239 results about "Acarbose" patented technology

The present invention relates to a pentacyclic triterpanoid derivative of multiple-oxide substitution of the A ring and the C ring and the medicine salt or solvate of the derivative, and the present invention also relates to the preparation method, the drug combination, and medical use of the derivative. The compound of the present invention has the functions of inhibiting the activity of six human tumor cell strains in vitro, such as human prostate cancer cell (PC-3), nasopharyngeal carcinoma cells (CNE), oral squamous carcinoma cell(KB), human lung cancer cell (A549), human hepatoma cell (BEL-7404), and human cervix cancer cell (Hela), and the function of the invention is at the same magnitude of the positive control of cisplatin, thereby the compound can be used as expected antitumor drug. The compound of the present invention also inhibits the alpha glucosidase strongly, and the inhibiting effect is greater than the positive control of acarbose, thereby the compound can be used as expected medicine for preventing and treating diabetes and the treatment of the virus diseases.

The invention discloses a method for preparing acarbose, which comprises the following steps: (1) actinoplane slants are inoculated in a slant culture medium for slant culture; (2) slants with full growth are selected and inoculated in a seed culture medium for seed culture; (3) fermentation cylinder culture is carried out, and glucose and maltose are added into a fermentation culture medium in afluid mode in a culture process. The method is characterized in that a nitrogen source is also added in the fluid mode in the step (3); and the content of amino nitrogen in the culture medium after adding the nitrogen source in the fluid mode is controlled to be smaller than or equal to 0.15 mg/ml except 0 mg/ml. The method overcomes the defect of difficult separation of components C which are impurities in the prior art, replenishes the nitrogen source in the process of fermentation, controls the content of the nitrogen source and can reduce the formation of the impurities C while greatly improving the yield of the acarbose.

The invention relates to a medicine composition containing acarbose. The composition can be made into orally disintegrated ablets through screening each minor ingredient and dosage thereof. Therefore, the invention overcomes the defect of inconvenient taken existing in the prior tablet and capsule, and provides an acarbose preparation which can be disintegrated quickly in oral cavity, and can be taken more easily without water.

The invention discloses a method for preparing acarbose through microbial fermentation. The method comprises the following steps: inoculating acarbose producer (CCTCC NO:M 209022) in fermentation medium which is suitable for the strain and contains carbon source, nitrogen source and inorganic salt, fermenting and culturing at 20-32 DEG C for 96-192 hours, obtaining fermentation liquor after fermentation, extracting to obtain acarbose. The method is characterized in that fermenting and culturing are performed for 0-48h and validamycin A solution is added to ensure that the one litre of fermentation medium contains 0.04-0.4g of validamycin A. By supplementing validamycin A in the fermentation process of acarbose, the fermentation level of acarbose can be increased.

The invention discloses sargassum pallidum polysaccharide selenium as well as a preparation method and an application thereof. The preparation method mainly comprises steps as follows: raw material pretreatment, hot water extraction, decoloration, deproteinization, freeze drying and selenylation reaction, wherein the selenylation reaction is implemented as follows: sargassum pallidum polysaccharide and dilute nitric acid are mixed and stirred at the room temperature, sodium selenite and barium chloride are added respectively, the mixture is heated to 60-80 DEG C, stirred and mixed uniformly toreact at the microwave power of 100-500 W for 3-5 min, a sargassum pallidum polysaccharide selenium solution is obtained, cooled to the room temperature, placed in a dialysis bag for dialysis and freeze-dried, and sargassum pallidum polysaccharide selenium is obtained. The preparation method is simple, the reaction condition is mild, the sargassum pallidum polysaccharide selenium is pollution-free and high in selenylation degree, has remarkable alpha-glucosidase inhibition activity, has the activity superior to that of acarbose and can remarkably improve the antioxidase activity of cells andreduce the content of malondialdehyde, a dietary supplement with antioxidant and blood sugar reducing efficacy can be developed, and the sargassum pallidum polysaccharide selenium can be applied to the field of food or medicines.

The invention discloses a preparation method of an alpha-glycosidase inhibitor 2,3,4-trihydroxy benzaldehyde-9'-O-berberine acylhydrazone, and can be used for preparing the medicines to treat diabetes. A structural formula of a compound is shown in the description. The preparation method comprises the following steps: 1) taking berberine hydrochloride as an initial raw material, demethylating under pressure reduction 190 DEG C condition, wherein the products can not be separated to obtain berberrubine (I), bridging the obtained compound I and alpha-ethyl bromoacetate through a nucleophilic substitution reaction to form a berberine ethyl acetate derivative (II); 2) performing hydrazinolysis of the compound II and hydrazine hydrate to obtain berberine hydrazides (III); and 3) performing nucleophilic addition-dehydration reaction on the compound III and the 2,3,4-trihydroxy benzaldehyde to obtain the 2,3,4-trihydroxy benzaldehyde-9'-O-berberine acylhydrazone (TM), and purifying the products through a recrystallization method. The 2,3,4-trihydroxy benzaldehyde-9'-O-berberine acylhydrazone has strong alpha-glucosidase inhibition activity through alpha-glucosidase inhibition experiment, and its inhibition performance is higher than that of a comparison product acarbose by 1.2 times.

The invention discloses a method for preparing high- purity acarbose. The foreign substance A content in purified acarbose is far behind pharmacopeia standard by controlling the temperature being 0- 25 Deg. C during pretreating process. The invention is characterized by low production cost and suitability for industrial production.

The invention discloses a simple fermentation method for acarbose. The method adopts actinoplanessp or a strain of the same species of the actinoplanessp as a fermentation strain. The method comprises fermentation steps of: (1) shaking flask fermentation, (2) carrying out fermenting in a 100-L fermenter, (3) carrying out fermenting in a 30-m<3> fermenter. According to the simple fermentation method for the acarbose provided by the present invention, a carbon source control strategy for fed-batch fermentation of the acarbose is researched through adopting the actinoplanessp or other strains ofthe same species of the actinoplanessp, and research results show that a controlled concentration of total sugar in a feeding phase, especially the controlled concentrations of maltose and glucose have remarkable effects on the synthesis of the acarbose. Based on this point, two key parameters of the total sugar and reducing sugar (the maltose and the glucose) are screened as amplification factors, such that an industrial fermentation scale-up of the acarbose from the 100-L fermenter to the 30-m<3> fermenter is realized.

The invention discloses an application of a cardiospermum halicacabum extract in the preparation of medicinal preparations for treating diabetes. The cardiospermum halicacabum extract comprises taraxerol and/or 3[beta]-alnusonol. The results of alpha-glucosidase inhibition experiment show that taraxerol and 3[beta]-alnusonol can both inhibit the activity of alpha-glucosidase, the inhibition performance of taraxerol and 3[beta]-alnusonol is highly similar with that of a reference substance (acarbose), and thus the cardiospermum halicacabum extract can be used to treat diabetes.

The invention provides applications of four kaurane diterpene compounds in preparation of glycosidase inhibitor medicines. The four compounds capable of highly inhibiting alpha-glycosidase activity are natural compounds which are high in safety and capable of rapid natural degradation without residue in the environment. The four compounds are obtained by separation from wedelia trilobata, and other plant materials. The plant materials are rich in source. A preparation process is easy in operation. Monomers of the four compounds are stable and liable to store. The alpha-glucosidase inhibition activity of the four compounds is obviously higher than or equivalent to that of acarbose that is a clinic medicine. The four compounds are extremely likely developed into effective and safe alpha-glucosidase inhibitor medicines used for preventing and treating type II diabetes, and have good prospects.

The invention discloses a method for preparing acarbose, which adopts four enzymes to cooperatively carry out starch liquefaction and saccharification, and comprises the following steps that: (1) starch emulsion is liquefied with alpha-amylase at appropriate pH and temperature, and the DE (Dextrose Equivalent) value is controlled between 11 and 18; (2) the starch liquefied liquid is cooled to an appropriate temperature, the appropriate pH is adjusted, pullulanase, fungal enzyme and beta-amylase are added, certain time is maintained, and the composite maltose conversion rate can reach 85-95%; and (3) the liquefied starch is used for acarbose fermentation after being sterilized. According to the starch liquefaction method provided by the invention, the compound maltose content is high, and the high yield and the low impurities of acarbose fermentation are ensured. The method is simple, is easy to operate and is low in cost, and is suitable for the industrial production of acarbose fermentation.

The invention provides a preparation method of spermacoce latifolia triterpenoids and an application of the spermacoce latifolia triterpenoids in preparation of a glycosidase inhibitor medicine. Six compounds for intensively inhibiting the activity of alpha-glycosidase provided by the invention are natural compounds which are high in safety, and can be naturally degraded rapidly without a residue in the environment. The compounds can be separated from plant materials such as spermacoce latifolia; the plant materials are abundant in source; and the preparation process is easy to operate. Monomers of the six compounds are relatively stable and easy to store; the alpha-glycosidase inhibiting activity is obviously higher than that of clinical medicine acarbose; and the compounds are extremely likely to be further developed into the effective and safe alpha-glycosidase inhibitor medicines for preventing and treating type 2 diabetes mellitus, and have relatively good prospects.

The invention discloses Actinoplanes utahensis MYIH97 and application thereof, the strain is preserved by China Center for Type Culture Collection, the preservation number is CCTCC NO:M 2016237, and the preservation date is May 3<rd>, 2016 .The invention further discloses a method for preparing acarbose through fermentation of the strain .For the fermentation process, it is proved through mass production practice that the fermentation unit is high, the impurities are less, the post-extraction difficulty is greatly reduced, the fermentation process is suitable for industrial mass production, and the quality of the obtained acarbose products is high.

The invention discloses a method for establishing and analyzing a scale metabolism network model of actinoplanetes genomes, and belongs to the field of systems biology. Cell growth simulation, essential growth essential genes and reaction verification are carried on the scale metabolism network model of actinoplanetes genomes established based on the method on a system level, a strategy is provided for simulating and improving acarbose yield, and an important platform is provided for comprehensively understanding the metabolic characteristics of actinoplanetes and improving the acarbose fermentation level. The invention provides multiple methods for improving the acarbose yield, the acarbose yield can be increased by 53.5% by adding nicotinic acid, and the acarbose yield is respectively increased by 29.6%, 26.5%, 26.3%, 11.8% and 9.2% by adding glutamic acid, cysteine, lysine, glutamine and asparagines.

The invention provides a triterpene compound represented by the formula (1) or formula (2). The preparation method comprises the following steps: grinding dry fruiting bodies of lucid ganoderma, extracting the fruiting bodies by isopropanol, concentrating the liquid extract in vacuum to obtain an extract; and subjecting the obtained extract to MCI column chromatography and silica gel column chromatography in sequence to obtain the triterpene compound represented by the formula (1) or formula (2). A pharmaceutical composition made of the triterpene compound and pharmaceutical auxiliary materials can be used to prepare drugs for treating diabetes. The provided triterpene compound has a better activity on inhibiting alpha-glycosidase, compared with acarbose sold on the market. Moreover, the molecular weight of the triterpene compound is small, and thus the dosage is little.

The invention relates to a method for detecting acarbose through high performance liquid chromatography. The chromatographic conditions are as follows: chromatographic column: XBridge Amide column (waters, 4.6mm*250mm, 3.5mu m); mobile phase: organic phase-water phase; flow velocity: 1.0-1.4mL/min; detection wavelength: 210nm; column temperature: 60-70 DEG C; sample size: 10-20mu l. An ultraviolet detector is adopted as a detector; the volume ratio of organic phase to water phase in the mobile phase is (75:25)-(80:20); acetonitrile is taken as the organic phase in the mobile phase; ammonium acetate is contained in the mobile phase; the concentration range of ammonium acetate is 5-10mM and pH range is 5.0-10.0. Compared with the existing method, the method has the advantages that the complete separation of acarbose and impurity A is realized, another unknown impurity can be additionally separated and the product quality of the acarbose can be preferably controlled.

The invention relates to a chewing tablet taking acarbose as an active component. The acarbose is taken as the medical active component, and the acarbose is mixed with a pharmaceutically acceptable auxiliary material to form the drug composition. The acarbose has the defect of easy hardening due to absorption of moisture, but the novel compound auxiliary material, namely Avicel CL611 is used in the chewing tablet, so that the chewing tablet has the advantages of simple process, direct tabletting, time conservation and labor conservation, and can also overcome the defect of easy absorption of moisture existing in the common chewing tablet.

The invention discloses a method for improving the purity of acarbose. According to the method, impurities A in acarbose extracting solution are removed by an aluminum oxide chromatographic column. In the regenerating process, acid and base are utilized and organic solvents are not related, and compared with the traditional aluminum oxide regenerating process, the method has the following differences: the high-temperature activation is not needed, so that the process operation is simplified. According to the method, the impurities A in the acarbose extracting solution are removed by the aluminum oxide chromatographic column, and the high-purity acarbose bulk drug can be produced; the acarbose is purified by aluminum oxide, so that the content of the impurities A in the acarbose can be reduced effectively, part of pigments can be removed, and compared with the other method for preparing the high-purity acarbose, the method has the advantages that the purity of the acarbose is improved by 2%, the pigments in feed liquid are removed effectively, the safety and the stability of drug use of a patient can be improved finally. According to the method, the total yield is increased obviously, and the yield is high and is more than 88.95%.

The invention discloses a method for fermenting acarbose. The method comprises the following steps of: (1) taking Actinoplanes species and inoculating into actinomyces seed culture medium to prepare seed solution; and (2) taking the seed solution prepared in the step (1), inoculating into an actinomyce fermentation medium, and fermenting, thereby obtaining acarbose fermentation broth, wherein selenium with the concentration of 2-21mg/L is added in the fermentation medium. The fermentation method disclosed by the invention has the advantages of increasing the yield of the acarbose, remarkably reducing the content of an impurity A in the acarbose and shortening the fermentation period.

The invention discloses an acarbose drug combination and a preparing method thereof and particularly relates to an acarbose tablet. According to the composition, a filling agent is one or more of lactose anhydrous and low-moisture starch. Compared with the prior art, the acarbose drug combination and the preparing method thereof have the advantages that by selecting the varieties of auxiliary materials in the tablet, the acarbose drug combination which is prepared through a simple preparation technology and is low in moisture content, not prone to moisture absorption, resistant to humidity to a certain extent and high in stability is provided. The product prepared through the method is high in stability, the stability of all item indexes such as the appearance of the tablet and the impurities is obviously superior to those of acarbose sold on the market of Bayer; in addition, the preparation technology is simple and easy to control, the production efficiency is high, and energy consumption for production is low.

A purification process for manufacturing a high pure acarbose relates to a process for preparing high pure acarbose from acarbose-containing fermentation broth. The acarbose was purified through steps of alcohol precipitation, a strongly acidic cation exchanger chromatography and an immobilized enzyme affinity chromatography. Acarbose is generally applied in treating diabetes.