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公开(公告)号：KR1020110100944A
公开(公告)日：2011-09-15
申请号：KR1020100020044
申请日：2010-03-05
Applicant: 한국화학연구원 , 한국콜마홀딩스 주식회사
IPC: A61K31/675 , A61K9/70 , A61P19/10 , A61P19/00
CPC classification number: A61K31/675 , A61K9/0009 , A61K9/0014 , A61K47/14 , A61K47/183 , A61K47/26
Abstract: 본 발명은 경구 투여 시 생체 내 낮은 흡수율과 위장관 부작용을 나타내는 리세드로네이트에 피부 투과 가속제, 폴리아미노폴리카르복실릭계 킬레이트 첨가제, 또는 이들의 혼합물을 첨가한 조성물로서, 이온토포레시스를 통하여 경피 투여 하는 경우 위장관 부작용을 회피하면서도, 높은 체내 흡수율을 나타낼 수 있는 리세드로네이트 함유 경피 투여용 조성물에 관한 것이다.
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公开(公告)号：KR1020080094473A
公开(公告)日：2008-10-23
申请号：KR1020070038959
申请日：2007-04-20
Applicant: 한국화학연구원
CPC classification number: A61K9/1271 , A61K9/1277 , A61K9/5123 , A61K9/5146 , A61K31/7048
Abstract: An anionic lipid nanosphere is provided to show increased encapsulation efficiency of an insoluble drug in an aqueous phase by introducing a polyethylene glycol(PEG) containing polyol onto the surface of particles formed from an anionic phospholipid, reduce toxicity of the drug against normal cells and increase in vivo circulation time of the drug by encapsulating a very strongly toxic drug into lipid nanosphere. An anionic lipid nanosphere for encapsulating an insoluble drug such as amphotericin B is characterized in that a PEG containing polymer is coated on the surface of particles formed by an anionic phospholipid. A method for preparing the anionic lipid nanosphere comprises the steps of: (a) mixing 100 parts by weight of lipid prepared by mixing phosphatidylcholine, anionic phospholipd and sterol in a weight ratio of 40-70:5-20:10-40 with 10-30 parts by weight of the polymer containing the PEG and dissolving a mixture in an organic solvent to prepare a lipid-PEG mixture solution; (b) dissolving an insoluble drug in C1-6 linear or branched alcohol to prepare a drug solution; (c) mixing the lipid-PEG mixture solution with the drug solution in a volumetric ratio of 1:1-1:9 to prepare a lipid-PEG-drug mixture solution; (d) dispersing the mixture solution into an aqueous phase in a volumetric ratio of 2:1-10:1 to form lipid nanosphere; and (e) after subjecting the lipid nanosphere solution obtained from the step(d) to distillation at a temperature of 20-50 deg.C under reduced pressure to remove the organic solvent therefrom, filtering it to prepare the anionic lipid nanosphere encapsulating the drug.
Abstract translation: 提供阴离子脂质纳米球，通过将含有聚乙二醇（PEG）的多元醇引入到由阴离子磷脂形成的颗粒表面上，在水相中显示不溶性药物的包封效率，降低药物对正常细胞的毒性并增加 药物的体内循环时间通过将非常强毒性的药物包封在脂质纳米球中。 用于包封不溶性药物如两性霉素B的阴离子脂质纳米球的特征在于将含PEG聚合物涂覆在由阴离子磷脂形成的颗粒的表面上。 制备阴离子脂质纳米球的方法包括以下步骤：（a）将100重量份通过将磷脂酰胆碱，阴离子磷脂和甾醇以40-70:5-20:10-40的重量比混合制备的脂质与10 -30重量份含有PEG的聚合物，并将混合物溶解在有机溶剂中以制备脂质-PEG混合溶液; （b）将不溶性药物溶解在C1-6直链或支链醇中以制备药物溶液; （c）以1：1-1：9的体积比混合脂质-PEG混合溶液与药液，制备脂质-PEG-药物混合溶液; （d）将混合溶液以2:1-10:1的体积比分散在水相中以形成脂质纳米球; 和（e）在将步骤（d）获得的脂质纳米圈溶液在20-50℃的温度下减压蒸馏除去有机溶剂之后，过滤以制备包封该药物的阴离子脂质纳米球 。
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公开(公告)号：KR1020120133310A
公开(公告)日：2012-12-10
申请号：KR1020110051931
申请日：2011-05-31
Applicant: 한국화학연구원
CPC classification number: A61K9/1272 , A61K47/24 , A61K49/103 , A61K49/1812
Abstract: PURPOSE: A liposome containing ionic lipid and lipid which is combined with Gd-complex by covalent bond is provided to control release of a drug by ultrasonic wave. CONSTITUTION: A sonosensitive liposome for a contrast contains cationic lipid and contrast metal atom-complex-conjugated lipid. The lipid is denoted by chemical formula 1. The contrast metal atoms include: a transition metal atom of Ba, Cr, Mn, Fe, Co, Ni, Cu, Zn, Cd, Hg, Nb, Mo, Zr, Te, W, Pd, Ag, Pt, or Au; a 13-15 group atom of Ga, In, Sn, Pb, or Bi; a lanthanide or actinoid metal atom of Gd, Tb, Dy, Ho, Er, Sm, or Nd; or a metal atom of radioactive isotope. A drug delivery system contains the liposome and a drug encapsulated in the liposome. The liposome is released at 20kHz-5MHz.
Abstract translation: 目的：提供含有通过共价键与Gd-络合物结合的离子脂质和脂质的脂质体，以通过超声波控制药物的释放。 构成：用于对比的声敏脂质体包含阳离子脂质和对比金属原子 - 复合物共轭脂质。 脂肪由化学式1表示。对比金属原子包括：Ba，Cr，Mn，Fe，Co，Ni，Cu，Zn，Cd，Hg，Nb，Mo，Zr，Te，W的过渡金属原子， Pd，Ag，Pt或Au; Ga，In，Sn，Pb或Bi的13-15组原子; Gd，Tb，Dy，Ho，Er，Sm或Nd的镧系元素或锕系金属原子; 或放射性同位素的金属原子。 药物递送系统包含脂质体和包封在脂质体中的药物。 脂质体以20kHz-5MHz释放。
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公开(公告)号：KR1020090021065A
公开(公告)日：2009-02-27
申请号：KR1020080019750
申请日：2008-03-03
Applicant: 한국화학연구원
CPC classification number: A61K47/42 , A61K9/1271 , A61K9/1277 , A61K31/663 , A61K38/12
Abstract: A liposome coated with protein is provided to improve the in vivo circulation time in bloodstream compared to the conventional liposome, strengthen the stability in plasma, and inhibit adsorption to plasma protein, thereby enhancing drug delivery efficiency to the target area in the body and continuance of medicine effect exhibition. The liposome coated with protein having increased in vivo circulation time in bloodstream is prepared by binding the protein to the surface of liposome including cationic lipid through ionic bond, wherein the protein is selected from albumin, globulin, glutenin, prolamine, albuminoid, nucleoprotein, glycoprotein, phosphoprotein, lipoprotein, chromoprotein, gelatin, proteose, peptone, dipeptide and tripeptide, and has the average molecular weight of 2,000-1,500,000 Da.
Abstract translation: 提供涂覆有蛋白质的脂质体，以改善血液中体内循环时间，与常规脂质体相比，增强血浆中的稳定性，抑制血浆蛋白的吸附，从而提高药物对体内目标区域的输送效率，并持续 药效展览。 通过将蛋白质与包括通过离子键结合的阳离子脂质的脂质体表面结合来制备涂有血液中体内循环时间增加的蛋白质的脂质体，其中蛋白质选自白蛋白，球蛋白，谷蛋白，谷醇溶蛋白，类白蛋白，核蛋白，糖蛋白 ，磷蛋白，脂蛋白，生色蛋白，明胶，蛋白质，蛋白胨，二肽和三肽，平均分子量为2,000-1,500,000 Da。
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Patent Agency Ranking
公开(公告)号：KR100832553B1
公开(公告)日：2008-05-26
申请号：KR1020060128139
申请日：2006-12-14
Applicant: 한국화학연구원
IPC: A61K9/16 , A61K9/51 , A61K31/7048 , B82Y5/00
CPC classification number: A61K9/1617 , A61K31/7048 , B82Y5/00
Abstract: A lipid nanosphere encapsulating amphotericin B is provided to coat the lipid nanosphere surface with heparin by using an anionic phospholipid or introducing a polymer having a polyethyleneglycol(PEG) group thereinto, thereby increasing circulation time in a body and decreasing toxicity of the amphotericin B. A lipid nanosphere encapsulating amphotericin B is characterized in that a PEG is exposed to the surface of the lipid nanosphere including an anionic phospholipid and the surface of the lipid nanosphere is coated with heparin to prolong circulation time in a body. A method for preparing the lipid nanosphere comprises the steps of: (a) after mixing phosphatidylcholine, the anionic phospholipid, sterol and a polymer having a PEG group in a weight ratio of 40-70:5-20:10-40:10-30, dissolving the mixture in an organic solvent; (b) dissolving the amphotericin B in a linear or branched C1-6 alcohol; (c) mixing the solution obtained from the step(a) and the solution obtained from the step(b) in a volumetric ratio of 1:1-1:9; (d) dispersing the mixture solution into an aqueous phase in a volumetric ratio of 2:1-1:10 to form the lipid nanosphere; (e) after distilling the lipid nanosphere solution at a temperature of 20-50 deg.C under reduced pressure to remove the organic solvent therefrom, filtering it to prepare the anionic lipid nanosphere encapsulating the amphotericin B; (f) mixing the lipid nanosphere obtained from the step(e) with heparin to have the lipid forming the lipid nanosphere and the heparin in a weight ratio of 100:0.1-100:10; and (g) removing the heparin or a derivative therefor not-coating the lipid nanosphere from the mixture solution of the step(f). Further, an average molecular weight of the heparin is 500 to 50000.
Abstract translation: 通过使用阴离子磷脂或引入具有聚乙二醇（PEG）的聚合物的聚合物来提供包封两性霉素B的脂质纳米球B用肝素包被脂质纳米球表面，从而增加体内的循环时间并减少两性霉素B的毒性。 脂质纳米球包封两性霉素B的特征在于PEG暴露于包含阴离子磷脂的脂质纳米球表面，脂质纳米圈的表面涂有肝素以延长体内的循环时间。 制备脂质纳米球的方法包括以下步骤：（a）在混合磷脂酰胆碱后，阴离子磷脂，固醇和具有PEG基团的聚合物的重量比为40-70:5-20:10-40:10 30，将混合物溶解在有机溶剂中; （b）将两性霉素B溶解在直链或支链C 1-6醇中; （c）将步骤（a）获得的溶液与步骤（b）获得的溶液的体积比为1:1-1:9混合; （d）以2:1-1:10的体积比将混合溶液分散到水相中以形成脂质纳米球; （e）在20-50℃的温度下在减压下蒸出脂质纳米球溶液以除去有机溶剂，过滤以制备包封两性霉素B的阴离子脂质纳米球; （f）将从步骤（e）获得的脂质纳米球与肝素混合以使脂质纳米球和肝素的重量比为100：0.1-100：10; 和（g）除去肝素或其衍生物，从步骤（f）的混合溶液中不包被脂质纳米球。 此外，肝素的平均分子量为500〜50000。
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公开(公告)号：KR100996975B1
公开(公告)日：2010-11-29
申请号：KR1020080019750
申请日：2008-03-03
Applicant: 한국화학연구원
Abstract: 본 발명은 혈류 내 순환시간을 증가시킨 단백질로 수식된 리포솜 및 이의 제조방법에 관한 것으로서, 더욱 상세하게는 생체적합성 단백질을 양이온성 리포솜 표면에 정전기적 상호인력으로 이온 결합시키고, 리포솜 표면에 결합된 단백질을 변성시켜 리포솜과의 결합력이 강화시킴으로써 리포솜이 혈류 내에서 순환할 때 혈장 내 단백질의 흡착을 방지하여 혈류 내에서 리포솜의 안정성을 강화하는 한편, 체내 순환시간을 증가시키는 리포솜 및 이의 제조방법에 관한 것이다.
단백질, 수식, 리포솜, 이온 결합, 체내 순환시간-
公开(公告)号：KR101350497B1
公开(公告)日：2014-01-22
申请号：KR1020110051931
申请日：2011-05-31
Applicant: 한국화학연구원
Abstract: 본 발명은 초음파 감응성을 위해 이온성 지질과 지질의 말단에 Gd-컴플렉스가 공유결합된 지질을 함유하는 리포솜에 관한 것으로, 더욱 상세하게는 조영작용 위하여 Gd-컴플렉스를 초음파 감응성 지질에 공유결합시켜 제조된 Gd-컴플렉스 공유결합된 지질과 초음파 감응성을 위한 양이온성 지질을 함유하는 리포솜에 관한 것으로 제조된 리포솜은 초음파에 의해 약물을 방출제어 할 수 있으며 동시에 Gd-컴플렉스에 의한 조영작용을 할 수 있다.
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公开(公告)号：KR100979462B1
公开(公告)日：2010-09-02
申请号：KR1020070077934
申请日：2007-08-03
Applicant: 한국화학연구원
Abstract: 본 발명은 안트라사이클라인계 항암약물 봉입용 리포솜 및 이의 제조방법에 관한 것으로, 더욱 상세하게는 양전하를 갖는 지질과 인지질을 함유하는 리포솜에 폴리에틸렌글리콜(PEG) 유도체를 도입하여 이온성 리포솜을 제조함으로써 암세포 내로 효과적으로 이입되어 항암약물의 투여가 용이한 세포이입성이 증진된 안트라사이클라인계 항암약물 봉입용 리포솜 및 이의 제조방법에 관한 것이다.
안트라사이클라인계 항암약물, 리포솜, 폴리에틸렌글리콜 유도체, 세포이입성-
公开(公告)号：KR1020090013848A
公开(公告)日：2009-02-06
申请号：KR1020070077934
申请日：2007-08-03
Applicant: 한국화학연구원
CPC classification number: A61K9/1273 , A61K47/34
Abstract: A liposome for encapsulating anthracycline anticancer drug is provided to improve absorption efficiency of liposome delivered to the tumor tissue into the cancer cell by introducing PEG(polyethylene glycol) to the phospholipid having positive charge or the surface of liposome containing this. The ionic liposome for encapsulating anthracycline anticancer drug is prepared by introducing PEG derivative into the phospholipid having positive charge which is 1,2-disteroyl-3-trimethylammonium-propane(DOTAP), dimethyldioctadecylammonium(DDAB), 1,2-diacyl-3-dimethyl ammonium propane(DAP) or L-a-dioleylphosphatidylethanolamine(DOPE), or the surface of liposome containing this.
Abstract translation: 提供用于包封蒽环类抗癌药物的脂质体，以通过将PEG（聚乙二醇）引入具有正电荷的磷脂或含有这种脂质体的表面来提高向肿瘤组织递送至肿瘤组织的脂质体的吸收效率。 通过将PEG衍生物引入具有1,2-二甲酰基-3-三甲基铵 - 丙烷（DOTAP），二甲基二十八烷基铵（DDAB），1,2-二酰基-3-甲基丙烷的正电荷的磷脂中制备用于封装蒽环类抗癌药物的离子脂质体， 二甲基铵丙烷（DAP）或者La-二油基磷脂酰乙醇胺（DOPE），或含有此的脂质体的表面。
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