Abstract: Provided are a novel streptomyces filamentosus strain with improved daptomycin productivity, and a method for producing daptomycin using the same.

Abstract: The present invention relates to a composition for parenteral administration, containing donepezil as an active ingredient, and a preparation method therefor. Donepezil, which has been conventionally used for oral or transdermal administration, is prepared as microparticles comprising a biodegradable and biocompatible polymer and a release controller so as to be provided as a pharmaceutical composition for sustained release parenteral administration, thereby enabling in vivo sustained release continuously for 2-12 weeks or more. Therefore, it is possible to reduce the frequency of administration to a patient and maintain an effective concentration in the blood for a long time.

Abstract: Provided are a novel streptomyces filamentosus strain with improved daptomycin productivity, and a method for producing daptomycin using the same.

Abstract: The present invention relates to entecavir microspheres and a pharmaceutical composition for parenteral administration containing the same. The entecavir microspheres are manufactured by a method comprising the steps of: dissolving entecavir and a biodegradable biocompatible polymer in at least one solvent; putting the solution of the entecavir and biodegradable biocompatible polymer in a hydrophilic polymer solution, followed by stirring, to form microspheres; and removing the solvent. The entecavir is sufficiently sealed in the entecavir microsphere at approximately 80% or more based on the input amount, and the elution of the entecavir is maintained for 30 days or more, and thus the entecavir microspheres can continuously exhibit efficacy, thereby improving medication compliance of patients.

Abstract: The present invention relates to a composition for parenteral administration, containing donepezil as an active ingredient, and a preparation method therefor. Donepezil, which has been conventionally used for oral or transdermal administration, is prepared as microparticles comprising a biodegradable and biocompatible polymer and a release controller so as to be provided as a pharmaceutical composition for sustained release parenteral administration, thereby enabling in vivo sustained release continuously for 2-12 weeks or more. Therefore, it is possible to reduce the frequency of administration to a patient and maintain an effective concentration in the blood for a long time.

Abstract: Disclosed are a novel montelukast 4-halobenzylamine salt, and a method for preparing a montelukast sodium salt by using the same. In the disclosed method, a montelukast 4-halobenzylamine salt represented by Formula 2 or a montelukast sodium salt represented by Formula 1 is prepared by obtaining a compound represented by Formula 3 from a compound represented by Formula 5, in the same reactor, without an additional obtaining process. In Formula 2, X represents F, Cl, Br or I.

Abstract: Provided is a process for preparing Voriconazole represented by Chemical Formula 1. More particularly, the process for preparing Voriconazole of Chemical Formula 1 includes: carrying out the Reformatsky-type coupling reaction between a ketone derivative of Chemical Formula 4 and a pyrimidine derivative of Chemical Formula 5 to obtain a compound of Chemical Formula 3; reacting the substituents halo and oxysulfonyl with a hydrogen donor to obtain racemic Voriconazole of Chemical Formula 2; and carrying out optical isolation of the racemic Voriconazole by adding an adequate optically active acid thereto to obtain Voriconazole having high optical purity with high cost-efficiency and high yield.

Abstract: Disclosed is a method for preparing a longer sustained-release formulation containing bioactive substances. More particularly, the present invention provides a method for preparing longer sustained-release microcapsules comprising: adding an emulsion including bioactive substances, biocompatible polymer and polyvinylpyrrolidone to an aqueous solution.

Abstract: Provided is a process for preparing Voriconazole represented by Chemical Formula 1. More particularly, the process for preparing Voriconazole of Chemical Formula 1 includes: carrying out the Reformatsky-type coupling reaction between a ketone derivative of Chemical Formula 4 and a pyrimidine derivative of Chemical Formula 5 to obtain a compound of Chemical Formula 3; reacting the substituents halo and oxysulfonyl with a hydrogen donor to obtain racemic Voriconazole of Chemical Formula 2; and carrying out optical isolation of the racemic Voriconazole by adding an adequate optically active acid thereto to obtain Voriconazole having high optical purity with high cost-efficiency and high yield.

Abstract: The present invention relates to a method for preparing a sustained-release microsphere which can control the long-term release of a drug. More particularly, as the preparation of a microsphere in which a drug is loaded in a carrier comprising a biodegradable polymer, the present invention relates to a method for preparing a sustained-release microsphere wherein a solvent intra-exchange evaporation method by means of co-solvent is used for suppressing the initial burst release of physiologically active substance, to release the physiologically active substance in the body continuously and uniformly.

Abstract: Disclosed is a method for preparing a longer sustained-release formulation containing bioactive substances. More particularly, the present invention provides a method for preparing longer sustained-release microcapsules comprising: adding an emulsion including bioactive substances, biocompatible polymer and polyvinylpyrrolidone to an aqueous solution.

Abstract: Disclosed is a method of producing teicoplanin. The method includes purifying teicoplanin from a culture broth, obtained by culturing microorganisms capable of producing teicoplanin by a porous adsorption resin under selective elution conditions and recovering highly pure teicoplanin using activated carbon and/or ultrafiltration. In this regard, the method can further include ultrafiltration as pre-treatment before the culture broth is adsorbed into the porous adsorption resin so as to increase the purity of teicoplanin.

Abstract: Disclosed is a method of producing teicoplanin. The method includes purifying teicoplanin from a culture broth, obtained by culturing microorganisms capable of producing teicoplanin by a porous adsorption resin under selective elution conditions and recovering highly pure teicoplanin using activated carbon and/or ultrafiltration. In this regard, the method can further include ultrafiltration as pre-treatment before the culture broth is adsorbed into the porous adsorption resin so as to increase the purity of teicoplanin.

Abstract: Nucleoside derivatives represented by formula (I); ##STR1## wherein, R.sub.1 represents hydrogen, phosphate or phosphonate group, R.sub.2 represents substituted or unsubstituted pyrimidine or purine base, and Z represents S, SO, SO.sub.2, O or C; or pharmaceutically acceptable salts thereof. Compound (I) can be obtained by reacting a compound of the formula (II); ##STR2## wherein, R.sub.7 represents hydrogen or hydroxy-protecting group, L represents aromatic or nonaromatic acyl, halide or alkoxy, and Z represents S, SO, SO.sub.2, O or C, with a base.