Pharmaceutical Research And Preliminary Pharmacodynamic Study Of Jinhu Qingyan Granules

Chronic pharyngitis is a common clinical disease.When wind-heat pathogens invade the oral and nasal cavities,they directly attack the throat.This situation can cause swelling and pain in the pharynx.Over time,it becomes chronic pharyngitis.As a common clinical disease,this disease is difficult to cure or recurs easily after cure.The prescription is made up of Lonicerae japonicae,Dendrobium nobile,Ophiopogon japonicus,Platycodon grandiflorum,Belamcanda chinensis,Glycyrrhiza uralensis,XX and so on.It has the effects of Ziyin Qingre,Qutan Shengjin,Jiedu Liyan,and it has a certain curative effect on the treatment of burning throat,dry itching,excessive phlegm,and other diseases.This prescription is a clinically experienced prescription from Jiangsu Province Hospital on the integration of Chinese and Western Medicine.We designed the dosage form as granules under the guidance of the theory of Chinese medicine.The granules are easy to carry and the patients have a high degree of acceptance.On the one hand,the medicine can be quickly dissolved and absorbed by the human body to accelerate the onset of action;on the other hand,it can also ensure the accuracy of the patient’s dosage.This article mainly carried out the pharmaceutical part research and preliminary pharmacodynamic research on the preparation.Preparation technology:Through literature research on the chemical components of the main Chinese herbal medicines in this prescription,including their physicochemical properties and pharmacological activity research progress,we designed the extraction route and determined the content of chlorogenic acid as the detection index.With chlorogenic acid content and yield rate as comprehensive evaluation index,and with the number of extractions,extraction time,water addition,and soaking time as factors,using L9(34)methods orthogonal experiment to optimize the best extracting process of Jinhu Qingyan Fang.The optimum extraction conditions were as follows:the medicinal materials were extracted for two times with 8 folds of water,45 mins each time.The optimized extraction process of Jinhu Qingyan granules was stable and feasible.By investigating the concentration process,it is determined that the concentration method is reduced pressure concentration and the concentration temperature is 85℃.According to the yield rate of this recipe and the characteristics of the thick extract,we determined that the granulation method is wet granulation.Through the screening of auxiliary materials,flavoring agents,etc.,according to the degree of difficulty in the granulation process,the hygroscopicity of the material,the molding rate,and other indicators,combined with the actual production situation,the final decision is to select dextrin as the auxiliary material.Choose steviosin for corrgent.Finally,according to the laboratory test results,a pilot scale-up experiment was carried out.Quality Standard Section:The name of this preparation was drafted as "Jinhu Qingyan Granules",and its properties were described according to the appearance and smell of the granules.The identification methods of the medicinal herbs such as Lonicerae japonicae,Ophiopogon japonicus,Platycodon grandiflorum,Belamcanda chinensis,Glycyrrhiza uralensis,in the preparation have been established using TLC.The specificity and durability were investigated,and the results showed that the characteristic spots in each medicinal material were clear,with good separation and strong reproducibility,so we included them in the quality standard.To determine the content of chlorogenic acid in Jinhu Qingyan Granules by HPLC.The linear range of chlorogenic acid was 5.00～368.20 μg/mL and the average recovery was 101.38%with RSD 2.34%.At the same time,the content of six phenolic acids including chlorogenic acid in Jinhu Qingyan Granules was determined and methodologically investigated.Neochlorogenic acid,Chlorogenic acid,Cryptochlorogenic acid,Isochlorogenic acid B,Isochlorogenic acid A,Isochlorogenic acid C are respectively 3.00-100.05 μg/mL,2.99-99.94 μg/mL,2.99-99.90 μg/mL,3.00～100.05 μg/mL,1.00～100.03 μg/mL,3.00～100.08μg/mL have a good linear relationship within the mass concentration range;The established method has high sensitivity,good accuracy,and reproducibility,which provides a scientific basis for the stability of the preparation.Finally,we conducted a series of inspections on the three batches of pilot products following the relevant requirements under the general rule 0104 of the Chinese Pharmacopoeia(2020 edition)and established the quality standard for Jinhu Qingyan Granules.Stability Section:This study conducted long-term stability studies and accelerated stability studies on three batches of pilot samples;the results showed that the quality of the preparations was stable during the investigation period.The stability study part is still going on to determine its actual validity period.Pharmacodynamics Section:The model of chronic pharyngitis in rats was constructed by using the Aqueous Ammonia sprayed directly into the rats’ throat to treat the modeled rats by intragastric administration.According to the animal’s appearance during the pharmacological experiment,the results of HE stained sections of the throat mucosa and the results of hemorheological tests,as well as the level of inflammatory factors in the rat serum measured by ELISA,such as:TNF-α,IL-1β,IL-6.In addition,we used Western Blot experiment to determine the phosphorylation level of NF-κB-p65 protein in the throat mucosal tissues of animals.A series of studies have shown that Jinhu Qingyan Formula has a good therapeutic effect on chronic pharyngitis in rats,and the mechanism of action may be related to its involvement in regulating the NF-κB signal transduction pathway and the expression of downstream inflammatory factors.