60 results about "Moxidectin" patented technology

The invention discloses a trace element solution, which comprises at least one metal selected from the group comprising selenium, copper, zinc, manganese and chromium; and at least one component selected from the group comprising a vitamin, a vaccine, a growth stimulant, a dewormer, iron dextran, an antibiotic and a synchronization preparation. The synchronization preparation is a combination of injectable hormonal preparations, inplantable hormonal preparations, intravaginal hormonal preparation and other slow release hormonal preparation. The antibiotics include oral, injectable and implantable theurapeutic remedies. The vaccine includes antigens and a combination of antigens and adjuvents. The growth stimulants include zeranol, estradiol, testosterone, progesterone and trenbolone acetate. The dewormer includes macrocydic lactones, leramizoles, benzimidazoles and salicylanilides. The macrocydic lactones include doramectin, ivermectin, abamectin and moxidectin.

The invention relates to a method for preparing high-purity Moxidectin, which comprises the following steps: (1) macroporous absorption resin chromatography is carried out on Moxidectin solution which is purified in advance, the obtained product is eluted by the mixed solution of polar organic solvent and water; (2) the eluent is extracted by methylene dichloride, and then solvent is removed by conventional concentration; (3) protective reaction is carried out on the condensate to obtain upper protective liquid; (4) macroporous absorption resin chromatography is carried out on the upper protective liquid, and the chromatography is eluted by the mixed solution of the polar organic solvent and the water; (5) the eluted upper protective liquid is oxidized, and then deprotection and oximation reaction are carried out to obtain the reaction liquid of the Moxidectin; (6) macroporous absorption resin chromatography is carried out on the reaction liquid of the Moxidectin, and the chromatography is eluted by the mixed solution of the polar organic solvent and the water, so that the obtained eluent is the high-purity Moxidectin solution; the product can be separated out of the solution by using the conventional concentration and crystallization technology if necessary. As the macroporous absorption resin chromatography is used for separating instead of silica gel chromatography, the method is not only stable and controllable as well as is easy to industrialize, but also improves the product purity, the quality and the yield.

PCT No. PCT / NZ96 / 00099 Sec. 371 Date Mar. 25, 1998 Sec. 102(e) Date Mar. 25, 1998 PCT Filed Sep. 19, 1996 PCT Pub. No. WO97 / 11709 PCT Pub. Date Apr. 3, 1997A composition comprising an anthelmintic chosen from the class of macrocyclic lactones including but not limited to the avermectins, ivermectin, doramectin, abamectin, milbemycin and moxidectin, together with a vegetable oil and a co-solvent chosen from the group comprising alcohols having four or more carbons atoms. The compositions of the inventions may be formulated as injections, drenches or for topical administration and are suitable for treating helminthiasis in animals.

Methods for the purification of the macrolide moxidectin result in higher purity levels than can often otherwise be obtained. The crystalline moxidectin is then used in a wide variety of pharmaceutical and veterinary applications, including the prevention, treatment and control of parasites in plants, animals and humans.

The present invention provides a stable veterinary oral composition which comprises one or more surfactants, a water-miscible solvent, optionally an oil and an effective amount of each of a benzimidazole antihelmintic compound, such as triclabendazole and a macrocyclic lactone, such as moxidectin. Said composition is useful for treating and controlling endo- and ectoparasitic infection and infestation in a homeothermic animal.

High load concentrate compositions comprising metaflumizone, a substantially water-insoluble anti-parasitic macrolide compound,such as moxidectin, an optional bridging agent, a surfactant, and a suitable carrier solvent are prepared. These compositions may be topically administered to animals, and are useful for preventing or treating ectoparasitic infestations in warm-blooded animals for prolonged periods of time. Additionally, they may be further diluted to provide other types of formulations useable for both topical and oral administration.

A spot-on pesticide composition for animals, specifically mammals, namely dogs, which composition comprises a combination of a pyrethroid and a macrocyclic lactone selected from avermectin, ivermectin, selamectin, moxidectin, milbemycin and any combination thereof, and optionally fipronil and / or an insect growth regulator, in doses and proportions which are parasiticidally effective against a variety of insects and pests, and in a formulation which is convenient for local application to the animal's skin, preferably localized over a small surface area.

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.

The invention provides a novel and environmental-friendly Moxidectin pour sprinkling preparation and an industrialized preparation method thereof. The pour sprinkling preparation developed in the invention is prepared by taking Moxidectin as an active ingredient for resisting parasites inside and out of animals and adding an appropriate amount of auxiliaries, such as an antioxidant, a trandermal absorbent, an adhesive, an oil solvent and the like; and the formulation of the preparation is the oily pour sprinkling preparation and belongs to the field of novel veterinary medicinal antiparasitic preparations. The pour sprinkling preparation does not contain an aromatic compound with a low flash point and the potential safety hazard in industrial production. In order to improve medicinal effect, the trandermal absorbent is selected through an in-vitro trandermal absorption test so as to improve the bioavailability of the Moxidectin pour sprinkling preparation in the animals. The environmental-friendly Moxidectin pour sprinkling preparation which has a long-term effect, and is safe and easy to industrially produce is prepared finally.

The present invention relates to methods of treating a mycobacterial infection. In particular, this invention relates to methods, uses and compounds for use in treating mycobacterial infections, including tuberculosis. For example, the compounds may be an avermectin or a milbemycin. The avermectin or milbemycin may be selected from, but not limited to, one or more of ivermectin, moxidectin or selamectin. Exemplary microbial infections that may be treated include, but are not limited to, infections caused by Mycobacterium tuberculosis, Mycobacterium bovis, other mycobacteria of the tuberculosis complex, and non-tuberculous mycobacteria, including Mycobacterium ulcerans.

The invention provides compound moxidectin drops as well as a preparation method and application thereof. The compound moxidectin drops have the advantages that moxidectin and ingredients with insecticidal effect, such as imidacloprid, are compounded and used, so that the drops have good insecticidal effect; meanwhile, in the drops, propylene glycol, moringa seed oil and eucalyptus oil are taken as transdermal agents, wherein the moringa seed oil and the eucalyptus oil are natural plant essential oil with fragrance and can cover up peculiar smell in the drops and improve sense of a user; and further the drops can be used for killing endoparasite and ectoparasite of animals due to good insecticidal effect. In the preparation method, the components of the drops are taken as raw materials and mixed to prepare corresponding drops, so that the preparation method provided by the invention has the advantages of simplicity, high efficiency, good insecticidal effect of the obtained drops, and the like.

The invention discloses a method for removing by-product dimethyl sulfide in a moxidectin production process, and belongs to the technical field of chemical industry production. The method comprises the following steps: in the production process of moxidectin, after oxidation reaction steps are ended, adding excessive water quenching reaction liquid to oxidation reaction liquid; transferring a by-product dimethyl sulfide generated in the oxidation step and used solvent to a sodium hypochlorite absorption kettle through a condenser in a manner of advocating gas desolvation or negative pressure desolvation; oxidizing and absorbing dimethyl sulfide through a sodium hypochlorite solution in the sodium hypochlorite absorption kettle and recovering a reaction solvent, wherein the content of dimethyl sulfide contained in oxidation reaction can be quickly reduced to 1.0% or less, the solvent recovery rate is greater than 60%, and the method has the advantages of low raw material cost, simple absorption process and the like.

The invention discloses a trace element solution, which comprises at least one metal selected from the group comprising selenium, copper, zinc, manganese and chromium; and at least one component selected from the group comprising a vitamin, a vaccine, a growth stimulant, a dewormer, iron dextran, an antibiotic and a synchronisation preparation. The synchronisation preparation is a combination of injectable hormonal preparations, inplantable hormonal preparations, intravaginal hormonal preparation and other slow release hormonal preparation. The antibiotics include oral, injectable and implantable theurapeutic remedies. The vaccine includes antigens and a combination of antigens and adjuvents. The growth stimulants include zeranol, estradiol, testosterone, progesterone and trenbolone acetate. The dewormer includes macrocydic lactones, leramizoles, benzimidazoles and salicylanilides. The macrocydic lactones include doramectin, ivermectin, abamectin and moxidectin.

The invention discloses a method for separating and purifying moxidectin. The method comprises the step of carrying out separation and purification to obtain the moxidectin of which the purity is 96% or above, wherein a supercritical fluid chromatographic system is adopted, a silica-gel-based filler is used as a stationary phase, supercritical CO2 is used as a mobile phase, and a mixture of methanol, ethanol and acetonitrile is used as an entrainer. The method for separating and purifying moxidectin is simple to operate; and more importantly, by using the supercritical CO2 as the mobile phase, only small amounts of organic solvents are added, thereby reducing the environmental pollution caused by organic solvents, and being green and environment-friendly.

The invention discloses a preparation method of moxidectin. The preparation method comprises the following steps: 1) inoculating a strain in a strain culture medium for culture to obtain spore suspension M1; 2) inoculating the spore suspension M1 in a seed culture medium for culture to obtain seed solution M2; 3) inoculating the seed solution M2 in a fermentation culture medium for culture to obtain primary extract solution M3; 4) performing protection reaction, oxidation reaction, deprotection reaction and oximation reaction to the primary extract solution M3 to obtain the moxidectin, wherein the strain is Streptomyces cyaneogriseus and / or Streptomyces hygroscopicus. By adopting the method, the total yield of the prepared moxidectin is enabled to be obviously higher and thus the effects of simpler and more convenient production manner and higher yield are realized.

The invention relates to a moxidectin preparation and a preparing method of the moxidectin preparation. The moxidectin preparation and the preparing method of the moxidectin preparation are efficient and can be stored for long time. The moxidectin preparation comprises, by weight, 100-300 parts of moxidectin, 1-5 parts of rhodium coordination compounds, 1-5 parts of preservative, 500-700 parts of water, 5-10 parts of surface active agents, 100-400 parts of methanol, and 10-50 parts of ethyl acetate. In the preparing process, the temperature of fermentation liquor rises to 600 DEG C at first, then fermentation liquor filter aid is added, plate-frame pressure filtration is carried out to collect filter cakes, filter liquid is left for sewage treatment, the filter cakes are dried to obtain dry mycelia, stock solution is obtained after procedures of digestion, resin absorption, elution and centrifugation, and the moxidectin preparation is obtained after granulation, drying and packaging.

The invention provides a purification method for moxidectin. The purification method comprises the steps: mixing a moxidectin crude product with a solvent and adding an antioxidant; stirring the mixture at 60-80 DEG C to prepare a solution; and then adding a solventing-out reagent and finally drying mixture under the vacuum condition through cooling crystallization to obtain high purity moxidectin with the purity being over 96%. The purification method for moxidectin provided by the invention has the advantages of short crystallization time, low cost and high yield and provides a novel method for improving the purity of moxidectin.

The invention discloses an imidacloprid and moxidectin dihydric alcohol plastid and a preparation method and application thereof. An insect repellent preparation is prepared from the following components: imidacloprid, moxidectin, soybean lecithin, dihydric alcohol (including ethanol and propylene glycol), polysorbate-80 and a phosphate buffer solution. It is confirmed by animal experiments that the imidacloprid and moxidectin dihydric alcohol plastid preparation has the effect of resisting in-vivo and in-vitro parasite infection in dogs and cats. Meanwhile, compared with an imidacloprid and moxidectin compound transdermal agent, the toxicity of the imidacloprid and moxidectin dihydric alcohol plastid preparation is greatly reduced, and the advantages such as good skin permeability, biologically slow release, longer action time and comparatively excellent treatment effect are achieved.

The invention relates to a purification method of a crude moxidectin product. The purification method comprises the following process steps: dissolving the crude moxidectin product, performing resin adsorption, crystallizing and drying to obtain a pure moxidectin product. By the purification method, moxidectin is extracted and purified through the resin adsorption, impurities in the moxidectin are removed to the maximum extent, the finished product content of the moxifloxacin is effectively increased, the finished product content thereof reaches 97% or above, and the product quality accords with the quality standard specified in European Pharmacopoeia; meanwhile, by the purification method, the process is simple, the production cycle is short, the production cost is low, and improvement on the competitiveness of the mothocetin in the international market is facilitated.

The present invention provides a safe and effective process for the selective oxidation of a 5-O-protected-LLF-28249-α compound to the corresponding 23-keto compound of formula I wherein R is a protecting group. The present invention also provides the use of the selective oxidation process in the manufacture of moxidectin.

The present invention relates to microparticles comprising moxidectin and a biodegradable polymer, wherein the microparticles comprising moxidectin have a shape allowing a moxidectin drug to be uniformly distributed in spherical biodegradable polymer particles, and the average particle diameter of the microparticles is 80-130 microns. The present invention relates to: extended release microparticles capable of continuously maintaining a heartworm disease prevention effect for 3-6 months by administering microparticles comprising moxidectin; and a preparation method therefor. In addition, the present invention is prepared such that the average diameters of the particles have a predetermined micrometer size, and thus reduces a foreign body sensation and pain during administration into an animal through injection, thereby enabling administration through injection to be facilitated.

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.

A monodose veterinary composition for topical application (spot on) for canines, the said composition comprising: (a) Imidacloprid, between 8.18 and 10.00%, (b) Moxidectin, between 2.86 and 3.50%, (c) Praziquantel, between 8.18 and 10.00%, and (d) an aprotic solvent selected from Dimethyl sulfoxide (DMSO), N,N-dimethylacetamide (DMAC), N,N-dimethylformamide (DMF) and their mixtures, between 65.45 and 80.00%; together with excipients acceptable from the veterinary viewpoint, where the percentages are related to the composition's total weight. The use of an effective amount of (a) Imidacloprid, (b) Moxidectin; (c) Praziquantel; and (d) an aprotic solvent selected from Dimethyl sulfoxide (DMSO), N,N-dimethylacetamide (DMAC), N,N-dimethylformamide (DMF) and mixtures of these, together with veterinary acceptable excipients, for the preparation of a monodose veterinary composition for the treatment, control and prevention of ecto and endoparasitoses in canines, where the said veterinary composition is adapted to be administered topically (spot on).

The invention provides an oily injection containing antiparasitic agent / polyethylene glycol drug-loading microparticles which is prepared by suspending drug-loading microparticles, which are composed of antiparasitic agent and solid polyethylene glycol, in an oily medium. The antiparasitic agent comprises ivermectin, abamectin, eprinomectin, doramectin, milbemycin oxime, moxidectin, albendazole oxide or hydrochloride thereof, oxfendazole or hydrochloride thereof, closantel base or sodium salt thereof; polyethylene glycol with molecular weight of more than 6,000is preferably selected for preparation of the oily injection; and one of isopropyl myristate, injection soybean oil, maize oil and tea seed oil is preferably selected for preparation of the oily injection.

The invention discloses a slow-release gel preparation containing moxidectin for injection and a preparation method of the preparation. The slow-release gel preparation containing moxidectin for injection is prepared by using moxidectin, a slow-release agent, a moisturizer, a preservative and a gel substrate according to a certain ratio and the certain method. The preparation has a high-efficiencykilling effect on the digestive tract nematodes and parasites on the body surfaces of pets such as domestic animals, dogs and cats, especially on nematodes resistant to ivermectin in sheep, and can effectively prevent and control parasitic diseases of the domestic animals, the dogs and the cats in vivo and vitro. The gel preparation provided by the invention has the characteristics of the simplepreparation method, good biocompatibility, slow release and high efficiency, and can be used for subcutaneous and intramuscular local injection to prevent and control the parasitic diseases of the pets such as the domestic animals, the dogs and the cats.

The invention discloses a polyclonal antibody for detecting moxidectin as well as a preparation method and an application thereof. Firstly, a compound (a hapten) is protected, and a structural formula is shown in a formula (I). The invention also provides a conjugate obtained by conjugation of the compound shown in the formula (I) and a carrier protein. The invention also provides an antibody obtained by using the conjugate as an immunogen. The antibody is concretely a polyclonal antibody. The invention also provides a kit for detecting moxidectin, and the kit comprises the polyclonal antibody. The structure of moxidectin is reconstructed for the first time, the hapten is obtained, the polyclonal antibody of moxidectin is prepared, and home and abroad blanks are filled. The conjugate of the hapten and the carrier protein is used for preparing the moxidectin antibody, and the preparation process has the advantages of simplicity, economy, high sensitivity and high practical value. The product has good application prospects in the residual detection of veterinary drug.

The invention discloses a moxidectin preparation and a preparation method of the moxidectin preparation. The preparation method comprises the following steps: inoculating streptomyces cyaneogriseus sp. noncyanogenus into a culture medium for culturing, thus obtaining a suspension M; carrying out suction filtration on the suspension M to obtain a filter cake N; drying the filter cake N to obtain dry mycelia; mixing the dry mycelia and methanol, and carrying out filtering to obtain leach liquor; carrying out protective reaction, oxidation reaction and oximation reaction on the leach liquor to obtain moxidectin; and mixing water, the moxidectin, methylpropanol, ethyl acetate and a surfactant, thus obtaining the moxidectin preparation. With the adoption of the moxidectin preparation and the preparation method of the moxidectin preparation, the problems that the traditional moxidectin preparation is relatively low in insect killing rate, and has difficulty in volatilizing after use, so that the secondary pollution is easily caused, are solved.

The invention relates to a macrolide biopesticide aqua. The macrolide biopesticide aqua is prepared from the following raw materials by weight: 0.1 to 10 parts of nemadectin or moxidectin, 1 to 30 parts of a surfactant, 0.1 to 10 parts of an osmotic agent, 1 to 10 parts of an antifreezing agent and 1 to 85 parts of water. The surfactant is a mixture of a nonionic surfactant and an anionic surfactant and / or an ampholytic surfactant. The macrolide biopesticide aqua provided by the invention does not need usage of organic solvents for dissolving of nemadectin or moxidectin; through combined usage of the surfactants, the biopesticide aqua is allowed to have stable and uniform properties, which is more beneficial for application of nemadectin or moxidectin in pesticide products.