The present invention is heart-benefiting Yixinshu micropill and its preparation process. The heart-benefiting Yixinshu micropill is prepared with ginseng 100-500 weight portions, ophiopogon root 100-500weight portions, schisandra 100-300weight portions, astragalus root 150-450weight portions, red sage 200-600weight portions, Chuanxiong rhizome 100-300weight portions, haw 200-400weight portions, avicel 300-500weight portions, and mannitol 50-200weight portions. It has diameter smaller than 0.05mm, excellent disintegrating and dissolving performance, fast acting, high bioavailability, and other advantages, and possesses functions of promoting blood circulation to disperse blood clots, benefiting qi, nourishing yin, etc.