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(12) Patent Application Publication (10) Pub. No.: US 2008/0317844 A1 Dudley Et Al

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(12) Patent Application Publication (10) Pub. No.: US 2008/0317844 A1 Dudley Et Al US 20080317844A1 (19) United States (12) Patent Application Publication (10) Pub. No.: US 2008/0317844 A1 Dudley et al. (43) Pub. Date: Dec. 25, 2008 (54) PHARMACEUTICAL DELVERY SYSTEMS Related U.S. Application Data FOR HYDROPHOBC DRUGS AND COMPOSITIONS COMPOSITIONS (60) Provisional application No. 60/671,454, filed on Apr. COMPRISING SAME 15, 2005, provisional application No. 60/721,971, filed on Sep. 30, 2005. (75) Inventors: Robert E. Dudley, Rosemary Beach, IL (US); Panayiotis P. Constantinides, Gurnee, IL (US) Publication Classification (51) Int. Cl. Correspondence Address: A69/48 (2006.01) FOLEY AND LARDNER LLP A6II 3/56 (2006.01) SUTESOO A6IP 5/00 (2006.01) 3OOOK STREET NW WASHINGTON, DC 20007 (US) (52) U.S. Cl. .......... 424/456; 514/179; 514/170: 514/171 (73) Assignee: Clarus Therapeutics, Inc., Northbrook, IL (US) (57) ABSTRACT (21) Appl. No.: 11/911,446 A drug delivery system for oral administration of hydropho PCT Fled: Apr. 14, 2006 bic drugs with enhanced and extended absorption and (22) improved pharmacokinetics is provided. In one embodiment, (86) PCT NO.: PCT/USO6/142O7 formulations comprising testosterone and testosterone esters, e.g., testosterone palmitate, are disclosed. Methods of treat S371 (c)(1), ing a hormone deficiency or effecting male contraception (2), (4) Date: Nov. 12, 2007 with the inventive formulations are also provided. Patent Application Publication Dec. 25, 2008 Sheet 1 of 15 US 2008/0317844 A1 FIGURE 1 es iNpf Normal Range g t wer 9 s O CD s s was s Lower Limit of Nortarange O 72 76 80 84 88 92 96 100 104 108 112 116 120 24 128 132 136 140 144 Time (hr) Patent Application Publication Dec. 25, 2008 Sheet 2 of 15 US 2008/0317844 A1 FIGURE 2 ah - 9. 1 o w s O () " (s wV t C E iower Limit of Normat Range O 72 76 80 84 88 92 96 100 104 108 112 116 120 124 128 132 136 140 144 Time (hr) Patent Application Publication Dec. 25, 2008 Sheet 3 of 15 US 2008/0317844 A1 FIGURE 3 an - Upper Limit of Normal Rang g 1 o C WM t s O O T s E t Lowerint of Normal Range 72 76 80 84 88 92 96 100 104 108 112 116 120 124 128 132 136 140 144 Time (hr) Patent Application Publication Dec. 25, 2008 Sheet 4 of 15 US 2008/0317844 A1 FIGURE 4 Upper limit of Normal Range 1-n - O a. o Mr. () () S O C) "C Gy w E () Lower Limit of Normal Range 72 76 80 84 88 g2 96 100 104 108 112 116 120 124 128 132 136 140 144 Time (hr) Patent Application Publication Dec. 25, 2008 Sheet 5 Of 15 US 2008/0317844 A1 FIGURE 5 Agha - 9. 10 O) C . M U O O o s s E D 72 76 80 84 88 92 96 100 104 108 112 116 120 124 128 132 136 140 144 Time (hr) Patent Application Publication Dec. 25, 2008 Sheet 6 of 15 US 2008/0317844 A1 FIGURE 6 as - 9. 1 W O O C und s E () Lower Limit of Normal Range 72 76 80 84 88 92 96 OO 104 108 112 16 120 124 128 132 136 140 144 Time (hr) Patent Application Publication Dec. 25, 2008 Sheet 7 of 15 US 2008/0317844 A1 FIGURE 7 a Upper Limit of Normal Range 9. 1 O C We 9 O C s () w E Lower Limit of NortaTRange O 72 76 80 84 88 92 96 100 104 108 112 16 120 124 128 132 136 140 144 Time (hr) Patent Application Publication Dec. 25, 2008 Sheet 8 of 15 US 2008/0317844 A1 FIGURE 8 Upper Limit of Normal Range ma - s wr O d C und E of) Lower Limit of Normal Range O 72 76 80 84 88 92 96 100 104 108 112 116 120 124 128 132 136 140 144 Time (hr) Patent Application Publication Dec. 25, 2008 Sheet 9 of 15 US 2008/0317844 A1 FIGURE 9 -e- Formulation it 9 o-E-Formulation #23 - A - Formulation #24 60 40 20 Patent Application Publication Dec. 25, 2008 Sheet 10 of 15 US 2008/0317844 A1 FIGURE 10 120 100 80 60 40 -0-Formulation ii 47 -E-Formulation #50 20 -A-Formulation #51 -G-Formulation #54 1. 2 3 4. 5 Time (hours) Patent Application Publication Dec. 25, 2008 Sheet 11 of 15 US 2008/0317844 A1 FIGURE 11 -E-50 QD -A- 54 BO Time (hr) Patent Application Publication Dec. 25, 2008 Sheet 12 of 15 US 2008/0317844 A1 FIGURE 12 Time (hr) Patent Application Publication Dec. 25, 2008 Sheet 13 of 15 US 2008/0317844 A1 FIGURE 13 -e- 54 BO -E-5O BID Sinn Time (hr) Patent Application Publication Dec. 25, 2008 Sheet 14 of 15 US 2008/0317844 A1 FIGURE 14 OO 60 -9-62A -A-64A -6-70 -E-71 40 Time (Hours) Patent Application Publication Dec. 25, 2008 Sheet 15 of 15 US 2008/0317844A1 FIGURE 15 90 A===s== 80 uta- ass 70 60 50 40 30 -6-62A - A-64A -e- 70 10 -- 71 -O-71A -g- 78 Time (Hours) US 2008/0317844 A1 Dec. 25, 2008 PHARMACEUTICAL DELVERY SYSTEMS prises a lipophilic surfactant that provides for the controlled FOR HYDROPHOBC DRUGS AND release of TP. said lipid components together providing for COMPOSITIONS COMPOSITIONS the solubilization of TP. The pharmaceutical composition COMPRISING SAME may further comprise at least three lipid components at least the first of which comprises a hydrophilic surfactant, at least CLAIM OF PRIORITY the second of which comprises a lipophilic Surfactant that 0001. This application claims priority to U.S. provisional provides for the controlled release of TP and at least the third of which comprises a lipophilic surfactant that further pro application Nos. 60/671,454 filed Apr. 15, 2005 and 60/721, vides for the solubilization of TP. As well, the pharmaceutical 971 filed Sep. 30, 2005, both of which disclosures have been composition may further comprise a second lipid-soluble incorporated by reference herein in their entirety. therapeutic agent, Such as a synthetic progestin. Formulations FIELD OF THE INVENTION comprising same may be preferably in the form of an orally active male contraceptive. 0002 The present invention relates generally to pharma 0008. The first lipid component may exhibit an HLB of 10 ceutical delivery systems of hydrophobic drugs and compo to 45, preferably 10 to 30, and more preferably 10 to 20. The sitions comprising same. More particularly, the present second lipid component may exhibit an HLB of less than invention relates to pharmaceutical compositions comprising about 10, preferably less than about 7, and more preferably testosterone and esters thereof with enhanced and extended less than about 5. Further, the second lipid component may absorption and pharmacokinetics. exhibit a melting point in the range of about 25°C. to about 80° C., preferably about 35° C. to about 65° C., and more BACKGROUND OF THE INVENTION preferably about 40° C. to about 60° C. The second lipid 0003. Many pharmaceutically active compounds intended component may be chosen from the group consisting of for oral administration are poorly soluble in water providing stearic acid, palmitic acid, glycerol and PEG esters thereof, a challenge to formulate these drugs in a drug delivery system Precirol ATO 5 and Gelucires. that exhibits the desirable pharmacokinetic profiles in vivo. 0009. In some embodiments, the lipophilic surfactant fur Poor oral bioavailability may lead to ineffective therapy, the ther comprises a “sustained’ or controlled-release' surfactant need for higher dosing and/or undesirable side effects. As which may be chosen from the group consisting of Stearic well, pharmaceutical preparations with relatively short half acid, palmitic acid, glycerol and PEG esters thereof. Precirol lives require frequent dosing at the expense of patient incon AT05, Imwitor 191, Myverol 18-06, Imwitor 370, Imwitor Venience and higher therapy costs. 375, Caprol ET, Cithrol 2MS, Marosol 183 and combinations 0004 Sex hormones (e.g., testosterone and its esters) are thereof. The hydrophilic surfactant may be a poloxyl deriva marginally water Soluble, and attempts have been made to tive of castor oil. Commercially available products of this increase their bioavailability, particularly when taken orally. class are Supplied under the tradenames, Cremophor or Eto However, administration of testosterone, per se, presents cas and include, Cremophor EL and RH 40 and Etocas 35 and additional challenges. Indeed, while testosterone given by 40. Chemophor, RH40 or Etocas 40 are preferred. mouth is essentially completely absorbed into the portal cir 0010 Compositions of the present invention may com culation, because of extensive first-pass hepatic metabolism, prise, based on weight, 10-70% alipophilic surfactant; 1-40% the serum concentration of testosterone following this route a controlled release surfactant; and 5-60% a hydrophilic sur of administration is low unless very large doses are adminis factant; and preferably 30-50% alipophilic surfactant; 5-25% tered. To overcome this problem, attempts have been made to a controlled release surfactant; and 30-40% a hydrophilic alkylate testosterone at the C-17 position (e.g., with a methyl surfactant. The compositions further comprise about 5 to group to form methyltestosterone) thereby reducing metabo about 50 percent, by weight, testosterone palmitate, prefer lism by the liver. Unfortunately, however, mere alkylation of ably, about 20 to about 40 percent, by weight, testosterone testosterone has not yielded desirable bioavailability and has palmitate. The inventive pharmaceutical compositions may been associated with potentially serious hepatotoxicity. also comprise one or more cosolvents and/or filled into a hard 0005.
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