Bregni Carlos, Chiappetta Diego, Faiden Natalia, Carlucci Adriana, García Roberto, Pasquali Ricardoc
Department of Pharmaceutical Technology, Faculty of Pharmacy and Biochemistry, University of Buenos Aires, Junín 956 (1113) Buenos Aires, Argentina.
Pak J Pharm Sci. 2008 Jan;21(1):12-6.
Carbopol gels were prepared using a traditional polymer with mucoadhesive properties (974P). A new Carbomer derivative Ultrez 21 was also evaluated. Mineral oil, as occlusive ingredient, glycerol as humectant and ethanol were included in all the compositions. The feasibility of preparing these formulations with or without a bioadhesive polymer (Polycarbophil AA-1) and a second oil phase with enhancer activity (Miglyol 840) was evaluated. Further characterization including physical stability during a year was carried out. In vitro release behaviour of diclofenac sodium in Franz diffusion cell was evaluated with some selected formulations using an ethanol-water (50% w/w) solution as receptor medium. Addition of Polycarbophil AA-1 increased formulation viscosity and decreased drug release. These types of topical dosage forms could give sustained delivery of drug onto the skin, could tolerate the incorporation of an enhancer, a humectant and an occlusive phase, so they are interesting promises to improve skin absorption of nonsteroidal anti-inflammatory drugs and to prevent side effects associated.
使用具有粘膜粘附特性的传统聚合物（974P）制备卡波姆凝胶。还对一种新型卡波姆衍生物Ultrez 21进行了评估。所有配方中均包含作为封闭成分的矿物油、作为保湿剂的甘油和乙醇。评估了制备这些配方时添加或不添加生物粘附聚合物（聚卡波非AA - 1）以及具有增强活性的第二油相（Miglyol 840）的可行性。进行了包括一年物理稳定性在内的进一步表征。使用乙醇 - 水（50% w/w）溶液作为受体介质，在Franz扩散池中对一些选定配方评估双氯芬酸钠的体外释放行为。添加聚卡波非AA - 1会增加配方粘度并降低药物释放。这些类型的局部剂型可以使药物在皮肤上持续递送，可以耐受添加增强剂、保湿剂和封闭相，因此它们有望改善非甾体抗炎药的皮肤吸收并预防相关副作用，是很有前景的。
