Abstract: A composition for preventing or treating diabetes mellitus includes insulin and a GLP-1/glucagon dual agonist. The composition can inhibit the weight gain and reduce the danger of hypoglycemia due to the administration of insulin, lower the administration dose and greatly improve the compliance of drugs through a combined administration of a long-acting insulin conjugate and a long-acting GLP-1/glucagon dual agonist conjugate. In addition, the long-acting insulin conjugate and the long-acting GLP-1/glucagon dual agonist conjugate can improve the in vivo sustainability and stability because an insulin and a GLP-1/glucagon dual agonist are linked to the immunoglobulin Fc region via a non-peptidyl linker. A method for preventing or treat diabetes mellitus includes administration of the insulin and a GLP-1/glucagon dual agonist.

Abstract: The present invention relates to a liquid formulation comprising a solubilizer and montelukast or pharmaceutically acceptable salt thereof in a solution state as an active ingredient, and a method for preparing same. The liquid formulation of the present invention allows montelukast or pharmaceutically acceptable salt thereof to be substantially dissolved and present in a solution state, thereby preventing decrease of dissolution over time and increasing its bioavailability. In addition, because the liquid formulation of the present invention shows superior stability, taste and flavor, its medication compliance can be enhanced, and it can be effectively utilized for asthma and allergic rhinitis patients.

Abstract: The present invention relates to an insulinotropic peptide derivative with a modified N-terminal charge and a pharmaceutical composition including the same. Specifically, the insulinotropic peptide derivative is characterized in that the N-terminal positive charge of the insulinotropic peptide is modified to a neutral or net negative charge at neutral pH. The insulinotropic peptide derivative according to the present invention is rapidly dissociated from the GLP-1 receptor owing to the above modification in the N-terminal charge, and exhibits enhanced insulinotropic ability and blood glucose-lowering activity compared to the native insulinotropic peptide while maintaining its stability in blood. Accordingly, the insulinotropic peptide derivative of the present invention is very useful for the treatment of type 2 diabetes.

Abstract: The present invention relates to a method for improving the solubility of a physiologically active protein or peptide compared to that of a physiologically active protein or peptide which is not conjugated to an immunoglobulin Fc fragment, in which the method comprises conjugating the physiologically active protein or peptide to an immunoglobulin Fc fragment; and a composition for improving the solubility of a physiologically active protein or peptide, comprising an immunoglobulin Fc fragment, in which the composition improves the solubility compared to a composition without an immunoglobulin Fc fragment.

Abstract: Provided is an amorphous solid dispersion including a taxane or a pharmaceutically acceptable salt thereof, a pharmaceutically acceptable polymer, and a pharmaceutically acceptable surfactant, which has enhanced solubility. Also provided is a method for preparing the solid dispersion. The present subject matter also provides a tablet having good solubility, bioavailability and stability, which comprises the amorphous solid dispersion, an intragranular excipient, and an extragranular excipient.

Abstract: The present invention relates to an insulin analog that has reduced insulin receptor binding affinity for the purpose of increasing the blood half-life of insulin, and long-acting insulin, a conjugate, and a method of preparing long-acting insulin using the same.

Abstract: The present invention relates to a method for increasing serum half-life of a protein or peptide and decreasing immunogenicity thereof by site-specifically binding a carrier to a protein or peptide, and to the use thereof. The conjugate of the physiologically active protein or peptide of the present invention can significantly decrease immunogenicity in the human body and thus reduce antibody production rate against the protein or peptide. Therefore, the present conjugate has advantages in that a phenomenon of reduced clinical effects of the physiologically active protein or peptide is low, and it can be effectively used in the development of long-acting formulations having a high safety against the immune response.

Abstract: The present invention relates to a novel bicyclic derivative that has an inhibitory activity against sodium-glucose linked transporters (SGLTs) present in the intestines and kidneys, or a pharmaceutically acceptable salt, isomer, hydrate or solvate thereof, and a pharmaceutical composition including the same as an active ingredient, which effectively inhibit the SGLT activity, and thus can be used as a therapeutic agent to treat diseases caused by hyperglycemia, such as diabetes including insulin-dependent diabetes (type I diabetes mellitus) and non-insulin-dependent diabetes (type II diabetes mellitus), diabetic complications, and obesity.

Abstract: Disclosed is a pharmaceutical combination formulation comprising a first discrete part containing amlodipine and rosuvastatin and a second discrete part containing losartan, which exhibits improved dissolution rate and stability. The inventive combination formulation comprising amlodipine, losartan and rosuvastatin having different action mechanisms from one another can be effectively used to prevent or treat a cardiovascular disorder. Designed to minimize an interaction among active ingredients, the pharmaceutical combination formulation exhibits excellent storage stability and dissolution rates of amlodipine, losartan and rosuvastatin, and thus can be useful in pharmaceutical industries.

Abstract: Disclosed are a dry powder for inhalation formulation comprising salmeterol xinafoate, fluticasone propionate and tiotropium bromide, as pharmaceutically active ingredients, and a carrier, and an inhalation formulation comprising same and a method for preparing the same. The inventive dry powder inhalation formulation having good content uniformity and showing small changes in the aerodynamic size distribution in accordance with the flow rate changes can effectively deliver said pharmaceutically active ingredients to a target site upon administration, and thus can be useful in the prevention or treatment of respiratory diseases, particularly asthma and COPD.

Abstract: The present invention relates to a complex granule formulation comprising a first granular part comprising levocetirizine or its pharmaceutically acceptable salt, cyclodextrin or its derivative, and an alkalinizing agent; and a second granular part comprising montelukast or its pharmaceutically acceptable salt, cyclodextrin or its derivative, and an alkalinizing agent. This formulation can effectively inhibit the production of related compounds of levocetirizine and montelukast by allowing levocetirizine and montelukast to form clathrate complexes with cyclodextrin, and using an alkalinizing agent. This formulation not only shows increased stability and bioavailability, but also improves patient compliance owing to its effective masking of bitter taste.

Abstract: The present invention relates to a novel method for preparing 1-(4-(4-(3,4-dichloro-2-fluorophenylamino)-7-methoxyquinazolin-6-yloxy)piperidin-1-yl)prop-2-en-1-one in a simpler process as compared with conventional methods by allowing 4-(3,4-dichloro-2-fluorophenylamino)-7-methoxyquinazolin-6-ol to react with an N-acyl piperidine derivative in an inert polar protic solvent in the presence of a base.

Abstract: Provided are a solid composite formulation for oral administration, the solid composite formulation including: an ezetimibe granules-part including ezetimibe, said ezetimibe having a particle size distribution wherein the average particle size d(0.9) for the bottom 90% is about 10 ?m or less; and a rosuvastatin mixture-part including rosuvastatin or a pharmaceutically acceptable salt thereof, and a method of preparing the composite formulation.

Abstract: The present invention relates to a pharmaceutical formulation for oral administration for preventing or treating allergic rhinitis or asthma, which comprises: (a) a first particle part comprising levocetirizine or a pharmaceutically acceptable salt thereof and an organic acid; and (b) a second particle part comprising montelukast or a pharmaceutically acceptable salt thereof. The pharmaceutical formulation according to the present invention comprises an organic acid as a stabilizing agent, which can effectively inhibit the production of levocetirizine and montelukast related substances, and thus, show good stability.

Abstract: The present invention relates to a sustained type human growth hormone conjugate preparation comprising: a sustained type human growth hormone (hGH) conjugate resulting from conjugation between the immunoglobulin Fc region and a human growth hormone (hGH) constituting a bioactive peptide; a buffer solution; a nonionic surfactant; and a sugar alcohol. More specifically, the present invention relates to a sustained type human growth hormone conjugate freeze dried preparation and liquid preparation, to a production method for the freeze dried preparation, to a method of reconstituting the freeze dried preparation, and to a kit comprising the freeze dried preparation and a reconstituting solution.

Abstract: A method for mass production of human coagulation factor VII derivatives. The method employs an expression vector, containing i) a nucleotide sequence of DHFR promoter devoid of at least one CCGCCC repeat sequence from the GC-rich region thereof and a nucleotide sequence encoding a DHFR operably linked thereto, and ii) a nucleotide sequence of CMV early gene promoter and a nucleotide sequence encoding a human coagulation factor VII derivative operably linked thereto; and adds at least one selected from the group consisting of sodium butyrate, vitamin K, and a culture medium supplement.

Abstract: The present invention relates to a transformant prepared by introducing an expression vector comprising a polynucleotide encoding for a human immunoglobulin Fc fragment into Pichia sp. yeast, a method for producing an immunoglobulin Fc fragment comprising culturing the transformant, and recovering the immunoglobulin Fc fragment from the culture, and an immunoglobulin Fc fragment, prepared by the above method for use as a drug carrier. The transformant is suggested as a solution to the problems associated with the use of E. coli or animal cells as hosts for producing immunoglobulin Fc fragments useful as drug carriers, so that it can find various applications in the effective and economical production of drugs.

Abstract: The present invention relates to a composition for preventing or treating hyperlipidemia, fatty liver disease or arteriosclerosis, comprising an oxyntomodulin derivative as an active ingredient. The oxyntomodulin derivative has a high ability to activate GLP-1 receptor and glucagon receptor compared to native oxyntomodulin and has the effects of reducing the blood total cholesterol, low-density cholesterol and triglyceride levels that were increased by high-fat diet, and increasing high-density cholesterol levels and the high-density cholesterol/low-density cholesterol ratio. Thus, the oxyntomodulin derivative can be effectively used for the treatment of hyperlipidemia and related diseases.

Abstract: A compound selected from the group consisting of an isoquinoline-5-carboxamide derivative of formula (I), a pharmaceutically acceptable salt, an isomer, a hydrate and a solvate thereof is effective for the prevention or treatment of diseases associated with abnormal cell growth, which are caused by abnormal activation of a protein kinases.

Abstract: Provided is a long-acting pharmaceutical composition containing a conjugate comprising a physiologically active polypeptide linked to an immunoglobulin Fc fragment, wherein the composition contains a monomeric conjugate comprising one molecule of the physiologically active polypeptide linked to a single immunoglobulin Fc fragment, and optionally contains a multimeric conjugate comprising two or more molecules of the same physiologically active polypeptide linked to a single immunoglobulin Fc fragment, provided that the molar ratio of the monomeric conjugate to the multimeric conjugate in the composition is at least 19; a physiologically active polypeptide monomer-immunoglobulin Fc fragment conjugate that comprises a physiologically active polypeptide monomer linked via a non-peptidyl linker to an immunoglobulin Fc fragment, wherein the physiologically active polypeptide is linked via the non-peptidyl linker to the immunoglobulin Fc fragment in a monomeric form.