Bahri-Najafi Rahim, Mostafavi Abolfazl, Tavakoli Naser, Taymouri Somayeh, Shahraki Mohammad-Mehdi
Department of Pharmaceutics and Novel Drug Delivery Systems Research Center, School of Pharmacy and Pharmaceutical Science, Isfahan University of Medical Science, Isfahan, I.R. Iran.
Department of Pharmaceutics, School of Pharmacy and Pharmaceutical Science, Isfahan University of Medical Science, Isfahan, I.R. Iran.
Res Pharm Sci. 2017 Apr;12(2):128-136. doi: 10.4103/1735-5362.202451.
In the current study, floating dosage form containing acyclovir was developed to increase its oral bioavailability. Effervescent floating tablets containing 200 mg acyclovir were prepared by direct compression method with three different rate controlling polymers including Hydroxypropyl methylcellulose K4M, Carbapol 934, and Polyvinylpyrrolidone. Optimized formulation showed good floating properties and drug release characteristics with mean dissolution time and dissolution efficacy of about 4.76 h and 54.33%, respectively. X-ray radiography exhibited that the tablet would reside in the stomach for about 5 ± 0.7 h. After oral administration of floating tablet containing 200 mg acyclovir, the , and AUC of optimized gastroretentive formulation were found to be 551 ± 141 ng/mL, 2.75 ± 0.25 h and 3761 ± 909.6 ng/mL/h, respectively.
在当前研究中，开发了含阿昔洛韦的漂浮剂型以提高其口服生物利用度。采用直接压片法，使用三种不同的控释聚合物（包括羟丙基甲基纤维素K4M、卡波姆934和聚乙烯吡咯烷酮）制备了含200mg阿昔洛韦的泡腾漂浮片。优化后的制剂表现出良好的漂浮性能和药物释放特性，平均溶出时间和约54.33%的溶出效率分别约为4.76小时。X射线造影显示该片剂将在胃中停留约5±0.7小时。口服含200mg阿昔洛韦的漂浮片后，优化的胃滞留制剂的Cmax、Tmax和AUC分别为551±141ng/mL、2.75±0.25小时和3761±909.6ng/mL/h。
