Breviscapine has the function of expanding cerebrovascular, reducing cerebrovascular resistance, increasing cerebral blood flow, improving microcirculation, and anti-platelet aggregation. Therefore, it can be used for the treatment of ischemic cerebrovascular diseases, such as cerebral thrombosis, cerebral embolism, cerebral hemorrhage and other sequelae caused by paralysis patients, with good curative effect.
Breviscapine is a water-insoluble, oil-insoluble and weak acidic drug. Its solubility in organic solvents is very low, and its oil/water partition coefficient is low when it dissolves in acidic solution. Studies have shown that breviscapine can be absorbed quickly in vivo after intravenous administration, with short half-life, rapid elimination and short maintenance time of effective concentration. Oral tablets have low bioavailability and almost no absorption. It is necessary to use large doses of oral tablets for multiple doses in order to achieve therapeutic purposes.
Hydroxypropyl beta-cyclodextrin is hydrophobic in its tubular structure, so hydrophobic guest molecules are easily encapsulated to form inclusion complexes. The study shows that the new formulation of Breviscapine by inclusion of hydroxypropyl beta-cyclodextrin can effectively overcome the shortcomings of Breviscapine injection, such as short half-life, rapid elimination in vivo and low bioavailability of oral administration, and at the same time, it can ensure the curative effect of Breviscapine and make it convenient for patients to use medicine.