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(12) Patent Application Publication (10) Pub. No.: US 2015/0018324 A1 Chickmath Et Al

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(12) Patent Application Publication (10) Pub. No.: US 2015/0018324 A1 Chickmath Et Al US 201500 18324A1 (19) United States (12) Patent Application Publication (10) Pub. No.: US 2015/0018324 A1 Chickmath et al. (43) Pub. Date: Jan. 15, 2015 (54) TESTOSTERONE UNDECANOATE Publication Classification COMPOSITIONS (51) Int. Cl. (71) Applicants: Basawaraj Chickmath, Plymouth, MN A619/28 (2006.01) (US); Chandrashekar Giliyar, North A647/38 (2006.01) Maple Grove, MN (US); Chidambaram A647/10 (2006.01) Nachiappan, Sandy, UT (US); Mahesh A619/20 (2006.01) V. Patel, Salt Lake City, UT (US); A613 L/568 (2006.01) Srinivasan Venkateshwaran, Salt Lake A647/36 (2006.01) City, UT (US) (52) U.S. Cl. CPC ............... A61K 9/286 (2013.01); A61 K3I/568 (72) Inventors: Basawaraj Chickmath, Plymouth, MN (2013.01); A61 K47/36 (2013.01); A61 K (US); Chandrashekar Giliyar, North 9/2853 (2013.01); A61K 9/282 (2013.01); Maple Grove, MN (US); Chidambaram A647/10 (29.91) A6 IK9/2054 Nachiappan, Sandy, UT (US); Mahesh USPC (2013.01); A61 K47/38 E. V. Patel, Salt Lake City, UT (US); ' ' “” Srinivasan Venkateshwaran, Salt Lake (57) ABSTRACT City, UT (US) The present disclosure is drawn to pharmaceutical composi tions and oral dosage forms containing testosterone unde canoate, as well as related methods of treatment. In one (21) Appl. No.: 14/500,498 embodiment, the oral dosage form can include a therapeuti cally effective amount of testosterone undecanoate and a pharmaceutically acceptable carrier. The dosage form can be (22) Filed: Sep. 29, 2014 formulated such that, when measured using a USPType II apparatus in 1000 mL of 8 wt % TritonX-100 in water at 37° C. and 100 rpm, the oral dosage form releases at least 20% Related U.S. Application Data more testosterone undecanoate after the first 120 minutes than an equivalent dose testosterone undecanoate containing (63) Continuation of application No. 12/965,703, filed on oral dosage form without the pharmaceutically acceptable Dec. 10, 2010. carrier. US 2015/0018324 A1 Jan. 15, 2015 TESTOSTERONE UNDECANOATE induction resulting in potential drug-drug interactions. Cur COMPOSITIONS rently, modified testosterones, in form of methyl analogue of testosterone, and as an undecanoate ester, testosterone unde FIELD OF THE INVENTION canoate (TU) are available for oral administration for patients in need of testosterone therapy. However, liver damage 0001. The present invention relates to solid testosterone including cholestasis, peliosis hepatitis, nodular regenerative undecanoate containing pharmaceutical compositions and hyperplasia, and primary hepatic tumors has been reported oral dosage forms as well as associated methods of treatment. with use of methyl testosterone. Testosterone undecanoate, a Accordingly, this invention involves the fields of chemistry, prodrug of testosterone, containing oral dosage forms are pharmaceutical Sciences, medicine and other health Sciences. marketed in various countries under various trade names, e.g. Andriol R, Restandol R, Andriol Testocap(R) etc., each of BACKGROUND OF THE INVENTION which are liquid filled Soft-gelatin capsule formulations con 0002 The need for testosterone supplementation, often taining about 40 mg of TU in a liquid carrier. Testosterone caused by testosterone deficiency, is a condition that can undecanoate is converted in vivo to pharmacologically active affect both men and women. Testosterone deficiency can be testOSterOne. accompanied by a variety of symptoms including sexual dys 0006. However, a huge drawback of the current state of the function, reduced muscle mass and muscle strength, art oral liquid testosterone undecanoate formulations is that it depressed mood, and osteoporosis. Male hypogonadism and has to be encapsulated in a capsule dosage form presenting it female sexual dysfunction is characterized by a deficiency of with limitations with respect to acceptable capsule sizes and endogenous testosterone production resulting in abnormally related drug loading limitations due to testosterone unde low levels of circulating testosterone. Currently, common canoate's poor solubility. Such limitations present challenges testosterone therapy treatment can include administration of with respect to patient compliance, because patients typically invasive intramuscular products, topical gels, topical Solution have to take multiple capsule units in order to get a sufficient and patches, or multiple units of liquid oral dosage capsules. dose to provide the desired efficacy. Additionally, liquid cap There are challenges and drawbacks associated with each of Sule formulations tend to require more complicated and these therapies. For example, use of topical gels or topical costly manufacturing processes and often require special Solutions can resultinaccidental transfer of the active agent to storage and handling. Moreover, liquid lipidic compositions others, such as children or partners. can present oxidative instability challenges with respect to 0003 Current standard therapies for males aim at restor testosterone and its derivatives. Due to testosterone unde ing physiologically relevant levels of testosterone in serum. It canoate's poor solubility, the production of a solid oral dos is generally recognized that in a normal adult man of age 17 age forms such as tablets, caplets, and particulates remains an to 54 yrs, the average serum testosterone (T) a major andro area of continuous research and development. genic hormone in males, is between about 300 ng/dL to about 1100 ng/dL, known as the eugonadal range. Testosterone SUMMARY OF THE INVENTION replacement in males should in theory approximate the natu 0007. The present disclosure is drawn to pharmaceutical ral, endogenous production of the hormone. The average compositions and oral dosage forms containing testosterone male produces 4-7 mg of testosterone per day in a circadian undecanoate, as well as related methods of treatment. In one pattern, with maximal plasma levels attained in early morning embodiment, a solid composition is provided. The dosage and minimal levels in the evening. form can include a therapeutically effective amount of test 0004 Low or reduced sexual desire is a condition that osterone undecanoate and a pharmaceutically acceptable car impacts millions of women, particularly those over the age of rier. The oral dosage form can beformulated to release at least 50. Testosterone (T) levels can steeply decline in women as 35 wt % of the dosage forms testosterone undecanoate in the they age or after Surgical menopause. Endogenous testoster first 120 minutes when measured using a USPType II appa one levels in women at age 40 are one half of those of women ratus in 1000 mL of 8 wt % TritonX-100 in water at 37°C. and at age 21 and endogenous testosterone levels in women after 100 rpm. In one embodiment, the testosterone undecanoate oophorectomy are 50% less than before oophorectomy. There can be present in the composition as a Solid particulate. In yet is strong indication that Supplemental testosterone therapy a further embodiment, the carrier can be free of lipid sub may be beneficial for the treatment of women with reduced stance, or lipophilic Surfactant or hydrophilic Surfactants. sexual desire. Currently in the United States, there is no 0008. In another embodiment, a solid oral dosage form is approved testosterone product available for the treatment of provided. The oral dosage form can include a therapeutically female sexual dysfunction and reduced sexual desire. The effective amount of testosterone undecanoate and a pharma human female has substantially lower normal blood levels of ceutically acceptable carrier. The dosage form can be formu total testosterone (10-100 ng/dL compared to males ~300 lated Such that, when measured using a USPType II apparatus 1100 ng/dL) so it can be logically surmised that efficacious in 1000 mL of 8 wt % Triton X-100 in water at 37° C. and 100 doses for women can be substantially lower (about 10-50 rpm, the oral dosage form releases at least 20% more test times) than that for men. osterone undecanoate after the first 120 minutes than a 0005 While oral is typically the most preferred and equivalent dose testosterone undecanoate containing oral patient friendly route for administration, the oral delivery of dosage form without the pharmaceutically acceptable carrier. testosterone as testosterone remains a huge challenge. This is In one embodiment, testosterone undecanoate is not present due to extremely poor bioavailability requiring very high in the solid composition in a solubilized form. In another dose as well as the short serum half-life requiring frequent embodiment the oral dosage form can be formulated to dosing. These problems with orally administered testosterone include the testosterone undecanoate dose in the form of solid are primarily due to first pass metabolism. Moreover, direct, particulates. In another embodiment the oral dosage form of oral delivery of testosterone is also known to cause enzyme this invention can include a composition comprising Solid US 2015/0018324 A1 Jan. 15, 2015 particulates that can be solid testosterone undecanoate and/or than Ce) or fatty acid esters or glycerides of fatty acid esters, a solid pharmaceutically acceptable carrier. mixtures thereof and derivatives thereof, although not includ 0009. In yet another embodiment, a method for treating a ing salts thereof. subject in need of testosterone therapy is provided. The 0016. As used herein, “subject” refers to a mammal that method includes administering a solid oral dosage form of the may benefit from the administration of a drug composition
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