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    • 3. 发明申请
    • WATER SOLUBLE POLYVINYL LACTAM-DRUG COMPLEXES
    • 水溶性聚乙烯乳液 - 药物复合物
    • WO1987006464A1
    • 1987-11-05
    • PCT/US1987000763
    • 1987-04-06
    • GAF CORPORATION
    • GAF CORPORATIONBARABAS, Eugene, S.
    • A61K31/34
    • C07D207/12A61K9/146A61K47/58C08F8/44C08F8/34C08F126/10
    • Water soluble complexes of normally water insoluble drugs such as chlorothiazide, aminobenzoic acid, furosemide and mixtures thereof wherein the complexing agent is a polyvinyl lactam such as polyvinylpyrrolidone, polyvinylpyrrolidone-halogen complex or mixtures thereof. The invention also relates to the preparation of these complexes which involves dissolving the reactive components in an aqueous inert solvent combining the complexing agent and drug in a weight ratio of from about 1:1 to about 10:1 with agitation for a period of at least 5 minutes at a temperature above 3 DEG C and below the boiling point of the aqueous solvent solution under a pressure up to about 50 psig.
    • 通常水不溶性药物如氯噻嗪,氨基苯甲酸,呋塞米及其混合物的水溶性络合物,其中络合剂是聚乙烯基内酰胺如聚乙烯吡咯烷酮,聚乙烯吡咯烷酮 - 卤素络合物或其混合物。 本发明还涉及这些配合物的制备,其包括将反应性组分溶解在结合络合剂和药物的水性惰性溶剂中,重量比为约1:1至约10:1,同时搅拌至少一段时间 在高于3℃的温度下,在高达约50psig的压力下低于水性溶剂溶液的沸点5分钟。
    • 6. 发明申请
    • METHOD OF PREPARING A POLYVINYLPYRROLIDONE-HALOGEN COMPLEX OF IMPROVED STABILITY
    • 制备改进稳定性的聚乙烯吡咯烷酮 - 卤化物复合物的方法
    • WO1987006134A1
    • 1987-10-22
    • PCT/US1987000526
    • 1987-03-13
    • GAF CORPORATION
    • GAF CORPORATIONBARABAS, Eugene, S.
    • A61K31/79
    • A01N59/12
    • Process for making a highly stable polyvinylpyrrolidone-halogen complex by forming a reaction solution in a diffusion zone containing a 3 to 9 percent aqueous solution of polyvinylpyrrolidone and halogen dissolved in an alcohol solution wherein the concentration of alcohol is not less than 40 % of the total solutions and wherein a portion of the halogen requirement, up to 35 %, may be in the form of hydrogen halide or a salt thereof; reacting the polypyrrolidone and halogen components and forming a water/alcohol azeotrope simultaneously with the corresponding polyvinylpyrrolidone-halogen complex; subjecting the reacted mixture to azeotropic distillation to remove an aqueous alcohol distillate; recycling the distillate to the halogen solubilizing or diffusion zone and subjecting the remaining liquid product solution, containing not more than about 35 % solids, to spray drying to recover the polyvinylpyrrolidone/halogen product in the form of a particulate solid wherein each particle is of a uniform brownish yellow color throughout.
    • 通过在含有3〜9%聚乙烯吡咯烷酮水溶液和溶解在醇溶液中的卤素的扩散区中形成反应溶液来制备高度稳定的聚乙烯吡咯烷酮 - 卤素络合物的方法,其中酒精浓度不低于总量的40% 溶液,其中卤素需求的一部分高达35%可以​​是卤化氢或其盐的形式; 使聚吡咯烷酮和卤素组分反应,并与相应的聚乙烯吡咯烷酮 - 卤素络合物同时形成水/醇共沸物; 对反应后的混合物进行共沸蒸馏以除去醇酒精馏出物; 将馏出物再循环到卤素增溶或扩散区,并使含有不超过约35%固体的剩余液体产物溶液喷雾干燥以回收颗粒状固体形式的聚乙烯吡咯烷酮/卤素产物,其中每个颗粒为 均匀的棕黄色贯穿整个颜色。