A mechanistic model was developed and tested to predict the release of sumatriptan succinate from dissolving microneedles and its permeation across the epidermal skin layers. Material balance equations were written to describe molecular transport followed by absorption into the systemic circulation. The solid drug particles were encapsulated in pyramid-shaped, polyvinylpyrrolidone-based water-soluble microneedles. Plots, generated from literature values and designed to simulate concentration distributions in the epidermal layers, agreed with optical coherence tomography (OCT)images captured at early stages of the experiments. Simulations showed that an increase in the pitch width led to a faster release of the medication. By modifying the governing equations to include a microneedle baseplate, the model was able to estimate short- and long-term release behaviors from in vitro Franz cellexperiments. These studies were performed using three distinct dissolving microneedle formulations and minipig skin as the biological membrane. The calculated diffusion coefficients were one order of magnitude greater than the value estimated when the drug was directly applied to the skin surface. The dissolution rate constant was affected by the concentration of the polymer matrix.

中文翻译：

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从基于聚乙烯吡咯烷酮的微针中透皮递送琥珀酸舒马曲坦的实验和数学研究。

建立了机械模型并进行了测试，以预测舒马曲坦琥珀酸酯从溶解性微针的释放及其在表皮皮肤层中的渗透。编写了物质平衡方程来描述分子的运输，然后吸收到体循环中。将固体药物颗粒包封在金字塔形的，基于聚乙烯吡咯烷酮的水溶性微针中。从文献值生成并设计为模拟表皮层中浓度分布的图，与实验早期捕获的光学相干断层扫描（OCT）图像一致。模拟表明，节距宽度的增加导致药物的更快释放。通过修改控制方程以包括微针底板，该模型能够估计体外Franz细胞实验的短期和长期释放行为。这些研究是使用三种不同的溶解性微针制剂和微型猪皮肤作为生物膜进行的。计算出的扩散系数比将药物直接应用于皮肤表面时估计的扩散系数大一个数量级。溶解速率常数受聚合物基质浓度的影响。