Purpose

The main objective of this present study was the investigation of potential novel transdermal patch technology (TEPI®) delivering ibuprofen as the active pharmaceutical ingredient (API) using a novel poly(ether-urethane)-silicone crosslinked pressure-sensitive adhesive (PSA) as the drug reservoir in a solvent-free manufacturing process.

Methods

The patch was synthesized utilizing the hot-melt crosslinking technique without the addition of solvents at 80 °C in 100% relative humidity. Dissolution and permeation studies performed utilizing diffusion cells and subsequently HPLC validated methods were employed to determine the API content in the acceptor solution. Accelerated stability studies were also performed at 40 °C and 70% relative humidity. The adhesive performance of the fabricated patch was evaluated utilizing loop tack adhesion tests.

Results

In vitro permeation experiments across both Strat-M® and human skin demonstrated that ibuprofen can easily be released from the adhesive matrix and penetrate through the studied membrane. A comparison on the permeation rates of the API across the two membranes indicated that there is not a strong correlation between the obtained data. The presence of chemical enhancers facilitated an increased flux of the API higher than observed in the basic formulation. Initial stability studies of the optimized formulation showed no degradation with respect to the drug content. Adhesion studies were also performed indicating higher values when compared with commercially available products.

Conclusions

The present study demonstrated the fabrication of an ibuprofen patch utilizing a versatile, solvent-free drug delivery platform. Upon optimization of the final system, the resulting patch offers many advantages compared to commercially available formulations including high drug loading (up to 25 wt%), good adhesion, and painless removal leaving no residues on the skin. This PSA offers many advantages over existing adhesive technology.

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中文翻译：

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利用新型无溶剂压敏粘合剂 (PSA) 透皮递送布洛芬：TEPI® 技术。

目的

本研究的主要目的是研究潜在的新型透皮贴剂技术 (TEPI®)，使用新型聚（醚-氨基甲酸酯）-有机硅交联压敏粘合剂 (PSA) 作为活性药物成分 (API) 递送布洛芬。无溶剂制造过程中的药物储存器。

方法

该贴片是在 80 °C 和 100% 相对湿度下使用热熔交联技术在不添加溶剂的情况下合成的。利用扩散池进行的溶解和渗透研究以及随后通过 HPLC 验证的方法来确定受体溶液中的 API 含量。还在 40 °C 和 70% 相对湿度下进行了加速稳定性研究。制造的贴片的粘合性能是利用环粘性粘合测试来评估的。

结果

Strat-M® 和人体皮肤的体外渗透实验表明，布洛芬可以很容易地从粘合剂基质中释放出来并穿透所研究的膜。比较 API 在两种膜上的渗透率表明，获得的数据之间没有很强的相关性。化学增强剂的存在促进了 API 通量的增加，高于在基本配方中观察到的通量。优化配方的初步稳定性研究表明药物含量没有降解。与市售产品相比，还进行了附着力研究，表明其值更高。

结论

本研究展示了利用多功能、无溶剂给药平台制造布洛芬贴剂。在优化最终系统后，所得贴剂与市售配方相比具有许多优势，包括高载药量（高达 25 wt%）、良好的附着力和无痛去除，不会在皮肤上留下残留物。与现有的粘合剂技术相比，这种 PSA 具有许多优势。

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