Strap-on Buoyant Device to Enhance Gastrointestinal Tract Retention of Felodipine Osmotic Pump Tablets

IF 3.4 4区医学 Q2 PHARMACOLOGY & PHARMACY

AAPS PharmSciTech Pub Date : 2024-11-01 DOI:10.1208/s12249-024-02976-7

Qijia Ni, Zeru Li, Libumo Baqing, Tianfu Li, Huipeng Xu, Falan Li, Ningning Peng, Caifen Wang, Jianhua Lu, Zhigang Wang, Kai Wang, Chao Jiang, Li Wu, Ye Yang, Hua Zhou, Yongdong Gu, Jiwen Zhang

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引用次数: 0

Abstract

Osmotic pump systems require prolonged retention time in the stomach to provide enhanced bioavailability and regulated release, which is quite challenging. This study used a three-dimensional printing (3DP) technique combined with a gastro-retentive floating device (GRFD) to extend the retention of the osmotic pump in the stomach and enhance its bioavailability. The strap-on buoyant device was fabricated by stereolithography 3DP and incorporated a felodipine osmotic pump tablet used in clinical practice, which enabled it to float in the stomach or dissolution media without any floating lag time. The components of the device were affixed using a snap-fix mechanism. GRFD dissolution study revealed a notable in vitro floating capability, lasting over 24 h, with a release profile similarity factor f₂ = 65.28 compared to the naked tablet dissolution profile. The pharmacokinetics of felodipine osmotic pump in beagles showed a C_max of 1.893 ng/mL, which increased to 4.511 ng/mL with GRFD. The delivery of an osmotic pump with GRFD enhanced the AUC_0−∞ of felodipine from 10.20 ng/mL·h to 26.54 ng/mL·h. In conclusion, the strap-on buoyant device has been successfully designed to enhance gastrointestinal tract retention of felodipine osmotic pumps and bioavailability in beagles.

Graphical Abstract

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用于增强非洛地平渗透泵片胃肠道滞留的带式浮力装置

渗透泵系统需要延长在胃中的滞留时间，以提高生物利用度和调节释放，这具有相当大的挑战性。本研究采用三维打印（3DP）技术，结合胃保留浮动装置（GRFD），延长渗透泵在胃中的保留时间，提高其生物利用度。这种带式浮力装置是通过立体光刻 3DP 技术制作而成的，并结合了临床上使用的非洛地平渗透泵片剂，使其能够漂浮在胃或溶解介质中，而不会有任何漂浮滞后时间。该装置的各组件采用卡扣固定机制固定。GRFD 溶出研究表明，该装置具有显著的体外漂浮能力，可持续 24 小时以上，与裸片溶出曲线相比，其释放曲线相似系数 f2 = 65.28。小猎犬体内非洛地平渗透泵的药代动力学显示，Cmax 为 1.893 纳克/毫升，使用 GRFD 后增加到 4.511 纳克/毫升。使用 GRFD 输送渗透泵后，非洛地平的 AUC0-∞ 从 10.20 纳克/毫升-小时提高到 26.54 纳克/毫升-小时。总之，捆绑式浮力装置的设计成功提高了非洛地平渗透泵在小猎犬胃肠道的滞留率和生物利用度。

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

AAPS PharmSciTech 医学-药学

CiteScore

6.80

自引率

3.00%

发文量

264

审稿时长

2.4 months

期刊介绍： AAPS PharmSciTech is a peer-reviewed, online-only journal committed to serving those pharmaceutical scientists and engineers interested in the research, development, and evaluation of pharmaceutical dosage forms and delivery systems, including drugs derived from biotechnology and the manufacturing science pertaining to the commercialization of such dosage forms. Because of its electronic nature, AAPS PharmSciTech aspires to utilize evolving electronic technology to enable faster and diverse mechanisms of information delivery to its readership. Submission of uninvited expert reviews and research articles are welcomed.