公开(公告)号：EP0268215B1

公开(公告)日：1993-10-06

申请号：EP87116738.3

申请日：1987-11-12

申请人： LEK, tovarna farmacevtskih in kemicnih izdelkov, d.d.

发明人： Zmitek, Janko ,  Milovac, Jenny ,  Kopitar, Zdravko ,  Zorz, Mirjam ,  Rusjakovski, Boris

IPC分类号： C08B37/16 ,  A61K31/735

CPC分类号： B82Y5/00 ,  A61K31/165 ,  A61K47/6951 ,  C08B37/0015 ,  Y10S514/965

公开(公告)号：EP0551626A1

公开(公告)日：1993-07-21

申请号：EP92121410.2

申请日：1992-12-16

申请人： LEK, tovarna farmacevtskih in kemicnih izdelkov, d.d.

发明人： Kramaric, Anton ,  Resman, Aleksander ,  Kofler, Bojan ,  Zmitek, Janko

IPC分类号： A61K47/10 ,  A61K47/32 ,  A61K9/00

CPC分类号： A61K9/0014 ,  A61K9/0048 ,  A61K47/10 ,  A61K47/32 ,  A61L26/0052 ,  A61L29/085 ,  C08L71/02

摘要： There is disclosed a thermoreversible gel as a liquid pharmaceutical carrier for a galenic formulation having improved thermo-rheological properties and with a gelling temperature interval between about 25°C and 37°C, which comprises

a) 10 to 30 wt.% of block copolymers of α-hydro-ω-hydroxypoly(oxyethylene)/poly(oxypropylene)/poly(oxy-ethylene) (Poloxamer) of the formula
wherein a is at least 2 and b is at least 15 and the total portion of hydrophilic polyethylene units amounts to from 20 to 90 wt.% of the copolymer having a molecular weight from 1000 to above 16000;
b) 0.01 to 5 wt.% of carboxyvinyl polymer (carbomer) having a molecular weight from 1 x 10⁶ to 4 x 10 ⁶;
c) such an amount of a pharmaceutically acceptable base as necessary for adjusting the pH to a value between 4 and 8;
d) 20 to about 85 wt.% of water, and
e) optionally usual auxiliary agents.

There is also disclosed a liquid galenic formulation containing a therapeutically active amount of an active substance and a thermoreversible gel as a liquid pharmaceutical carrier, the active substance being selected from the group consisting of β-lactamic antibiotics and other antibacterial agents, chemotherapeutics, antiinfectives, topical anesthetics, anti-inflammatory and analgesic agents, antifungal agents, coronary vasodilators, antiviral agents, miotics and anticholinergics, mydriatic agents, antiglaucoma agents, antihistaminics, biogenic peptides and cosmetic agents.
At room temperature, such a formulation is in the sol form, which is converted into a gel form at a temperature about the body temperature and thus the application onto eye, skin and mucous membranes of the body cavities as well as the improved biopharmaceutical usefulness are made possible.

摘要翻译： 公开了一种热可逆凝胶作为具有改进的热流变性能并具有约25℃至37℃之间的胶凝温度间隔的盖仑制剂的液体药物载体，其包含a）10至30重量％的嵌段共聚物 其中a为至少2且b为至少15的α-羟基 - 羟基聚（氧乙烯）/聚（氧丙烯）/聚（氧 - 乙烯）（泊洛沙姆） 聚乙烯单元占分子量为1000至16000以上的共聚物的20至90重量％; b）0.01至5重量％的分子量为1×10 6至4×10 6的羧基乙烯基聚合物（卡波姆）; c）将pH调节至4至8之间所需的可药用碱的量; d）20至约85重量％的水，和e）任选通常的助剂。 还公开了含有治疗活性量的活性物质和作为液体药物载体的热可逆凝胶的液体盖仑制剂，活性物质选自β-乳酸抗生素和其它抗菌剂，化学治疗剂，抗感染剂， 抗炎剂和止痛剂，抗真菌剂，冠状动脉血管扩张剂，抗病毒剂，迷走神经和抗胆碱能药物，散瞳剂，抗青光眼剂，抗组胺剂，生物源性肽和化妆剂。 在室温下，这样的制剂是溶胶形式，其在约体温下被转化为凝胶形式，因此在体腔的眼睛，皮肤和粘膜上的应用以及改善的生物药物用途是 成为可能

公开(公告)号：EP0268215A1

公开(公告)日：1988-05-25

申请号：EP87116738.3

申请日：1987-11-12

申请人： LEK, tovarna farmacevtskih in kemicnih izdelkov, d.d.

发明人： Zmitek, Janko ,  Milovac, Jenny ,  Kopitar, Zdravko ,  Zorz, Mirjam ,  Rusjakovski, Boris

IPC分类号： C08B37/16 ,  A61K31/735

CPC分类号： B82Y5/00 ,  A61K31/165 ,  A61K47/6951 ,  C08B37/0015 ,  Y10S514/965

摘要： A new inclusion complex of ibuproxam with beta-cyclodextrin is described, which is prepared by adding ibuproxam to a boiling aqueous solution of beta-cyclodextrin, stirring the reaction mixture at the boiling temperature, cooling to a temperature of 0° to 5°C and isolating the title complex.
The analgesic, antipyretic and antiinflammatory propeties of the inclusion complex of ibuproxam with beta-cyclodextrin are equivalent to those of ibuproxam alone, but owing to its better water-solubility the complex can be more easily formulated into pharmaceutical forms.

摘要翻译： 与β-环糊精ibuproxam的新包合复合物所描述的，所有这些制备通过添加ibuproxam到β-环糊精的沸点wässrige溶液，在沸点温度下搅拌反应混合物，冷却至0℃的温度〜5℃，并 分离标题复杂。 止痛，解热和与β-环糊精ibuproxam的包合络合物的抗炎化子性质等同于那些单独ibuproxam的，但由于其更好的水溶性复合物可以更容易地配制成药物形式。