Abstract

Repaglinide (RPG, antidiabetic) and Diltiazem HCL (DIL, antihypertensive) loaded ethyl cellulose (EC) nanoparticles were prepared by the spray drying process using Placket Burman Design (PBD). The amount of EC (A, mg), Methanol (B, ml), Inlet temperature (C, ^OC), Feed rate (D, rpm), Nozzle diameter (E, mm) and Aspiration (F, rpm) were considered independent variables while EE of RPG (Y1) and EE of DIL (Y2) were selected as dependent variables. The optimized DIL and RPG loaded EC nanoparticles were further used for the development of oral fast disintegrating sustained release tablets by direct compression method. The tablets were evaluated for weight variation, thickness, hardness, disintegration time, friability and dissolution test. FTIR study showed no chemical interaction between drug and polymer. Scanning electron microscope showed spherical as well as oval shape and discrete nature of both nanoparticles. The physical parameters of oral fast disintegrating tablets developed with optimized formulation of drug loaded nanoparticles were found within the range. Drug loaded nanoparticles as well as oral fast disintegrating tablets showed very good sustained release behavior.

摘要

使用 Placket Burman Design (PBD) 通过喷雾干燥工艺制备了载有瑞格列奈 (RPG，抗糖尿病药) 和盐酸地尔硫卓 (DIL，抗高血压药) 的乙基纤维素 (EC) 纳米颗粒。EC的量（A，mg），甲醇（B，ml），入口温度（C，^OC)、进料速率 (D, rpm)、喷嘴直径 (E, mm) 和吸气 (F, rpm) 被视为自变量，而 RPG 的 EE (Y1) 和 DIL (Y2) 的 EE 被选为因变量。优化的 DIL 和 RPG 负载 EC 纳米粒进一步用于通过直接压制法开发口腔速崩缓释片。评估片剂的重量变化、厚度、硬度、崩解时间、脆性和溶出度测试。FTIR 研究表明药物和聚合物之间没有化学相互作用。扫描电子显微镜显示两种纳米粒子的球形和椭圆形以及离散性质。优化载药纳米粒配方研制的口腔速崩片的物理参数均在该范围内。