用于靶向胃部 H. pylori 的双重药物递送系统:载阿莫西林的 Carbopol®纳米球的制备和体外特性研究。

Dual drug delivery system for targeting H. pylori in the stomach: preparation and in vitro characterization of amoxicillin-loaded Carbopol® nanospheres.

机构信息

Department of Pharmaceutical Sciences, College of Clinical Pharmacy, King Faisal University, Al-Asha, Saudi Arabia.

出版信息

Int J Nanomedicine. 2012;7:4787-96. doi: 10.2147/IJN.S34312. Epub 2012 Sep 4.

Abstract

BACKGROUND AND METHODS

A dual (immediate/sustained-release) oral amoxicillin suspension was developed as a new dosage form to eradicate Helicobacter pylori. Carbopol®-loaded amoxicillin nanospheres could bind with the mucosa after delivery to the stomach and could increase the efficiency of the drug, providing both an immediate and a sustained action.

RESULTS

The objective of this research was to develop amoxicillin nanospheres using a spray-drying technique and to investigate such features as their particle size, drug content, percentage yield, surface morphology, in vitro release, and stability. The nanospheres had a particle size range of 280-320 nm after optimizing the preparation method using a central composite design. The drug content and percentage yield was 85.3% ± 0.7% and 92.8% ± 0.9%, respectively. The in vitro release profile of the amoxicillin nanospheres was consistent with a Korsmeyer-Peppas pattern, and the release after one hour was 19%, while for the original drug, amoxicillin, under the same conditions, 90% was released in the first 30 minutes.

CONCLUSION

The nanospheres used in this study enabled controlled release of amoxicillin over an extended period of time for up to 12 hours and the formulation was stable for 12 months.

摘要

背景与方法

为根除幽门螺杆菌,我们研发了一种新型的双(速释/缓释)口服阿莫西林混悬剂。载有 Carbopol®的阿莫西林纳米球在进入胃部后能够黏附在黏膜上,提高药物效率,发挥即时和持续的作用。

结果

本研究旨在采用喷雾干燥技术开发阿莫西林纳米球,并考察其粒径、药物含量、收率、表面形态、体外释放和稳定性等特征。通过中心复合设计优化制备方法后,纳米球的粒径范围为 280-320nm。药物含量和收率分别为 85.3%±0.7%和 92.8%±0.9%。阿莫西林纳米球的体外释放曲线符合 Korsmeyer-Peppas 模式,1 小时的释放量为 19%,而在相同条件下,原药阿莫西林在前 30 分钟内释放了 90%。

结论

本研究中的纳米球能够在 12 小时内实现阿莫西林的控释,并且制剂在 12 个月内稳定。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/6765/3435120/856132c3c090/ijn-7-4787f1.jpg

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