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(12) Patent Application Publication (10) Pub. No.: US 2002/0012674 A1 SAETTONE Et Al

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(12) Patent Application Publication (10) Pub. No.: US 2002/0012674 A1 SAETTONE Et Al US 2002001.2674A1 (19) United States (12) Patent Application Publication (10) Pub. No.: US 2002/0012674 A1 SAETTONE et al. (43) Pub. Date: Jan. 31, 2002 (54) BIOADHESIVE COMPLEXES OF (30) Foreign Application Priority Data POLYCARBOPHILAND AZOLE ANTIFUNGAL OR ANTIPROTOZOAL Aug. 2, 1996 (IT).................................. RM96AOOO559 DRUGS Publication Classification (76) Inventors: MARCO FABRIZIO SAETTONE, PISA (IT); LUANA PANICHI, PISA (51) Int. Cl." ....................................................... A61K 9/00 (IT); BORIS GIANNACCINI, PISA (52) U.S. Cl. .............................................................. 424/400 (IT); ENRICO BOLDRINI, PISA (IT): PIETRO BIANCHINI, PISA (IT) (57) ABSTRACT Mucoadhesive antimicrobial complexes of polycarbophil, Correspondence Address: i.e. a croSS-linked polyacrylic acid with bioadhesive prop JOSEPH A DEGRANDI erties, and an imidazole or triazole derivative with antifungal SMITH GAMBRELL & RUSSELL or antiprotozoal activity, in its basic form, for use in the BEVERIDGE DEGRAND WELACHER & topical treatment of mucosal affections. The complexes are YOUNG obtainable by dissolving each of the two starting products in 1850 M STREET NW SUTE 800 a common Solvent, then joining together the two Solutions in WASHINGTON, DC 20036 relative amounts Such as to contain the Same number of equivalents of the two starting products, evaporating the (*) Notice: This is a publication of a continued pros Solvent and then drying and, if required, pulverizing and ecution application (CPA) filed under 37 Sieving the product So obtained. CFR 1.53(d). Particularly preferred are formulations in gel in propylene (21) Appl. No.: 09/230,863 glycol comprising an econazole-polycarbophil or omocona Zole-polycarbophil complex, with an excess of polycarbo (22) PCT Filed: Jul. 25, 1997 phil, together with pharmaceutically acceptable carrier and excipient Substances, for use as Sustained release antifungals (86) PCT No.: PCT/IT97/001.87 for vaginal administration. Patent Application Publication Jan. 31, 2002. Sheet 1 of 6 US 2002/0012674 A1 TEMPERATURE (C) 15O 130 1 O 90 7O 5O --|--|-- b 1 N 3. econazole (base) b econazole - polyCarbOphil F.G. 1 Patent Application Publication Jan. 31, 2002. Sheet 2 of 6 US 2002/0012674 A1 TEMPERATURE (C) -T-I-T-I- r d C C d O O C. B 2 X O b--Na. C clotrimaZOle (base) clotrimazole-polycarbophil metronidazole (base) metronidazole-polycarbophil FIG. 2 Patent Application Publication Jan. 31, 2002 Sheet 3 of 6 US 2002/0012674 A1 TEMPERATURE (°C) i8O 160 140 120 OO 80 60 ------ s E 3 ?t S X O a. v assausaramanamomorphanowhere. b "ram-lar" a omoconazole (base) b omoconazole-polyCarbophil FIG. 3 Patent Application Publication Jan. 31, 2002 Sheet 4 of 6 US 2002/0012674 A1 60 4 O O 5 O 15 2O Time, hours O econazole-polycarbophil Complex KX physical mixture FIG. 4 Patent Application Publication Jan. 31, 2002. Sheet 5 of 6 US 2002/0012674 A1 n Time, hours o FORMULATION A (with the econazole-polycarbophil Complex) o FORMULATION B (with econazole (base)) F.G. 5 Patent Application Publication Jan. 31, 2002 Sheet 6 of 6 US 2002/0012674 A1 'sS 2s2,5- <> 2 K> O) 2 s s “C 15 - C 2 S 1 - KX S KX C 0.5 C O O t w N cy r () CO N Time, hours O FORMULATION A (with the Omoconazole-polycarbophil Complex) & FORMULATION B (with Omoconazole (base)) FIG. 6 US 2002/0012674 A1 Jan. 31, 2002 BOADHESIVE COMPLEXES OF 0005 Among the antifungal drugs mentioned above, POLYCARBOPHILAND AZOLE ANTIFUNGAL OR econazole, i.e. 1-2-(4-chlorophenyl)methoxy-2-(2,4- ANTIPROTOZOAL DRUGS dichlorophenyl)ethyl)-1H-imidazole, is particularly wide 0001. The present invention concerns bioadhesive com Spread and extensively tested. It has been Synthesised by plexes of polycarbophil and azole antifungal or antiproto Godefroi et al. in 1969 (J. Med. Chem., 12, 1969, 784, and Zoal drugs. More specifically, the invention relates to the U.S. Pat. No. 3,717.655). The antimicrobial activity of formulation of a complex of a cross-linked polyacrylic acid econazole, which has been extensively shown in vitro, is having remarkable mucoadhesive properties, known with exerted against a wide variety of fungi and against Some the name of polycarbophil, and an imidazole or triazole gram-positive bacteria, while no activity on gram-negative derivative having antifungal or antiprotozoal activity, in the bacteria is present. The main site of the antimicrobial action is represented by the cellular membrane System, Similarly to base form, for use in the topical treatment of mucosal what happens for the other imidazole antifungal agents. In affections. vitro tests with Trichophyton rubrum, Saccharomyces cer 0002. As it is known, the diseases of a microbial origin evisiae, and Candida albicans have shown an increase in the affecting the mucous membranes, which may be treated by permeability of the cell covering exposed to econazole. Said exploiting the trans-mucosal administration route, are many increase occurs both in the growing and in the grown-up and widespread. In particular, among the diseases of this cells, thus showing that the antimicrobial activity is due to kind which affect the urogenital System, the mycotic infec an action on the formed membranes, and not to the forma tions are very common, and among these, Specifically, the tion of defective membranes in the growth phase. The main candidiases. action of the drug is the inhibition of 14-O-demethylase, a 0.003 Candida albicans represents the species belonging cytochrome Piso-dependent microSomial enzyme System to the Candida genus which is most commonly involved in important for the Synthesis of Sterols. The Said action has human candidiases, and is the only Species pathogenic on two effects: it causes a build-up of 14-O-methylsterols, and laboratory animals. The Said Species is held to be responsible compromises the Synthesis of ergosterol, which is necessary of most Superficial mycoses (muco-cutaneous mycoses) and to the cytoplasm membrane. The built-up methylsterols may of Some Serious deep mycoses, and is commonly present on desegregate the close packing of the phospholipids acyl the mucous membranes Surfaces, Such as those of the buccal chains, thus compromising the functions of Some enzyme cavity and of the gastrointestinal tract in man, in equilibrium Systems connected to the membrane. with the endemic flora of the said regions. In the healthy 0006 Econazole is used mainly for topical administration population equilibrium conditions are normally established in the treatment of vaginal dermatomycoses and candidiases. between the invasive potential of the fungus and the defence Several medicinal products containing econazole as the mechanisms of the host, which are able to limit the tissue active ingredient are present on the market, Specially for invasion and, possibly, to eradicate the infection from the vaginal administration. In most of the Said medicinal prod mucous membranes Surface. The onset of a pathological ucts econazole is not present as the base, but in the form of proceSS is the consequence of the breach of Such equilib its nitrate Salt. rium, and this may be either due to the different virulence of the infecting yeast or to the reduced resistance of the host. 0007 Another kind of microbial diseases which have The importance of the host defence mechanisms, both been treated with therapies based on azole active ingredi natural and acquired, against candidiases is strongly con ents, to be administered normally through the trans-mucosal firmed by the incidence of fungal infections, and, Specifi route, are the infections caused by protozoa of the genus cally, candidiases, in immunocompromised Subjects. Tnchomonas. These infections generally occur in Women, as 0004. The candidiases of the urogenital system, much cervicites, vaginites and Vulvovaginites, which may also be more widespread in Women than in men, are characterised asSociated with candidiases or with other bacterial infec by itch and discharge and, upon clinical examination, by tions. The active ingredient of choice for trichomoniases is erythema, edema and, Sometimes, ulcerous or papular metronidazole, which also belongs to the group of imidazole lesions. Epidemiologic Statistics on the incidence of vaginal derivatives. For the topical treatment of infections caused by candidiases are difficult to establish, although it may be Trichomonas, both in the man and in the woman, metron considered that the Said incidence has greatly increased in idazole is advantageously combined with an imidazole the last few years, also due to a wider use of hormone derivative having mainly an antifungal action, i.e. clotrima contraceptives and of antibiotic antimicrobials. Candidiases, Zole. and in general all of the fungal affections of the urogenital 0008. The conventional administration forms used for the System, may be therapeutically treated with antimicrobial topical antimicrobials of the kinds referred to above are most drugs for topical use, Specifically imidazole derivatives Such commonly creams, Suppositories for vaginal administration as econazole, tioconazole, miconazole and the like, or tria (pessaries, inserts, ovules) and tablets. In the case of econa Zole derivatives Such as terconazole, or also with drugs for Zole, for instance, there are commercially available pessaries oral administration, in particular of the triazole type, Such as and creams based on econazole nitrate, which represent the fluconazole. It is usually recommended to initially use the preparations of choice. as well as douches (lavages) and topical azole therapy,
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