51 results about "Echinocandin" patented technology

The invention discloses a method for preparing pneumocandin B0. The method comprises the following steps of: a) centrifuging the fermentation liquid of echinocandin B0, taking mycelium, leaching the echinocandin B0 in the mycelium with a first solvent and filtering and removing the mycelium; b) distilling the solvent in the first solvent leaching solution of echinocandin B0 to dryness, soaking with a second solvent and then filtering and removing the insoluble substances; c) distilling the second solvent soak solution of echinocandin B0 to dryness and then dissolving in the first solvent, andcollecting effluent liquid through overly acidic alumina column; d) distilling the collected solution of echinocandin B0 to dryness and then dissolving in the first solvent, utilizing adsorbent resin,performing eluting with the first solvent and then collecting the part with higher purity; e) distilling the collected solution of echinocandin B0 to dryness and then dissolving in the first solvent,utilizing inverse resin, performing eluting with the first solvent and collecting the part with higher purity; and f) distilling the collected solution of echinocandin B0 to dryness and then dissolving in the first solvent, adding in a small amount of water by dripping to achieve the purpose of separation by crystallization after supersaturation, and then preparing the echinocandin B0. The methodfor preparing the echinocandin B0 not only can well remove the pigment, but also leads the purity of the echinocandin B0 to be improved by more than 96 percent.

The invention discloses a preparation method for an echinocandin compound by using a Coleophoma sp. fermentation culture. The method comprises the following steps: carrying out filtration, macroporous resin adsorption, desorption, condensation, crystallization and the like on the Coleophoma sp. fermentation culture so as to obtain a crude extract of the echinocandin compound FR179642; and carrying out chromatographic separation on the crude extract of the echinocandin compound FR179642 by using a reversed-phase filling material so as to obtain an echinocandin compound FR179642 product with high purity. The invention has the following advantages: a macroporous resin is used to extract and separate the echinocandin compound FR179642 in the method, and the method is simple and feasible and is suitable for industrial production; and through application of the reversed-phase filling material in chromatographic separation of the echinocandin compound FR179642, the echinocandin compound FR179642 product with high purity is prepared.

This invention relates to an improved process for the minimization of acid-catalyzed reactions of certain echinocandins of the kind disclosed in U.S. Pat. No. 5,378,804. The process involves the use of a boronic acid.

The invention belongs to the technical field of organic synthesis and provides a method for preparing caspofungin. The preparation method of the caspofungin comprises the following steps: a) reacting a compound II with phenylboronic acid and a stereochemical structure selecting agent so as to generate a compound III, wherein the stereochemical structure selecting agent is 2-sulfydryl benzothiazole or 1-phenyl-5-sulfydryl-tetrazole; b) reducing the compound III into amine, namely, a compound IV; and c) finally reacting the compound IV with quadrol for substitution, so as to obtain a target compound. According to the preparation method of the caspofungin, the non-toxic stereochemical structure selecting agent is adopted, so that the preparation process is safer and the preparation method is more suitable for industrial production.

The invention belongs to the field of pharmaceutical preparations and relates to an echinocandin antifungal pharmaceutical composition sustained release microsphere preparation and a preparation method thereof. The pharmaceutical active ingredients of the echinocandin antifungal pharmaceutical composition comprises caspofungin acetate and antifungal agents respectively being polyenes and triazoles; and the sustained release microsphere comprises the following materials in percentage by total weight of microsphere: 0.1%-30% (w/w) of active ingredients, 60%-99.9% daltonian biodegradable and biocompatible high polymer material with molecular weights of 5,000-200,000 and 0%-10% of pharmaceutically acceptable other auxiliary materials. The average grain diameter of the sustained release microsphere is 5-20 microns, and the encapsulation efficiency is more than 85%. The sustained release period of the sustained release microsphere is up to 50 days, the drug use frequency is significantly reduced, the bioavailability is improved, and the toxic and side effects of the drug are reduced, thus being beneficial to clinical treatment. The product is good in reproducibility of production technology and good in feasibility.

The invention discloses an echinocandin antifungal agent caspofungin containing medicinal composition, which contains cane sugar used as an excipient. The medicinal composition provide by the invention has good stability.

The invention relates to an echinocandin compound purifying method, and especially relates to a WF11899A purifying method. The method comprises the processes of pre-purifying solution preparation, resin chromatography separation, crystallization and the like. The method has the advantages of simplicity, no use of a mixed solvent, high sample purity and the like.

A complex of an echinocandin compound with a carbohydrate is described having improved thermal stability and water solubility. A process for making the echinocandin/carbohydrate complex is also described as well as the use of the complex in pharmaceutical formulations and treatments of fungal infections.

The invention relates to a medicinal composition for treating complex infection and a preparation method thereof. The medicinal composition is characterized by comprising an active ingredient selected from one of glycopeptides antibacterial drugs of telavancin, dalbavancin, oritavancin, vancomycin, teicoplanin or a pharmaceutically acceptable salt thereof, and also comprising polyene and echinocandin type antifungal agents, and being prepared into a freeze-dried powder injection by adopting a conventional process. The medicinal composition provided by the invention realizes combined application of the antibacterial drugs and the antifungal agents, can simultaneously give play to an antibacterial infection effect and an antifungal infection effect, and is convenient for clinical use.

The invention discloses a medicinal composition containing an echinocandin antifungal agent, wherein the pharmaceutical composition contains a pharmaceutically acceptable amount of excipient, and a pharmaceutically acceptable amount of phosphate buffer agent. The invention provides the medicinal composition having good stability.

The invention discloses a method for obtaining high purity echinocandin D. The method comprises the steps of: (1) mixing a solution containing an echinocandin D crude product with a methanol aqueous solution 1 so as to obtain a solution 1; (2) loading the solution 1 to a reversed-phase chromatography column; and (3) conducting elution with a methanol aqueous solution 2, thus obtaining the high purity echinocandin D.

The invention belongs to the field of medicines, and particularly relates to a pharmaceutical composition for treating invasive infection of candida albicans echinocandin drug-resistant bacteria and an application of the pharmaceutical composition. The active components of the pharmaceutical composition are composed of caspofungin and a compound L-269289, and in a strain for inhibiting drug resistance of candida albicans echinocandin in vitro, the mass ratio of caspofungin to the compound L-269289 is 1: 3-1: 36; and for treating invasive infection of a candida albicans echinocandin drug-resistant strain on mice, and the mass ratio of caspofungin to the compound L-269289 is 1: 10. In-vitro experiments prove that the combined use of caspofungin and the compound L-269289 can effectively killthe candida albicans echinocandin drug-resistant bacteria, and is suitable for treating invasive infection of the candida albicans echinocandin drug-resistant bacteria on mice.

The invention relates to compounds of the echinocandin family or a semi-synthetic derivative thereof or a salt thereof or an ester thereof, or an ester salt thereof which is intended to be used as a cytoprotective drug, particularly as a drug for the prevention and/or protection and/or treatment of cell death and/or of degenerative pathological situations or processes which result in cell death, and even more particularly as a drug for the prevention and/or protection and/or treatment of cell death and/or degenerative pathological situations or processes which result in cell death, when they are associated with ischaemia-reperfusion.

The invention features echinocandin class compounds that have been modified to (i) have activity against one or more fungal species or genera; (ii) have increased aqueous solubility; (iii) have an increased therapeutic index; (iv) be suitable for topical administration; and/or (v) be suitable for oral administration. The echinocandin class compounds of the invention include, for example, a PEG, alkyl-PEG, aryl-PEG, alkaryl-PEG, PEG-alkyl, PEG-aryl, or PEG-alkaryl substituent.

The invention belongs to the technical field of medicines, and provides a high performance liquid chromatography method for detecting echinocandin B0 and C0, wherein the detection conditions are as follows: a chromatographic column is Ultra Amide, 4.6 * 250 mm, the filler particle size is 3.5 [mu]m, the column temperature is 30-50 DEG C, the flow rate is 1-2.5 mL/min, the sample injection volume is 10-20 microlitres, the detection wavelength is 200-230 nm, and a mobile phase adopts water and acetonitrile for gradient elution. The detection method is high in precision, high in accuracy, good inreproducibility, simple, convenient and practical, can realize simultaneous detection of echinocandin B0 and echinocandin C0, and has a very wide application prospect.