缬沙坦与氢氯噻嗪药物-药物共晶的制备与表征

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Abstract：Valsartan-hydrochlorothiazide co-crystals were prepared bya liquid-asisted miling method to improve the dissolution performanceof the insoluble drugs.Samples of cocrystal，valsartan，hydrochlorothiazide powders and valsartan-hydrochlorothiazide mixtures werecharacterizedbypowder X-ray diffraction，Raman spectroscopy，infrared spectroscopy and other methods.The in vitro dissolution properties of Active Pharmaceutical Ingredient（API）in the abovefour samples were analyzed by high performance liquid chromatography.Theresults confirmthe cocrystal formationof valsartanandhydrochlorothiazide，andshowthatthedissolutionperformanceof theAPIsinthecocrystal is significantly improved whencomparedwith thebulk drugs.The two APIs hadatendencytodissolve synergistically in the cocrystal.The results provide a new option for the co-administration of valsartanand hydrochlorothiazide.

Key words：drug-drug cocrystal；cardiovascular disease；hydrochlorothiazid；valsartan；cumulative dissolutioninvitro

1前言

药物-药物共晶指2种或2种以上药物活性分子（APIs）以一定的化学计量比，通过诸如氢键、卤键、范德华力、 π-π 堆叠作用等非共价相互作用而形成的新晶体[1-3]。（剩余11821字）