Musial Witold
Drug Form Technology Unit, Wroclaw Medical University, Wroclaw, Poland.
Chem Pharm Bull (Tokyo). 2007 Aug;55(8):1141-7. doi: 10.1248/cpb.55.1141.
Topical treatment of acne rosacea, a chronic condition characterized by recurrent course for many years, is primarily based on metronidazole preparations. The aim of this study was to evaluate the effect of various acrylic acid polymers, in composition with methylcellulose on metronidazole release rate from hydrogels proposed for the treatment of acne rosacea. Viscosity and release studies using "Paddle over Disk" system with semipermeable membrane of MWCO 3500 were performed. Compositions of Carbopol 971P and methylcellulose revealed an increase in viscosity with increasing concentration of methylcellulose in the range of 17200-26166 mPa.s. In all the examined formulations, the release process was characterized by a two-stage course. Among bipolymeric formulations, the highest first-stage release rate of 9.18 x 10(-3) min(-1) was determined for the gel consisting of 2.00% Carbopol 980NF with 1.00% methylcellulose. The second-stage release rates ranged between 2.88 x 10(-3) and 8.00 x 10(-3) min(-1). Two-stage release course can thus be attributed to metronidazole distribution into two compartments of hydrogel matrix. Proposed gels, with similar rheological properties, may be used for ex vivo and in vivo studies to obtain a suitable drug activity of metronidazole in the treatment of acne rosacea.
酒渣鼻是一种多年来反复发作的慢性疾病,其局部治疗主要基于甲硝唑制剂。本研究的目的是评估各种丙烯酸聚合物与甲基纤维素组成的组合物对拟用于治疗酒渣鼻的水凝胶中甲硝唑释放速率的影响。使用具有MWCO 3500半透膜的“桨盘法”系统进行了粘度和释放研究。卡波姆971P和甲基纤维素的组合物显示,随着甲基纤维素浓度在17200 - 26166 mPa·s范围内增加,粘度增加。在所有测试配方中,释放过程具有两阶段特征。在双聚合物配方中,由2.00%卡波姆980NF和1.00%甲基纤维素组成的凝胶的第一阶段最高释放速率为9.18×10⁻³ min⁻¹。第二阶段释放速率在2.88×10⁻³至8.00×10⁻³ min⁻¹之间。因此,两阶段释放过程可归因于甲硝唑在水凝胶基质的两个隔室中的分布。所提出的具有相似流变学性质的凝胶可用于体外和体内研究,以在酒渣鼻治疗中获得合适的甲硝唑药物活性。