Simvastatin and Captopril Combined Transdermal Delivery System for Controlling Blood Pressure and Fat: Design, Characterization, and In Vivo Pharmacokinetic Evaluation

Q1 Mathematics

Applied Sciences Pub Date : 2024-10-08 DOI:10.3390/app14199092

Ya-jing Ni, Run-jia Wang, Zhao Liu, Li-hui Xiao, Yan‐qiang Liu

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引用次数: 1

Abstract

We developed a sustained-release transdermal drug delivery system (TDDS) containing simvastatin (SIM) and captopril (CAP) to treat hypertension and hyperlipidemia and overcome treatment drawbacks, including significant liver first-pass effects, low bioavailability, and the short half-life of SIM and CAP oral tablets. We used a transdermal diffusion meter to preselect the formula of the SIM-CAP TDDS. Based on in vitro permeation experiments, we optimized the formula of the SIM-CAP TDDS to include 24% SIM, 24% CAP, 34% polyvinyl alcohol (PVA), 16% oleic acid (OA)–azone, and 2% polyacrylic acid resin II. We evaluated the optimized SIM-CAP TDDS formula by its appearance, stability, stickiness, drug content, in vivo pharmacokinetics, and skin irritation tests. The results indicated that the patch had good stability and stickiness. The SIM and CAP contents were 5.02 ± 0.41 mg/cm2 in the 1 cm2 SIM-CAP TDDS. The pharmacokinetic results indicated that the system continuously released SIM and CAP for 24 h and significantly enhanced their bioavailability, with a higher area under the curve. The SIM-CAP TDDS exhibits a sustained-release effect with good characteristics and pharmacokinetics. And it is safe and has no irritating effects on the skin; therefore, it is an ideal formulation.

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辛伐他汀和卡托普利联合经皮给药系统控制血压和脂肪：设计、表征和体内药代动力学评价

我们开发了一种含有辛伐他汀（SIM）和卡托普利（CAP）的缓释经皮给药系统（TDDS）来治疗高血压和高血脂，并克服了治疗的缺点，包括显著的肝脏首过效应、低生物利用度以及SIM和CAP口服片剂半衰期短。我们使用透皮扩散仪预先选择SIM-CAP TDDS的配方。通过体外渗透实验，优化了SIM-CAP TDDS的配方，包括24% SIM、24% CAP、34%聚乙烯醇（PVA）、16%油酸(OA) -偶氮酮、2%聚丙烯酸树脂II。我们通过外观、稳定性、黏性、药物含量、体内药代动力学和皮肤刺激试验对优化后的SIM-CAP TDDS配方进行评价。结果表明，该贴片具有良好的稳定性和黏性。在1 cm2的SIM-CAP TDDS中，SIM和CAP含量为5.02±0.41 mg/cm2。药动学结果表明，该体系可连续释放SIM和CAP 24 h，显著提高其生物利用度，且曲线下面积增大。SIM-CAP TDDS具有良好的缓释特性和药代动力学。它是安全的，对皮肤没有刺激作用；因此，它是一个理想的配方。

本文章由计算机程序翻译，如有差异，请以英文原文为准。

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来源期刊

Applied Sciences Mathematics-Applied Mathematics

CiteScore

6.40

自引率

0.00%

发文量

审稿时长

11 weeks

期刊介绍： APPS is an international journal. APPS covers a wide spectrum of pure and applied mathematics in science and technology, promoting especially papers presented at Carpato-Balkan meetings. The Editorial Board of APPS takes a very active role in selecting and refereeing papers, ensuring the best quality of contemporary mathematics and its applications. APPS is abstracted in Zentralblatt für Mathematik. The APPS journal uses Double blind peer review.