环维黄杨星D的结构修饰及黄杨宁片的剂型改进研究进展

Reaearch progress on structural modification of cyclovirobuxine D and dosage form improvement of Huangyangning Tablets

环维黄杨星D(cyclovirobuxine D,CVB-D)为小叶黄杨Buxus microphylla及其同属植物的主要活性成分,具有保护心脑血管等多种药理作用。以其为主要成分的临床常用药黄杨宁片对于冠心病和心绞痛具有明确治疗作用。但是,在临床应用过程中发现,黄杨宁片作为一种口服片剂,存在着水溶性差、生物利用度低,在胃肠道内具有多个吸收位点、释药不稳定,难以透过血脑屏障,并具有心脏蓄积及肝肾毒性等缺点。因此,有必要通过结构修饰或剂型改变来解决CBV-D存在的上述问题。对CVB-D的结构修饰及黄杨宁片剂型改进的研究进展进行综述,以期为其进一步的研究开发提供理论依据。

As the main active constituent of Buxus microphylla and Buxus plants,cyclovirobuxine D(CVB-D)has a variety of pharmacological effects such as cardio-cerebrovascular protection.Huangyangning Tablets(黄杨宁片),a commonly used clinical drug with CVB-D as its main ingredient,has a clear therapeutic effect on coronary heart disease and angina pectoris.However,in the process of clinical application,it was discovered that Huangyangning Tablets,as an oral tablet,had the disadvantages of poor water solubility,low bioavailability,multiple absorption sites in the gastrointestinal tract,unstable drug release,difficulty in penetrating the blood-brain barrier,as well as heart accumulation,liver and kidney toxicity,etc.Therefore,it is necessary to solve the above-mentioned problems through structural modification and/or dosage form change.Reaearch progress on structural modification of cyclovirobuxine D and dosage form improvement of Huangyangning Tablets are reviewed in this paper,in order to provide theoretical basis for its further research and development.