Development Of Baihuaxianglian Detoxification Granules

Objective: In this paper,a new drug is developed for baihua xianglian jiedu decoction which decided to preparate granulation.The preparation process,quality standard,stability,acute toxicity and antihepatitis B virus action five aspects of baihua xianglian jiedu granules were studied by using modern pharmaceutical preparation technology to improve the stability of the preparation and make it carry and take convenient,quality assurance,the effect is stable and better serve in clinical.Methods: Methyl ethyl oxalate and the paste yield were used as the index,using single factor,orthogonal test to formulate the best extraction technology of baihua xianglian jiedu granules.Based on various indexes such as rate solubility,fluidity,the species of excipients,dosage and process conditions were investigated to preliminarily determine the prescription molding process.Formulations processes were determined by pilot test.The TLC method was used to identify the thin layer of Oldenlandia diffusa(willd)Roxb and Herba isodonis ternifoliae(HIT).HPLC method was used to determination the content of a methyl ethyl oxalate of the specific components of the herb of Oldenlandia diffusa(willd)Roxb.Inspection items according to granules preparation requirements of the 2015 version of "Chinese Pharmacopoeia" and the requirements of the research and development of traditional Chinese medicine,the stability of baihua xianglian jiedu granules was determined by apearance character,TLC identification,inspectionand content determination.The acute toxicity of baihua xianglian jiedu granule was evaluated by maximum dosage method.The expression level of HBV DNA was detected by fluorescence quantitative PCR after the use of HBV 1.3P cell model in vitro.The expression of HBs Ag and HBe Ag in cells was detected by chemilum inescence.The expressionintensity of HBe Ag in cells was detected by indirect immunofluo rescence assay.Results: The best extraction process of baihua xianglian jiedu granules is as follows: adding 10 times the amount of water,extracting two times,each time 1.5 h.Molding process is as follows: according to thick paste: dextrin =1: 2 ratio of dextrin added to 0.25 % aspartame and 0.25% stevia as a flavoring agent,and then adding 75% ethanol as wetting agent,mixed uniformly,passed through 14 mesh sieve granulation,dried at 80℃.TLC was used to identify the herb of Oldenlandia diffusa(willd)Roxb and Herba isodonis ternifoliae(HIT).The results showed that the test granule solution had the same color spot at the same position as the control solution and Contrast medicinal solution,and the negative granule had no interference at the corresponding position.Results the linear relation was good,the precision,stability,repeatability and recovery were all in accordance with the regulations by using the HPLC method to determine the content of methyl ethyl oxalate.The inspection items of the baihua xianglian jiedu granules were in accordance with the regulations of the 2015 edition of Chinese pharmacopoeia.During the stability study,the appearance,TLC identification,examination and content determination of the three batches of the experimental granules were in accordance with the regulations,which indicated that the preparation was basically stable during the six-month period of the simulated market.During the acute toxicity test,the activity status,feeding,drinking water and excretion of the experimental mice were all normal after the maximum dosage was given repeatedly.During the whole experiment,mices had no death or poisoning.The volume,color and texture of the main organs were not significantly altered.Comparing with control group,There was no significant difference in main organ coefficient(P>0.05).The experimental results showed that under the dosage did not affect the proliferation of HBV hepatocytes,the longer the duration of continuous drug use,the stronger the inhibition effect on HBV and with the increase of dosage,the inhibitory effect on HBV was also enhanced.Conclusion: The method of preparing the preparation process of baihua xianglian jiedu granules is reasonable and feasible.The quality standard can effectively control the quality of the preparation.The drug This preparation has no obvious acute toxicity and has the effect of anti-hepatitis B virus in vitro.