Investigation Of The Absorption Mechanism And Absorption Characteristics Of Toutongning Nasal Spray

Toutongning nasal spray is a hospital preparation used in clinic for many years.The prescription of Toutongning nasal spray is composed of Aconiti Radix Cocta,Chuanxiong Rhizoma,Saposhnikoviae,Radix Schizonepeta Herba,Menthae Haplocalycis Herba and other herbs.With invigorate the circulation of blood and dispel the wind,warming and pain relieving effect,and is mainly used for the treatment of migraine,headache and other headache symptoms.After all the previous work,we registered according to the requirements of the drug,the use of modern technology on the preparation process,quality standard and stability were studied.Access to relevant literature that the breathing zone is the largest part of the nasal cavity,the mucous membrane rich in blood vessels,rich blood flow,and drug can be quickly absorbed through the mucous membrane in the blood directly into the blood circulation,the drug after intranasal administration into the systemic absorption of main ways of settlement.The upper part of the nasal cavity and sinus direct anastomosis of cerebral vessels the relationship,to provide the anatomical basis for nasal drug delivery into the brain and brain pathways.The nasal sinus,the relationship is very close,there is a slight channel potential between the nasal cavity and brain,three of the cranial nerve in twelve distribution in the nasal mucosa.Drugs through the nose can stimulate the intranasal nerve,resulting in reflex regulation,causing changes in the body’s physiological and neurotransmitters to regulate the function of the brain and other organs,so as to effect on the treatment of brain disease and other systemic diseases.In order to verify the above hypothesis,the following research work has been carried out.1.The determination of the main active components in nasal sprayAccording to the prescription of Toutongning nasal spray,to prepare three batches of samples,each batch of about 1000 mL,set aside.On analysis of prescription,the author presents 6 kinds of components,each of the 6 components in three batches of samples were determined.The optimum content is high,stable property,one or several components of the measurement method is simple easy as active index.Further investigation eventually identified prim-oglucosylcimifugin,5-O-methylvisammioside as index components in subsequent research.2.Study on the absorption of in rats in vivo by prim-o-glucosylcimifugin and 5-OmethylvisammiosideAny of the main active ingredient Toutongning nasal spray in prim-o-glucosylcimifugin,5O-methylvisammioside rat in situ nasal cycle,using the HPLC method to determine the content of circulating fluid before and after effects of Toutongning nasal spray of prim-oglucosylcimifugin,5-O-methylvisammioside of nasal absorption.According to the results,Three concentration of Prim-O-glucosylcimifugin’s absorption rate constant is(0.588±0.041)×10-3,(0.547±0.023)×10-3,(0.592±0.063)×10-3min-1.Three concentration of 5-Omethylvisammioside’s absorption rate constant is(0.438±0.041)×10-3,(0.407±0.023)× 10-3,(0.412±0.063)× 10-3 min-1.We can get the conclusion that the main active ingredient of Toutongning nasal sprays can be absorbed through the nasal mucosa.3.Investigation of the absorption characteristics of Toutongning nasal sprayThe rats were randomly divided into two groups,intravenous injection group and nasal administration group after administration at the time points of blood samples of brain tissues,tissue samples were processed in accordance with the requirements of HPLC-MS to determine the content of components in the sample index,the content of two kinds of drug administration and blood in the brain is not the same time points were calculated,drawing drug time curve,calculated for different drugs and blood pathways in the brain of AUC.Using AUC brain/AUC plasma in cerebral blood vein administration group as the ratio of brain targeting coefficient,analysis of brain target of prim-o-glucosylcimifugin,5-O-methylvisammioside of different modes of administration are to investigate coefficient.The possibility of medicine across the blood brain barrier absorbed through nasal mucosa directly into the brain.The concentration of prim-o-glucosylcimifugin and 5-O-methylvisammioside in the brain reached the peak within 10 min,the ratio of AUC brain/AUC plasma obtained after intranasal administration was significantly higher than that of I.V administration after intranasal administration.The brain targeting coefficients of prim-oglucosylcimifugin,5-O-methylvisammioside were 1.2791and 1.4679 respectively.The results showed that the two components could absorbed into the brain via the nasal cavity.