Abstract: The present invention relates to an inclusion compound of fumagillol derivative or its salt with hydroxypropyl-?-cyclodextrin or sulfobutylether-7-?-cyclodextrin, and pharmaceutical compositions comprising the same. The inclusion compound according to the present invention has superior water solubility and stability while exhibiting low toxicity, rendering it valuable as an anticancer agent or inhibitor of tumor metastasis.

Abstract: The present invention relates to an inclusion compound of fumagillol derivative or its salt with hydroxypropyl-?-cyclodextrin or sulfobutylether-7-?-cyclodextrin, and pharmaceutical compositions comprising the same. The inclusion compound according to the present invention has superior water solubility and stability while exhibiting low toxicity, rendering it valuable as an anticancer agent or inhibitor of tumor metastasis.

Abstract: The present invention relates to an inclusion compound of fumagillol derivative or its salt with hydroxypropyl-?-cyclodextrin or sulfobutylether-7-?-cyclodextrin, and pharmaceutical compositions comprising the same. The inclusion compound according to the present invention has superior water solubility and stability while exhibiting low toxicity, rendering it valuable as an anticancer agent or inhibitor of tumor metastasis.

Abstract: The present invention relates to an inclusion compound of fumagillol derivative or its salt with hydroxypropyl-?-cyclodextrin or sulfobutylether-7-?-cyclodextrin, and pharmaceutical compositions comprising the same. The inclusion compound according to the present invention has superior water solubility and stability while exhibiting low toxicity, rendering it valuable as an anticancer agent or inhibitor of tumor metastasis.

Abstract: The present invention relates to an inclusion compound of fumagillol derivative or its salt with hydroxypropyl-?-cyclodextrin or sulfobutylether-7-?-cyclodextrin, and pharmaceutical compositions comprising the same. The inclusion compound according to the present invention has superior water solubility and stability while exhibiting low toxicity, rendering it valuable as an anticancer agent or inhibitor of tumor metastasis.

Abstract: The present invention relates to an inclusion compound of fumagillol derivative or its salt with hydroxypropyl-?-cyclodextrin or sulfobutylether-7-?-cyclodextrin, and pharmaceutical compositions comprising the same. The inclusion compound according to the present invention has superior water solubility and stability while exhibiting low toxicity, rendering it valuable as an anticancer agent or inhibitor of tumor metastasis.

Abstract: The present invention relates to an inclusion compound of fumagillol derivative or its salt with hydroxypropyl-?-cyclodextrin or sulfobutylether-7-?-cyclodextrin, and pharmaceutical compositions comprising the same. The inclusion compound according to the present invention has superior water solubility and stability while exhibiting low toxicity, rendering it valuable as an anticancer agent or inhibitor of tumor metastasis.

Abstract: The present invention relates to an inclusion compound of fumagillol derivative or its salt with hydroxypropyl-?-cyclodextrin or sulfobutylether-7-?-cyclodextrin, and pharmaceutical compositions comprising the same. The inclusion compound according to the present invention has superior water solubility and stability while exhibiting low toxicity, rendering it valuable as an anticancer agent or inhibitor of tumor metastasis.

Abstract: Disclosed herein is a pharmaceutical composition for oral absorption of polar drugs. The composition consists essentially of (a) at least one polar active substance having a bioavailability of less than 30% which is poorly absorptive through lipid membranes because of its high hydrophilicity and charged ion; (b) at least one organic alkalizing agent having an amino acid or polyol structure which shows alkalinity in aqueous solution and is ionically bonded to the polar active substance; and (c) at least one surfactant having a C6-18 fatty acid structure which has an HLB of 4 to 18. Alternatively, the composition consists essentially of (d) at least one organic alkalizing agent having the characteristics of both the organic alkalizing agent and the surfactant instead of the organic alkalizing agent and the surfactant. The composition enables polar active drugs to penetrate the gastro-intestinal membrane and oral dosage forms to be substituted for injections.

Abstract: The present invention relates to an improved process for preparing simvastatin and more particularly, the improved process for preparing simvastatin expressed by formula 1 with high yield and high purity by performing the following sequential processes comprising: (i) hydrolysis of lovastatin as starting material with potassium t-butoxide in an organic solvent and small amount of water under a mild reaction condition, followed by lactonization of the obtained solid intermediate with preventing from formation of by-products; (ii) protection of an alcohol group with t-butyldimethylsilyl group which can be easily removed with concentrated hydrochloric acid without the formation of by-products; (iii) acylation of the obtained protected intermediate with acyloxytriphenyl phosphonium salt as an acylating agent under a mild reaction condition; and (iv) removal of the silyl protective group with a concentrated hydrochloric acid.

Abstract: The present invention relates to a thiazolidinedione derivative, represented in formula (1) below, pharmaceutically acceptable salts thereof, and/or pharmaceutically acceptable solvates thereof. Further, the present invention provides a pharmaceutical composition comprising the compound represented in formula (1) below, wherein: X represents a carbon or nitrogen atom, Y represents a hydrogen atom, an alkyl group, an alkoxy group, a halogen, or an aryl group, Z represents an oxygen, nitrogen, or sulfur atom, and R1 and R2 each represent a hydrogen atom; or R1 and R2 together form a bond.

Abstract: Disclosed herein is a process for preparing highly pure acarbose of formula (I) useful as medicine for the treatment of diabetes. The disclosed process comprises prepurifying an acarbose-containing solution using a synthetic adsorbent to produce a prepurified acarbose having an acarbose content of a predetermined level or more; and contacting the prepurified acarbose with a monodispersed, strongly acid cation exchanger, in one step, to absorb acarbose.

Abstract: The present invention relates to Streptomyces sp. producing tautomycetin which possesses an immunosuppressive or antibacterial activities, a process for preparing tautomycetin from the said microorganism, and an immunosuppressant or immunosuppressive pharmaceutical composition comprising tautomycetin as an active ingredient which suppresses interleukin-2 production, CD69 and interleukin-2 receptor(IL-2R) expression on the cell surface, and graft rejection in the organ transplantation. The present inventors isolated a soil microorganism which produces a substance possessing antibiotic and immunosuppressive activities, and identified the said microorganism and substance as a novel Streptomyces sp. and tautomycetin, respectively.

Abstract: The present invention relates to a novel pharmaceutical composition of a self-emulsifying matrix preparation, which is a preparation for transmucosal or transdermal absorption in which a self-emulsifying drug delivery system is grafted to a polymeric matrix preparation. For this, fatty alcohol, fatty acid or their derivatives of 6 to 20 carbon atoms having a drug absorption-accelerating action through the skin or mucous membrane is used as an oil phase. Also, to increase the drug content in the matrix, a liquid phase material having a boiling point of 100° C. or more is used as a solution adjuvant. Using such materials, the self-emulsifying system with a surfactant is prepared. A hydrophilic or hydrophobic polymer is added and dissolved in the self-emulsifying system, and the resulting mixture is dried to prepare the matrix preparation containing the self-emulsifying system.

Abstract: A pharmaceutical composition comprising a cyclosporin solid-state microemulsion is disclosed. In a preferred embodiment, the composition comprises a cyclosporin microemulsion dispersed in an enteric carrier. The composition does not dissolve in external phases such as artificial gastric fluid, but dissolves rapidly in artificial intestinal fluid, whereby it releases the cyclosporin microemulsion, providing rapid delivery of cyclosporin. The composition effectively maintains a therapeutic blood concentration of cyclosporin with once a day dosing, providing for convenience of administration and avoiding adverse effects induced by increasing peak blood cyclosporin concentrations associated with conventional cyclosporin formulations.

Abstract: Compounds useful as angiogenesis inhibiting agents and processes for their preparation are disclosed. In one embodiment, the compounds of the invention are represented by Formula 1: ##STR1## Also disclosed is a pharmaceutical composition for inhibiting angiogenesis in a mammal, said composition comprising a compound of Formula 1, or a pharmaceutically acceptable salt thereof, as an active ingredient.

Abstract: The present invention relates to a microemulsion preconcentrate composition comprising (1) cyclosporin as an active component; (2) alkyl ester of polycarboxylic acid and/or carboxylic acid ester of polyols as a lipophilic solvent; (3) oil; and (4) surfactant. The composition according to the present invention is characterized in that it dissolves in an external phase such as water, artificial gastric fluid and artificial intestinal fluid by controlling the mixing ratio of the components thereby to get the microemulsion form of inner phase diameter of 100 nm or below. The composition according to the present invention can be formulated as the dosage form of a soft capsule, a hard capsule sealed with a gelatin banding at the conjugated portion, or an oral liquid preparation for oral administration.

Abstract: The present invention relates to a microemulsion preconcentrate composition comprising (1) cyclosporin as an active component; (2) alkyl ester of polycarboxylic acid and/or carboxylic acid ester of polyols as a lipophilic solvent; (3) oil; and (4) surfactant. The composition according to the present invention is characterized in that it dissolves in an external phase such as water, artificial gastric fluid and artificial intestinal fluid by controlling the mixing ratio of the components thereby to get the microemulsion form of inner phase diameter of 100 nm or below. The composition according to the present invention can be formulated as the dosage form of a soft capsule, a hard capsule sealed with a gelatin banding at the conjugated portion, or an oral liquid preparation for oral administration.

Abstract: The present invention relates to a process for preparing human proinsulin which is represented as a following chemical formula(I): ##STR1## wherein, R is an amino acid residue or a peptide which is degradable enzymatically or chemically; and, X is a linkage of an amino group of A-1 in insulin A chain and a carboxyl group of B-30 in insulin B chain which can be separated from the A chain or the B chain enzymatically or chemically, provided that a region from A-1 to A-21 is the insulin A chain and a region from B-1 to B-30 is the insulin B chain. In accordance with the present invention, human recombinant insulin precursor can be simply manufactured with a good reproducibility, since dissolution, sulfonation, concentration, desalting and purification are remarkably simplified, while increasing the yield of refolding reaction.

Abstract: The present invention relates to a novel mutant of Aspergillus terreus which shows a resistance to both cerulenin and L-methionine analogue, and a process for preparing mevinolinic acid which comprises aerobic culture of the mutant strain and recovery of mevinolinic acid. The mutant of the present invention provides a remarkably high productivity of mevinolinic acid while reducing the production of byproducts such as mevinolinic acid analogues, when compared with a wild type Aspergillus terreus isolated from soil environment in Korea, and it successfully produce mevinolinic acid by employing monosaccharides such as glucose and galactose, unlike the mother strain.