485 results about "Deoxycholic acid" patented technology

A dermatological topical preparation such a cream, a lotion, an emulsion, a paste, an ointment and the likes including liposomes carrying lipo-dissolving substances encapsulated by the liposomes wall or incorporated with the liposomes wall components. The lipo-dissolving substance is released by the liposomes into the target adipose tissue or its proximity after penetration of the superficial skin layers by the liposomes carrying the lipo-dissolving substance.

The invention relates to a method for preparing binding-form ursodesoxycholic acid by a two-step enzymatic method, belonging to the field of biotechnology. Under the water solution state, a substrate, namely binding-form chenodeoxycholic acid, is converted into the binding-form ursodesoxycholic acid in the presence of 7alpha-HSDH and 7beta-HSDH, the separation is not needed in the intermediate step, thus the method disclosed by the invention is very simple, and furthermore, the conversion efficiency is very high. Especially chicken bile, duck bile or goose bile in a mixture form can be subjected to reaction without separating and purifying the binding-form chenodeoxycholic acid. The preparation process is simple and easy to implement, and the new, simple and convenient preparation method is provided for the binding-form ursodesoxycholic acid.

The invention provides a method for catalyzing chenodeoxycholic acids to compound ursodesoxycholic acids through efficient whole-cells. A 7a-hydroxysteroid dehydrogenase (7a-HSDH) and a lactic dehydrogenase (LDH) for regeneration of coenzyme nicotinamide adenine dinucleotide (NAD) are efficiently co-expressed in escherichia coli, escherichia coli whole cells are used to catalyze chenodeoxycholic acids (CDCA) to generate 3 alpha (Alpha)-hydroxyl-7-oxo-5bata (Beta)- cholanic acids (7-KLCA), and a reaction liquid which is obtained by catalyzing the chenodeoxycholic acids through whole cells is adjusted to be 7-KLCA crude products. Reconstitution cells can be easily obtained in low cost through a fermentation process, are better than a chemical synthesis method in production cost and product quality, and are suitable for commercial process.

The present application is directed to an aqueous pharmaceutical composition comprising from about 0.4% w / v to less than about 2% w / v of a salt of deoxycholic acid, wherein the composition is maintained at a pH from about 8.1 to about 8.5 such that the composition is stabilized against precipitation. Also disclosed herein, are methods for stabilizing an aqueous pharmaceutical composition comprising from about 0.4% w / v to less than about 2% w / v of a salt of deoxycholic acid against precipitation, said method comprising maintaining pH of the solution from about 8.1 to about 8.5.

The invention discloses a berberine electrostatic composite and a preparation method of the berberine electrostatic composite, which are applied to medical and health industries. The berberine electrostatic composite is prepared from anionic surfactant and berberine or berberine salt by compositing; the molar ratio of the anionic surfactant to the berberine or berberine salt is 1 to 0.5-10; the molar ratio of anion to the berberine salt is 1 to 1; the anionic surfactant is one or more of alkyl sulfate or alkyl sulfonate or fatty acid salt; the alkyl sulfate is one or more of sodium cholesteryl sulfate, lauryl sodium sulfate and deoxysodium cholate; the alkyl sulfonate is one or more of sodium heptanesulfonate and sodium dodecyl sulfate; the fatty acid salt is one or more of sodium caprate and sodium enanthate, and the berberine and berberine salt are obtained by chemical synthesis or by extracting traditional Chinese medicine. The berberine is prepared into the berberine electrostatic composite to increase the biological membrane penetrating ability of the berberine and improve the oral bioavailability of the berberine, and the berberine electrostatic composite plays a significant treatment role on important chronic metabolic disorder diseases such as diabetes mellitus, complication of the diabetes mellitus, hyperlipidemia and the like.

The invention provides a process of separating anthrodsoxycholic acid by using fresh swine bile as raw material, the invention further provides a process for preparing ursodeoxycholic acid by using fresh swine bile as raw material, which comprises extracting conjugated bile acid from swine bile after acidification, removing foreign materials such as aliphatic acid and protein and the like, preparing purified pig bile acid through hydrolysis (saponification) and hydroperoxide decolourization, extracting anthrodsoxycholic acid through solution immersion cleaning, preparing ursodeoxycholic acid through oxidization and reduction of anthrodsoxycholic acid which is obtained through separating. The process of the invention improves the preparation technology of ursodeoxycholic acid, and achieves positive effects on the aspects of technology simplification and output increase.

The invention discloses an amphipathic chitosan derivative PAMAM-Cs-DCA (Poly(amido amine)-chitosan-deoxycholic acid). The PAMAM-Cs-DCA is prepared by sequentially grafting a PAMAM unit and a deoxycholic acid unit on a main chain of chitosan by click chemical reaction and amidation reaction. The preparation method has mild reaction conditions, high efficiency and selectivity. The invention also discloses an application of the amphipathic chitosan derivative in preparing an anticancer drug carrier: the amphipathic chitosan derivative forms nanomicelle which takes the PAMAM unit and chitosan asa hydrophilic shell and takes the DCA unit as a hydrophobic core by self assembly in a water solution, wherein hydrophobic anticancer drugs can be coated in the core, and the shell can be compounded with pDNA (plasmid deoxyribonucleic acid) to realize co-transmission of the drugs and genes. Due to the unique molecular structure, the amphipathic chitosan derivative has potential application valuesin the fields of gene therapy, controlled release of drugs, tissue engineering and the like.

The invention provides a mutant of 7 beta-hydroxyl steroid dehydrogenase, application of the mutant and a synthesis method. The mutant of the 7 beta-hydroxyl steroid dehydrogenase is characterized in that amino acid sequences of the mutant are Seq ID NO:4, and coded nucleotide sequences are Seq ID NO:3; or amino acid sequences of the mutant are Seq ID NO:6, and coded nucleotide sequences are Seq ID NO:5. The mutant, the application and the synthesis method have the advantages that cholic acid compounds, particularly ursodeoxycholic acid, can be catalytically synthesized by the efficient 7 beta-hydroxyl steroid dehydrogenase, mutant enzymes of the 7 beta-hydroxyl steroid dehydrogenase and coenzyme regeneration systems, accordingly, the substrate concentration can reach 100 g / L, the conversion rate is 99.2-99.5%, and the weight yield can reach 94-96%; and the enzymes can be inexpensively and easily obtained by the aid of a fermentation process, accordingly, the production cost and the product quality are superior to the production cost and the product quality of chemical synthesis methods, and the mutant and the synthesis method are applicable to industrial production.

The invention provides a preparation method of ursodeoxycholic acid. Commercial available chenodeoxycholic acid is taken as raw materials, the ursodeoxycholic acid is obtained by four steps including selective oxidation, esterification, deoxidation and hydrolyzation, and the total yield is 85.7%. In a mixture of acetone and water, NBS is used for selective oxidation of hydroxy at C- 7 bit of the chenodeoxycholic acid, and the selective oxidation possesses excellent selectivity and high yield. NaBH14 / CeC13 may be used to deoxidize carbonyl at C-7 bit into hydroxy, and the ratio of alpha / beta is as high as 5 / 95.

The invention relates to an industrialized preparing method of extracting and purifying chenodeoxycholic acid from fowl and animal biles. Its process includes the steps of saponifying bile by lye, preparing calcium salt deposit of total bile acid, decolorizing by oxydol and active carbon, converting calcium salt deposit of chenodeoxycholic acid by sodium carbonate and HCl, purifying by the marcoporous absorbing resin, and so on. It has advantages of friend environment, safety and innocuity, low cost and be easy for large-scale operation.

A chemical-enzyme method of preparing ursodeoxycholic acid is disclosed. The method adopts chenodeoxycholic acid as an initial substrate, and prepares the ursodeoxycholic acid through a chemical process and a bio-enzyme process in order, wherein 7-KLCA reductase is adopted as a biological catalyst. A situation that an oxidant residual in a process of preparing 7-ketolithocholic acid through a chemical manner causes later enzyme inactivation in the prior art does not occur. A product prepared by the method is high in ee value and low in comprehensive cost.

The invention discloses a preparation method of ursodesoxycholic acid, which comprises the flowing steps of: a. carrying out 3-bit esterification on chenodeoxycholic acid to obtain 3-esterification protected chenodeoxycholic acid; b. carrying out 7-bit oxidation reaction on 3-bit ester to obtain 3-estergroup-7-oxocompounds; c. carrying out hydrolysis reaction or reduction reaction on the 3-estergroup-7-oxocompounds; d, carrying out 7-bit reduction reaction on 3a-hydroxy-7-oxo-5 beta-cholic acid or hydrolysis reaction on 3a-estergroup-7 beta- hydroxyl-5 beta-cholic acid to obtain crude products of the ursodesoxycholic acid; e. forming salt through the crude products of the ursodesoxycholic acid and organic base; and f. carrying out steps such as water adding dissolution, acid adding crystallization and the like on ursodesoxycholate to obtain pure ursodesoxycholic acid products with the purity higher than 99.0 percent. The invention aims at overcoming the defects in the prior art to provide a novel method for preparing the ursodesoxycholic acid, and the ursodesoxycholic acid prepared by the method has high yield and high purity.

The present invention relates to process of extracting cholic acid, deoxycholic acid and bilirubin from bile of pig, ox and sheep. Bile of pig, ox and sheep consists of water in about 97 %, bile acid in about 2.5 % and bilirubin in about 0.4 %; and contains also phospholipid, cholesterol, Na, K, Ca, phosphate, carbonate, small amount of protein, and other components. Fresh bile is treated through cooling, filtering to defat, basic hydrolysis, acidification and organic solvent extracting to obtain bilirubin; the rest solution is further treated through deep saponification, acidification and organic solvent precipitation to obtain the mixture of cholic acid and deoxycholic acid; and the mixture is re-crystallization separated to obtain high purity cholic acid and deoxycholic acid.

The feature of the invention includes: adopting frozen chicken gallbladder slicing, heating to 70 degree centigrade, adding 10% weight of the bile boiling for 24 hours, reflux cooling, adjusting the pH value by hydrochloric acid to gain cream, washing to neutrality; adding 95% alcohol and 10% diatomite, reflux cooling and adding active carbon, reflux, cooling and filtering, adding petrol to the filtrate to take degreasing, reflux, standing, separating alcohol liquid and washing to neutrality in reaction kettle, adding 95% alcohol, after resolving, adding barium chloride and active carbon, reflux, hot filtering, concentrating white crystal from the filtrate, washing, and adding water and sodium carbonate water solution, heating and reflux, filtering, adjusting the pH value, drying. The invention has simple technology, low cost, and could drastically separate cholesterol, lithocholic acid, and cholic acid from gall, and improves the purity.

The invention relates to a method for extracting the hyodeoxycholic acid from the leftovers of pig bile or extracted bilirubin, including saponify the leftovers with alkali, adjusting pH value, acetic ester extraction, decoloring with active carbon; concentrating the mother liquid to a proper volume, precipitating deposit, separating the deposit and drying to get coarse hyodeoxycholic acid; esterifying the coarse product, then doing an addition reaction with benzene, separating the methylhyodeoxycholanate-benzene addition compound; decomposing the addition compound with alkali, adjust pH value, getting the purified deoxycholic acid. The obtained mother liquid can be further extracted to get precious chenodeoxycholic acid. The craft has a lot of material, a low pollution, safety and no poison, a low cost, a high product purity and is suitable for industry production in a large scale.

The invention discloses a folic acid-modified O-carboxymethyl chitosan-deoxycholic acid complex which is an active-targeting nano-micelle carrier material prepared by using folic acid, O-carboxymethyl chitosan and deoxycholic acid as raw materials; O-carboxymethyl chitosan is used as a carrier material; deoxycholic acid is used for hydrophobicity reconstruction; folic acid is used for surface modification; and folic acid-mediated tumor tissue-targeting polymer micelle is prepared. Drug-loaded nano-micelle is prepared by a self-assembly method with paclitaxel as a model drug; experiment demonstrates that the drug-loaded nano-micelle has high drug load and encapsulation efficiency, has sustained release effect, is intaken into tumor cells through a folic acid acceptor approach, can increase the distribution of the drug in tumor tissue, thus improves curative effect, reduces toxic and side effect, and reaches the purpose of targeting treatment. The invention provides an ideal and novel drug carrier and preparation form for hard-soluble antitumor drugs.

The invention relates to a preparing method of a chenodeoxycholic acid derivative, and particularly relates to a preparing method of a compound shown as a formula I. The method includes (1) subjecting a compound shown as a formula 1 to Swern oxidation to obtain a compound shown as a formula 2; (2) subjecting the compound shown as the formula 2 to hydroxy protection to obtain a compound shown as a formula 3; (3) bringing the compound shown as the formula 3 into contact with iodoethane to obtain a compound shown as a formula 4; (4) subjecting the compound shown as the formula 4 to a reduction reaction to obtain a compound shown as a formula 5; and (5) bringing the compound shown as the formula 5 into contact with hydrogen under the existence of palladium / carbon that is a catalyst to obtain the compound shown as the formula I. The method is short in steps, simple in operation, and suitable for industrial production, and raw materials are easily available.

A nanoformulation that includes loaded nanoparticles. Each nanoparticle includes a modified chitosan polymer encapsulating at least one vitamin D derivative, at least one vitamin D metabolite, or combinations thereof. The modified chitosan polymer includes chitosan covalently linked to at least one entity selected from the group consisting of fatty acids (omega-3-fattay acids), amino acids, deoxycholic acid, alginate, arginine-alginate, hyaluronic acid, collagen, collagen-hydroxyapatite, poly(lactic-co-glycolic acid) (PLGA), and combinations thereof. A structure includes a medium and the nanoformulation, wherein the nanoparticles are dispersed in the medium. A method of using the nanoformulation to treat a disorder and improve efficacy of current therapies where resistance develop in a patient includes administering to the patient a therapeutically effective amount of the nanoformulation for treating the disorder. A nano-cosmetic formulation, comprising a cosmetic includes the nanoformulation, wherein the modified chitosan polymer encapsulates the at least one vitamin D derivative, and wherein the at least one vitamin D derivative encompasses 0.1 to 20.0 wt % of the nano-cosmetic formulation's total weight.

The invention discloses a method to manufacturing high purity chemocholic acid from fowl bile that belongs to refinement chemical and medicine field. It includes the following steps: a. saponification reaction: mixing the fowl bile and sodium hydroxide and reacting for 20-30 hours under the certain temperature; b. neutral reaction: adding dilute hydrochloric acid after saponification reaction and gaining raw cholic acid after filtering; c. column chromatography: adding dilute sodium hydroxide into raw cholic acid and injecting into chromatography column, uniting the eluent; super filtering: taking super filtering by super filtering film; e. gaining chemocholic acid that the purity is over 96% after adding dilute acid, filtering and drying. The invention has simple technology, high purity, low cost and environment protection.

The invention relates to a bio-degradable alb derivative and the related pharmaceutical combinations; wherein, the derivative introduces alkyl, or fatty acyl or deoxycholic acid in the alb skeleton to enable the amphiphilic property and form a nano-micelle by self-organization in water, and can enwrap the drugs through the double effects of the hydrophobic group, the alb molecular chain and the drugs, thereby substantially improving the drug enwrapping ability of the alb and prolonging the stability time. The excipient can be used as the carrier for organic drugs, water-insoluble drugs or dugs with poor water solubility and the carrier of amphipathic drugs, and for the administration inside the vein or muscle injection and oral administration. The preparation method of the bio-degradable alb derivative and the related pharmaceutical combinations is simple and of mature techniques, which is suitable for large scale continuous production.

Use of chenodeoxycholic acid is disclosed to reduce adipose tissue and thereby reduce weight in mammals. The chenodeoxycholic acid can be administered orally through the use of a tablet, pill, capsule or liquid suspension.

A process for separating the chenodeoxycholic acid from pig's gall and purifying it includes such steps as preparing general cholic acid from the mother liquid generated by extracting the cholerythrin from pig's gall, saponifying, regulating pH value to obtain crude chenodeoxycholic acid, decoloring, defatting, preparing the deposit of barium chenodeoxycholate, reacting on potassium carbonate to remove Ba, regulating pH value, and purifying by silicon gel column.

The invention discloses a method for preparing chenodeoxycholic acid in pig bile by an esterification method, which comprises the following steps that: methanol, concentrated sulfuric acid and sodium hydroxide are used for esterification; acetic anhydride is used for acidylation; sherwood oil is used for extraction; the primary crystallization and the secondary crystallization are realized through ethanol and the sherwood oil; the sodium hydroxide is used for hydrolytic acidification; ethyl acetate and active carbon are used for crystallization; and the chenodeoxycholic acid is obtained through drying. The chenodeoxycholic acid is prepared by the method disclosed by the invention, the preparation method is simple, safety and environment protection are realized, the method can be used for large-scale industrial production, the content of the extracted chenodeoxycholic acid is higher or equal to 98 percent, the extraction rate is high, and the purity requirement on products in markets can be met.

The invention provides a method for separating and purifying chenodeoxycholic acid from duck gall, and concretely comprises to the following steps: dissolving and extracting a duck gall paste crude product, extracting ethyl acetate, and ultrafiltering and removing impurities. The method has the following advantages that 1) the raw material source of chenodeoxycholic acid can be enlarged, the method for separating and purifying chenodeoxycholic acid from the duck gall is provided; and 2) the content of chenodeoxycholic acid extracted from the duck gall by a traditional method is low with about 60%. The HPLC content of chenodeoxycholic acid obtained by using the method of the invention can reach more than 96%, and the extraction efficiency of chenodeoxycholic acid is enhanced.

The invention relates to a chenodeoxycholic acid (3 alpha, 7 alpha-dihydroxyl-5 belta-cholestane-24-acid) chemical synthesis method, belonging to the field of organic chemical synthesis. Chenodeoxycholic acid is prepared by the following steps of: (1) preparing cholate; (2) preparing 3 alpha, 7 alpha-acetyl-12 alpha-hydroxy cholate; (3) preparing 3 alpha, 7 alpha-acetyl-12-oxo-chenodeoxycholic acid ester; (4) preparing 12-oxo-chenodeoxycholic acid; and (5) preparing chenodeoxycholic acid. The application of the method for synthesizing chenodeoxycholic acid has the advantages of high yield rate, low cost and no pollution and is particularly convenient for industrial production.

A method for extracting chenodeoxycholic acid from bile of fowl comprises the following steps of: acquiring rough bile acid or rough bile acid calcium salt from fresh or frozen bile of fowl through saponification reaction, heating the bile acid resin solution together with the aqueous solution of organic nitrogenous compound A, removing the majority of hydrophilic impurities from the rough bile acid by using the organic nitrogenous compound A, reacting the acquired bile acid resin solution with organic nitrogenous compound B, dissolving the sediment, filtering, decolorizing and refining, so as to acquire chenodeoxycholic acid with a purity about 95%. The method of the invention has simple operation, the generality of the production equipment is high, and the chemic matter is harmless, therefore the invention is fit for industrialization of chenodeoxycholic acid.

The invention relates to a method of distilling the chenodeoxychoilc acid from the offcuts which be gained by distilling the bilirubin from the bile of the pig. With the offcuts of the alkali saponification, the deposit is treated with the oxidation treatment by means of the hydrogen peroxide, the filtrate is treated by the dilute sulfuric acid and decolored by means of the active carbon and solved, crystaled using the ethyl acetate again and again; the coordinate production of the hyodeoxycholic acid is purified, the mother liquor is concentrated to the cream and melted using the alkali and have the salifying treatment with the chloride of barium, so the cholate is formed, the cholate is treated to take off barium when the cholate suspending the aqueous solution containing the sodium carbonate, then it is acidificated with the dilute sulfuric acid and is separated ,deposited and dried to gain the crude chenodeoxycholic acid which is decolored using the active carbon and is melted, rimed and dried using the ethyl acetate. Then the finished production of the chenodeoxycholic acid form.The whole technics has some merits of the abundant material, the amity of the environment, the safety and innocuity, producing many outputs from the single stuff and easy to the mass production. The invention is used for distilling the chenodeoxycholic acid.

A process for synthesizing chenodeoxycholic acid includes such steps as preparing the ester used for cholic acid, preparing diacetyl-12a-hydroxy-methyl cholate, preparing 3a, 7a-diacetyloxy-12-oxy-methyl cholanic acid, preparing 12-oxy- chenodeoxycholic acid, preparing chenodeoxycholic acid, and purifying.

The present invention discloses one kind of freeze dried polyene phosphatidylcholine powder for injection and its preparation process. It features that the preparation contains polyene phosphatidylcholine and solubilizer sodium deoxycholate, sodium dehydrocholate or sodium cholate in the weight ratio of 0.5-1.5.

The invention discloses a method for preparing an ursodesoxycholic acid by the chiral catalytic hydrogenation of a 7-ketodesoxycholic acid, which is characterized by comprising the following steps of: performing oxidation to prepare the 7-ketodesoxycholic acid from a chenodeoxycholic acid serving as an initiative raw material by using a common method; dissolving the 7-ketodesoxycholic acid into a solvent, adding a chiral catalyst, maintaining the pressure of 0 to 20 MPa under alkali condition, introducing nitrogen to perform hydrogenation reduction reaction at 10 to 80 DEG C, and performing distillation after the reaction is finished to remove the solvent; adding purified water in a volume which is 10 to 100 times that of a hydrogenation reduction reaction product, and adding acid liquor to crystallize the hydrogenation reduction reaction product; and separating solids from liquid, and performing washing and drying to obtain solid powder which is the ursodesoxycholic acid. The method for preparing the ursodesoxycholic acid by the chiral catalytic hydrogenation of the 7-ketodesoxycholic acid aims to overcome the shortcomings of the prior art, and ensures a short production flow, high yield and high quality.