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卡波姆是合成的高分子量丙烯酸交联聚合物。由聚(丙烯酸)聚合物与烯丙基蔗糖或烯丙基季戊四醇交联制得。聚合反应最常用的溶剂是苯。而较新的卡波姆型号是用乙酸乙酯或环己烷-乙酸乙酯共溶剂的混合物制备的。商品Carbopol ETD树脂是用一种专利聚合助剂在共溶剂中使树脂与聚烯基聚醚交联制得。 14 安全性

卡波姆广泛应用于非注射制剂,特别是局部的液体和半固体制剂。有某些级别可以应用于口服制剂中,见第18项。动物急性口服毒性研究表明,卡波姆934P的口服毒性较低。狗按照每千克体重8g的剂量给药,无死亡。一般认为卡波姆基本上是无毒、无刺激性的辅料。没有证据表明局部应用卡波姆有过敏反应。人口服卡波姆 1~3g的剂量可被用作强腹泻剂。

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卡波姆934 LD50(豚鼠,口服):2.5g/kg 卡波姆934P LDb50(豚鼠,口服):2.5g/kg 卡波姆940 LD50(豚鼠,口服):2.5g/kg 卡波姆934P LD50(小鼠,IP):0.04g/kg 卡波姆940 LD50(小鼠,IP):0.04g/kg 卡波姆934P LD50(小鼠,IV):0.07g/kg 卡波姆940 LD50(小鼠,IV):0.07g/kg 卡波姆934P LD50(小鼠,口服):4.6g/kg 卡波姆934 LD50(小鼠,口服):4.6g/kg 卡波姆940 LD50(小鼠,口服):4.6g/kg 卡波姆910 LD50(大鼠,口服):10.25g/kg 卡波姆934P LD50(大鼠,口服):2.5g/kg 卡波姆934 LD50(大鼠,口服):4.1g/kg 卡波姆940 LD50(大鼠,口服):2.5g/kg 卡波姆941 LD50(大鼠,口服):>1g/kg 15 操作注意事项

遵守材料操作的环境和数量相应的注意事项。应尽量避免产生过多的粉末,以避免爆炸

3

的危险。最低爆炸浓度为100g/m。卡波姆粉末对眼、黏膜、呼吸道有刺激。与眼接触时,卡波姆粉末由于形成凝胶状的膜,难以用水除去,需要用盐水冲洗。建议在操作时使用手套,保护眼睛和防尘呼吸器。 16 法规

已收载于FDA《非活性组分指南》(用于口服混悬剂和片剂,眼用制剂、直肠制剂和局部用制剂)。欧洲许可用于非注射制剂中。 17 同类物质

无。 18 注释

许多不同型号的卡波姆市上已有售,不同型号的卡波姆其分子量、交联度、聚合物结构和残留成分有所不同。这些不同是造成各种型号独特的流变性,处理和应用特点的原因。用长链烷基丙烯酸酯修饰的聚合物骨架的卡波姆可用作聚合物乳化剂和需要增加耐离子作用的制剂中。

聚卡波菲(Polycarbophil),是聚(丙烯酸)聚合物与二乙烯基二醇交联的聚合物,可用于生物黏附或医学实践中。标有字母P的卡波姆,如卡波姆971P,是惟一可用于口服或与黏膜接触的药用级别的聚合物,这些树脂在制备透明凝胶时特别有用。 19 专门参考文献

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delivery.Part 2:carbomer and polycarbophil are potent inhibitors of the intestinal proteolytic enzyme trypsin. Pharm Res 1995; 12: 1293-1298.

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20 一般参考文献

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BFGoodrichCompany.Technical literature: Carbopol,Noveon,Pemulen resins handbook,1995.

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21 执笔人

J JKoleng, J W McGinity, W R Wilber。 22 修订日期 2002-11-6。