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 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 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: 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 is related to a new analgesic composition of acetaminophen targeting decreasing of liver toxicity and releasing of hangover, which comprises aspartic acid promoting alcohol metabolism and methionine alleviating liver toxicity of acetaminophen. The analgesic combination preparation according to the present invention showed same analgesic and excellent protection effect against liver toxicity compared with the single preparation of acetaminophen, and decreased the blood concentration of alcohol and acetaldehyde causing hangover through improving metabolism rates of them. The combination preparation according to the present invention, therefore, is coincident with ideal new analgesic composition of acetaminophen having a minimized side effect and a hangover releasing effect.

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 pharmaceutical composition containing cyclosporin. More specifically, the present invention relates to a pharmaceutical composition containing cyclosporin, an oil component, a hydrophilic cosurfactant consisting of propylene carbonate or a mixture of propylene carbonate and polyoxyethylene-polyoxypropylene block copolymer, and a surfactant. The composition of the present invention is characterized in that it can be dissolved in an external phase such as water, artificial gastric juice and intestinal juice, etc. to form a self-emulsion with mild stirring and therefore, by appropriately adjusting the constitutional ratio of each component the diameter of particles in the inner phase of the emulsion thus formed can be readily controlled to 100 nm or below. The composition of the present invention can be formulated into the oral preparations such as soft capsules, hard capsules sealed with gelatin bending at the conjugated portion, oral liquid preparations, etc.