250 results about "Bilobalides" patented technology

The present invention discloses one kind of bilobalide powder for injection and features its composition including bilobalide, meglumine and hydroxypropyl-beta-cyclodextrin in the weight ratio of 1 to 0.2-0.5 to 6-9. The present invention also discloses the preparation process of the bilobalide powder for injection. The bilobalide powder for injection has supplementary material capable of dissolving bilobalide completely without destroying its structure, and bilobalide as the main material is slightly soluble in water and easily soluble in acetone. The key point of the present invention is to select hydroxypropyl-beta-cyclodextrin as the solubilkizing supplementary material to raise the solubility of bilobalide greatly, and this raises the bioavailability of bilobalide and the curative effect of the injection greatly.

The invention discloses a process for extraction and separation of ginkgolides A, B, C, J, M and bilobalide. The process comprises the following steps of: utilizing ginkgo leaves or gingko tree root skin as a raw material; extracting with weakly alkaline water as a solvent; concentrating, filtering and neutralizing extract; filling filtrate in polyamide column; collecting effluent; eluting the polyamide column with water; combining eluate with the effluent on macroporous resin column; eluting with ethanol; concentrating to small size; and separating in steps and crystallizing, wherein rough crystals are recrystallized by using ethanol, methanol and the like to obtain ginkgolides A, B, C, J, M and bilobalide monomer respectively; through HPLC (High Performance Liquid Chromatography) detection, the purity of the ginkgolides A, B, C and the bilobalide can reach 98 percent, and the purity of the ginkgolides J, M can reach 97.5 percent. The process has the advantages of simplicity, low cost and high yield.

The present invention discloses a preparation method for extracting bilobalide B from gingko leaf or its extract, which comprise: high speed countercurrent extraction, column chromatography for separation, recrystallization. The method can not only remove the harmful substance as alkylphenolic acids from gingko crude extract, but promote the yield of bilobalide B, promote the product content, and be suitable for industrial production.

The invention discloses a separating and purifying method of ginkgolides A, B, C and J and bilobalide monomers, which comprises the following processing steps: a. ginkgoic acid is removed from the extractive of ginkgo leafs; b. the total lactones of ginkgo is obtained; c. the preparation solution of the total lactones is prepared; d. the high-performance liquid chromatographic separation of the ginkgolides A, B, C and J and the bilobalide monomers in the total lactones is carried out; and e. the preparation solution of the monomers is processed and the product is dried. By using a preparative high-performance liquid chromatographic column to carry out separation and purification and a differential refractive index detector to carry out on-line detection, the invention can synchronously separate and obtain the ginkgolides A, B, C and J and the bilobalide monomers, the purity of which is more than 98 percent, and has the advantages of large preparative scale, high yield, good product quality, low cost and being suitable for industrial production.

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 present invention discloses new process of extracting and separating high purity bilobalide and ginkgetin. By means of macroporous adsorption resin chromatographic separation technology, the water extract of ginkgo material is eluted in macroporous adsorption resin column successively with distilled water, 5-25 % concentration alcohol solution, 0.01-10 % concentration alkali solution, distilled water and 30-95 % concentration alcohol solution, and the elute of alkali solution and the elute of 30-95 % concentration alcohol solution are collected separately, concentrated and purified to obtain bilobalide or ginkgetin. The process has high efficiency, simple operate, low production cost and environment friendship, and the product has high quality and high yield.

The present invention relates to an extraction technique of natural plant active component. In the concrete, it relates to a preparation process of ginkgo extract with low ginkgolic acid content. In the ginkgo extract obtained by adopting the invented preparation method the ginkgo total flavone content is 28-40%, bilobalide content is 6-14% and ginkgolic acid content is less than 5ppm. Its preparation method includes the steps of extraction, separation, purification, concentration and drying.

The invention relates to the field of phytoextraction, in particular to an extraction separation method of ginkgolides. The ginkgolides with fixed components can be obtained through the extraction separation method. The ginkgolides obtained through the steps of extraction, column chromatography, crystallization and crystal mixing in the method comprises bilobalide (C15H1808) of 25.0%-50.0%, ginkgolide A (C20H24O9) of 20.0%-45.0%, ginkgolide B (C20H24O10) of 10.0%-30.0%, ginkgolide C (C20H24O11) of 5.0%-15.0%. The total quantity of the bilobalide, the ginkgolide A, the ginkgolide B and the ginkgolide C amounts for over 95% of the ginkgolides.

The invention provides a bilobalide B derivative having the structural formula described in the specification, wherein when R2 represents -COOH, R1 represents -X-, X represents C1-C18 alkylidene, the alkylidene is unsubstituted or substituted by C1-C5 straight chain or branch chain alkane. When R2 represents -NR3R4, R1 represents -XCO-, X represents C1-C5 alkylidene, the alkylidene is unsubstituted or substituted by C1-C5 straight chain or branch chain alkane, R3 and R4 are identical or different, and both are H, C1-C8 alkyl or C3-C10 cycloalkyl.

The invention discloses a process for extracting ginkgolide, ginkgolide injection and process for preparing same, wherein the extracting process consists of disintegrating the ginkgo leaves, leaching by diluted acetone solution, recovering acetone, removing impurities, extracting and purifying with acetic ether, removing impurities with sodium acetate again, reclaiming acetic ether, recrystallizing in ethanol or methanol, filtering, low temperature drying, solubilizing the bilobalide with hydroxypropyl-beta-cyclodextrin to obtain the bilobalide injection.

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 extracting process of bilobalide A, B and C includes the polyamide column adsorption of the gingko extract as material, concentration and crystallization to obtain coarse crystal; or twice extraction of gingko leaf as material, concentration, filtering, polyamide column adsorption, collecting effluent, eluting polyamide column with alcohol, merging the effluent and the eluent, elution in macroporous resin column with alcohol, concentration and crystallization to obtain coarse crystal; and re-crystallizing the coarse crystal in methanol water to obtain bilobalide A, B and C. Bilobalide A, B and C may be produced into dripping pill, granule or capsule. The present invention has simple process, high yield, and product with bilobalide A, B and C content up to 70 %.

The invention discloses a novel process for extracting bilobalide B from ginkgo leaf or ginkgo leaf extract through liquid-liquid extraction and refining, wherein the extraction solvent being n-butanol or other solvents having similar dissolving property and polarity. The obtained bilobalide B has a purity higher than 95% and a yield higher than 1%.

The present invention relates to a method for therapeutically and/or prophylactically treating ischemia and/or the pathologies associated with ischemia or an energy deficit in a patient comprising administering to the patient a pharmaceutical composition comprising bilobalide and a pharmaceutically acceptable excipient where the composition has a therapeutic and/or prophylactic effect on ischemia and/or the pathologies associated with ischemia or an energy deficit.

The invention discloses a bilobalide drop pill. The bilobalide drop pill is prepared from, by weight, 10 parts of bilobalide, 20-40 parts of matrix and 2-6 parts of disintegrating agent. The invention further provides a preparation method of the bilobalide drop pill. Acceleration experiment results show that with the disintegrating agent CMC-Na added into a preparation formula, the bilobalide drop pill is free of obvious change on dissolution rate in vitro and dissolution time limit after 6 months, thereby being high in stability and capable of avoiding ageing effectively.

The present invention relates to a new-type high-effective safety medicine-ginkgo leaf total lactone for curing depression. It is a terpene lactone extracted from ginkgo biloba. L or other portions of said plant, such as ginkgo nut, ginkgo root bark and ginkgo twing, in which five terpene lactone compounds of bilobalide A, bilobalide B, bilobalide C, bilobalide J and bilobalide are mainly contained.

The invention relates to a method for preparing bilobalide tablet, which is characterized in that it is prepared from bilobalide drug as active component and relative findings, wherein, the bilobalide drug can be bilobalide or bilobalide B, and the findings contain hydrophilic gel which can quickly expand in the stomach acid condition and float in gastric; and the tablet has significant slow-release effect. The mass ration between the bilobalide drug and the findings is 1:0.3-30. The bilobalide drug is extracted from ginkgo leaf. And the preparation is characterized in that screening the bilobalide drug and findings via the screen at 80-100 deals to be mixed uniformly and pressed into tablet, or using wetting particle making technique or drying particle technique to press the tablet.

The present invention discloses a kind of ginkgo leaf extract, injection containing the said extract and its preparation process. The ginkgo leaf extract contains flavonol glycoside 18-40 wt%, bilobalide 2.5-25 wt%, and heavy metals less than 9.4 ppm, with the bilobalide comprising bilobalide A, bilobalide B and bilobalide C in the weight proportion of 7-27 to 3-20 to 4-40. The ginkgo leaf extract with high effective component content and high purity, and the prepared medicine preparation, especially injection, has obvious curative effect on cardiac and cerebral vascular diseases, clinical use safety and no side effect.

A separation and purification process for bilobalide monomers is provided. The column chromatography-recrystallization-supercritical CO2 refinement purification combined process is adopted to prepare high purity bilobalide monomers. The column chromatography adopts positive or reverse fixed packing material. Water and ethyl acetate are used for gradient elution. Supercritical CO2 is used for refinement purification and crystallographic form arrangement. The process conditions are: the pressure is less than or equal to 100Mpa, and the temperature is less than or equal to 150 Celsius degrees. The obtained monomers content amounts to 99.8% at the utmost, and the total yield is greater than or equal to 90%.

The invention discloses two bilobalide B hydrolyzed derivatives of which the structural formulae are disclosed in the specification, and also discloses application thereof as impurity reference substances in inspection of related substances of methylsulfonyl 10-O-(dimethylaminoethyl)bilobalide B raw materials and preparations. The methylsulfonyl 10-O-(dimethylaminoethyl)bilobalide B preparations are methylsulfonyl 10-O-(dimethylaminoethyl)bilobalide B water injection, methylsulfonyl 10-O-(dimethylaminoethyl)bilobalide B freeze-dried powder injection, methylsulfonyl 10-O-(dimethylaminoethyl)bilobalide B high-capacity injection and methylsulfonyl 10-O-(dimethylaminoethyl)bilobalide B solid oral liquid. The invention effectively controls the related substances of the methylsulfonyl 10-O-(dimethylaminoethyl)bilobalide B raw materials and preparations, thereby ensuring the safety and effectiveness of the methylsulfonyl 10-O-(dimethylaminoethyl)bilobalide B preparations in clinical use.

The invention discloses a process for extracting and purifying gingko total terpene lactone, which comprises, weighing dried leaves of ginkgo, disintegrating, extracting with or ethanol or methanol, reclaiming alcohols from the extract, removing impurities with defatted solvents, extracting and removing impurities again, obtaining the crude product, recrystallizing with ethanol, finally filtering and drying.

The invention discloses a preparing method and application of bilobalide K with general formula as (I), which is characterized by the following: G is alkaline material; possessing stability and water-solubility.

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 present invention discloses a bilobalide soft capsule formed from two portions of liquid medicine and capsule shell, in which the liquid medicine is formed from bilobalide, vegetable oil and bee wax, and the capsule shell is made up by using gelatin, water, glycerin and antiseptic nipagin. Said invention also discloses its preparation method, said product possesses good stability, and can obtain good therapeutic effect for curing apoplexy and coronary heart disease.

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 relates to a drug compound used to treat ischemia cerebrovascular disease, which is formed by panaxoside and bilobalide, wherein, the invention can significantly reduce the infarct size of brain to treat the ischemia condition, cerebral thrombus or the like.