影响药物玻璃化形成能力的因素及评判方法的研究概况

Survey Research of Influence Factors and Evaluation Methods for Glass-forming Ability of Drugs

目前,诸多药用活性成分由于溶解度低、生物利用度低而未能被开发成药物制剂。因此,提高药物的溶解度和生物利用度是制剂研究的重要挑战。将药物由晶态转变为非晶态,能大幅增加药物的溶解度,从而改善其溶出速度和生物利用度。了解并掌握药物的玻璃化形成能力(即由晶态转变成非晶态的能力)及其影响因素,是判断是否适宜制备非晶态药物的基础。因此,本研究从药物结构、热力学性质、动力学性质和外部环境等方面分析了药物玻璃化形成能力的影响因素,总结了评判药物玻璃化形成能力的方法,以期为非晶态制剂的开发与设计提供帮助。

At present,many active pharmaceutical ingredients have not been developed in formulations due to their low aqueous solubilities,which cause low bioavailabilities of drugs.Therefore,improving the solubility and bioavailability of drugs is an important challenge in preparation research.The transformation of drugs from crystalline state to amorphous state can greatly increase the solubility,resulting in higher dissolution rate and bioavailability.Understanding and mastering the glass-forming ability(GFA)of drugs(namely the transformation ability of a crystalline compound to an amorphous state)and their influence factors are the basis for judging the suitability of preparation of amorphous drugs.Therefore,this review analyzes the influence factors of GFA from the aspects of drug structure,thermodynamic properties,kinetic properties and external environment.The methods to evaluate GFA of drugs are also summarized.It is hoped to provide a reference for the development and design of amorphous preparations.