公开(公告)号：US4863970A

公开(公告)日：1989-09-05

申请号：US218702

申请日：1988-07-13

申请人： Dinesh C. Patel ,  Yunik Chang

发明人： Dinesh C. Patel ,  Yunik Chang

IPC分类号： A61K9/00 ,  A61K47/10 ,  A61K47/12 ,  A61K47/14

CPC分类号： A61K47/14 ,  A61K47/10 ,  A61K47/12 ,  A61K9/0014 ,  Y10S514/947

摘要： Penetration-enhancing pharmaceutical compositions for topical transepidermal and percutaneous application are disclosed which are non-irritating to the skin. These compositions are made up of a safe and effective amount of an active pharmaceutical permeant, including hydrophilic salt forms, contained in a novel penetration-enhancing vehicle comprising, (i) 1-95% w. of a cell-envelope disordering compound selected from the group consisting of oleic acid, oleyl alcohol, glycerol monoleate, glycerol dioleate, glycerol trioleate and mixtures thereof, (ii) 5-75% w., and preferably 5-49% w., of a lower alkanol selected from the group consisting of ethanol, propanol and isopropanol and mixtures thereof and (iii) 0-45% w., and preferably 1-45% w., of an inert diluent which, according to properties of the permeant used, may range from hydrophilic to hydrophobic. Water, polyethylene or polypropylene glycols and mineral oil are exemplary diluents.

摘要翻译： 公开了用于局部经皮和经皮应用的渗透增强药物组合物，其对皮肤无刺激性。 这些组合物由安全有效量的包含亲水盐形式的活性药物渗透剂组成，其包含在新的渗透增强载体中，其包含（i）1-95％w。 选自油酸，油醇，甘油单油酸酯，甘油二油酸酯，甘油三油酸酯及其混合物的细胞包膜失调化合物，（ii）5-75重量％，优选5-49重量％ 的选自乙醇，丙醇和异丙醇的低级链烷醇及其混合物，和（iii）0-45％重量，优选1-45％重量的惰性稀释剂，其根据渗透剂的性质 使用，可以从亲水到疏水。 水，聚乙烯或聚丙二醇和矿物油是示例性的稀释剂。

公开(公告)号：US4983395A

公开(公告)日：1991-01-08

申请号：US326536

申请日：1989-03-21

申请人： Yunik Chang ,  Dinesh C. Patel ,  Charles D. Ebert

发明人： Yunik Chang ,  Dinesh C. Patel ,  Charles D. Ebert

IPC分类号： A61F13/02 ,  A61K9/70

CPC分类号： A61K9/703 ,  A61K9/7084

摘要： A transdermal drug delivery device comprising a drug formulation-containing reservoir defined by a backing layer and a drug-permeable membrane layer, a peelable inner liner that underlies the reservoir and a portion of the backing/membrane outwardly of the reservoir periphery, an adhesive layer that underlies the inner liner and outwardly extending portions of the membrane/backing layers, and a peelable release liner layer that underlies the adhesive layer with a first permanent heat seal between the backing and the membrane about the perimeter of the reservoir and another concentric peelable (impermanent) heat seal between the membrane and the inner liner positioned underlying and at a radius not less than the first permanent heat seal, the heat seals and peelable barrier layer providing barriers that isolate the drug formulation from the adhesive.

摘要翻译： 一种透皮药物递送装置，其包括由背衬层和药物可渗透膜层限定的含药物制剂储存器，位于储存器下方的可剥离内衬层和位于储存器周边外部的背衬/膜的一部分，粘合剂层 位于膜/背衬层的内衬层和向外延伸部分之下的可剥离剥离衬垫层，以及位于粘合剂层下面的可剥离衬垫层，其中衬垫和膜周围围绕储存器的第一永久热密封，另一个同心可剥离（ 膜和内衬之间的热密封，其位于下方并且半径不小于第一永久热封，热密封和可剥离阻挡层提供将药物制剂与粘合剂隔离的障碍物。

公开(公告)号：US4888354A

公开(公告)日：1989-12-19

申请号：US136115

申请日：1987-12-21

申请人： Yunik Chang ,  Dinesh C. Patel

发明人： Yunik Chang ,  Dinesh C. Patel

IPC分类号： A61K9/00 ,  A61K45/06 ,  A61K47/10 ,  A61K47/14 ,  A61K47/20 ,  A61K47/22

CPC分类号： A61K45/06 ,  A61K47/10 ,  A61K47/14 ,  A61K47/20 ,  A61K47/22 ,  A61K9/0014

摘要： The invention is directed to compositions for topical application made up of active pharmaceutical permeants capable of existing in both free base and acid addition salt form. The permeants are present as a combination of both free base and acid addition salt forms. These combined forms provide skin penetration rates which are greater than the penetration rate of either the free base or acid addition salt forms utilized separately. The combined free base-acid addition salt permeants are formulated in a carrier vehicle which preferably also possesses skin penetration enhancement activity.

公开(公告)号：US4849224A

公开(公告)日：1989-07-18

申请号：US119617

申请日：1987-11-12

申请人： Yunik Chang ,  Dinesh C. Patel ,  Charles D. Ebert

发明人： Yunik Chang ,  Dinesh C. Patel ,  Charles D. Ebert

IPC分类号： A61L15/58 ,  A61K9/70 ,  A61M37/00

CPC分类号： A61K9/703 ,  A61K9/7084

摘要： A transdermal drug delivery device comprising a drug formulation-containing reservoir defined by a backing layer and a drug-permeable membrane layer, a ring-shaped layer made of an adhesive that is incompatible with one or more components of the drug formulation that is peripheral to the reservoir outwardly of the membrane layer and a peelable liner layer that underlies at least the membrane layer with a first heat seal between the backing and the membrane about the perimeter of the reservoir and another concentric heat seal between the backing and the release liner positioned outwardly of the first heat seal, the heat seals providing barriers that isolate the drug formulation from the adhesive.

公开(公告)号：US20050032895A1

公开(公告)日：2005-02-10

申请号：US10495889

申请日：2002-11-18

申请人： Yunik Chang ,  Robert Lathrop ,  Erwin Bohm ,  Irene Gander-Meisterernst ,  Ulrich Moebius ,  Johanna Holldack ,  Ulrich Moebius

发明人： Yunik Chang ,  Robert Lathrop ,  Erwin Bohm ,  Irene Gander-Meisterernst ,  Ulrich Moebius ,  Johanna Holldack ,  Ulrich Moebius

IPC分类号： A61K31/12 ,  A61K31/20 ,  A61K31/23 ,  A61K31/25 ,  A61K31/353 ,  A61K36/18 ,  A61K45/00 ,  A61K45/06 ,  A61K47/06 ,  A61K47/10 ,  A61K47/14 ,  A61P15/00 ,  A61P17/00 ,  A61P17/12 ,  A61P31/12 ,  A61P31/20 ,  A61P31/22

CPC分类号： A61K9/0014 ,  A61K31/23 ,  A61K31/353 ,  A61K47/06 ,  A61K47/10 ,  A61K47/14 ,  Y10S514/934 ,  Y10S514/947 ,  Y10S514/967 ,  Y10S514/969 ,  A61K2300/00

摘要： The invention relates to a medicament containing a compound of general formula (1), where R1=independently, a straight or branched, saturated, singly- or multiply-unsaturated, optionally substituted C11-C21 alkyl, alkylene or alkinyl group, preferably a C11-C15 alkyl, alkylene or alkinyl group, particularly a C11-C13 alkyl, alkylene or alkinyl group, most preferably a C13 alkyl group, R2=independently, a straight or branched C1-C8 alkyl, alkylene or alkinyl group, preferably a C1-C6 alkyl, alkylene or alkinyl group, in particular a C2-C4 alkyl, alkylene or alkinyl group, most preferably a C3 alkyl group, a —[CH2—(CH2)m—O]nH group with n=1 to 10, preferably n=1 to 5, m==1 to 5, preferably m=1 to 3, a —CH2—[CH—(OH)]p[CH2-(R3)]— group, where R3=independent H or OH, p=1 to 7, preferably p=1 to 4, a pentose group or a hexose group, as therapeutically active agent, alone or in combination with one or several further pharmaceutical agents as a combination preparation for the treatment of viral skin diseases and/or tumour diseases, in particular caused by human papilloma virus (HPV) and/or herpes viruses and a topically acting medicament formulation and the use thereof.

摘要翻译： 本发明涉及含有通式（1）化合物的药物，其中R1独立地为直链或支链的饱和的，单或多不饱和的任选取代的C 11 -C 21烷基，亚烷基或炔基，优选C 11 -C 15烷基，亚烷基或炔基，特别是C 11 -C 13烷基，亚烷基或炔基，最优选C 13烷基，R 2独立地为直链或支链C 1 -C 8烷基，亚烷基或炔基，优选C1- C 1 -C 6烷基，亚烷基或炔基，特别是C 2 -C 4烷基，亚烷基或炔基，最优选C 3烷基， - n = 1-10的α-[CH 2 - （CH 2）m O] n H基，优选n = 1〜5，m = 1〜5，优选m = 1〜3，-CH 2 - [CH-（OH）] p [CH 2 - （R 3）] - 基，其中R 3 =独立的H或OH，p = 1至7，优选p = 1至4，戊糖基或己糖基团，作为治疗活性剂，单独或与一种或几种其它药剂组合，作为用于治疗病毒的组合制剂 特别是由人乳头瘤病毒（HPV）和/或疱疹病毒引起的皮肤疾病和/或肿瘤疾病以及局部作用的药物制剂及其用途。

公开(公告)号：US20090306172A1

公开(公告)日：2009-12-10

申请号：US12455525

申请日：2009-06-03

申请人： Yunik Chang ,  Gordon J. Dow

发明人： Yunik Chang ,  Gordon J. Dow

IPC分类号： A61K31/4025 ,  A61K31/327 ,  A61P17/10

CPC分类号： A61K31/7056 ,  A61K8/0241 ,  A61K8/042 ,  A61K8/044 ,  A61K8/345 ,  A61K8/38 ,  A61K8/55 ,  A61K9/0014 ,  A61K9/14 ,  A61K31/075 ,  A61K31/235 ,  A61K31/327 ,  A61K45/06 ,  A61K47/10 ,  A61K47/32 ,  A61K2800/33 ,  A61K2800/413 ,  A61Q19/00 ,  A61K2300/00

摘要： An aqueous formulation for topical application to the skin comprising water, a water-miscible organic solvent, and benzoyl peroxide, wherein the concentration of the organic solvent is sufficient to provide a stable suspension of benzoyl peroxide in the aqueous formulation without the inclusion of a surfactant in the formulation, wherein the ratio of concentrations of water and organic solvent in the formulation is sufficient to maintain the benzoyl peroxide in saturated solubility in the formulation following application to the skin, and wherein the concentration of benzoyl peroxide in the formulation is less than 5.0% and at least 1.0% w/w. The formulation may further contain a chemical compound in addition to benzoyl peroxide that is effective in the treatment of acne. The aqueous formulations of the invention are useful in the treatment of acne and acne rosacea.

摘要翻译： 用于局部施用于皮肤的水性制剂，包括水，水混溶性有机溶剂和过氧化苯甲酰，其中有机溶剂的浓度足以提供过氧化苯甲酰在水性制剂中的稳定悬浮液，而不包含表面活性剂 在制剂中，其中制剂中水和有机溶剂的浓度的比例足以在施用于皮肤后将过氧化苯甲酰保持在制剂中饱和溶解度，并且其中制剂中过氧化苯甲酰的浓度小于5.0 ％和至少1.0％w / w。 制剂还可以含有除了过氧化苯甲酰之外的化学化合物，其有效治疗痤疮。 本发明的水性制剂可用于治疗痤疮和痤疮性红斑痤疮。

公开(公告)号：US06881726B2

公开(公告)日：2005-04-19

申请号：US10033835

申请日：2001-12-24

申请人： Yunik Chang ,  Gordon J. Dow

发明人： Yunik Chang ,  Gordon J. Dow

IPC分类号： C07D233/94 ,  A61K9/06 ,  A61K9/08 ,  A61K31/415 ,  A61K31/4164 ,  A61K31/455 ,  A61K31/724 ,  A61K47/10 ,  A61K47/22 ,  A61K47/38 ,  A61K47/40 ,  A61P17/00 ,  A61P17/02 ,  A61P31/04 ,  A61P33/00 ,  C08B37/00 ,  A61K31/40

CPC分类号： A61K9/0014 ,  A61K9/06 ,  A61K31/4164 ,  A61K31/724 ,  A61K47/10 ,  A61K47/38 ,  A61K47/40 ,  A61K47/6951 ,  B82Y5/00 ,  C08B37/0015 ,  C08J3/075 ,  C08J2301/02 ,  C08J2305/16 ,  C08L5/16 ,  A61K2300/00

摘要： An aqueous solution of metronidazole in which the concentration of metronidazole is higher than 0.75%. The solution contains a combination of solubility-enhancing agents, one of which is a cyclodextrin such as beta-cyclodextrin and the second is a compound other than a cyclodextrin. Methods of manufacture and therapeutic use of the solution are disclosed.

摘要翻译： 甲硝唑浓度高于0.75％的甲硝唑水溶液。 该溶液含有溶解度增强剂的组合，其中之一是环糊精如β-环糊精，第二种是环糊精以外的化合物。 公开了制备和治疗用途的方法。

公开(公告)号：US4956171A

公开(公告)日：1990-09-11

申请号：US384342

申请日：1989-07-21

申请人： Yunik Chang

发明人： Yunik Chang

IPC分类号： A61K9/00 ,  A61K9/70 ,  A61K47/14 ,  A61K47/26

CPC分类号： A61K9/7053 ,  A61K47/14 ,  A61K47/26 ,  A61K9/0014 ,  A61K9/7061 ,  A61K9/7084 ,  Y10S514/946

摘要： A transdermal drug delivery system with a dual permeation enhancer is described. The transdermal system comprises a body that contains supplies of drug and a dual permeation enhancer comprising sucrose cocoate and methyl laurate, and has a basal surface that contacts an area of skin and transmits the drug and the dual permeation enhancer to the area for absorption thereby. A method for coadministering a drug and a dual permeation enhancer comprising sucrose cocoate and methyl laurate is also described.

摘要翻译： 描述了具有双重渗透增强剂的透皮药物递送系统。 透皮系统包括含有药物供应的身体和包含蔗糖椰子酸酯和月桂酸甲酯的双重渗透增强剂，并且具有接触皮肤区域的基底表面，并将药物和双重渗透促进剂传递到用于吸收的区域。 还描述了一种共纳入药物和包含蔗糖椰子酸酯和月桂酸甲酯的双重渗透增强剂的方法。

公开(公告)号：US20110009481A1

公开(公告)日：2011-01-13

申请号：US12887250

申请日：2010-09-21

申请人： Yunik Chang ,  Robert Lathrop ,  Erwin Böhm ,  Irene Gander-Meisterernst ,  Regina Greger ,  Johanna Holldack ,  Ulrich Moebius

发明人： Yunik Chang ,  Robert Lathrop ,  Erwin Böhm ,  Irene Gander-Meisterernst ,  Regina Greger ,  Johanna Holldack ,  Ulrich Moebius

IPC分类号： A61K31/353 ,  A61P35/00 ,  A61P17/00

CPC分类号： A61K9/0014 ,  A61K31/23 ,  A61K31/353 ,  A61K47/06 ,  A61K47/10 ,  A61K47/14 ,  Y10S514/934 ,  Y10S514/947 ,  Y10S514/967 ,  Y10S514/969 ,  A61K2300/00

摘要： The invention relates to a medicament containing a compound of general formula (I), where R1=independently, a straight or branched, saturated, singly- or multiply-unsaturated, optionally substituted C11-C21 alkyl, alkylene or alkinyl group, preferably a C11-C15 alkyl, alkylene or alkinyl group, particularly a C11-C13 alkyl, alkylene or alkinyl group, most preferably a C13 alkyl group, R2=independently, a straight or branched C1-C8 alkyl, alkylene or alkinyl group, preferably a C1-C6 alkyl, alkylene or alkinyl group, in particular a C2-C4 alkyl, alkylene or alkinyl group, most preferably a C3 alkyl group, a —[CH2—(CH2)m-O]nH group with n=1 to 10, preferably n=1 to 5, to m=1 to 5, preferably m=1 to 3, a —CH2—[CH—(OH)]p[CH2—R3]- group, where R3=independently H or OH, p=1 to 7, preferably p=1 to 4, a pentose group or a hexose group, as therapeutically active agent, alone or in combination with one or several further pharmaceutical agents as a combination preparation for the treatment of viral skin diseases and/or tumor diseases, in particular caused by human papilloma virus (HPV) and/or herpes viruses and a topically acting medicament formulation and the use thereof.

摘要翻译： 本发明涉及含有通式（I）化合物的药物，其中R 1独立地为直链或支链的，饱和的，单或多不饱和的任选取代的C 11 -C 21烷基，亚烷基或炔基，优选C 11 -C 15烷基，亚烷基或炔基，特别是C 11 -C 13烷基，亚烷基或炔基，最优选C 13烷基，R 2独立地为直链或支链C 1 -C 8烷基，亚烷基或炔基，优选C1- C 1 -C 6烷基，亚烷基或炔基，特别是C 2 -C 4烷基，亚烷基或炔基，最优选C 3烷基， - n = 1-10的α-[CH 2 - （CH 2）m O] n H基，优选n = 1至5，m = 1至5，优选m = 1至3，-CH 2 - [CH-（OH）] p [CH 2 -R 3] - 基，其中R 3独立地为H或OH，p = 7，优选p = 1〜4，戊糖基或己糖基作为治疗活性剂，单独或与一种或几种其它药剂组合，作为tre的组合制剂 特别是由人乳头瘤病毒（HPV）和/或疱疹病毒和局部作用的药物制剂引起的病毒性皮肤病和/或肿瘤疾病的发生及其用途。

公开(公告)号：US20080154030A1

公开(公告)日：2008-06-26

申请号：US12072578

申请日：2008-02-27

申请人： Yunik Chang ,  Gordon J. Dow

发明人： Yunik Chang ,  Gordon J. Dow

IPC分类号： C08B37/16

CPC分类号： A61K9/0014 ,  A61K9/06 ,  A61K31/4164 ,  A61K31/724 ,  A61K47/10 ,  A61K47/38 ,  A61K47/40 ,  A61K47/6951 ,  B82Y5/00 ,  C08B37/0015 ,  C08J3/075 ,  C08J2301/02 ,  C08J2305/16 ,  C08L5/16 ,  A61K2300/00

摘要： The solubility of betacyclodextrin in aqueous fluid is increased by combining niacin or niacinamide in the aqueous fluid with the betacyclodextrin.

摘要翻译： 通过将含水流体中的烟酸或烟酰胺与betacyclodextrin组合，可以增加betacyclodextrin在水性液体中的溶解度。