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用于酮洛芬经皮递送的贴剂中含药贴剂的设计与评价

Design and evaluation of a drug-in-adhesive patch for the transdermal delivery of ketoprofen.

作者信息

Bai Ran, Yang Miaomiao, Sun Xiaoyang, Hu Yanqin, Chen Kaiwen, Cui Xiaoyue, Sun Yinghua, Zhang Tianhong

机构信息

Wuya College of Innovation, Shenyang Pharmaceutical University, 103 Wenhua Road, Shenyang, 110016, China.

School of pharmacy, Shenyang Pharmaceutical University, 103 Wenhua Road, Shenyang, 110016, China.

出版信息

Drug Deliv Transl Res. 2025 May;15(5):1685-1692. doi: 10.1007/s13346-024-01703-w. Epub 2024 Sep 6.

Abstract

The purpose of this study was to design a drug-in-adhesive (DIA) patch for transdermal delivery of ketoprofen, using hot-melt pressure-sensitive adhesive as the matrix of the patch. The adhesion properties and skin permeation of the patches were examined, and in vivo pharmacokinetics and tissue distribution of patches were evaluated. The novel ketoprofen patch with high adhesion was prepared by holt-melt method. The effects of different percentages of L-menthol on in vitro permeation were screened, 3% was added as the amount of permeation enhancer and the 24 h cumulative permeation amount(277.46 ± 15.58 µg/cm) comparable to that of commercial patch MOHRUS(279.74 ± 29.23 µg/cm). Pharmacokinetic and the tissue distribution study showed no matter in plasma, muscle or skin, the drug concentration of self-made ketoprofen patch was equivalent to that of commercial patch. These data indicated that the self-made patch provided a new reference for the development of ketoprofen dosage forms and promising alternative strategy for analgesic treatment.

摘要

本研究的目的是设计一种用于酮洛芬经皮给药的贴剂(药物-胶粘剂贴剂,DIA),使用热熔压敏胶粘剂作为贴剂的基质。研究了贴剂的粘附性能和皮肤渗透性,并评估了贴剂的体内药代动力学和组织分布。采用热熔法制备了具有高粘附性的新型酮洛芬贴剂。筛选了不同比例的L-薄荷醇对体外渗透的影响,添加3%作为渗透促进剂的用量,其24小时累积渗透量(277.46±15.58μg/cm)与市售贴剂MOHRUS(279.74±29.23μg/cm)相当。药代动力学和组织分布研究表明,自制酮洛芬贴剂在血浆、肌肉或皮肤中的药物浓度与市售贴剂相当。这些数据表明,自制贴剂为酮洛芬剂型的开发提供了新的参考,是镇痛治疗的一种有前景的替代策略。

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