80 results about "Minodronic acid" patented technology

The invention discloses a high-purity 1-hydroxyl-2-(imidazo(1,2-a) pyridine-3-group) ethylidene-1, 1-diphosphonic acid and a preparation method thereof. The target product of the invention can be applied to the treatment of osteoporosis and hypercalcemia caused by malignant tumor, with higher safety and effectiveness. The preparation method has mild reaction condition and simple post treatment, and can obtain high-purity final products and is easier to implement industrialized production.

An environment-friendly high-density solid-free weighting agent comprises components in parts by weight as follows: 0.02-0.05 parts of a dispersant, 0.3-1 part of a tackifier, 0.5-1.2 parts of chelating agent, 0.6-2 parts of a corrosion inhibitor and the balance of soluble weighting materials, wherein the dispersant is one or two of sodium polyacrylate and copolymer of phosphono and carboxylic acid; the tackifier is one or more of chitosan, agar, polyacrylamide, xanthan gum and hydroxypropyl methyl cellulose; the chelating agent is one or two of aminophosphonic acid chelate resin and ethylenediamine tetraacetic acid disodium; the corrosion inhibitor is one or two of multiple polycarboxylate and sodium gluconate; the soluble weighting materials are one or more of potassium formate, potassium citrate, potassium acetate, potassium silicate and potassium sulfate. The process steps are as follows: the raw materials are taken in weight proportion, mixed and uniformly stirred; the raw materials are added to water and dissolved at the high temperature of 70-80 DEG C; a product is evaporated to dryness, and solid is obtained; the obtained solid is ground into powder, and the solid weighting agent is obtained.

The invention discloses a detection method of minodronic acid by using high performance liquid chromatography. The method includes following chromatogram conditions: employing a mixed solution, which is composed of methanol and an aqueous solution containing sodium acid pyrophosphate and tetra butyl ammonium bromide, as a mobile phase with a volume ratio of the aqueous solution to the methanol ranging from 90:10 to 100:0, wherein the pH value of the aqueous solution is 7.0-8.0, the concentration of the sodium acid pyrophosphate is 0.02-0.04 mol/L and the concentration of the tetra butyl ammonium bromide is 0.272-0.322 g/L; employing octade-cylsilane (ODS) as a packing material, setting a flow velocity of a high performance liquid chromatography instrument to be 0.8-1.2 ml/min, a detection wavelength to be 218-282 nm and a sample size being 5-50 [mu]l. With the detection method, separation degrees, between a main peak and a neighboring impurity peak, in both a to-be-tested sample and a raw material are more than 1.5; and main peak column efficiencies in both the to-be-tested sample and the raw material are more than 3000. The detection method is good in trailing factor and system applicability.

An aminophosphonic acid compound used for nuclear medicine is prepared through adding amine and phosphoruc acid to reactor, dropping concentrated acid and formaldehyde, reaction, cooling, and precipitation in water or absolute alcohol. It along with Tc, Re, Or Sm can be used to prepare medicine for treating cancers.

The invention discloses an amino phosphonic acid compound and further discloses a preparation method of the amino phosphonic acid compound. The general formula of the compound is shown as the formula(I) (Please see the specifications for the formula). The amino phosphonic acid compound is prepared through the mode that 3,7-dimethyl-2,6-octadienal, aniline or aniline containing a substituent group, and phosphorous acid are subjected to a Mannich reaction under the action of acid catalysts. The amino phosphonic acid compound can be used as a floatation collector of ilmenite, bauxite, fluorite ores, rare earth ores or collophanite and has the characteristics of good selectivity, high water solubility, good dispersibility and the like, and the flotation recovery rate can be increased by 2-16percent points. The preparation method adopts a one-pot synthesis method, operation is easy to control, the product yield is high, and industrial production is easy.

The invention belongs to the field of pharmaceutical preparation, and specifically relates to minodronic acid tablets and a preparation method thereof. With large amounts of experiments, proportions of auxiliary materials and hydroxypropyl beta-cyclodextrin are determined, and tablets containing minodronic acid and hydroxypropyl beta-cyclodextrin are prepared. The tablets are composed of minodronic acid, hydroxypropyl beta-cyclodextrin, a filling material, a disintegrating agent, a lubricant, and other pharmaceutically acceptable auxiliary materials. During a preparation process, hydroxypropyl beta-cyclodextrin and minodronic acid are added in a water solution form into mixed powder of the filling material and the disintegrating agent. The dissolution rate of the tablets provided by the invention is substantially improved, such that rapid dissolution and absorption of minodronic acid in gastrointestinal-tract bodily fluids is facilitated. The preparation process is simple, and operation is convenient, such that the method is suitable for industrialized productions.

The invention discloses a preparation method of minodronic acid. The preparation method comprises the following steps: performing acetal hydrolysis on a compound I to obtain a compound II, performing closed-loop treatment and hydrolysis on the compound II and 2-aminopyridine to obtain a compound III, and finally, performing phosphorylation on the compound III to obtain a compound IV. By adopting the preparation method disclosed by the invention, highly toxic chemical reagents including sodium cyanide or bromine and the like are avoided, the reaction conditions are mild and controllable, the reaction steps are relatively short, the yield is relatively high, and the cost is relatively low, so that the preparation method is suitable for industrial production.

The invention discloses a pretreatment method of minodronic acid in a plasma sample based on derivatization on a solid-phase extraction column and a detection method, and belongs to the field of biological analysis. The detection method provided by the invention comprises the following steps: firstly, carrying out pretreatment on the plasma sample containing minodronic acid, and then detecting theconcentration of minodronic acid in the plasma by using a liquid phase-mass spectrometry method, wherein the pretreatment comprises the following steps: injecting the plasma sample containing minodronic acid into the activated solid-phase extraction column, leaching, adding a derivatization reagent, carrying out a column derivatization reaction, collecting a reaction solution, blow-drying by using nitrogen, redissolving, and directly injecting a supernatant. According to the method, the defect that minodronic acid cannot be subjected to liquid phase analysis due to the polarity of minodronicacid is overcome, compared with an existing derivatization method, the dosage of plasma is greatly reduced, and sample pretreatment steps are simplified.

The application relates to a method for separating and detecting minodronic acid. The method adopts a reverse-phase chromatographic column through high performance liquid chromatography, and uses a buffer solution of pH=2-7.5 containing sodium alkylsulfonate as mobile phase A, and Methanol or acetonitrile was used as mobile phase B, the detection wavelength was 215nm, and linear gradient elution was used for separation and detection.

The invention discloses a preparation method of minodronic acid for treating osteoporosis. The preparation method comprises the following steps of firstly, reacting a compound as shown in a formula (I) with 2-aminopyridine to obtain a compound as shown in a formula (II); secondly, hydrolyzing the compound as shown in the formula (II) obtained in the first step to obtain a compound as shown in a formula (III); thirdly, phosphorylating the compound as shown in the formula (III) obtained in the second step to obtain the minodronic acid, wherein X is chlorine or bromine, and R is alkyl radicals of C1 to C4; in the first step, a reaction promotor M is added and consists of one or more substances selected from zinc nitrate, silver nitrate and copper nitrate and one or more substances selected from glycine and alanine. According to the preparation method, the yield of a key intermediate in a preparation process of the minodronic acid can be greatly improved; the preparation method has the advantages of few side products, easiness in purification, mild conditions and higher reaction speed, and is suitable for large-scale production and popularization.

The invention belongs to the technical field of pharmacy, and relates to a minodronic acid medicinal composition and a preparation method thereof, in particular to a tablet consisting of a crystal form E minodronic acid monohydrate, a filling agent, a bonding agent, a lubricating agent, a disintegrating agent, a coating agent and other acceptable medicinal auxiliary materials. Active components account for 1 percent of the total weight of the minodronic acid tablet prepared by using the method. By mixing through a method for equivalently adding auxiliary materials, the content uniformity of the tablet can be increased effectively, so that the minodronic acid tablet is safe, effective and controllable in quality.

The invention discloses a preparation method of minodronic acid for treating osteoporosis. The method comprises the following steps: (1) reacting a compound expressed by the formula (I) with 2-aminopyridine to obtain a compound expressed as the formula (II); (2) hydrolyzing the compound expressed by the formula (II) obtained by the step (1) to obtain a compound expressed by the formula (III); and (3) phosphorylating the compound expressed by the formula (III) obtained in the step (2) to obtain minodronic acid, wherein the formulae (I), (II) and (III) are described in the specification; in the formulae (I), (II) and (III), X1 and X2 independently represent halogen, and R represents C1-C4 alkyl. Through the method, the yield of key intermediates in the preparation process of minodronic acid can be greatly increased; meanwhile, the method is few in impurities of product, few in by-products and mild in condition, and is suitable for large-scale production and popularization.

The invention relates to a minodronic acid tablet and a preparation process thereof. According to the preparation process, a direct tabletting method is used, Flowac100 type spray-dried lactose is used as a filling agent and polylactic acid is added at the same time, so that the prepared minodronic acid tablet is uniform in content and favorable to release; and compared with the prior art, the direct tabletting method is capable of solving the problem that the minodronic acid tablets obtained via powder direct tableting are easy to crack and not good for coating, so that the medicine quality is ensured.

The invention discloses a preparation method of a beta-aminophosphonic acid derivative. The preparation method comprises the following steps of dissolving N-(arylvinyl)benzamide, dialkyl phosphite, manganese acetate and potassium carbonate in a solvent, performing reaction at a room temperature to acquire a (2-benzamido-1-arylvinyl)dialkyl phosphonate derivative, and performing reductive hydrolyzation on a compound to acquire the beta-aminophosphonic acid derivative. By using an N-(arylvinyl)benzamide derivative as an initiator, the preparation method is available in raw material and various in preparation method. The preparation method is simple and short in synthetic route, mild in reaction condition, simple in reaction operation and aftertreatment process and better in yield and is suitable for scale production.

The present invention provides β-hydroxy-γ-aminophosphonates, β-amino-γ-aminophosphonates, and analogs thereof that inhibit carnitine acyltransferases. The invention also provides compositions comprising these β-hydroxy-γ-aminophosphonates, β-amino-γ-aminophosphonates, and analogs, and methods of the use of such compounds and compositions in the treatment, amelioration or prevention of pathological conditions, diseases or disorders that are linked with fatty acid metabolism, such as non-insulin dependent diabetes or obesity. The invention also provides processes for the preparation of such compounds and compositions.