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straps-on 浮力装置增强非洛地平渗透泵片在胃肠道中的滞留。

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

机构信息

Anhui University of Chinese Medicine, Hefei, 230000, China.

Yangtze Delta Drug Advanced Research Institute, Nantong, 226133, China.

出版信息

AAPS PharmSciTech. 2024 Nov 1;25(8):260. doi: 10.1208/s12249-024-02976-7.

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 f = 65.28 compared to the naked tablet dissolution profile. The pharmacokinetics of felodipine osmotic pump in beagles showed a C 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 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.

摘要

渗透泵系统需要在胃中长时间滞留,以提供增强的生物利用度和调节释放,这是相当具有挑战性的。本研究采用三维打印(3DP)技术与胃滞留漂浮装置(GRFD)相结合,延长渗透泵在胃中的滞留时间,提高其生物利用度。通过立体光刻 3DP 制造了带式浮力装置,并结合了临床实践中使用的非洛地平渗透泵片剂,使其能够在胃或溶解介质中漂浮,而无需任何漂浮滞后时间。该装置的组件通过快速固定机制固定。GRFD 溶解研究显示出显著的体外漂浮能力,持续超过 24 小时,与裸片溶解曲线的相似因子 f = 65.28。在比格犬中,非洛地平渗透泵的药代动力学显示 C 为 1.893 ng/mL,而使用 GRFD 后增加到 4.511 ng/mL。使用 GRFD 输送渗透泵可将非洛地平的 AUC 从 10.20 ng/mL·h 提高到 26.54 ng/mL·h。总之,成功设计了带式浮力装置,以增强非洛地平渗透泵在胃肠道中的滞留时间和生物利用度。

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