Department of Pharmaceutical Engineering and Drug Delivery Science, Graduate School of Pharmaceutical Sciences, University of Shizuoka, 52-1 Yada, Suruga-Ku, Shizuoka-Shi, Shizuoka, 422-8526, Japan.
Department of Resarch, Division of Resarch & Development, Dojin Iyaku-Kako Co., Ltd., 8-1, Higashi Nakakawara, Senoue-Machi, Fukushima-Shi, Fukushima, 960-0101, Japan.
AAPS PharmSciTech. 2024 Oct 15;25(7):244. doi: 10.1208/s12249-024-02959-8.
Understanding the relationship between the release characteristics of the active ingredient in the tape formulation and the pharmaceutical characteristics of the adhesive layer can optimize therapeutic efficacy and improve patient adherence. This study aimed to clarify the effect of liquid paraffine (LP)/styrene-isoprene-styrene (SIS) triblock copolymer ratio on pressure-sensitive adhesive (PSA) formulation properties, such as adhesive properties and drug release, with a certain amount of diclofenac sodium (DFS) and tackifier. The effects of changes in PSA composition in DFS-containing tape formulations on adhesive and drug release properties were evaluated. The viscoelasticity results showed rigid gel-like behavior at low angular frequencies regardless of the LP/SIS ratio, and deformable gel-like behavior at high angular frequencies, with a maximum plasticizing effect of LP up to an LP/SIS ratio of 3.7. The peel adhesion test results showed that peel adhesion was not affected, but indicated a decreasing trend by increasing the LP/SIS ratio in the presence of DFS. Drug release test results showed that DFS release increased up to 24 h for LP/SIS ratios of up to 3.7, but decreased when the LP/SIS ratio was 6. The results of the drug permeation tests were similar to those of the drug release tests. In conclusion, it is possible to change the drug release properties by changing the amount of LP in the tape formulation; however, no definitive correlation was found between the adhesive and drug release properties.
了解贴剂配方中活性成分的释放特性与压敏胶层的药物特性之间的关系，可以优化治疗效果并提高患者的顺应性。本研究旨在阐明一定量的双氯芬酸钠（DFS）和增粘剂的情况下，液体石蜡（LP）/苯乙烯-异戊二烯-苯乙烯（SIS）嵌段共聚物比对压敏胶（PSA）配方性能（如粘性和药物释放）的影响。评估了含 DFS 的贴剂配方中 PSA 组成变化对粘性和药物释放性能的影响。粘弹性结果表明，无论 LP/SIS 比例如何，在低角频率下均表现出刚性凝胶样行为，而在高角频率下表现出可变形凝胶样行为，LP 的最大塑化作用可达 LP/SIS 比为 3.7。剥离附着力测试结果表明，剥离附着力不受影响，但在存在 DFS 的情况下，随着 LP/SIS 比例的增加，呈现出下降的趋势。药物释放试验结果表明，LP/SIS 比高达 3.7 时，DFS 的释放持续增加至 24 小时，但当 LP/SIS 比为 6 时，释放减少。药物渗透试验的结果与药物释放试验的结果相似。总之，通过改变贴剂配方中 LP 的用量，可以改变药物释放特性；但是，粘性和药物释放特性之间没有明确的相关性。
