Chong Kun Dang Corporation

Chong Kun Dang Pharmaceutical Corporation

Samjin Pharmaceutical Co., Ltd.

Astech. Co., Ltd.

Incheon University Industry Academic Cooperation Foundation

Bamichem Co., Ltd.

Aptabio Therapeutics Inc.

Hee Jong Shin

Jung Woo Kim

Chung Il Hong

Min Hyo Ki

Nam Hee Choi

Eui Hwan Cho

Su Geun Yang

Jae Hyun Kim

Hyun Tae Kim

Sung Woo Lee

Eui-Hwan Cho

Soon Kil Ahn

Jong Lae Lim

Jae Woong Lee

Ho Seok Kwon

Jeong Ho Joo

Sung Ju Choi

Ki Seok Park

Jong Bae Yoon

Ho Tae Nam

Jong Min Kim

Sung Hwan Moon

Sung Pyo Hong

Soo Jin Lee

Kyeong Bok Min

Woo Heon Song

Tae Won Kang

Su Geon Yang

Joon K Park

Chong Kook Kim

Keun Kuk Lee

Sang Joon Lee

Jae Soo Shin

Su Kyung Lee

Hong Woo Lee

Hyoung Min Cho

Su Kyoung Lee

Bok Young Kim

Ho Joon Park

Dong Ock Cho

Sung Hye Kim

Won Kyu Choi

Sung Hyun Kang

Yong Bin Park

Woo-Heon Song

Ji Hyun Um

Yu Mi Ji

Disclosed is an oral pharmaceutical composition for preventing or treating dry eye syndrome, which comprises rebamipide or a prodrug thereof, or a pharmaceutically acceptable salt thereof, as an active ingredient. The compounds can treat dry eye syndrome via oral route, and can be thus employed safely and conveniently compared to conventional eye drops.

Oral pharmaceutical composition for preventing or treating dry eye syndrome comprising rebamipide or a prodrug thereof

Disclosed are a novel rebamipide prodrug, a method for preparing the same, and use thereof. Also, a pharmaceutical composition comprising the novel rebamipide prodrug as an active ingredient is provided. The rebamipide prodrug is increased 25-fold in absorption rate compared to rebamipide itself, and can be applied to the prophylaxis or therapy of gastric ulcer, acute gastritis, chronic gastritis, xerophthalmia, cancer, osteoarthritis, rheumatoid arthritis, or obesity.

Rebamipide prodrugs, preparation method and use thereof

The present invention provides a novel pyridine derivative, a pharmaceutically acceptable salt thereof, a method for preparing the same, and a pharmaceutical composition containing the same as an active ingredient. The pyridine derivative according to the present invention inhibits Raf kinase (B-Raf, Raf-1, or B-RafV600E) and a vascular endothelial growth factor receptor (VEGFR2) involved in angiogenesis, and thus, can be favorably used for the prevention or treatment of melanoma, colorectal cancer, prostate cancer, thyroid cancer, lung cancer, pancreatic cancer, ovarian cancer, or the like, which is induced by RAS mutation.

Pyridine derivative inhibiting RAF kinase and vascular endothelial growth factor receptor, method for preparing same, pharmaceutical composition containing same, and use thereof

The present invention relates to an inclusion compound of fumagillol derivative or its salt with hydroxypropyl-&#x3b2;-cyclodextrin or sulfobutylether-7-&#x3b2;-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.

Inclusion compounds of fumagillol derivative or its salt, and pharmaceutical compositions comprising the same

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.

Paroxetine cholate or cholic acid derivative salts, and composition comprising paroxetine and cholic acid or derivative thereof

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. The present invention is to provide the improved process of preparing simvastatin expressed by formula 1 environmentally sound, economically efficient, and industrially useful.

Process for preparing simvastatin

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.

Pharmaceutical composition comprising cyclosporin solid-state microemulsion

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. Especially, in the case that the composition according to the present invention is formulated in a soft capsule, the resultant capsule does not show the disadvantages of the prior arts such as the reactivity of hydrophilic solvent with gelatin shell of soft capsule and the volatility of hydrophilic solvent. It is because the existing patents use a hydrophilic solvent as an essential component of their compositions but the present invention does not use any hydrophilic solvent.

Cyclosporin-containing microemulsion preconcentrate composition

Acetamenophen composition with reduced liver toxicity

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. Especially, if the cyclosporin microemulsion preconcentrate comprising cyclosporin, oil, lipophilic solvent and surfactant is formulated in a soft capsule according to the present invention, the resultant capsule removes the disadvantages of the prior arts showing the reactivity of hydrophilic solvent with gelatin shell of soft capsule and the volatility of hydrophilic solvent wherein the hydrophilic solvent was essential component in the composition according to the existing patents.

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. When the composition of the present invention using propylene carbonate or its mixture with polyoxyethylene-polyoxypropylene block copolymer in a liquid state at room temperature is formulated into the soft capsule, it provides some advantages that it can inhibit the change in the capsule appearance and the precipitation of active ingredient due to the change in the solvent content, reduces the manufacturing cost to provide an economical effect and is substantially less toxic, in comparison to the soft capsule using ethanol, transcutol, propylene glycol, glycofurol, dimethylisosorbide, etc., in the prior art.

Cyclosporin-containing pharmaceutical composition

The present invention relates to a cyclosporin-containing powder composition which comprises cyclosporin, a non-ionic hydrophilic surfactant and a porous carrier. In addition, the present invention relates to a method for preparing the cyclosporin-containing powder composition which comprises dissolving cyclosporin and a non-ionic hydrophilic surfactant in an organic solvent, adding a porous carrier to the resulting solution and then evaporating the organic solvent from the mixture. The powder composition of the present invention is stable and does not require a special manufacturing technique when it is formulated. In addition, since the powder composition of the present invention does not contain an organic solvent, the necessity of a special package is excluded. Furthermore, the composition of the present invention provides an improved bioavailability which results in decrease of a single dosage, and therefore, can contribute to the alleviation of the side effects associated with cyclosporin.

Cyclosporin containing powder composition

Growing community of inventors

Kyunggi-do, South Korea

Hee Jong Shin