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公开(公告)号：WO2010024576A2
公开(公告)日：2010-03-04
申请号：PCT/KR2009/004734
申请日：2009-08-25
IPC: A61K9/22
CPC classification number: A61K9/2086
Abstract: 본 발명은 탈니플루메이트 함유 서방정 정제에 관한 것으로, 보다 구체적으로는 난용성 약물인 탈니플루메이트의 용해성을 증가시키기 위해 용해보조제를 사용하고 체내에서 안정적으로 서방성을 유지할 수 있도록 친수성 고분자를 포함하는 유핵정, 이중정 또는 약물 코팅층을 가지는 약물코팅정 형태의 탈니플루메이트 서방정에 관한 것이다. 본 발명에 의한 탈니플루메이트의 서방성 정제는 제조 공정이 비교적 쉽고, 방출 속도 조절이 가능하며, 기존의 시판중인 속방성 탈니플루메이트 370, 720 mg 제제보다 체내에서 일정한 속도로 약물 성분을 서서히 방출시킬 수 있는 우수한 용출 특성을 나타내므로 1일 3회 투여하는 불편함을 1일 1-2회 투여로 감소시킬 수 있는 장점이 있다.
Abstract translation: 本发明涉及含有脱硝酸盐的缓释片剂。 更具体地说，本发明涉及形成为包衣片剂和双层片剂或药物包衣层的药物包衣片剂的脱硝酸缓释片剂。 增溶助剂用于增加片剂中不溶性药物的塔芬酸盐的溶解度。 片剂含有亲水聚合物以稳定使用者身体的持续释放。 含有根据本发明的泼尼酸盐的缓释片剂具有相对容易的制造过程，并且能够控制释放速率。 此外，与常规的立即释放塔硝氟酸盐370,720mg制剂相比，该片剂具有优异的释放效率，用于以恒定速率逐渐释放身体中的药物成分。 因此，平板电脑具有每天一次或两次给药一日三次的不便之处。
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公开(公告)号：KR1020110000259A
公开(公告)日：2011-01-03
申请号：KR1020090057679
申请日：2009-06-26
Applicant: 한국화학연구원 , 주식회사 중앙백신연구소
IPC: A61K39/39 , A61K31/765 , A61P37/02
CPC classification number: A61K31/765 , A61K9/113 , A61K39/39 , Y10S514/885
Abstract: PURPOSE: An immune enhancer composition containing polymer emulsifier as a stabilizing agent and a vaccine composition containing the same are provided to continuously maintain immunity and to ensure formulation stability. CONSTITUTION: An immune enhancer composition contains oil ingredient, non-ionic emulsifier, aqueous ingredient and polymer emulsifier of A-B-A type block copolymer. A and B are denoted by chemical formula 1 and 2, respectively. The molecular weight of A and B is 500-50,000 each. A polymer emulsifier is contained in 0.1-5.0 weight% based on total weight. The immune enhancer is an emulsion of water-in-oil form. A vaccine composition contains the immune enhancer composition and biologically acceptable amount of immunogenic material.
Abstract translation: 目的：提供含有聚合物乳化剂作为稳定剂的免疫增强剂组合物和含有其的疫苗组合物，以连续地保持免疫力并确保制剂的稳定性。 构成：免疫增强剂组合物含有A-B-A型嵌段共聚物的油成分，非离子乳化剂，水性成分和聚合物乳化剂。 A和B分别由化学式1和2表示。 A和B的分子量分别为500-50,000。 基于总重量，聚合物乳化剂的含量为0.1-5.0重量％。 免疫增强剂是油包水形式的乳液。 疫苗组合物含有免疫增强剂组合物和生物可接受量的免疫原性物质。
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公开(公告)号：KR1020080101056A
公开(公告)日：2008-11-21
申请号：KR1020070047259
申请日：2007-05-15
Applicant: 한국화학연구원
IPC: A61K9/10 , A61K31/337 , B82B1/00 , B82Y5/00
CPC classification number: A61K9/127 , A61K31/685 , A61K31/688 , A61K47/44 , A61K9/107 , A61K31/337 , A61K2300/00 , B82B1/00 , B82Y5/00
Abstract: A diterpenoid alkaloid group drug solution is provided to become soluble in a water phase at a high concentration without a surfactant harmfulness to human body by including a lipid nano particle, to have a size distribution of a uniform particle and to be used as an injection having a high safety. A diterpenoid alkaloid group drug solution is manufactured by dispersing diterpenoid alkaloid group drug having a solid solution state and lipid nano particles in an aquatic medium. The lipid nano particles are manufactured by dispersing a lipid mixture comprising phospholipid, sterols, cationic lipid or anionic lipid and polyethylene glycol in an organic solvent. A mixing ratio of the phospholipid, the sterols, the cationic lipid or the anionic lipid and the polyethylene glycol is 3 ~ 8 : 2 ~ 6 : 1 ~ 5 : 0 ~ 3.
Abstract translation: 提供二萜类生物碱类药物溶液，通过包含脂质纳米颗粒，高浓度而不会对人体具有表面活性物质的危害而在水相中溶解，具有均匀粒子的粒度分布，并用作具有 安全性高。 通过将具有固溶态的二萜生物碱类药物和脂质纳米颗粒分散在水性介质中制备二萜类生物碱类药物溶液。 通过将包含磷脂，固醇，阳离子脂质或阴离子脂质和聚乙二醇的脂质混合物分散在有机溶剂中来制备脂质纳米颗粒。 磷脂，固醇，阳离子脂质或阴离子脂质和聚乙二醇的混合比为3〜8：2〜6：1〜5：0〜3。
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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：KR100795221B1
公开(公告)日：2008-01-17
申请号：KR1020060045214
申请日：2006-05-19
Applicant: 한국화학연구원
Abstract: 본 발명은 암포테리신 B 봉입하고 표면이 헤파린으로 수식된 리포솜 및 그 제조 방법에 관한 것으로, 더욱 상세하게는 리포솜을 형성하는 지질중 에서 양이온성 지질을 일정량 포함하고, 암포테리신 B를 봉입한 리포솜의 표면이 헤파린으로 수식된 것을 특징으로 하는 리포솜 및 그 제조 방법에 관한 것이다. 본 발명의 리포솜은 수상에서 난용성인 암포테리신 B의 봉입효율을 양이온성 지질을 사용하여 증가시키고, 독성이 매우 강한 암포테리신 B를 생체 친화성이 우수한 리포솜에 봉입하여 정상세포에 대한 독성을 감소시킴은 물론, 헤파린으로 수식하여 체내 순환시간의 증가와 지속적 방출효과를 갖도록 한다.
암포테리신 B, 리포솜, 헤파린, 양이온성 지질, 체내 순환시간, 지속적 방출-
Patent Agency Ranking
公开(公告)号：KR101952297B1
公开(公告)日：2019-02-26
申请号：KR1020170121647
申请日：2017-09-21
Applicant: 한국화학연구원
IPC: A61K49/10 , A61K31/704 , G01N33/553
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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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公开(公告)号：KR100829595B1
公开(公告)日：2008-05-14
申请号：KR1020060125542
申请日：2006-12-11
Applicant: 한국화학연구원
CPC classification number: C07H15/12 , A61K9/1277 , A61K47/26
Abstract: A liposome containing saccharide-conjugated phospholipid is provided to improve in vivo stability by increasing retention time, and incidence rate of liposome into a target cell, so that a drug is delivered efficiently to the target cell. A saccharide-conjugated phospholipid for modifying liposome is represented by the formula(1), wherein R1 and R2 are each independently C8-C24 acyl, X is disaccharide, n is an integer from 3 to 150. A liposome is modified by 0.1-20 mol% of the saccharide-conjugated phospholipid represented by the formula(1) based on the weight of total lipid components through a covalent bond. A method for preparing the liposome modified by saccharide-conjugated phospholipid comprises the steps of: adding an amine group to a saccharide; activating the carboxyl terminal of phospholipid containing polyethylene glycol and binding the activated phospholipid with the amine-added saccharide to prepare the saccharide-conjugated phospholipid represented by the formula(1); and modifying the liposome with the saccharide-conjugated phospholipid.
Abstract translation: 提供含有糖共轭磷脂的脂质体，以通过增加保留时间和脂质体进入靶细胞的发生率来提高体内稳定性，使得药物有效地递送至靶细胞。 用于修饰脂质体的糖共轭磷脂由式（1）表示，其中R 1和R 2各自独立地为C 8 -C 24酰基，X为二糖，n为3至150的整数。脂质体改性为0.1-20 基于通过共价键的总脂质成分的重量，由式（1）表示的糖共轭磷脂的摩尔％。 制备由糖共轭磷脂改性的脂质体的方法包括以下步骤：向糖中加入胺基; 活化含有聚乙二醇的磷脂的羧基末端，并将活化的磷脂与加入胺的糖结合，制备由式（1）表示的糖共轭磷脂; 并用糖结合的磷脂修饰脂质体。
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公开(公告)号：KR100768265B1
公开(公告)日：2007-10-17
申请号：KR1020050107472
申请日：2005-11-10
Applicant: 한국화학연구원
IPC: A61K9/127
Abstract: 본 발명은 헤파린과 같은 음전하를 지니고 있는 고분자를 양전하를 띄고 있는 리포솜의 표면에 정전기적 결합에 의하여 결합시킴으로서 친수성 고분자가 결합된 리포솜을 제조하는 것으로, 더욱 상세하게는 혈액 내에서 리포솜의 구조적인 안정성과 체내 순환시간을 증가시키기 위하여 음전하의 헤파린을 리포솜의 표면에 결합 하여 리포솜의 체내순환시간을 증가시키는 한편 항암제의 체내 독성을 감소시키고 종양 조직 내부로 약물을 효과적으로 전달 할 수 있는 효율적인 리포솜의 제조방법에 관한 것이다.
안정성, 순환시간, 리포솜, 헤파린, 친수성 고분자
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