纳米碳酸钙生物黏附片体外黏附力及释放度的测定

Determination of adhesive force and releasing rate of calcium carbonate nanoparticle bioadhesive tablets in vitro

目的通过纳米碳酸钙生物黏附片的制备和片芯体外黏附力及释放度测试,探讨羟丙基甲基纤维素（HPMC）以及卡波姆（CP）在黏附片中的不同含量对片芯黏附力及释放度的影响机制。方法以纳米碳酸钙为主药,CP与HPMC作为生物黏附性材料,测定不同比例制备的片芯在体外肠道的黏附力和释放度。结果黏附力测试结果显示,HPMC∶CP为1∶3的黏附力最高。在1~4 h作用下,HPMC∶CP为1∶1、1∶2、1∶3、2∶1及3∶1的释放度分别是22.21%~74.19%、21.15%~69.43%、19.21%~62.14%、28.88%~87.62%及35.33%~91.55%,其中HPMC∶CP为3∶1的片芯在4 h后基本释放完全;HPMC∶CP为1∶3的片芯在4 h后仅释放62%。结论经过黏附片片重测定片芯均符合差异标准,不影响实验结果。在单因素实验中,黏附材料的含量比例对片芯的黏附力和释放度有直接影响,且HPMC与CP作为黏附材料测定的黏附力结果与释放度结果成正比,HPMC∶CP为1∶3的配方为最优配方。

Objective To determine the adhesive force and releasing rate of calcium carbonate nanoparticle bioadhesive tablets in vitro. Methods Calcium carbonate nanoparticle bioadhesive tablets were made of different ratios of carbomer（CP） and hydroxypropyl methyl cellulose（HPMC） with calcium carbonate nanoparticle as the basic remedy. The in vitro adhesive force and releasing degree of the core tablets were detected in isolated intestine. Results The adhesive force of calcium carbonate nanoparticle bioadhesive tablets was the highest when HPMC/CP ratio was 1 ： 3. In 1-4 hours the releasing rate was 22.21%-74.19%, 21.15%-69.43%, 19.21%-62.14%, 28.88%-87.62% and 35.33%-91.55% when the HPMC/CP ratio was 1 ： 1, 1 ： 2,1 ： 3, 2 ： 1 and 3 ： 1 respectively. The tablets with the HPMC/CP ratio of 3 ： 1 was almost completely released in 4 hours, but only 62% of the tablets with the HPMC/CP ratio of 1 ： 3 was released in 4 hours.Conclusions When the tablets＇ weight is in small difference, it does not affect the result of the experiment.The content ratio of the adhesive materials has direct influence on the adhesive power and releasing rate of the tablets. When HPMC and CP are used as adhesive materials, the adhesive power is inversely proportional to releasing rate. HPMC/CP ratio of 1 ： 3 is the best formulation.