星点设计-效应面法优化复方左氧氟沙星原位凝胶的制备工艺

Optimization of Preparation Process of Compound Levofloxacin in Situ Thermo Sensitive Gel by Central Composite Design-Response Surface Methodology

目的优化复方左氧氟沙星温敏型原位凝胶的制备工艺。方法以胶凝温度为指标,考察凝胶基质泊洛沙姆407(PluronicF127)与温度调节剂泊洛沙姆188(PluronicF68)的用量及加入药物对胶凝温度的影响,并采用星点设计-效应面法优化复方左氧氟沙星温敏型原位凝胶的处方。结果在一定浓度范围内,胶凝温度随着PluronicF127用量的增大而逐渐降低,随着PluronicF68用量的增大而升高;最佳处方为:PluronicF127用量192.7 g、PluronicF68用量93.1 g,加水至1 000 mL。结论优化的处方稳定可行,制备的复方左氧氟沙星原位凝胶在常温下为可流动的粘稠液体,在体温下为不流动的凝胶,具温敏性质,符合质量要求。

Objective To optimize the preparation process of compound levofloxacin in situ thermo sensitive gel. Methods Gelation temperature served as the indicator. Dosage of gel base PluronicF127 and temperature regulator PluronicF68, and the influence of drug on the gelation temperature were investigated. By using the star design-response surface method,the prescription of compound levofloxacin temperature sensitive in situ gel type was optimized. Results In a certainconcentration range, the gelation temperature reduced gradually with the increased dose of PluronicF127 and decreased dose ofPluronicF68. The optimal prescription was as follows： PluronicF127 192. 7 g, PluronicF68 93. 1 g, water added to1 000 mL. Conclusion The optimized prescription process is stable and feasible. The prepared compound in situ thermosensitive gel with levofloxacin is viscous liquid at room temperature, but immobile at body temperature. The prepared gel meetsthe quality requirements. KEY WORDS Levofloxacin,