98 results about "Ginkgolide-B" patented technology

The invention discloses a method for extracting and separating ginkgolides B from folium ginkgo, which comprises the following steps: 1) taking the folium ginkgo, carrying out extraction by ethanol with different concentrations from high to low, combining extracting solutions, and reclaiming the ethanol to obtain concentrated extracting solution; 2) adding ethyl acetate into the concentrated extracting solution for extraction, reclaiming organic phase and concentrating the extracting solution into extract; 3) diluting the extract obtained in step 2), putting the extract to preferential polar imperforate adsorption resin, washing the preferential polar imperforate adsorption resin by ethanol, reclaiming the ethanol in eluate, and crystallizing by the ethanol to obtain ginkgolides compounds; 4) putting the ginkgolides compound crystal to silica gel column, washing the silica gel column by miscible liquids of normal hexane and ethyl acetate, and collecting eluate to obtain eluate of ginkgolides B; and 5) reclaiming solvent in eluate collected in step 4), and crystallizing the solvent by ethanol to obtain ginkgolides B monomer. The method has the advantages of simple process, low production cost, high purity of products, and easy industrial production.

The invention relates to application of 10-O-(dimethylaminoethyl) Ginkgolide B in preparing antipyretic, analgesic and anti-inflammatory medicaments. Indicated by tests, the 10-O-(dimethylaminoethyl) Ginkgolide B can inhibit cyclooxygenase-2, has obvious effects of dissociating heat, easing pain and resisting various acute and chronic inflammations and has the advantages of less side effect and low toxicity.

The invention discloses a ginkgolide B raw material, which is characterized in that: the ginkgolide B raw material is made through the following method that: ginkgo leaves or ginkgo leaf extracts are taken and boiled in a hydrochloric acid solution; the boiled liquid undergoes organic extraction after filtration; when the obtained extract is condensed, 100 to 200-mesh silica gel is added in the extract to be mixed and dried; silica gel column chromatography is used to collect eluent rich in ginkgolide B, and the ginkgolide B raw material is obtained through crystallization; and the content of ginkgolide B in the ginkgolide B raw material is more than or equal to 90 percent. The ginkgolide B raw material made through adopting the method has high purity of ginkgolide B, simple preparation technological process, high transfer rate and low cost, and is suitable for industrial production.

The invention discloses application of ginkgolide B to preparation of medicament for preventing and / or treating autosomal dominant polycystic kidney disease. A madin-darby canine kidney (MDCK) vesicle model is used for screening to find that the ginkgolide B inhibits formation and growth of vesicles. An experimental result shows that: the ginkgolide B has an obvious inhibiting effect on the formation and growth of MDCK vesicles and the effect of the ginkgolide B is in dose response relationship; the ginkgolide B has no cytotoxicity to MDCK cells, so that the vesicle inhibiting effect of the ginkgolide B is independent of the cytotoxicity; the ginkgolide B does not obviously induce MDCK cell apoptosis, so that the vesicle inhibiting effect of the ginkgolide B is independent of cell apoptosis promotion of the ginkgolide B; the ginkgolide B can promote the MDCK cells or vesicles to form tubular structures; and the effect is in dose response relationship; and the ginkgolide B has an inhibiting effect on the growth of the embryonic kidney vesicles. The ginkgolide B provides experimental data for development of a specific medicament for preventing and / or treating autosomal dominant polycystic kidney disease.

The invention relates to a ginkgolide B nanoliposomes drug and a method for preparing the same. The invention provides the ginkgolide B nanoliposomes drug including the following materials and the following radios: 8-12 mol compositions of cephalin and distearoyl choline with mole ratio of 1:3-6; 6-8 mol compositions of sojasterol and cholesterin with mole ratio of 1:2-4; 4-6 mol compositions of gamma-cyclodextrin / 2-hychoxypropyl-beta-cyclodextrin and alpha-cyclodextrin with mole ratio of 3:1; 0.2-0.4 mol methoxy polyethylene glycol 2000-hydrogenated soybean phosphatidylethanolamine; 2 mol ginkgolide B; and 0.1-0.5 mol vitamine E. A method for preparing the ginkgolide B nanoliposomes drug is also provided in the invention to produce the ginkgolide B nanoliposomes for target treating blocking of vessel or endothelial cell thereof, with a better healing effect than ordinary preparations of ginkgolide B.

The invention relates to an amino-acid ester derivative of ginkgolide B shown as a formula I and pharmaceutical salts thereof, a medicinal composition taking the compounds as active ingredients, and application of the compounds and the medicinal composition in serving as medicaments for treating cardiovascular and cerebrovascular diseases. In the formula I, A1 and A2 is residues of H, glycyl, L-alanyl, L-leucyl, L-valyl, L-isoleucyl, or L-phenylaminoacyl and other amino acids; A1 is the same as or different from A2; and A1 and A2 cannot be H at the same time.

The present invention relates to a bilobalide B dripping pills preparation and its preparation method. It is formed from effective component bilobalide B and matrix for making dripping pills. The weight ratio of bilobalide B and matrix is 1:1.5-9.

The invention relates to a ginkgolide B injection and a method for making the same. The method comprises the following steps that: ginkgolide B is taken as a raw material and is added in ethanol, glycerol and PEG600, wherein the ratio between the ginkgolide B and the ethanol is between 1:25 and 1:200; the ratio between the ginkgolide B and the PEG600 is between 1:25 and 1:600; and the ratio between the ginkgolide B and the glycerol is between 1:12.5 and 1:50. The ginkgolide B injection has good stability and low cost, and each index of the injection meets the requirements of preparation; moreover, the making process of the injection has the characteristics of quick dissolution of a raw material and simple process, and is suitable for industrialized production.

The invention provides a ginkgolide osmotic pump tablet and a preparation method thereof. The ginkgolide osmotic pump tablet provided by the invention is a double-layer tablet composed of a drug-containing layer and a push layer, and is coated, wherein the drug-containing layer comprises drug release holes. The ginkgolide osmotic pump tablet uses ginkgolide at effective positions of the ginkgo biloba extract as an active component, and a total amount of ginkgolide A, ginkgolide B, ginkgolide Cand bilobalide is not less than 70 %. According to the invention, by combining a solid dispersion solubilising technique and an osmotic pump tablets control-release technology, the ginkgolide is firstly prepared into the solid dispersion, and then further prepared into the ginkgolide osmotic pump tablet on a basis of improving solubility of poorly soluble components, thereby realizing synchronous slow release of complex components in the ginkgolide, reducing drug administration times and improving patient compliance.

The present invention is directed to the use of the extract of Ginkgo biloba leaves or isolated Ginkgolide B (GKB), a component of the extract of Ginkgo biloba leaves in a method for decreasing the expression of peripheral-type benzodiazepine receptor (PBR) in cells of a patient in need thereof. Further, the present invention is directed to the use of the extract of Ginkgo biloba leaves or isolated GKB in a method for decreasing the proliferation of cancer cells in a patient. More particularly, the present invention is directed to the use of the extract of Ginkgo biloba leaves or isolated GKB in a method of decreasing cancer cell proliferation in a patient wherein the cancer cell is human breast cancer cell. Even more particularly, the present invention is directed to the use of the extract of Ginkgo biloba leaves or isolated GKB in method of decreasing cancer cell proliferation in a patient wherein the cancer cell is of the aggressive and invasive phenotype and expresses high levels of PBR in comparison to non-aggressive cancer cell.

The invention aims to industrially produce ginkgolide B liposome medicinal composition injection and ginkgolide B liposome medicinal composition oral preparations through uniform formula, process and equipment by a molecule dispersing method. The invention provides a molar ratio formula of the component raw materials for preparing the ginkgolide B liposome medicinal composition, steps and method for preparing ginkgolide B liposome medicinal composition freeze-dried injection and oral preparations, and embodiments for preparation. The ginkgolide B liposome medicinal composition is used for treating cerebral and vascular diseases.

The invention relates to a high-purity ginkgolide and its composition. It is a white powder with slightly bitter taste. The content of ginkgolide A is 10-20%, the content of ginkgolide B is 10-20%, and the content of ginkgolide C is 10-20%. 5-15%, the bilobalide content is 30-50%, and the total lactone content is 80-95%. Ginkgo biloba is used as raw material, heated and refluxed with ethanol solution with a mass fraction of 20-80% to extract, the extract is concentrated to recover ethanol, separated by a macroporous resin column, desorbed by ethanol, diluted with water, and then passed through a gel-type hydrogen bond Adsorption and desorption of the adsorption resin, collection of effluent and desorption liquid, concentration, drying, ethanol dissolution, activated carbon decolorization, concentration and drying. The preparation process is simple, reliable, low in cost and high in yield, and no toxic organic solvent is used in the process, which is an environment-friendly process. The high-purity ginkgolide is used as an active ingredient to prepare a composition that can be used as various preparations (capsules, tablets, oral liquids, granules, powders, injections, etc.) of ginkgolide medicines or health care products.

The invention discloses a preparation method of a high purity monomer of lactone components of a ginkgo leaf extract. The preparation method comprises the following steps: raw material pretreatment, high speed counter-current extraction, vacuum liquid chromatography separation, high performance liquid chromatography (HPLC) separation, and solvent recrystallization. The obtained high purity monomer comprises ginkgolide A, ginkgolide B, ginkgolide C, ginkgolide J, ginkgolide M, and bilobalide. The preparation method is simple. The purity of prepared ginkgolides can reach 99% or above. The separation efficiency is high, the solvent consumption is little, and the preparation method is suitable for industrial production.

The invention discloses a method for separating and purifying GA (Ginkgolide A), GB (Ginkgolide B) and bilobalide from a folium ginkg extractive. The method comprises the following steps that 1), ethyl acetate is adopted for extraction; 2), a lower alcohol-water mixed solvent is adopted for leaching; an alcohol leaching extraction solution and an undissolved substance are obtained; 3), the undissolved substance is subjected to silica gel column chromatography separation to form GA and GB; and 4), the alcohol leaching extraction solution is concentrated till no alcohol exists, cooled and filtered; a mother solution is concentrated to dryness, and then subjected to crystallization with 30-35% of methanol for 3-5 times; and bilobalide is obtained. The method for separating and purifying GA, GB and bilobalide is simple in process route and is suitable for industrial production. The purity of GA, GB and bilobalide obtained by separation and purification is greater than 98%; transfer rates of GA, GB and bilobalide are greater than 80%; the yield is high; the production cost is low.

The invention discloses a method for preparing ginkgolide K. The method includes the following steps: 1, ginkgolide B is dissolved into organic solvents to obtain a solution; 2, fluorinating agents are added into the solution obtained in the step 1 for conducting a dehydration reaction, and the ginkgolide K is obtained through separation and purification. The method for preparing the ginkgolide K is easy to operate; meanwhile, the high yield and the high purity are achieved, and convenience is brought to industrialization large-scale production. (please see the specification for the formula).

The invention relates to the application of ginkgolide B in the preparation of drugs promoting the regeneration of nerve cell, wherein, the nerve cell is the nerve cell at the positions of brain tissue hippocampus, striaturn and lateral ventricle. The ginkgolide B can penetrate the blood-brain barrier to promote the neural stem cells at the positions of cerebral cortex, the hippocampus and the like to proliferate and be transformed into neuron, thus increasing the number of regenerative cells, so as to achieve the goal of rehabilitating neural damnification and preventing and remedying the disease of cerebral stroke.

The invention discloses a method for synthesizing ginkgolide B through converting a ginkgolide mixture by using stereum hirsutum thalli as a catalyst, belonging to the field of biotechnologies. The method comprises the following steps: carrying out amplification culture on stereum hirsutum strains, taking thalli which are obtained through a test tube slant, a liquid shake flask, seed culture and thallus separation as the catalyst, converting ginkgolide into ginkgolide B, and enabling a conversion solution to be subjected to centrifugation, ethyl acetate extraction and anhydrous alcohol crystallization, so as to separate ginkgolide B from fermentation liquor. By using the method, the purity of obtained ginkgolide B is not lower than 99%, and the ginkgolide conversion ratio is higher than 90%.

The invention discloses a detection method for residual solvents of bilobalide B. The detection method comprises the following steps: (1) conducting a chromatographic condition and system suitability test; (2) preparing a control solution; (3) preparing a test solution; (4) measuring: respectively precisely sucking up a right amount of control solution and test solution, and directly injecting a sample into a gas chromatograph, measuring, calculating the content of methyl alcohol, ethyl alcohol and ethyl acetate by an external standard method, and finally, working out residual quantities of all the solvents in the bilobalide B. Proved by methodology validation, the detection method disclosed by the invention has a good separating effect, and limit of detection, limit of quantitation, linearity, stability, recovery rate and the like all meet the requirements; the detection method can be used for detecting the residual quantities of the methyl alcohol, the ethyl alcohol and the ethyl acetate in the ginkgolide B; the method is high in sensitivity and repeatability; by adopting a direct sample injection method, the method is simple in treatment, convenient in operation, suitable for industrial production and use, and has greater application value.

The invention relates to a method for analyzing a high performance liquid chromatography of methanesulfonic amine ginkgolide B, comprising the following steps: using chromatographic columns with different polarities, adopting one or more organic solvents and aqueous-phase mixing liquid as a flowing phase, and under the detection conditions that the column temperature is 10-50 DEG C, the flow velocity of the flowing phase is 0.1-10ml / min, and the detection wavelength is 190-400nm, identifying bulk drugs and preparations of the methanesulfonic amine ginkgolide B, detecting relative matters and measuring the content by adopting an ultraviolet detector or a diode array detector so as to control the quality of the methanesulfonic amine ginkgolide B.

The invention discloses a Dengyin naotong pharmaceutical composition and a preparation method thereof, a preparation and an application thereof. The Dengyin naotong pharmaceutical composition is composed of 2-60 parts of scutellarin, 1-20 parts of ginkgolide B, 5-80 parts of ginsenoside Rg1, and 5-80 parts of ginsenoside Rb1 in parts by mass. The preparation method comprises the steps of pretreatment, preparation and post-treatment. The preparation is a freeze-drying powder injection prepared by adding a pharmaceutically acceptable auxiliary material in the Dengyin naotong pharmaceutical composition. The invention also provides the application of the Dengyin naotong pharmaceutical composition in preparation of medicines for preventing / treating ischemic cardio cerebrovascular disease. The Dengyin naotong pharmaceutical composition has strong drug effect and can effectively mitigate pathology change, cognition and behavior obstacle of ischemic cerebrovascular disease; security is good, the adverse reaction due to an impure compound cannot be generated when the Dengyin naotong pharmaceutical composition is used in a prescribed dosage scope; quality controllability is good, batch-to-batch difference of the traditional Chinese medicine injections can be effectively avoided; stability is good, and the Dengyin naotong pharmaceutical composition can be used for preparing the preparations comprising an injection.

The invention discloses application of tremella fuciformis thalli in preparation of ginkgolide B. According to the application, a method for preparing ginkgolide B comprises the following steps: carrying out amplification culture on tremella fuciformis strains, taking thalli which are obtained through a test tube slant, a liquid shake flask, seed culture and thallus separation as a catalyst, converting ginkgolide into ginkgolide B, and enabling a conversion solution to be subjected to centrifugation, ethyl acetate extraction and anhydrous alcohol crystallization, so as to separate ginkgolide B from fermentation liquor. By using the method, the purity of obtained ginkgolide B is not lower than 99%, and the ginkgolide conversion ratio is higher than 90%.

A ginkgolide type compound which serves as a powerful antagonist of platelet activating factors (PAF) has very good protective effects on focal cerebral ischemia and diffuse total cerebral ischemia. Ginkgolide is divided into ginkgolide A, ginkgolide B, ginkgolide C, bilobalide, ginkgolide K, ginkgolide L and the like. The content of ginkgolide L in ginkgo leaves is extremely low, so that ginkgolide L is difficult to obtain, and research report on ginkgolide L is nearly zero. The invention relates to a preparation method of ginkgolide L. Ginkgolide L is extracted from commercially available ginkgo total lactone or ginkgo total lactone obtained based on a known method. The preparation method is simple to operate, the raw materials are low in cost, a plenty of ginkgolide L can be obtained rapidly, and basis is provided for research on ginkgolide L.

The present invention discloses a Ginkgolide composition and a method for the preparation thereof. The composition includes two active components, Ginkgolide A and Ginkgolide B, and the weight ratio of Ginkgolide A to Ginkgolide B is 1: (2-9). A strong synergistic effect is found between Ginkgolide A and Ginkgolide B, which has a remarkable application effect on the treatment of cardio-cerebral vascular disease. The invention realizes simultaneous determination for the component content of the Ginkgolides preparation. Experiments show that the Ginkgolide A and Ginkgolide B have the advantages of good separating degree with better linear relation, reproducibility, precision, stability, and recovery rate. The dosage form of the preparations provided by the present invention is beneficial for improving the bioavailability in vivo and drug efficacy.

The invention discloses a Ginkgolide B powder injection, which is characterized in that: it is a powder injection consisting of main medcine and pharmacological acceptable filter aid, excipient and stabilizer. Said main medicine is Ginkgolide B, and filter aid is meglumine, and excipient is mannitol or dextran 40, and stabilizer is EDTA-2Na or EDTA-CaNa. The weight ratio is: Ginkgolide B:EDTA-2Na or EDTA-CaNa:mannitol or dextran 40 = 1:0.5-3:0.01-2:1-20. The preparation solves the problems such as Ginkgolide B indissolvable problem, redissolve clarity and stability.

The invention relates to a natural pharmaceutical composition for preventing or treating cardiovascular and cerebrovascular diseases, in particular relates to a pharmaceutical composition consisting of ginkgolide and natural C-glycosyl flavone compounds, and especially relates to a medicine which takes ginkgolide B and vitexin or orientin as major active ingredients. Experimental researches show that the composition has a significant effect on improving and treating diseases of cardiovascular and cerebrovascular system. The pharmaceutical composition disclosed by the invention is wide in source of the adopted raw materials, natural and non-toxic, low in side effect and relatively low in cost, and the pharmaceutical composition has a broad value of practical application.

The invention provides a methanesulfonic acid 10-O-(dimethyl amido ethyl) bilobalide B calcium sulfate hemihydrate compound and relative preparation method, which formula is represented as right. The preparation method comprises that methanesulfonic acid 10-O-(dimethyl amido ethyl) bilobalide B is crystallized in organic solvent containing water, while the compound has the advantages of better stability, solubility, and drug effect, which can treat the diseases as ischemic stroke, inflammation, asthma relative PAF factor.

The invention discloses a ginkgolide sublingual tablet, belonging to the technical field of a pharmaceutical composition, and a preparation method thereof. The sublingual tablet comprises the following materials in parts by weight: 1-200 parts of ginkgolide, 2-20 parts of a disintegrating agent and 40-200 parts of a filler, wherein the ginkgolide includes the following components in percentage by weight: 35-50% of ginkgolide A, 6-16% of ginkgolide B, 15-25% of ginkgolide C and 30-45% of bilobalide. The ginkgolide sublingual tablet disclosed by the invention is prepared by organically combining the disintegrating agent, the filler and the like; the sublingual tablet, which is located under the tongue when being taken, can disintegrate rapidly under the tongue; the sublingual tablet is absorbed through sublingual mucosa and directly participates in blood circulation through jugular vein and superior vena cava to become effective rapidly, so as to relieve migraine rapidly.

The invention discloses a compound shown as a formula I or a formula II or pharmaceutically acceptable salts thereof. In the formula, R1 is selected from pyrazinyl or substituted pyrazinyl; and R2 is selected from pyrazinyl or substituted pyrazinyl, phenyl or substituted phenyl and alkyl or substituted alkyl. The structural formula is as shown in the specification.

The invention discloses a method for extracting and separating ginkgolide B from ginkgo leaves. The method comprises the following steps of: extracting the ginkgo leaves with ethanol; performing reduced-pressure concentration of the extracting solution to obtain extract; adding water to dilute the extract, and adsorbing with a macroporous resin column; eluting with ethanol; performing reduced-pressure concentration on the eluent to obtain thick paste; uniformly mixing the thick paste with a diluent, and drying; packing the dry paste, eluting with ethyl acetate, and concentrating the ethyl acetate eluent until the smell of ethyl acetate does not exist; adding ethanol for dissolution; crystallizing with ethanol to obtain coarse crystal; and re-crystallizing the coarse crystal with ethanol and ethyl acetate to obtain the ginkgolide B with purity greater than or equal to 98%. According to the method provided by the invention, the technology is simple, the production cost is relatively low, the product purity is high, the yield is relatively high, and the method is favorable for industrial production.

The invention discloses application of stereum hirsutum thalli in preparation of ginkgolide B. According to the application, a method for preparing ginkgolide B comprises the following steps: carrying out amplification culture on stereum hirsutum strains, taking thalli which are obtained through a test tube slant, a liquid shake flask, seed culture and thallus separation as a catalyst, converting ginkgolide into ginkgolide B, and enabling a conversion solution to be subjected to centrifugation, ethyl acetate extraction and anhydrous alcohol crystallization, so as to separate ginkgolide B from fermentation liquor. By using the method, the purity of obtained ginkgolide B is not lower than 99%, and the ginkgolide conversion ratio is higher than 90%.