Abstract:
A transdermal preparation is provided to promote the drug absorption by the skin hydration through a hydrophobic adhesive layer, show continuous and high effect of a drug by maintaining the thermodynamic activity of the hydrophobic drug in an adhesive caused by moisture discharged from skin and be able to reduce the cost and the time due to a very simple preparing process. A transdermal preparation for a hydrophobic drug comprises a supportive layer(1) which is the uppermost portion of a layered structure and has the elasticity; a hydrophobic adhesive layer(2) which is layered under the supportive layer and prevents the loss of moisture absorbed from skin and the reverse conversion of the drug; and a drug containing adhesive layer(3) which is layered under the hydrophobic adhesive layer, includes a drug and attaches the transdermal preparation to the skin and is characterized in that the drug adhesive layer includes a hydrophobic drug such as a non-steroidal antiphlogistics and an absorption promoting agent, where a hydrophobic adhesive of the hydrophobic adhesive layer is selected from the group consisting of polyisobutylene adhesive, styrene-isoprene-styrene adhesive, and styrene-butadiene-styrene adhesive, the drug containing adhesive layer is an acrylate polymer made from acrylate, hydroxypropyl acrylate, acrylamide, acrylamide vinyl acetate, vinyl derivative, methacrylate, hydroxypropyl methacrylate and methacrylamide. The preparation further comprises a release layer(4) which is layered under the drug adhesive layer and protects the drug adhesive layer before use.
Abstract:
A transdermal preparation is provided to continuously allow a highly concentrated hydrophobic drug to be absorbed into skin until a patch is detached from the skin with minimized skin side effects and provide the enough adhesive capability during the time of exhibiting the medical efficacy by being attached to the skin. A transdermal preparation for a hydrophobic drug comprises a supportive layer(1) which is the uppermost portion of a layered structure and has the elasticity; a hydrophobic adhesive layer(2) which is layered under the supportive layer and prevents the loss of moisture absorbed from skin and the reverse conversion of the drug; and a drug adhesive layer(3) which is layered under the hydrophobic adhesive layer, includes a drug and attaches the transdermal preparation to the skin and is characterized in that the drug adhesive layer includes a hydrophobic drug such as a non-steroidal antiphlogistics and an acryl adhesive agent and the acryl adhesive agent includes a hydrophilic monomer promoting the skin absorption from the skin and is selected from the group consisting of acrylic acid, methyl methacrylate, ethyl acrylate, hydroxyethyl acrylate, butyl acrylate, octyl acrylate, 2-ethylhexyl acrylate, and hexyl acrylate. The preparation further comprises a release layer(4) which is layered under the drug adhesive layer and protects the drug adhesive layer before use.
Abstract:
A sustained-release porous microparticle for pulmonary delivery of a charged protein drug is provided to rapidly deliver the charged protein drug to epidermal cells in deep part of the lung without macrophage damage, thereby maintaining stability of the protein drug and continuously releasing the protein drug for a long period of time. A sustained-release porous microparticle for pulmonary delivery of a charged protein drug is prepared by (1) solubilizing cyclodextrin derivatives, ionic polysaccharides and a charged protein drug in water to prepare an inner water phase, (2) adding biodegradable polymer into organic solvent to prepare an organic phase, (3) mixing the inner water phase of step (1) with the organic phase of step (2) to prepare a first emulsion, and (4) spraying the first emulsion to an outer aqueous continuous phase containing an aqueous coating material, and has an average particle diameter of 5-100 mum.
Abstract:
본 발명은 수크로스 아세테이트 이소부티레이트(sucrose acetate isobutyrate, SAIB)를 포함하는 미세입자의 제조방법에 관한 것으로, (1) 단백질 약물을 수성 용액에 녹여 수상(water phase)을 제조하는 단계; (2) 수크로스 아세테이트 이소부티레이트와 생분해성 고분자를 유기용매에 녹여 유상(oil phase)을 제조하는 단계; (3) 단계 (1)의 수상을 단계 (2)의 유상에 첨가하여 1차 에멀젼을 형성하는 단계; 및 (4) 1차 에멀젼을 외부 수성 연속상에 첨가하여 2차 에멀젼을 형성한 후, 2차 에멀젼 중에 생성된 고형물을 분리하는 단계를 포함하는 본 발명에 의하면, 약물의 초기 과다 방출 없이 생리적 활성을 유지하면서 약물을 장기간 지속적으로 방출할 수 있는 서방형 미세입자를 제조할 수 있다. 수크로스 아세테이트 이소부티레이트, 생분해성 고분자, 서방형 미세입자, 지속적 약물 방출
Abstract:
본 발명은 수용성 고분자 및 친수성 계면활성제를 포함하는 수용액에 비스포스포네이트를 용해 및 분산시켜 제조한 고분자 용액을, 생분해성 고분자 및 소수성 계면활성제를 포함하는 1차 유기용매 내에 2차 유기용매를 가하여 제조된 고분자 용액에 가하여 1차 에멀젼 용액 (water-in oil (W/O))을 제조하고, 1차 에멀젼 용액을 외부 연속상에 분산시켜 제조한 비스포스포네이트-함유 고분자 미립구를 포함하는, 골-관련 질환 치료 또는 예방용 서방 효과를 갖는 주사제에 관한 것이다. 상기 주사제는 1회 투여로 생체내에서 4주 이상의 지속적 서방출 효과를 나타내므로, 매일 투여되는 경구제에 비해 상당히 적은 투여 횟수 및 적은 투여 용량으로, 또한 비스포스포네이트의 직접 주사에 비해 국소 독성이 상당히 감소되어 비스포스포네이트 약물이 나타내는 치료 또는 예방 활성을 얻을 수 있다. 비스포스포네이트, 미립구, 서방, 주사제
Abstract:
본 발명은 서열번호: 1의 염기서열 중에서 선택된 활성 부위를 포함하는 프로모터; 상기 프로모터 및 리포터 유전자를 포함하는 벡터; 상기 벡터를 포함하는, 지방분해를 촉진하는 후보물질을 검색하기 위한 키트; 및 상기 벡터를 이용하여 지방분해를 촉진하는 후보물질을 검색하는 방법에 관한 것이다. 본 발명에서 제공되는 프로모터는 퍼록시좀 증식인자-활성화 수용체-감마(peroxisome proliferator-activated receptor-gamma, PPAR-γ)와 결합하여 멜라노코르틴 2 수용체 부속 단백질(melanocortin 2 receptor accessory protein, Mrap) 유전자의 발현을 증진시켜 부신피질자극 호르몬(Adrenocorticotropic hormone, ACTH)에 의한 지방 분해를 촉진하기 때문에, 상기 프로모터를 적절한 리포터 유전자와 융합시킨 벡터를 이용하면 지방 분해를 촉진하는 후보물질을 효과적으로 검색할 수 있으며, 이를 통해 얻어진 후보물질은 Mrap 유전자의 발현을 증진시켜 ACTH에 의한 지방 분해를 촉진하여, 비만 관련 질환을 치료 및 예방할 수 있다.
Abstract:
A pharmaceutical composition regulating the activity of sphingosylphosphorylcholine(SPC) is provided to regulate cell proliferation, inflammation and pruritus and treat inflammmatin or pruritus of dermatitis such as atopic dermatitis. A pharmaceutical composition which regulates the activity of sphingosylphosphorylcholine(SPC) comprises a compound of the chemical formula 1 or its pharmaceutically allowable salt. In the chemical formula 1, X is O or S, Y is CH2 or carbonyl. R1 is hydrogen or C1-10 alkyl, R2 is hydrogen or methyl, but when X is O, either R1 or R2 cannot be hydrogen, R3 is C1-4 alkyl. A method for manufacturing a compound of the chemical formula 1a comprises: a step of reacting a compound of the chemical formula 2 and a compound of the chemical formula 3 under the presence of base to obtain a compound of the chemical formula 4; a step of stirring the compound of the chemical formula 4 under the presence of base to obtain a compound of the chemical formula 5; and a step of performing the peptide bond between the compound of the chemical formula 5 and a compound of the chemical formula 6 to obtain the compound of the chemical formula 1a.
Abstract:
A composition for external application for treating and preventing the pruritus or irritant skin disease is provided to have excellent fluxes and stability by containing the thiourea derivative and to be useful in pruritus or irritant skin disease. A composition for external application of O/w-shaped emulsion form comprises (1) drug expressed as a compound of a chemical formula 1, (2) a component selected from a group consisting of squalene, dimethicone, propylene glycol, butylene glycol and mineral oil, (3) a component selected from a group consisting of polyethylene glycol 400, polyoxyethylene alkyl ether, cetyl alcohol and solbitan stearate, (4) water and (5) a component selected from a group consisting of ethanol, twin 60, carbomer 940, EDTA.2Na and triethanolammine.