Long Baicalensis Grass Tablet Pharmacy, Pharmacodynamics And Mechanism Of Action Discussed

1. Objective:Based on the theories of Traditional Chinese Medicine, active parts of Lumbricus,Radix Scutellaria,Radix Glycyrrhizae are extracted to constitute Longqincao buccal tablets. Their ingredients is primitively definite,and drug action is certain,and quality can control through the research of pharmacy,pharmacodynamics as well as mechanism of action. We will determine reasonable preparation technology, establish scientific quality control standard,also increase bioavailability and promote curative effect by administration through oral mucous membrane.2.Methods:This research includes studies on preparation technolog, quality standard, pharmacodynamics, pharmacokinetics, and mucosal toxicology of Longqincao buccal tablets.The prescription is made of Lumbricus, Radix Scutellaria, Radix Glycyrrhizae.The optimal prescription is obtained by combining flu and respiratory infection feature, abiding by compatibility method of Chinese midcine, filting by pharmacology.The group is made high performance preparation of active parts,and through oral membrana mucosa administration.It can clearing lung-heat to ease the throat,removing toxic purging heat.⑴The preparation technolog of Longqincao buccal tablets: Active part of lumbricus was extracted by biochemical technology. According to requirements on extractive of Radix Scutellariae in primary part of Pharmacopoeia of the People's Republic of China (version 2005) and requirements of Ammonium Radix Glycyrrhizae in State Drug Standard (WS-10001(HD1269)-2002), content of baicalin was controlled with HPLC; According to preparation requirement of buccal tablets, parameters of manufacture process were ascertained and preparation craft was established.⑵Quality standard of Longqincao buccal tablets: Radix Scutellariae, Radix Glycyrrhizae and Lumbricus were identified by thin-layer chromatography (TLC), the content of baicalin was determined by high performance liquid chromatography (HPLC), and content limitation of baicalin in preparation was identified. According to requirements on buccal tablets in appendix of Pharmacopoeia, items of test were determined.⑶Pharmacodynamical research of Longqincao: To observe the antifebrin effect of Longqincao spray and buccal tablets,change of expression of TNF-αin rabbits febrile model induced by Bacillus coli endotoxin after administration; To observe cough-relieving effect of Longqincao spray and buccal tablets in mouse cough model induced by ammonia water; mucosa toxicity experiment, pertinent items were tested and pathological condition of tissues was observed.⑷Pharmacokinetic study of Longqincao buccal tablets in rabbits: Rabbits were administrated drugs intragastrically or though oral mucosa; to collect blood of rabbits in different time, determine and compare drug concentration in blood, and determine relative bioavailability; after atomization administration, oral mucosa of rabbits was dissected and drug concentration in mucosa was determined.3. Results:⑴The preparation technolog of Longqincao buccal tablets: It could retain each kind of enzyme activeness in the Lumbricus by the biochemistry extraction. Examined by HPLC, baicalin 85.5% in Radix Scutellaria extractive, ammonium glycyrrhizinate 75% in Radix Glycyrrhizae extractive, both of them conformed to the standard.Longqincao buccal tablets prepared by the method conformed to their standard.⑵The quality standard of Longqincao buccal tablets: Defined the TLC method,inspection item,content limitation of baicalin in the preparation, there should be no less than 5.0mg baicalin in 75mg sample, the experimental methodology conforms to the requirement.⑶The pharmacodynamic action of Longqincao buccal tablets: It could relieve fever remarkably in febrile rabbit induced by LPS(P<0.01),and the effect was enhanced when increasing dose, LPS could stimulate ATⅡsecreting TNF-α,but Longqincao buccal tablets could depress the abnormal increase of TNF-α; The moderate dose of Longqincao buccal tablets could decline the number of cough in mice lead by ammoniae aqua, there is most notably difference compared with control group(p<0.01), other groups haven't cause remarkable change(P>0.05); There are no obvious pathological changes in the organ of mucosa toxicity experiment, so they could be think innoxious.⑷The study of pharmacokinetics of Longqincao buccal tablets in rabbit body: Blood drug level reach peak at 70min by both routes of administration, and the blood drug level in rabbit that dosage by mouse was 1.6 times of that by intragastric administration, and the relative bioavailability reached 166.5%, also, baicalin could be detected in mucous membrane of the rabbit that dosage by atomization.4. Conclusions:From above results, active parts of Lumbricus,Radix Scutellaria,Radix Glycyrrhizae are extracted to constitute Longqincao buccal tablets. Longqincao buccal tablets have effect of clearing lung-heat to ease the throat,removing toxic purging heat, they could be used to treat flu caused by virus and upper respiratory infection, and could avoid first pass effect through oral and nasal membrana mucosa administration, also increase bioavailability.