36 results about "Glimepiridum" patented technology

The invention discloses a Glimepiride tablet, wherein the Glimepiride tablet comprises the following components: Glimepiride tablet bulk pharmaceutical chemical, lactose, sodium starch glycolate, microcrystalline cellulose, microcrystalline silica gel and magnesium stearate at the weight ratio of (2-6):(60-90):(10-30):(10-60):(2-6):1, wherein the Glimepiride tablet bulk pharmaceutical chemical ispowder with the particle size less than 2 mu m. The invention also discloses a preparation method. With regard to Glimepiride, pharmaceuticals are smashed into particulates with the particle size less than 2mu m by an improved technology, and the hydrophilicity of the pharmaceuticals is improved; and the problem that the dissolution velocity of the pharmaceuticals is influenced is solved. Statistical analysis indicates that the average dissolution degree is above 98.5% by adopting the improved prescription and technology, and the accelerated test result for 6 months is very stable; and the research on primary pharmacokinetic parameters indicate that the preparation has the advantages of better dynamic course in human bodies and better absorption elimination properties through the checkingof statistics.

The invention provides glimepiride orally disintegrating tablets. The orally disintegrating tablets are prepared by an inclusion technology, effectively solve the problems about the taste and disintegration of a main medicine, are convenient to operate, transport and store, have broad application range, and are suitable for large-scale production.

The preparation method of the glimepiride tablet comprises the following steps: S1, micronizing a glimepiride raw material medicine by adopting an airflow crushing method, and controlling the particlesize of glimepiride raw material medicine powder to be less than 10 microns; S2, weighing the glimepiride raw material medicine powder crushed in the step S1 and auxiliary materials in proportion; S3, mixing, crushing and sieving the glimepiride raw material medicine weighed in the step S2 and lactose, and adding the mixture and part of carboxymethyl starch sodium into a wet granulator for mixingto obtain premixed powder; S4, adding povidone into the wet granulator in the step S3 to prepare a soft material, granulating, and drying in a fluidized bed; and S5, adding the dried granules into the remaining sodium carboxymethyl starch, pregelatinized starch and magnesium stearate weighed in the step S2, mixing, and tabletting. The invention solves the problem of poor similarity of multiple dissolution curves of the main drug and the reference preparation in the preparation process in the prior art.

The invention discloses a glimepiride dispersible tablet. After filling agent lactose contained in the prescription is screened by a 150-mesh sieve, micronization treatment does not need to be carried out to the basic remedy, glimepiride, the dissolution rate at the time of 15 minutes can reach above 90 percent, all indexes meet the medical standard, and the stability is good. The invention also discloses a preparation method of the dispersible tablet, which has no special requirement on equipment, and is simple in operation and suitable for industrial production and application.

The invention discloses a method for determining the concentration of glimepiride in blood plasma by liquid chromatography-mass spectrometry, which adopts a liquid chromatography-mass spectrometry system for determination and comprises the following steps: taking a sample to be determined, adding a certain amount of mixed organic solvent for extraction and pretreatment, performing separating by achromatographic column, and performing detecting by using a mass spectrometry detector. The method disclosed by the invention is rapid, accurate, high in sensitivity and simple and convenient to operate, and provides a basis for measuring the blood concentration of glimepiride; the linear range of a plasma standard curve of the method is 0.5-500 ng / mL, the intra-batch precision RSD and the inter-batch precision RSD are both smaller than + / -15%, and the method is suitable for measuring the concentration of glimepiride in plasma.

The invention relates to the field of pharmaceutical preparations, and in particular discloses a compound controlled-release preparation of metformin hydrochloride and glimepiride and a preparation method of the controlled-release preparation. The controlled-release preparation disclosed by the invention consists of an internal controlled-release tablet which contains the metformin hydrochloride and an external drug-loaded coating which contains the glimepiride, wherein the internal controlled-release tablet which contains the metformin hydrochloride comprises a tablet core, an insoluble semipermeable coating film and drug-release small pores. The controlled-release preparation disclosed by the invention can significantly improve the linearity and the uniformity of drug release, the process (the preparation method) is simple and easy to implement, and the tablet is better in compressibility; and the glimepiride, without micronizing treatment or other special treatment, is excellent in dissolving effect.

The invention relates to a glimepiride tablet and a preparation method thereof. The tablet is prepared by the following method: dissolving glimepiride in a sodium hydroxide solution, adding mesoporous silicon dioxide, stirring evenly, and stirring Add glacial acetic acid to this solution, the glimepiride and mesoporous silica complex precipitates, filter, dry, then mix with fillers and disintegrants, granulate, dry, add lubricant to the dry granules, Formed into tablets. Compared with the prior art, the tablet prepared by the invention dissolves rapidly in water, has a simple preparation process and is suitable for industrial production.

The invention provides a specific primer for detecting the T1369G polymorphic site (rs757110) genotype of the SUR1 gene by a PCR method, and the specific primer is used in the preparation of reagents for detecting the T1369G polymorphic site of the SUR1 gene by PCR amplification of biological samples The application in the invention, the SUR1 gene T1369G polymorphic site detection kit containing specific primers and the application of the detection kit to predict the effect of sulfonylurea drugs. Sulfonylurea drugs are selected from glibenclamide, glibenclamide, glibenclamide, glibenclamide, glimepiride, glibenclamide, glibenclamide, glibenclamide, glibenclamide , glipizide, gliclazide, glipizide, and gliquidone, preferably gliclazide or glimepiride.

The invention relates to a preparation method of glimepiride intermediate compound I, which belongs to the technical field of preparation of raw materials. The preparation method of the present invention comprises the following steps: reacting compound II and diphenyl carbonate under the catalysis of a base (refer to Synlett, 28(18), 2495-2498; 2017) to prepare compound IX; then compound IX and 4‑(2‑Aminoethyl)benzenesulfonamide is fed at a ratio of 1:1, a weak acid is added, isopropanol is added, and the reaction is heated under reflux. The technical scheme of the present invention provides a method for preparing a high-purity glimepiride intermediate.

The invention relates to a preparation method for a glimepiride tablet. A formula technology of the glimepiride tablet is optimized, working procedures of granulation and drying are combined and simplified, glimepiride raw materials and lactose are added together as base materials, the glimepiride raw materials and the lactose are subjected to particle size regulation and control, proper mist spray pressure is adopted, and the dissolving property of raw materials in a fluidization and granulation process generates unexpected change, i.e., a dissolution rate can be guaranteed. Meanwhile, a similarity between an own product and a plurality of dissolution curves of a reference preparation can be improved, and an in vivo equivalence possibility with the reference preparation is improved.

The invention relates to a preparation method of glimepiride crystal form I, which belongs to the technical field of preparation of raw materials. The preparation method of the Limepiride crystal form I of the present invention comprises the following steps: dissolving the crude glimepiride in an aqueous alcohol solution, adding an appropriate amount of ammonia water, stirring to dissolve; filtering, adding acetic acid to the filtrate, and neutralizing the filtrate Ammonia in the crystalline form II, to obtain glimepiride crystal form II; to the crystal form II, add a ketone solvent 4 to 8 times its mass, stir at a temperature range of 10 to 35 °C for more than 10 hours, filter, and bake at 70 °C dry to obtain the glimepiride crystal form I product. The invention obtains a high-quality glimepiride crystal form I bulk drug.

The invention provides a glimepiride detection method which comprises the following steps: preparing standard solutions with at least three concentrations of glimepiride and internal standard substances, and ensuring that the quantities of the internal standard substances in the standard solutions are the same; detecting each standard solution by using a liquid chromatograph-mass spectrometer under a detection condition to obtain a first detection result corresponding to the standard solution; simulating a standard curve equation of qualified glimepiride according to each first detection result, the concentration of glimepiride in the standard solution and the concentration of an internal standard substance; taking a first supernatant of a sample to be treated after centrifugation; addingthe internal standard substance into the first supernatant, uniformly mixing in a vortex manner, sequentially adding an extracting agent, and extracting the first supernatant to obtain a sample to bedetected; detecting the sample to be detected by utilizing the liquid chromatograph-mass spectrometer under the detection condition to obtain a second detection result of the sample to be detected; and based on the standard curve equation and the second detection result, obtaining the concentration of glimepiride in the sample to be detected. The scheme can shorten the sample detection time.

The invention discloses a qualitative analysis detection method for illegally mixed high-polar chemical anti-diabetic components in anti-diabetic traditional Chinese medicine products. The method comprises the following steps that: 1) high efficient liquid phase chromatography conditions: an ammonium acetate-triethylamine-acetonitrile moving phase system and a C18 chromatographic column with certain specification are used, the wavelength is detected by ultraviolet, and the flow rate is 1.0ml / min; 2) analysis result: glibenclamide, glipizide, gliclazide, glimepiride, gliquidone, repaglinide, nateglinide, rosiglitazone and pioglitazone hydrochloride can realize the complete separation; 3) result judgment: when retention time of a chromatographic peak in an anti-diabetic traditional Chinese medicine product is consistent with that of anti-diabetic medicine in the step 2) and the apparent absorption is shown out, which indicate that the anti-diabetic medicine is contained in the sample tobe tested. The method has the advantages of quickness, simplicity, convenience, high sensitivity, strong specialization, broad coverage and so on.

The invention belongs to the technical field of analysis, and relates to a rapid pretreatment method for detecting glimepiride and metformin in blood plasma, in particular to a rapid pretreatment method for enriching and detecting glimepiride and metformin in blood plasma based on a magnetic mesoporous graphene composite material. According to the method, the functionalized magnetic mesoporous graphene material is synthesized, and is used for the pretreatment process of the plasma sample and the method comprises the steps of extraction, cleaning, elution and detection, the sample treatment steps are obviously simplified, and the sample treatment time is shortened; the method can effectively eliminate interference caused by a matrix effect, is wide in linear range, good in recovery rate andhigh in sensitivity, can be used for simultaneously detecting the concentrations of glimepiride and metformin in blood plasma, and is further used for in-vivo pharmacokinetic analysis of glimepirideand metformin.

The invention belongs to the technical field of medicinal chemistry and particularly relates to a preparation method of a glimepiride impurity. The preparation method comprises the following steps: dropwise adding acetic anhydride into a solution of 2-phenethylamine and an organic solvent with a low boiling point to be subjected to reaction to generate N-acetyl phenethylamine; dropwise adding chlorosulfonic acid into the N-acetyl phenethylamine at the temperature of lower than 20 DEG C to be subjected to chlorosulfonation reaction, and performing hydrolysis after the reaction is completed to remove excess chlorosulfonic acid; performing filtration and washing to obtain an impurity J benzenesulfonyl chloride; performing ammonolysis on the impurity J benzenesulfonyl chloride to obtain an impurity J benzene sulfonamide; in acetone, enabling the impurity J benzene sulfonamide to firstly react with a catalyst and then react with trans-p-methylcyclohexyl isocyanate to obtain an impurity J acetyl substance; enabling the impurity J acetyl substance and ethanol to be subjected to alcoholysis under the condition of the catalyst to generate an impurity J and ethyl acetate; and performing refining to obtain a high-purity impurity J. The purity of the glimepiride impurity J prepared by the method is high, the liquid phase content of the glimepiride impurity J is greater than 98.5%, the rawmaterials used in the method are easily available, the process parameters are controllable, and the reaction is mild.