羰基嘧啶衍生物软剂型的研制

M. Boldina, V. Grikh, A. Gubanova, Maxim Stantsov, A. Kozlova
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摘要

在改进已知原料药的获取技术和扩大剂型范围的过程中,减少副作用和保证使用的方便性是一个重要的方面。同时,药物应提供原料药最重要的特性,即从剂型的基底部最迅速、最完全地释放并渗透到靶器官,这应作为有效、安全药物的配方和技术的合理因素[3,4]。由于副作用较小且易于使用,软剂型(凝胶、软膏)是现代制药市场上需求量最大的剂型之一。用亲水碱基取代软剂型中的疏水碱基的趋势在药剂学上已经追踪了很长时间,因为相对于疏水软膏,凝胶由于药物物质通过皮肤屏障的渗透性更好而提供了更高的应用效率。凝胶中聚合物胶凝剂的存在不仅决定了药物的流变性能,而且还允许药物物质的高度分散的固相包含在聚合物的网络结构中,并且在储存期间保持药物物质难溶于水的分散。甲基尿嘧啶,也称为二氧甲基四氢嘧啶,是嘧啶的衍生物,是核酸的结构元素,用于治疗各种病因的疾病,主要是为了改善受损组织的再生过程。甲基尿嘧啶的一个显著缺点是其在水中的溶解度低,这严重影响了药物物质从药物底部的释放程度[1]。由于医药市场上甲基尿嘧啶凝胶的缺乏,利用丙烯酸衍生物开发甲基尿嘧啶凝胶以提高药用物质的生物制药性能是药学领域的一个重要问题。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
Development of soft dosage forms of pyrimidine derivatives based on carbopols
In the process of improving the technology for obtaining and expanding the range of dosage forms of known pharmaceutical substances, an important aspect is to reduce side effects and ensure ease of use. At the same time, medicines should provide the most important properties of pharmaceutical substances, namely, their most rapid and complete release from the base of the dosage form and penetration into the target organ, which should serve as factors in justifying formulations and technologies of effective and safe medicines [3, 4]. Due to the lesser manifestation of side effects and ease of use, soft dosage forms (gels, ointments) are among the most demanded dosage forms on the modern pharmaceutical market. The trend towards replacing hydrophobic bases in soft dosage forms with hydrophilic ones has been traced in pharmacy for quite a long time, since gels provide higher efficiency in application due to better penetration of pharmaceutical substances through the skin barrier relative to hydrophobic ointments. The presence of a polymer-gelling agent in gels determines not only the rheological properties of medicines, but also allows a highly dispersed solid phase of a pharmaceutical substance to be included in the network structure of a polymer and to maintain the dispersion of a pharmaceutical substance poorly soluble in water during storage. Methyluracil, also known as dioxomethyltetrahydropyrimidine, is a derivative of pyrimidine, a structural element of nucleic acids and is used in the treatment of diseases of various etiologies, mainly to improve the course of regeneration in damaged tissues. A significant disadvantage of methyluracil is its low solubility in water, which significantly affects the degree of release of the pharmaceutical substance from the base of the drug [1]. Due to the lack of methyluracil gels on the pharmaceutical market, their development using acrylic acid derivatives in order to improve the biopharmaceutical properties of a pharmaceutical substance is an important problem in pharmacy.
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