难溶性药物新型速崩片的研究进展

Research Progress in Novel Rapidly Disintegrating Tablets of Insoluble Drugs

难溶性药物由于其溶解度低,导致吸收差,生物利用度低,临床应用受到很大局限。运用各种增溶技术,增加难溶性药物的溶解度,进而提高其生物利用度十分必要。然而现有的增溶技术常常会造成增溶后含药量低、粘度高等问题,容易造成服用量的增大以及制剂困难。速崩片可通过局部快速释放达到提高患者顺应性以及增溶的目的。本文针对近年来出现的难溶性药物速崩片增溶技术,综述了固体分散体速崩片、包合物速崩片、乳剂冻干片、自微乳分散片、纳米混悬剂冻干片、微丸速崩片、水分散体冻干片等制剂新技术在增加难溶性药物溶解度、改善生物利用度、提高患者用药依从性等方面的应用。

The insoluble drugs with low solubility have poor absorption and low bioavailability, which limit their clinical applica- tion. It is necessary to increase the solubility of poorly soluble drugs using diverse solubilization techniques in order to enhance their bioavailability. However, the existing solubilization techniques often result in lower drug loading and higher viscosity, which increase the dose and cause the preparation difficulties. Rapidly disintegrating tablets can make local quick drug release, which results in the improvement of medication compliance and the enhancement of solubilization effect. The study focused on the techniques such as solid dispersion rapidly disintegrating tablets, clathrate rapidly disintegrating tablets, emulsion freeze-dried tablets, self microemulsion dis- persible tablets, nano-suspension lyophilized tablets, pellets rapidly disintegrating tablet, and freeze-dried aqueous dispersion tablets, which all show the abilities of improving the solubility of poorly soluble drugs, bioavailability, patient medication compliance and so on.