredients. 
     
     
         2 . An injectable monotherapeutic formulation for treating a body contour defect in a human subject, wherein the single active agent is a lipophilic long acting selective beta-2 adrenergic receptor agonist, or a salt, solvate, or polymorph thereof that is present in an effective amount that is less than about 10 micrograms/milliliter and wherein the formulation is formulated for subcutaneous administration and further consists of one or more subcutaneously acceptable inactive ingredients. 
     
     
         3 . A method for regional adiposity reduction by a monotherapy treatment regimen, comprising subcutaneously administering a monotherapeutic formulation, wherein each administration during the monotherapy treatment regimen comprises the single active agent selected from a lipophilic long-acting selective beta-2 adrenergic receptor agonist, or a salt, solvate, or polymorph thereof that is present in an effective amount that is equal to or less than about 20 micrograms, and wherein the formulation further consists of one or more subcutaneously acceptable inactive ingredients. 
     
     
         4 . The formulation of  claim 1  wherein the lipophilic long-acting selective beta-2 adrenergic receptor agonist is salmeterol, formoterol, salts, solvents, polymorphs, or a combination thereof. 
     
     
         5 . The formulation of  claim 4  wherein the lipophilic long-acting selective beta-2 adrenergic receptor agonist is salmeterol xinafoate. 
     
     
         6 . The formulation of  claim 5  wherein the formulation is formulated into a weekly dose of salmeterol xinafoate in an amount that is between about 12 nanograms to about 1 microgram. 
     
     
         7 . The formulation of  claim 1  wherein the lipophilic long-acting selective beta-2 adrenergic receptor agonist, or a salt, solvate, or polymorph thereof selectively partitions into adipose tissue relative to blood plasma when administered to the human subject. 
     
     
         8 . The formulation of  claim 1  that provides a partition ratio of between 0.01 to about 0.4 when the lipophilic long-acting selective beta-2 adrenergic receptor agonist, or a salt, solvate, or polymorph thereof is administered subcutaneously. 
     
     
         9 . The formulation of  claim 5  wherein the formulation is formulated to be administered to the human subject once per week at a single session dose of salmeterol xinafoate that is equal to or less than about 1 microgram. 
     
     
         10 . The formulation of  claim 9  wherein the session dose is divided into at least two sub-doses of salmeterol xinafoate wherein each sub-dose is in an amount that is between about 12 nanograms to about 1 microgram. 
     
     
         11 . The formulation of  claim 9  wherein the session dose is divided into at least two sub-doses of salmeterol xinafoate wherein each sub-dose is in an amount that is between about 900 nanograms to about 14 nanograms. 
     
     
         12 . The formulation of  claim 5  wherein the formulation is administered to the human subject once per week at a session dose of salmeterol xinafoate that is equal to or less than about 650 nanograms. 
     
     
         13 . The formulation of  claim 5  wherein the formulation is administered to the human subject in sub-doses of about 5 to about 28 sub-doses. 
     
     
         14 . The formulation of  claim 13  wherein each sub-dose comprises an amount of salmeterol xinafoate that is equal to or less than about 950 nanograms. 
     
     
         15 . The formulation of  claim 1  wherein the formulation is formulated to be administered to a human subject into a submental region, an abdominal region, a hip region, a thigh region, a buttocks region, a back region, an upper arms region, or a chest region. 
     
     
         16 . The formulation of  claim 1  wherein the formulation further comprises a subcutaneously acceptable excipient wherein the excipient is present in an amount of about 0.1 milliliter to about 20 milliliters. 
     
     
         17 . The formulation of  claim 1  wherein the formulation is administered to the human patient in a periodic dose wherein the periodic dose comprises between 1 and 52 times per year. 
     
     
         18 . The formulation of  claim 1  wherein the formulation is free of a co-solvent. 
     
     
         19 . The method of  claim 3  wherein the method is a cosmetic treatment, an aesthetic treatment, or a treatment for thyroid eye disease. 
     
     
         20 . The method of  claim 3  wherein the lipophilic long-acting selective beta-2 adrenergic receptor agonist, or a salt, solvate, or polymorph thereof is present in an amount that is between about 980 nanograms and 4 micrograms.