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(12) Patent Application Publication (10) Pub. No.: US 2004/019870.6 A1 Carrara Et Al

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(12) Patent Application Publication (10) Pub. No.: US 2004/019870.6 A1 Carrara Et Al US 2004O1987O6A1 (19) United States (12) Patent Application Publication (10) Pub. No.: US 2004/019870.6 A1 Carrara et al. (43) Pub. Date: Oct. 7, 2004 (54) METHODS AND FORMULATIONS FOR Related U.S. Application Data TRANSIDERMAL OR TRANSMUCOSAL APPLICATION OF ACTIVE AGENTS (60) Provisional application No. 60/510,613, filed on Oct. 10, 2003. Provisional application No. 60/453,604, (76) Inventors: Dario Norberto R. Carrara, Oberwill filed on Mar. 11, 2003. (CH); Arnaud Grenier, Sierentz (FR); Celine Besse, Saint Louis (FR); Publication Classification Stephen M. Simes, Long Grove, IL (US); Leah M. Lehman, Green Oaks, (51) Int. Cl. ................................................ A61K 31/56 IL (US) (52) U.S. Cl. .............................................................. 514/169 Correspondence Address: ABSTRACT WINSTON & STRAWN (57) PATENT DEPARTMENT 1400 L STREET, N.W. Methods, formulations, and kits for providing transdermal or WASHINGTON, DC 20005-3502 (US) transmucosal delivery of active agents to Subjects in need thereof. The formulations and methods treat symptoms of (21) Appl. No.: 10/798,111 hormonal disorders including hypogonadism, female Sexual desire disorder, female menopausal disorder, and adrenal (22) Filed: Mar. 10, 2004 insufficiency. Patent Application Publication Oct. 7, 2004 Sheet 1 of 11 US 2004/019870.6 A1 -- T1%-LA 0% NS. -- T1%-LA 1% -A- T1%-LA.2% -0- T1%-LA 0% rNs -- T1%-LA 1% -- T1%-LA 2% Time (h) FIG, 2 Patent Application Publication Oct. 7, 2004 Sheet 2 of 11 US 2004/019870.6 A1 -A-Day 1(DoSe 0.22g) -- Day 7(Dose 0.22g) -o- Day14(Dose 0.44 g) -H Day 21(Dose 0.88 g) Time (Hours) Since Application FIG, 3A 40 -A-Day 1 (Dose 0.22g) 35 -- Day 7(Dose 0.22g) -o- Day 14(Dose 0.44 g) : -- Day 21 (Dose 0.88 g) 1 0 Time (Hours) Since Application FIG, 3B Patent Application Publication Oct. 7, 2004 Sheet 3 of 11 US 2004/019870.6 A1 -A-Day 1(Dose 0.22g) -0- Day 7(Dose 0.22g) -o- Day14(Dose 0.44 g) 50 -H Day 21(4 to Dose 0.88 g) 4 O 30 20 O O DO DOD Do UIN= 12.7 10 - - - - - - - - - - - - - - LLWF1.6 0 2 4 6 8 10 12 14 16 18 20 22 24 Time (Hours) Since Application FIG, 3C 400 -E-HE-a=Day 0 baseline featment -A-A-a-b-Day 1; single dose, 0.5gge?/day -e- e -e- c=Day 7 multiple dose, 0.5gge?/day -o-e-o- d-Day 14: multiple dose, 19 ge/day 300 e=Day 14; multiple dose, 0.5g gel/day - B -- B- f-Day 7 multiple dose, 0.35g gel/day Patent Application Publication Oct. 7, 2004 Sheet 4 of 11 US 2004/019870.6 A1 featment --a-a-a-b=Day---- a-Day 0,1: Singlebaseline dose, 0.5gge?/da -e- e -e- C=Day 7 multiple dose, 0.5g gel/day -O-e-o-d=Day 14: multiple dose, 19 gel/day 80 - e=Day 14: multiple dose, 0.5gge?/day -B -- B- f=Day 7 multiple dose, 0.35gge?/day 60 ---E-a=Day 0 baseline featre -a-a-a-b=Day 1; single dose, 0.5gge?/day -e- e -e- c=Day 7 multiple dose, 0.5gge?/day -O-e-o- d=Day 14: multiple dose, 19 ge/day e=Day 14: multiple dose, 0.5gge?/day - B -- B- f-Day 7 multiple dose, 0.35gge/day 3 00 2 O Patent Application Publication Oct. 7, 2004 Sheet 5 of 11 US 2004/019870.6 A1 10 -E-S-S- a Treatment - A - A - A - b 5 Treatment s as a amar as b -24 144 312 480 Time (h) FIG. 4B Patent Application Publication Oct. 7, 2004 Sheet 6 of 11 US 2004/019870.6 A1 Treatment ---- b s 144 312 480 Time (h) FIG, 4C 25 20 S.S 15 N 10 -24 144 312 480 Patent Application Publication Oct. 7, 2004 Sheet 7 of 11 US 2004/019870.6 A1 20 -E-B-E- a Treatment - A - A - A - b 1 5 I 0 312 3.18 324 330 336 Time (h) FIG, 4E -EHEE- 3 Treatment - A - A - A - b Patent Application Publication Oct. 7, 2004 Sheet 8 of 11 US 2004/019870.6 A1 20 -SHSHE- a Treatment 1 5 - A - A - A - b. 1 O 24 144 312 480 20 -EHEHS- a Treatment - A - A - A - b. l 5 10 312 316 320 324 328 332 336 Time (h) FIG, 4H. Patent Application Publication Oct. 7, 2004 Sheet 9 of 11 US 2004/019870.6 A1 -B-E-E- a Treatment - A - A - A - b 350 -B-E-S- a 300 Treatment 250 200 150 100 24 144 312 480 Time (h) FIG, 4 J Patent Application Publication Oct. 7, 2004 Sheet 10 of 11 US 2004/019870.6 A1 -EHE-E-3 Treatment - A - A - A - b 312 316 320 3.24 328 332 336 Time (h) FIG, 4K - A - Placebo -o- 0.625g/day (0.375 mg estradiol) -o- 1.25g/day (0.75 mg estradiol) -H 2.5g/day (1.5 mg estradiol) -1 O -1 2 Baseline Week-1 Week 1 Week 2 Week 3 Week 4 Week of Treatment FIG 5A Patent Application Publication Oct. 7, 2004 Sheet 11 of 11 US 2004/019870.6 A1 - A - Placebo -o- 0.625g/day (0.375 mg estradiol) -O- 1.25g/day (0.75 mg estradiol) c S -- 2.5g/day (1.5 mg estradiol) - SV -4 S S.s -6 S. S -8 s S -1 0 -12 Baseline Week-1 Week 1 Week 2 Week 3 Week 4 Week Of Treatment -A - Placebo -o- 0.625g/aay (0.375 mg estradiol) -o- 1.25g/day (0.75 mg estradiol) -- 2.5g/day (1.5 mg estradiol) 0 5 Baseline Week-1 Week 1 Week 2 Week 3 Week 4 Week Of Treatment FIG 5C US 2004/O1987O6 A1 Oct. 7, 2004 METHODS AND FORMULATIONS FOR plasma difficult. Testosterone injections are also associated TRANSIDERMAL, OR TRANSMUCOSAL with mood Swings and increased Serum lipid levels. Injec APPLICATION OF ACTIVE AGENTS tions require large needles for intramuscular delivery, which leads to diminished patient compliance due to discomfort. CROSS REFERENCE TO RELATED Commonly, estrogen is often administered orally. This route APPLICATIONS of administration has been also associated with complica tions related to hormone metabolism, resulting in inadequate 0001. This application claims priority to U.S. Provisional levels of circulating hormone. Further, Side-effects Seen with Patent Application 60/510,613 filed Oct. 10, 2003 and U.S. the use of oral estrogen include gallstones and blood clots. Provisional Patent Application 60/453,604 filed Mar. 11, To overcome these problems, transdermal delivery 2003. Each prior application is expressly incorporated approaches have been developed to achieve therapeutic herein in its entirety by reference thereto. effects in a more patient friendly manner. BACKGROUND OF THE INVENTION 0008 Advantageously, transdermal and/or transmucosal delivery of active agents provide a convenient, pain-free, 0002) 1. Field of Invention and non-invasive method of administering active agents to a 0003. The present invention relates generally to formu Subject. Additionally, the administration of active agents lations, methods, and kits for providing transdermal or through the skin or mucosal Surface avoids the well-docu transmucosal delivery of active agents to Subjects. In par mented problems associated with the “first pass effect” ticular, the invention relates to formulations and methods for encountered by oral administration of active agents. treating Symptoms of hypogonadism, female menopausal 0009. Although the transdermal and/or transmucosal Symptoms, female Sexual desire disorder, hypoactive Sexual delivery of active agents overcome Some of the problems disorder and adrenal insufficiency. asSociated with oral administration of active agents, Such as 0004 2. Background Art that described above, they are not free of their own draw backS. Problematically, transdermal drug delivery Systems 0005 Reduced levels of endogenous steroid hormones in are typically restricted to low-molecular weight drugs and humans often leads to a variety of undesirable clinical those with Structures having the proper lipophilic/hydro Symptoms. For example, men with low testosterone levels philic balance. High molecular weight drugs, or drugs with (hypogonadism) may result in clinical Symptoms including too high or low hydrophilic balance, often cannot be incor impotence, lack of sex drive, muscle weakness, and porated into current transdermal Systems in concentrations Osteoporosis. Similarly, in women, reduced levels of test high enough to overcome their impermeability through the osterone and/or estrogen may result in female Sexual disor Stratum corneum. Specifically, polar drugs tend to penetrate der, which include clinical Symptoms Such as lack of SeX drive, lack of arousal or pleasure, low energy, reduced Sense the Skin too slowly, and Since most drugs are of a polar of well-being, and Osteoporosis. Moreover, reduced levels of nature, this limitation is significant. estrogen and/or progesterone in Women, Such as that due to 0010. Efforts have been made in the art to chemically menopause, often result in clinical Symptoms including hot modify the barrier properties of Skin to permit the penetra flashes, night Sweats, vaginal atrophy, decreased libido, and tion of certain agents (since diffusion is primarily controlled Osteoporosis. through the Stratum corneum), enhance the effectiveness of 0006. In addition to reduced levels of endogenous steroid the agent being delivered, enhance delivery times, reduce hormones Such as those described above, adrenal insuffi the dosages delivered, reduce the Side effects from various ciency leads to reduced levels of dehydroepiandrosterone delivery methods, reduce patient reactions, and So forth. (DHEA) in men and women. The adrenal glands are also 0011. In this regard, penetration enhancers have been involved in the production of many hormones in the body, used to increase the permeability of the dermal Surface to including DHEA and SeX hormones Such as estrogen and drugs, and are often proton accepting Solvents Such as testosterone.
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