The purpose of this research was the preparation of four formulations containing hydrocortisone acetate (HCA) for topical application, including two aqueous systems (hydrophilic microemulsion and aqueous gel) and two systems with dominant hydrophobicity (hydrophobic microemulsion and ointment). The formulations were tested for the release and permeation of HCA across an animal membrane. The release of HCA was found comparable for the four systems. The two microemulsions promote permeation across an ex-vivo membrane, examined by means of a Franz cell. Hydrophobic microemulsion guarantees the highest solubility (2,370 μg/ml) and flux (133 μg/cm2.h) of the drug, since it contains almost 40% Transcutol, a permeation enhancer. Gel and ointment provide lower solubility and flux, being the values, related to the ointment, the lowest ones (562 μg/ml and 0.4 μg/cm2.h). Experimental results allow the conclusion that gel and ointment can be suitable when it is desirable to minimize absorption of topically applied HCA as to keep the drug restricted to the diseased area and prevent side effects of the systemic presence of HCA.
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机译:这项研究的目的是制备四种包含醋酸氢化可的松(HCA)的局部用制剂,包括两种水性体系(亲水性微乳液和水性凝胶)和两种具有显着疏水性的体系(疏水性微乳液和软膏)。测试了制剂在动物膜上HCA的释放和渗透。发现HCA的释放与四个系统相当。两种微乳状液均促进通过夫兰兹细胞检查的离体膜的渗透。疏水性微乳液可确保药物的最高溶解度(2,370μg/ ml)和通量(133μg/ cm 2 sup> .h),因为它含有近40%的Transcutol(一种渗透促进剂)。凝胶和软膏的溶解度和通量较低,与软膏相关,为最低值(562μg/ ml和0.4μg/ cm 2 sup> .h)。实验结果得出这样的结论:当希望最大程度地减少局部施用的HCA的吸收以保持药物局限于患病区域并防止HCA全身存在的副作用时,凝胶和软膏剂可能是合适的。
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