背景:乳液凝胶结合了乳液的品质和凝胶的品质。为了创建乳液w/o或o/w,乳液必须配制,然后与胶凝剂混合,导致双重控制药物释放。塞来昔布表现出镇痛作用,解热和抗炎活性,用于治疗骨关节炎,剧烈疼痛,类风湿性关节炎,和其他医疗条件。
方法:通过使用不同浓度的天然油和卡波姆-940作为胶凝剂来开发和评估塞来昔布乳液凝胶。各种油的筛选,进行助表面活性剂和表面活性剂以测定溶解度。使用精油(桉树油和松节油)作为渗透改性剂。已经进行了与聚合物相容性的研究,结果表明,聚合物和药物之间不应有物理或化学相互作用。对于制备乳化剂,用Smix(助表面活性剂和表面活性剂)比例(1:1、2:1和3:1)制备各种乳液。胶凝剂的选择通过将所选择的乳液体系比例1:1与聚合物卡泊940、卡泊934和HPMC(0:1:0:0,0:0.5:1,0:0:3,0.5:0:1,1:0:0)凝胶基质的组合掺入以制备均匀的乳液凝胶来进行。
结果:目视检查乳液凝胶是否有任何相行为,感觉,传播能力,通过将其薄层应用于幻灯片和砂砾。然后,用选定的胶凝剂制备所有6种乳剂。对所有的乳液进行pH值评估,物理性质(一致性,同质性,颜色,纹理),药物含量,铺展性,可挤出性,肿胀指数,粘度,稳定性和离心。使用Franz扩散池和卵膜进行体外药物释放。
结论:在所有制备的配方中,EG1有一个更好的释放,更高的粘度,药物含量较高,和比其他人更高的膨胀指数。制剂EG1在8小时内显示出更高的药物释放(91.25%)。
BACKGROUND: Emulgel combines the qualities of an emulsion with those of a gel. In order to create an emulgel w/o or o/w, emulsions have to be formulated, which are then combined with a gelling agent, resulting in a dual-control drug release. Celecoxib exhibits analgesic, antipyretic and anti-inflammatory activities and is used to treat osteoarthritis, severe pain, rheumatoid arthritis, and other medical conditions.
METHODS: Celecoxib Emulgel was developed and evaluated by using natural oil and carbopol- 940 as a gelling agent in different concentrations. The screening of various oils, co-surfactants and surfactants was performed to determine the solubility. The essential oils (eucalyptus oil and
turpentine oil) were used as penetration modifiers. Studies on compatibility with polymers have been conducted, and the results indicate that there should be no physical or chemical interactions between the polymers and the drug substance. For the preparation of emulgel, various emulsions were prepared with Smix (cosurfactant and surfactant) ratios (1:1, 2:1 and 3:1). The selection of a gelling agent was done by incorporating the selected emulsion system ratio of 1:1 with the combinations of polymers carbapol 940, carbapol 934, and HPMC (0:1:0, 0:0.5:1, 0:0:3, 0.5:0:1, 1:0:0) gel base to make a homogenous emulgel.
RESULTS: The emulgel was examined visually to see if it had any phase behaviour, feel, spreadability, and grittiness by applying its thin layer to a slide. Then, all six formulations of emulgel were prepared with the selected gelling agent. All emulgels were evaluated for pH, physical properties (consistency, homogeneity, colour, texture), drug content, spreadability, extrudability, swelling index, viscosity, stability and centrifugation. A Franz diffusion cell and an egg membrane were used to perform in-vitro drug release.
CONCLUSIONS: Among all prepared formulations, EG1 had a better release, higher viscosity, higher drug content, and a higher swelling index than the others. The formulation EG1 showed higher drug release (91.25%) within 8 hours.