The patent's inventors are Hodge,
This patent was filed on
From the background information supplied by the inventors, news correspondents obtained the following quote: "Recently published literature reports that the aqueous solutions of DCA has fat removing properties when injected into fatty deposits in vivo (See, WO 2005/117900 and WO 2005/112942, US2005/0261258; US2005/0267080; US2006/127468; and US2006/0154906). DCA injected into fat tissue degrades fat cells via a cytolytic mechanism to provide the desired aesthetic results.
"Notwithstanding the benefits of aqueous formulations of DCA, it has been found that at low concentrations of DCA (i.e., less than or about 2% w/v;) in aqueous solutions which optionally contain benzyl alcohol, forms a precipitate after storage over a period of time. Surprisingly, it has been found that the lower the concentration DCA, the higher is the rate of precipitation notwithstanding any significant change in the pH of the solution. This precipitation at very low concentrations is a problem for commercialization as a precipitate is counter-indicated for subcutaneous injections of DCA.
"In each treatment regimen, the current clinical trials of aqueous formulations of DCA employ multiple injections of small amounts of the aqueous formulation into different sites defining the fat deposit to be treated.
"As it apparent, aqueous formulations of DCA used in such treatments overlap with the problems arising from precipitation of the DCA. That is to say that an initially clear aqueous solution of DCA when stored for a period of time, will form a precipitate at commercially relevant concentrations of DCA notwithstanding the fact that the pH of these solutions are between about 7.50 and about 8.0 which are substantially above the pKa of deoxycholic acid.
"Thus, there is a need for stabilizing the low concentration aqueous solutions of deoxycholic acid or a salt thereof against precipitation during a shelf life of at least 2 months.
"All publications and patent applications mentioned in this specification are herein incorporated by reference to the same extent as if each individual publication or patent application was specifically and individually indicated to be incorporated by reference."
Supplementing the background information on this patent, NewsRx reporters also obtained the inventors' summary information for this patent: "It has been surprisingly found that aqueous solutions of a salt of deoxycholic acid at concentrations of from about 0.4% w/v to less than about 2% w/v can be stabilized by adjusting the pH of the solution to above about 8 and preferably from a physiologically acceptable pH from about 8.1 to about 8.5. The pH is preferably maintained within this range by using buffers.
"Accordingly, in one of its composition aspects, this invention is directed to aqueous formulations consisting essentially of a salt of deoxycholic acid at a concentration of from about 0.4% w/v to less than about 2% w/v and optionally a preservative effective amount of benzyl alcohol which formulations are stabilized against precipitation by adjusting the pH of the initially formed clear solution to a pH of from about 8.1 to about 8.5.
"In another embodiment, this invention is directed to an aqueous formulation consisting essentially of:
"a sterile aqueous solution buffered to a pH of about 8.3;
"about 0.5% w/v or about 1% w/v of a salt of deoxycholic acid;
"optionally a preservative effective amount of benzyl alcohol; and
"about 1% w/v of sodium chloride,
"wherein the composition is stable against precipitation.
"Also disclosed herein is a method for stabilizing an aqueous composition of a salt of deoxycholic acid against precipitation during storage wherein the concentration of the deoxycholic acid salt is an amount effective to lyse fat cells provided that the amount of the deoxycholic acid salt ranges from about 0.4% w/v to less than 2% w/v, which method comprises:
"forming an aqueous solution of a deoxycholic acid salt at an initial pH above its pKa; adjusting the pH of the aqueous solution to a pH of from about 8.1 to about 8.5; and optionally including a sufficient amount of buffer to maintain the pH at from about 8.1 to about 8.5.
"Also disclosed herein is a method to lyse a fat cell comprising administering to said cell a composition according to this invention."
For the URL and additional information on this patent, see: Hodge,
Keywords for this news article include: Drugs, Therapy, Hydrocarbons, Benzyl Alcohols, Benzyl Compounds, Benzene Derivatives, Clinical Trials and Studies,
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