| The stability of anthocyanins depended on pH,oxygen concentration,light,humidity,temperature,etc.Therefore,the validity period of the anthocyanin preparation usually short,and there are few studies to the stability of the anthocyanins preparation,which limits its application in the market.In this paper,The black rice anthocyanin tablets were prepared by dry granulation for the first time,which prevented the black rice anthocyanin from contacting with moisture during the preparation process.In addition,we studied film coating technology of black rice anthocyanin tablets.The coating can improve the stability(light protection,moisture and gas barrier)of black rice anthocyanin tablets and prolong the validity period of preparations.In recent years,with the aggravation of environmental pollution,the incidence of allergic rhinitis shows increasing trend.Allergic rhinitis can seriously affect the work and learning efficiency of the patients,and reduce the quality of life of the patients.It is also a predisposing factor for major diseases such as sinusitis,conjunctivitis,and asthma.About 40% of patients with allergic rhinitis are accompanied by asthma.At present,there are still adverse reactions and strong resistance of chemical drugs in the treatment of AR.Black rice anthocyanins are water-soluble pigments extracted from the seed coat of black rice,it has the characters of natural,safety and rich in resources.Many studies have shown that black rice anthocyanins have anti-inflammatory,anti-itch and anti-allergic effects,but have not yet reported on the role of AR.In this paper,we are established allergic rhinitis guinea pig model to observe the effects of black rice anthocyanin on nasal symptoms,serum inflammatory factors and nasal mucosa histology in allergic rhinitis guinea pigs model,and its mechanism was explored.Methods and Results:First,methodological research on the determination of material content: HPLC method was used to determine the content of Cy3 G in black rice anthocyanin extracts which use cyanide-3-glucoside as the reference substance.The experimental data show that the method is suitable for the determination of Cy3 G in black rice anthocyanin extracts.The content of Cy3 G in the extracts was determined to be 21.58%.In addition,the total anthocyanin content in the extracts was determined by the p H differential method.The results showed that the total anthocyanins accounted for21.68% in the extracts.So,the ratio of the Cy3 G in the total anthocyanins accounted for 93.25 %.Second,the preparation of black rice anthocyanin film coated tablets:The excipients compatilities with trimetazidine hydrochloride were determined by compatibility test,and screened out excipients with low hygroscopic rate after mixing with black rice anthocyanins.On the basis of the single factor test of dry granulating,Orthogonal experiments were designed to further optimize the parameters of dry granulating process.The results show that the best process parameters for dry granulation are: roll pressure 2.5 MPa,feed frequency conversion 11 Hz,compression frequency conversion 12 Hz,granulation frequency conversion 10 Hz.The black rice anthocyanin granules were prepared using the best process parameters.The proportion of black rice anthocyanin and excipients in the prescription is optimized by the primary molding rate.According to the 2015 edition of the Chinese Pharmacopoeia,the appearance,weight difference,disintegration time,hardness and brittleness of the black rice anthocyanin tablets were examined.The results were all in line with the requirements.To prepare the black rice anthocyanin film coating tablets,the results showed that the best coating parameters were: coating liquid volume 0.65 g.min-1,atomizing pressure 0.2MPa,air inlet temperature 65 Centigrade,and coating speed 14 r.min-1.Third,quality standards of black rice anthocyanin film coated tablets:The contents of research include character,identification,examination and content determination.The appearance of the coated tablet is pale yellow convex circular film-coated tablets.The surface of the coating film is completely smooth,uniform in color,and is dark purple after removing the coating.The identification method is HPLC which Cy3 G as the identification index.The identification result is consistent with the black rice anthocyanin.The quality inspection of the coated tablets included appearance,weight difference,and disintegration time limit,all in compliance with the 2015 edition Pharmacopoeia requirements.The results of content determination showed that the content of Cy3 G and the total anthocyanin content in each coated tablet were not significantly different from those of API,indicating that the active ingredients of black rice anthocyanin extracts were almost not lost during the preparation of the film coated tablet.So,the preparation process was reasonable and reliable.Fourth,black rice anthocyanin film coated tablets stability test: In the influence factor test,black rice anthocyanin tablets and film coated tablets were placed under high temperature,high humidity,strong light conditions for 10 days.High humidity and strong light have a greater influence on the stability of the tablets than high temperature.Compared with the tablet core,the stability of the black rice anthocyanin in the film-coated tablets was improved.In the accelerated test of black rice anthocyanin film coated tablets,there was no significant changes in the black rice anthocyanin,indicating that the stability of the coated tablets was good.Finally,effect of black rice anthocyanin on allergic rhinitis guinea pig model:The allergic rhinitis guinea pig model was established with ovalbumin as a allergen.Then the AR guinea pigs model were randomly divided into 5 groups: ovalbumin model group,high,medium,low dose anthocyanin group,prednisone acetate group,and blank control group.Intragastric administration for two weeks.The scores of nasal symptoms in guinea pigs were recorded to evaluate the symptoms of allergic rhinitis;ELISA kits were used to measure the levels of Ig E,histamine,IL-4 and IL-5in guinea pigs serum;HE stained sections were used to observe the pathological changes of nasal mucosa in guinea pigs.The results showed that after the administration of three doses of black rice anthocyanin,the nasal symptom scores and serum inflammatory factors of AR guinea pigs were reduced,and the pathological morphology of nasal mucosa in guinea pigs was improved.And the effect of black rice anthocyanidins on AR guinea pigs was dose-dependent.Conclusion: Film coating significantly improves the stability of black rice anthocyanin tablets.Black rice anthocyanins have a better therapeutic effect on AR model guinea pigs,its mechanism may be related to its inhibition effect of Ig E mediated mast cell activation,and inhibition the release of inflammatory mediators such as histamine,IL-4,IL-5 and so on. |
PDF Full Text Request