| Drinking alcohol in moderation has the effect of invigorating blood circulation,strengthening the heart and brain,and improving sleep.However,excessive alcohol consumption can lead to dizziness,vomiting and blurred consciousness,which in the long run can cause damage to the body’s organs and also lead to physiological dysfunctions in the body,triggering cardiovascular diseases and posing a threat to the health of the body.Excessive alcohol consumption poses a serious threat to human health and social development,therefore,the research of anti-alcohol and liver medicine is one of the major concerns of society today.Gastric floating extended-release tablets have a longer residence time in the stomach than ordinary preparations.After oral administration,due to its inherent characteristics,it can float above the liquid in the stomach,prolonging the drug release time,enhancing the absorption of the drug by the body and enabling better efficacy.Pueraria Mirifica has the effects of relieving muscle and fever,generating body fluid to quench thirst,penetrating rash,raising yang to stop diarrhoea,activating the meridians and detoxifying alcohol.The Pueraria Mirifica contained can improve the regenerative capacity of liver cells and restore normal liver function,which can effectively reduce symptoms such as dizziness,headache and nausea in alcoholic patients and can significantly improve their liver function.The flavonoids in Pueraria Mirifica,Hawthorn and Chen Pi can promote the body’s oxidative metabolism of ethanol by scavenging free radicals and activating the activity of ethanol dehydrogenase.They can also increase renal blood flow by dilating blood vessels and improving the spasm of renal tubules,resulting in increased urine output and enhanced excretion,thereby reducing the concentration of ethanol in the blood.The phenolic hydroxyl radicals structure it contains can scavenge a large number of free radicals and reduce damage to liver cells from immune stress reactions,and also inhibit metal ion-induced lipid peroxidation and reduce oxidative damage.Due to the instability of flavonoid components,they are poorly absorbed in an acidic environment.Ordinary preparations excrete the drug before it is fully absorbed,which can affect the effectiveness of the drug.The long release time,stable nature,good drug absorption and low side effects of the gastric floating slow-release formulation can be used to prepare gastric floating slow-release tablets for alcohol detoxification,which can prolong the action time of flavonoid components in the body,reduce the large number of free radicals produced in the metabolic pathway of ethanol decomposition,and reduce the damage to liver cells caused by immune stress reactions.It can activate the activity of ethanol dehydrogenase to promote the metabolism and excretion of alcohol in the blood to achieve the effect of alcohol detoxification.In this study,total flavonoids were extracted from Pueraria Mirifica,Hawthorn and Chen Pi,and the ethanol concentration,herb ratio and extraction time were used as the key factors to investigate the total flavonoids content respectively,and the total flavonoids content was used as the quality evaluation index of the extract infusion.The highest total flavonoid content was obtained after 1.5 hours of extraction with 70%ethanol.In vitro antioxidant tests on Pueraria lobata,Hawthorn and Chen Pi showed that the extract total flavonoids had free radical scavenging ability.The higher the content in the range of 0.3 mg/mL to 5.0 mg/mL,the more significant the scavenging ability.In the experiments on intoxicated animals,when the ratio of Pueraria lobata,Hawthorn and Chen Pi was 6:4:1,the extract infusion had the best antidote effect on intoxicated mice,and the sobering time was significantly shortened compared to the control group.This shows that the extracted infusion has an antidotal effect,which provides a theoretical basis for the preparation of tablets at a later stage.On the basis of the pre-prescription study the fluidity,compressibility and hygroscopicity of the extracted infusion powder were investigated,the results showed that the fluidity of the powder was good and the compressibility was poor,when the relative humidity was 75.3%,the hygroscopicity of the powder was 15.65%,which was already more than 10%.Therefore,the moisture in the air must be strictly controlled during the production and in the compression of the tablets to avoid the powder from absorbing moisture and reducing the quality of the tablets;the excipients and processes of the alcoholic gastric floating slow release tablets were screened,and Pueraria Mirifica,Hawthorn and Chen Pi were used as the main drugs for the preparation of the alcoholic gastric floating slow release tablets,with each of the screened excipients,and the preparation was carried out according to the prescription dosage;the star point designeffect surface method was used to optimize the optimum The optimal prescription results were:hydroxypropyl methylcellulose(HPMC K4m)88 mg,polyvinylpyrrolidone(PVP)34 mg,NaHCO35 mg,CaCO315 mg,octadecanol 85 mg,lactose 25 mg,microcrystalline cellulose 43 mg,drug infusion powder 55 mg,total tablet weight 350 mg;the tablets were screened by using direct powder pressing and wet granulation pressing.The tablets prepared according to the prescription had good floating and releasing properties;the study of the drug release mechanism showed that the release of the tablets was in accordance with the zero-level release process,and the release mechanism was in the form of non-Fick diffusion,i.e.diffusion and dissolution had a significant role in the release of the drug.The study showed that the release mechanism of the tablets is in line with the zero-level release process,and its release mechanism is in the form of non-Fick diffusion,i.e.diffusion and dissolution have synergistic effects in the release process of the drug.The prepared tablets were investigated for their properties,weight variation,hardness and fragility according to the Chinese Pharmacopoeia 2020 edition standard.The results showed that all the indicators were in accordance with the pharmacopoeia.In this study,the in vitro release of Antitussive Gastric Floating Delayed Release Tablets was analysed by UV spectrophotometry,and the identification of geraniol in Pueraria Mirifica,quercetin in Hawthorn and Chuan Chen Pi and orange peel in Chen Pi was carried out by thin layer chromatography.The content of geraniol,quercetin,Chuan Chen Pi and orange peel was determined by HPLC,and the sensitivity and accuracy of each method were good and could meet the requirements of the experiment.The results of the stability study of the alcoholic gastric floating slow-release tablets showed that the appearance,content,floating capacity and release of the tablets did not change significantly under strong light,high temperature and humidity,and were relatively stable in nature.The results of accelerated and long-term tests showed that the tablets were stable to light and heat and not easily absorbed moisture,which provided a basis for the transportation and storage of the drug. |
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