Formulations for substituted 3-pyrrolidines, compositions containing, and uses of same

A method of treating a patient afflicted with obesity which comprises applying to a patient's skin a pharmaceutical composition effective to treat the patient and alleviate the patient's obesity, wherein the pharmaceutical composition comprises a pharmaceutically acceptable carrier and a compound which has the structure:

• or a pharmaceutically acceptable salt or ester of the compound in an amount effective to treat the patient, and
• wherein the pharmaceutically acceptable carrier (A) provides an environment of physical and chemical stability, (B) enables retention of the amount of the compound effective to treat the patient in the patient's skin, (C) permits only a low level of the compound to enter and accumulate in the patient's systemic circulation, and (D) comprises:
• (i) ethanol at a concentration of 10.00% w/w;
• (ii) phenoxyethanol at a concentration in the range 0.1-5.0% w/w;
• (iii) diethylene glycol mono-ethyl ether (otherwise known as DEGEE or Transcutol P®) at a concentration in the range 5.0-40.0% w/w;
• (iv) propylene glycol at a concentration in the range 5.0-40.0% w/w;
• (v) PEG400 at a concentration in the range 5.0-40.0% w/w;
• (vi) carbomer homopolymer type C980 at a concentration in the range of 0.5 to 2.0% w/w;
• (vii) butylated hydroxytoluene (BHT) at a concentration of at least 0.05% w/w;
• (viii) di-sodium EDTA at a concentration of at least 0.001% w/w;
• (ix) trolamine at a concentration sufficient to provide an apparent pH in the range 6.50 to 7.50;
• and
• (x) water at a concentration of 19.02-22% w/w.