Department of Pharmacy, Faculty of Medicine and Pharmacy, University of Oradea, 1st December Square 10, 410068 Oradea, Romania.
Department of Pharmaceutical Technology, Faculty of Pharmacy, University of Debrecen, Nagyerdei Körút 98, 4032 Debrecen, Hungary.
Molecules. 2020 Dec 23;26(1):24. doi: 10.3390/molecules26010024.
Topical anti-inflammatory and analgesic effect for the treatment of rheumatoid arthritis is of major interest because of their fewer side effects compared to oral therapy. The purpose of this study was to prepare different types of topical formulations (ointments and gels) containing synthetic and natural anti-inflammatory agents with different excipients (e.g.,: surfactants, gel-forming) for the treatment of rheumatoid arthritis. The combination of Non-Steroidal Anti-Inflammatory Drugs (NSAIDs), diclofenac sodium, a topical analgesic agent methyl salicylate, and a lyophilized extract of with antioxidant effect were used in our formulations. The aim was to select the appropriate excipients and dosage form for the formulation in order to enhance the diffusion of active substances and to certify the antioxidant, analgesic, and anti-inflammatory effects of these formulations. To characterize the physicochemical properties of the formulations, rheological studies, and texture profile analysis were carried out. Membrane diffusion and permeability studies were performed with Franz-diffusion method. The therapeutic properties of the formulations have been proven by an antioxidant assay and a randomized prospective study that was carried out on 115 patients with rheumatoid arthritis. The results showed that the treatment with the gel containing diclofenac sodium, methyl salicylate, and lyophilized as active ingredients, 2-propenoic acid homopolymer (Synthalen K) as gel-forming excipient, distilled water, triethanolamine, and glycerol had a beneficial analgesic and local anti-inflammatory effect.
治疗类风湿关节炎的局部抗炎和镇痛效果非常重要，因为与口服治疗相比，其副作用较少。本研究的目的是制备含有不同抗炎剂的不同类型的局部制剂（软膏和凝胶），这些抗炎剂具有不同的赋形剂（例如：表面活性剂、凝胶形成剂），用于治疗类风湿关节炎。本研究将非甾体类抗炎药（NSAIDs）、双氯芬酸钠、局部镇痛剂水杨酸甲酯，以及具有抗氧化作用的冻干提取物组合在一起。目的是选择适当的赋形剂和剂型来进行制剂，以增强活性物质的扩散，并证明这些制剂的抗氧化、镇痛和抗炎作用。为了表征制剂的物理化学性质，进行了流变学研究和质地分析。采用 Franz 扩散法进行了膜扩散和渗透性研究。通过抗氧化测定和对 115 例类风湿关节炎患者进行的随机前瞻性研究证明了制剂的治疗特性。结果表明，含有双氯芬酸钠、水杨酸甲酯和冻干的作为活性成分的凝胶，以 2-丙烯酸钠均聚物（Synthalen K）作为凝胶形成赋形剂，蒸馏水、三乙醇胺和甘油的治疗，具有有益的镇痛和局部抗炎作用。
