因子设计-效应面法优化5-氨基水杨酸原位凝胶灌肠液处方

Formula Optimization of 5-Aminosalicylic Acid Enema In Situ Gel by Factorial Design/Response Surface Methodology

目的：优化5-氨基水杨酸原位凝胶灌肠液处方。方法：以卡波姆作为凝胶基质,以黄原胶作为增稠剂,采用冷溶法制备具有pH敏感的5-氨基水杨酸原位凝胶灌肠液。采用3-2满因子设计试验,考察卡波姆、黄原胶的用量对原位凝胶灌肠液成胶前和成胶后粘度、倒置管试验持续时间以及沉降体积比等指标的影响,通过响应面法对处方进行优化。结果：2个影响因素和4个考察指标存在着定量关系。最优处方为：卡波姆和黄原胶在处方中的含量分别为0.7%和0.15%。按最优处方制备的5-氨基水杨酸原位凝胶灌肠液成胶前黏度为500-1 000 m Pa·s,成胶后黏度为2 200-2 700 m Pa·s,倒置管试验时间为40-80 min,沉降体积比大于98.5%。结论：通过因子设计-效应面法完成了5-氨基水杨酸原位凝胶灌肠液的多目标同步优化。

Objective： To optimize the formula of 5-aminosalicylic acid enema in situ gel. Methods： 5-Aminosalicylic acid enemas in situ gel was prepared using a cold dissolution method with earbomer as the gel matrix and xanthan gum as the thickener. A 32 full factorial design was used to investigate the effects of the concentrations of carbomer and xanthan gum on the viscosity before and after the gelling, duration of inversion tube and sedimentation rate. Response surface methodology was used to optimize the formula. Results ： The quantitative relationships between the two factors and the four evaluation indices were obtained. The optimum formula was as follows： the concentration of carhopol and xanthan gum in the enema was 0.7% and 0.15%, respectively. The viscosity before and after the gelling was 500-1 000 mPa ·s and 2 200-2 700 mPa· s, respectively. The duration of inversion tube test was 40-80 min and the sedimentation rate was more than 98.5 %. Conclusion： The multi-objective simultaneous optimization of the formula of 5-aminosal- icylic acid enema in situ gel is accomplished by factorial design and response surface methodology.