摘要
目的 筛选口服缓释地尔硫的生物粘附材料。方法 通过测定可用于制药的粘附聚合物羟丙基甲基纤维素 (HPMC)类、卡波姆 (Cb)类、聚维酮 (PVP)K30和羧甲基纤维素钠 (CMCNa)与大鼠胃和肠黏膜的最大粘附力及其在大鼠胃和肠道的排空速度 ,筛选出最佳粘附材料 ,再用放射性核素体内示踪技术验证其在犬胃、肠的粘附能力。结果 Cb与大鼠肠黏膜的粘附力为 19.6～ 31.0g,显著大于其他材料 (4.0～ 2 4 .3g)。Cb934在大鼠胃内的排空半衰期为 7.4h,大于其他材料。含5 0 %Cb934的粘附颗粒能将其在犬胃内的排空半衰期延长 1倍 ;8h时犬小肠含Cb9345 0 %和 10 0 %的粘附颗粒滞留量分别为 2 9.6 %和 5 5 .1% ,而不含Cb934的粘附颗粒 6h时即为 0。结论 Cb934可作为口服缓释剂生物粘附材料。
ObjectiveTo screen bioadhesive materials for oral sustained-release diltiazem. MethodsThe bioadhesion force of adhesive hydroxypropylmethylcellulose (HPMC) polymer, carbomers (Cb), PVPk30 and CMCNa with rat gastric and intestinal mucosa and the excretion rate of the adhesives in gastrointestinal tract of rats were measured to screen the best bioadhesive material, then, the bioadhesive ability of the best bioadhesive material was tested in gastrointestinal tract of dogs with in vivo radionuclide tracing imaging. ResultsThe bioadhesion force of Cb with rat intestinal mucosa (19.6～31.0 g) was bigger than that of other materials (4.0～24.3 g), and the excretion rate of Cb934 was the slowest in gastrointestinal tract of rats. The Cb934 remarkably increased the retention time of its preparation in the gastrointestinal tract of dogs. ConclusionCb934 can be used as bioadhesive material of oral sustained-release medicine.
出处
《中华核医学杂志》
CAS
CSCD
北大核心
2002年第6期376-378,T002,共4页
Chinese Journal of Nuclear Medicine
关键词
放射性核素示踪技术
地尔硫ZHUO
缓释粘附材料
生物相容性材料
迟效制剂
剂型
Biocompatible materials
Delayed-action preparations
Radionuclide imaging
Hydroxypropylmethy lcellulose
Carbomer
Povidone
Dogs
Rats
