Study On The Screening Of Petasites Japonicus Fr.Schmidt Anti-allergic Active Constituent And Preparation Of Tablet

Objective ① Obtaining the anti-allergic active constituent from Petasites japonicus Fr.Schmidt and analyzing its chemical composition.② Study the anti-allergic effects of Petasites japonicus Fr.Schmidt effective part by a variety of different anti-allergic models in vivo and vitro.③ Anti-allergic tablets are made from Petasites japonicus Fr.Schmidt effective part.Establish it’s quality standard(draft)and investigate it’s preliminary stability.Methods ① Separating and analyzing of anti-allergic active constituent:By solvent extraction,silica gel column chromatography,combined with the anti-allergic experimental screening anti-allergic effective parts,and analyzing its chemical composition.② Anti-allergic effects study:evaluating the anti-allergic effects on guinea pig ileum experiments,guinea pig’s isolated trachea test,passive cutaneous anaphylaxis reaction of ICR mice,and allergic rhinitis model of allergic mouse.To discuss the anti-allergic mechanism by determining the content of histamine and NO in the serum.③ The preparation of anti-allergic tablets:Investigating the hygroscopicity and liquidity of the most effective part in order to evaluating the tablet preparation process.The best prescription of anti-allergic tablets is established by selecting excipient and screening formula.To apprise the quality of tablets by investigating the tablets appearance,tablets weight difference,tablets hardness,friability and disintegration time.④ Anti-allergic tablets’ quality standards:According to 2010 version of Chinese pharmacopoeia,determining the tablets appearance,thin-layer identification,weight difference and disintegration time.⑤ The preliminary stability test:Examining the preliminary stability in the 0 to 3months(once every month)by investigating the character,identification,weight difference,disintegration time at room temperature.Results ① Many effective subatances were separated from Petasites japonicus Fr.Schmidt.They are PJE4、PJE4-1、PJE4-2、PJE4-3、PJE4-4 和 PJE4-5 respectively.And PJE4-3 accounts for 0.082%.PJE4-3 has three main peak in the retention time of 2.235,7.688 and 10.561min in the liquid chromatogram.The percentage is 9.12%,1.25%and 89.63%respectively.② PJE4,PJE4-1,PJE4-2,PJE4-3,PJE4-4 and PJE4-5 can inhibit markedly the contraction of isolated guinea pig ileum and isolated guinea pig trachea caused by histamine(p<0.05).PJE4-3 has the strongest inhibition and the inhibition rate is 66.06%and 60.53%respectively.③ High and low dose group of PJE4-3 reduced significantly the permeability of blood vessel and decrease the leakage of Evans blue in the Passive Cutaneous Anaphylaxis reaction(p<0.05).The inhibition rate is 51.19%and 41.02%respectively.④ High and low dose group of PJE4-3 improved significantly allergic symptoms of allergic rhinitis induced by OVA(p<0.05).High dose group had no obvious difference compared with the normal group(p>0.05).Low dose group was lower than the normal group(p<0.05).The ELISA experiment showed high dose group can reduce significantly the content of histamine and NO in the serum,but low dose group not obviously declined.High dose group’s anti-allergic effects are consistent with Loratadine group’s.⑤ Preparation of prescription of anti-allergic tablets:PJE4-3 power 10g,starch 64g,lactose 96g,PVPK30 22g,PVPP 6g,magnesium stearate 2g,produced 1000 tablets.⑥ Anti-allergic tablets are faint yellow round,taste salty and astringent.According to thin layer identification,the tablets have the same points with PJE4-3.weight difference and disintegration time conform to 2010 version of Chinese pharmacopoeia.⑦ The test results of character,identification,weight difference,disintegration time of 1,2,3 months anti-allergic tablets,compared with 0 month,these indicators have no obvious changes.Conclusion ① Many effective substances were separated from Petasites japonicus Fr.Schmidt.They are PJE4,PJE4-1,PJE4-2,PJE4-3,PJE4-4 and PJE4-5 respectively,and PJE4-3 has the strongest anti-allergic effects.② The most effective part PJE4-3 has obvious inhibitory effects on guinea pig ileum experiments,guinea pig’s isolated trachea test,passive cutaneous anaphylaxis reaction and allergic rhinitis model of allergic mouse.③The anti-allergic effects may be related to decline of the content of histamine and NO in the allergic rhinitis in mice induced by OVA.④The preparation process of anti-allergic tablets is reasonable and feasible.Its quality can be well controlled according to 2010 version of Chinese pharmacopoeia.And anti-allergic tablets have good stability from appearance to inner quality.