6305results about How to "Small toxicity" patented technology

The invention relates to a 2-(2-(2, 6-dichlorophenyl amido) phenyl) methyl acetate, relative synthesis method and application, belonging to the technical field of chemical pharmacy, which comprises that adds acid into diclofenac salt to acidify the salt into diclofenac, reacts diclofenac with methanol, or adds acid into diclofenac salt to acidify the salt into diclofenac, to be reacted with chloracetyl chloride to obtain 2-(2-(2, 6-dichlorophenyl amido) phenyl) methyl acetate. The inventive drug has significant anti-inflammatory and analgesic effects.

The invention relates to a multifunctional double-layer core-shell structure magnetic nano particle. In the invention, a magnetic nano particle with a particle size of 1-300 nm is used as a core and coated with a double-layer shell consisting of a SiO2 layer with a thickness of 1-200 nm and a hydrolyzed silane coupling agent layer is 1-100 nm thick and comprises one or more multifunctional groups; the particle size and the shell layer thickness can be controlled through regulating the volumes, the weight ratios and the reaction time of the magnetic core, a silicon dioxide precursor, a silane coupling agent and a catalyst in a preparation process; the total particle size of the nano particle can be as small as 5-50 nm and as large as 700-800 nm; the nano particle can have superparamagnetism, paramagnetism and ferromagnetism according to the change of the magnetic core particle size; and one or more bioactive molecules can be connected into the shell layer of the magnetic nano particle or to the surface of the shell layer through a chemical method or a physical method. The invention also provides a preparation method of the multifunctional double-layer core-shell structure magnetic nano particle and application thereof. The particle preparation method has the advantages of simplicity, moderate condition, low cost and easy realization of industrial production. The nano particle can obtain different functions through connecting different bioactive molecules and can be applied to the fields of protein enrichment, biological detection, separation and purification, targeted drug carriers, cell imaging and medical imaging.

The invention discloses a medicament for treating deficiency of kidney, frequent micturition, urgent urination and prostatitis, which is prepared from 38 Chinese medicinal herbs: common curculigo rhizome, tuber fleeceflower root, ginseng, hippocamp, common macrocarpium fruit, malaytea scurfpea, siberian solomonseal rhizome, hairy antler, songaria cynomorium herb, root of red-rooted salvia, sevenlobed yam rhizome, epimedium, astragalus, raw rehmannia root, prepared rehmannia root, cochinchnese asparagus root, ophiopogon root, shizandra berry, medlar, cinnamomvine, white poria, seal's genitals, hawthorn fruit, raspberry, chaff flower root, platycladi seed, eucommia bark, Chinese angelica, medicinal indianmulberry root, south dodder seed, desertliving cistanche, polygala root, phellodendron, anemarrhena root, cassia bark, placenta, prepared common monkshood daughter root and black sesame seed. The medicament has the advantages of addressing both symptoms and root causes along with appropriate compatibility, good curative effect, short treatment course, high cure rate, low recurrence rate, no toxic or side effect, convenience for application, low treatment cost and the like.

The invention belongs to the field of pharmaceutical agents, relates to a polymer micelle lyophilized agent encapsulating an insoluble antitumor drug as well as a preparation method and an application thereof. The polymer micelle lyophilized agent is prepared by carrying out molecular self-assembly on a methoxy poly(ethylene glycol) 2000-polyester block copolymer to form micelles, and then encapsulating the insoluble antitumor drug in a hydrophobic core formed by the polyester. The lyophilized agent has high encapsulation rate, high drug loading and small particle size, can significantly improve the water solubility of the insoluble drug and result in passive targeting of more antitumor drugs to concentrate in the tumor tissues, thus improving an anti-tumor treatment effect and reducing the toxic and side effects of drugs, and can be used to prepare the drugs used for the treatment of lung cancer, intestinal cancer, mammary cancer, ovarian cancer, etc. The lyophilized agent can also be quickly dissolved and dispersed to form a transparent micellar solution after water for injection, normal saline solution and the like are added, and is used for the preparation of the drugs for treating primary intestinal cell carcinoma.

The invention provides hollow fluorescent carbon quantum dots as well as a preparation method and application thereof and belongs to the technical field of light-emitting nano materials. The preparation method comprises the following steps: adding ethanediamine and concentrated acid into water soluble saccharides serving as a carbon source, so as to obtain a puce viscous material; after reaction stops, naturally cooling a glass container, adding a certain amount of secondary water, stirring for dissolving to obtain a dark brown solution, and dialyzing to remove impurities, thereby obtaining a hollow carbon quantum dot aqueous solution; and freeze-drying to obtain the hollow carbon quantum dots. The preparation method is simple in process, wide in raw material source, low in price, low in preparation condition requirement, and free from energy consumption; the obtained hollow carbon quantum dots are relatively high in yield, small in particle diameter and uniform in size; the preparation method is capable of realizing batch production; the obtained hollow carbon quantum dots can be used for anticancer drug carriers, are capable of reducing the toxic and side effects of anticancer drugs and also can be used in detection of VI ions in water.

The present invention belongs to the field of Chinese medicine technology, and provides one kind of plaster for treating arthralgia. The plaster is prepared with dragon's blood, curcuma, dahurian angelica root, Chinese ephedra, pubescent angelica root, and other Chinese medicinal materials. Clinical application for years shows that the plaster has high curative effect, no toxic side effect, and other advantages, and can heal arthralgia radically.

The invention provides an antibacterial wound dressing and a preparation method thereof. The antibacterial compound type wound dressing is characterized by comprising a chitosan-based medicine carrying compound antibacterial ultrafine fibrous membrane, a calcium alginate fiber non-woven fabric and a supporting protective layer which are sequentially arranged from top to bottom. The medicine carrying ultrafine fibrous membrane obtained by adopting an electrostatic spinning method has the advantages that the surface area of a medicament can be effectively increased, medicines can be slowly and sustainably released by virtue of high porosity and uniform pore diameter of ultrafine fibers, so that the medicines can be fully absorbed by a human body, medication is not need to be carried out frequently, the effect of the medicines can be maintained, and toxic and side effects of the medicines are reduced.

The invention relates to a natural active drug-polysaccharide targeted compound with antitumor activity and targeting property. A natural active drug is introduced onto a polysaccharide framework by chemical grafting, and physically mixed with a ligand distearoylphosphatidyl ethanolamine-polyethyleneglycol-anisoyl amine with targeted transmission capacity to form a natural active drug-polysaccharide targeted compound, and the natural active drug-polysaccharide targeted compound can be self-assembled in water to form a nano micelle. The method is characterized in that the natural active drug-polysaccharide targeted compound has targeted transmission capacity, enhances the tumor transfer efficiency of the preparation, reduces the untoward reaction and enhances the tolerance of the patient; the hydrophobic inner core formed by the hydrophobic group can physically wrap the antineoplastic drug, thereby obviously improving the water solubility of the antineoplastic drug; and the antineoplastic drug which is physically wrapped by the chemically coupled ursolic acid can implement combined treatment of tumors and lower the toxic or side effect. The preparation method is simple and easy to operate, has the advantage of higher yield, and can easily implement industrialization.

The invention belongs to the medicinal preparation field, relates to a cell-penetrating peptide modified nanoparticle, and concretely relates to a nanoparticle delivery system for oral polypeptide and protein medicines, and its preparation method. The medicine delivery system is composed of the nanoparticle, cell-penetrating peptides modified on the surface of the nanoparticle, and the polypeptide protein medicines sealed by the nanoparticle, wherein the average particle size range of the medicine delivery system is 10-500nm. The cell-penetrating peptide modified nanoparticle and glucosaminoglycan having electronegative cell surfaces undergo electric property attraction and then undergo endocytosis, so the cell-penetrating peptide modified nanoparticle and the glucosaminoglycan are integrally taken into cells; and the cell-penetrating peptide modified nanoparticle has an alimentary canal mucous membrane penetrating capability after the cell-penetrating peptide modified nanoparticle is orally taken, and can deliver the polypeptide protein medicines carried by the cell-penetrating peptide modified nanoparticle to the whole body for blood circulation, so the oral biological utilization degree of the medicines are improved. The cell-penetrating peptide modified nanoparticle has the advantages of improvement of the stability of polypeptide and protein medicines in the alimentary canal, reduction of the application amount of cell-penetrating peptides, and reduction of possible toxic side effects caused by the cell-penetrating peptides.

The invention provides a [(indole-3-yl)pyrimidine-2-yl]aminophenylpropyl-2-eneamide derivative and its salt, a preparation method of the derivative, and application of the derivative and the salt. The [(indole-3-yl)pyrimidine-2-yl]aminophenylpropyl-2-eneamide derivative has a structure shown in the formula I below. Deuterium-carbon bonds in the derivative enable the derivative to decompose slowly in a human body, a medicament of the derivative has a longer half-life period and a higher concentration in blood, the dosage of the medicament is finally reduced, and toxic and side effects of the medicament are decreased. Experiments show that compared with AZD 9291 mesylates, AZD 929-D9 mesylate of the deuterium-substituted derivative has Cmax which is 1.32 times as high as that of AZD 9291, exposed dose 1.41 times as high as that of AZD 9291, and elimination half-life 1.31 times as long as that of AZD 9291.

The coenzyme Q10 injection emulsion has coenzyme Q10 as the effective medicine component, and each 1000 ml emulsion contains coenzyme Q10 1-10g, vegetable oil for injection 0-200g, emulsifier 1-50g, isoosmotic regulator 5-50g, antioxidant 0.05-5g, pH regulator in the quantity of regulating pH value to 3.0-9.0, co-emulsifier 10-500g and water for injection for the rest. It provides the patient with treating medicine and essential nourishing matter. It has high physical stability and may be prepared into freeze dried preparation for further raised stability and convenient storing and transportation. The coenzyme Q10 injection emulsion has certain targeting effect, so that it has raised bioavailability and lowered toxic side effect.

The invention discloses nanometer medicament microspheres. The microspheres comprise a medicament, nanoparticles, a polymer and medicinal auxiliary materials. The invention further provides a preparation method of the nanometer medicament microspheres. The method comprises the following steps of: preparing a medicament and medicinal auxiliary materials into a nanometer medicament; adding the nanometer medicament into a polymer-containing organic solvent mixed solution for emulsifying; adding a nanometer medicament-in-oil mixed suspension into a water mixed suspension containing nanoparticles or containing nanoparticles and a surfactant for emulsifying to obtain an oil-in-nanoparticle mixed suspension-nanometer medicament-in-oil compound emulsion; and curing the obtained compound emulsion, and centrifugally collecting microspheres, wherein the obtained microspheres comprise the medicament, nanoparticles, the polymer and the medicinal auxiliary materials. An appropriate polymer material and an appropriate microsphere preparation method are selected, the prepared microspheres have high envelop rate, and a layer of self-assembled nanoparticles on the surfaces of the microspheres has the effects of improving cell adhesion and reducing inflammation and microencapsulation caused by local excessive acid and hydrophobic materials. The method disclosed by the invention can be applied to preparation of other medicament slow release or controlled release microspheres.

The invention discloses a fluoroquinolone acetal isoniazone, of which the chemical structure general formula is disclosed as Formula I shown in the description, wherein R1 is hydrogen atom or methyl group; R2 is hydrogen atom or amino group; R3 is hydrogen atom, methyl group, ethyl group, formacyl group, acetyl group, aroyl group or sulfonyl group; R4 is hydrogen atom or methyl group; and X is oxygen atom or sulfur atom. The fluoroquinolone isoniazone disclosed by the invention implements complementarity between the two anti-tuberculosis medicines fluoroquinolone and the isoniazide, lowers the toxic and side effect of the fluoroquinolone and the isoniazide, reduces the generation probability of drug resistance of Mycobacterium tuberculosis for the double-effect antimicrobial agent, and can be used as an anti-Mycobacterium tuberculosis medicine for brand-new structure development of medicinal active substances.

The invention provides an artificial blood vessel loaded with pseudo-ginseng medicines, and a preparation method and application for the artificial blood vessel. The artificial blood vessel sequentially consists of an inner layer, a middle layer and an outer layer which are closely connected with one another; the outer layer consists of nondegradable polymer materials; the middle layer consists of degradable high polymer materials and pseudo-ginseng powder distributed on the surface and/or the inside of the middle layer; the inner layer consists of degradable natural biological materials and pseudo-ginseng powder distributed on the surface and/or the inside of the inner layer; the mass percent of the pseudo-ginseng powder in the inner layer is larger than 5%; the content of the pseudo-ginseng powder in the middle layer is higher than that of the pseudo-ginseng powder in the inner layer; the outer layer is a nondegradable layer and is mainly used for protecting and replacing a blood vessel for a long time; the middle layer is a long-acting antithrombosis layer, can degrade high polymers, and can slowly release medicines so as to realize a long-acting antithrombosis effect; and the inner layer is a quick degrading layer, when the blood vessel is punctured and injured by a foreign object, the pseudo-ginseng medicines wrapped in the blood vessel are directly exposed on a wound, blood is stopped quickly, and the artificial blood vessel is particularly suitable for application to products such as hematodialysis.

The present invention provides a bicyclic triazolone derivative represented by the formula: J-Ar (I) [wherein, J is ], which has excellent selective weeding activity and weed killer containing the said bicyclic triazolone derivative.

The invention belongs to the field sustained/controlled-release preparations, in particular to an oral sustained/controlled-release pellet combination containing ginkgo biloba extract and a preparation method. The oral sustained/controlled-release pellet combination is composed of (A) a core containing a pill; (B) an insulating coating layer; (C) a sustained-release coating layer; (D) and an enteric-coated coating layer. The invention is the traditional Chinese medicine multi-component sustained-release pellet combination which is taken once by 24 hours and the multi-unit sustained-release pellet combined preparation with the different drug release systems, the core containing the pill is prepared by adopting the extrusion pill rolling method, a novel sustained-release multi-layer coating technology and a fluidized bed are utilized for coating the sustained-release pellet, the rapid-release part and the sustained-release part of the coated pellet are mixedly filled into a hard capsule or pressed into a pellet tablet. The sustained-release pellet has stable coating process and good reproducibility, thereby being applicable to the industrial mass production; and the drug quality of the preparation is stable through the long-term storage. The in vitro release test shows that the multiple components of the traditional Chinese medicine can achieve the sustained-release role, the sustained-release preparation can significantly increase the transmembrane absorption and the stability of various effective active ingredients by oral drug administration, the curve of plasma drug concentration in vivo is smooth, and the design purpose of 24-hour sustained-release is achieved.

The invention discloses a total bufogenin extract with antitumor function and also discloses a preparation method of the extract and application thereof in the preparation of antitumor medicines. The total bufogenin extract of the invention is prepared by organic solvent extraction, column chromatography separation and purification of dried toadskin; the content of total bufogenin is over 80 percent, wherein the content of resibufogenin is over 12 percent, the content of cinobufagin is over 4 percent, and the content of bufotalin is over 10 percent. Compared with the prior art, the invention eliminates bufotenine alkaloid which has irritation, is easy to cause hypersensitivity but has no antitumor activity, efficiently collects the effective part of total bufogenin which has significant antitumor activity, therefore pharmacological action is stronger, the clinical curative effect is higher and the toxic and side effect is lower. The total bufogenin extract can be prepared into various pharmaceutical preparations for clinical application, therefore the invention has the functions of killing tumor cells, inducing differentiation and apoptosis of tumor cells, inhibiting the neovascularization of tumor cells and lowering the neoplasm metastasis rate, etc.