Department of Pharmaceutics, College of Pharmacy, King Khalid University, Greiger, Abha, Kingdom of Saudi Arabia.
Pak J Pharm Sci. 2021 Jul;34(4):1297-1303.
Neratinib is a potent anticancer drug, used for the treatment of breast cancer. It is poorly soluble at higher pH, which tends to minimize the therapeutic effects in the lower GIT leads to its poor bioavailability. An attempt has been made to prepare and develop a novel gastro-retentive system of neratinib to improve the drug bioavailability in the GIT by enhancing the gastric retention time. The floating matrix tablets were prepared by various proportions of carbopol 940, micro-crystalline cellulose (MCC) and ethyl cellulose (EC), sodium bicarbonate (NaHCO) as gas forming agent, by direct compression. The formulation mixture was assessed for pre and post compression test, lag time, in-vitro floating, FTIR, water uptake/swelling index, in vitro and kinetic release studies. The findings revealed that, the parameters of compression (pre and post) were within USP limits. The floating tablets swelled well and floated for more than 24h, with less than 120 seconds of buoyancy lag time. The optimized formulation F3 showed sustained release up to 12h; a non-Fickian mechanism. Therefore, all the results and findings have shown that developed neratinib floating matrix system is a promising approach as a drug delivery system and application in the treatment of breast cancer.
奈拉替尼是一种有效的抗癌药物，用于治疗乳腺癌。它在较高的 pH 值下溶解度较差，这往往会降低其在胃肠道下部的治疗效果，导致其生物利用度较差。人们试图制备和开发一种新型的奈拉替尼胃滞留系统，通过延长胃滞留时间来提高药物在胃肠道中的生物利用度。通过直接压缩，用不同比例的卡波姆 940、微晶纤维素 (MCC) 和乙基纤维素 (EC)、碳酸氢钠 (NaHCO) 作为气体形成剂来制备漂浮基质片。对制剂混合物进行了预压和抗压测试、滞后时间、体外漂浮、FTIR、吸水率/溶胀指数、体外和动力学释放研究。结果表明，压缩（预压和抗压）参数均在 USP 范围内。漂浮片在水中溶胀良好，能漂浮 24 小时以上，漂浮滞后时间小于 120 秒。优化后的配方 F3 表现出长达 12 小时的持续释放；一种非菲克扩散机制。因此，所有的结果和发现都表明，开发的奈拉替尼漂浮基质系统是一种很有前途的药物传递系统，可应用于乳腺癌的治疗。
