THE MAIN TEA ETA US DAN20170304317A1 MA TA AT MAN AT MAN ( 19) United States (12 ) Patent Application Publication ( 10) Pub . No. : US 2017/ 0304317 A1 DiMaggio ( 43 ) Pub . Date : Oct. 26 , 2017 ( 54 ) DIETARY SUPPLEMENTS FOR MUSCLE A61K 31 / 366 ( 2006 .01 ) GROWTH AND STRENGTH A61K 31 /4525 ( 2006 .01 ) ( 52 ) U .S . CI. (71 ) Applicant : Robert DiMaggio , Henderson , NV CPC . .. A61K 31/ 5685 (2013 .01 ) ; A61K 31/ 4525 (US ) (2013 . 01 ) ; A61K 9 /48 ( 2013 .01 ) ; A61K 31/ 366 (72 ) Inventor : Robert DiMaggio , Henderson , NV ( 2013 .01 ) (US ) (57 ) ABSTRACT (21 ) Appl. No. : 15 /643 , 894 A compound is provided for oral administration of dehy droepiandrosterone (DHEA ) derivatives to a human so as to ( 22 ) Filed : Jul . 7 , 2017 improve at least one of adrenal hormonal balance , improved immune system function , reduction of adipose tissue , skel Related U . S . Application Data etal muscle growth , reduction of abdominal bloating , (63 ) Continuation - in -part of application No . 14 /736 , 103 , improved recovery from training , increased strength , and increased endurance . The compound includes a first portion filed on Jun . 10 , 2015 . comprised of any one of 3a -enanthoxy - 5a -androstan -17 (60 ) Provisional application No . 62 / 360 , 241, filed on Jul. one , 3b - undecyloxy - 5a -androstan - 17 - one , and 3b -hydroxy 8 , 2016 . androstane - 3b - ol- one . A second portion of the compound is comprised of 6 , 7 -dihydrogergamottin . A third portion is Publication Classification comprised of piperine , and a fourth portion is comprised of (51 ) Int. Ci. any one or more of rice flour , gelatin , magnesium stearate , A61K 31/ 5685 ( 2006 . 01 ) and silica . The compound preferably is administered in A61K 9 /48 ( 2006 .01 ) capsule form one or two times in a 24 -hour period . - 104 THI wa miche 5 -DHEA Heptanoyl Chloride missed5 -DHEA Enanthated Patent Application Publication Oct . 26, 2017 Sheet 1 of 2 US 2017/ 0304317 A1 ?? ????????????? 5 -DHEA Heptanoyl Chloride 5 -DHEA Enanthated FIGFIG . 11 2018 ???.???ift? Or?? +???? ???. 1 - DHEA Heptanoyl Chloride 1 -DHEA Enanthated FIG . 2 ?? 312 ?? ?? 4 - DHEA Heptanoyl Chloride 4 -DHEA Enanthated??? FIG . 3 Patent Application Publication Oct . 26, 2017 Sheet 2 of 2 US 2017/ 0304317 A1 - 404 ?????? ??? ??? re * 6-) R -DHEA SUPER R -DHEA (Reduced R - DHEA ) FIG . 4 508 - ? 19 -Nor - DHEA Heptanoyl??????? Chloride 19 Nor- DHEA Enanthated FIG . 5 612 \ ???- ?????? Epiandrosterone Hendecanoic Acid Epiandrosterone FIG . 6 Undecanoate US 2017 /0304317 A1 Oct. 26 , 2017 DIETARY SUPPLEMENTS FOR MUSCLE compound . In addition , DHEA sulfate does not restore the GROWTH AND STRENGTH balance of the adrenal steroids discussed above . As a result , frequent and larger doses of DHEA must be taken to achieve PRIORITY a desired result . [ 0001] This continuation - in - part application claims the [ 0008 ] DHEA is also metabolized in the body to one of benefit of and priority to U . S . patent application , entitled several compounds including , for example , etiocholanolone “ Method For DHEA Enanthate Processing, ” filed on Jun . 10 , ( 5 -beta - androstan - 3 - alpha - ol- 17 -one ), beta etiocholanolone 2015 having application Ser. No . 14 /736 , 103 and U . S . ( 5 -beta -androstan - 3 -beta - ol - 17 -one ) , androsterone ( 5 - alpha Provisional Patent Application No . 62 / 360 , 241 filed on Jul. androstan - 3 - alpha -ol - 17 -one ) , epiandrosterone ( 5 -alpha - an 8 , 2016 . drostan - 3 - beta - ol- 17 -one ) , 7 -keto - DHEA , 7 - alpha -hydroxy DHEA , 7 - beta -hydroxy - DHEA , androstenedione, estrone , FIELD and estradiol. [0002 ] The field of the present disclosure generally relates [ 0009 ] There is great individual variability in the metabo to dietary supplements . More particularly , the field of the lism of oral DHEA . The DHEA metabolites estrone and present disclosure relates to compounds for oral adminis estradiol can result in negative estrogenic side effects for tration of dehydroepiandrosterone (DHEA ) derivative to males including growth of male breast tissue , known as improve human physical performance . gynecomastia . Some individuals have poor bioavailability of DHEA as a result of sulfation in the liver , and large doses BACKGROUND must be taken to elicit any desired effects . These increased doses of DHEA can result in increased conversion to estrone [ 0003 ] The adrenal gland produces many steroid hor and estradiol, with resulting negative side effects . mones . These steroid hormones play a major role in many body processes including , for example, skeletal muscle [ 0010 ] What is needed , therefore, are compounds which growth , red blood cell production ( erythropoiesis ), regula provide the beneficial effects of high DHEA levels in the tion of glucose and insulin levels , and cellular aging . The body for extended periods of time, yet reduce the undesired steroids produced by the adrenal gland can be divided into DHEA side effects discussed above . three groups: glucocorticoids, which influence carbohydrate metabolism ; mineralocorticoids, which control electrolyte SUMMARY and water balance; and sex steroid hormones . [0004 ] Glucocorticoids such as cortisol regulate catabo [0011 ] A compound is provided for oral administration of lism of skeletal muscle proteins into amino acids. These dehydroepiandrosterone (DHEA ) derivatives to a human so amino acids are then transported to the liver and converted as to improve at least one of adrenal hormonal balance , into glucose during gluconeogenesis . Excessive amounts of improved immune system function , reduction of adipose glucocorticoids can result in higher blood glucose and tissue , skeletal muscle growth , reduction of abdominal insulin levels and can contribute to increased body fat and bloating , improved recovery from training , increased type II diabetes . Glucocorticoids are also known to play a strength , and increased endurance . The compound includes role in the aging process by increasing cellular and mito a first portion comprised of any one of 3a - enanthoxy - 5a chondrial breakdown. Mineralocorticoids such as aldoster androstan - 17 - one , 3b - undecyloxy - 5a - androstan - 17 -one , and one help the body to retain sodium and water. Excesses of 3b -hydroxy -androstane - 3b - ol- one . A second portion of the mineralocorticoids can result in hypertension and cardio compound is comprised of 6 , 7 -dihydrogergamottin (DHB ) . vascular disease . The sex steroid hormones include adrenal A third portion is comprised of piperine , and a fourth portion androgens and DHEA . Adrenal androgens oppose the is comprised of any one or more of rice flour, gelatin , actions of glucocorticoids and result in skeletal muscle magnesium stearate , and silica . In one embodiment, the first anabolism ( the opposite action of catabolism ) , reductions in portion may be comprised of substantially 100 mg of blood glucose and insulin levels , reduction in body fat, and 3a - enanthoxy -5a - androstan - 17 -one , the second portion may are believed to decrease the rate of cellular aging and be comprised of substantially 15 mg of DHB 45 % , and the increased red blood cell production . DHEA production by third portion may be comprised of substantially 5 mg of the adrenal glands is known to decline markedly as aging piperine . In another embodiment, the first portion may be progresses . comprised of substantially 50 mg of 3b - undecyloxy -5a [ 0005 ] With normal younger adults , all three groups of androstan - 17 - one , the second portion may be comprised of adrenal steroids are produced in a healthy balance . As people substantially 15 mg of DHB 45 % , and the third portion may age , however , less DHEA is produced resulting in relatively be comprised of substantially 5 mg of piperine . In still greater amounts of glucocorticoids and mineralocorticoids, another embodiment, the first portion may be comprised of resulting in a disruption of a healthy hormone balance . substantially 50 mg of 3b - hydroxy -androstane - 3b - ol- one , [0006 ] DHEA supplementation is believed to be useful in the second portion may be comprised of substantially 15 mg treatment of aging and obesity , and to stimulate erythropoi of DHB , and the third portion may be comprised of sub esis and skeletal muscle anabolism . In addition , supplemen stantially 5 mg of piperine . The compound preferably is tal DHEA may help restore the balance of adrenal steroids. administered in capsule form one or two times in a 24 - hour [0007 ]. DHEA is commonly used as a dietary supplement . period . Unfortunately , DHEA is rapidly metabolized by liver [0012 ] In an exemplary embodiment, a compound for oral enzymes , such as sulfotransferases. Sulfotransferases rap administration of dehydroepiandrosterone (DHEA ) deriva idly convert much of the supplementary DHEA into DHEA tives to a human comprises a first portion comprised of one sulfate , which is quickly excreted from the body and is not or more prohormones ; a second portion comprised of one or effective as an anti - aging , muscle - building or fat reduction more compounds to increase the bioavailability of the one or US 2017 /0304317 A1 Oct. 26 , 2017 more prohormones ; and a third portion comprised of one or tially 15 mg of DHB 45 % , and the third portion is comprised more compounds to decrease a conversion of testosterone to of substantially 5 mg of piperine . In another exemplary estrogen . embodiment, the first portion is comprised of substantially [0013 ] In another exemplary embodiment , the
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