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第一行主标题 请输入要描述的内容进行内容补充请输入 - Salt and Solid State Screening 第一行主标题 请输入要描述的内容进行内容补充请输入 - Assessment of Drug Efficacy 第一行主标题 请输入要描述的内容进行内容补充请输入 - Evaluation of Eutectic Systems 第一行主标题 请输入要描述的内容进行内容补充请输入 - Development of Co-crystal |
Development of Amorphous form Reasonable design of amorphous solid dispersion Stable, efficient, and industrializable Amorphous form is the most significant enhancement in efficacy among metastable crystal forms. Amorphous drugs exhibit high surface free energy and are prone to crystallization during storage and dissolution, potentially losing advantages over crystalline formulations. Our company’s latest generation solid dispersion technology achieves nearly infinite stability for amorphous drug systems, driving commercialization of amorphous drugs. Leveraging extensive experience in amorphous preparation and analysis, we offer comprehensive services tailored to your amorphous-related projects. To stabilize the amorphous state of drugs and prevent crystallization in both solid-state and aqueous phases, excipients are typically introduced into multi-component amorphous systems (amorphous solid dispersions). This approach enhances the stability of amorphous drugs while improving the functionality and processability of their formulations. It can address issues such as viscosity, powder flowability, and hygroscopicity. Figure: Preparation target of amorphous solid dispersion Properties of amorphous products Amorphous materials exhibit unique characteristics due to their disordered state compared to crystalline forms: ■ Amorphous forms typically demonstrate significantly higher apparent solubility than crystalline forms. When solutes in supersaturated solutions begin to crystallize and reach dynamic equilibrium, the solubility can increase dramatically (often more than 10-fold). Therefore, utilizing amorphous forms can significantly enhance the bioavailability of drugs. ■ Due to the structural disorder of amorphous materials, their mechanical properties can differ noticeably from their crystalline counterparts. Experimental findings indicate that tablets formed from powders of amorphous drugs can be more brittle under certain conditions compared to tablets made from crystalline drugs.Amorphous materials also exhibit higher hygroscopicity, absorbing more moisture in typical environmental conditions than crystalline forms. ■ Amorphous forms have very strong water absorption properties, and in ordinary environments, amorphous forms absorb more water than crystalline forms. Typically, marketed amorphous solid dispersions refer to single-phase dispersions where the drug is amorphously dispersed in a solid carrier. Amorphous drugs in such systems exhibit higher apparent solubility compared to crystalline drugs. Additionally, the solid carrier enhances drug dispersion, increasing the drug's dissolution surface area and improving the dissolution rate of poorly soluble drugs, thereby further enhancing their oral bioavailability. Advantages of amorphous drugs: High solubility, fast dissolution rate, and high bioavailability can improve the water solubility and bioavailability of poorly soluble drugs. |