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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。
Objective To screen bioadhesive materials of oral sustained release diltiazem. Methods The drug-loaded adhesive polymers, hydroxypropylmethylcellulose (HPMC), carbomer (Cb), povidone (PVP) K30 and sodium carboxymethylcellulose (CMCNa) The maximum adhesion of rat stomach and intestinal mucosa and its emptying rate in the stomach and intestine of rats were screened for the best adhesion material and then the radionuclide in vivo tracing technique was used to verify its adhesion in canine stomach and intestine Attached capacity. Results The adhesion of Cb to rat intestinal mucosa was 19.6-31.0g, significantly higher than that of other materials (4.0-2.43g). The empty half-life of Cb934 in the rat stomach was 7.4 h, which was greater than other materials. The adherence particles containing 50% Cb934 could double its half-life of emptying in the canine stomach. The accumulation of 0% and 10% of the adhered particles in the small intestine of dogs at 8 hours was 29.6% and 55%, respectively .1%, while the adhesion particles without Cb934 6h when it is 0. Conclusion Cb934 can be used as oral sustained-release bioadhesive material.