| With the continuous increase of the pace of life,the accompanying various pressures and dietary changes have a significant impact on gastrointestinal health.Constipation has become the main problem affecting the quality of life of human beings.In this study,we have developed a laxative health product,Yuliren Cassia tablet,which consists of three herbs: Yuliren,Cassia and Aloe,to prevent chronic constipation by moistening the intestines and laxing the fires,thus achieving the goal of preventing diseases before they occur and improving the health of life.Firstly,a model was established to optimize the extraction process.Secondly,two kinds of tablet forming processes were investigated,and the quality of tablets obtained by wet granulation was studied,and the stability and safety toxicological evaluation were carried out.The extraction technology of effective components of three herbs was studied.Box-Behnken analysis was used to establish the response surface models for the water extraction process and alcohol precipitation process,respectively.The two models were designed with three factors,three levels and three indicators,and the effect of each factor was analyzed comprehensively,and the response surface results were optimized to obtain the best water extraction and alcoholic sedimentation process: the herbs and water were decocted twice at a 1:8 ratio for two hours.The two extracts were combined and concentrated under reduced pressure to a relative density of 1.05（temperature: 50-60°C,vacuum:-0.06-0.08 MPa）,95% ethanol was added until the ethanol concentration was 65%,stirred and precipitated for 17 h,and then filtered.The filtrate was recovered under reduced pressure until there was no smell of ethanol,and concentrated to a thick paste with a relative density of 1.20-1.25.The thick paste was dried under vacuum（temperature: ≤80℃,vacuum:-0.06～-0.08MPa）to obtain the dried extract paste.Two formulation processes were studied: direct powder tablet pressing and wet granulation tablet pressing.In the study of powder direct pressing,12 powder parameters of extract powder and different direct pressing excipients were determined according to SeDeM expert system,physical fingerprints were established,and the compressibility and formability of the formula were systematically evaluated.Finally,the powder direct compression tablet prescriptions were obtained by validating the predicted results: 13.52% extract dry paste powder is mixed with 82.98% corn starch,then standard lubricant（2.36% talc,1% magnesium stearate and 0.14% silica）is added,mixed well and then directly pressed into tablets.In the process of wet granulation and tablet pressing,the formula was screened out according to the indexes of wetting ability,granulation condition,Angle of rerest,grain yield and disintegration time,and the wet granulation preparation process was obtained: Dry paste powder and corn starch were evenly mixed in the ratio of 1:0.9,and then 85%ethanol water was sprayed to granulate.The wet particles were dried at ≤30℃ for 4 h,screened through 20 mesh,and then 0.5% magnesium stearate was added to mix evenly and pressed.Due to the high proportion of prescription excipients obtained by direct tablet pressing,poor patient compliance,comprehensive production efficiency and process reproducibility,wet granulation was selected as the final preparation process,and the follow-up study was conducted.In order to guarantee the product quality and provide the basis for content limitation,the quality standard of Yuliren Cassia tablet was established.Conducted routine checks of hardness,friability,weight differences,etc.,all in accordance with the corresponding provisions of the Pharmacopoeia.cassia and aloe vera were identified by TLC and both were detected.The contents of landmark components amygdalin,Aurantio-obtusin and efficent components chrysophanol and aloin were determined by HPLC,and the four components were limited.In order to ensure the safety of the product,the UV spectrophotometric method was used to detect the total anthraquinone content and limit.Limit of five ingredients: amygdalin ≥0.7g/100 g,aurantio-obtusin ≥30mg/100 g,chrysophanol ≥30mg/100 g,aloin ≥1.6g/100 g,total anthraquinone: ≤1.0g/100 g.In order to investigate the stability and safety of the product,preliminary stability investigation and safety toxicology evaluation were conducted.In the long-term stability test and accelerated stability test,the results of each index were stable;Acute oral toxicity test in rats showed no obvious poisoning symptoms and no animal death,indicating that the product is actually non-toxic.During the 28-day oral toxicity test,the animals grew well,and no obvious toxic reaction and histopathological abnormalities were observed,It proves that this product is relatively stable in a certain period of time,and it is actually non-toxic and safe to eat. |
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