Ameye D, Mus D, Foreman P, Remon J P
Laboratory of Pharmaceutical Technology, Ghent University, Harelbekestraat 72, B-9000 Gent, Belgium.
Int J Pharm. 2005 Sep 14;301(1-2):170-80. doi: 10.1016/j.ijpharm.2005.05.016.
In the present study, spray-dried Amioca starch/Carbopol 974P mixtures were evaluated as potential buccal bioadhesive tablets. Carbopol (C 974P) concentrations from 5 to 75% were tested. All spray-dried mixtures showed a comparable or better bioadhesive capacity compared to a reference formulation (DDWM/C 974P 95/5). The bioadhesive capacities of Amioca/Carbopol 974P mixtures were improved by spray-drying. All spray-dried mixtures showed significantly higher work of adhesion values compared to their equivalent physical mixtures. The influence of Carbopol concentration on the in vivo adhesion time of placebo tablets and in vitro miconazole nitrate release was tested. The ratio Amioca/C 974P 70/30 showed the longest in vivo adhesion time (24.5+/-8.5 h). Lower and higher C 974P concentrations had a shorter in vivo adhesion time. The mixtures containing between 15 and 30% C 974P could all sustain the in vitro miconazole nitrate release over 20 h. Again, lower and higher C 974P concentrations showed a faster in vitro miconazole release. The drug loading capacity of a spray-dried mixture containing 20% C 974P was investigated in vivo in dogs using testosterone as model drug. The spray-dried mixture could be loaded with 60% drug without loosing its in vivo bioadhesive and pharmacokinetic properties.
在本研究中，喷雾干燥的木薯淀粉/卡波姆974P混合物被评估为潜在的口腔生物黏附片。测试了卡波姆（C 974P）浓度为5%至75%的情况。与参考制剂（DDWM/C 974P 95/5）相比，所有喷雾干燥的混合物均表现出相当或更好的生物黏附能力。喷雾干燥提高了木薯淀粉/卡波姆974P混合物的生物黏附能力。与它们相应的物理混合物相比，所有喷雾干燥的混合物均表现出显著更高的黏附功值。测试了卡波姆浓度对安慰剂片体内黏附时间和体外硝酸咪康唑释放的影响。木薯淀粉/C 974P 70/30的比例显示出最长的体内黏附时间（24.5±8.5小时）。较低和较高的C 974P浓度具有较短的体内黏附时间。含有15%至30% C 974P的混合物均可使体外硝酸咪康唑释放持续20小时以上。同样，较低和较高的C 974P浓度显示出更快的体外咪康唑释放。以睾酮作为模型药物，在犬体内研究了含有20% C 974P的喷雾干燥混合物的载药能力。该喷雾干燥混合物可装载60%的药物，且不会丧失其体内生物黏附性和药代动力学特性。
