Pharmaceutics and Pharmaceutical Technology Department, Faculty of Pharmacy for Girls, Al-Azhar University, Cairo, Egypt.
Design Workshops Department, Faculty of Applied Sciences and Arts, The German University in Cairo, Cairo, Egypt.
AAPS PharmSciTech. 2023 Jun 1;24(5):127. doi: 10.1208/s12249-023-02578-9.
Mosapride citrate (MC) is a poorly soluble short half-life drug with more pronounced absorption in the stomach. The present study aimed to incorporate MC co-crystals with enhanced solubility into 3D-printed floating tablets. MC co-crystals were prepared via the green method using Saccharin sod. as a co-former at a (1:1) molar ratio. The prepared co-crystals were assessed for solubility, FTIR, thermal behavior, and SEM. Then, it was incorporated into zero % infill 3D-printed tablets of different configurations at two thickness levels by the FDM printing technique. Printed tablets were evaluated for dimensions, weight deviation, friability, and in vitro floating behavior. Drug release and kinetic of the MC release were also assessed. Solubility study of the co-crystals showed a significant (p value < 0.05) increased solubility over pure MC. FTIR and thermal behavior confirmed hydrogen bonding formation during co-crystallization. The obstructed particles had an erratic protrusion form, similar to a nodule, as illustrated by SEM. The printed tablets showed acceptable physicochemical properties. Tablets floated for about ≥ 12 h without floating lag time. In vitro drug release exhibited variable extended release profiles with different lag times depending on the configuration indicating that the tablet's wall thickness and surface area were the factors manipulated to control drug release. Kinetic analysis of the release data displayed intermediate kinetics between zero-order and diffusional kinetics. The intragastric extended release profile for MC co-crystals of improved solubility could be successfully, economically, and quickly developed utilizing the 3D printing technique.
枸橼酸莫沙必利（MC）是一种水溶性差、半衰期短的药物，在胃中吸收更明显。本研究旨在将具有增强溶解性的 MC 共晶体纳入 3D 打印漂浮片剂中。MC 共晶体通过绿色方法使用糖精钠作为共晶形成剂以 1:1 摩尔比制备。对所制备的共晶体进行了溶解度、FTIR、热行为和 SEM 的评估。然后，通过 FDM 打印技术将其以两种厚度水平的不同构型纳入零填充 3D 打印片剂中。对打印片剂进行了尺寸、重量偏差、脆性和体外漂浮行为的评估。还评估了药物释放和 MC 释放的动力学。共晶体的溶解度研究表明，与纯 MC 相比，溶解度显著提高（p 值 < 0.05）。FTIR 和热行为证实了共晶化过程中氢键的形成。受阻颗粒具有不规则的突起形式，类似于结节，SEM 也证实了这一点。打印片剂表现出可接受的物理化学性质。片剂漂浮时间约为 ≥ 12 小时，无漂浮滞后时间。体外药物释放呈现出不同的延释释放曲线，具有不同的滞后时间，这表明片剂的壁厚和表面积是控制药物释放的因素。释放数据的动力学分析显示，释放动力学介于零级和扩散动力学之间。利用 3D 打印技术，可以成功、经济、快速地开发出具有改善溶解性的 MC 共晶体的胃内延释释放曲线。
