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(12) United States Patent (10) Patent No.: US 7,163,699 B2 Besse (45) Date of Patent: Jan

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(12) United States Patent (10) Patent No.: US 7,163,699 B2 Besse (45) Date of Patent: Jan US007163699B2 (12) United States Patent (10) Patent No.: US 7,163,699 B2 Besse (45) Date of Patent: Jan. 16, 2007 (54) PROGESTIN CO-MICRONIZED WITH A A6IR 9/16 (2006.01) SURFACTANT PHARMACEUTICAL A69/20 (2006.01) COMPOSITION COMPRISING SAME A69/48 (2006.01) METHODS FOR MAKING SAME AND USES (52) U.S. Cl. ...................... 424/489: 424/465; 424/456: THEREOF 424/484 (75) Inventor: Jerome Besse, Listrac Medoc (FR) (58) Field of Classification Search ................ 424/489, (73) Assignee: Laboratories Besins International, 424/465, 484, 456 Paris (FR) See application file for complete search history. (*) Notice: Subject to any disclaimer, the term of this (56) References Cited patent is extended or adjusted under 35 U.S.C. 154(b) by 284 days. U.S. PATENT DOCUMENTS 4,196,188 A 4, 1980 Besins (21) Appl. No.: 10/469,441 4,895,726 A 1/1990 Curtet et al. 6,063,404 A 5/2000 Timpe et al. (22) PCT Filed: Feb. 27, 2002 6,086,916 A 7/2000 Agnus et al. 6,124,358 A 9, 2000 Estanove et al. (86). PCT No.: PCT/FRO2/OO714 FOREIGN PATENT DOCUMENTS S 371 (c)(1), FR 2 775 599 3, 1998 (2), (4) Date: Feb. 10, 2004 WO WO 89.02742 10, 1988 WO WOOO,2897O 11, 1999 (87) PCT Pub. No.: WO02/069978 Primary Examiner Edward J. Webman PCT Pub. Date: Sep. 12, 2002 (74) Attorney, Agent, or Firm—Foley & Lardner LLP (65) Prior Publication Data (57) ABSTRACT US 2004/O131553 A1 Jul. 8, 2004 The invention concerns a progestin co-micronized with a (30) Foreign Application Priority Data Surfactant and a pharmaceutical composition comprising Mar. 1, 2001 (FR) ................................... O1 O2814 said gestagenic. The invention also concerns methods for preparing Same. (51) Int. Cl. A6 IK 9/14 (2006.01) 36 Claims, 2 Drawing Sheets 5 O O 2O 4O SO 8O 1OO 2O AO SO 18O TIME (Inn.) -- PROGESTERONE + SLS COMiGRONISEDC 100mg PROGESTERONE) -- PROGESTERONE NOT COMiCRONSED 100ing PROGESTERONE) g- PROGESTERONE SLS COMICRONISED 200mg PROGESTERONE) A PROGESTERONE NOT COMicRONiSED (200mg PROGESTERONE) US 7,163,699 B2 1. 2 PROGESTIN CO-MICRONIZED WITH A estrogenic effect (a consequence of which is hyperestro SURFACTANT PHARMACEUTICAL genism: hot flushes, psychogenic difficulties such as anxiety COMPOSITION COMPRISING SAME or depression, weight gain, etc.). This progesterone insuffi METHODS FOR MAKING SAME AND USES ciency may lead to functional impairment and various THEREOF clinical manifestations, in particular: premenstrual syndromes, The present invention relates, as a new product, to a menstrual irregularities through disovulation or anovula progestin co-micronized with a Surfactant, to a pharmaceu tion, tical composition containing same, to methods for preparing benign mastopathies, same, and also to uses thereof. 10 perimenopause and menopause. In the context of the present invention, the term “proges The use of hormone replacement therapy is well estab tin' is intended to mean any steroid having affinities for lished to date for relieving menopausal symptoms. Given progesterone receptors and capable of more or less fully that it has been demonstrated that progestins prevent the reproducing the biological effects of progesterone. development of hyperplasia and endometrial cancer, sequen A progestin is a compound capable, by definition, of 15 tial or combined therapy with estrogens and progestins is maintaining gestation and of promoting implantation of the advised in menopausal women who have not undergone a egg. This biological role is reflected essentially by a change hysterectomy. Among progestins suitable for hormone in the vaginal mucosa (desquamation), in the endometrium replacement therapy, micronized progesterone is preferably (cell proliferation, formation of the uterine lining), and in the used due to its lack of androgenic effect and its metabolic endocervical glandular epithelium (decrease in the produc innocuity. tion of glairy mucus and thickening thereof). However, oral administration of progesterone suffers from The only property that all progestins have in common is a serious handicap due to the considerable metabolizing their endometrial action. thereof in the liver. The effect on gestation is real for progesterone and very Now, the oral administration method has clear advantages inconstant with synthetic progestins. 25 compared to other methods of its administration. Specifi Progestins comprise progesterone and also synthetic cally, it is, firstly, more practical than vaginal administration progestins. The latter may be classified into three groups and, secondly, it allows a dose to be taken independently, (unofficial classification) according to their biological activi which is impossible with parenteral administration. ties (and their structure, which determines said activities): LABORATORIES BESINS-ISCOVESCO have already the order of classification thus takes into account their 30 proposed a solution to this problem of progesterone degra structural difference relative to physiological progesterone. dation, in patent application FR 76 36007. Specifically, they The first group comprises molecules similar to progest have developed a formulation of soft capsules containing erone or synthetic progestins 1 (SP1) (pregnanes), for progesterone micronized in oily Suspension, which allows example the progesterone isomer (retroprogesterone), improved bioavailability of the progesterone. Medrogesterone, norprogesterone derivatives (demegestone 35 The method for preparing Such capsules proves, however, or promegestone). These molecules have peripheral extrag to be complex and expensive to carry out, and also requires estative activity which is virtually identical to progesterone, considerable know-how. Attempts have therefore been made and have no androgenic effects. to develop alternative effective, but also economically The second group comprises 17O-hydroxyprogesterone viable, formulations such as progesterone-based tablets (see derivatives or synthetic progestins 2 (SP2) (pregnanes), for 40 patent applications FR97 16168 and FR 98 02830). example cyproterone acetate and medroxyprogesterone However, there is still a need to find pharmaceutical acetate. These molecules have more powerful and more formulations containing progesterone or another progestin intense peripheral gestative activity than that of progester and having improved bioavailability. one and, in addition, have an androgenic effect. In general, the bioavailability of an active principle can be The third group comprises the norsteroids or synthetic 45 improved by chemical means: administration of prodrugs, progestins 3 (SP3) (estranes or norandrostanes). These are complexation, combination with lipids or phospholipids, 19-nortestosterone derivatives, for example norethindrone. most often in the presence of a Surfactant; or by physical These molecules have particularly powerful peripheral ges means such as micronization. tative activity (this is the group of synthetic progestins Micronization is a well-known technique which can be which has the most pronounced endometrial action) and also 50 carried out either in hammer or ball mills or in gas jet have an androgenic effect. From these norandrostanes or micronizers. As was recalled above, the micronization tech estranes are derived molecules of the gonane type containing nique has already been used (see BESINS patent FR 76 a methyl group at C18 and an ethyl group at C13. Examples 36007) to develop a composition based on progesterone that may be mentioned include norgestimate (levonorg which is bioavailable and which can be administered orally. estrel), desogestrel (3-keto desogestrel) and gestodene. 55 Patent application FR 2757 397 also recalls this fact and These chemical modifications increase the endometrial Subsequently indicates, on page 2, that co-micronization of power and decrease the intrinsic androgenic activity of the phenofibrate in the presence of sodium lauryl sulfate has molecule. already been described in patent EP 330532. However, that Progesterone is a hormone which is synthesized, in patent application underlines, at the same time, the fact that women, essentially by the ovary during the post-ovulatory 60 it is not automatic and inescapable that the bioavailability of or luteal (yellow body) phase and, to a lesser degree, by the an active principle is systematically improved by co-mi adrenal glands and the placenta during the second part of cronization in the presence of a Surfactant. Thus, the inven pregnancy. A non-endocrine synthesis of progesterone, in tors of that patent application recall that M. OTSUDA et al. particular in the neurones, is also possible. (JPS 84, 1995, p. 1434–37) studied the micronization of The consequence of insufficiency of progesterone secre 65 phenitoin in the presence of a Surfactant and that they tion in women is a loss of its biological effects: progestin showed that the solubility of phenitoin is not improved in the effect; anti-androgenic effect (action on the skin) and anti case of co-micronization with a Surfactant Such as sodium US 7,163,699 B2 3 4 lauryl Sulfate or a Sucrose ester of Stearic acid, whereas it is A Subject of the invention is also a pharmaceutical com multiplied by 30 compared to the mixture of powders in the position comprising the progestin co-micronized with a case of co-grinding with sodium deoxycholate. surfactant as described above. The same authors underlined moreover which is According to an advantageous embodiment, the pharma entirely relevant—that even though micronization or grind ceutical composition in accordance with the invention ing of a Substance
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