Studies On Nasal Absorption Of Main Active Compounds In Xyp Spray

XueYaPing spray is used to cure hypertension, which is composed of Spica prunellae, Flos chrysanthemi, Radix paeoniae rubre, Flos magnoliae, Cortex cinnamomi, Rhizoma chuanxiong, Radix angelicae sinensis and Herba menthae. In the earlier experiment and clinical research, we find that the concentration of xueyaping spray which can exert therapeutic effects is only 3g/time. What is the reason for the good therapeutic effect? On the one hand maybe the special structure of the nasal is not only avoid of first pass effect, but also the medicine can bypass the blood brain barrier though the pathway between brain and nasal. On the other hand, the interaction of the complex components of xueyaping prescription maybe changes the ADME process of these active components.The advantage of Nasal drug delivery is confirmed. In order to demonstrate the second idea, the subject beginning with the absorption of the nasal membrane, study the situation of the absorption by in situ nasal recirculation method in xueyaping prescription. The goal is to confirm the absorptive characteristics of the main active components. So that it can supply theoretical evidences for the selection of dosage form and excipients.To review the study on chemical constituents and pHarmacological activities of this prescription, we confirm these active components closely related to decrease blood pressure. They are chlorogenic acid, Ferulic Acid, peoniflorin and Cinnamic acid. This article establishes a HPLC method for the determination of these components in XueYaPing spray.The absorption of active components in the nasal membrane is evaluated by nasal circulatory perfusion test in vivo in this article. However, this method has many deficiencies:the intubation in esopHageal is very difficult, and the successful rate is very low. so we decide to intubate in tracheal, and then we use three model medicine(Ditong biyan shui, Fuma dibiye, Xueyaping spray) to verify weather this new improved circulatory perfusion is feasible.Based on the improved nasal circulatory perfusion method, we study the absorption of the main active componets in nasal, including osmotic pressure, pH, flow rate, volume and concentration of administration. Finally, the optimum parameters are as follows:flow rate is 1.8mL/min, the volume is 10mL, the nasal absorption of chlorogenic acid, Ferulic Acid, Peoniflorin, Paeonol and Cinnamic acid is passive transport, and the absorption is good. Meanwhile we find that the absorption of single Peoniflorin is not so ideal, but in the Xueyaping prescription the result shows good absorption.Accroding to the poor absorption of Peoniflorin, we study weather the volatile oil and the mixture compatibility of chlorogenic acid, Ferulic Acid, Paeonol and Cinnamic acid have an influence on the absorption of Peoniflorin. The results show that the mixture has a certain promoting influence on the absorption, but it still has a certain distance compared with the spray. This situation is better improved when the volatile oil is added to the mixture.Also we find that the excipients which are added to the spray have an influence on the absorption of the medicine. So we choose Peoniflorin has a poor absorption to investigate the excipients. The results show that chitosan and HP-P-CD have a strong promoting influence on the absorption, and they can be used to the spray as supplementary agents.