Bitay Enikő, Gergely Attila Levente, Szabó Zoltán-István
Department of Mechanical Engineering, Faculty of Technical and Human Sciences, Sapientia Hungarian University of Transylvania, Calea Sighișoarei nr. 2, 540485 Târgu-Mureş, Romania.
Bánki Donát Faculty of Mechanical and Safety Engineering, Óbuda University, Népszínház u. 8, 1081 Budapest, Hungary.
Polymers (Basel). 2023 Dec 29;16(1):123. doi: 10.3390/polym16010123.
An amorphous fiber-based solid dispersion of chlorzoxazone was prepared for the first time by employing centrifugal spinning, using polyvinylpyrrolidone as the fiber-forming polymer. After optimization of the spinning parameters, the obtained fibers were characterized using a set of analytical techniques, both in a solid- and solution-state. Morphological characterization revealed a slightly aligned, defect-free fibrous structure with an average fiber diameter of d = 3.07 ± 1.32 μm. The differential scanning calorimetric results indicated a crystalline-to-amorphous transition of the active substance during the centrifugal spinning process, while gas chromatographic determinations revealed a residual ethanol content of 0.42 ± 0.04%. UV spectroscopy indicated the incorporation of chlorzoxazone in the fibrous structures, with an average active substance content of 15.91 ± 0.36 /%. During small-volume dissolution studies, the prepared fiber mats presented immediate disintegration upon contact with the dissolution media, followed by rapid dissolution of the active substance, with 84.8% dissolved at 1 min and 93.7% at 3 min, outperforming the micronized, pure chlorzoxazone. The obtained results indicate that centrifugal spinning is a low-cost, high-yield, viable alternative to the currently used methods to prepare fiber-based amorphous solid dispersions of poorly soluble drugs. The prepared chlorzoxazone-loaded microfibers could be used as a buccal dosage form for the systematic delivery of chlorzoxazone and could potentially lead to a rapid onset of action and longer efficacy of the muscle relaxant drug.
首次采用离心纺丝法，以聚乙烯吡咯烷酮为成纤聚合物，制备了氯唑沙宗的非晶态纤维基固体分散体。优化纺丝参数后，采用一系列分析技术对所得纤维进行了固态和溶液态表征。形态表征显示，纤维结构排列略有对齐，无缺陷，平均纤维直径为d = 3.07 ± 1.32μm。差示扫描量热法结果表明，在离心纺丝过程中活性物质发生了晶态到非晶态的转变，而气相色谱测定显示残留乙醇含量为0.42 ± 0.04%。紫外光谱表明氯唑沙宗已掺入纤维结构中，活性物质平均含量为15.91 ± 0.36/%。在小体积溶出度研究中，制备的纤维垫与溶出介质接触后立即崩解，随后活性物质迅速溶解，1分钟时溶解84.8%，3分钟时溶解93.7%，优于微粉化的纯氯唑沙宗。所得结果表明，离心纺丝是一种低成本、高产率的可行方法，可替代目前用于制备难溶性药物的纤维基非晶态固体分散体的方法。制备的载氯唑沙宗微纤维可作为氯唑沙宗全身给药的口腔剂型，并可能导致肌肉松弛药物起效迅速且疗效持久。
