期刊
INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES
卷 23, 期 21, 页码 -出版社
MDPI
DOI: 10.3390/ijms232113051
关键词
transdermal delivery; losartan potassium; verapamil hydrochloride; pharmacokinetics; skin irritation
资金
- Natural Science Foundation of Tianjin City [20JCYBJC01370]
- Fundamental Research Funds for the Central Universities of Nankai University [BE123081]
- University-Enterprise Cooperation Project [F1023741]
This study developed a sustained-release transdermal delivery system containing losartan potassium and verapamil hydrochloride, and evaluated its pharmacokinetics and skin irritation in vitro and in vivo. The results showed that the system continuously released the drugs for 24 hours and had good characteristics and pharmacokinetics, making it an ideal formulation.
In this study, we developed a sustained-release transdermal delivery system containing losartan potassium (LP) and verapamil hydrochloride (VPH). LP and VPH have low bioavailability and long half-life. Therefore, the development of an optimum administration mode is necessary to overcome these drawbacks and enhance the antihypertensive effect. A transdermal diffusion meter was used to determine the optimal formulation of LP-VPH transdermal drug delivery systems (TDDS). Based on in vitro results, a sustained-release patch was prepared. Physical characteristics, including quality, stickiness, and appearance, were evaluated in vitro, while pharmacokinetics and skin irritation were evaluated in vivo. The results showed that 8.3% polyvinyl alcohol, 74.7% polyvinylpyrrolidone K30, 12% oleic acid-azone, and 5% polyacrylic acid resin II provided an optimized TDDS product for effective administration of LP and VPH. Furthermore, in vitro and in vivo release tests showed that the system continuously released LP and VPH for 24 h. The pharmacokinetic results indicated that although the maximum concentration was lower, both the area under the curve from 0-time and the mean residence time of the prepared patch were significantly higher than those of the oral preparations. Furthermore, the prepared LP-VPH transdermal patch showed good stability and no skin irritation. The developed LP-VPH TDDS showed a sustained-release effect and good characteristics and pharmacokinetics; therefore, it is an ideal formulation.
作者
我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。
推荐
暂无数据