84 results about "Doramectin" patented technology

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.

The invention relates to a process for preparing avermectin and derivant dimethylamino avermectin, ivermectin, and doramectin slow release nanometer micro-balloon preparation. The technical procedures comprise suspending the suspending solution of 1%-40% unequal avermectin-type medicine, 0%-4% divinylbenzene (cross linking agent), (metyl group) methyl acrylate of 1% BPO (initiating agent) or solvent of methacrylic acid glycidyl ester in an aqueous phase of 40 DEG C with 1% sodium dodecyl benzene sulfonate and 0.5% gelatine or 0.5% PVA (the size ratio of an oil phase and the aqueous phase is 1:3) in a three-mouth bottle with an agitator, a reflux condensing tube and a thermometer, adding numerous ml of 0.5% methylene blue, regulating ultrasonic homogenization power, heating-up to 61 DEG C at 5 DEG C/10mins after the grain size is even, aggregating for two hours, heating-up to 85 DEG C with the same speed, aggregating for 8 hours and preparing 50nm-100nm avermectin-type medicinal nanometer micro-balloon preparation with different medicine-loading amount, and the packaging and loading rate reaches more than 91%. The invention solves the problem of long-acting controlled release of biological medicament, reduces the toxic and side effect simultaneously, improves the biological availability, reduces the cost and is friendly to the environment.

The invention discloses a method for detecting the residual quantity of ivermectin in sheep muscle tissues by using a liquid chromatograph/mass spectrometer with doramectin as an internal standard substance. The method comprises the following steps: extracting ivermectin residual in the sheep muscle tissues with acetonitrile as an extraction solvent, adopting an impurity adsorption and solid phase extraction mode, adopting an alkaline alumina column as a solid phase extraction column, introducing acetonitrile, eluting, and collecting all obtained eluate. The method solves the problems of complex extraction and purification processes and high detection limit of traditional detection methods, realizes enrichment and purification of ivermectin residual in the sheep muscle tissues, improves the detection sensitivity, repeatability and accuracy, and is suitable for batch sample detection.

The invention discloses a method for preparing a high-purity doramectin. The method comprises the steps of extracting the fermenting solution, condensing, pulping, crystallizing and the like to obtain the high-purity doramectin. The doramectin can be extracted by adopting a pulping and crystallizing process, and the method has the advantages of simple and easy process, high yield, high product quality, low production cost, and suitability for industrial production.

The invention provides a new preparation method of doramectin, and in particular relates to a method for fermenting doramectin. The method is characterized by comprising a step of adding cyclohexanol carboxylic acid or salt of the cyclohexanol carboxylic acid twice in a fermentation process, wherein the first addition time of the cyclohexanol carboxylic acid or the salt of the cyclohexanol carboxylic acid is 22-60 hours after fermentation, and the second addition time of the cyclohexanol carboxylic acid or the salt of the cyclohexanol carboxylic acid is 170-194 hours after fermentation. The method is high in fermentation yield and suitable for industrial massive production, and can be applied to production of doramectin by a 500-L fermentation tank in a fermentation manner.

The invention relates to the field of fermentation engineering, and concretely discloses a fermentation medium for producing doramectin, and a preparation method and an application thereof. The fermentation medium adopts cottonseed cake powder preheated at 40-60 DEG C and having a granularity of 10-40 meshes and corn protein powder as a combined nitrogen source, and is better than fermentation media using single nitrogen sources in Streptonmyces avermitilis metabolism, so the production of doramectin is benefited. The control of granularity of the cottonseed cake powder and the corn protein powder is combined with the preheating treatment, so the paste formation phenomenon of a feed liquid in fermentation process (especially the middle and late fermentation stage) is effectively avoided, and the fermentation level of doramectin is significantly improved.

The invention discloses a method for preparing strain which can generate protoplast fusion by using marked plasmid. The invention has the advantages that marks can be easily added and removed, thereby being convenient for performing breeding and improvement of the strain based on the gene shuffling technology. The invention also has the advantages that the operation is simple, the cost is low, the requirement for equipment is low, and the chromosome of the strain can not be damaged.

The invention discloses a doramectin microemulsion transdermal agent and a preparation method thereof. The doramectin microemulsion transdermal agent comprises the following components in percentage by weight: 0.2-2.0 percent of doramectin, 7-22 percent of oil phase, 10-22 percent of emulsifier, 5-50 percent of co-emulsifier, 1-5 percent of antifreezer, 1-10 percent of penetration enhancer and the balance of water. The doramectin microemulsion transdermal agent has the advantages of stable quality, good drug efficacy, low cost, little environmental pollution, high safety, little irritation, simple operation in application, convenient use, good clinical application effect and long sustained release period, can efficiently reduce the drug administration time, can be used for treatment and also prevention and overcome the defects of trouble and cost increase to animal husbandry production due to repeated drug administration.

The invention provides a high-yield fermentation production method of doramectin. The high-yield fermentation production method comprises the following steps: dissolving a doramectin precursor into water, methanol or ethanol or dispersing the doramectin precursor into a glycerol emulsifying system so as to be convenient for disinfection and material supplementation, wherein the doramectin precursor is cyclohexanecarboxylic acid or sodium cyclohexanecarboxylate; inoculating a strain seed solution into a fermentation culture medium and fermenting; adding the precursor which accounts for 0.02 to0.08 percent of the total weight of the fermentation culture medium at the early period of fermentation for induction; adding the precursor which accounts for 0.18 to 0.22 percent of the total weightof the fermentation culture medium at the middle period of the fermentation; adding the precursor which accounts for 0.02 to 0.08 percent of the total weight of the fermentation culture medium at thelater period of the fermentation. The method is simple and effective, and can be used for rapidly improving a fermentation level of the doramectin; the production cost is reduced and extra equipment and manpower do not need to be increased; the fermentation level of the doramectin can be relatively greatly improved and the production method is relatively suitable for commercial large-scale production.

The invention discloses a compound serving as an anti-tumor medicine synergist and a reversal agent and belongs to the technical field of medicines. The invention provides application of an avermectinmedicine to preparation of an anti-tumor medicine and application of the avermectin medicine to preparation of the anti-tumor medicine synergist or the reversal agent. The invention also provides ananti-tumor medicine composition which comprises one or more anti-tumor medicines and one or more avermectin medicines as effective components. The avermectin medicine is avermectin, ivermectin, epiomycin, doramectin or eprinomectin, and the anti-tumor medicine is vincristine and salt thereof, daunorubicin, taxol and salt thereof or doxorubicin. The avermectin medicine can improve the sensibility of tumors to chemotherapeutic medicines and thus can be used as the anti-tumor medicine synergist; and the avermectin medicine has an excellent effect on reversing the medicine resistance of tumor cells to the anti-tumor medicine.

The invention discloses an insecticidal composition containing doramectin and pyriproxyfen. The weight ratio is (1 to 80) to (80 to 1), preferably (1 to 40) to (40 to 1), further preferably (1 to 20) to (1 to 10). The composition and appropriate additives can be prepared into pesticidally acceptable preparations; the more suitable preparations are water dispersible granules, wettable powder and aqueous emulsions. The composition is reasonable in component compatibility; compared with a single preparation, the composition has obvious synergistic effect, is safe to environment, is low in toxicity to people and livestock, and has a good prospect in development of pesticide mixtures.

The invention discloses an externally applied medicament for treating mite infection of pets. The externally applied medicament consists of the following medicines: 0.005 to 0.01g of doramectin, 1 to 5g of borneol, 20 to 50mL of propylene glycol and 40 to 70mL of absolute ethanol. The externally applied medicament has a broad applicable range, and can be used by big animals, small animals and economic animals; and the administration method is simple, the externally applied medicament is directly applied to affected parts, an oiling agent is insoluble in water, and the externally applied medicament has incomparable advantages compared with aqueous medicaments. The clinical application shows that: the cure rate of the externally applied medicament for skin diseases caused by secondary bacterial infection of mites of the pets is 80 percent and above; the pets can be cured within 1 to 2 treatment courses; the diseases do not relapse after the pets are cured; and in addition, the externally applied medicament is low in toxicity and cost, is convenient to use, and can be popularized and industrially produced.

The invention discloses a broad-spectrum anti-parasitic compound imidacloprid transdermal composition preparation for pets. The transdermal composition preparation contains the following components in parts by weight: 500000-5000000 parts of imidacloprid, 1000-500000 parts of doramectin, 100-20000 parts of pyrethroid, 2000000-8000000 parts of a solvent, 100000-2000000 parts of a penetration enhancer, 1-10 parts of an antioxidant, 500000-5000000 parts of an auxiliary agent. The compound imidacloprid transdermal composition preparation is stable in quality, high in safety, good in transdermal absorption property, good in pesticide effect, good in pesticide effect, low in stimulation, simple and convenient to use and low in environmental pollution, has a relatively long slow release period, can be used for expelling and killing endoparasite and ectoparasite, and simultaneously has functions of preventing mosquitoes and fleas.

The invention belongs to the field of antiparasitic pharmaceutical preparations, and particularly relates to a doramectin sustained-release microcapsule injection. The doramectin sustained-release microcapsule injection comprises doramectin microcapsule particles, a wetting agent, a suspending agent, a deflocculating agent and water for injection, wherein the doramectin microcapsule particles takedoramectin-loaded silicon dioxide aerogel particles as a capsule core and polylactic acid as a capsule membrane. The prepared polylactic acid-coated silicon dioxide aerogel-doramectin microcapsule particles have a sustained-release effect, are stable to light and are prepared into an injection, and the injection can achieve a long-acting effect after being administered in animal testing.

The invention discloses a doramectin O/W (oil in water) type injection taking water as the matrix and a preparation method thereof. The O/W type injection is composed of OP emulsifier, PEG 400, ethyl oleate, doramectin, and injection water. The key point of the invention is the determination of formula of the injection and the content of each component. The injection mainly takes water as the matrix, comprises a little organic solvent, reduces affection of organic solvent on livestock, poultry and environment, does little harm to producers and users, is safer in storage and transportation, has little by-effect on livestock and poultry, and solves the problems of harms to livestock and poultry and pollution to environment, which are generated during the production and use processes of the conventional dosage form (oil dosage).

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 an agricultural acaricide composition containing active components composed of doramectin and bifenazate. The weight ratio of the active components is (1:80)-(80:1), is preferably (1:40)-(40:1) and further preferably (1:16)-(15:1). The composition disclosed by the invention can be prepared into a pesticide acceptable dosage form together with an appropriate aid, and the appropriate dosage form is wettable powder, water-dispersible granules and a water emulsion. The composition realizes reasonable matching of the components, thereby mutually making up the defect during use of a single agent; the composition has a favorable acaricide effect, a long lasting period, a favorable fast-acting property and a synergic effect; the composition is safe to the environment and low toxic to humans and animals; and the composition has favorable application prospects in the aspect of pesticide mixture development.

The invention provides a synthesis method for high-purity selamectin. The synthesis method comprises the following steps: with doramectin as a raw material, subjecting the doramectin to hydrogenation,oxidation, oximation and desugaring so as to obtain a crude selamectin product, wherein an oxidation system adopted by oxidation is a manganese dioxide/Dess Martin oxidant or manganese dioxide/2-iodoylbenzoic acid. According to the invention, the use of a traditional single oxidant is broken through; the manganese dioxide/Dess Martin oxidant or the manganese dioxide/2-iodoxybenzoic acid is selected as the oxidation system; the oxidation system is mild and controllable; oxidation reaction is more thorough; reaction byproducts are few; thus, the obtained crude selamectin product is high in purity, and conditions are provided for abandoning a C18 high-pressure preparation process in a subsequent refining process. Generally speaking, the synthesis method provided by the invention is short insynthetic route, not tedious in post-treatment process and low in cost, can obtain the selamectin with a purity of 99% or above, and has high total yield.

The invention relates to the technical field of new application of medicines, in particular to new application of doramectin in treatment of gliomas. Through in-vivo and in-vitro experiments, the anti-glioma effect of the doramectin is investigated. The doramectin can inhibit proliferation and migration of glioma and promote apoptosis and autophagy of glioma cells. Therefore, the doramectin can beused for preparing the medicine for treatment of the glioma, and has a good effect on treatment and prognosis of the glioma.

The invention discloses an acaricide composition containing active components composed of doramectin and fenazaquin. The weight ratio of the active components is (1:80)-(80:1), and the weight ratio range is preferably (1:60)-(1:40) and further preferably (1:40)-(1:20). The composition disclosed by the invention can achieve the following technical effects: the active components having different action mechanisms are mixed, thereby mutually making up the defect during use of a single agent; the composition has a wide insecticidal spectrum, and has a favorable effect for preventing and controlling resistant pest mites; the composition is environment-friendly; and the composition has favorable application prospects in the aspect of pesticide mixture development.

The invention discloses an acaricidal composition. The active ingredient is composed of doramectin, tebufenfen and flubenzuron. The acaricidal composition has a control effect better than that of a single ingredient, reduced dosage, low cost, and delayed The advantage of pest resistance has a good control effect on common agricultural pest mites such as citrus spider mite and cotton spider mite, and has a good application prospect in the development of new pesticide compound preparations.