Department of Pharmaceutics of Drug Delivery, University of Mississippi, University Park, Oxford, Mississippi, USA.
Pharmaceutics, KLE University's College of Pharmacy, Bangalore, Karnataka, India.
AAPS PharmSciTech. 2020 Oct 6;21(7):273. doi: 10.1208/s12249-020-01808-8.
The use of hot-melt extrusion (HME) technique in the preparation of semi-solid products offers several advantages over conventional processes. However, the optimization of the technique for preparation of semi-solid pharmaceuticals is challenging due to involvement of ingredients with different physical properties. Hence, a simple tool to optimize the mixing of ingredients that results in a target ratio and drug content uniformity is utmost important. In this study, a handheld colorimeter has been explored to optimize the process variables of twin screw processor for preparation of hydrophilic PEG-based ointment. The process parameters which were optimized with use of handheld colorimeter have been used for preparation of polyethylene glycol-based metronidazole ointment. The metronidazole ointment prepared by twin screw processor was compared with commercially available metronidazole gel for in vitro release testing and ex vivo permeation. The flux, ex vivo bioavailability, and T of polyethylene glycol-based metronidazole ointment was found to be similar to that of marketed metronidazole gel.
热熔挤出（HME）技术在半固体产品的制备中具有优于传统工艺的几个优点。然而，由于涉及具有不同物理性质的成分，因此优化用于制备半固体药物的技术具有挑战性。因此，需要一种简单的工具来优化混合成分，以达到目标比例和药物含量均匀性。在这项研究中，探索了手持分光光度计来优化双螺杆处理器制备亲水性 PEG 基软膏的工艺变量。使用手持分光光度计优化的工艺参数已用于制备基于聚乙二醇的甲硝唑软膏。通过双螺杆处理器制备的甲硝唑软膏与市售甲硝唑凝胶进行了体外释放试验和离体渗透试验比较。基于聚乙二醇的甲硝唑软膏的通量、离体生物利用度和 T 发现与市售甲硝唑凝胶相似。
