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    于洋, 华成云, 许颖, 等. 一种温敏型凝胶子宫灌注液的制备及药物浓度的监测[J]. 华南农业大学学报, 2021, 42(2): 9-16. doi: 10.7671/j.issn.1001-411X.202005003
    引用本文: 于洋, 华成云, 许颖, 等. 一种温敏型凝胶子宫灌注液的制备及药物浓度的监测[J]. 华南农业大学学报, 2021, 42(2): 9-16. doi: 10.7671/j.issn.1001-411X.202005003
    shu
    YU Yang, HUA Chengyun, XU Ying, et al. Preparation of a thermo-sensitive gel uterine perfusate and drug concentration monitoring[J]. Journal of South China Agricultural University, 2021, 42(2): 9-16. doi: 10.7671/j.issn.1001-411X.202005003
    Citation: YU Yang, HUA Chengyun, XU Ying, et al. Preparation of a thermo-sensitive gel uterine perfusate and drug concentration monitoring[J]. Journal of South China Agricultural University, 2021, 42(2): 9-16. doi: 10.7671/j.issn.1001-411X.202005003
    shu

    一种温敏型凝胶子宫灌注液的制备及药物浓度的监测

    Preparation of a thermo-sensitive gel uterine perfusate and drug concentration monitoring

      摘要
    • 摘要:
      目的  研制一种多西环素温敏型原位凝胶子宫灌注液，并对其进行质量评价及子宫内药物浓度的监测。
      方法  以泊洛沙姆407(P407)和泊洛沙姆188(P188)为主要温敏材料，采用“冷法”工艺制备原位凝胶。采用单因素分析和正交试验对处方进行筛选与优化，通过无膜溶出模型考察制剂体外溶蚀和释药情况，并在高温、高湿、强光等条件下对研制的温敏凝胶稳定性进行考察。选用5头二元杂交母猪对制剂进行子宫内药物浓度的监测。
      结果  最终优化处方为50 g制剂含多西环素1 g、P407 10 g、P188 2.5 g、氯化镁2.3 g和亚硫酸氢钠0.1 g，用乙醇胺调pH至4.0±0.2，余量为超纯水。制剂体外溶蚀及释药时间长达48 h，累积溶蚀率和释药率均达100%。制剂稳定性符合兽用化学药物稳定性研究技术指导原则的要求，在第2次给药96 h后母猪子宫内药物浓度仍能保持在68.54 μg/mL。
      结论  多西环素温敏型原位凝胶子宫灌注液制备方法简单，性质稳定，猪子宫灌注给药后局部药物浓度长时间维持在较高水平，具有缓释效果，有望为临床治疗母猪子宫内膜炎开创新途径。

       

      Abstract:
      Objective  To prepare a doxycycline thermo-sensitive in situ gel uterine perfusate, evaluate its quality, and monitor drug concentration in sow uterus.
      Method  Poloxamer 407 (P407) and poloxamer 188 (P188) were used as the main thermo-sensitive materials. The in situ gel was prepared by “cold” process. The prescription was screened and optimized by single factor analysis and orthogonal experiment. The in vitro dissolution and drug release of the preparation were measured by membrane free dissolution model. The stability of the developed thermo-sensitive gel was investigated under the conditions of high temperature, high humidity and strong light. Five binary hybrid sows were selected to monitor drug concentration in sow uterus.
      Result  The final optimized prescription was doxycycline 1 g, P407 10 g, P188 2.5 g, magnesium chloride 2.3 g and sodium bisulfite 0.1 g in per 50 g preparation, pH was adjusted to 4.0±0.2 with ethanolamine, and the residue was ultrapure water. The in vitro dissolution and drug release time of the preparation lasted for 48 h, the cumulative dissolution rate and drug release rate were up to 100%. The preparation stability was complied with technical guidelines for the stability of veterinary chemical drugs. The drug concentration remained at 68.54 μg/mL after 96 h of the second administration.
      Conclusion  The doxycycline thermo-sensitive in situ gel uterine perfusate is a simple preparation method and shows good stability. The local concentration of the drug in sow uterus maintains at a high level for a long time. The preparation has a sustained release effect and is expected to be an innovative way to treat sow endometritis.

       

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