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Methods of reducing the body weight of a subject by administering a fatty acid ester of an estrogen or estrogen derivative in an oil and compositions containing the same

a technology of fatty acid ester and body weight, which is applied in the field of compositions and methods of reducing the body weight of a subject, can solve the problems of limited success, difficulty in all these approaches, and limited room for external manipulation, so as to reduce body weight, reduce body weight, and reduce body weigh

Inactive Publication Date: 2008-10-23
MANHATTAN PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

The approach allows for effective absorption and utilization of fatty acid esters, promoting weight loss by signaling the body's weight control system, reducing body fat mass, and improving insulin resistance.

Problems solved by technology

Treatment of obesity and / or overweight is a therapeutic and / or cosmetic problem of major importance that does not have a satisfactory solution yet.
But also known are the difficulties, limitations and general lack of success of all these approaches.
Apparently the sheer complexity of mechanisms involved in the control of body mass allows little room for external manipulation, thus limiting the possible damage to body reserves by increased thermogenic stimulation or diminished energy intake.
However, many fatty acid esters of estrogens or estrogen derivatives, including oleoyl-estrone, are poorly soluble or insoluble in water.
Moreover, manipulation of the pH and also the addition of surfactants may not improve the water solubility of fatty acid esters of estrogens or estrogen derivatives.
The insolubility or limited solubility of fatty acid esters of estrogens or estrogen derivatives in water introduces difficulties in formulating such compounds into pharmaceutical compositions.
In addition, because of the insolubility or limited solubility of the fatty acid esters of estrogens or estrogen derivatives in water, such compounds will not be able to be absorbed and used by the body unless such compounds are presented in a dissolved state at the site of absorption.

Method used

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  • Methods of reducing the body weight of a subject by administering a fatty acid ester of an estrogen or estrogen derivative in an oil and compositions containing the same
  • Methods of reducing the body weight of a subject by administering a fatty acid ester of an estrogen or estrogen derivative in an oil and compositions containing the same
  • Methods of reducing the body weight of a subject by administering a fatty acid ester of an estrogen or estrogen derivative in an oil and compositions containing the same

Examples

Experimental program
Comparison scheme
Effect test

example 1

[0052]An oil evaluation was done to determine the solubility behavior of oleoyl-estrone as a function of type of oil, concentration and temperature. The solubility of oleoyl-estrone was evaluated at concentrations of 60 mg / g and 200 mg / g. For the 60 mg / g solutions, the solubility was observed for 96 hours at room temperature, then the temperature was cycled to 5° C. for 96 hours, after which the solution was returned to room temperature. For the 200 mg / g solutions, the solubility was observed for 96 hours at 40° C., then the temperature was cycled to room temperature for 24 hours, then stored at 5° C. for 96 hours before being returned to room temperature. Table 1 and Table 2 show the oils tested and the test results.

TABLE 160 mg / g of Oleoyl-Estrone in Oil at RoomTemperature (RT) (about 22° C.)Cycledto 5° C.OilAfter 24 hrAfter 96 hrafter 96 hrCanolaDissolvedDissolvedDissolvedLabrasolDissolvedDissolvedPrecipitatedafter 4 hrLabrafil M 125CSNOTNOT Dissolved more oilDissolvedDissolvedad...

example 2

[0054]The compatibility of oleoyl-estrone in various oil systems was also assessed. The respective stability of oleoyl-estrone in various oils was assessed following storage at (A) 25° C. / 60% and relative humidity (RH), (B) 40° C. / 75% RH, (C) 50° C. and (D) 60° C. in canola oil, safflower oil, Captex and a 2:1 Captex: Labrafil mixture. The stability test methods include appearance / color, potency, and related substances (e.g. impurities or degradant in the oleoyl-estrone and oil mixture). The results of the three week tests are set forth in Tables 4-7.

TABLE 4Time ZeroOne WeekTwo WeeksAnalysisCANOLACANOLACANOLAConditionN / A25° C. / 60%40° C. / 75%50° C.60° C.25° C. / 60%40° C. / 75%RHRHRHRHPull DateN / A11 AUG 0411 AUG 0411 AUG 0411 AUG 0418 AUG 0418 AUG 04Assay Date04 AUG 0411 AUG 0411 AUG 0411 AUG 0411 AUG 0418 AUG 0418 AUG 04Appearance / Clear andClear andClear andClear andClear andClear andClear andColorpale yellowpale yellowpale yellowpale yellowpale yellowpale yellowpale yellowReference Std ...

example 3

[0057]Capsules containing 1 mg, 10 mg and 50 mg of oleoyl-estrone are prepared according to the formulations shown in Table 8 and according the method shown in FIG. 1.

TABLE 8Amount of Component per BatchComponent1 mg capsule10 mg capsule50 mg capsuleOleoyl-Estrone1.160 g14.0 g72.50 gSafflower Oil56.84 g98.0 g507.5 gTotal58.00 g112.0 g 580.0 g

[0058]FIG. 1 is a flow diagram that illustrates the manufacturing process of making the oleoyl-estrone capsules as discussed herein. Each of the three batch formulations were manufactured by dissolving the indicated amount of oleoyl-estrone in safflower oil (Step A of FIG. 1). To facilitate dissolution, heat was applied to maintain a temperature of 40° C. Then gelatin capsules are filled with each batch of oleoyl-estrone and safflower oil and then placed upright in a capsule holder (Step B of FIG. 1). The fill weights of the 1 mg, 10 mg, and 50 mg dosage strength capsules are provided in Table 9.

TABLE 9Dosage (mg)Capsule Fill Weight (mg) ± 5%150...

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Abstract

Compositions and methods for reducing the body weight of a subject are disclosed. The invention is directed to methods for reducing the body weight in a subject comprising administering therapeutically effective amounts of a fatty acid ester of an estrogen or estrogen derivative in an oil. Furthermore the invention is directed to compositions for reducing the body weight in a subject comprising administering therapeutically effective amounts of a fatty acid ester of an estrogen or estrogen derivative in an oil.

Description

CROSS-REFERENCE TO RELATED APPLICATIONS[0001]This application is a continuation of U.S. patent application Ser. No. 11 / 475,461, filed Jun. 26, 2006. The entire contents of this application are expressly incorporated herein by reference thereto.FIELD OF THE INVENTION[0002]This invention relates generally to compositions and methods of reducing the body weight of a subject. More particularly, the invention is directed to methods of reducing the body weight in a subject comprising administering therapeutically effective amounts of a fatty acid ester of an estrogen or estrogen derivative in an oil. Furthermore the invention is directed to compositions comprising a fatty acid ester of an estrogen or estrogen derivative in an oil.BACKGROUND OF THE INVENTION[0003]Treatment of obesity and / or overweight is a therapeutic and / or cosmetic problem of major importance that does not have a satisfactory solution yet. Attempts to solve the problem by physical exercise or reduction of food intake are...

Claims

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Application Information

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Patent Type & Authority Applications(United States)
IPC IPC(8): A61K31/56A61P3/04
CPCH01Q5/371H01Q9/42A61P3/04
Inventor MAURIN, MICHAEL B.GANGRADE, NUTAN K.LENZ, KRISTI O.TEJURA, BINDU
Owner MANHATTAN PHARMA