Pharmakinetic Research Of Xiongbin Nasal Spray In The Brain

IntroductionStroke is one of the three main deadly diseases of human being. It becomes a heavy burden of society and family because of its high incidence, high mortality, high disability and high relapse. Acute ischemic stroke (AIS) consists 80% of total patients, and the ratio is increasing in recent years. It's a important project that attract the attention of the whole medical field to find a effective method of prevention and cure AIS, lower the mortality and disability rate. Up to now, no idea method is found.Nasal administration of medicine is a characteristic of traditional Chinese medicine(TCM) with the advantage of simplicity, utility, non-injury, safety, small dose, rapid and strong efficacy. Exploration of TCM nasal spray with the function of activating circulation and resuscitation to cure AIS is practical for clinical application and with theoretic sense in finding new TCM method for emergency.Part One Bibliography ReviewTreating cerebrovascular diseases with pernasal therapy, or with Chuan Xiong and Acorus Tatarinowi (Brouneol) can be found in many recording, which provides solid theoretic basis for our research of Xiong Bin nasal spray. According to TCM theory, there is close relation between opening and visceral or channel, besides, brain controls the seven opening, so give medicine through nasal, one of the opening, can adjust the function of visceral and channel, and will affect brain. Modern medical theory supports formal knowledge from these aspects: 1. absorption of medicine by nasal capillary , 2. nerve stimulation and brain adjust, 3. supplemental absorption by the surface of trachea and lung alveolus.Pharmacologic research of the mechanism of treating cerebravascular diseases with Chuanxiong indicated it has following role: 1. improve circulation and brain perfusion, 2. antithrombosis; 3. exclude free radicals; 4. block calcium-channel; 5. improve studyability. Acorus Tatarinowi promote absorption, and traverse blood-cerebral barrier.Part TwoGas chromatography is applied to analyge the Tetramethylpyragine (TMPz) in rat's brain , the condition of GC is : glass column(2mm><2m) filled with white load (80-100 sifter) covered with 4%BuGs, BCD detector with high purity N2. The coeffieient of liner regression is good enough (r2=0.9995) for the TMPz cerebral concentration range in 25ng/ml~1000ng/ml. The recovery is more than 90%.There are three administration modes: Xiongbin nasal spray(A), Chuanxiong nasal spray(B) and Xiongbin decoction(C). All the cerebral of TMPz in various time points after administration were assayed with GC. The TMPz cerebral concentration-time curves then were obtainedThe concentration-time process of A can be described with open two-department model, which is looks like to be similar to the process of intravenous administration. Comparing A with B and C, A has following characteristic. 1. quick absorption of TMPz. TMPz transfers blood-brain barrier almost at the same time of administration, and reach the peak concentration 1 minute after the administration. 2. Quick distribution and excretion. 95.7% of TMPz has been cleared from brain within l.Sh, which means multi-administration in short time is possible, TMPz will not accumulate in brain. 3. Acorus Tatarinowi (Borneol) facilitate absorption of TMPz: promote its entrance into brain, prolong the action time, and increase its bioavailability, as comparing A with B.Conclusion: Xiongbin nasal spray is a quick-effect preparation for emergency of acute ischemic stoke.