초록

This invention provides for novel antiparasitic and pesticidal forms of moxidectin, including a long-acting polymeric implant. The resulting compounds may be used in veterinary compositions which are used in treating, controlling and preventing of endo- and ectoparasite infections in animals.

대표청구항 ▼

1. Polymorphic A form of moxidectin having a melting point of 210° C. 2. Moxidectin.2EtOH solvate characterized by the following parameters: a) monoclinic P21 space group with theb) a=11.2731(15) Å;c) b=8.9286(12) Å;d) c=21.955(3) Å;e) β=93.623(2)°;f) V=2205.4(5) Å3;g) Z=2. 3. Moxidectin.1.5BuOH sol

1. Polymorphic A form of moxidectin having a melting point of 210° C. 2. Moxidectin.2EtOH solvate characterized by the following parameters: a) monoclinic P21 space group with theb) a=11.2731(15) Å;c) b=8.9286(12) Å;d) c=21.955(3) Å;e) β=93.623(2)°;f) V=2205.4(5) Å3;g) Z=2. 3. Moxidectin.1.5BuOH solvate. 4. Moxidectin.2IPA solvate. 5. A process for making a moxidectin crystal form having a melting point of 210° C., comprising either the step of heating amorphous moxidectin under specific conditions of temperature and time, or the step of rapidly desolvating the moxidectin solvate of claim 2, thereby making the crystal form. 6. A long-acting polymeric implant for non-human animals comprising PLGA and the crystalline form or solvate of moxidectin as set forth in any one of claims 1 to 4. 7. The implant of claim 6 wherein the PLGA has an L:G ratio of about 50-75% to about 25-50% L:G. 8. The implant of claim wherein the L:G ratio is 75:25. 9. The implant of claim 8 which is active against endoparasites for a period of greater than 3 months. 10. The implant of claim 9 which is active against endoparasites for a period of greater than 4 months. 11. The implant of claim 10 which is active against endoparasites for a period of greater than 6 months. 12. The implant of claim 6 wherein the endoparasites are heartworms. 13. The implant of claim 6 wherein the animals are cats or dogs or cattle. 14. A composition for the treatment or prevention of a parasitic infection in an animal comprising the moxidectin crystal form of any one of claims 1 to 4, or a pharmaceutically acceptable salt thereof, a pharmaceutically acceptable carrier, and an antioxidant. 15. The process of claim 5, wherein the heating of the amorphous moxidectin is carried out from about 180 to about 210° C., to yield the Polymorphic A form of moxidectin. 16. The process of claim 15, wherein the heating is carried out at about 190° C.