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142results about How to "Low acute toxicity" patented technology

Nano Anticancer Micelles of Vinca Alkaloids Entrapped in Polyethylene Glycolylated Phospholipids

The present invention provides a nano-micellar preparation containing vinca alkaloids antitumor agent for intravenous injection, which cincludes a therapeutically effective amount of vinca alkaloids antitumor agent (vinblastine, vincristine, vindesine and vinorelbine), a phosphatide derivatized with polyethylene glycol, together with pharmaceutically acceptable adjuvants. The preparation is prepared by encapsulating the medicament with a nano-micelle to obtain the nano-micellar preparation containing vinca alkaloids antitumor agent for injection. The vinca alkaloids antitumor agent and the phosphatide derivatized with polyethylene glycol form a nano-micelle with a highly uniform particle size. In the micelle, the hydrophobic core of encapsulated medicament is surrounded by polyethylene glycol molecules to form a hydrophilic protective layer, so that the medicament is prevented from contacting with the enzymes and other protein molecules in blood and being recognized and phagocytozed by reticuloendothelial system in body, and the circulation time in vivo of the micelle is prolonged.
Owner:BEIJING DIACRID MEDICAL TECH

Cyclohexane amine compound and application of cyclohexane amine compound as anti-schizophrenia medicine

InactiveCN103130737ASignificant anti-schizophrenia effectPromote oral absorptionOrganic active ingredientsNervous disorderDiseaseIn vivo tests
The invention discloses a cyclohexane amine compound and application of the cyclohexane amine compound as anti-schizophrenia medicine. The cyclohexane amine compound has high affinity to a dopamine D3 receptor and a 5-HT1A, and representative compounds have a high selectivity of D3 / D2 receptors. According to in vivo tests, the representative compounds such as I-1 compound can remarkably improve relative symptoms of apomorphine model mice and MK-801 model mice. The cyclohexane amine compound has the advantages of being good in anti-schizophrenia effect, low in acute toxicity and good in safety, and having development value of serving as novel high-efficiency and low-toxicity medicine for anti-neurological disorder diseases. The cyclohexane amine compound is a compound with a structural general formula (I) or stereomer, free alkali, aquo-complex or salt.
Owner:JIANGSU HENGYI PHARMA +1

Insecticide microcapsule suspension type liquid medicine fertilizer and preparation method and application thereof

The invention discloses an insecticide microcapsule suspension type liquid medicine fertilizer and a preparation method and application thereof.The insecticide microcapsule suspension type liquid medicine fertilizer is prepared from insecticide, an organic solvent, a cyst wall material, a pH adjusting agent I for preparing microcapsules, a nitrogen fertilizer, a phosphate fertilizer, a potash fertilizer, a micronutrient fertilizer, an emulsifying agent, a filler, a dispersing agent, a defoaming agent, a thickening agent, an antifreezing agent and water, wherein the pH adjusting agent I is acid.The raw materials further include a pH adjusting agent II for adjusting the pH value of the liquid medicine fertilizer, wherein the pH adjusting agent II is alkali.The average control effect of the insecticide microcapsule suspension type liquid medicine fertilizer on wheat aphid is 80.0% or above, meanwhile, the yield of eggplants can be increased, and the N, P and K unit nutrient partial productivity is improved.The insecticide microcapsule suspension type liquid medicine fertilizer is simple and reasonable in technology, reduces the material grinding size as much as possible, is low in energy consumption, suitable for industrial production and suitable for being adopted in a small area, and saves material resources, financial resources and labor force.
Owner:CHINA AGRI UNIV

Aminocarboxylate ligands having substituted aromatic amide moieties

Novel metal-chelate complexes comprising aminocarboxylate ligands including substituted aromatic amide moieties, such as those having the formula wherein R13, A1, R1 and R2 are as defined herein, are disclosed.
Owner:BRISTOL MYERS SQUIBB CO +1

Nano-micellar preparation of anthracylcline antitumor antibiotics encapsulated by the phosphatide derivatized with polyethylene glycol

The present invention provides a nano-micellar preparation of anthracycline antitumor antibiotics for intravenous injection, which comprises a therapeutically effective amount of anthracycline antitumor antibiotics, a phosphatide derivatized with polyethylene glycol, together with pharmaceutically acceptable adjuvants. The preparation is prepared by encapsulating the medicament with a nano-micelle to obtain the nano-micellar preparation of anthracycline antitumor antibiotics for injection. The anthracycline antitumor antibiotics and the phosphatide derivatized with polyethylene glycol form a nano-micelle with a highly homogeneous particle size. In the micelle, the hydrophobic core of encapsulated medicament is surrounded by polyethylene glycol molecules to form a hydrophilic protective layer, so that the medicament is prevented from contacting with the enzymes and other protein molecules in blood and being recognized and phagocytozed by reticuloendothelial system in the body, and the circulation time in vivo of the micelle is prolonged.
Owner:INSITUTE OF BIOPHYSICS CHINESE ACADEMY OF SCIENCES

Preparation of avermectin medicament sustained-release nano microsphere preparations and uses thereof

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.
Owner:INST OF PLANT PROTECTION CHINESE ACAD OF AGRI SCI

Piperazine (piperidine) cyclohexyl derivative and applications of piperazine (piperidine) cyclohexyl derivative in treatment of neuropsychiatric diseases

ActiveCN105367565AGood receptor selectivityImproving the effect of cognitive impairmentOrganic active ingredientsNervous disorderLow affinityAcute toxicity testing
The present invention discloses a piperazine (piperidine) cyclohexyl derivative and applications of the piperazine (piperidine) cyclohexyl derivative in treatment of neuropsychiatric diseases. According to the present invention, the pharmacological experiment results show that the piperazine (piperidine) cyclohexyl derivative provides high affinity with a dopamine D2 receptor, a dopamine D3 receptor, a serotonin 5-HT1A receptor and a serotonin 5-HT2A receptor, provides good D3/D2 receptor selectivity and good 5-HT1A/5-HT2A receptor selectivity, and provides low affinity with alpha receptor; the in vivo test results show that the preferred compound has characteristics of good anti-schizophrenia effect, good pharmacokinetic property, low side effect, low acute toxicity and high safety, and has the development value of being adopted as the novel efficient and low-toxic anti-neuropsychiatric disease; and the piperazine (piperidine) cyclohexyl derivative is a compound represented by the structural general formula (I), or a geometric isomer, an optical isomer, a salt, a hydrate or a solvate thereof. The formula (I) is defined in the specification.
Owner:SHANGHAI INST OF PHARMA IND +1

Methyl-amino-ivermectin water suspension nano capsule prepn and its preparing method

The present invention discloses a water suspended nano methyl-amino-Ivermectin capsule preparation prepared via emulsion polymerization process. It has capsule shell of styrene, isocyanate, acrylate and methacrylate copolymer, and core comprising biologically originated pesticide and animal remedy methyl-amino-Ivermectin as effective component; contains methyl-amino-Ivermectin 0.2-2 wt%, capsule shell 5-30 wt%, additive 10-35 wt% and water in proper proportion. The nano capsule is disersive spherical particle of size smaller than 100 nm. Compared with traditional pesticide preparation forms, the present invention has the features of water based solvent, nano level dispersive effective component, high stability, etc. and may be used in killing animalí»s parasite and various pests of fruit tree, vegetable, flower, cotton, tobacco, etc.
Owner:HEBEI UNIVERSITY OF SCIENCE AND TECHNOLOGY

Melamino-formaldehyde resin encapsulated acetamiprid microcapsule, and preparation method thereof

The invention relates to a melamino-formaldehyde resin encapsulated acetamiprid microcapsule, and a preparation method thereof. The microcapsule is technically characterized by comprising the following components: melamine, a formaldehyde solution, acetamiprid, chloroform, an emulsifying agent, a dispersing agent, water, an acid catalyst and a base catalyst. The preparation method comprises the following steps of: putting melamine and the formaldehyde solution in a three-neck flask, adding the base catalyst and regulating, and heating to obtain a melamino-formaldehyde prepolymer; putting the acetamiprid, chloroform, the emulsifying agent, and water in a reaction flask, and stirring to obtain a pre-emulsification solution; mixing the pre-emulsification solution and the prepolymer, adding acid and catalyzing, and adding an appropriate amount of dispersing agent, raising temperature to 60 DEG C, reacting for three hours and stopping reaction; and washing a product by using water for multiple times, and suction-filtering and drying to obtain a microcapsule product. The encapsulation rate of the microcapsule is relatively high, sustained release time is long, pollution to environment is reduced, the preparation method is simple, wall materials are low in cost and the microcapsule is suitable for large-scale production and application.
Owner:BEIJING UNIV OF CHEM TECH

Alkaloid microcapsule and preparation method thereof

The invention relates to an alkaloid microcapsule and a preparation method thereof. The alkaloid microcapsule comprises a capsule core and a capsule wall, wherein the capsule core comprises one or more alkaloids extracted from aconite, aconitum pendulum, mandala, black false hellebore, radix sophorae flavescentis and semen strychni; the capsule wall comprises polyurea which is prepared from polyamine and polyisocyanate. The bitter taste of the alkaloid is covered by microcapsule coating, and the stability of the alkaloid is certainly improved. The alkaloid inside the microcapsule can be slowly released for a long time by the effect of the external environment, so the medicinal effect time is prolonged; the acute toxicity of the alkaloid is certainly alleviated and the alkaloid is chronic in toxicity; on one hand, the vigilance of insects can be reduced; on the other hand, harms to beneficial organisms and humans can be reduced, so the alkaloid microcapsule belongs to an environment-friendly pesticide.
Owner:LANZHOU UNIVERSITY
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