Faculty of Pharmaceutical Science, Burapha University, Chonburi, 20131, Thailand.
Pharmaceutical Biopolymer Group (PBiG), Faculty of Pharmacy, Silpakorn University, Nakhon Pathom, 73000, Thailand.
AAPS PharmSciTech. 2016 Jun;17(3):693-9. doi: 10.1208/s12249-015-0398-6. Epub 2015 Aug 28.
The present study aims to develop floating drug delivery system by sublimation of ammonium carbonate (AMC). The core tablets contain a model drug, hydrochlorothiazide, and various levels (i.e., 0-50% w/w) of AMC. The tablets were then coated with different amounts of the polyacrylate polymers (i.e., Eudragit® RL100, Eudragit® RS100, and the mixture of Eudragit® RL100 and Eudragit® RS100 at 1:1 ratio). The coated tablets were kept at ambient temperature (25°C) or cured at 70°C for 12 h before further investigation. The floating and drug release behaviors of the tablets were performed in simulated gastric fluid USP without pepsin at 37°C. The results showed that high amount of AMC induced the floating of the tablets. The coated tablets containing 40 and 50% AMC floated longer than 8 h with a time-to-float of about 3 min. The sublimation of AMC from the core tablets decreased the density of system, causing floating of the tablets. The tablets coated with Eudragit® RL100 floated at a faster rate than those of Eudragit® RS100. Even the coating level of polymer did not influence the time-to-float and floating time of coated tablets containing the same amount of AMC, the drug release from the tablets coated with higher coating level of polymer showed slower drug release. The results suggested that the sublimation technique using AMC is promising for the development of floating drug delivery system.
本研究旨在通过碳酸铵（AMC）的升华来开发漂浮型药物传递系统。核心片剂包含一种模型药物氢氯噻嗪和各种浓度（即 0-50%w/w）的 AMC。然后，将片剂用不同量的聚丙烯酸酯聚合物（即 Eudragit®RL100、Eudragit®RS100 以及 Eudragit®RL100 和 Eudragit®RS100 以 1:1 比例的混合物）进行包衣。将包衣后的片剂在环境温度（25°C）下保存或在 70°C 下固化 12 小时，然后再进行进一步的研究。在 37°C 的无胃蛋白酶的模拟胃液 USP 中进行片剂的漂浮和药物释放行为的研究。结果表明，高浓度的 AMC 会诱导片剂的漂浮。含有 40%和 50%AMC 的包衣片剂的漂浮时间超过 8 小时，浮起时间约为 3 分钟。核心片剂中 AMC 的升华降低了系统的密度，导致片剂漂浮。用 Eudragit®RL100 包衣的片剂的漂浮速度比用 Eudragit®RS100 包衣的片剂快。即使聚合物的包衣水平不影响含有相同 AMC 量的包衣片剂的浮起时间和漂浮时间，用较高包衣水平聚合物包衣的片剂的药物释放也显示出较慢的药物释放。结果表明，使用 AMC 的升华技术有望开发漂浮型药物传递系统。
