CN1161435C - 亲水性胶粘物 - Google Patents
亲水性胶粘物 Download PDFInfo
- Publication number
- CN1161435C CN1161435C CNB991085043A CN99108504A CN1161435C CN 1161435 C CN1161435 C CN 1161435C CN B991085043 A CNB991085043 A CN B991085043A CN 99108504 A CN99108504 A CN 99108504A CN 1161435 C CN1161435 C CN 1161435C
- Authority
- CN
- China
- Prior art keywords
- paste
- acid
- methyl
- wetting ability
- agent
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Expired - Lifetime
Links
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- -1 aluminum compound Chemical class 0.000 claims description 47
- 238000009736 wetting Methods 0.000 claims description 29
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 15
- 239000002253 acid Substances 0.000 claims description 14
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- RUJUQAPQALJUPC-UHFFFAOYSA-K bis[(2-aminoacetyl)oxy]alumanyl 2-aminoacetate Chemical compound [Al+3].NCC([O-])=O.NCC([O-])=O.NCC([O-])=O RUJUQAPQALJUPC-UHFFFAOYSA-K 0.000 description 3
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Abstract
一种亲水性胶粘物含有0.05-10%重量(甲基)丙烯酸氨基烷基酯和(甲基)丙烯酸烷基酯的共聚物。这种亲水性胶粘物的粘结性优异，特别是当与药理活性成分组合时，适合用于形成亲水性膏剂。
Description
本发明涉及亲水性胶粘物和亲水性膏剂，特别是粘结性强和用感优良的亲水性胶粘物以及使用这种胶粘物的亲水性膏剂。
含有作为外用制剂铺展在衬材上的亲水性胶粘物的各种亲水性膏剂已使用多年。这些亲水性膏剂必须与皮肤牢固粘合，在使用过程中不分离。
已知常规的膏剂包括由聚丙烯酸、聚丙烯酸盐、羧甲基纤维素和碱金属藻酸盐组成的非明胶类泥敷剂(JP 59-110617)；由粘度为100-1000厘泊的聚丙烯酸10％水溶液、一种水溶性高聚物、一种多元醇和水组成的经皮制剂(JP 6-135828A)；由N-乙烯基乙酰胺-丙烯酸钠共聚物、水溶性铝盐和水组成的含水凝胶膏剂(JP-143060A)；和加有聚丁烯及明胶的泥敷剂(JP 9-208462A)。但它们都有这样或那样的问题，例如粘结性不足和/或工业生产困难。
因此，长久以来都希望能提供一种具有充分粘结性的亲水性胶粘物。
基于上述的目前状况，本发明人进行了广泛的研究。结果发现，一种含有特定比例(甲基)丙烯酸氨基烷基酯和(甲基)丙烯酸烷基酯的共聚物的亲水性胶粘物对皮肤有优异的粘结性，而且用感良好，这样就完成了本发明。
本发明的一个方面是提供了一种亲水性胶粘物，其中含有0.05-10％重量的(甲基)丙烯酸氨基烷基酯和(甲基)丙烯酸烷基酯的共聚物。
在本发明的另一方面，还提供了一种亲水性膏剂，该膏剂包括一种衬材和铺展在该衬材上的由上述亲水性胶粘物和至少一种药理活性成分形成的糊状物。
本发明的亲水性胶粘物和亲水性膏剂对皮肤有很强的粘结性，而且用感良好。
对于作为制备用于本发明的共聚物的单体之一的(甲基)丙烯酸氨基烷基酯，没有特别的限制。不过，其中含有叔胺或季铵盐作为分子中胺部分者是优选的实例。含有叔胺作为分子中胺部分的实例包括(甲基)丙烯酸二甲基氨基乙酯，(甲基)丙烯酸二乙基氨基乙酯，(甲基)丙烯酸二丁基氨基乙酯，(甲基)丙烯酸吗啉代乙酯，(甲基)丙烯酸哌啶子基乙酯，(甲基)丙烯酸二甲基氨基-2-丙基酯，以及(甲基)丙烯酸二甲基氨基新戊酯。
另一方面，含有季铵盐作为分子中胺部分的实例包括(甲基)丙烯酸三甲基铵乙酯，(甲基)丙烯酸三乙基铵乙酯，(甲基)丙烯酸三丁基铵乙酯，(甲基)丙烯酸三吗啉代铵乙酯，(甲基)丙烯酸三哌啶子基铵乙酯，(甲基)丙烯酸三甲基铵-2-丙酯，以及(甲基)丙烯酸三甲基铵新戊酯。另外，分子中的叔胺部分可以用盐酸或类似物质转化成相应的季铵盐部分。作为(甲基)丙烯酸氨基烷基酯，特别优选的是(甲基)丙烯酸二甲基氨基乙酯或氯化的(甲基)丙烯酸三甲基铵乙酯(chlorinated trimethylammoniumethyl(meth)acrylate)。
对于作为构成共聚物另一单体的(甲基)丙烯酸烷基酯，没有特别的限制。但是，优选的实例包括(甲基)丙烯酸甲酯，(甲基)丙烯酸乙酯，(甲基)丙烯酸正丁酯，(甲基)丙烯酸正己酯，(甲基)丙烯酸正辛酯，(甲基)丙烯酸2-乙基己基酯以及(甲基)丙烯酸正十二烷基酯。它们可以单独使用或组合使用。特别适用的是(甲基)丙烯酸甲酯，(甲基)丙烯酸乙酯和(甲基)丙烯酸正丁酯。
共聚物可以是无规的、交替共聚、嵌段和接枝结构中的任何一种，但优选是嵌估共聚物。
特别优选用于本发明的共聚物的实例包括(甲基)丙烯酸二甲基氨基乙酯、(甲基)丙烯酸甲酯和(甲基)丙烯酸丁酯的嵌段共聚物；以及氯化的(甲基)丙烯酸三甲基铵乙酯、(甲基)丙烯酸甲酯和(甲基)丙烯酸乙酯的嵌段共聚物。
可以使用商业产品作为用于本发明的共聚物。这类商业产品的例子有“EUDRAGIT RL 12，5”，“EUDRAGIT RL 100”，“EUDRAGITRL PO，”，“EUDRAGIT RL 30 D”，“EUDRAGIT RS 12，5”，“EUDRAGIT RS 100”，“EUDRAGIT RS PO，”，“EUDRAGIT RS30 D”，“EUDRAGIT E 12，5”，“EUDRAGIT E 100”，“PLASTOIDE 35 L”，“PLASTOID E 35 M”，“PLASTOID E 35 H”和“PLASTOID L 50”(全是Rhm AG的产品)。
用在本发明中的共聚物的比例优选为亲水性胶粘物总重量的0.05-10％，更优选为0.1-6％，特别优选为0.2-4％。比例小于0.05％难以得到高的粘结性，而比例大于10％不能产生额外的改进粘结性的效果，因此是不经济的。
本发明的亲水性胶粘物的粘结性可以通过在上述共聚物之外再掺入亲水性粘结剂来进一步改进。这类亲水性粘结剂的实例有：聚丙烯酸及其盐，例如聚丙烯酸、聚丙烯酸钠、交联的支化聚丙烯酸、交联的支化聚丙烯酸钠、聚丙烯酸钾、聚丙烯酸单乙醇胺、聚丙烯酸二乙醇胺、聚丙烯酸三乙醇胺和聚丙烯酸铵；用丙烯酸或其盐作为组分之一得到的共聚物，例如淀粉接枝丙烯酸酯，和N-乙烯基乙酰胺-丙烯酸钠共聚物；纤维素衍生物及其盐，例如羟乙基纤维素、羟丙基纤维素、羟丙基甲基纤维素、疏水化的羟丙基甲基纤维素、甲基纤维素和羧甲基纤维素钠；聚乙烯醇；聚乙烯吡咯烷酮；聚氧乙烯；甲氧基亚乙基-马来酸酐共聚物；聚丙烯酰胺；海藻酸；海藻酸钠；海藻酸丙二醇酯；明胶；阿拉伯胶；黄蓍胶；槐树豆胶；瓜尔胶；罗望果籽胶；黄原胶；洁冷胶；角叉胶；和琼脂。其中，特别优选聚丙烯酸、聚丙烯酸钠、交联接枝的聚丙烯酸、交联接枝的聚丙烯酸钠、淀粉接枝的丙烯酸酯、N-乙烯基乙酰胺-丙烯酸钠共聚物、羟乙基纤维素、羟丙基纤维素、羟丙基甲基纤维素、疏水羟丙基甲基纤维素和羧甲基纤维素钠。这些亲水性粘结剂可以单独使用或者组合使用。它们的比例可以为胶粘物总重量的0.5-50％，优选2-40％，特别优选为3-30％。
在本发明中，还优选使用共聚物增溶剂以便将(甲基)丙烯酸氨基烷基酯与(甲基)丙烯酸烷基酯的共聚物溶解。对于这种共聚物增溶剂没有特殊的限制，只要它能够溶解该共聚物并且是药学上可接受的。例如，可以使用选自多元醇、脂肪酸酯、表面活性剂、脂肪酸、醇类和烃类的一种或多种物质。具体的实例包括：多元醇，如1，3-丁二醇、丙二醇和二丙二醇；脂肪酸酯，如己二酸二丁酯、己二酸二异丙酯、癸二酸二乙酯、癸二酸二异丙酯、肉豆蔻酸异丙酯、棕榈酸异丙酯、乳酸十六烷基酯、乳酸十四烷基酯、亚油酸乙酯、亚油酸异丙酯、丙二醇油酸酯、丙二醇单辛酸酯、丙二醇二辛酸酯及丙二醇双十二烷酸酯；表面活性剂，如聚氧乙烯十二烷基醚，聚氧乙烯十六烷基醚，聚氧乙烯油基醚和十二烷基二乙醇酰胺；脂肪酸，如乳酸、月桂酸、油酸、亚油酸；作为醇，如乙醇、异丙醇、月桂醇、油醇、苯甲醇、苯乙醇和薄荷醇；以及烃类，如液体石蜡和角鲨烷。这些共聚物增溶剂在亲水性胶粘物中的加入量优选为0.5-70％重量，更优选为1-60％，特别优选为5-50％。
在本发明的亲水性胶粘物中，还可以加入经皮渗透促进剂、交联剂和湿润剂。它们可以单独加入或者组合加入。
用于促进活性成分经皮渗透的经皮渗透促进剂包括已知的经皮渗透促进剂，例如脂肪酸，脂肪酸酯，多元醇，醇，表面活性剂，有机碱，有机酸，维生素和卵磷脂。
对于交联剂的种类没有特别的限制，只要它可以将亲水性胶粘剂交联。但是，特别优选多价的金属化合物。作为这类多价金属化合物，特别优选铝化合物、镁化合物和钙化合物。
铝化合物、镁化合物和钙化合物的实例包括硫酸铝钾、硫酸铝铵、氢氧化铝、硫酸铝、氯化铝、甘氨酸二羟铝、乙酰谷氨酰胺铝、乙酸铝、氧化铝、合成的硅酸铝、偏硅酸铝、氢氧化钙、碳酸钙、硫酸钙、硝酸钙、氯化钙、乙酸钙、氧化钙、磷酸钙、氢氧化镁、碳酸镁、硫酸镁、乙酸镁、硅酸镁、氧化镁、氢氧化镁-氢氧化铝共沉淀剂、偏硅酸铝镁、硅酸铝酸镁和合成的水滑石；以及这些化合物的水合物和脱水物。这些化合物可以单独使用或者组合使用。交联剂比例宜为0.001-10％重量，优选为0.01-5％重量，更优选为0.1-2％，但要随化合物的种类而变。
对于湿润剂没有特别的限制，只要它是通常所使用的。湿润剂的实例有浓甘油、木糖醇、山梨醇、麦芽糖醇、吡咯烷酮羧酸、吡咯烷酮羧酸钠、乳酸钠、透明质酸、透明质酸钠和尿素。其比例优选为5-40％重量。
本发明的亲水性胶粘物可以含有1-85％重量的水，优选含5-70％重量的水，更优选含15-60％重量的水。
这种亲水性胶粘物可以不特地加入药理活性成分而原样使用，例如，作为冷却局部热度的糊剂或作为支承物受压的。或者是，可以向亲水性胶粘物中加入一种或多种药理活性成分以形成亲水性膏剂。以下药物是可作为用于制造亲水性膏剂的药理活性成分的实例。
止痛消炎药：作为非甾类止痛消炎药，有乙二醇水杨酸酯、水杨酸甲酯、阿氯芬酸、ufenamate、噻吩甲酰布洛芬、丁苯羟酸、炎痛喜康、meloxicam、消炎痛、酮基布洛芬、扎托洛芬、舒林酸、替诺西康、扑热息痛、甲苄氨茴酸、氟芬那酸、布洛芬、洛索丙普钠、普拉洛芬、芬布芬、双氯酚酸、双氯酚酸钠、羟基保泰松、联苯乙酸和氟比洛芬；作为甾类止痛消炎药，有amcinonide、强的松龙戊酸醋酸酯、双氟皮甾松戊酸酯、缬草酸地塞米松、戊酸倍他米松、醋酸二氟松、醋酸氟美松、醋酸氢化可地松、醋酸甲基氢化泼尼松、醋丁二氟龙、二丙酸倍他米松、地塞米松、醋酸曲安缩松、氯氟舒松、特戊酸二氟美松、布地缩松、呋喃羧酸莫米他松、氟轻松、醋酸氟轻松、丙酮缩氟氢羟龙、泼尼松龙、丙酸别氯地米松、丙酸氯氟米松、丙酸钙地塞米松、丙酸地泼罗酮、丙酸倍氯米松、倍他米松、丁酸氯氟美松酮、氢化可的松丁酸酯、丁酸丙酸氢化可的松以及丁酸丙酸倍他米松。
抗真菌剂：盐酸氯康唑，盐酸萘替康唑，克霉唑，酮康唑，硝酸异康唑，益康唑，硝酸羟康唑，硝酸硫康唑，硝酸咪康唑，thioconazole，bifenazole和lanoconazole。
抗尿失禁药：盐酸羟丁宁，盐酸双苯丁胺和盐酸黄酮哌酯。
骨骼肌肉松弛剂：盐酸乙苯哌丁酮，氟喹酮，氨甲酸氯苯甘油醚，盐酸替扎尼定，盐酸甲哌酮，甲噁安定，盐酸氟胺安定，安定，环丙安定，氟硝安定，氟胺安定，溴替唑仑，溴吡二氮，氯唑沙宗，苯丙醇胺酯，舒筋灵，硝苯呋海因钠和甲磺酸哌二苯丙醇。
解痉药：丁溴东莨菪碱，硫酸阿托品，盐酸罂粟碱。
强心剂：硝酸甘油和消心痛。
戒烟剂：尼古丁。
抗过敏剂：盐酸氮斯丁，盐酸依匹那丁，苯咪唑嗪，serotrodast，利喘平和酮替芬。
局部麻醉药：盐酸普鲁卡因，盐酸待布卡因和利多卡因。
防腐消毒药：碘，碘酊，碘仿和聚乙烯吡咯烷酮碘。
皮肤刺激剂：辣椒辣素，辣椒提取物和4-羟基-3-甲氧基苄基壬酰胺。
应该指出，用于本发明亲水性膏剂中的药理活性成分不限于上面列举的这些。这些药理活性成分根据需要可以单独使用或组合使用。
在本发明的亲水性胶粘物中和用在本发明亲水性胶粘物中的糊剂中，可以掺入通常加到亲水性胶粘物和类似物中的添加剂，上述的亲水性胶粘物和糊剂以后统称为“亲水性胶粘物”。例如，作为交联速度调节剂，可以加入螯合剂如乙二胺四乙酸钠和偏磷酸钠，有机酸如乳酸、柠檬酸和酒石酸，这些有机酸的金属盐，无机酸如硫酸和盐酸，有机碱如二乙胺、二乙醇胺、三乙醇胺和二异丙醇胺，无机碱如氢氧化钠和氨；作为填料，可以加入高岭土，二氧化钛，轻质二氧化硅和疏水性轻质二氧化硅；作为抗氧化剂，可以加入亚硫酸盐如无水亚硫酸钠、亚硫酸氢钠、焦亚硫酸钠和硫代硫酸钠，雕白粉，乙二胺四乙酸钠，二丁基羟基甲苯和二丁基羟基苯甲醚。此外，根据需要还可以加入表面活性剂、香料、防腐剂、pH调节剂等。
对于本发明的亲水性胶粘物的制造方法没有特别的限制，可以使用常规的亲水性胶粘物或亲水性膏剂的制造方法。例如，在本发明的亲水性膏剂的情形，将上述的基本成分和必要时的其它成分在水中混合，随后充分捏合直到形成均匀的糊状物。将该糊状物铺展在诸如纸张、纺织品、无纺布或塑料薄膜等衬材上，如果需要，再盖上聚乙烯薄膜或类似物。
下面将利用实施例说明本发明。但是应该指出，本发明决不受这些
实施例的限制。
实施例1
按照以下制造方法制造亲水性膏剂，该膏剂含有表1中所列成分的亲水性胶粘物。
(制造方法)
(A)将聚氧乙烯(9)十二烷基醚和一部分丙二醇充分混合成紧密混合物，加入双氯高灭酸钠、“EUDRAGIT RL PO”和L-薄荷醇使其溶于混合物中。(B)将高岭土和乙二胺四乙酸钠分散在纯化水和D-山梨醇溶液(70％)的液体混合物中。(C)将聚丙烯酸钠、羧甲基纤维素钠和干燥的硫酸铝钾均匀地分散在剩余部分的丙二醇和浓甘油的液体混合物中。将这样得到的溶液(A)和分散体(B)、(C)装入捏合机中并在其中搅拌。再加入酒石酸，将所形成的混合物充分搅拌直到形成均匀的糊状物，从而制得亲水性胶粘物。将其均匀地铺展在无纺布上，得到带有亲水性胶粘物的亲水性膏剂。
试验1
将上面制造的亲水性膏剂敷贴到志愿者的肘部，进行器官感觉人类皮肤粘结性试验。
(试验方法)
将这样得到的各膏剂的样品分别敷贴在20名志愿者的肘部，8小时后撕下膏剂样品。
按照以下分级系统对粘结度定级。结果也列在表1中。
分级系统(器官感觉人类皮肤粘结性试验)
A：强(在试验期间保持牢固粘合)。
B：稍弱(试验期间发生部分剥离)。
C：弱(试验期间脱离)。
表1
| 组分(wt.％) | 本发明产品 | 对照产品 | |||||||||||
| 1 | 2 | 3 | 4 | 5 | 6 | 7 | 8 | 9 | 10 | 1 | 2 | 3 | |
| 双氯高灭酸钠聚氧乙烯(9)十二烷基醚L-薄荷醇丙二醇浓甘油D-山梨醇溶液(70％)聚丙烯酸钠羧甲基纤维素钠EUDRAGIT RL PO高岭土乙二胺四乙酸钠干燥的硫酸铝钾酒石酸纯水总量(wt.％) | 1.001.000.505.0015.0030.005.002.000.053.000.050.500.1036.80100.00 | 1.001.000.505.0015.0030.005.002.000.103.000.050.500.1036.75100.00 | 1.001.000.505.0015.0030.005.002.000.203.000.050.500.1036.65100.00 | 1.001.000.505.0015.0030.005.002.000.503.000.050.500.1036.35100.00 | 1.001.000.505.0015.0030.005.002.001.003.000.050.500.1035.85100.00 | 1.001.000.505.0015.0030.005.002.002.003.000.050.500.1034.85100.00 | 1.001.000.505.0015.0030.005.002.003.003.000.050.500.1033.85100.00 | 1.001.000.505.0015.0030.005.002.004.003.000.050.500.1032.85100.00 | 1.001.000.505.0015.0030.005.002.005.003.000.050.500.1031.85100.00 | 1.001.000.505.0015.0030.005.002.006.003.000.050.500.1030.85100.00 | 1.001.000.505.0015.0030.005.002.003.000.050.500.1036.85100.00 | 1.001.000.505.0015.0030.005.002.000.013.000.050.500.1036.84100.00 | 1.001.000.505.0015.0030.005.002.000.043.000.050.500.1036.81100.00 |
| 器官感觉人类皮肤粘结性试验 | A | A | A | A | A | A | A | A | A | A | C | C | B |
由表1所列的试验1的结果显然可见，本发明的含有本发明亲水性胶粘物的亲水性膏剂(本发明产品1-10)，与对照产品1-3不同，在预定时间内保持对皮肤的强粘结性。对照产品在预定时间内或是脱落，或是部分剥离，不能提供强粘结性。
实施例2
带有列在表2中的亲水性胶粘物的亲水性膏剂按照与实施例1中本发明产品1-6的同样方式制造，只是将“EUDRAGIT RL PO”换成“EUDRAGIT E 100”。器官感觉人类皮肤粘结性试验也按照与试验1相同的方式进行。试验结果也列在表2中。
表2
| 组分(wt.％) | 本发明产品 | 对照产品 | |||||
| 11 | 12 | 13 | 14 | 15 | 16 | 4 | |
| 双氯高灭酸钠聚氧乙烯(9)十二烷基醚L-薄荷醇丙二醇浓甘油D-山梨醇溶液(70％)聚丙烯酸钠羧甲基纤维素钠EUDRAGIT E 100高岭土乙二胺四乙酸钠干燥的硫酸铝钾酒石酸纯化水总量(wt.％) | 1.001.000.505.0015.0030.005.002.000.053.000.050.500.1036.80100.00 | 1.001.000.505.0015.0030.005.002.000.103.000.050.500.1036.75100.00 | 1.001.000.505.0015.0030.005.002.000.203.000.050.500.1036.65100.00 | 1.001.000.505.0015.0030.005.002.000.503.000.050.500.1036.35100.00 | 1.001.000.505.0015.0030.005.002.001.003.000.050.500.1035.85100.00 | 1.001.000.505.0015.0030.005.002.002.003.000.050.500.1034.85100.00 | 1.001.000.505.0015.0030.005.002.003.000.050.500.1036.85100.00 |
| 器官感觉人类皮肤粘结性试验 | A | A | A | A | A | A | C |
带有本发明亲水性胶粘物的本发明的亲水性膏剂(本发明产品11-16)显示出强粘结性。
实施例3
制备带有表3和表4中所列成分的亲水性胶粘物的亲水性膏剂。
表3
| 组分(wt.％) | 本发明产品 | |||||
| 17 | 18 | 19 | 20 | 21 | 22 | |
| 双氯高灭酸钠炎痛喜康Meloxicam盐酸萘替康唑盐酸羟丁宁盐酸乙哌立松硝酸甘油尼古丁苯咪唑嗪利多卡因己二酸二异丙酯癸二酸二乙酯癸二酸二异丙酯聚氧乙烯(9)十二烷基醚聚氧乙烯(10)油基醚乳酸十四烷基酯油酸苯甲醇角鲨烷L-薄荷醇丙二醇浓甘油 | 1.002.501.0010.00 | 1.004.005.001.0040.0020.00 | 1.001.000.5010.0015.00 | 0.501.005.000.5020.00 | 0.505.005.000.5010.0020.00 | 1.002.502.5025.00 |
表3(续)
| 组分(wt.％) | 本发明产品 | |||||
| 17 | 18 | 19 | 20 | 21 | 22 | |
| D-山梨醇溶液(70％)聚丙烯酸聚丙烯酸钠交联的支化聚丙烯酸N-乙烯乙酰胺/丙烯酸钠共聚物羟丙基纤维素疏水化的羟丙基甲基纤维素羧甲基纤维素钠聚乙烯基吡咯烷酮EUDRAGIT RL POEUDRAGIT E 100高岭土轻质二氧化硅乙二胺四乙酸钠干燥的硫酸铝钾甘氨酸铝合成的羟基水滑石酒石酸三乙醇胺纯化水总量(wt.％)物料重量(g/m2) | 3.004.001.000.150.357.0070.00100.001000 | 3.001.002.000.300.0122.69100.00200 | 1.005.001.000.105.000.050.250.1060.00100.001000 | 20.005.001.003.000.505.000.052.000.3036.15100.001000 | 20.005.001.001.003.002.000.050.450.3026.20100.001000 | 30.001.005.000.200.502.000.200.050.012.0028.94100.00200 |
表4
| 组分(wt.％) | 本发明产品 | |||||
| 23 | 24 | 25 | 26 | 27 | 28 | |
| 双氯高灭酸钠炎痛喜康Meloxicam盐酸萘替康唑盐酸羟丁宁盐酸乙哌立松硝酸甘油尼古丁苯咪唑嗪利多卡因己二酸二异丙酯癸二酸二乙酯癸二酸二异丙酯聚氧乙烯(9)十二烷基醚聚氧乙烯(10)油基醚乳酸十四烷基酯油酸苯甲醇角鲨烷L-薄荷醇丙二醇浓甘油 | 1.505.005.000.5040.0025.00 | 0.505.005.0010.0010.00 | 0.101.0020.0040.00 | 0.100.5020.00 | 2.005.005.0010.0020.00 | 2.002.502.5040.0015.00 |
表4(续)
| 组分(wt.％) | 本发明产品 | |||||
| 23 | 24 | 25 | 26 | 27 | 28 | |
| D-山梨醇溶液(70％)聚丙烯酸聚丙烯酸钠交联的支化聚丙烯酸N-乙烯乙酰胺/丙烯酸钠共聚物羟丙基纤维素疏水化的羟丙基甲基纤维素羧甲基纤维素钠聚乙烯基吡咯烷酮EUDRAGIT RL POEUDRAGIT E 100高岭土轻质硅酸酐乙二胺四乙酸钠干燥的硫酸铝钾甘氨酸铝合成的羟基水滑石酒石酸三乙醇胺纯化水总量(wt.％)物料重量(g/m2) | 2.500.202.003.000.050.150.1015.00100.00200 | 20.005.002.001.002.002.000.100.350.2036.85100.001000 | 20.005.003.005.000.050.450.405.00100.00200 | 30.005.003.000.101.003.000.150.401.0035.75100.001000 | 20.005.002.000.505.003.000.120.091.2021.09100.00200 | 10.003.004.004.000.100.501.2015.20100.001000 |
Claims (10)
1.一种亲水性膏剂，其含有一种衬材和一种糊状物，该糊状物由亲水性粘胶物形成，其中含有0.05-10％重量的(甲基)丙烯酸氨基烷基酯和(甲基)丙烯酸烷基酯的共聚物，和选自铝化合物、镁化合物和钙化合物的交联剂，并铺展在所述衬材上。
2.权利要求1的亲水性膏剂，其中该(甲基)丙烯酸氨基烷基酯内的胺部分是由叔胺或季铵盐得到的。
3.权利要求1的亲水性膏剂，其中(甲基)丙烯酸氨基烷基酯内的胺部分是由二甲胺或氯化三甲铵得到的。
4.权利要求1-3之任一项的亲水性膏剂，其中还含有至少一种亲水性粘结剂，该粘结剂选自聚丙烯酸及其盐，用丙烯酸或其盐得到的共聚物，以及纤维素衍生物及其盐。
5.权利要求4的亲水性膏剂，其中所述的至少一种亲水性粘结剂是选自聚丙烯酸、聚丙烯酸钠、交联的支化聚丙烯酸、交联的支化聚丙烯酸钠、丙烯酸-淀粉接枝共聚物的交联产物、N-乙烯基乙酰胺-丙烯酸钠共聚物、羟乙基纤维素、羟丙基纤维素、羟丙基甲基纤维素、疏水化的羟丙基甲基纤维素和羧甲基纤维素钠。
6.权利要求1-3之任一项的亲水性膏剂，其中还含有至少一种组分作为所述(甲基)丙烯酸氨基烷基酯和所述(甲基)丙烯酸烷基酯的共聚物的增溶剂，该组分选自多元醇、脂肪酸酯、表面活性剂、脂肪酸、醇类和烃类。
7.权利要求1-3之任一项的亲水性膏剂，其中含有比例为1-85％重量的水。
8.权利要求1-3之任一项的亲水性膏剂，其中还含有选自透皮促进剂和湿润剂的至少一种组分。
9.权利要求1-3之任一项的亲水性膏剂，其中的糊状物另外含有至少一种药理活性成分。
10.权利要求9的亲水性膏剂，其中的至少一种药理活性成分选自止痛消炎药、抗真菌剂、尿失禁药、骨骼肌肉松弛剂、解痉药、强心剂、戒烟剂、抗过敏药、局部麻醉药、防腐消毒剂和皮肤刺激剂。
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP17110398A JP4275768B2 (ja) | 1998-06-18 | 1998-06-18 | 水性粘着膏体 |
| JP171103/1998 | 1998-06-18 | ||
| JP171103/98 | 1998-06-18 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN1243851A CN1243851A (zh) | 2000-02-09 |
| CN1161435C true CN1161435C (zh) | 2004-08-11 |
Family
ID=15917042
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CNB991085043A Expired - Lifetime CN1161435C (zh) | 1998-06-18 | 1999-06-18 | 亲水性胶粘物 |
Country Status (12)
| Country | Link |
|---|---|
| US (1) | US6207184B1 (zh) |
| EP (1) | EP0965626B1 (zh) |
| JP (1) | JP4275768B2 (zh) |
| KR (1) | KR100593717B1 (zh) |
| CN (1) | CN1161435C (zh) |
| CA (1) | CA2274358C (zh) |
| DE (1) | DE69911116T2 (zh) |
| ES (1) | ES2201595T3 (zh) |
| HK (1) | HK1024497A1 (zh) |
| MY (1) | MY118651A (zh) |
| SG (1) | SG83722A1 (zh) |
| TW (1) | TW576862B (zh) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101171298B (zh) * | 2005-05-03 | 2011-10-26 | 赛拉尼斯国际公司 | 具有n-烷基丙烯酰胺的盐敏性粘合剂组合物和包括该组合物的纤维状制品 |
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| JPS62123112A (ja) * | 1985-11-22 | 1987-06-04 | Sunstar Inc | 軟膏基剤 |
| JPH07100652B2 (ja) * | 1987-05-22 | 1995-11-01 | サンスタ−株式会社 | 透明状軟膏基剤 |
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| US5913840A (en) * | 1997-08-15 | 1999-06-22 | Minnesota Mining And Manufacturing Company | Soft orthopedic casting article with reinforcement system |
-
1998
- 1998-06-18 JP JP17110398A patent/JP4275768B2/ja not_active Expired - Lifetime
-
1999
- 1999-06-08 SG SG9902727A patent/SG83722A1/en unknown
- 1999-06-11 TW TW088109828A patent/TW576862B/zh not_active IP Right Cessation
- 1999-06-11 US US09/330,065 patent/US6207184B1/en not_active Expired - Lifetime
- 1999-06-14 CA CA002274358A patent/CA2274358C/en not_active Expired - Lifetime
- 1999-06-15 KR KR1019990022196A patent/KR100593717B1/ko not_active IP Right Cessation
- 1999-06-15 MY MYPI99002438A patent/MY118651A/en unknown
- 1999-06-18 CN CNB991085043A patent/CN1161435C/zh not_active Expired - Lifetime
- 1999-06-18 DE DE69911116T patent/DE69911116T2/de not_active Expired - Lifetime
- 1999-06-18 EP EP99111095A patent/EP0965626B1/en not_active Expired - Lifetime
- 1999-06-18 ES ES99111095T patent/ES2201595T3/es not_active Expired - Lifetime
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Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101171298B (zh) * | 2005-05-03 | 2011-10-26 | 赛拉尼斯国际公司 | 具有n-烷基丙烯酰胺的盐敏性粘合剂组合物和包括该组合物的纤维状制品 |
Also Published As
| Publication number | Publication date |
|---|---|
| JP4275768B2 (ja) | 2009-06-10 |
| MY118651A (en) | 2004-12-31 |
| CA2274358A1 (en) | 1999-12-18 |
| DE69911116D1 (de) | 2003-10-16 |
| ES2201595T3 (es) | 2004-03-16 |
| CA2274358C (en) | 2009-10-20 |
| EP0965626B1 (en) | 2003-09-10 |
| SG83722A1 (en) | 2001-10-16 |
| US6207184B1 (en) | 2001-03-27 |
| TW576862B (en) | 2004-02-21 |
| KR100593717B1 (ko) | 2006-06-28 |
| DE69911116T2 (de) | 2004-06-17 |
| HK1024497A1 (en) | 2000-10-13 |
| JP2000007559A (ja) | 2000-01-11 |
| KR20000006178A (ko) | 2000-01-25 |
| EP0965626A1 (en) | 1999-12-22 |
| CN1243851A (zh) | 2000-02-09 |
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