Sharma Garima, Jain S, Tiwary A K, Kaur Gurpreet
Department of Pharmaceutical Sciences, and Drug Research, Punjabi University, Patiala-147002, India.
Acta Pharm. 2006 Sep;56(3):337-45.
In this study, a bioadhesive dosage form of clotrimazole was designed using a combination of bioadhesive polymers Carbopol 934P, sodium carboxymethyl cellulose and sodium alginate in different ratios. The bioadhesive strength was evaluated by measuring the force required to detach the tablets from porcine vaginal mucosal membrane. The strong interaction between polymer and mucus lining of the tissue helps increase the contact time and permits localization of activity. Carbopol 934P showed maximum bioadhesion and required maximum force for detachment; the force required for detachment was directly proportional to its content. The formulations were tested for their swelling behavior using the agar gel plate method. The swelling index was a function of the concentration of the hydrophilic polymer and the formulations containing Carbopol 934P and sodium carboxymethyl cellulose were found to swell to a greater extent than those containing Carbopol and sodium alginate. In vitro release studies showed that the batch consisting of 2:1 ratio of Carbopol 934P/sodium alginate (batch C3) released clotrimazole over 24 h. The similarity factor showed that the dissolution profiles of fresh and aged tablets were similar, suggesting good stability of vaginal tablets prepared using a combination of Carbopol 934P and sodium alginate.
在本研究中，使用生物粘附性聚合物卡波姆934P、羧甲基纤维素钠和海藻酸钠以不同比例组合设计了克霉唑的生物粘附剂型。通过测量将片剂从猪阴道粘膜上分离所需的力来评估生物粘附强度。聚合物与组织粘液层之间的强相互作用有助于增加接触时间并使活性定位。卡波姆934P表现出最大的生物粘附性，分离所需的力最大；分离所需的力与其含量成正比。使用琼脂凝胶平板法测试制剂的溶胀行为。溶胀指数是亲水性聚合物浓度的函数，发现含有卡波姆934P和羧甲基纤维素钠的制剂比含有卡波姆和海藻酸钠的制剂溶胀程度更大。体外释放研究表明，由卡波姆934P/海藻酸钠比例为2:1的批次（批次C3）在24小时内释放克霉唑。相似性因子表明新鲜片剂和老化片剂的溶出曲线相似，表明使用卡波姆934P和海藻酸钠组合制备的阴道片剂具有良好的稳定性。
