26 results about "Fusidic acid" patented technology

The invention provides a preparation method of fusidic acid emulsifiable paste, and relates to the field of pharmaceutical preparations, and the preparation method comprises the following steps: step 1, preparation of fusidic acid nanoparticles, step 2, preparation of an oil phase of the emulsifiable paste, step 3, preparation of a water phase of the emulsifiable paste, step 4, emulsification, and step 5, mixing. According to the fusidic acid nanoparticles, firstly, a composite carrier is prepared, then fusidic acid, PLGA, the composite carrier and absolute ethyl alcohol are mixed, a nanoparticle oil phase is obtained, then PVA, PVP, sodium dodecyl glucoside sulfonate and dipotassium ethylenediaminetetraacetate are mixed with deionized water, a nanoparticle water phase is obtained, and finally a nanoparticle suspension is obtained through mixing. The fusidic acid emulsifiable paste prepared by the method can effectively solve the problems that the traditional emulsifiable paste bulk drugs are easy to agglomerate, the drug molecule particle size is large and the like, and the transdermal absorption rate and bioavailability of fusidic acid are improved, so that the antibacterial effect is enhanced.

The present invention provides a fusidic acid cream preparation, comprising an active ingredient fusidic acid, an aqueous phase part and an oil phase part, wherein the aqueous phase part comprises glycerol, a preservative and purified water; the oil phase part comprises an oily base and an emulsifier; further, in order to avoid the increase of impurities caused by the addition of antioxidants to the excipients due to their thermal instability, the cream does not contain antioxidants. After testing, the stability of the fusidic acid cream of the present application is better than that of the commercially available reference preparation, and it can maintain the stability of the paste properties and active ingredients under high temperature, high humidity, low temperature, freeze-thaw and light conditions. The maximum single impurity and total impurity content in the product do not increase significantly, and the quality is controllable. At the same time, the preparation process of the fusidic acid cream disclosed in the present application is simple and easy to industrialize.

The utility model discloses an efficient defoaming and stirring device for fermentation of fusidic acid, which relates to the technical field of fermentation engineering and comprises a fermentation tank body, a temperature adjusting cover is wrapped on the surface of the fermentation tank body, supporting legs are arranged at the bottom of the temperature adjusting cover, a speed reducing motor is arranged at the top of the fermentation tank body, and a stirring motor is arranged at the bottom of the speed reducing motor. The output end of the gear motor is fixedly sleeved with a stirring main shaft, and stirring blades and a defoaming assembly are rotationally mounted on the surface of the stirring main shaft; according to the defoaming device, the position of the defoaming component can be automatically adjusted along with the height of the liquid level through the buoyancy cavity, the defoaming paddle can effectively eliminate bubbles on the liquid level all the time, and a certain amount of purified water can be injected into the cavity through the connecting pipe orifice to change the weight of the buoyancy cavity, so that the height between the defoaming paddle and the liquid level is controlled, and the defoaming effect is improved. Therefore, the maximum defoaming efficiency is kept.

The invention provides a staphylococcus aureus drug resistance prediction method based on whole genome association analysis and machine learning, and belongs to the technical field of bioinformatics and artificial intelligence crossing. Five common antibiotics such as erythromycin, ciprofloxacin, penicillin, fusidic acid and methicillin are selected as modeling objects. Performing comparison and SNP site detection on a strain genome by using a reference genome, and constructing a variation matrix; then, a pyseer tool is adopted for GWAS analysis, and genetic loci significantly related to the drug resistance of each antibiotic are screened as modeling features; and for each antibiotic, respectively constructing an independent machine learning model, inputting the SNP features screened by the GWAS, and outputting a drug resistance / sensitivity classification label. Through cross validation and independent test set evaluation, the model has excellent accuracy and F1 score on multiple antibiotics. According to the method, drug resistance prediction can be achieved based on genome data without traditional drug sensitivity experiments, and the method has the remarkable time advantage, popularization value and scientific research significance.

The application is a preparation method of fusidic acid cream, which comprises fusidic acid in a dispersed form, wherein the concentration of fusidic acid is 2%, the fusidic acid is in a dispersed form through ions, the ions are generated by hydrochloric acid, the drug phase is prepared by an acid combination, the emulsification reaction is carried out at a homogenization head speed of 0.55-1.00 m / s, a stirring speed of less than 0.55 m / s and a temperature of 75 DEG C for 20+ / -5 minutes; and the drug phase is prepared at a stirring speed of 0.3+ / -0.2 m / s and a temperature of 50+ / -5 DEG C for 40+ / -10 minutes. The application has the advantages that: by adding hydrochloric acid in the drug phase and reasonably designing the emulsification, drug phase preparation and adding steps, the fusidic acid is uniformly dispersed in the finished product, and the fusidic acid agglomeration is not formed in the finished product, and the dispersion uniformity is improved.

The present application provides a fusidic acid cream composition and a preparation method thereof. The fusidic acid cream composition comprises or consists of the following components: fusidic acid, liquid paraffin, cyclomethicone, an emulsifier, a co-emulsifier, a thickener, a preservative, an antioxidant, and water; wherein the emulsifier is polysorbate 80, the co-emulsifier is ethylene glycol palmitostearate, the thickener is isopropyl palmitate, the preservative is potassium sorbate, and the antioxidant is butylated hydroxyanisole. The fusidic acid cream composition exhibits good emulsification and excellent stability during preparation and long-term storage, making it suitable for industrial production.

The utility model discloses a distribution station for producing fusidic acid by using a fermentation method, which relates to the technical field of fermentation engineering, and comprises a steam pipeline connected with a steam source, a distribution main pipe for supplying steam and a blow-off pipeline connected with a wastewater treatment system, a plurality of branch pipes are arranged on the distribution main pipe, seed transfer valves are arranged on the branch pipes, and the seed transfer valves are communicated with the steam pipeline. The branch pipe is connected with a seed transferring pipeline through a seed transferring valve; the exhaust valve and the flow control valve are integrally connected, the pipeline inner wall of the seed transferring pipeline is smooth and free of dead corners, in the fermentation environment, dirt is easily hidden in the dead corners, microorganisms are easily accumulated and bred in the dead corners, the whole connecting part is smoother and more continuous due to the integrated design of the seed transferring valve and the smooth and dead-corner-free internal design of the seed transferring pipeline, and the seed transferring effect is better. And no gaps, recesses and other places where impurities are easy to remain exist, cleaning and disinfection are facilitated, the sanitary condition of the environment where gas and materials are located in the exhausting and seed transferring process is guaranteed, and the risk that bad influences are generated on the quality of fermented products is reduced.

The invention provides a method for extracting fusidic acid hemihydrate from fusidic acid fungus residues, belongs to the field of fermentation engineering, aims at reutilizing fungus residues obtained after separation of an extracting solution, breaks through the limitation of separation and purification of the extracting solution in the prior art, and improves the yield of fusidic acid. The preparation of fusidic acid is remarkably improved in the aspects of titer, yield, energy conservation, emission reduction and pollution reduction.

The utility model discloses a dead-corner-free tank bottom valve for a fusidic acid production fermentation tank, which relates to the technical field of fermentation engineering and comprises a fermentation tank body, a sanitary hoop joint is integrally formed at the bottom of the fermentation tank body, and the bottom of the sanitary hoop joint is connected with a dead-corner-free diaphragm valve through a hoop device; according to the utility model, the smooth inner wall of the arc-shaped elbow is tightly matched with the spherical valve core and the diaphragm piece, so that material residues are effectively prevented. In the actual production process, compared with multi-batch operation, when a traditional valve is used, a certain amount of materials are left in the valve after each fermentation, a large amount of time and resources need to be consumed for cleaning, the materials are difficult to thoroughly clean, and pollution is easily caused to next-batch fermentation. And by adopting the dead-corner-free tank bottom valve, almost no material residue exists, the purity of the fermentation raw material is obviously improved, a solid foundation is laid for producing high-purity and high-quality fusidic acid products, and the stability and the consistency of the product quality are ensured.

The invention relates to the field of organic synthesis, and discloses a synthesis method of an impurity B of fusidic acid. The method comprises the following steps: 1, dissolving fusidic acid in a first organic solvent, adding an epoxidation agent, reacting for a first time at a first temperature, and extracting to obtain a compound I; 2, dissolving the compound I in a second organic solvent, adding a catalyst, reacting for a second time at a second temperature, and pulping and washing by using a third organic solvent to obtain a compound II; in the embodiment of the invention, reagents used in the synthesis route of the fusidic acid impurity B are easy to obtain and low in cost, the whole route only needs two steps, the total yield can reach more than 50%, and the technical problem that the cost is too high when a large amount of fusidic acid impurity B is synthesized in the prior art is solved.

The invention discloses a method for reducing the content of an M impurity in fusidic acid fermentation liquor. The generation of the M impurity is inhibited from a fermentation source by optimizing a fermentation culture medium and regulating and controlling pH in stages. A fermentation culture medium adopts a composite organic nitrogen source, contains soybean cake powder with specific grease content, and is matched with a yeast extract and corn steep liquor, so that a key precursor can be provided for fusidic acid synthesis, and the enzyme activity can be regulated; the pH is regulated in the early stage of fermentation to adapt to the proliferation requirement of the strain, M impurity synthesis is preliminarily inhibited, the pH is regulated in the middle and later stages to strengthen the activity of a target product synthetase, and M impurity synthetase expression is remarkably inhibited. The process is simple, subsequent complex purification is not needed, the yield of fusidic acid is increased, M impurities are reduced to 2% or below, and the method is suitable for industrial large-scale production.

The utility model discloses a fermentation feed supplement system for fusidic acid production, which relates to the technical field of fermentation feed supplement and comprises a feed supplement tank, a fermentation tank and a feed supplement cup, the feed supplement tank is connected with the feed supplement cup, the feed supplement cup is connected with the fermentation tank, and a peristaltic pump is arranged on a connecting pipeline of the feed supplement cup and the fermentation tank. Through cooperative operation of the material supplementing tank, the material supplementing cup, the flow sensor, the peristaltic pump and the like, accurate material supplementing can be realized according to dynamic requirements of microorganisms for nutrition in different fermentation stages of fusidic acid. The problem of overnutrition or insufficiency in a traditional material supplementing mode is effectively avoided, generation of by-products is reduced, microorganisms can obtain appropriate nutrients in all growth stages, a stable material basis is provided for efficient synthesis of fusidic acid, and then the yield and quality of products are improved.

The present application belongs to the field of pharmaceutical preparations, and particularly relates to a gel of Duiyiwai and application thereof. The gel of Duiyiwai is an external preparation prepared from raw and auxiliary materials including the following parts: Duiyiwai extract 1.25-5 parts by weight, carbomer 940 0.5-1 part by weight, hydroxyphenyl ethyl ester 0.01-0.05 part by weight, triethanolamine 0.5-1 volume part, glycerol 1-2 volume parts, 1,2-propylene glycol 1.5-2 volume parts. The gel of Duiyiwai has the same curative effect as the Duiyiwai extract of the same dosage in repairing acute wounds; but has a significantly better curative effect than the Duiyiwai extract of the same dosage in repairing infected wounds, and is also better than the commonly used fuscide acid cream and compound Huangbai liquid in the clinic, and has practical popularization and application value.

The application belongs to the technical field of medicine, and discloses a kind of amidine compound and its preparation method and application in treating bacterial infection, specifically discloses a kind of amidine compound and its pharmaceutically acceptable salt and preparation method and application in treating bacterial infection as shown in the following general formula (I).The amidine compound of the application is used in the preparation of products for enhancing the activity of other antibiotics.The antibiotics include macrolide drugs, pleuromutilin drugs, quinolone drugs, rifamycin drugs, dihydrofolate reductase inhibitor drugs, oxazolidinone drugs, lincosamide drugs, capreomycin drugs, mupirocin drugs and fusidic acid drugs.

The present invention provides a fusidic acid derivative, a preparation method and an application thereof. By connecting 1-carboxy-2-(β-indolyl)ethylamine (or L-tryptophan methyl ester fragment) to the carboxyl group at the C-21 position of fusidic acid, the introduction of 1-carboxy-2-(β-indolyl)ethylamine can promote the interaction of the fusidic acid derivative with the receptor, thereby improving the anti-tumor activity of the fusidic acid derivative, and it has good selectivity for normal cells. Finally, a fusidic acid derivative with a specific structure, excellent anti-tumor activity and good selectivity for normal cells is obtained. The present invention performs structural modification and optimization on the basis of the natural product fusidic acid, improves its physicochemical properties, enhances its pharmacological activity and improves its drug-likeness. The preparation method of the fusidic acid derivative provided by the present invention has the advantages of rich raw material sources, mild reaction conditions, simple operation in the reaction process, and cheap and easily available reagents.

The application belongs to the technical field of medicine, and discloses a kind of amidine compound and its preparation method and application in treating bacterial infection, specifically discloses a kind of amidine compound and its pharmaceutically acceptable salt and preparation method and application in treating bacterial infection as shown in the following general formula (I).The amidine compound of the application has the use in preparing the product for enhancing the activity of other antibiotics.The antibiotics include macrolide drugs, pleuromutilin drugs, quinolone drugs, rifamycin drugs, dihydrofolate reductase inhibitor drugs, oxazolidinone drugs, lincosamide drugs, capreomycin drugs, mupirocin drugs and fusidic acid drugs.

The invention belongs to the field of pharmaceutical preparations, and particularly relates to lamiophlomis rotata gel and application thereof. The lamiophlomis rotata gel is an external preparation prepared from the following raw and auxiliary materials in parts by weight: 1.25 to 5 parts of lamiophlomis rotata extract, 0.5 to 1 part of carbomer 940, 0.01 to 0.05 part of ethylparaben, 0.5 to 1 part of triethanolamine, 1 to 2 parts of glycerol and 1.5 to 2 parts of 1, 2-propylene glycol. The curative effect of the lamiophlomis rotata gel is equivalent to that of the lamiophlomis rotata extract with the same dosage when the lamiophlomis rotata gel is used for repairing acute wounds; however, when the composition is used for repairing infectious wounds, the curative effect of the composition is obviously superior to that of the same dosage of lamiophlomis rotata extract, and is also superior to that of fusidic acid cream and compound cortex phellodendri liquid which are commonly used clinically at present, so that the composition has practical popularization and application values.

The invention discloses high-stability fusidic acid cream and a preparation method thereof, and belongs to the field of pharmaceutical preparations. The fusidic acid cream provided by the invention comprises fusidic acid, propylene glycol, an oil phase component, a water phase component, an antioxidant and an amphiphilic lipid composition, wherein the oil phase component is prepared from white vaseline, mineral oil, cetyl alcohol, glycerol monooleate, phytantriol and phospholipid-PEG (Polyethylene Glycol). The preparation method comprises the following steps: carrying out drying pretreatment on the amphiphilic lipid, mixing the water phase and the drug-loaded oil phase under the protection of nitrogen, sequentially carrying out high-speed shearing emulsification and high-pressure homogenization treatment, and finally adding the phospholipid-PEG to prepare the fusidic acid cream. Through a unique amphiphilic lipid combination and step-by-step process, the dispersion uniformity and chemical stability of fusidic acid are remarkably improved, and the obtained cream is controllable in particle size, not prone to agglomeration, good in storage stability and suitable for industrial production.

Provided herein are compositions for topical application to a subject for the treatment of epidermolysis bullosa (EB). Also disclosed are methods for treating skin in a human with EB. The methods comprise providing a composition comprising fusidic acid and one or more pharmaceutically acceptable excipients; and topically applying, or instructing the topical application of, the composition to the skin of a human with EB. In certain embodiments, the composition is topically administered to treat non-healing wounds, chronic wounds, or diseased skin in a patient with EB, to reduce the likelihood of skin infection, to reduce the likelihood of scarring, to prevent or reduce the risk of an infected skin blister, to treat intact blisters on the skin, to treat skin dysbiosis, to alter bacterial diversity of the skin microbiome, or to improve the quality of life of a subject with EB.

The application belongs to the technical field of medicine, and discloses a kind of amidine compound and its preparation method and application in treating bacterial infection, specifically discloses a kind of amidine compound and its pharmaceutically acceptable salt and preparation method and application in treating bacterial infection as shown in the following general formula (I).The amidine compound of the application is used in the preparation of products for enhancing the activity of other antibiotics.The antibiotics include macrolide drugs, pleuromutilin drugs, quinolone drugs, rifamycin drugs, dihydrofolate reductase inhibitor drugs, oxazolidinone drugs, lincosamide drugs, capreomycin drugs, mupirocin drugs and fusidic acid drugs.

The invention provides a method for separating and purifying fusidic acid through salting-out crystallization. The method comprises the following steps: (1) filtering fermentation liquor: filtering the fermentation liquor; (2) salting-out crystallization: adding salt for crystallization into the filtrate, then adjusting the pH value, and then salting out; (3) dissolving and extracting: adding an extracting solvent into the salting-out substance, adding drinking water for extracting, standing for layering, and collecting an extracted lipid phase; (4) crystallization: concentrating the extracted lipid phase, cooling, stirring and crystallizing, and filtering; (5) recrystallization: adding an extraction solvent into the fusidic acid crude product, concentrating, and cooling for crystallization; and (6) drying: drying to obtain a fusidic acid finished product. The production process is simple, the production cost is low, and industrial production is easier to realize. And the salting-out crystallization step and the recrystallization step use the same extraction solvent, and one solvent is singly used, so that the doping of multiple solvents is reduced, the loss of the solvents is reduced, the recovery is convenient, the recovery rate is high, and the production cost is low.

The application provides a method for extracting fusidic acid hemihydrate from fusidic acid bacterial residue, belongs to the field of fermentation engineering, and reutilizes the bacterial residue after separation of an extraction liquid, breaks through the limitation of separation and purification of the extraction liquid in the prior art, and significantly improves the potency, yield, energy saving and emission reduction and pollution reduction of the preparation of fusidic acid.

The invention discloses a fusidic acid C-3-site oxazole substituted, C-24-site reduced and C-21-site benzyl ester modified derivative as well as a preparation method and application thereof, and belongs to the technical field of organic chemistry. The structure of the fusidic acid derivative with oxazole substitution at the C-3 site, reduction at the C-24 site and benzyl ester modification at the C-21 site is shown in the specification, wherein R represents 3-methyl benzyl, 3-chlorobenzyl, 2-bromobenzyl, 3-bromobenzyl or 4-cyanobenzyl. The fusidic acid derivative provided by the invention has the beneficial effects that the MDR reverse activity of the fusidic acid derivative substituted at C-3 position by oxazole, reduced at C-24 position and modified by benzyl ester at C-21 position is excellent, the druggability is better, and the fusidic acid derivative can be combined with common antitumor drugs to play a good antitumor role in clinical treatment.

The invention belongs to the technical field of pharmaceutical preparations, and particularly relates to fusidic acid gel based on a deep eutectic solvent (DES) and a preparation method of the fusidic acid gel. The invention aims to solve the problems that the stability of cream is poor, and the curative effect is poor due to the fact that raw materials exist in a suspension form. According to the invention, a plurality of deep eutectic solvents are firstly screened, and it is accidentally found that DES formed by taking glycerol as a hydrogen bond acceptor and arginine as a hydrogen bond donor has the best dissolution effect on fusidic acid, and the dissolution effect is far better than that of traditional solvents and other types of DES. Based on the discovery, the fusidic acid gel provided by the invention is prepared by taking the preferable DES as a core component, dissolving the medicine at high concentration, and then mixing with a gel matrix for forming. The preparation is simple in preparation process, green and safe, and has the advantages of high stability, efficient in-vitro release, remarkable antibacterial ability and the like.

The invention discloses an external medicine composition for treating vulva lichen sclerosus, which is prepared from the following components in percentage by weight: 0.2 percent of fusidic acid, 0.03 percent of hydrocortisone / 0.015 percent of mometasone furoate, 3 percent of progesterone, 20 percent of collagen III, 20 percent of lithospermum oil, 1 percent of borneol and the balance of matrix, the matrix is one or more of vaseline, wool fat, liquid paraffin, carbomer and pure water. In addition, the invention also provides a preparation method of the external pharmaceutical composition for treating vulva lichen sclerosus. In addition, the invention also provides a vulva mask dressing, which comprises the components of the external pharmaceutical composition. The traditional Chinese medicine composition can be used for treating vulva lichen sclerosus, has the effects of resisting inflammation, relieving itching and promoting skin repair, and is small in side effect, simple in preparation process, convenient to use and small in drug dependence of patients.

The present invention provides a production device for sodium fusidic acid, comprising a salt-forming reaction tank, a material transfer pump, a liquid filter, a reflux crystallizer, a centrifuge, a mother liquor distillation tank, a solvent collection tank, a solvent delivery pump, and a reflux water separator. The device can effectively recover and recycle the solvent, without consuming the solvent and at a low cost. When the reflux crystallizer and the mother liquor distillation tank are heating, a certain vacuum is applied to the reflux crystallizer and the mother liquor distillation tank via a vacuum main pipe, thereby lowering the boiling point, saving energy required for heating, and saving costs. After the heating is completed, nitrogen is then filled via a back-pressure pipe to return the pressure to normal.