ABSTRACT
OBJECTIVE To establish the quality standard of Kuipingning gastric floating tablets. METHODS Kuipingning gastric floating tablets were prepared and investigated in terms of property ，weight difference and friability. Crydalis yanhusuo was identified qualitatively by thin layer chromatography （TLC）method. High performance liquid chromatography method was used to determine the content of total anthraquinones in Rheum palmatum ，and set the content limit of total anthraquinones. The floating performance and release degree of the preparation were investigated ，and the release kinetic process was fitted. RESULTS Kuipingning gastric floating tablets prepared in this study were gray white to gray tablets with slight smell and bitter taste ；the weight difference and friability were all in line with relevant regulations ；the established TLC method possessed strong specificity and could accurately identify C. yanhusuo . The average content of total anthraquinones in R. palmatum was 17.95 mg/tablet，and its content limit would not be less than 14.36 mg/tablet. The initial floating time of the preparation was no more than 10 s，and the holding time was more than 8 h. The release kinetics process accorded with the Retger-Peppas release model. CONCLUSIONS The method established in this study shows good reliability ，stability and feasibility ，and can effectively control the quality of Kuipingning gastric floating tablets.
ABSTRACT
OBJECTIVE：To study the prepar ation technology of gastric floating tablets of Schisandra chinensis total lignans （SCTL），and evaluate the quality of prepared tablets. METHODS ：Based on single factor test ，the orthogonal experiment was conducted to optimize the formulation of SCTL gastric floating tablets with the contents of hydroxypropylmethylcellulose （HPMC） K15M，NaHCO3 and microcrystalline cellulose as the factors ，using starting time ，holding time and cumulative release rate of gastric floating tablets as evaluation indexes. The properties ，weight difference ，floatability and accumulative release rate of the prepared SCTL gastric floating tablets were determined. The gastric floating tablets were qualitatively identified by TLC ，and the contents of schisandrin A and total lignans were determined by HPLC and UV spectrophotometry. RESULTS ：The optimal formulation of SCTL gastric floating tablets was made up of 23％ SCTL extract ，20％ HPMC K 15M，40％ microcrystalline cellulose，15％ sodium bicarbonate ，1％ octadecyl alcohol and 1％ polyvinylpyrrolidone. The results of detection of this preparation were in line with the related provisions of “0101 tablet”stated in 2015 edition of Chinese Pharmacopoeia （part Ⅳ）. TLC indicated that the chromatogram of the test sample showed the main spots of same color as the corresponding positions of the chromatogram of schizandrol A control ，Schisandra chinensis reference substance and raw material ，while the negative control has no interference. Content determination results shows that the average content of schizandrol A and total lignans in SCTL gastric floating tablets is 3.187，19.617 mg. It was preliminarily formulated that the content limitation of schizandrol A in one tablet should not be less than 2.50 mg，and the content of total lignans （calculated by schizandrol A ）should not be less than 15.50 mg. CONCLUSIONS：The preparation technology of SCTL gastric floating tablets is stable ，feasible and controllable in quality.
ABSTRACT
To investigate the preparation technology and release mechanism of tectorigenin intragastric floating sustained-release tablets. The tablet was produced by wet granulation compression method, with hydroxypropyl methyl cellulose (HPMCK15M), cross-linked polyvinyl pyrrolidone (PVPP), octadecanol and sodium bicarbonate as excipient. The prescriptions were screened and optimized by orthogonal experimental design with in vitro floating capacity and drug release characteristics as the evaluation indexes. The optimization results were as follows: tectorigenin 33.3%, HPMCK15M 16.7%, PVPP 20.0%, octadecanol 13.3%, sodium bicarbonate 5%, and starch gel 10.7%. The prepared tablet can be floated within 10 s in the artificial gastric juice, lasting for 12 h in vitro, with a cumulative release rate of 70% in 10 h. The analysis of Rritger-Peppas equation showed that the sustained-release tablet had two advantages of both drug diffusion and skeleton dissolution. The tablet had good appearance and compressibility, as well as favorable floating capacity and drug release characteristics.