Drug – bio-affecting and body treating compositions – Preparations characterized by special physical form – Biocides; animal or insect repellents or attractants
Patent
1995-06-13
1998-09-29
Lovering, Richard D.
Drug, bio-affecting and body treating compositions
Preparations characterized by special physical form
Biocides; animal or insect repellents or attractants
252312, 252314, 424423, 514383, 514938, A01N 2504, A61K 3141, B01J 1300
Patent
active
058143246
DESCRIPTION:
BRIEF SUMMARY
This application is a 371 of PCT/JP95/00260 filed Feb. 23, 1995.
TECHNICAL FIELD
The present invention relates to injectable compositions containing a triazole compound useful as antifungal therapeutic agents (antimycotics) and methods of producing the same.
BACKGROUND ART
Recently, there have been found increasing numbers of profunda fungal infections caused by fungi such as those belonging to the genus Candida, the genus Aspergillus and the genus Cryptococcus, specifically as a complication in, for example, a patient transplanted with an organ, a patient administered with a large quantity of an antibiotic, an anticancer drug (cartinostatic) or a steroidal agent in a long period, a patient suffering from AIDS, or a patient suffering from cancer in terminal stage ("Medical Mycology", Harukuni Urabe, Tadahiko Matsumoto and Shozo Motofusa, published on Jun. 10, 1993, Kanehara Publishing Co., Ltd., Japan). Against these profunda fungal infections, various azole drugs having antifungal functions or activities due to, for instance, inhibition of ergosterol synthesis in fungal cell membrane or disturbance of double membranes of the cell membrane have been researched and developed in 1980's, and some of these drugs have already been on the market (Hideyo Yama-guchi, Nippon Rinsho, 49, 2176-2185 (1991)).
There have been known, as triazole antifungal agents among azole antifungal agents, fluconazole, itraconazole, saperconazole, D0870 (1047, Abstract of the 1992 ICAAC) and so on. Further, a compound shown by the general formula (I) described in EP-A1-0567982 is expected as a novel triazole compound having antifungal activity.
These triazole compounds, however, generally have poor water-solubility, and therefore, can hardly be formulated into a composition for intravenous administration. Such drugs which are poorly or sparingly soluble in water can be solubilized by, for instance, solubilizing with a clathrate or inclusion compound such as cyclodextrin, dissolving in a water-soluble solvent such as polyethylene glycol, or solubilizing with using a surfactant such as polyoxyethylene hardened castor oil and the like. These liquid preparations, however, have been limited for an application as a medicine, since the solubilizing agent in itself has some toxicity and large quantity of such solubilizing agent is required in the preparations. Therefore, development of methods for preparing an injectable composition having higher safety is a principle problem in such triazole compounds.
The EP-A1-0567982, regarding to a pharmaceutical preparation (composition) containing the triazole compounds, discloses that the triazole compound can be formulated into an aqueous injection together with a dispersing agent, a preservative, an isotonic agent or the like, and that the compound can be formulated into an oily injection by dissolving, suspending or emulsifying in a plant oil (vegetable oil) such as soybean oil, propylene glycol and the like. In such triazole compounds having poor solubility not only in water but also in an oil, however, the drug concentration in an injection can hardly be increased.
EP-A1-315079 corresponding to Japanese Patent Application Laid-open No. 203/1990 (JP-A-2-203) discloses a drug carrier in the form of a fat emulsion, which contains a drug and has a mean particle diameter of less than 200 nm, preferably not less than 5 nm to less than 200 nm, and particularly preferably less than 100 nm. The drug carrier comprises a substance as the core and a substance as the surface layer of the emulsion. The core substance of the fat emulsion includes a simple lipid, a derived lipid, a drug itself or a mixture thereof, and a proportion of the core substance in the drug carrier is 30 to 85%. The substance constituting the surface layer of the fat emulsion is a complex lipid, a derived lipid, a drug itself or a mixture thereof and a ratio of the surface layer substances in the drug carrier is 15 to 70%.
WO91/07962 discloses an emulsion comprising (a) 0.001 to 10% (W/V) of an imidazole antifungal agent (miconazo
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Iwasa Susumu
Sato Jun
Watanabe Akiko
Lovering Richard D.
Takeda Chemical Industries Ltd.
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