Abstract: Disclosed herein are novel benzophenone derivatives represented by formula I, a pharmaceutically acceptable salt thereof, a hydrate thereof or a solvate thereof, a pharmacological composition containing the same, and a use of the composition as therapeutic drugs. The benzophenone derivatives have an inhibition activity of microtubule formation and can be used to treat a normal proliferative state of a malignant tumor by killing the actively proliferating cells.

Abstract: Disclosed relates to a simplified method for resolving enantiomers by dissolving a racemic mixture having chiral carbon in ?-position of nitrogen and an amino acid to prepare a diastereomeric salt, not using catalyses or enzymes, with enhancing the optical purity remarkably. Moreover, the present invention can prepare the enantiomers in large quantities without using expensive catalysts or without controlling the reaction conditions for the activity of enzymes applied.

Abstract: The present invention is a novel resinate complex of (+)-clopidogrel optical isomer, wherein the (+)-clopidogrel isomer is bounded to a water-soluble cation exchange resin having sulfonic acid groups. The novel resinate complex has recognized some advantages in that (1) its chemical structure is stable, and (2) it can be formulated into a solid form that may provide taste-masking capabilities associated with bitter drugs (e.g., strong irritation, bitterness and sour taste), thus requiring no drink of water.

Abstract: Provided is a pharmaceutical composition having improved oral absorption of a bisphosphonate drug, comprising at least one active substance selected from bisphosphonate drugs having non-permeability to a lipid biomembrane due to ionization and high water-solubility in vivo and having bioavailability of less than 10%, and at least one selected from biocompatible water-soluble chitosan, as essential ingredients.

Abstract: Disclosed herein is a paroxetine cholate or cholic acid derivative salt and a composition comprising paroxetine and cholic acid or a derivative thereof. Further disclosed is a pharmaceutical composition comprising the paroxetine salt or the composition. The pharmaceutical composition can be formulated into an oral preparation for swallowing without water as an orally disintegrating tablet for paroxetine.

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: 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: A nystatin-resistant mutant microorganism belonging to Aspegillus genus is provided for preparing triol heptanoic acid, a precursor of 3-hydroxy-3-methylglutaryl-CoA reductase inhibitor. A mutant Aspergillus terreus CLS247-13, KCTC 0673 BP is prepared by treating Aspergillus terreus CLS216-7, KCTC 0359 BP with ultraviolet ray or chemical mutagens. The mutant provides high productivity (at least 11.5 g/L, 95/6% of the total product) of triol heptanoic acid, while reducing (less than 0.53 g/L, 4.4% of total product) productivity of triol heptanoic acid analogues. Since the nystatin-resistant mutant strain CLS347-13 has a capability of producing triol heptanioc acid with a high yield in a short period of culture time compared with known triol heptanoic acid producing strains, it can be widely used in industrial applications.