Heinrich-Heine-Universitaet Duesseldorf, Institute of Pharmaceutics and Biopharmaceutics, Universitaetsstraße 1, 40225 Duesseldorf, Germany.
Heinrich-Heine-Universitaet Duesseldorf, Institute of Pharmaceutics and Biopharmaceutics, Universitaetsstraße 1, 40225 Duesseldorf, Germany.
Eur J Pharm Biopharm. 2021 Feb;159:170-176. doi: 10.1016/j.ejpb.2021.01.004. Epub 2021 Jan 15.
Metformin hydrochloride is a drug used in the treatment of type 2 diabetes and is administered orally using high-dose tablets. Due to its poor flowability and agglomeration during storage, metformin is commonly processed using an intermediate step such as granulation before the material can be compressed into tablets. Spherical crystallization is a method, which can be used to improve the flowability and tabletability of drugs and excipients. This study set out to create a simple quasi-emulsion solvent-diffusion crystallization method for the highly water-soluble metformin hydrochloride using a single solvent and antisolvent with surfactants so that a direct compression of the material can be realized. Hollow, spherical agglomerates of metformin with good flowability and reduced storage agglomeration were successfully produced using this method. The effect of different surfactants (HPMC, polysorbate 80 and sorbitane monooleate) used to stabilize the transient emulsion during crystallization as well as different system parameters on the morphology, flowability of the particles and storage agglomeration was analyzed.
盐酸二甲双胍是一种用于治疗 2 型糖尿病的药物，以高剂量片剂的形式口服给药。由于其在储存过程中流动性差且易于结块，因此在将其压缩成片剂之前，通常需要经过造粒等中间步骤进行处理。球形结晶是一种可以改善药物和赋形剂流动性和可压性的方法。本研究旨在开发一种简单的准乳液溶剂扩散结晶方法，使用单一溶剂和含有表面活性剂的反溶剂来高度水溶性的盐酸二甲双胍，从而可以直接对该物质进行压缩。使用该方法成功制备出具有良好流动性和减少储存结块的空心、球形盐酸二甲双胍团聚体。分析了在结晶过程中用于稳定瞬时乳液的不同表面活性剂（HPMC、聚山梨酯 80 和山梨坦单油酸酯）以及不同系统参数对颗粒形态、流动性和储存结块的影响。
