Kittipongpatana Ornanong S, Burapadaja Siriporn, Kittipongpatana Nisit
Department of Pharmaceutical Sciences, Department of Pharmaceutical Care, Faculty of Pharmacy, Chiang Mai University, Chiang Mai, Thailand.
Drug Dev Ind Pharm. 2009 Jan;35(1):34-42. doi: 10.1080/03639040802144229.
An application of carboxymethyl mungbean starch (CMMS) as a gelling agent in the topical pharmaceutical preparation was investigated. CMMS was prepared using specific conditions that yielded a high-viscosity product. Polymer gels and gel bases were prepared at 1-10% (wt/wt), and physicochemical studies were carried out in comparison with four standard gelling agents: carbopol 940 (CP), hydroxypropylmethyl cellulose (HPMC), methyl cellulose (MC), and sodium carboxymethyl cellulose (SCMC). Piroxicam was used as a model drug to study the drug release profile of the gel formulations. The tackless, greaseless, and transparent CMMS gels exhibited pseudoplastic behavior with thixotropy at concentrations less than 5% (wt/wt). At a concentration of 5% (wt/wt) and higher, the semisolid gels showed plastic flow characteristics. Viscosity and X-ray diffraction results indicated a good compatibility between CMMS and the acidic piroxicam. No precipitation of piroxicam or phase separation was observed during a stability test. The release rate of piroxicam from 3% (wt/wt) CMMS gel was 1,003.79 +/- 105.08 microg/cm(2), which was comparable with 947.66 +/- 133.70 microg/cm(2) obtained from a 0.5% (wt/wt) carbopol formulation. The release profiles of both formulations were consistent and remained unchanged after 2 months' storage. Viscosity played an important role in controlling the release rate of low concentration CMMS formulations by regulating the drug diffusion. At a concentration of 5% (wt/wt) CMMS and higher, the release rates of piroxicam were not significantly different. A plausible explanation based on the nature of the gelling agent was proposed. Stability and drug release profiles of CMMS and commercial gelling agents were compared. The results supported the potential use of CMMS as a new, effective gelling agent for topical gel preparation.
研究了羧甲基绿豆淀粉(CMMS)作为凝胶剂在局部用药物制剂中的应用。采用特定条件制备了具有高粘度的CMMS。以1-10%(重量/重量)制备聚合物凝胶和凝胶基质,并与四种标准凝胶剂:卡波姆940(CP)、羟丙基甲基纤维素(HPMC)、甲基纤维素(MC)和羧甲基纤维素钠(SCMC)进行了物理化学研究比较。以吡罗昔康作为模型药物研究凝胶制剂的药物释放情况。无粘性、无油腻感且透明的CMMS凝胶在浓度低于5%(重量/重量)时表现出具有触变性的假塑性行为。在浓度为5%(重量/重量)及更高时,半固体凝胶表现出塑性流动特性。粘度和X射线衍射结果表明CMMS与酸性吡罗昔康之间具有良好的相容性。在稳定性试验中未观察到吡罗昔康沉淀或相分离现象。吡罗昔康从3%(重量/重量)CMMS凝胶中的释放速率为1003.79±105.08μg/cm²,与从0.5%(重量/重量)卡波姆制剂中获得的947.66±133.70μg/cm²相当。两种制剂的释放曲线一致,储存2个月后保持不变。粘度通过调节药物扩散在控制低浓度CMMS制剂的释放速率方面发挥重要作用。在CMMS浓度为5%(重量/重量)及更高时,吡罗昔康的释放速率无显著差异。基于凝胶剂的性质提出了一个合理的解释。比较了CMMS和市售凝胶剂的稳定性和药物释放情况。结果支持了CMMS作为局部凝胶制剂新型有效凝胶剂的潜在用途。