64results about How to "Comply with medicinal requirements" patented technology

The invention relates to an industrial preparation method of officinal histamine dihydrochloride. The preparation method comprises the following steps of: suspending histidine in hexahydrocresol which is used as a reaction solvent; carrying out a decarboxylation reaction at the temperature of 170 DEG C-175 DEG C; and then quantitatively dropwise adding the hexahydrocresol solution containing hydrochloric acid twice so as to synthesize histamine dihydrochloride. According to the invention, the content of the related substances in histamine dihydrochloride is less than 0.5%, and the content of a single impurity in histamine dihydrochloride is less than 0.1%, thus the histamine dihydrochloride completely meets officinal grade; and the preparation method is simple in equipment, easy and simple in process operation and safe and reliable in reaction; and the solvent can be recycled, thus the preparation method is environment-friendly and is beneficial to industrial large-scale production.

The invention provides a silybin and phosphatidy lcholine compound which is prepared into capsules with high dissolving degree. The invention also provides a process for preparing the silybin and phosphatidy lcholine compound and its capsule medicament, the preparing process is characterized by simple manufacturing method, high yield and fitting for mass production.

The invention discloses a vortioxetine hydrobromide crystal preparation method. The method comprises a, dissolving vortioxetine free alkali in ethyl acetate at a temperature of 20-30 DEG C, b, carrying out filtration, cooling the filtrate to a temperature of 0-10 DEG C, dropwisely adding an ethyl acetate solution of hydrobromic acid into the filtrate along with thermal insulation and then carrying out thermal insulation stirring for 2-8h, c, filtering the mixture subjected to thermal insulation stirring in the step b to obtain filter cake 1, leaching the filter cake 1 by ethyl acetate, and carrying out stirring washing in ethyl acetate at a temperature of 0-10 DEG C for 0.5-5h, d, filtering the mixture subjected to stirring washing in the step c to obtain filter cake 2, leaching the filter cake 2 by methyl tert-butyl ether / ethyl acetate pre-cooled at a temperature of 0-10 DEG C and carrying out stirring washing in methyl tert-butyl ether at a temperature of 10-30 DEG C for 15-24h, and e, filtering the mixture subjected to stirring washing in the step d to obtain filter cake 3, leaching the filter cake 3 by methyl tert-butyl ether and carrying out vacuum drying at a temperature of 40-50 DEG C to obtain the product. The method has the advantages of good repeatability, simple processes, a high yield and high product purity and is suitable for industrial production.

The invention provides a maleic acid levorotation amlodipine drug active pharmaceutical composition which comprises the following components: component I: maleic acid levorotation amlodipine; component II: dextrorotation amlodipine; component III: aspartic acid amlodipine; component IV: impurity D; and the active pharmaceutical composition does not contain impurity A, impurity B, impurity C, impurity E, impurity F, impurity G and impurity H basically. The active pharmaceutical composition is stable in quality, and can completely meet the quality requirement of maleic acid levorotation amlodipine preparation on active pharmaceutical composition; and the prepared preparation is safe, effective and controllable in quality, and ensures the clinical effect and medication safety of the maleic acid levorotation amlodipine preparation.

The present invention discloses a hydrobromic acid vortioxetine crystal that has diffraction peaks at 8.55+ / -0.2, 13.05+ / -0.2, 13.44+ / -0.2, 14.46+ / -0.2, 15.20+ / -0.2, 16.63+ / -0.2, 16.94+ / -0.2, 17.22+ / -0.2, 17.85+ / -0.2, 19.83+ / -0.2, 20.43+ / -0.2, 21.33+ / -0.2, 23.14+ / -0.2, 23.60+ / -0.2, 24.77+ / -0.2, 26.25+ / -0.2, 26.72+ / -0.2, 26.96+ / -0.2, 29.69+ / -0.2, 30.52+ / -0.2, 33.33+ / -0.2, 33.89+ / -0.2, 34.89+ / -0.2, 35.54+ / -0.2, 37.03+ / -0.2, and 38.33+ / -0.2 in a powder X-ray diffraction diagram represented with 2 theta. In addition, the present invention further discloses a preparation method for the crystal. The hydrobromic acid vortioxetine crystal and the preparation method therefor in the present invention have good repeatability, easy operation, good product stability, and high yield and purity, and are suitable for industrial production.

The invention provides a butylphthalide pharmaceutical active composition, comprising the following components: component I: butylphthalide content ≥ 98.0%; component II: selected from methylenephthalide, vinylphthalide, propylenephthalide, butylphthalide One or more of enphthalide, pentylenephthalide, phthalide, toluene, ethylphthalide, propylphthalide, and pentylenephthalide, and the content of component II > 0 and ≤ 2.0%; when the component When any one of methylenephthalide, vinylphthalide, propylenephthalide, butylenephthalide, and amylenephthalide is contained in II, the maximum content of any one of the ingredients contained therein shall not exceed 0.5%. When component II contains When any one of phthalide, methylphthalide, ethylphthalide, propylphthalide, and pentaphthalide is used, the maximum content of any one of the ingredients contained in it shall not exceed 1.0%. The pharmaceutical active composition has stable quality and can guarantee the clinical curative effect and drug safety of the butylphthalide preparation.

The invention discloses a pharmaceutical composition containing flurbiprofen and a patch, namely a pharmaceutical composition. The pharmaceutical composition contains flurbiprofen serving as an active ingredient and pharmaceutically acceptable auxiliary materials, and the pharmaceutically acceptable auxiliary materials at least comprise a stabilizer, wherein the weight ratio of the flurbiprofen to the stabilizer is 1: (0.5-2). In the pharmaceutical composition, the flurbiprofen is dispersed in an amorphous manner, wherein all the components are matched with one another, so that the hot-melt pressure-sensitive adhesive transdermal preparation containing the composition has the characteristics of good stability of active components and excellent transdermal absorption performance.

The invention discloses a synthesis method of high-purity histamine dihydrochloride, and belongs to the technical field of organic synthesis. The method comprises the steps: in a solvent A, carrying out a decarboxylation reactionon L-histidine at the temperature of 110-150 DEG C under the effect of a composite decarboxylation catalyst, and carrying out filtering after the reaction is completed, wherein the composite decarboxylation catalyst is composed of a main catalyst and an auxiliary catalyst, the main catalyst is selected from sodium hydroxide, potassium hydroxide, sodium carbonate, potassium carbonate, pyridine, 4-methylpyridine, aniline, 4-methylaniline, ,N,N-dimethylaniline and N, N-dimethylformamide, and the auxiliary catalyst is one selected from benzophenone, acetophenone, benzophenone and p-methyl acetophenone; carrying out reduced pressure distillation on a filtrate, adding water into residues, and adjusting the pH value to 5-6 by using hydrochloric acid to obtain an aqueous solution; extracting the aqueous solution at least once by using an extracting agent to remove impurities; and evaporating to remove water in the aqueous solution, pulping with a solvent B, filtering and drying to obtain the product.

The invention relates to the technical field of pharmaceutical chemicals, and provides a refining method of thymol. The refining method comprises the steps that a refining solvent is added to crude thymol, and the mixture is heated and stirred sufficiently to obtain a first mixed solution; the amount of the refining solvent is 0.5-3 times the mass-volume ratio of the crude thymol; an adsorbent isadded to the first mixed solution, and thermal insulation decolorization treatment is performed to obtain second mixed liquid; and the second mixed liquid is filtered, the obtained filtrate is subjected to cooling crystallization, thermal insulation crystallization and cooling crystallization separately, then centrifugal filtering is performed, and the thymol is obtained. The refining method can refine impurities such as citronellal and isopulegol in the crude thymol to a hardly detected degree, the purity of the product is effectively improved, and the medical requirements are met; and meanwhile, compared with a traditional rectification method, the refining method is simple, and the refining cost is greatly reduced.

The invention provides a butylphthalide bulk drug product, the butylphthalide content of which is not less than 99.0%. The bulk drug has stable quality and can ensure the clinical curative effect and medication safety of the butylphthalide preparation.

The invention relates to a method for preparing cariprazine and an intermediate thereof, and the method comprises the following steps: taking trans-4-aminocyclohexane acetate hydrochloride as a starting material, and carrying out Boc protection, reduction, halogenation, nucleophilic substitution, Boc protection removal and amidation reaction to prepare the cariprazine. The alcoholic hydroxyl group of the trans-2-{1-[4-(N-tert-butoxycarbonyl)-amino]-cyclohexyl} ethanol is activated and converted into a group easy to leave, the alcoholic hydroxyl group is creatively converted into the halogen atom, the reaction condition is mild, the yield is high, the raw material medicine which is high in purity and low in impurity content and meets the medicinal requirement can be obtained, and the method is suitable for industrial production.

The invention discloses a method for expressing and preparing staphylokinase (Staphylokinase, SAK), comprising: 1. Construction of staphylokinase fusion protein expression engineering bacteria: constructing a recombinant plasmid containing the gene sequence of SEQ NO.1, and introducing the recombinant plasmid into Escherichia coli to obtain fermentation strains. 2. The preparation method includes: a. fermenting and expressing a soluble fusion protein having an amino acid sequence such as SEQ NO.2 by engineering bacteria; b. absorbing the fusion protein in step a with a nickel ion affinity gel column to extract the fusion protein; c. Dilute the fusion protein in step b with enterokinase, dilute appropriately, pass through the gel column in step b, and collect the permeate; d, concentrate the permeate through ultrafiltration in step c, and pass through the Q gel column to obtain the staphylokinase stock solution . The method of the invention has simple and reliable steps, and is especially suitable for large-scale production. The staphylokinase obtained by the method of the invention has high purity, high specific activity and good thrombolytic activity; it provides a new way for producing medicinal staphylokinase.

The invention discloses a preparation method of a benzamide histone deacetylase inhibitor with differentiation and anti-proliferation activity. The structure of the benzamide histone deacetylase inhibitor is as shown in a general formula (I), wherein A, Z, Y, B, R1, R2, X1, X2, X3 and X4 are defined as the specification. The compound as a histone deacetylase inhibitor can be used for curing and differentiating the diseases, such as cancer and psoriasis which are related to proliferation.