Mohamed Magdy I
Department of Pharmaceutics, Faculty of Pharmacy, Cairo University, Cairo, Egypt.
AAPS J. 2004 Oct 11;6(3):e26. doi: 10.1208/aapsj060326.
This study was conducted to develop an emulgel formulation of chlorphenesin (CHL) using 2 types of gelling agents: hydroxypropylmethyl cellulose (HPMC) and Carbopol 934. The influence of the type of the gelling agent and the concentration of both the oil phase and emulsifying agent on the drug release from the prepared emulgels was investigated using a 2(3) factorial design. The prepared emulgels were evaluated for their physical appearance, rheological behavior, drug release, antifungal activity, and stability. Commercially available CHL topical powder was used for comparison. All the prepared emulgels showed acceptable physical properties concerning color, homogeneity, consistency, spreadability, and pH value. They also exhibited higher drug release and antifungal activity than the CHL powder. It was found that the emulsifying agent concentration had the most pronounced effect on the drug release from the emulgels followed by the oil phase concentration and finally the type of the gelling agent. The drug release from all the emulgels was found to follow diffusion-controlled mechanism. Rheological studies revealed that the CHL emulgels exhibited a shear-thinning behavior with thixotropy. Stability studies showed that the physical appearance, rheological properties, drug release, and antifungal activity in all the prepared emulgels remained unchanged upon storage for 3 months. As a general conclusion, it was suggested that the CHL emulgel formulation prepared with HPMC with the oil phase concentration in its low level and emulsifying agent concentration in its high level was the formula of choice since it showed the highest drug release and antifungal activity.
羟丙基甲基纤维素(HPMC)和卡波姆934来开发氯苯甘醚(CHL)的乳胶凝胶制剂。采用2(3)析因设计研究了胶凝剂类型以及油相和乳化剂浓度对所制备乳胶凝胶药物释放的影响。对所制备的乳胶凝胶进行了外观、流变学行为、药物释放、抗真菌活性和稳定性评估。使用市售的CHL外用粉剂作为对照。所有制备的乳胶凝胶在颜色、均匀性、稠度、铺展性和pH值方面均表现出可接受的物理性质。它们还表现出比CHL粉剂更高的药物释放和抗真菌活性。发现乳化剂浓度对乳胶凝胶药物释放的影响最为显著,其次是油相浓度,最后是胶凝剂类型。发现所有乳胶凝胶的药物释放均遵循扩散控制机制。流变学研究表明,CHL乳胶凝胶表现出具有触变性的剪切变稀行为。稳定性研究表明,所有制备的乳胶凝胶在储存3个月后其外观、流变学性质、药物释放和抗真菌活性均保持不变。总的来说,建议选择用低水平油相浓度和高水平乳化剂浓度的HPMC制备的CHL乳胶凝胶制剂,因为它显示出最高的药物释放和抗真菌活性。