The Preparation Of Kuijieling Colonic Localization Tablet And In Vitro Evaluation

Objective: In this study,the compound drugs for the treatment of nonspecific chronic colitis was used as a model drug to prepare kuijieling colonic-specific delivery system for p H-dependent and time-dependent tablets.Methods: ①Extraction methods:the menstrua were screened and extracted by single factor method. The amount of paeoniflorin and atractylenolide I extracted was measured to determine the times to menstua extracted. The central composite design-response surface method(CCD) was used to get the optimum extraction range and the optimum extraction process. ②Preparation method:the affecting factors of the formulation of the core were determined by single factor tests. ③Coating method: based on single factor method,CCD was used to further optimize the prescription to screen the optimum prescription. ④Quality standard: the main drugs in colon-specific delivery tablets were qualitatively and quantitatively determined by TLC and HPLC to make the quality standard of preparation.⑤ Preliminary stability: the influencing factors were tested to observe the preliminary stability of Kuijie Ling colonic-specific delivery tablets.Results: ①Extraction process: 12 times the amount of medicinal materials in prescription were extracted by 75% ethanol for two times, each time 130 min. ②Formulation of the tablet core : L-HPC and PVPPwere determined as disintegrating agent,accounting for 8%,respectively. 95% ethanol as the adhesion agent, 0.25% magnesium stearate as lubricant. Coating formulation from inside to outside were isolation layer, enteric layer, delay layer in sequence, of which coating weight were 1%, 4%, 5.5%,respectively. The isolation layer of prescription was HPMC15 g, 95% ethanol 500 ml, PEG6000 10 g, talcum powder 2.5 g. The enteric layer of prescription were acrylic resin II and acrylic resin III 2: 5(90 g), 95% ethanol 1800 ml, DEP9 g,talc powder 45 g. Delay layer of prescription were ethyl cellulose(EC) 20 g, 95% ethanol 2000 ml, PVPk30 12 g, talc powder 2 g. ③ Release rate: Kuijieling colon-specific delivery tablets hardly dissolved in hydrochloric acid solution(p H=1.2)and phosphate buffer solution( p H=6.8) for 4h,,while they began to release in the phosphate buffer solution(p H=7.6) for 8.5 h, and the cumulative release rate at 8.5h was more than 80%.④The preliminary stability test showed that Kuijie Ling colon-specific delivery tablets could keep stable at high temperature, high humidity and strong light.Conclusions: The opitimum preparation process of prescription screened is simple, feasible and reasonable,and the indicators are in line with the relevant requirements. The quality standard of Kuijie Ling colon-specific delivery tablets was established by simple, accurate and sensitive methods. The preliminary stability test showed that Kuijie Ling colon-specific delivery tablets prepared has good quality stability.