Preparation And Quality Investigation Of Baicalin Dispersible Tablets

OBJECTIVE:To research and develop a new solid quick effectivity preparation of traditional Chinese medicine——Baicalin dispersible tablet.METHODS:1.Solid dispersoins were carried out for basic studies.Diferent carriers (PEG4000,PEG6000 and Poloxamer188) with diferent ratios were used to form the solid disperse systems with baicalin.The best carrier was choosed by studying on dissolution rate in vitro and status of baicalin in solid dispersions.2.The formulae of baicalin dispersible tablet were optimized in terms of disintegrating time by orthogonal design test.3.Anassay method for baicalin was established with HPLC,and dissolution in vitro of baicalin from the dispersible tablet was determined by HPLC.4.The effects of light,humidity and temperature on baicalin dispersible tablet have been investigated in terms of appearance,content,dissolution rate and disintegrating time.5.Infulence of release media on dissolution rate of baicalin dispersible tablet were determined by paddle method,which are 0.1mol·l^-1 hydrochloric acid,buffer solution(pH=4),buffer solution(pH=6.8) and water.In vitro dissolution rate studies were compared with baicalin dispersible tablet and conventional tablet by paddle method.RESULTS:1.Baicalin-PEG6000(l:6,1:9) solid dispersion made by dissolvent-fusion method and Baicalin-Poloxamer188(1:9) solid dispersion made by melting method dissolved rapidly 75%in 45min,T₅₀ of Baicalin-PEG6000(1:6) solid dispersion and Baicalin-PEG6000(1:9) solid dispersion made by dissolvent-fusion method was 3.40±0.53 and 2.93±0.33 respectively,which have no difference according to statistics analysis.The Fourier Transform infrared spectra(FT-IR) of baicalin and carriers suggested that there were no non-covalent molecular interactions between baicalin and carriers,such as C-H-pi and hydrogen bond interaction.So PEG6000 was choosed as the best carrier,and Baicalin-PEG6000(1:6) solid dispersion made by dissolvent-fusion method was used to prepare baiealin dispersible tablet.2.The optimized formulation contained 40%crospovidone,6%Sodium Starch Glycolate and 2%amylum pregelatinisatum.3.HPLC can be used as the quality control method of baicalin dispersible tablet.The method is accurate,reliability,highly sensitiveness and repeatability to be used.The optimized dispersible tablets could disintegrate completely within 3 minutes.4.The result of effects of light,humidity and temperature on baicalin dispersible tablet showed that,the appearance,content,dissolution rate and disintegrating time of dispersible tablet was steady with 40℃,RH 75%±5%and light.5.The dissolution rates of baicalin in four different release media were high.It suggested that baicalin dispersible tablets can release in different internal environment The dissolution rate of baicalin dispersible tablet could reach 90%in 15 minutes and faster than that of conventional tablet.CONCLUSION:The optimized baicalin dispersible tablets can be prepared conveniently and easily disintegrate and dissolve.